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6740663 |
Mono- and di-fluorinated benzothiepine compounds as inhibitors of apical sodium co-dependent bile acid transport (ASBT) and taurocholate uptake
Mono-flourinated and di-fluorinated benzothiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same...
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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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6723332 |
Oxomidazopyridine-carboxamides
Disclosed are compounds of the formula: wherein: A, B, C, E, F, and G are substituents as defined herein, which compounds bind to the benzodiazepine site of GABA A receptors and are therefore...
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6723734 |
Salt of naphthyridine carboxylic acid derivative
7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropy
l-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation,...
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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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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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6716830 |
Ophthalmic antibiotic compositions containing moxifloxacin
Ophthalmic, otic and nasal compositions containing a new class of antibiotics (e.g., moxifloxacin) are disclosed. The compositions preferably also contain one or more anti-inflammatory agents. The...
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6716852 |
Amino acid derivatives and use thereof as NEP, ACE and ECE inhibitors
The invention relates to compounds of formula (I): wherein 0≦n≦3, 0≦m≦6, R 3 and R 4 together form phenyl, B represents heteroaryl, R 1 and R 2 represent hydrogen or groups as...
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6706736 |
Antidepressant azaheterocyclylmethyl derivatives of oxaheterocycle-fused-&lsqb 1,4&rsqb -benzodioxans
Compounds of the formula useful for the treatment of depression such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction,...
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6703404 |
Tert -butyl-(7-methyl-imidazol &lsqb 1,2-a&rsqb pyridin-3-yl)-amine derivatives
A Tert.-butyl-(7-methyl-imidazo[1,2-a]pyridin-3-yl)-amine derivatives of Formula I: wherein the pharmaceutically acceptable salts, methods of making and method of use, in particular for the...
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6703403 |
Method for improving pharmacokinetics
A method is disclosed for improving the pharmacokinetics of a drug which is metabolized by cytochrome P450 monooxygenase.
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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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6696463 |
3-heteroarylidenyl-2-azaindolinones active as protein tyrosine kinase inhibitors
The invention relates to 3-heteroarylidenyl-2-azaindolinone compounds of the formula: wherein, A is selected from the group consisting of nitrogen, oxygen and sulfur; only one of B, D, E, F or G...
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6696469 |
Cyclobutenedione compounds
Compounds of formula (I): wherein: X represents a heterocycle bonded to the remainder of the molecule by a nitrogen atom of the heterocycle, or an —NR 2 R 3 group wherein R 2 represents...
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6696437 |
Heterocyclically substituted benzimidazoles, the production and application thereof
The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.
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6693101 |
αv integrin receptor antagonists
The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present...
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6693114 |
4-oxo-1,4-dihydro&lsqb 1,8&rsqb naphthyridine-3-carboxamides as antiviral agents
A compound of formula III: or a pharmaceutically acceptable salt thereof wherein, the variables are as in the specification is provided. The compounds are particularly effective in the treatment...
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6689787 |
Method of using an integrin antagonist and radiation therapy as combination therapy in the treatment of neoplasia
The present invention provides methods to treat neoplasia disorders in a mammal using a combination of radiation and an integrin antagonist.
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6689772 |
3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
This invention provides compounds of Formula (I), having the structure where T, Z, X, A, R 1 , R 2a , R 2b , R 2c , R 3 , R 4 , and n are defined herein, or a pharmaceutically acceptable salt...
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6689788 |
Method and composition for treatment of inflammatory bowel disease
A composition in unit dosage form for the inhibition, prevention or treatment of inflammatory bowel disease comprising an effective amount of a compound having the formula: and a...
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6677354 |
Piperdines for use as orexin receptor antagonists
Disclosed are compounds of formula (I): wherein: Y represents a group (CH 2 ) n , wherein n represents 0, 1 or 2; R 1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3...
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6677351 |
1-biaryl-1,8-naphthyridin-4-one phosphodiesterase-4 inhibitors
Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterrase 4 inhibitors useful in the treatment of asthma and inflammation.
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6673811 |
1H-pyrrolo &lsqb 3,2-b&rsqb pyridine-3-carboxylic acid amines as GABAA receptor ligands
Disclosed are 1H-Pyrrolo[3,2-b]pyridine-3-carboxylic acid amides that bind to the benzodiazepine site of GABA A receptors. Such compounds can be used to modulate ligand binding to GABA A ...
