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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 Two Nitrogens And Four Carbon Atoms (e.g., Pyridazines, Etc.) > 1,4-diazine As One Of The Cyclos 1,4-diazine As One Of The Cyclos1,4-diazine As One Of The Cyclos 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.02/01/07 - 20070027157 - Quinoxalinone-3-one derivatives as orexin receptor antagonists The invention relates to quinoxalinone derivatives of general Formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as ... 01/25/07 - 20070021431 - Reverse-turn mimetics and method relating thereto Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed ... 01/25/07 - 20070021430 - Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor The present invention relates to a novel crystalline anhydrate polymorph of the dihydrogenphosphate salt of (2R)-4-oxo-4-[3-trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine as well as a process for their preparation, pharmaceutical compositions containing this novel form, and methods of use of the novel form and pharmaceutical compositions for the treatment of diabetes, obesity, and high blood ... 01/25/07 - 20070021429 - Condensed n-heterocyclic compounds and their use as crf receptor antagonists The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof (Formula (I)) wherein the dashed line may represent a double bond; R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 ... 01/11/07 - 20070010520 - Triazolopyrazines and methods of making and using the same The invention is based on the discovery that compounds of formula (I) possess unexpectedly high affinity for the A2a adenosine receptor, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including Parkinson's disease. In one embodiment, the invention features a compound of formula I (See formula ... 01/04/07 - 20070004738 - Substituted pyrazoles Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S. ... 01/04/07 - 20070004737 - Process of purifying tadalafil The invention is directed to a method of purifying tadalafil by crystallization of tadalafil from a solution of crude tadalafil in a suitable crystallization solvent. ... 01/04/07 - 20070004736 - Imidazole derivative, process for producing the same, and use wherein R represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent linear hydrocarbon group, X represents an optionally substituted divalent hydrocarbon group, Y represents —CO—, —S(O)—, —S(O)2— or a bond, ring A represents an optionally substituted pyrrolidine ... 12/28/06 - 20060293334 - Nitrogen-containing heteroaryl compounds having inhibitory activity against hiv integrase (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase. ... 12/28/06 - 20060293333 - Therapeutic amides wherein A, X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides pharmaceutical compositions comprising a compound of the above formula or a salt thereof, intermediates useful for preparing a compound of the above formula, and therapeutic methods comprising administering ... 12/28/06 - 20060293332 - Sulfonylquinoxalone derivatives and related compounds as bradykinin antagonists Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists. ... 12/28/06 - 20060293331 - Process of synthesizing tadalafil The present invention provides tadalafil of high purity and processes of making such tadalafil by cyclization of TDCl in a solution. ... 12/21/06 - 20060287327 - Helix 12 directed non-steroidal antiandrogens are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. ... 12/21/06 - 20060287326 - 17-acetamido-4-azasteroid derivatives as androgen receptor modulators Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. ... 12/21/06 - 20060287325 - Combinations of paroxetine and 2-(r)-(4-fluoro-2-methyl-phenyl)-4-(s)-((8as)-6-oxo-hexahydro-pyrrolo'1,2-a!-pyrazin-2-yl)-piperidine-1-carboxylicacid'1-(r)-(3,5-bis-trifluoromethyl-phenyl)- The present invention relates to therapeutic combinations comprising paroxetine or physiologically acceptable salts or solvates thereof and 2-(R)-(4-Fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-a]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide or pharmaceutically acceptable salts or solvates thereof, to pharmaceutical compositions containing said combinations and their use in the treatment of depression and/or anxiety. ... 12/14/06 - 20060281751 - Raf inhibitor compounds and methods of use thereof Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, ... 11/30/06 - 20060270679 - Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to ... 11/23/06 - 20060264441 - Derivatives of n-heterocyclylmethylbenzamides, prepartion method thereof and application of same in therapeutics Wherein R, R1, R2, X and n are as described herein. Also disclosed and claimed in certain of the embodiments herein are the methods of preparation of compound of formula (I)and its use in therapeutics. ... 