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Drug, Bio-affecting And Body Treating Compositions > Designated Organic Active Ingredient Containing (doai) > Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai > Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbon Atoms > Piperidines > Additional Ring Containing Additional Ring ContainingAdditional Ring Containing patent applications listed are from June 2005 to current and include Date, Patent Application Number, Patent Title, Patent Abstract summary and are linked to the corresponding patent application page.01/25/07 - 20070021462 - Processes for preparing anhydrous and hydrate forms of antihistaminic piperidine derivatives, polymorphs and pseudomorphs thereof which are useful as antihistamines, antiallergic agents and bronchodilators. ... 01/25/07 - 20070021461 - Processes for preparing anhydrous and hydrate forms of antihistaminic piperidine derivatives, polymorphs and pseudomorphs thereof which are useful as antihistamines, antiallergic agents and bronchodilators. ... 01/25/07 - 20070021460 - Novel piperidine derivative The present invention provides a piperidine derivative represented by the following formula or analogs thereto, which are used for agents for treating or preventing various diseases related to 5-HT7. ... 01/18/07 - 20070015791 - Serotonin and norepinephrine reuptake inhibitors and uses thereof Selective dual serotonin and norepinephrine reuptake inhibitors are provided. These compounds have a lower side-effect profile and are useful in compositions and products for use in treatment of a variety of conditions including depression, fibromyalgia, anxiety, panic disorder, agorophobia, post traumatic stress disorder, premenstrual dysphoric disorder, attention deficit disorder, obsessive ... 01/04/07 - 20070004776 - Novel hydroxamic acid-containing amino acid derivatives Novel hydroxamic acid containing amino acid derivatives are provided that are useful for treatment of inflammation, inflammatory and immunological diseases; lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyceride levels; and for treatment or prophylaxis of metabolic disorders. ... 12/28/06 - 20060293360 - 4-(2-phenyloxyphenyl)-piperidine or-1,2,3,6-tetrahydropyridine derivatives as serotonin reuptake inhibitors The invention provides compounds represented by the general formula (I) wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder. ... 12/21/06 - 20060287362 - Organic compounds in salt or zwitterionic form wherein, wherein R1, R2, R3, R4, R5, J, L and M have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds ... 12/21/06 - 20060287361 - Diarylmethylidene piperidine derivatives, preparations thereof and uses thereof as opoid receptors ligands Compounds of general formula: (I) wherein R1, R2, R3 and A are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the treatment of pain and anxiety. ... 12/07/06 - 20060276508 - Amide derivatives as somatostatin receptor 5 antagonists wherein R1 to R5, R5′ and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated ... 12/07/06 - 20060276507 - Hydroxamate sulfonamides as cd23 shedding inhibitors A class of piperidine and related heterocyclic derivatives, C-substituted by a substituted aryl or heteroaryl moiety, and N-substituted by an ethylsulfonyl group which in turn is substituted at the 2-position by a hydroxamic acid moiety and also by a range of alternative substituents, being potent inhibitors of CD23 shedding, are ... 11/30/06 - 20060270706 - Cyclic amine derivative having heteroaryl ring wherein R1 represents C1-C6 alkyl, etc., R2 represents hydrogen, C2-C7 alkanoyl, C7-C11 arylcarbonyl, the formula R4—(CH2)1—, etc., R3 represents C6-C10 aryl, etc., X1, X2, X3, X4 and X5 each independently represents hydrogen, halogen, etc., and n represents an integer of 0 to 2, pharmacologically acceptable salts thereof or prodrugs thereof. ... 11/23/06 - 20060264468 - Use of substituted-1, 5-dideoxy-1, 5-imino-d-glucitol compounds for treating hepatitis virus infections N-Substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds of Formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections, the compounds of Formula I may be used alone, or in combination with another antiviral agents selected from among nucleosides, nucleotides, immunomodulators, immunostimulants or various combinations of such ... 11/23/06 - 20060264467 - Method for the treatment of pompe disease using 1-deoxynojirimycin and derivatives The present invention provides a method for increasing the activity of a mutant or wild-type α-glucosidase enzyme in vitro and in vivo by contacting the enzyme with a specific pharmacological chaperone which is a derivative of 1-deoxynojirimycin. The invention also provides a method for the treatment of Pompe disease by ... 11/23/06 - 20060264466 - Selective serotonin 2a/2c receptor inverse agonists as therapeutics for neurodegenerative diseases Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP ... 11/23/06 - 20060264465 - Selective serotonin 2a/2c receptor inverse agonists as therapeutics for neurodegenerative diseases Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP ... 11/23/06 - 20060264464 - Amidino compounds as cysteine protease inhibitors The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. ... 11/16/06 - 20060258704 - 2-oxo-piperidinyl- and 2-oxo-azepanyl alkanoic acid derivatives for the treatment of epilepsy and other neurological disorders This invention relates to new 2-oxo-piperidinyl- and 2-oxo-azepanyl alkanoic acid derivatives of formula (1) having anticonvulsant activity which are useful as therapeutic agents for the treatment or prevention of epilepsy and other neurological disorders. The invention also concerns processes for preparing these derivatives and novel intermediates used in the preparation ... 11/16/06 - 20060258703 - Remedy for pruritus comprising piperidine derivative as the active ingredient It is intended to find out a novel pharmacological effect of a piperidine derivative (I). Because of having an excellent antipruritic effect, the piperidine derivative (1) is useful as a therapeutic agent for itching of any types such as eye itching, skin itching and systemic itching. ... 11/09/06 - 20060252796 - Androgen modulators The present invention is directed to a new class of benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth. ... 10/19/06 - 20060235049 - Non-imidazole aryloxyalkylamines Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ... 