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7407950 N-(heteroaryl)-1H-indole-2-carboxamide derivatives and their use as vanilloid TRPV1 receptor ligands  
The invention concerns compounds of general formula (I), wherein n, X 1 , X 2 , X 3 , X 4 , Z 1 , Z 2 , Z 3 , Z 4 , Z 5 and W are as defined herein. Said compounds are ligands of the TRPV 1 ...
7390799 Apoptosis promoters  
Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than...
7390798 Carboxamide spirolactam CGRP receptor antagonists  
The present invention is directed to compounds of Formula I: I (where variables A 1 , A 2 , B, J, K, m, n, R 4 , R 5a , R 5b and R 5c are as defined herein) useful as antagonists of CGRP...
7378413 2-amino-3-(alkyl)-pyrimidone derivatives  
A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C 1-6 alkyl group which may be substituted by a C 6,10 aryl group; R2...
7351700 Aminomethylpyrimidines as allosteric enhancers of the GABAB receptors  
The present invention relates to compounds of formula wherein X is —S— or —NH—; R 3 /R 4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7...
7329652 Diaminotriazole compounds useful as protein kinase inhibitors  
The present invention relates to inhibitors of protein kinases, particularly to inhibitors of JAK2 and JAK3. The invention also provides pharmaceutical compositions comprising the compounds of the...
7244722 Amino-substituted 1H-pyrazin-2-ones and 1H-quinoxalin-2-ones  
Compounds of the general formula (I): wherein m, n, R 1 , R 2 , R 3 and R 4 are as described in the specification. Further included are pharmaceutical compositions comprising the...
7241745 Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives  
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds...
7229983 4-substituted or unsubstituted-7-hydro-1,4-thiazepine-7-[bicyclic or tricyclic heteroaryl] substituted-3,6-dicarboxylic acid derivatives as β-lactamase inhibitors  
The present invention relates to novel, low molecular weight broad spectrum compounds in particular to a class of 4-substituted or unsubstituted-7-hydro-1,4-thiazepine-7-[bicyclic or tricyclic...
7223749 Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them  
The present invention relates to bicyclic heterocycles of general formula wherein R a , R b , R c , R d , R e and X are defined as in claim 1 , the tautomers, the stereoisomers, the mixtures...
7214701 Active substance combinations having insecticidal and acaricdal properties  
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) in which W, X, Y, Z, A, B, D and G...
7208487 Compounds, compositions and methods  
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
7119084 Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them  
The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the...
RE39112 Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes  
The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine...
7030110 Cyclic oxyguanidine pyrazinones as protease inhibitors  
Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R 3 , R 4 , R 5 , W, and A are as set forth in the specification, as well as hydrates,...
7030150 Benzimidazole compounds and antiviral uses thereof  
The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion...
6960575 Thiazine derivatives  
A compound having 3-oxo-3, 4-dihydro-2H-1, 4-thiazine 4-tetrahydropyrazine as a main skeleton. The compound is a chymase inhibitor and is represented by the following formula [I] and salts thereof:...
6919359 Azabicyclic-substituted-heteroaryl compounds for the treatment of disease  
The invention provides compounds of Formula I: Azabicyclo-N(R 1 )—C(═X)—W Formula I
6906057 Methods for modulating FXR receptor activity  
Methods for modulating the activity of the mammalian FXR receptor. The methods include methods of treating a hyper- or hypocholesterolemic mammal comprising contacting the mammal with synthetic...
6861419 Substituted 1, 4-thiazepine and analogs as activators of caspases and inducers of apoptosis and the use thereof  
The present invention is directed to substituted 1,4-thiazepine and analogs thereof, represented by the general Formula I: wherein the dashed lines, A 1 , A 2 , A 3 , X 1 and R 1 are defined...
6844335 2-amino-3-(alkyl)-pyrimidone derivatives as GSK3.β.inhibitors  
A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C 1-6 alkyl group which may be substituted by a C 6,10 aryl group; R2...
6743817 Substituted fused pyrroleimines and pyrazoleimines  
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R 1 and R 2 are defined herein. These compounds are highly selective agonists,...
6713472 Thiazine or pyrazine derivatives  
A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R 6 —(A 2 ) n —N, R 1 and R 2 are H, alkyl, cycloalkyl or aryl, R...
6656932 Benzo thiadiazine matrix metalloproteinase inhibitors  
Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R 2 is hydrogen or alkyl; R 1 and R 3 include hydrogen, alkyl, and...
6635637 Cyclic oxyguanidine protease inhibitors  
Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R 1 , R 3 -R 6 , R 21 -R 26 , L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or...
6620806 Methods and kits for improving vascular health  
The present invention provides methods and kits for improving or maintaining vascular health, including preventing myocardial infarction or stroke; maintaining or improving vascular reactivity;...
6617329 Aminoquinazolines and their use as medicaments  
Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the...