11/23/06 - 20060264440 - Pyrazoles and methods of making and using the same The invention is based on the discovery that compounds of formula I possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. In one embodiment, the invention features a compound of formula I (I). ... 11/16/06 - 20060258663 - Cyclic g-2allylproline in treatment of parkinson's disease Embodiments of this invention provide methods for thereapeutic use of cyclic G-2-Allyl Proline to treat disorders of dopaminergic neurons, including Parkinson's disease. Cyclic G-2Allyl P is neuroprotective and has utility as a therapeutic agent for treatment of diseases and other conditions characterised by degeneration and/or death of dopaminergic neurons and ... 11/16/06 - 20060258662 - Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases The present invention relates to compounds useful as inhibitors of Aurora protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. ... 11/16/06 - 20060258661 - 17-acetamido-4-azasteroid derivatives as androgen receptor modulators Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, ... 11/09/06 - 20060252760 - Farnesyl transferase inhibitors A family of compounds capable of inhibiting the activity of farnesyl transferase. ... 11/09/06 - 20060252759 - New tetracyclic 6 azapyrazinoindolines as 5ht2c receptor agonists for obesity as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments. ... 11/09/06 - 20060252758 - Spiroheterocyclic compounds and their uses as therapeutic agents k, j, p, Q, R1, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, that are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical ... 11/02/06 - 20060247245 - Substituted imidazolopyrazine and triazolopyrazine derivatives: gabaa receptor ligands Compounds of Formula (1) are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8, and Ar in the above Formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are ... 11/02/06 - 20060247244 - Quinoxalinones and their use especially in the treatment of cardiovascular diseases The invention relates to quinoxalinones and to methods for producing the same as well as the use thereof for preparing drugs for the treatment and/or prophylaxis of diseases, especially of cardiovascular diseases. ... 10/12/06 - 20060229311 - Isatine derivatives with neurotrophic activity The present invention relates to novel isatin derivatives, pharmaceutical compositions comprising the isatin derivatives of the invention, methods of preparing the isatin derivatives of the invention, their use in the treatment of neurodegenerative diseases and for the regeneration or prevention of degeneration of lesioned and damaged neurons, and methods of ... 10/05/06 - 20060223810 - Bicyclic pyrazole compounds as antibacterial agents Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection. ... 09/21/06 - 20060211699 - Quinoxaline dihydrohalide dihydrates and synthetic methods therefor Crystalline polymorph forms of Gonadotropin Releasing Hormone receptor antagonists, including crystalline polymorphs of quinoxaline dihydrohalide dihydrates, in particular crystalline polymorphs of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]-piperazin-1-yl}methyl)-quinoxaline dihydrochloride dihydrate, methods of making the same, as well as pharmaceutical compositions, and dosage forms containing them are disclosed. ... 09/21/06 - 20060211698 - Bicyclic heteroaryl derivatives for treating viruses Disclosed are compounds having formula I and related compositions and methods thereof. The compounds are useful for treating viral infections caused by the Flaviviridae family of viruses. ... 09/07/06 - 20060199823 - Heteroaryl fused pyridines, pyrazines and pyrimidines as crf1 receptor ligands Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and ... 08/31/06 - 20060194806 - Optically active 5h-pyrrolo [3,4-b] pyrazine derivative, its preparation and pharmaceutical compositions containing same Dextrorotatory isomer of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, its preparation and pharmaceutical compositions containing it which are usable as tranquillisers and hypnotics. ... 08/31/06 - 20060194805 - Capsaicin receptor agonists Capsaicin receptor agonists are provided. Such compounds are ligands that may be used to modulate VR1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to capsaicin receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using ... 08/24/06 - 20060189619 - 3-({4-[2-(4-tert-butylphenyl)-1h-benzimidazol-4-yl]piperazin-1-yl}methyl)pyrido[2,3-b]]pyrazi ne compounds The present invention relates to Gonadotropin Releasing Hormone (“GnRH”) (also known as Leutinizing Hormone Releasing Hormone) receptor antagonists. ... 08/24/06 - 20060189618 - 4-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists. ... 