10/19/06 - 20060235048 - Treatment of connective tissue diseases of the skin The present invention provides effective and safe medicaments for the treatment of connective tissue diseases of the skin, particularly with respect to the treatment of cutaneous forms of Lupus Erythematous. The medicaments comprise as the therapeutically active ingredient a beta2 adrenoceptor agonist. The invention furthermore relates to dermatological compositions without ... 10/19/06 - 20060235047 - Antibacterial compounds and uses thereof The invention relates to antibacterial compounds and their use to treat bacterial infections. More particularly, the invention relates to substituted biphenyl compounds having antibacterial activity. The invention provides methods for treating bacterial infections using PBDEs that have not previously been used to treat bacterial infections. The invention further provides novel ... 10/12/06 - 20060229336 - Ccr5 antagonists as therapeutic agents The present invention relates to compounds of formula (I) or a pharmaceutically acceptable derivatives thereof, useful in the treatment of prophylazis of CCR5-related diseases and disorders, for example, in the inhibition of HIV replication, the prevention or treatment of HIV infection, and in the treatment of the resulting acquired immune ... 10/05/06 - 20060223860 - Biphenyl derivatives wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl ... 10/05/06 - 20060223859 - Biphenyl derivatives wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl ... 10/05/06 - 20060223858 - Biphenyl derivatives wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl ... 10/05/06 - 20060223857 - Combination of a serotonin reuptake inhibitor and a glycine transporter type 1 inhibitor for the treatment of depression The present invention relates to the use of a compound, which is a serotonin reuptake inhibitor, and a compound, which is a GlyT-1 inhibitor for the preparation of a pharmaceutical composition for the treatment of depression, anxiety disorders and other affective disorders. In particular the present invention relates to treatment ... 09/28/06 - 20060217419 - Piperidinyl substituted cyclohexane-1,4-diamines and pharmaceutically acceptable forms thereof, as α1a/α1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as method ... 09/28/06 - 20060217418 - Substituted alkyl amido piperidines This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective ... 09/21/06 - 20060211733 - Methods of preventing and treating opioid bowel dysfunction Methods of preventing and treating opioid bowel dysfunction are disclosed. In addition, methods of increasing the frequency of spontaneous complete bowel movements, methods for improving the quality of life of a patient suffering from opioid bowel dysfunction, methods for reducing a patient's dependence on laxatives, and methods for preventing or ... 09/21/06 - 20060211732 - Hydroxamic acid derivatives as antibacterials A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof: ... 09/14/06 - 20060205782 - Method of providing an antihistaminic effect in a hepatically impaired patient R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A and B is hydrogen or hydroxy with the proviso that at least one of A or B is hydrogen; or a pharmaceutically acceptable salt and individual ... 09/14/06 - 20060205781 - Synthesis of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates. ... 09/14/06 - 20060205780 - Synthesis of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates. ... 09/14/06 - 20060205779 - Biphenyl compounds useful as muscarinic receptor antagonists wherein a, b, c, p, W, A, X1, R1, R2, R3, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using ... 09/14/06 - 20060205778 - Biphenyl compounds useful as muscarinic receptor antagonists wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods ... 09/14/06 - 20060205777 - Biphenyl compounds useful as muscarinic receptor antagonists wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods ... 09/14/06 - 20060205776 - Methylphenidate solution and associated methods of administration and produciton A methylphenidate solution and associated methods of administration and production, which includes methylphenidate and at least one organic acid dissolved in a solvent system, where the solvent system includes at least one non-aqueous solvent. The solvent system may include water. The non-aqueous solvent can include, but is not limited to ... 09/07/06 - 20060199842 - Selective serotonin 2a/2c receptor inverse agonists as therapeutics for neurodegenerative diseases Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP ... 09/07/06 - 20060199841 - Pharmaceutical combination for the treatment of spasticity and/or pain The present invention relates to a pharmaceutical combination for the treatment of spasticity and/or pain characterized by that the combination contains as active ingredient 70-95% w/w compound of formula (I), wherein R represents a methyl or ethyl group, and 5-30% w/w dextromethorphan (chemical name: (+/−)-3-methoxi-17-methylmorphinan). ... 08/31/06 - 20060194841 - Benzylamine derivative The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor. The compound is a benzylamine derivative represented by formula (1) or a salt thereof. ... 08/24/06 - 20060189657 - Novel compounds and compositions as cathepsin inhibitors Novel inhibitors of cathepsin S, K, B, and L, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making. ... 08/24/06 - 20060189656 - Piperidine derivatives and agent comprising the derivative as active ingredient Since the compound represented by formula (I) has a PDE4 inhibitory activity, it is useful for preventing and/or treating inflammatory diseases, diabetic diseases, allergic diseases, autoimmune diseases, osteoporosis, bone fracture, obesity, depression, Parkinson's disease, dementia, ischemia-reperfusion injury, leukemia and the like. ... 08/24/06 - 20060189655 - Methylphenidate derivatives and uses of them and salts and prodrugs thereof, wherein n, R1 and R2 are defined herein. The invention also provides certain novel compounds of formula I and pharmaceutical compositions comprising them. ... 08/17/06 - 20060183774 - Methods for treatment of cognitive and menopausal disorders with d-threo methylphenidate In one aspect, the present invention is directed to methods for treating fatigue, neurobehavioral slowing and other cognitive disorders and defects due to cancers and treatments associated with cancers, and similar conditions. In a further aspect, the present invention is directed to methods for treating disorders related to menopause, including ... 08/17/06 - 20060183773 - Uses of methylphenidate derivatives and salts and prodrugs thereof, wherein n, R1 and R2 are defined herein. ... 