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7342115 |
3-substituted-6-aryl pyridines
3-substituted-6-aryl pyridines of Formula I are provided:
wherein R 1 , R 2 , R 3 , R 8 , R 9 , A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of...
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7320993 |
Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents
The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or...
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7307092 |
Compounds Capable of Activating Cholinergic Receptors
Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine,...
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7288559 |
Carboxamide spirohydantoin CGRP receptor antagonists
The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache,...
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7273877 |
5-substituted-4-[(substituted phenyl) amino]-2-pyridone derivatives
The present invention relates to 5-substituted-4-(substituted)phenylamino-2-pyridone derivatives, pharmaceutical compositions and methods of use thereof.
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7271181 |
Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods...
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7265213 |
Methodology of conjugating chelators to biomolecules
A novel method of conjugating chelators to biomolecules such as proteins is provided. More particularly, the invention provides compositions and methods of using those compositions for the...
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7256295 |
Process for producing 2,3-diamino-6-methoxypyridine
The present invention relates to a novel process for producing 2,3-diamino-6-methxoypyridine. The process comprises neutralizing 2,3-diamino-6-methoxy pyridine dihydrochloride, which, in turn, is...
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7230098 |
Aminoheteroaryl compounds as protein kinase inhibitors
Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided. Preferred compounds of formula 1 have activity as protein...
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7223868 |
Heteroaromatic glucokinase activators
2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides...
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7223778 |
5-substituted-2-arylpyridines
Novel 5-substituted-2-arylpyridine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyridine compounds provided herein are useful in...
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7196198 |
Benzoic acid derivatives, processes for the preparation thereof and pharmaceutical agents comprising the same as active ingredient
An agent comprising the benzoic acid of formula (I)
wherein A, B, R 6 , R 7 are carbocyclic ring, heterocyclic ring, etc.; R 1 is hydroxy etc.; R 2 , R 3 , R 4 are alkyl etc.; R 5 , D, E are...
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7151182 |
Intermediates for N-substituted carbamoyloxyalkyl-azolium derivatives
N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.
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7151112 |
Pharmaceutical uses and synthesis of nicotinamides
This invention is directed to methods of using a compound of the formula
and pharmaceutically acceptable salts thereof, wherein n, X, R 1 and R 2 are disclosed herein, for treating...
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7129246 |
N-adamantlmethyl derivatives and intermediates as pharmaceutical compositions and processes for their preparation
The invention provides compounds of general formula (I) in which m, A, R 1 and Ar have the meanings defined in the specification; a process for, and intermediates used in, their preparation;...
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7129238 |
Mandelic acid derivatives
The invention is concerned with novel mandelic acid derivatives of formula (I)
wherein R 1 to R 10 , X and Y are as defined in the description and in the claims, as well as pharmaceutically...
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7109220 |
Amino substituted pyridinyl methanone compounds useful in treating kinase disorders
The present invention provides amino substituted pyridinyl methanone compounds; pharmaceutical compositions comprising the compounds and methods of synthesis thereof. The compounds, which are...
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7087622 |
Pyridone compounds as inhibitors of bacterial type III protein secreation systems
In accordance with the present invention, compounds that inhibit Type III protein section have been identified, and methods for their use provided. In one aspect of the invention, compounds useful...
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7074813 |
Substituted N′-(arylcarbonyl)-benzhydrazides, N′-(arylcarbonyl)-benzylidene-hydrazides and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted N′-(arylcarbonyl)-benzhydrazides, N′-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II:
...
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7056932 |
Heterocyclyl substituted 1-alkoxy acetic acid amides
The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I)
wherein R 1 to R 6 and A are as defined in the description and in the claims, as...
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7045538 |
Compounds capable of activating cholinergic receptors
The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt...
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7037928 |
Compositions of N-(methylethylaminocarbonyl)-4-(-3-methylphenylamino)-3-pyridylsulfonamide and cyclic oligosaccharides
The invention relates to compositions of N-(1-methylethylaminocarbonyl)-4-(3-methylphenylamino)-3-pyr
idylsul fonamide and cyclic oligosaccharides with increased release, to methods for their...
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7030145 |
Pyridinyl derivatives for the treatment of depression
The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF...
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7029654 |
Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII:
wherein X is O or NR 9 and Het, R 1 , R 7 , R 8 , R 12 —R 15 , R a , R b , R c , Z, and n...
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7015237 |
Pyridine matrix metalloproteinase inhibitors
Selective MMP-13 inhibitors are pyridine derivatives of the formula
or a pharmaceutically acceptable salt thereof,
wherein:
R 1 and R 2 independently are hydrogen, halo, hydroxy, C 1 –C...