08/17/06 - 20060183746 - Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton's tyrosine kinase by such compounds and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, may in certain embodiments be used to treat patients suffering from one or more diseases responsive to inhibition of tyrosine kinase activity. The diseases may, for instance, be responsive to inhibition of Btk activity and/or B-cell ... 08/03/06 - 20060173010 - Modulators of tnf-alpha signaling The present invention provides compounds which are modulators of TNF-α signaling and methods of use thereof for treating a patient having a TNF-α mediated condition. The compounds can be represented by the following structural formulas: ... 07/27/06 - 20060167000 - Neurologically-active compounds The present invention relates to neurologically-active compounds, processes for their preparation and their use as pharmaceutical or veterinary agents, in particular for the treatment of neurological conditions, more specifically neurodegenerative conditions such as Alzheimer's disease. ... 07/13/06 - 20060154931 - Heteroaromatic quinoline compounds The invention pertains to heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in ... 07/06/06 - 20060148808 - Substituted heterocycle fused gamma-carbolines or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The compounds used in the method of treatment of this invention are serotonin agonists and antagonists and are useful in the control or ... 06/29/06 - 20060142294 - Novel compounds for treatment of cancer and disorders associated with angiogenesis function Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian ... 06/15/06 - 20060128712 - Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups and R2, R′, R″, R3, R4, R5, R6, R7, X1, X1′, X2, and N are as defined in the specification. Compounds of the invention are useful for the treatment of neurological and neuropsychiatric disorders. ... 06/15/06 - 20060128711 - Antitumoral analogs Derivatives of ecteinascidin 736 of general formula (I) wherein the groups R1, R2, R3, R4 and R5 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, C(═O)R′, C(═O)OR′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, substituted or unsubstituted C1-C25 alkyl, substituted or ... 05/25/06 - 20060111357 - Quinoline compounds for use in mch receptor related disorders The present invention relates to the use of quinoline compounds for the preparation of a pharmaceutical and/or a cosmetic composition for the treatment, prophylaxis and/or diagnosis of a condition caused by or involving a melanin-concentrating hormone. The invention also relates to novel quinoline compounds per se. The quinoline compounds have ... 05/25/06 - 20060111356 - External preparation for allergic diseases The invention presents an external preparation for allergic diseases containing 3′-hydroxymethyl-4-hydroxypyrrolido[1,2-f]2′,5′-pipera-zinedione as an active ingredient. This compound has a prophylactic and therapeutic effect of allergic diseases, and the external preparation of the invention can be used in prophylaxis and treatment of various allergic diseases (for example, atopic dermatitis, urticaria, allergic ... 05/18/06 - 20060106023 - Novel imidazopyrazines as cyclin dependent kinase inhibitors In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, ... 05/18/06 - 20060106022 - Imidazo[4,5-b]pyrazinone inhibitors of protein kinases wherein Q, Y, A are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein kinases, especially Aurora-1, Aurora-2 and Aurora-3 kinases. ... 05/18/06 - 20060106021 - New antitumoral derivatives of et-743 Derivatives of Et-743 or Et-770 or Et-729 are provided. The derivatives are of the general formula (Ia) wherein the substituent groups take various permitted meanings. ... 05/04/06 - 20060094724 - Fused furan compound wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; ... 04/27/06 - 20060089361 - Methods for treating retinal diseases wherein the 2-imidazolin-2-ylamino group is in either the 5- or 6-position of the quinoxaline nucleus; x, y and z are in any of the remaining 5-, 6-, 7- or 8-positions and are selected from hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; and R is an optional substituent in either ... 04/27/06 - 20060089360 - Vanilloid receptor ligands and their use in treatments Substituted nitrogen-containing heterocycles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with ... 04/20/06 - 20060084656 - Compositions and methods for intranasal, buccal, sublingual and pulmonary delivery of varenicline A composition for nasal administration comprising varenicline or its pharmaceutically acceptable salt and at least one excipient. The invention also provides a composition for buccal administration comprising varenicline or its pharmaceutically acceptable salt and at least one excipient to form a solid dosage form, wherein the solid dosage form disintegrates ... 