08/17/06 - 20060183772 - Anti-cancer compounds The invention provides bradykinin antagonists and pharmaceutically acceptable salts thereof having anti-cancer activity. These anti-cancer compounds are particularly useful for inhibiting the growth of lung and prostate cancers. ... 08/10/06 - 20060178401 - Aminophenoxyacetamide derivatives and pharmaceutical composition containing thereof wherein R1 to R4 are, independent from each other, a hydrogen atom or an optionally substituted alkyl group; E1 is —NR4—; and E2 is an oxygen atom or —NR10—; Q is the group —X—Y-Q′, wherein X and Y are connecting bonds or X is an alkylene or alkenylene group and ... 08/10/06 - 20060178400 - Novel acetyl-coa carboxylase (acc) inhibitors and their use in diabetes, obesity and metabolic syndrome which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans. ... 08/10/06 - 20060178399 - Nitrogen-containing heterocyclic derivatives and drugs containing the same as the active ingredient (wherein each symbol is as defined in the description.) The compounds represented by the general formula (I) are useful in preventing and/or treating various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation, immunosuppression, psoriasis, multiple sclerosis, ... 08/03/06 - 20060173044 - Substituted propargylamines c) R2 and R3 together with the nitrogen atom to which they are attached form N-heteroaryl or N-heterocyclyl, unsubstituted or mono- or polysubstituted by identical or different radicals, if appropriate also as N-oxide or salt, as pesticide against arthropods and helminths for protecting plants and animals. ... 08/03/06 - 20060173043 - Use of novel 2-oxo-heterocyclic compounds and the pharmaceutical compositions comprising the same The present invention is related to novel use of 2-oxo-heterocyclic compounds having anticancer activity and the process for preparing them and a pharmaceutical composition comprising the same. The present invention provides a pharmaceutical composition for preventing and treating the cancer disease comprising lung cancer, bone cancer, pancreatic cancer, skin cancer, ... 08/03/06 - 20060173042 - Process for the preparation of fexofenadine The present invention relates to a process for the preparation of cyclopropyl keto a,a-dimethylphenyl acetic acid of structural Formula I, and to the use of this compound as an intermediate for the preparation of an antihistamine, fexofenadine. ... 08/03/06 - 20060173041 - Sulphonylpiperidine derivatives containing an aryl or heteroaryl group for use as matrix metalloproteinase inhibitors A compound of formula (1), wherein B is an ortho substituted monocyclic aryl or heteroaryl group or a bicyclic aryl or heteroaryl group; useful in the inhibition of one or more metalloproteinases, and in particular TACE. ... 07/27/06 - 20060167050 - Combined use of methylphenidate and melatonin for treating attention-deficit hyperactive disorder The present invention relates to the combined use of methyl phenidate and at least one of melatonin, a melatonin analogue, or a pharmaceutically acceptable salt thereof in the treatment of attention deficit hyperactive disorder (ADHD). Methylphenidate and melatonin or its analogue may be used together or in combination with one ... 07/27/06 - 20060167049 - Terphenly derivatives, preparation thereof, compositions containing same These compounds exhibit an antagonist activity with respect to CB1 cannabinoid receptors. ... 07/06/06 - 20060148852 - Visual function disorder improving agents The present invention provides a visual function disorder improving agent containing a compound having Rho kinase inhibitory activity, particularly (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide, as an effective component. This agent has axon of the retinal ganglion cellal extension promoting action and optic nerve cell regeneration promoting action, and is useful for the treatment of ... 07/06/06 - 20060148851 - Fexofenadine crystal form and processes for its preparation thereof Provided is a crystalline form of fexofenadine free base and processes for its preparation. ... 07/06/06 - 20060148850 - 4-{'3-(sulfonylamino) phenyl!'1-(cyclymethyl) piperidin-4-ylidene! methyl}benazmide derivativess as delta opioid receptor ligands for the treatment of pain, anxiety and functional gastrointestinal disorder Compounds of general formula: (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain. ... 06/29/06 - 20060142337 - Piperidine derivative and use thereof wherein Ar is an aryl group optionally having substituents, R is a C1-6 alkyl group, R1 is a hydrogen atom, a hydrocarbon group optionally having substituents, an acyl group or a heterocyclic group optionally having substituents, X is an oxygen atom or an imino group optionally having substituents, ring A ... 06/29/06 - 20060142336 - N-sulfonylpiperidines as metalloproteinase inhibitors (tace) Compounds of formula (1), wherein Z is —CONR15OH or —N(OH)CHO and X is —(CR9R10)t-Q-(CR11R12)u- (where t and u are independently 0 or 1 with the proviso that t and u cannot both be 0);are inhibitors of metalloproteinases and in particular TACE. ... 06/22/06 - 20060135561 - 4-aminopiperidine derivatives wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, non-insulin dependent diabetes mellitus and/or impaired glucose tolerance, obesity, and/or metabolic syndrome or β-cell ... 06/22/06 - 20060135560 - Prevention and treatment of cardiovascular pathologies with tamoxifen analogues wherein Z is C═O or a covalent bond; Y is H or O(C1-C4)alkyl, R1 and R2 are individually (C1-C4)alkyl or together with N are a saturated heterocyclic group, R3 is ethyl or chloroethyl, R4 is H, R5 is I, O(C1-C4)alkyl or H and R6 is I, O(C1-C4)alkyl or H with ... 06/15/06 - 20060128753 - 4-aminopiperidine derivatives, processes for their preparation and their use as medicaments The present invention relates to 4-aminopiperidine derivatives, to processes for their preparation, to their use in therapy and to pharmaceutical compositions containing them. More particularly these compounds are useful for treatment of disorders of the central and/or peripheral nervous system. Of particular interest, is the potent antidepressant activity shown by ... 06/15/06 - 20060128752 - Chemical compounds provided that when m is 0, p is 2, q , r and n represent 1, R1, R2,R3, R4, R5 and R7 are hydrogen and R is chlorine, R5 is not iodine; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of ... 06/01/06 - 20060116398 - Compounds having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, W, a and b are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are ... 