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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 > Spiro Ring System

Spiro Ring System

Spiro Ring System 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 - 20070027174 - Phenylalanine enamide derivatives
or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and ...

02/01/07 - 20070027173 - Indol-3-yl-carbonyl-spiro-piperidine derivatives as vla receptor antagonists
wherein the spiro-piperidine head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, methods for preparing the compounds and pharmaceutical compositions, and their use in the treatment of dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of ...

01/25/07 - 20070021454 - Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in ...

01/25/07 - 20070021453 - Novel spirochromanone derivatives
or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders. ...

01/18/07 - 20070015784 - Subsitituted 1,4,8- triazaspiro [4,5]decan-2-one compounds
processes for the preparation thereof, related methods of treatment and pharmaceutical formulations containing such compounds. ...

01/18/07 - 20070015783 - Substituted 1,4,8-triazaspiro[4,5]decan-2-one compounds
processes for the preparation thereof, related methods of treatment and pharmaceutical formulations containing such compounds. ...

01/18/07 - 20070015782 - Benzimidazole compound
R4, R5, R6 and R7 represent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and W1 represents a single bond, methylene or ethylene group, a salt thereof or a solvate of these. ...

01/18/07 - 20070015781 - Certain substituted spirocyclic lactams and use thereof as pharmaceuticals
wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them. ...

01/18/07 - 20070015780 - Method of treating cancer with azaspirane compositions
A method of treating cancer by administering a therapeutically effective amount of a compound represented by the following Formula (I), or salt, hydrate, or solvate thereof; wherein: n represents a number from 3 to 7; m represents a number from 1 to 2; R1 and R2 independently represent a hydrogen ...

01/11/07 - 20070010542 - Benzimidazole compound
R4, R5, R6 and R7 represent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and W1 represents a single bond, methylene or ethylene group, a salt thereof or a solvate of these. ...

01/04/07 - 20070004766 - Methods for relaxation of smooth muscle contractions using trospium
Methods are disclosed using Trospium Chloride, an antimuscarinic smooth muscle relaxant, for the treatment of urinary incontnence, while avoiding the concomitant liability of adverse side effect associated with other antimuscarinic drugs. ...

01/04/07 - 20070004765 - New compounds
wherein R1 to R3 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 GHSR receptor-related disorder. Examples of such disorders are obesity and related disorders such as diabetes type II, dyslipidemia ...

12/28/06 - 20060293356 - Methods for treating smooth muscle contractions using trospium
Methods are disclosed using trospium, an antimuscarinic smooth muscle relaxant, for the treatment of smooth muscle disorders, while avoiding the concomitant liability of adverse side effects associated with conventional antimuscarinic treatment. ...

12/21/06 - 20060287347 - Methods for treating smooth muscle disorders using trospium
Methods are disclosed using Trospium Chloride, an antimuscarinic smooth muscle relaxant, for the treatment of urinary incontinence, and other disorders, while avoiding the concomitant liability of adverse side effects associated with conventional antimuscarinic treatment. ...

11/30/06 - 20060270696 - Hydantoin compounds
The invention relates to the use of hydantoin compounds useful for treating or preventing autoimmune disorders. The present invention also provides compositions and uses thereof. ...

11/30/06 - 20060270695 - Spirocyclic heterocyclic derivatives and methods of their use
Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions. ...

10/26/06 - 20060241133 - Electrically variable pneumatic structural element
There is disclosed the use of a compound of formula (I): or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for the treatment of age-related cognitive decline or mild cognitive impairment, in particular with a view to preventing or delaying the onset of Alzheimer's disease. ...

10/26/06 - 20060241132 - Spiro derivatives and adhesion molecule inhibitors comprising the same as active ingredient
Since the spiro acid derivatives according to the present invention are excellent in the effect of inhibiting cell adhesion via adhesion molecules, especially adhesion molecule VLA-4, they are useful as therapeutic drugs against various inflammatory diseases. For example, provided are the spiro derivative and the adhesion molecule inhibitor which includes ...

10/19/06 - 20060235037 - Heterocyclic inhibitors of protein arginine methyl transferases
methods of using such compounds in the treatment of hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases; and to pharmaceutical compositions containing such compounds. ...

