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6875765 |
Arylsulfonamide ethers, and methods of use thereof
The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1β converting enzyme and other cysteine proteases in the ICE family are...
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6872730 |
Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists
The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (αv) integrins, for example α v β 3 and α v β 5 integrins, their...
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6867208 |
Vitronectin receptor antagonists, their preparation and their use
The present invention relates to compounds of the formula I
A—B—D—E—F—G (I)
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6867202 |
Treatment of insulin resistance
This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I,
where the variables are defined in...
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6858613 |
Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease
The invention provides compounds of Formula I:
These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful...
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6855723 |
Methods of modulating serine/threonine protein kinase function with azabenzimidazole-based compounds
The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with azabenzimidazole-based compounds. The methods incorporate cells that...
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6852739 |
Methods using proton pump inhibitors and nitric oxide donors
The present invention describes novel nitrosated and/or nitrosylated proton pump inhibitor compounds, and novel compositions comprising at least one proton pump inhibitor compound that is...
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6852722 |
Compositions and methods for stimulating gastrointestinal mobility
The present invention is directed to methods for stimulating the motility of the gastrointestinal system in a patient which comprises administering a growth hormone secretagogue, a prodrug thereof...
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6849620 |
N-(azabicyclo moieties)-substituted hetero-bicyclic aromatic compounds for the treatment of disease
The invention provides compounds of Formula I:
wherein Azabicyclo is
W 0 is a bicyclic moiety and is
These compounds may be in the form of pharmaceutical salts or...
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6844354 |
Agent for prophylaxis and treatment of interstitial pneumonia and pulmonary fibrosis
An agent for the prophylaxis and treatment of interstitial pneumonia and pulmonary fibrosis, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the...
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6828330 |
Quinuclidine-substituted hetero-bicyclic aromatic compounds for the treatment of disease
The invention provides compounds of Formula I: wherein W 0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric...
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6818650 |
1H-imidazo dimers
1H-imidazo dimer compounds are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment...
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6803374 |
Compounds useful for treating hepatitis C virus
A series of compounds of Formula I are disclosed which are useful in treating viral hepatitus C.
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6797717 |
Anilide compounds and drugs containing the same
The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula: ...
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6750225 |
1,4,5,6-tetrahydropyrazolo-&lsqb 3,4,-c&rsqb -pyridin-7-ones useful as factor Xa inhibitors
The present application describes 1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-ones of the following formula or pharmaceutically acceptable salt forms thereof: wherein ring R b is 3-amido or...
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6743800 |
Naphthyridine derivatives, processes for their preparation, their use and pharmaceutical compositions comprising them
The present invention relates to compounds of formula (1), in which H, G, Z, X, Y, r, s and t have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs....
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6740654 |
Squaric acid derivatives
Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L 2 is a covalent bond or an atom or group —O—,...
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6740649 |
Cyclic hydroxamic acids as inhibitors of matrix metalloproteinases and/or TNF- α converting enzyme (TACE)
The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from...
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6737428 |
BIS hydrochloride monohydrate salt of RSV fusion inhibitor
The novel crystalline bis hydrochloride monohydrate salt having the formula and pharmaceutical dosage forms thereof is provided having use in the treatment of respiratory syncytial viral infection.
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6723735 |
Imidazo-pyridine derivatives as ligands for GABA receptors
The present invention is directed to 3-phenylimidazol[4,5-b]pyridine derivatives, that are selective ligands for GABA A receptors. These compounds are useful in the treatment and prevention of...
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6720341 |
Preventives/remedies for kidney diseases
A compound having a Rho kinase inhibitory activity, such as (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)-cyclohexan
e, has a renal interstitial fibrosis inhibitory action in renal interstitial...
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6720334 |
Urea substituted imidazopyridines
Imidazopyridine compounds that contain urea or thiourea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the...
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6716841 |
Nitrogen containing heterobicycles as factor Xa inhibitors
This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical...
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6716853 |
Cyclic N-substituted alpha-imino carboxylic acids for selective inhibition of collogenase
The invention is related to compounds of formula I to pharmaceutical compositions comprising such compounds, to processes for the preparation of such compounds, and to methods of prevention and...