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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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6673797 |
Heterocyclic indole derivatives and mono- or diazaindole derivatives
There is provided a compound represented by the general formula (1): wherein Het represents an optionally substituted heterocyclic group; A 1 and A 2 each independently represent —CH═,...
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6667322 |
Antidepressant chroman and chromene derivatives of 3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole
Compounds of the formula useful for the treatment of depression and other diseases such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder,...
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6664268 |
Crystal modification B of 8-cyano-1-cyclopropyl-7-(1S,6S-2, 8-diazabicyclo&lsqb 4.3.0&rsqb nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
The present invention relates to a defined crystal modification of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-
8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the...
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6660737 |
Medicinal uses of hydrazones
Compounds having a structure according to Formula (I): are effective in a method of increasing erythropoietin and vascularization of tissue in a subject in need thereof.
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6656950 |
Antidepressant azaheterocyclylmethyl derivatives of 1,4-dioxino&lsqb 2,3-b&rsqb pyridine
Compounds of the formula useful for the treatment of depression, obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction, eating...
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6653309 |
Inhibitors of IMPDH enzyme technical field of the invention
The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions...
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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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6642250 |
1,8-naphthyridin-2(1H)-one derivatives
The purpose is to provide selective PDE IV inhibitors which have a potent anti-asthmatic profile with excellent safety. A compound of the formula (1): wherein: A is an unsubstituted or...
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6642251 |
Geometrically restricted 2-indolinone derivatives as modulators of protein kinase activity
The present invention relates to novel geometrically restricted 2-indolinones and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected...
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6638933 |
Bicyclic imidazo-3-yl-amine derivatives
Substituted bicyclic imidazo-3-yl-amines and medicaments comprising these compounds, useful, inter alia, as analgesics.
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6638535 |
Modified release formulations containing a hypnotic agent
Hypnotic pharmaceutical compositions are made from pellets and exhibit a modified release. Zolpidem or a pharmaceutically acceptable salt thereof is a typical hypnotic. The pellets are preferably...
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6635652 |
Azaindolizinone derivatives and cerebral function improvers containing the same as the active ingredient
Azaindolizinon derivatives or pharmaceutically acceptable salts thereof represented by the formula I: wherein R 1 represents hydrogen atom, halogen atom or C 1 -C 6 alkyl, R 2 represents...
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6630485 |
p38 map kinase inhibitors
The present invention relates to compounds of Formula (I) that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these...
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6627639 |
Uses for indoletetrahydropyridine derivatives of 2,3-dihydro-7H-&lsqb 1,4&rsqb dioxino-&lsqb 2,3-e&rsqb indole
Compounds of the formula are useful in the treatment of central nervous system disorders including depression, obsessive compulsive disorder, panic attacks, generalized anxiety disorder, sexual...
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6624162 |
Imidazopyridine compounds as 5-HT4 receptor modulators
This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein R 1 is hydrogen, halo or alkyl; R 2 and R 3 are independently hydrogen, alkyl,...
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6624181 |
Synergistic combination
The invention relates to the combined administration of PDE inhibitors and β 2 adrenoceptor agonists for the treatment of respiratory tract disorders.
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6617334 |
Antidepressant azaheterocyclylmethyl derivatives of 7,8-dihydro-1,6,9-trioxa-3-aza-cyclopenta&lsqb a&rsqb naphthalene
Compounds of the formula: useful for the treatment of depression and other diseases such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder,...
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6613775 |
Imidazo&lsqb 1,2-a&rsqb pyridine compounds
The present invention relates to novel compounds, and therapeutically acceptable salts thereof of the formula (I), which inhibit exogenously or endogenously stimulated gastric acid secretion and...
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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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6610701 |
Thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R 3 is hydrogen or halogen,...
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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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6605614 |
&lsqb 1,8&rsqb naphthyridine derivatives having antiviral activity
The present invention is concerned with novel [1,8] naphthyridine derivatives useful for the inhibition of the hepatitis virus, more specifically the hepatitis C virus.
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6602882 |
Quinoline derivatives and their use as antibacterial agents
Piperidine derivatives and pharmaceutical derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
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