09/28/06 - 20060217406 - N-aryl diazaspiracyclic compounds and methods of preparation and use thereof
Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions ...

09/28/06 - 20060217405 - Interstitial cystitis treatment
An anti-muscarinic agent exemplified by trospium is administered by intravesicular instillation into the bladder and used to treat interstitial cystitis. The instilled medication does not interact systemically with the patient; the localized effect of the medication avoids any question of systemic side effects or untoward reactions with body organs or ...

09/21/06 - 20060211722 - Amino cyclobutylamide modulators of chemokine receptor activity
The present invention is directed to compounds of the formulas I and II: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R25, R26, Y, Z, l, m, n and the broken lines are as defined herein which are useful as modulators of ...

09/14/06 - 20060205750 - Novel benzimidazole derivatives
(wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is —N(SO2R4)—, —N(COR5)— or —CO—; Y is —C(R6)(R7)—, —O— or —N(R8)—, ...

09/14/06 - 20060205749 - Remedy and/or preventive for lung diseases
The present invention provides a therapeutic and/or preventive agent for pulmonary disease that exhibits neutrophilic inflammation, such as, chronic obstructive pulmonary disease (COPD), pulmonary emphysema, chronic bronchitis, acute respiratory distress syndrome (ARDS), acute lung injury (ALI) and the like, which comprises 7-[2-(3,5-dichloro-4-pyridyl)-1-oxoethyl]-4-methoxy-spiro[1,3-benzodioxol-2,1′-cyclopentane] or a pharmaceutically acceptable salt thereof as an ...

08/17/06 - 20060183764 - Combination of gh secret agogues and pde4 inhibitors for the treatment of alzheimers disease
There is disclosed the treatment or prevention of diseases involving deposition of beta-amyloid in the brain, e.g. Alzheimer's disease, via the combined administration of a growth hormone secretagogue and a PDE4 inhibitor. ...

08/10/06 - 20060178390 - 1,3,8-triazaspiro[4,5]decan-4-one derivatives useful for the treatment of orl-1 receptor mediated disorders
wherein all variables are as defined herein, useful in the treatment of disorders and conditions mediated by the ORL-1 G-protein coupled receptor. More particularly, the compounds of the present invention are useful in the treatment of disorders and conditions such as anxiety, depression, substance abuse, neuropathic pain, acute pain, migraine, ...

08/10/06 - 20060178389 - Use of siramesine in the treatment of cancer
The present invention relates to the treatment of cancer. In particular, the invention provides pharmaceutical compositions comprising siramesine for the treatment of cancer. The invention further provides a method of treatment comprising administering siramesine to a patient suffering from cancer. ...

08/03/06 - 20060173028 - Therapeutic and/or preventive agent for chronic skin disease
The present invention provides a therapeutic and/or preventive agent for chronic skin diseases which comprises 7-[2-(3,5-dichloro-4-pyridyl)-1-oxoethyl]-4-methoxy-spiro[1,3-benzodioxol-2,1′-cyclopentane] or a pharmaceutically acceptable salt thereof as an active ingredient. ...

08/03/06 - 20060173027 - Spirocvclic piperidines as mch1 antagonists and uses thereof
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 ...

07/20/06 - 20060160835 - Methods and compositions for treatment of central nervous system disorders
The invention provides methods of screening for substances having an effect on a nicotine receptor by contacting a cell having a nicotine receptor with a test substance; and determining any increase or decrease in phosphorylation of Janus-Activated Kinase 2 (JAK2). An increase in phosphorylation of JAK2 indicates that the test ...

07/20/06 - 20060160834 - Combination therapy for the treatment of hypertension
The present invention relates to compositions comprising an anti-obesity agent and an anti-hypertensive agent useful for the treatment of hypertension, hypertension associated with obesity, and hypertension-related disorders. The present invention further relates to methods of treating or preventing obesity, and obesity-related disorders, in a subject in need thereof by administering ...