05/25/06 - 20060111399 - Salts of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation Disclosed herein are salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide including the citrate, fumarate, maleate, malate, phosphate, succinate, sulphate, and edisylate salts. ... 05/18/06 - 20060106066 - Benzyl substituted (piperidin-4-yl)aminobenzamido derivatives The present invention is directed to N-benzyl substituted (piperidin-4-yl)aminobenzamido derivatives which are delta-opioid receptor modulators. ... 05/18/06 - 20060106065 - Methods of treating hepatitis virus infections with n-substituted-1,5-dideoxy-1,5-imino-d- glucuitol compounds in combination therapy Provided are methods and compositions for treating hepatitis virus infections in mammals, especially humans. The methods comprise (1) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, mixtures thereof, or immunomodulating/immunostimulating agents, or (2) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, or ... 05/18/06 - 20060106064 - Butyrophenones and sigma-1 receptor antagonists protect against oxidative-stress The present invention includes compositions and methods for the protection of one or more central nervous system cells from trauma, when administered before, during or after the trauma, wherein the composition includes an effective amount of a butyrophenone, e.g., a 1-linked phenyl butyrophenone that is electronegative along the butyl chain ... 05/18/06 - 20060106063 - Synthesis of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates. ... 05/11/06 - 20060100243 - Methylphenidate analogs and methods of use thereof Provided are analogs of methylphenidate (“MPH”) that are useful for the treatment of drug addiction, attention deficit disorder, attention deficit hyperactivity disorder, and depression. The MPH analogs are extended duration compounds that bind to the dopamine transporter and the reuptake of dopamine in the afflicted individual's brain. Because of the ... 05/11/06 - 20060100242 - 4-(2-phenylsulfanyl-phenyl)-piperidine derivates as serotonin reuptake inhibitors The invention provides compounds represented by the general formula (I) wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder. ... 05/04/06 - 20060094759 - Novel piperdine derivatives and their use as monoamine neurotransmitter re-uptake inhibitors This invention relates to novel piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. ... 04/27/06 - 20060089383 - Substituted piperidine compounds and methods of their use Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors. ... 04/13/06 - 20060079557 - Sulfamoyl benzamide derivatives and methods of their use Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or modulating ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ... 04/13/06 - 20060079556 - N-sulfonylpiperidine cannabinoid receptor 1 antagonists The present application describes compounds according to Formula I, wherein R1, R2, R3, R4, X and Y are described herein. Additionally, the present application describes pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents. Finally, the present application describes methods ... 04/13/06 - 20060079555 - Diarylmethylidene piperidine derivatives, preparations thereof and uses thereof Compounds of general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, m and n are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain. ... 04/13/06 - 20060079554 - Inhibitors of monomine uptake N,N-disubstituted 4-amino-piperidines of the general Formula (I) are inhibitors of the uptake of serotonin and/or norepinephrine and/or dopamine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system. ... 03/30/06 - 20060069124 - Use of mdl-100,907 for treatment of allergic and eosinophil mediated diseases Methods of modulating eosinophil migration, chemotaxis or generation, in vitro, ex vivo, and in vivo are provided. Methods include contacting eosinophils with an amount of 5-HT2A receptor agonist or antagonist sufficient to modulate eosinophil migration, chemotaxis or generation. ... 03/23/06 - 20060063808 - Process for production of piperidine derivatives with isobutyrate or an isobutyrate equivalent. ... 03/16/06 - 20060058351 - Novel ligands that modulate lxr-type receptors and cosmetic/pharmaceutical applications thereof and are formulated into pharmaceutical compositions useful in human or veterinary medicine, or alternatively into cosmetic compositions. ... 03/16/06 - 20060058350 - Alkynyl-substituted azasugar derivative and drug containing the same as the active ingredient An alkynyl-substituted azasugar derivative and a drug containing the same as an active ingredient are disclosed. This drug is useful as a preventive or remedy for insulin-independent diabetes, rheumatoid arthritis, osteoarthritis, sepsis, acquired immune deficiency syndrome (AIDS), graft-versus-host disease (GVHD), asthma, atopic dermatitis, and ulcerative colitis. ... 03/16/06 - 20060058349 - Piperidinetriol derivatives as inhibitors of glycosyceramid synthase Compounds of formula (I): wherein R represents various substituent groups, are useful as inhibitors of glucosylceramide synthase. ... 03/16/06 - 20060058348 - N-benzyl-3-phenyl-3-heterocyclyl-propionamide compounds as tachykinin and/or serotonin reuptake inhibitors c) when the heteroatom contained in the group R1 is substituted, p is not zero; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tachykinins and/or by selective inhibition of serotonin reuptake transporter protein. ... 02/23/06 - 20060040985 - Therapeutic agent for treating respiratory diseases containing 4-hydroxypiperidine derivative as active ingredient wherein A is a group represented by L-W [wherein L is a bond or CH2; and W is O, SOn (wherein n is 0 to 2), or —NR7— (wherein R7 is hydrogen or lower alkyl)]; each of G1 and G2 is (CH2)r (wherein r is 0 to 2), provided that ... 02/09/06 - 20060030587 - Method of treating attention deficit disorders with d-threo methylphenidate Methods for treating Attention Deficit Disorder, Attention Deficit Hyperactivity Disorder, AIDS Dementia Complex and cognitive decline in HIV-AIDS while minimizing drug hypersensitivity, toxicity, side effects, euphoric effect, and drug abuse potential by administration of d-threo-methylphenidate or pharmaceutically acceptable salts thereof. ... 02/02/06 - 20060025445 - 11-beta hsd1 inhibitors This invention relates to inhibiting 11-beta HSD1. ... 02/02/06 - 20060025444 - Fexofenadine base polymorphic forms The invention relates to novel crystalline forms of fexofenadine base, a process for the preparation thereof and the use thereof in therapy. ... 