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7008962 |
IL-8 receptor antagonists
This invention relates to the novel use of dianilino squarates in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
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6972296 |
Carboxylic acid derivatives that inhibit the binding of integrins to their receptors
A method for the inhibition of the binding of α 4 β 1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding;...
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6958399 |
Compounds capable of activating cholinergic receptors
Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine,...
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6900231 |
Aminopyridyl-substituted phenyl acetamides as protease inhibitors
Phenyl acetamide compounds are described, including compounds of
or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R 3 -R 6 , R 11 , B, Y and W are set forth in the...
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6872690 |
Herbicidal 2-alkynyl-pyri (mi) dines
The invention relates method of combating undesired plant growth at a locus, comprising application to the locus of an effective amount of at least one compound of formula (I):
wherein R...
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6867210 |
Aryl substituted pyrimidines
This invention relates aryl substituted pyridines, pyrimidines, pyrazines and triazines of Formula I:
or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A 1 , A 2 , A 3...
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6846819 |
Fab I inhibitors
Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.
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6833378 |
Corticotropin releasing factor antagonists
Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R 3 , R 4 , R 5 , R 6 , R 16 and R 17 are as defined in the application, and...
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6828441 |
2-pyridylmethylamine derivatives useful as fungicides
Compounds of formula (I) and salts thereof as phytopathogenic fungicides wherein A 1 is substituted 2-pyridyl; A 2 is optionally substituted phenyl; L is —(C═O)—, —SO 2 — or...
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6828276 |
Herbicidally active benzoylcyclohexanediones
There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), C 1 , C 2 , C 3 are cyclic...
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6809109 |
2, 4-disubstituted-pyridine N-oxides useful as HIV reverse transcriptase inhibitors
The present invention relates to 2,4-disubstituted pyridine-N-oxide compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof,...
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6806372 |
Coupler for use in oxidative hair dyeing
Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein X is selected from halogen and R 2 SO 4 ; R 3 is selected from C 1 to C 2 alkyl...
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6794398 |
Preventive/remedies for liver diseases
The invention provides an agent for the prophylaxis and treatment of liver disease and an activation inhibitor of hepatic stellate cells, which contains a compound having a Rho kinase inhibitory...
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6794397 |
Substituted nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted nicotinamides and analogs thereof, represented by Formula V: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Ar′ and Ar are...
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6787562 |
Substituted aryl and heteroaryl compounds as E-type prostaglandin antagonists
Compounds of the formula I; useful for the treatment of pain wherein A, Z, B, R 1 , X and D are as defined in the specification, methods of making such compounds, methods of using such compounds...
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6780874 |
Enamine derivatives
Enamine derivatives of formula (1) are described: wherein R 1 is a group Ar 1 L 2 Ar 2 Alk- in, which Ar 1 is an aromatic or heteroaromatic group, L 2 is a covalent bond or a linker atom or...
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6777432 |
Pharmaceutical uses and synthesis of nicotinamides
A compound of the formula and pharmaceutically acceptable salts thereof, wherein R 1 is selected from (R 3 )C(═O)—N(R 4 )— and (R 3 )(R 4 )N—C(═O)—; R 2 is selected from —OR 5 ...
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6765095 |
2,3-disubstituted pyridine derivative, process for the preparation thereof, pharmaceutical composition containing the same, and intermediate therefor
A compound of the formula (I) wherein A is O, S, CHR 1 or NR 2 , R 1 and R 2 are H, lower alkyl, X 1 and X 2 are H, halogen, nitro, cyano, etc., Y 1 is H, lower alkyl, Z 1 and Z 2 are H,...
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6762178 |
Acetylenic aryl sulfonamide and phosphinic acid amide hydroxamic acid TACE inhibitors
Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple...
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6747048 |
Pyridine-based thyroid receptor ligands
Novel pyridine-based thyroid receptor ligands are provided which have the general formula I wherein: X is oxygen (—O—), sulfur (—S—), sulfoxide (—S(O)—), sulfonyl (—SO 2 —), CR 8...
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6727265 |
Phenoxyethyl-thiourea-pyridine compounds and their use for treatment of HIV-infections
The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the...
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6716988 |
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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6716859 |
Substituted N′-(Arylcarbonyl)-benzhydrazides, N′(Arylcarbonyl)-benzylidene-hydrazides and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted N′-(arylcarbonyl)-benzhydrazides, N′-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: wherein...
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6713492 |
N-acyloxylated cycloalkyl compounds, composition containing the same and methods of use therefor
Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C 4 or C 5 cycloalkyl which...
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6710180 |
Diazonium salts which are intermediates for 3-substituted pyridines
The present invention relates to 3-substituted and 2,3-disubstituted pyridine compounds which are useful as intermediates in the synthesis of pyridylsulfonylurea herbicides. The invention also...
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