07/13/06 - 20060154945 - Spiro '1-azabicyclo' 2.2.2! octan-3,5'-oxazolidin - 2'-one! derivatives with affinity to the alpha7 nicotinic acetylcholine receptor
and pharmaceutically-acceptable salts thereof, wherein Q, Ar1, A and Ar2 are as defined in the specification, pharmaceutical compositions and formulations containing them, methods of using them to treat diseases and conditions either alone or in combination with other therapeutically-active compounds or substances, processes and intermediates used to prepare them, uses ...

07/13/06 - 20060154944 - Novel tricyclic heterocycle compound
(wherein A is a cyclic group which may have a substituent(s); X is a single bond or a spacer; Y is a single bond or a spacer; Z is a single bond or a spacer; B is a hydrocarbon group which may have a substituent(s) or a cyclic group which ...

07/06/06 - 20060148836 - Pyridyl-substituted spiro-hydantoin compounds and use thereof
its pharmaceutically acceptable salts, enantiomers, solvates, or prodrugs thereof, wherein R16 is a substituted pyridinyl group, as defined herein, is provided. Pharmaceutical compositions and methods of treating anti-inflammatory and/or immune diseases with the pyridyl-substituted spiro-hydantoin compounds are also objectives of this invention. ...

06/29/06 - 20060142319 - Pyridyl-substituted spiro-hydantoin crystalline forms and process
wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A1, A2, G, and Q are linkers; and R2, R4a, R4c, and R16 are defined in the specification. The process includes the reaction of N-substituted glycine compound and ...

06/22/06 - 20060135544 - Novel synthesis of irbesartan
Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4′-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid. ...

06/08/06 - 20060122210 - Inhibitors of 11-beta hydroxyl steroid dehydrogenase type i and methods of using the same
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 ...

05/25/06 - 20060111380 - Novel azole derivatives
wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are ...

05/18/06 - 20060106047 - Trisubstituted thiophenes as progesterone receptor modulators
The present invention is directed to novel trisubstituted thiophene derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by agonists and antagonists of the progesterone receptor. The clinical usage of these compounds are related to hormonal contraception, the treatment and/or prevention ...

05/18/06 - 20060106046 - Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient
[wherein R1 is hydrogen, hydroxyl, lower alkyl, or the like; R2, R3a, R3b, R4a, R4b, R5a, R5b and R6 each stands for hydrogen, halogen, or the like; W1 and W2 each independently stands for —O—, —CH2—, or the like; Y1, Y2, Y3 and Y4 stand for —CH—, —CF—, —N—, or ...

05/18/06 - 20060106045 - Spiroindolinepiperidine derivatives
Insecticidal, acaricidal, nematicidal or molluscicidal compounds of formula (I) wherein Y is a single bond, C═O, C═S or C═(O)q where q is 0, 1 or 2; and R1, R2, R3, R4, R8, R9 and R10 are as defined in the claims or salts or N-oxides thereof, processes for preparing them ...

05/11/06 - 20060100228 - Cannabinoid receptor ligands
and/or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions containing such compounds exhibit anti-inflammatory and immunomodulatory activity, and can be effective in treating cancer and inflammatory, immunomodulatory or respiratory diseases or conditions. ...

04/06/06 - 20060074099 - Crystalline forms and process for preparing spiro-hydantoin compounds
wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G′ is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the ...

04/06/06 - 20060074098 - Methods of treatment of amyloidosis using ethanolcyclicamine 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. ...

03/30/06 - 20060069112 - 4-heteroaryl-tetrahydroquinolines and their use as inhibitors of the cholesterin-ester transfer protein
Hetero-tetrahydroquinolines can be prepared either by condensing correspondingly substituted hetero-tetrahydroquinoline aldehydes with the desired substituent or by reducing the corresponding keto-substituted hetero-tetrahydroquinolines, followed by introduction of the desired substituent by customary methods. The hetero-tetrahydroquinolines are suitable for use as active compounds in medicaments, in particular in medicaments for treating artheriosclerosis ...

03/23/06 - 20060063791 - (spirocyclylamido)aminothiophene compounds
or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, R1, X and Y are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), ...