02/02/06 - 20060025443 - Piperidin-2,6-dione pamoate salts and their use for the treatment of stress-related affective disorders Novel pamoate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4-dimethylpiperidin-2,6-diones and pharmacologically acceptable solvates thereof are devoid of the weight loss and hepatocyte changes in the rat which limited to marginally effective levels the permitted clinical doses of the corresponding hydrochlorides in the treatment or prophylaxis of stress-related affective disorders such as anxiety, depression, ... 01/26/06 - 20060019993 - 1-amido-3-(2-hydroxyphenoxy)-2-propanol derivatives and a process for preparing 2-amidomethyl-1,4-benzodioxane derivatives wherein cycle A may have further 1 to 4 substituents, and said substituent means a substituent selected from the group consisting of saturated or unsaturated C1-4 alkyl group, aralkyl group in which alkyl moiety has 1 to 4 carbon atoms, aryl group, halogen atom, halogenated C1-4 alkyl group, C2-5 alkanoyl ... 01/26/06 - 20060019992 - Cycloalkylamine derivatives as nk-1/ssri antagonists useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors. ... 01/19/06 - 20060014793 - Process and diastereomeric salts useful for the optical resolution of racemic alpha-(4-(1, 1-dimethylethyl) phenyl] -4- (hydroxydiphenylmethyl) -1-piperidinebutanol and derivative compounds A process and diastereomeric salts useful for the optical resolution of racemic α-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1 -piperidinebutanol, 4-[4-[4-(hydroxydiphenylmethyl)-1 -piperidinyl]-1-hydroxybutyl]-α,α-dimethylbenzeneacetic acid and lower alkyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylbenzeneacetates. The process comprises placing into solution a chiral resolving agent, either (+)/(−)-di-paratoluoyltartaric acid or (−)/(+)-mandelic acid, in an amount equimolar to a compound corresponding to the desired enantiomer of ... 01/19/06 - 20060014792 - Heterocyclo inhibitors of potassium channel function Novel heterocyclo compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and ... 01/19/06 - 20060014791 - Process for manufacturing of chiral lobelin The present invention relates to a shortened process for preparing L-lobeline by rhodium-catalysed asymmetric hydrogenation on an industrial scale. ... 01/19/06 - 20060014790 - Methods of treatment of amyloidosis using spirocyclohexane aspartyl-protease inhibitors The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein. ... 01/19/06 - 20060014789 - Phenyl-piperidin-4-ylidene-methyl-benzamide derivatives for the treatment of pain or gastrointestinal disorders Compounds of general formula: wherein R1, R2 and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain. ... 01/12/06 - 20060009491 - Amido compounds and their use as pharmaceuticals The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or ... 01/05/06 - 20060004050 - Compositions and methods for the prevention or treatment of pain and other nervous system disorders A tolperisone-related compound or a compound of Formula Z is administered for the prevention and treatment of periodic paralyses and myotonias of several types, long QT syndrome, Brugada syndrome, malignant hyperthermia, myasthenia, epilepsy, ataxia, migraine, Alzheimer's Disease, Parkinson's Disease, schizophrenia, and hyperekplexia, neuropathic pain, and pain associated with nervous system ... 01/05/06 - 20060004049 - N-substituted piperidines and their use as pharrmaceuticals The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or ... 01/05/06 - 20060004048 - Novel biaromatic compounds which activate ppargamma type receptors and cosmetic/pharmaceutical compositions comprised thereof are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions. ... 12/29/05 - 20050288329 - 2-methylprop anamides and their use as pharmaceuticals The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or ... 12/29/05 - 20050288328 - Selective serotonin receptor inverse agonists as therapeutics for disease Disclosed herein are pharmaceutical compositions comprising an inverse serotonin receptor agonist or a serotonin receptor antagonist and an anti-insomnia agent. Disclosed herein are also methods of treating insomnia using the disclosed pharmaceutical compositions. ... 12/22/05 - 20050282861 - Cannabinoid receptor ligands or a pharmaceutically acceptable salt of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds. ... 12/22/05 - 20050282860 - Fexofenadine polymorphs and process for the preparation thereof The invention provides novel crystalline forms of fexofenadine hydrochloride, a process for the preparation of the novel forms and of the known form A, and their use in therapy. ... 12/22/05 - 20050282859 - Dual acting snri-nmda antagonists for the treatment of genitourinary disorders Discolsed herein are compositions and methods for treatment of genitourinary disorders (e.g., urge incontinence). The compositions may generally include a dual-acting SNRI-NMDA antagonist (e.g., bicifadine and/or milnacipran). Alternatively, the compositions may generally include an SNRI and an NMDA antagonist. ... 12/22/05 - 20050282858 - Amido compounds and their use as pharmaceuticals The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or ... 12/22/05 - 20050282857 - Selected cgrp-antagonists, process for preparing them and their use as pharmaceutical compositions wherein A, X and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these ... 12/15/05 - 20050277667 - Manufacturing process for methyl phenidate and intermediates thereof The present invention discloses selective and complete reduction of pyridine ring in a biaryl system comprising ∝-substituted or nonsubstituted benzene ring and relates more specifically, not exclusively, for the manufacture of methylphenidate, which is used for treatment of Attention Deficit Hyperactive Disorder (ADHD) and also acts as central nervous system ... 12/15/05 - 20050277666 - Process of preparing n-ureidoalkyl-piperidines reacting the compound of formula (III) with an amine of formula (IIa) using reductive amination to give the compound of formula (III) ... 12/08/05 - 20050272774 - Substituted cyclohexane derivatives wherein A1, A2, A3, A4, A5, A6, A7, A8 , A9, A10, U, V, W, m, n and p-are as indicated in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia and ... 12/08/05 - 20050272773 - Use of r (+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-flurophenyl)-ethyl]-4- piperidinemethanol for the treatment of sleep disorders and process for making pharmaceutical composition A process for making a pharmaceutical composition for treating a variety of sleep disorders comprising an effective amount of R-(+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol or a pharmaceutically acceptable salt thereof is disclosed and claimed. ... 