04/20/06 - 20060084655 - Reverse-turn mimetics and method relating thereto Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed ... 04/20/06 - 20060084654 - Imidazopyrazine tyrosine kinase inhibitors and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases. ... 04/13/06 - 20060079530 - Farnesyl transferase inhibitors A family of compounds capable of inhibiting the activity of farnesyl transferase. ... 04/13/06 - 20060079529 - Inhibitors of proton-gated cation channels and their use in the treatment of ischaemic disorders This invention relates to the use of compounds capable of inhibiting the activity of a proton-gated cation channel in the treatment of alleviation of diseases or disorders associated with, or mediated by a drop in extra cellular pH. ... 04/13/06 - 20060079528 - Carbamic acid compounds comprising a bicyclic heteroaryl group as hdac inhibitors This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic C9-10heteroaryl group (e.g., quinolinyl; quinoxalinyl; benzoxazolyl; benzothiazolyl); Q is an acid leader group, and is independently an unsubstituted or substituted, saturated or unsaturated ... 03/30/06 - 20060069098 - Bicyclic compound wherein symbol “A” represents a saturated heterocyclic group, a 5-membered heteroaromatic group having two heteroatoms in the ring, a group represented by the formula A1 (R2, R3, and R4 represent hydrogen atom, hydroxyl group, etc.), etc., B represents a group represented by the formula B1 (R11 represents hydrogen atom, hydroxyl ... 03/16/06 - 20060058309 - Respiratory syncytial virus replication inhibitors The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4- represents a radical of formula —CH═CH—CH═CH—; —N═CH—CH═CH—; —CH═N—CH═CH—; —CH═CH—N═CH—; CH═CH—CH═N—; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), ... 03/16/06 - 20060058308 - Vanilloid receptor ligands and their use in treatments Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints ... 03/16/06 - 20060058307 - Combination of an atp-competitive inhibitor of bcr/abl kinase activity and a tyrphostin analog The present invention relates to a combination of (a) an ATP-competitive inhibitor of Bcr/abl kinase activity and (b)) a tyrphostin analog, and the use of said combination or product for the treatment of bcr/abl-related diseases. ... 03/09/06 - 20060052382 - 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also ... 02/23/06 - 20060040946 - Methods and compositions for the treatment of metabolic disorders The present invention is directed to a novel methods and compositions for the therapeutic intervention in hyperphenylalaninemia. More specifically, the specification describes methods and compositions for treating various types of phenylketonurias using compositions comprising BH4. Combination therapies of BH4 and other therapeutic regimens are contemplated. ... 02/23/06 - 20060040945 - Annellated pyrrole compounds as proton pump inhibitors for treating ulcer Inhibiting gastric proton pump in a mammal is accomplished by the use of a compound of formula (1) wherein the variables have the meaning given in the present description. A preferred compound of formula (2) is this treatment ameliorates, diminishes, actively treats, reverses or prevents any injury, damage or lesions ... 02/16/06 - 20060035899 - Use of cysteine derivatives for the preparation of a medicament intended to treat pathologies which result from the formation of the heterotrimeric g protein The invention relates to the use of cysteine derivatives for preparing a medicament intended to treat diseases which result from the formation of the heterotrimeric G protein. These diseases include in particular diseases linked to the following biological functions or disorders: smell, taste, perception of the light, neurotransmission, neurodegeneration, endocrine ... 02/16/06 - 20060035898 - Fused ring heterocycle kinase modulators The present invention provides novel fused ring heterocycle kinase modulators and methods of using the novel fused ring heterocycle kinase modulators to treat diseases mediated by kinase activity. ... 02/09/06 - 20060030566 - Novel quinoxalinone norepinephrine reuptake inhibitors for the treatment of central nervous system disorders wherein R1-R8 and n are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system disorders. ... 02/09/06 - 20060030565 - Amide derivatives and nociceptin antagonists wherein R2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5 is halogen atom, hydroxy, lower alkyl optionally substituted by ... 02/02/06 - 20060025418 - Methods of making and using n-desmethylzopiclone The invention is directed to compositions comprising, and methods of using, racemic N-desmethylzopiclone, optically pure (+)-N-desmethylzopiclone, and optically pure (−)-N-desmethylzopiclone in the treatment and prevention of diseases and conditions in mammals. The invention is further directed to novel methods of preparing N-desmethylzopiclone, optically pure (+)-N-desmethylzopiclone, and optically pure (−)-N-desmethylzopiclone. ... 