6610697 Substituted 2-aryl-3-(heteroaryl)-imidazo&lsqb 1,2-a&rsqb pyrimidines, and related pharmaceutical compositions and methods  
This invention relates to a series of imidazopyrimidines of Formula I, and pharmaceutical compositions containing them. The compounds of the invention inhibit the production of a number of...
6608070 2,3-substituted indole compounds as anti-inflammatory and analgesic agents  
This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the...
6608048 Tricyclic protein kinase inhibitors  
This invention provides compounds of Formula (I), where A″, Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the...
6599926 Heteroaryl-phenyl substituted factor Xa inhibitors  
The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of...
6566362 Benzo&lsqb f&rsqb naphthyridine derivatives, their preparation and compositions containing them  
Benzo[f]naphthyridine derivatives of formula (I): benzo[f]naphthyridine derivatives and benzo[f]naphthyridine esters of formula (IVa): aminoquinoline derivatives of formula (X): processes for...
6559155 Pyrimidinone derivatives for the treatment of atherosclerosis  
Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA 2 and thereof use in treating inter alia atherosclerosis, in which: R 1 is COOH or a salt thereof, COOR 10 , CONR 11 R 12 , CN or...
6451790 Azadioxacycloalkenes and their use for combating harmful fungi and animal pests  
Compounds of formula I wherein W is optionally substituted alkylene; Y is N or CR a ; R a is hydrogen, halogen or alkyl; R 1 n represents hydrogen or 1 to 4 substituents; R 2 is hydrogen,...
6436943 Use of dihydropyrimidines as medicaments, and novel substances  
The invention relates to dihydropyrimidines of the general formula and to the use of dihydropyrimidines as medicaments for the treatment and prophylaxis of hepatitis B. The invention further...
6362176 Compositions, methods and kits for treating rheumatoid arthritis  
Disclosed are methods of treating rheumatoid arthritis by coadministering synergistic effective amounts of pentostatin and methotrexate to a host in need thereof, and kits and compositions that...
6358978 Substituted benzimidazoles  
Compounds of formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NFκB is involved.
6335325 Acylated 4-aminopyridine derivatives as pesticides and fungicides  
The present application relates to novel acylated 4-amino-pyridine derivatives in which R 1 , R 2 , R 3 , R 4 , A, X 1 , X 2 , m and n are as defined in the description, to process for their...
6294542 Pyrimidinone compounds, pharmaceutical compositions containing the compounds and the process for preparing the same  
The present invention relates to a novel pyrimidinone compounds and the pharmaceutical acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, thereby, being...
6262046 Azetidinylpropylpiperidine derivatives, intermediates and use as tachykinin antagonists  
Compounds of the formula (I): ##STR1## where X 1 , A, Ar 1 , X and R are as defined in the specification, and pharmaceutically-acceptable salts thereof, are new, and are useful as tachykinin...
6239126 Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives  
Compounds of the formula ##STR1## are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep...
6191125 Small molecule pipecolic acid derivative hair growth compositions and uses  
This invention relates to pharmaceutical compositions and methods for treating alopecia and promoting hair growth using pipecolic acid derivatives.
6107291 Azepine or larger medium ring derivatives and methods of use  
Selected novel azepine and larger medium ring compounds are effective for prophylaxis and treatment of inflammation, tissue degradation and related diseases. The invention encompasses novel...
6096736 Benzazepine derivatives with vasopressin agonistic activity  
Novel benzazepine derivative of the formula [1]: ##STR1## wherein R 1 is H or halogen, A is lower alkylene, R 2 and R 3 are the same or different and each H, lower alkoxy, lower alkyl having...
6083949 Substituted imidazoles having anti-cancer and cytokine inhibitory activity  
Compounds represented by formula I: ##STR1## are disclosed. AR represents an aromatic group containing 6-10 atoms; and ##STR2## represents a 4 to 10 membered non-aromatic heterocycle containing at...
6080758 Benzenesulfonamide derivatives as bradykinin antagonists  
The present invention relates to compounds selected from the group consisting of the compounds of formula (I): ##STR1## X is a halogen atom, A is --CH 2 --, --CH(OH)--, --CH(NH--COCH 3 )-- or S, R...
6075022 Methods and compositions for controlling biofouling using thiourea compounds  
The present invention relates to a method to inhibit bacteria from adhering to a submergible surface. The method contacts the submergible surface with an effective amount of at least one thiourea...
6048869 Tricyclic compounds  
The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, ester, or stereoisomer thereof, which are inhibitors of...
6034102 Atherosclerosis treatment  
A method of treating atherosclerosis, independent of lipid lowering, in mammals, including humans, in need of treatment by inhibiting progression of an atherogenic lesion or by stabilizing plaque....
6034082 5-azabicyclo(3.1.0)hexylalkyl-2-piperiodones and --glutarimides as neurokinin receptor antagonists  
Compounds of formula (I) ##STR1## and salts thereof, wherein: R 1 is C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkyl(C 1 -C 4 )alky aryl or aryl(C 1 -C 4 )alkyl; wherein the C 1 ...
Matches 1 - 50 out of 232 1 2 3 4 5 >