12/08/05 - 20050272772 - Pharmaceutical compositions for the treatment of pruritus Composition comprising: a carrier; a first active ingredient comprising capsaicin, a capsaicin analog, another vanilloid receptor agonist or mixtures thereof; and at least one second active ingredient that functions as a topical anesthetic to cause localized numbness to induced skin irritation. Technique for treating the symptoms of pruritus comprising the ... 12/08/05 - 20050272771 - Process for production of piperidine derivatives R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents. ... 12/08/05 - 20050272770 - Compositions and treatments for inhibiting kinase and/or hmg-coa reductase The present invention provides compositions of matter, kits and methods for their use in the treatment of MAP kinase-related conditions and/or HMG-CoA reductase-related conditions. In particular, the invention provides compositions for treating inflammatory and/or cardiovascular conditions in an animal subject by inhibiting p38α MAP kinase and/or HMG-CoA reductase, as well ... 11/24/05 - 20050261343 - Anthranilamides and their use as pharmaceutical agents Substituted anthranilamides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of anthranilamides are described. ... 11/24/05 - 20050261342 - Metabolites of (+)-(2s,3s)-3(2-methoxy-5- trifluoromethoxybenzylamino)-2-phenyl-piperidine Metabolites of (+)-(2S, 3S)-3-(2-methoxy-5-trifluoromethoxybenzylamino)-2-phenyl-piperidine, and use of same. ... 11/24/05 - 20050261341 - Novel processes for the preparation of (r)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol The present invention provides various processes for the preparation of (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol. These processes may be characterized by the following scheme: ... 11/24/05 - 20050261340 - Selective serotonin receptor inverse agonists as therapeutics for disease Disclosed herein are pharmaceutical compositions comprising an inverse serotonin receptor agonist or a serotonin receptor antagonist and an anti-psychotic agent. Disclosed herein are also methods of treating psychotic disorders using the disclosed pharmaceutical compositions. ... 11/17/05 - 20050256164 - Nk1 and nk3 antagonists The invention is to a compound exhibiting neurokinin inhibitory properties, a pharmaceutical composition comprising same and a method of treatment for neurokinin-mediated conditions. ... 11/17/05 - 20050256163 - Crystalline forms of fexofenadine hydrochloride and processes for their preparation Provided are crystalline forms of fexofenadine hydrochloride and processes for their preparation. ... 11/17/05 - 20050256162 - Fluoroalkoxybenzylamino derivatives of nitrogen containing heterocycles wherein Q, X1, X2 and X3 are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. ... 11/17/05 - 20050256161 - Melanin concentrating hormone receptor antagonists wherein W, X, Y, Z, R3-R6, and R11 are as defined in the specification, are provided. Also provided are methods of treating or preventing a melanin concentrating hormone-mediated disorder in a subject, comprising administering to a subject in need of such treatment or prevention a compound of Formula I. ... 11/17/05 - 20050256160 - Beta-alanine derivatives and the use thereof (wherein the symbols are as defined in the description), or a prodrug or a salt thereof. This compound engages in LPA receptor bonding and antagonism and hence is useful in the prevention and/or treatment of urinary system disease (symptom with prostatic hypertrophy or neurogenic bladder dysfunction disease, symptom to be ... 11/03/05 - 20050245574 - Aminophenoxyacetic acid derivatives and pharmaceutical composition containing thereof These compounds have neuroprotective effects by inducing calbindin D28Kd, one of Ca2+-binding proteins. ... 11/03/05 - 20050245573 - N-substituted benzene sulfonamides Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3′, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I). ... 11/03/05 - 20050245572 - Naphthyl ether compounds and their use Compounds having the following structure wherein R1, R2, R3, R4, R5, R6, R7 m and n are as defined in the specification, in vivo-hydrolysable precursors thereof, pharmaceutically-acceptable salts thereof, the use in therapy and pharmaceutical compositions and methods of treatment using the same. ... 10/27/05 - 20050239835 - Melanocortin receptor ligands wherein preferably R is substituted aryl and W2 is a heteroatom comprising unit. ... 10/27/05 - 20050239834 - Novel 4-diphenylmethyl piperidine derivatives This invention relates to novel substituted piperidine derivatives. More particularly, this invention relates to substituted phenyl 4-substituted-piperidinoalkanol derivatives which are useful as antihistamines, antiallergy agents and bronchodilators. ... 10/27/05 - 20050239833 - Compositions and methods for modulating interaction between polypeptides The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another. ... 10/27/05 - 20050239832 - Methods of treatment of amyloidosis using bi-cyclic aspartyl protease inhibitors The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein. ... 10/27/05 - 20050239831 - Bupivacaines The present invention describes a new method for the separation of bupivacaine enantiomers consisting in a continuous separation process performed without heating, by the selective precipitation of their diastereomeric salts with tartaric acid. This heatless process avoids the degradation of the reagents granting a continuous process feature to the procedure. ... 10/27/05 - 20050239830 - Methods of diminishing co-abuse potential Methods of diminishing or eliminating the co-abuse of a methylphenidate drug comprising identifying a patient or patient group suspected or likely to abuse said methylphenidate drug in combination with a substance known or suspected to give rise to l-ethylphenidate or psychotropic effect when ingested in the combination and making available ... 10/27/05 - 20050239829 - Novel piperidine compound The present invention provides a novel piperidine compound of the formula [I]: wherein Ring A represents an optionally substituted benzene ring, Ring B represents an optionally substituted benzene ring, R1 represents an optionally substituted alkyl group, an optionally substituted hydroxyl group, etc., or a group of the formula: (a) wherein ... 