01/26/06 - 20060019961 - Estrogen receptor ligands The present invention relates to estrogen receptor ligands, and compounds and methods for treating diseases associated with excessive estrogen receptor activity. ... 01/26/06 - 20060019960 - Antitumoral analogs of et-743 Antitumor compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected from an optionally protected or derivatised aminomethylene group or an optionally protected or derivatised hydroxymethylene ... 01/26/06 - 20060019959 - Novel quinoxalinone derivatives B′1, B′2, . . . , B′n-1 and B′n (in which n is 4, 5 or 6) are each independently hydrogen or the like; and R is hydrogen, lower alkyl or the like. ... 01/26/06 - 20060019958 - Immunity-related protein kinase inhibitors wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring ... 01/19/06 - 20060014750 - Pharmaceutical compositions for the treatment of cns and other disorders The present invention relates to a method of treating disorders of the central nervous system (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant α7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant ... 01/19/06 - 20060014749 - Aminopiperidine quinolines and their azaisosteric analogues with antibacterial activity Aminopiperidine derivatives of formula (I) and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man. ... 01/12/06 - 20060009457 - New pyridodihydropyrazinones, process for their manufacture and use thereof as medicaments while the groups L, R1, R2, R3, R4 and R5 may have the meanings given in the claims and specification. ... 01/12/06 - 20060009456 - Aryl-substituted piperazine derivatives Aryl-substituted piperazine derivatives are provided. Such compounds may be used to modulate MCH receptor activity in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating ... 01/12/06 - 20060009455 - Six-membered heterocycles useful as serine protease inhibitors or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, X1, X2, X3, X4, and X5 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for ... 01/05/06 - 20060004013 - Cinnamide compound or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents. The object of the present invention is to find a therapeutic or preventive agent for diseases caused by Aβ. According to the present invention, a therapeutic or preventive agents for diseases caused by Aβ can be ... 01/05/06 - 20060004012 - Compounds, pharmaceutical compositions and methods for use in treating metabolic disorders wherein the definitions of the variables Q, L1, P, L2, M, X, L3 and A are provided herein. The present invention also provides compositions and methods for use of the compounds, for instance, for treatment of type II diabetes. ... 01/05/06 - 20060004011 - Indolyl pyrazinone derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis This invention relates to a compound of Formula I (I) and its use in treating hyper-proliferative disorders and diseases associated with angiogenesis. ... 01/05/06 - 20060004010 - Ccr4 antagonist and medical use thereof The compound of formula (I) has CCR4 antagonistic activity, and therefore is useful as a preventive and/or therapeutic agent for diseases associated with CCR4, i.e., CCR4-mediated diseases such as inflammatory and/or allergic diseases [e.g., systemic inflammatory response syndrome (SIRS), anaphylaxis or anaphylaxis-like reaction, allergic vasculitis, reject reaction for graft organ, ... 12/29/05 - 20050288296 - Alkyl substituted indoloquinoxalines and pharmacologically acceptable salts thereof are described. The compounds are useful as drugs for preventing and/or treating autoimmune diseases. ... 12/29/05 - 20050288295 - Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof Methods of treating or preventing disorders in which aberrant kinase activity is implicated, pharmaceutically compositions, and methods for detecting the presence kinases in cells or biological preparations and for identifying kinases of therapeutic interest. ... 12/29/05 - 20050288294 - Inhibitors of akt activity The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyrazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration ... 12/29/05 - 20050288293 - 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors 8-Hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds are inhibitors of HIV integrase and inhibitors of HIV replication. More particularly, the compounds are of Formula (1): wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in ... 12/29/05 - 20050288292 - Pharmaceutical formulation and its use in the treatment of inner ear diseases A new pharmaceutical formulation, especially for trans-tympanic or intra-transtympanic administration, containing a quinoxalin-2-one compound of the formula (I) in which R1 and R2, independently of one another, are hydrogen, methyl-, ethyl-, propyl-, butyl- or R1 and R2 together are a cyclo-alkyl compound; R3 is methoxy, ethoxy, hydroxy, hydrogen, C1-C4 alkyl ... 