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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 ...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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7208487 |
Compounds, compositions and methods
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
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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...
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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...
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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,...
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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...
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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:...
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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
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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...
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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...
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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...
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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,...
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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...
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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...
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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...
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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;...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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,...
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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...
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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...
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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.
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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...
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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...
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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...
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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...
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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.
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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...
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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...
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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...
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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...
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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...
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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...
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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....
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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 ...
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