03/16/06 - 20060058328 - Use of n-aryl diazaspiracyclic compounds in the treatment of addiction
Compounds, compositions and methods for treating drug addiction, nicotine addiction, and/or obesity are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds are effective at ...

03/09/06 - 20060052408 - Cyclopropyl compounds as ccr5 antagonists
The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency ...

03/09/06 - 20060052407 - Novel crystals of triazaspiro [5.5] undecane derivative
The present invention relates to a new crystal of triazaspiro[5.5]undecane derivatives. The crystal of a non-solvate of (3R)-1-butyl-2,5-dioxo-3-[(1R)-1-hydroxy-1-cyclohexylmethyl]-9-[4-(4-carboxyphenyloxy)phenylmethyl]-1,4,9-triazaspiro[5.5]undecane hydrochloride have safety as drug substance, and have possibility to supply at large scale. And the crystal have an antagonistic activity against the interaction between chemokine and chemokine receptor, therefore, it is ...

03/09/06 - 20060052406 - Methods and compositions for treatment of central and peripheral nervous system disorders and novel compounds useful therefor
There are provided methods for the treatment of diseases involving dysfunction of the peripheral and central nervous system comprising administering one or more spiro compounds. Also provided are pharmaceutical compositions useful in such methods, compounds for use in the preparation of such pharmaceutical compositions, processes for preparing compounds useful in ...

02/09/06 - 20060030577 - Hydroxy alkyl substituted 1,3,8-triazaspiro[4.5]decan-4-one derivatives useful for the treatment of orl-1 receptor mediated disorders
wherein all variables are as defined herein, useful in the treatment of disorders and conditions mediated by the ORL-1 G-protein coupled receptor. More particularly, the compounds of the present invention are useful in the treatment of disorders and conditions such as anxiety, depression, panic, dementia, mania, bipolar disorder, substance abuse, ...

01/26/06 - 20060019978 - Spirocyclic compounds useful as modulators of nuclear hormone receptor function
Spirocyclic compounds, methods of using such spirocyclic compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds are disclosed. ...

01/26/06 - 20060019977 - Spiroheterocyclic derivative compounds and drugs comprising the compound as the active ingredient
(wherein R1 is H, alkyl, alkenyl, etc.; R2 is keto, thioketo, alkyl, etc.; R3 is alkyl, alkenyl, etc.; AB ring is fused bi-cyclic ring or spiro ring), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as an active ingredient. The compounds of the formula ...

01/19/06 - 20060014770 - Therapeutic compound and treatments
Compositions and uses associated with the MT477 family of compounds are disclosed. Particular structural features and properties of the compounds are described in detail. Uses include administering an MT477 family member to a patient for therapeutic purposes. Compositions include chemicals belonging to the MT477 family and pharmaceuticals that contain such ...

01/19/06 - 20060014769 - Spirohydantoin compounds and methods for the modulation of chemokine receptor activity
wherein R1, R2, R3 and R4 are as defined herein, and pharmaceutically acceptable salts, hydrates and solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity. ...

01/05/06 - 20060004034 - Spirocyclic cyclohexane compounds
a method for producing them, pharmaceutical compositions containing them, and methods of using them. ...

12/29/05 - 20050288317 - 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 ...

12/29/05 - 20050288316 - Beta-carbolines as growth hormone secretagogue receptor (ghsr) antagonists
wherein R3-R8, X, and Y 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 GHSR receptor-related disorder. Examples of such disorders are obesity and related disorders such as diabetes type II, ...

12/15/05 - 20050277659 - Alpha aryl or heteroaryl methyl beta piperidino propanoic acid compounds as orl1-receptor antagonists
These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc. ...

11/24/05 - 20050261328 - Pharmaceutical composition comprising beta-3-adrenoceptor-agonists and antimuscarinic agents
A pharmaceutical composition useful in the treatment of functional bladder disorders comprising an antimuscarinic agent and a beta-3-adrenoceptor agonist is described. ...

11/24/05 - 20050261327 - 2-(bicyclo)alkylamino-derivatives as mediatores of chronic pain and inflammation
Compounds disclosed herein are bradykinin B1 antagonist compounds useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. ...