12/22/05 - 20050282812 - Inhibitors of cholesteryl ester transfer protein This invention relates to inhibitors of CETP and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders mediated by CETP. ... 12/22/05 - 20050282811 - Diazabicyclic histamine-3 receptor antagonists as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I or II, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment ... 12/08/05 - 20050272738 - Combined treatment with oxaliplatin and an epidermal growth factor receptor kinase inhibitor The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an EGFR kinase inhibitor and oxaliplatin combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. ... 12/08/05 - 20050272737 - Combined treatment with irinotecan and an epidermal growth factor receptor kinase inhibitor The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an EGFR kinase inhibitor and irinotecan combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. ... 12/08/05 - 20050272736 - Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands wherein R1 or R2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R1, R2, R3, R3a, R3b, R4, R5, L, X, X′, Y, Y′, Z, and Z′ are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by ... 12/08/05 - 20050272735 - 1h-indazoles, benzothiazoles, 1,2-benzoisoxazoles, 1,2-benzoisothiazoles, and chromones and preparation and uses thereof The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands ... 12/01/05 - 20050267116 - Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or ... 12/01/05 - 20050267115 - Alkyne compounds with mch antagonistic activity and medicaments comprising these compounds wherein A, B, W, X, Y, Z, R1, and R2 have the meanings given herein, which have MCH-receptor antagonistic activity and are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes. ... 12/01/05 - 20050267114 - Triazaspiro[5.5]undecane derivatives and drugs comprising the same as the active ingredient (wherein all of the symbols have the same meanings as defined in specification.), quaternary ammonium salts thereof, N-oxides thereof or salts thereof. The compounds represented by formula (I) are used for prevention and/or treatment of various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, chronic rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis ... 11/24/05 - 20050261300 - Liquid pharmaceutical formulations containing 3.7-diazabicyclo[3,3,1]nonane compounds and methods of treatment relating to arrhythmic events A method of using 3,7-diazabicyclo[3,3,1]nonane compounds, preferably of 9,9-alkylene-3,7-diazabicyclo[3,3,1]nonane compounds, and most preferably to the use of tedisamil, and the physiologically acceptable acid addition salts and/or solvates thereof, in the form of a liquid pharmaceutical preparation for the treatment and/or inhibition of arrhythmic events in human patients, preferably in conversion ... 11/24/05 - 20050261299 - 2-pyridyl substituted imidazoles as alk5 and/or alk4 inhibitors wherein R1, R2, R3, A1 and A2 are as defined herein, which are used advantageously in inhibiting the TGF-β and/or activin signaling pathway in mammals. ... 11/24/05 - 20050261298 - Methods of treating conditions associated with an edg-7 receptor In one aspect, the present invention provides a method for modulating an Edg-7 receptor mediated biological activity in a cell. A cell expressing the Edg-7 receptor is contacted with a modulator of the Edg-7 receptor which is capable of modulating an Edg-7 receptor mediated biological activity. In another aspect, the ... 11/17/05 - 20050256125 - Pyrimidine derivatives for the treatment of abnormal cell growth or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof, wherein R1-R4 and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates a method of using such compounds in the treatment of ... 11/10/05 - 20050250778 - Topical brimonidine tartrate formulations that lack chlorine dioxide Topical solution compositions of brimonidine tartrate are disclosed. The solution compositions lack an oxidative preservative. ... 11/10/05 - 20050250777 - Novel derivatives of cycloalcanodiones, method for the production thereof and their pharmacological applications In general terms, said cycloalkanedione derivatives correspond to formula I: ... 11/03/05 - 20050245528 - Reverse-turn mimetics and compositions and methods related thereto wherein A, R1, R2, R2a and R3 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. ... 11/03/05 - 20050245527 - Nitrogen containing heterocyclic compounds and medicines containing the same salts thereof and hydrates of the foregoing. ... 11/03/05 - 20050245526 - Beta-agonists, methods for the preparation thereof and their use as pharmaceutical compositions wherein the groups R1 to R7 have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, processes for preparing these compounds and ... 