10/27/05 - 20050239828 - Spirocyclic amides as cannabinoid receptor modulators Novel compounds of structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, ... 10/20/05 - 20050234100 - Insulin resistance as new action of loperamide This application is going to claim a new action of old compound that can improve insulin resistance and this old compound named loperamide. ... 10/13/05 - 20050228018 - Chemical compounds Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a condition, disease, or disorder that can be ameliorated by the administration of an inhibitor of tryptase, e.g., asthma and inflammatory diseases, to name only a few. ... 10/13/05 - 20050228017 - Novel anticancer compounds The present invention relates to compounds of formula (I): (I) their pharmacologically acceptable salts, or solvates and hydrates, and their prodrugs, respectively, and to pharmaceutical compositions containing the same as active ingredient. These novel compounds are especially useful in the treatment of cancer. ... 10/06/05 - 20050222205 - Treatment of pain with ifendropil Ifenprodil is useful for the treatment of pain, e.g. on administration intranasally or by another route that avoids first-pass metabolism. ... 10/06/05 - 20050222204 - Opioid receptor antagonists A compound of the formula (I): or a pharmaceutically acceptable salt, enantiomer, racemate, diastereomers or mixtures thereof, or a solvate thereof, formulations and methods of use thereof are disclosed. ... 09/29/05 - 20050215590 - Formamide derivatives for the treatment of diseases and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions. ... 09/29/05 - 20050215589 - Inhibitors of 5-ht2a receptor wherein R and R′ are described herein, as are processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of a 5-HT2A receptor-related disorder. ... 09/29/05 - 20050215588 - Cyanoguanidine prodrugs Pyridyl cyanoguanidine compounds of the general formula I wherein A, X1, X2, X3, Y1, Y2, Y3, R1, R2, R5, R6 and n are as indicated in the description are suitable as prodrugs in human and veterinary therapy of proliferative diseases such as cancers. ... 09/22/05 - 20050209279 - Process for production of piperidine derivatives R5, R8, and R9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety and converting the regioisomer to the piperidine derivative compound with a piperidine compound. ... 09/22/05 - 20050209278 - Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for ... 09/15/05 - 20050203140 - Process for the preparation of paroxetine substantially free of alkoxy impurities The present invention is directed to methods for preparing intermediates useful in the synthesis of paroxetine wherein the intermediates are substantially free of alkoxy impurities as well as to methods for preparing paroxetine and pharmaceutically acceptable salts thereof substantially free of alkoxy impurities. The alkoxy impurity is reacted with an ... 09/15/05 - 20050203139 - Biphenyl compounds useful as muscarinic receptor antagonists wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and ... 09/15/05 - 20050203138 - Biphenyl compounds useful as muscarinic receptor antagonists wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and ... 09/15/05 - 20050203137 - Biphenyl compounds useful as muscarinic receptor antagonists wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of ... 09/15/05 - 20050203136 - Diastereomers of 4-aryloxy-3-hydroxypiperidines The present invention relates to essentially pure diastereomers of 4-aryloxy-3-hydroxypiperidines, including purified diastereomers of ifoxetine, methods of purifying said diastereomers, pharmaceutical compositions comprising said diastereomers and methods of treatment utilizing said pharmaceutical compositions. ... 09/15/05 - 20050203135 - Antagonists for treatment of cd/11cd18 adhesion receptor mediated disorders Compounds of the general structure D-L-B-(AA), for example (A), that are useful for treating Mac-1 or LFA-1-mediated disorders such as inflammatory disorders, allergies, and autoimmune diseases are provided. ... 09/08/05 - 20050197362 - Preventives/remedies for urinary disturbance Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood ... 09/01/05 - 20050192317 - Novel diamines having a casr modulating activity The invention concerns diamines of general formula (I), wherein: A represents a group A1 or A2 of general formula (II); B represents a group B1 or B2 of general formula (III); X represents a SO2, CH2, C═O or COO; YZ represents a group of formula CH(R25)—CH(R26) or CH(R27)═(R28), and R1 ... 08/25/05 - 20050187250 - Method of correcting herg channel dysfunction A method of shortening prolonged QT intervals in a patient with a trafficking defective HERG mutation is disclosed. In one embodiment, this method comprises the step of treating the patient with an effective amount of fexofenadine whereby the patient's prolonged QT interval is shortened. ... 08/25/05 - 20050187249 - Lypohilization product The present invention relates to an aqueous solution containing a physiologically active substance which may have a substituent and which has an amidino group, wherein the pH of the solution is higher than 2 and equal to or lower than 4. The invention also relates to a lyophilized product obtained ... 08/18/05 - 20050182096 - Haloalkyl containing compounds as cysteine protease inhibitors The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. ... 08/11/05 - 20050176766 - 2,3-oxidosqualene-lanosterol cyclase inhibitors The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes. ... 08/04/05 - 20050171159 - Synthesis of (4-bromophenyl)(4-piperidy)methanone-(z)-o-ethyloxime and salts In one embodiment, the present invention describes the synthesis of (4-bromophenyl) (4-piperidyl)methanone-(Z)-O-ethyloxime and its acid salts, and similar compounds, in high stereochemical purity. ... 08/04/05 - 20050171158 - Melanocortin receptor ligands L is a linking unit, Q is preferably a cyclic hydrocarbyl unit; W1 is preferably a carbocyclic unit and W2 is a heteroatom comprising unit. ... 08/04/05 - 20050171157 - Substituted piperidines wherein X, n, R1-R12 are defined herein, or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound represented by formula (II) and a pharmaceutically acceptable carrier or excipient. The invention further provides a method for treating cancer comprising administering ... 08/04/05 - 20050171156 - Prodrugs of potassium channel inhibitors Compounds useful as prodrugs of potassium channel inhibitor compounds, in particular as prodrugs of Kv1.5 channel inhibitors. ... 