11/24/05 - 20050261326 - Metabolites of ecteinascidin 743
The purification and structure elucidation of several products of the metabolism of Et 743 by human cytochrome CYP3A4 have been accomplished. These compounds are abbreviated herein as “ETM” followed by a numeric value which represents the approximate molecular weight. Three compounds have been identified to date, namely ETM 305, ETM ...

11/24/05 - 20050261325 - Gamma-aminoamide modulators of chemokine receptor activity
The present invention is directed to compounds of the formula (1), wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, W, X, and n are defined herein, which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor ...

11/17/05 - 20050256146 - Alpha-7 nicotinic receptor agonists and stains in combination
Combinations of α7-nAChR agonists and statins, pharmaceutical compositions containing the same and methods of using the same useful for treatment or prophylaxis of neurological degenerative diseases. ...

11/10/05 - 20050250802 - Novel substituted amines of spirofuropyridines useful in therapy
wherein A, R and R1 are as defined in the specification. ...

11/10/05 - 20050250801 - Method of treating cancer with azaspirane compositions
R3 and R4 independently represent a hydrogen atom or a saturated or unsaturated, substituted or unsubstituted, branched or unbranched or cyclic, hydrocarbyl radical. ...

11/10/05 - 20050250800 - Conformationally constrained compounds as pharmaceutical agents
are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed. ...

10/20/05 - 20050234084 - Triazaspiro compounds useful for treating or preventing pain
Triazaspiro Compounds, compositions comprising a Triazaspiro Compound, methods for treating or preventing pain in an animal comprising administering to an animal in need thereof an effective amount of a Triazaspiro Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor ...

10/13/05 - 20050228006 - Process and intermediates for obtaining 1-(1h-benzimidazol-2-yl)-4-(2-aminopyrimidine)piperidine derivatives
A method is provided for obtaining derivatives of 1-(1H-Benzimidazole-2-il)-4-(2-aminopyrimidine)piperidine (IV), wherein R1 represents hydrogen or 4-halobenzul and R5 represents optionally-substituted hydrogen, alkyl or benzyl. The method includes the conversion of a 1-[1-(R1)-1-(1H-Benzimidazole-2-il)-4-(R2)(R3)-piperidine (I), wherein R2 or R3 represents optionally-protected hydroxyl, or R2 and R3 represent, independently of each other, optionally-substituted ...

09/29/05 - 20050215579 - Fredericamycin derivatives as medicaments for treating tumours
The invention relates to novel fredericamycin derivatives of general formula (Ia) or (Ib), to medicaments containing said derivatives or the salts of the same, and to the use of said fredericamycin derivatives for treating diseases, especially tumour diseases. ...

09/22/05 - 20050209262 - Process for producing optically active sulfoxide
A process for preparing an optically active cyclic sulfoxide, by reacting a cyclic thioether with cumene hydroperoxide or isopropylcumyl hydroperoxide in the presence of alcohol, water or a mixture of water and alcohol and in the presence of a complex of an optically active tartaric acid diester and a titanium ...

09/01/05 - 20050192307 - Benzimidazolone compounds
wherein A, B, C, M1-M4, R, R1, R2 and n are as described herein. ...

08/25/05 - 20050187238 - Benzofuran derivatives, their production and use
wherein R4 indicates (1) an aliphatic hydrocarbon group, which may be substituted with an aromatic group, or (2) an acyl group containing an aromatic group, R5 is hydrogen atom, a C1-6 alkyl, or an acyl group, provided that, when W is Wa, R3 is hydrogen atom, a hydrocarbon group or ...

08/25/05 - 20050187237 - Therapeutic compounds and uses thereof
The compounds can be used, for example, to modulate growth hormone secretagogue receptor (GHS-R). In some instances, the compounds can be used to treat obesity. ...

08/11/05 - 20050176745 - Furyl compounds
and pharmaceutically-acceptable salts thereof, wherein Ar and R are as defined in the specification, compositions containing such compounds and methods of using such compounds and compositions in therapy. ...