10/27/05 - 20050239788 - Azaindoles having serotonin receptor affinity Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia. ... 10/27/05 - 20050239787 - Novel maxi-k channel blockers, methods of use and process for making the same This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions related to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to ... 10/20/05 - 20050234065 - Dipeptidyl peptidase-iv inhibitors or prodrugs thereof, or pharmaceutically acceptable salts of said compounds or prodrugs, or solvates of said compounds, prodrugs or salts, wherein A, N, X and R1 are as defined herein; pharmaceutical compositions thereof; and methods of using the pharmaceutical compositions for the treatment of diseases, including Type 2 diabetes, Type ... 10/20/05 - 20050234064 - Quinoxalines useful as inhibitors of protein kinases The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. ... 10/20/05 - 20050234063 - Therapeutic agent for brain hemorrhage It was found that an AMPA receptor antagonist zonampanel or a salt or the like thereof has an effect to improve cerebral hemorrhage and neurological symptoms accompanied by cerebral hemorrhage and therefore is useful as an agent for treating cerebral hemorrhage. ... 10/13/05 - 20050227987 - 11beta-hydroxysteroid dehydrogenase inhibitors wherein Q is an atom selected from the group consisting of S, O, N and C; the compound is selected from compounds of the formulae R1C(═O)—NR3-L-R2; R1—S(═O)(═O)—C(R4)(R5)-L-R2; R1—S—C(R4)(R5)-L-R2; R1—NR3—S(═O)(═O)-L-R2; R1—NR3—C(═O)-L-R2; R1—C(R4)(R5)—S(═O)(═O)-L-R2; and R1—C(R4)(R5)—S-L-R2. ... 10/06/05 - 20050222157 - Methods of treatment of menopause and perimenopause using eszopiclone The invention relates to the use of eszopiclone for the treatment of symptoms accompanying perimenopause or menopause. ... 10/06/05 - 20050222156 - Methods of treatment of chronic pain using eszopiclone The invention relates to the use of eszopiclone for the treatment of low-level, chronic pain and fatigue associated with pain. ... 10/06/05 - 20050222155 - Inhibitors of akt activity The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. ... 09/29/05 - 20050215557 - Triazaspiro[5.5]undecane derivative and pharmaceutical composition comprising the same as active ingredient Therefore the compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis or rheumatoid arthritis etc. ... 09/29/05 - 20050215556 - Macrocyclic kinase inhibitors are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds. ... 09/29/05 - 20050215555 - Inhibitors of 5-ht2a receptor wherein X, Y, Z, and R1 are as described herein, 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. ... 09/08/05 - 20050197340 - Fused-pyrazolo pyrimidine and pyrazolo pyrimidinone derivatives and methods for using the same wherein A, B, X, Y, Z, W, k, R1, R2, R3, R4 and R5 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing compounds of formula I and using the same in treating p38 mediated disorders in a subject. ... 08/18/05 - 20050182062 - 1,4-diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof in which X represents a nitrogen atom or a group of formula C—R2, P represents a group of formula C—R3, Q represents a group of formula C—R4, R represents a group of formula C—R5, W represents a group of formula C—R6, or one of the symbols P, Q, R and ... 08/18/05 - 20050182061 - Phthalimide compounds useful as protein kinase inhibitors The present invention provides compounds as inhibitors of protein kinase, particularly inhibitors of AKT, PDK1, p70S6K, or ROCK kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides processes for preparing the compounds of the invention, pharmaceutical compositions comprising the compounds, and methods of utilizing those ... 08/11/05 - 20050176720 - Pharmaceutical composition for the treatment of cns and other disorders The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant α7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant ... 08/11/05 - 20050176719 - Novel pyrazinone derivatives [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V is CH, etc., Wn is —(CH2)n— (n is zero to four), R1, is H or optionally substituted lower alkyl, etc., R2 ... 08/11/05 - 20050176718 - Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, ... 08/11/05 - 20050176717 - Quinoxaline compounds and methods of using them The present invention generally relates to quinoxaline compounds having Formula 1 or Formula 2 wherein the variables are as defined herein, and methods of using them. ... 08/11/05 - 20050176716 - Modulators of the glucocorticoid receptor, ap-1, and/or nf-kappab activity and use thereof its stereoisomers thereof, or a solvate thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR1R2 or CH2NR1R2 and where at least two of X1-X4 and/or X5-X8 is N or NR18, and R, Ra, Rb, Rc, Rd, R1, R2 and R18 are defined herein. Also ... 