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6710055 |
Disubstituted bicyclic heterocycles, the preparation thereof, and their use as pharmaceutical compositions
Disubstituted bicyclic heterocycles of general formula I R a —A—Het—B—Ar—E (I). Compounds of general formula I, wherein E is an R b NH—C(═NH)— group, have valuable pharmacological...
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6706728 |
Systems and methods for treating a mucosal surface
A system for treating a condition associated with a mucosal surface, the system comprising an immune response modifier (IRM) compound chosen from imidazoquinoline amines, imidazopyridine amines,...
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6706730 |
1,4,5,6-tetrahydropyrazolo-&lsqb 3,4-c&rsqb -pyridin-7-ones as factor Xa inhibitors
The present application describes 1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-ones of Formula I or pharmaceutically acceptable salt forms thereof: wherein ring R is 3-amido or 4-methoxy, R 1 ...
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6696459 |
Steroid receptor modulator compounds and methods
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds,...
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6696464 |
Triazolo-pyridines anti-inflammatory compounds
The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from...
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6696465 |
Sulfonamido substituted imidazopyridines
Imidazopyridine compounds that contain sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the...
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6693116 |
Adenosine receptor ligands
The present application relates to compounds of the formula wherein R 1 is hydrogen, halogen or lower alkoxy; R 2 is hydrogen or is —C(O)-lower alkyl or —C(O)-phenyl, wherein the phenyl...
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6689790 |
Substituted triazolopyridine compounds
A compound of formula wherein R 1 is —NR′R″, wherein R′ and R″ are independently selected from the group consisting of lower alkyl, —(CH 2 ) n —C(O)NR a R b , —(CH 2 ) n...
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6686359 |
Growth hormone secretagogues
This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the specification, which are growth hormone...
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6673812 |
Preventives/remedies for glaucoma
An agent for the prophylaxis and treatment of glaucoma, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the prophylaxis and treatment of glaucoma, which...
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6673810 |
Imidazo-heterobicycles as factor Xa inhibitors
The present application describes imidazo-heterobicycles of formulas I and III: or pharmaceutically acceptable salt or prodrug forms thereof. Compounds of the present invention are useful as...
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6653320 |
Imidazopyridine derivatives
The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel...
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6649625 |
Agent for prophylaxis and treatment of glaucoma
An agent for the prophylaxis and treatment of glaucoma, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the prophylaxis and treatment of glaucoma, which...
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6642230 |
Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders
Corticotropin releasing factor (CRF) antagonists of formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress...
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6630487 |
Treatment of insulin resistance with growth hormone secretagogues
This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, where the variables are defined in...
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6627645 |
Muscarinic agonists
Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial...
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6627646 |
Norastemizole polymorphs
Polymorphic crystalline forms of the antihistaminic drug norasternizole are disclosed. Processes for the production of the preferred polymorph are also disclosed.
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6613776 |
Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: wherein Z 1 is N, CR a , or CH, and Z 2 is N or CH, provided...
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6613778 |
Imidazopyridine derivatives as phosphodiesterase VII inhibitors
Compounds of the formula I in which R 1 denotes CONR 4 R 5 , R 2 denotes H or A, R 4 and R 5 , independently of one another, each denote H or A 1 , R 3 denotes Hal, Hal denotes F, Cl, Br or...
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6613777 |
CRF antagonistic pyrazolo&lsqb 4,3-b&rsqb pyridines
This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R 1 is C 1-6 alkyl, NR 5 R 6 , OR 6 or SR...
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6610692 |
Thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY...
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6593339 |
Use of compounds as antibacterial agents
The present invention discloses a new use of NO-releasing NSAIDs, especially NO-releasing NSAIDs of the formula I, or a pharmaceutically acceptable salt or enantiomer thereof, for the manufacture...
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6586478 |
Methods and compositions for improving sleep
Methods and compositions for improving sleep in individuals with sleep disorders or other conditions which interfere with normal sleep via administration of a NO-mimetic are provided.
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6579894 |
Prolines as antimicrobial agents
Transfer ribonucleic acid (tRNA) synthetase inhibitors, salts, and pharmaceutically acceptable compositions thereof of the general formula: wherein Ar is aryl and heteroaryl; L is —C(O)N(Q)CH...
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6559152 |
6-substituted pyrazolo&lsqb 3,4-d&rsqb pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of...
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6559174 |
N-arylsulfonyl aryl aza-bicyclic derivatives as potent cell adhesion inhibitors
Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds...
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