08/04/05 - 20050171135 - 1'-[4-[1-(4-fluorophenyl)-1h-indole-3-y1]-spiro[isobenzofuran-1(3h), 4'-piperidine]hydrohalogenides
The present invention relates to a hydrohalogenide of 1′-[4-[1-(4-fluorophenyl)-1H-indole-3-yl]-1-butyl]-spiro[isobenzofuran-1(3H),4′-piperidine], pharmaceutical compositions containing the acid addition salts and the use thereof for the treatment of psychic and neurological disorders. ...

07/28/05 - 20050165037 - Process for producing cyclic thioether and synthetic intermediate thereof
wherein G1 is an alkylene group, R1 is a thiol protecting group, R2 is hydrogen or an amino protecting group, and Ar is an aryl group or a 5- to 7-membered heteroaryl group. ...

07/21/05 - 20050159438 - Spirocyclic heterocyclic derivatives and methods of their use
Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions. ...

07/14/05 - 20050154001 - Diaza-spiropiperidine derivatives
n is 0, 1 or 2; or a pharmaceutically active salt thereof. The compounds of the invention may be used in the treatment of neurological and neuropsychiatric disorders. ...

07/14/05 - 20050154000 - Diaza-spiropiperidine derivatives
The compounds of formula I may be used in the treatment of neurological and neuropsychiatric disorders. ...

07/14/05 - 20050153999 - Pharmaceutical compositions
Disclosed are pharmaceutical compositions comprising NK1 Antagonists. ...

07/14/05 - 20050153998 - Tetrahydroisoquinoline or isochroman compounds
or its a pharmaceutically acceptable ester or amide of such compound, or a pharmaceutically acceptable salt thereof, wherein X1 is NH; R1, R2, R4 through R6 and R7 through R11 are all hydrogen; R3 is hydroxy; X2 and X3 are methylene; X4 is a bond; and X5 is a carbon ...

07/14/05 - 20050153997 - Fredericamycin derivatives
The invention relates to novel Fredericamycin derivatives, to medicaments containing these derivatives or salts thereof, and to the use of Fredericamycin derivatives for treating diseases, particularly tumor diseases. ...

06/30/05 - 20050143407 - Process for porducing quinolonecarboxylic acid derivative
Through a production process according to the following reaction scheme, compounds (2) which are useful for antibacterial agents can be provided at low cost and high yield. ...

06/23/05 - 20050137219 - Spirocyclic quinuclidinic ether derivatives
wherein n1 is 0, 1, or 2; n2 is 0, 1, or 2; X is a bond, O, S, or NR1; and Ar1 is a 5-membered aromatic ring, 6-membered aromatic ring, or a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 ...

06/23/05 - 20050137218 - Treatment of pancreatitis using alpha 7 receptor-binding cholinergic agonists
A method of treating a patient suffering from pancreatitis comprising treating said patient with a therapeutically effective amount of a cholinergic agonist selective for an α7 nicotinic receptor in an amount sufficient to decrease the amount of the proinflammatory cytokine that is released from a macrophage wherein said condition is ...

06/23/05 - 20050137217 - Spirocyclic quinuclidinic ether derivatives
wherein n1 is 0, 1, or 2; n2 is 0, 1, or 2; X is a bond, O, S, or NR1; and Ar1 is a 5-membered aromatic ring, 6-membered aromatic ring, or a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 ...

06/16/05 - 20050131004 - Hydronopol derivatives as agonists on human orl1 receptors
wherein the symbols have the meanings as given in the description. ...

06/16/05 - 20050131003 - Heterocyclic compounds
and pharmaceutically-acceptable salts thereof, wherein Ar and R are as defined in the specification, compositions containing such compounds and the use of such compounds and compositions for use in therapy. ...

06/02/05 - 20050119293 - Oxadiazole derivatives for inhibition of gamma secretase
Compounds of formula 1: wherein X represents a 5-(R-substituted)-1,2,4-oxadiazole-3-yl moiety are inhibitors of gamma-secretase, and hence useful for treating Alzheimer's disease. ...

06/02/05 - 20050119292 - 3-cyclyl-5-(nitrogen-containing 5-membered ring)methyl-oxazolidinone derivatives and their use as antibacterial agents
wherein m is 0, 1 or 2; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described. ...



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