08/11/05 - 20050176715 - Piperidine derivatives A represents C(O) or S(O)q, provided that when Y is nitrogen and Z is CH, A is not S(O)q; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p and q are independently an integer from 1 to 2; and pharmaceutically ... 08/04/05 - 20050171114 - Benzo[b]chromeno-naphthyridin-7-one and pyrano[2',3':7,8]quino[2,3-b]quinoxalin-7-one compounds A represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH—, —C(O)—CH(R8)— or —CH(R8)—C(O)— wherein R5, R6, R7 and R8 are as defined in the description, its isomers, N-oxides, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment ... 08/04/05 - 20050171113 - Product comprising an inhibitor of the transduction of heterotrimeric g protein signals combined with an anti-hypertensive agent for therapeutic use in the treatment of arterial hypertension wherein the substituents are defined as in the specification and the salts thereof and at least one other antihypertensive agent for the treatment of arterial hypertension. ... 08/04/05 - 20050171112 - Combinations useful for the treatment of neuronal disorders The present invention provides a method for the treatment of neuronal disorders, in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of at least one QC-inhibitor, optionally in combination with at least one agent, selected from the group consisting of PEP-inhibitors, ... 08/04/05 - 20050171111 - Benzylimidazolyl substituted 2-quinoline and quinazoline derivatives for use as farnesyl transferase inhibitors wherein r, t, Y1, Y2, R1, R2, R3, R5, R6and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine. ... 07/21/05 - 20050159421 - Ethylene diamine derivatives and their use as orexin-receptor antagonists This invention relates to heterocyclic substituted ethylene diamine derivatives and their use as pharmaceuticals. ... 07/07/05 - 20050148591 - Tartrate salts of 5,8,14-triazatetracyclo [10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaen and pharmaceutical compositions thereof and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, ... 07/07/05 - 20050148590 - Disubstituted chalcone oximes as selective agonists of rar retinoid receptors where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RARγ agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis. ... 06/30/05 - 20050143383 - Pharmaceutical compounds These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR. ... 06/30/05 - 20050143382 - Heterocyclic compounds as pharmaceutically active compounds wherein R1 to R9 in formula (I) represent independently of each other a variety of different substituents comprising alkyl, aryl, aralkyl, alkylaryl, heteroaryl groups and monofunctional moieties. ... 06/23/05 - 20050137202 - Indole derivative having heterocycle and mono- or diazaindole derivative wherein Het represents an optional substituted heterocylic group A1 and A2 each independently represent —CH═, etc.; A3 represents —CH2—, etc.; R1 represents a 4-fluorophenyl group, etc.; R2 represents an alkyl group; n represents 0, 1 or 2, provided that when A1 and A2 both are —CH═, A3 represents —CH2— or ... 06/23/05 - 20050137201 - Compositions useful as inhibitors of protein kinases The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. ... 06/16/05 - 20050130980 - Novel imidazopyrazines as cyclin dependent kinase inhibitors In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, ... 06/16/05 - 20050130979 - Treatment of demyelinating disorders This invention is directed to pharmaceutical compositions and methods for treating demyelinating disorders based upon inhibitors of the interaction of glutamate with the AMPA and of the interaction of glutamate with the kainite receptor complex. ... 06/16/05 - 20050130978 - Novel crystal of quinoxalinedione derivative anhydride The object of the present invention is to provide a novel crystal of a quinoxalinedione derivative as an AMPA antagonist, which enables providing a bulk for manufacturing pharmaceuticals that are stable under any humidity conditions. ... 06/16/05 - 20050130977 - Inhibitors of akt activity The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. ... 06/02/05 - 20050119268 - Treatment of crth2-mediated diseases and conditions The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2. ... 06/02/05 - 20050119267 - Diazabicyclo alkane derivatives with nk1 antagonistic activity The present invention relates to a group of unique diazabicyclo alkane derivatives having interesting neurokinin-NK1 receptor antagonistic activity represented by the general formula (1) wherein: R1 represents phenyl, 2-indolyl, 3-indolyl, 3-indazolyl or benzo[b]thiophen-3-yl, which groups may be substituted with halogen or alkyl (1-3C), R2 and R3 independently represent halogen, H, ... ### FreshPatents.com Support - Terms & Conditions |