08/04/05 - 20050171155 - Method to separate stereoisomers A method to resolve the stereoisomers of an optically active compound comprising an amine moiety. The method provides a mixture comprising two stereoisomers of a compound comprising a amine moiety. The method supplies l-fenchyloxyacetic acid, treats the mixture of stereoisomers with that l-fenchyloxyacetic acid, and collects one of those two ... 08/04/05 - 20050171154 - Carboxylic acid amides D, W, X, Y, T and R1 are as defined in patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours. ... 08/04/05 - 20050171153 - Piperidylcarboxamide derivatives and their use in the treatment of tachykinin-mediated diseases wherein R, R1, R2, R3, R4, R5, R6, X, Y, m and n are as defined herein; and pharmaceutically acceptable salts and solvates thereof; the process for their preparation and their use in the treatment of conditions mediated by tachykinins. ... 07/28/05 - 20050165057 - Novel piperidine derivative or a prodrug thereof, or a pharmaceutically acceptable salt of the same, which exhibits ACAT inhibitory activity, and is useful as an agent for treatment of hyperlipidemia and atherosclerosis. ... 07/28/05 - 20050165056 - Method for producing non-hydrated fexofenadine hydrochloride and a novel crystalline form obtained thereby The invention relates to non-hydrated fexofenadine hydrochloride which can be obtained from a fexofenadine base and hydrogen chloride, according to the reaction conditions, either in the form of a novel polymorph (“form A”), in an amorphous form, or in the form of a mixture of different polymorphs. Said novel polymorph ... 07/21/05 - 20050159450 - Derivative of n-[phenyl(piperidin-2-yl)methyl]benzamide, the preparation method thereof and application of same in therapeutics Application in therapy. ... 07/21/05 - 20050159449 - Cannabinoids wherein R, R1 and R4 are defined in the specification, and pharmaceutically acceptable salts, esters and tautomers thereof, having activity at peripheral cannabinoid receptors, commonly designated the CB2 receptor class. The compounds are useful for therapy, especially in the treatment of pain, inflammation and autoimmune disease. ... 07/14/05 - 20050154019 - Substituted cyclic amine metalloprotease inhibitors Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them. ... 07/14/05 - 20050154018 - Method for treating and preventing disorders using optically pure (+) norcisapride Methods for the prevention, treatment, or management of apnea, apnea disorders, bulimia nervosa, irritable bowel syndrome, urinary incontinence, bradycardia, bradyarrhythmia, syncope, other disorders, or symptoms thereof using (+) norcisapride, or a pharmaceutically acceptable salt thereof, substantially free of its (−) stereoisomer. ... 07/14/05 - 20050154017 - Novel azasugar derivative and drug containing the same as the active ingredient A novel azasugar derivative, and a drug containing the same as an active ingredient are disclosed. The drug is useful for treatment of keratinocyte-proliferative diseases. ... 07/07/05 - 20050148630 - Methods of preventing and treating non-opioid induced gastrointestinal dysfunction Methods of preventing and treating non-opioid induced gastrointestinal dysfunction, including chronic constipation, slow colonic transit, low stool frequency, and poor stool consistency, with reduced undesirable side effects are disclosed. ... 07/07/05 - 20050148629 - Compounds useful in the treatment of anthrax and inhibiting lethal factor This invention relates to compounds of formula (I), and a method for treating anthrax or inhibiting lethal factor by administrating a composition containing a compound of formula (I) and a pharmaceutically acceptable carrier. This invention further relates to the use of the compounds of formula (I) to treat other conditions ... 06/30/05 - 20050143418 - Pesticidal heterocycles It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ═NCH(R6)CH(R7)N(R8)—, ═NC(R6)═C(R7)N(R8)—, or ═CHN═C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken ... 06/23/05 - 20050137230 - Carboxamide derivatives R1, D, E, W, X and n are as defined in claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours. ... 06/23/05 - 20050137229 - Novel compounds and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is ... 06/16/05 - 20050131021 - Phenoxy piperidines for treating diseases such as schizophrenia and depression Compounds of the formula (1), in which R1, R2′, R2″, R2′″, R3 and n are as defined in claim 1, are effectors of the nicotinic and/or muscarinic acetylcholine receprot and are suitable for the prophylaxis or treatment of schizophrenia, depression, anxiety states, dementia, Alzheimer's disease, Lewy bodies dementia, neurodegenerative diseases, ... 06/09/05 - 20050124657 - Methods of preventing and treating gastrointestinal dysfunction Methods of preventing and treating gastrointestinal dysfunction, particularly postoperative ileus and post-partum ileus, in a patient undergoing surgery or other biological stress by administering 4-aryl-piperidine derivatives are disclosed. ... 06/09/05 - 20050124656 - Substituted methylene amide derivatives as modulators of protein tyrosine phosphatases(ptps) The present invention is related to substituted methylene amide derivatives of formula (I) and use thereof for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or pyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In ... 06/02/05 - 20050119307 - Method of treating attention deficit disorders with d-threo methylphenidate Methods for treating Attention Deficit Disorder, Attention Deficit Hyperactivity Disorder, AIDS Dementia Complex and cognitive decline in HIV-AIDS while minimizing drug hypersensitivity, toxicity, side effects, euphoric effect, and drug abuse potential by administration of d-threo-methylphenidate or pharmaceutically acceptable salts thereof. ... 06/02/05 - 20050119306 - Alkaloid that inhibits biosynthesis of mycotoxins and method for screening for mycotoxin inhibitors The present invention provides an alkaloid compound that is an inhibitor of mycotoxin biosynthesis. The alkaloid is an alkenyl piperidine amide wherein the alkenyl is a C18 alkenyl with one or more double bonds. The alkaloid inhibits transcription of the fungus genes nor-1, tri5, and ipnA. The present invention further ... 06/02/05 - 20050119305 - Il-6 production inhibitors (wherein all the symbols have the same meanings as defined in the specification), an equivalent thereof, a non-toxic salt thereof or a prodrug thereof as an active ingredient. Because of having an IL-6 production inhibitory activity, the compound of formula (I) may be useful for the prevention and/or treatment of ... ### FreshPatents.com Support |