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Class 544/405 - Additional hetero ring which is unsaturated


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds having, in addition to the six-membered hetero
No. of patents: 923
Last issue date: 09/20/2011


1                      
NumberTitleIssue Date
8022210Soluble amide and ester pyrazinoylguanidine sodium channel blockers
The present invention relates to pyrazinoylguanidine compounds represented by formula (I): where X, Y and R1-R4 are as defined herein. The compounds of the present invention are useful as sodium channel blockers. ...
09/20/2011
8008494Soluble amide and ester pyrazinoylguanidine sodium channel blockers
The present invention relates to pyrazinoylguanidine compounds represented by formula (I): where X, Y and R1-R4 are as defined herein. The compounds of the present invention are useful as sodium channel blockers. ...
08/30/2011
7642354Polycyclic pyrazines as potassium ion channel modulators
The present invention provides a genus of polycyclic pyrazines of formula (I): wherein A and B are independently substituted or unsubstituted 5- or 6- membered heterocycloalkyl, or substituted or unsubstituted 5- or 6- memb...
01/05/2010
7547782Met kinase inhibitors
The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer. ...
06/16/2009
7524957Compounds effecting glucokinase
The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or preventio...
04/28/2009
7442702Prostaglandin agonists
This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatmen...
10/28/2008
7442701Amino-heterocycles as VR-1 antagonists for treating pain
The present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C—Ar2, with the proviso that at least one, but no more than ...
10/28/2008
7419980Fused-aryl and heteroaryl derivatives and methods of their use
The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms...
09/02/2008
7410972Compounds
The invention provides N-pyrazinyl-thienylsulphonamides of formula (I) for use in the treatment of chemokine mediated diseases. Particularly inflammatory diseases, such as asthma ...
08/12/2008
7407976Thiazoles and oxazoles useful as modulators of ATP-Binding Cassette transporters
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to meth...
08/05/2008
7407961Pyrazine derivatives and pharmaceutical use thereof
A pyrazine derivative of the following formula (I): or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatme...
08/05/2008
7407972Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thro...
08/05/2008
7402606Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss
Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle ...
07/22/2008
73849573,4-dihydro-1H-isoquinolin-2-yl-derivatives
The present invention relates to novel compounds of formula I wherein the variable groups are as defined in the claims or a pharmaceutically acceptable acid addition salt thereof. The compounds of the invention are NK2 antagonists.
06/10/2008
7384946Mmuscarinic acetylcholine receptor antagonists
Novel dimeric benzoazabicyclohepatane compounds, pharmaceutical compositions, processes for their preparation and use thereof in treating M3 muscarinic acetylcholine receptor mediated diseases are disclosed. ...
06/10/2008
7381719Diaryl ethers as opioid receptor antagonist
A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3′, E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer o...
06/03/2008
7368451Capped pyrazinoylguanidine sodium channel blockers
The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers. ...
05/06/2008
7368450Sodium channel blockers
The present invention relates to compounds represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the st...
05/06/2008
73650733-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by VLA-4
Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, a...
04/29/2008
7351807Cyanine-sulfenates for dual phototherapy
Dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds comprise sulfenates having the formula, t,0080 where E is selected from the group consisting of somatostatin receptor binding molecules, heat se...
04/01/2008
73420195, 6-diaryl-pyrazine-2-amide derivatives as CBantagonists
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, in which R1 and R2 independently represent: a C1-6alkyl group; an optionally substitu...
03/11/2008
7326706Pyrazine modulators of cannabinoid receptors
The present application describes compounds according to Formula I, wherein A, G1, G2 and R1 are described herein. Additionally, the present application describes pharmaceutical compositions comprising at least one compound according...
02/05/2008
7323470Viral polymerase inhibitors
An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein wherein A, B, R2, R3, M1, M2, M3, M4, Y1 ...
01/29/2008
7319100Substituted pyrazinones, pyridines and pyrimidines as corticotropin releasing factor ligands
Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): Such compounds are particularly useful as CRF receptor ligands, and hence, in the treatment of vario...
01/15/2008
7312222Heterocyclic piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases. ...
12/25/2007
73096993-Quinuclidinyl amino-substituted biaryl derivatives
Compounds of formula (I) wherein A is N or N+—O−; n is 0, 1, or 2; Y is O, S, —NH—, and —N-alkyl-; Ar1 is both 6-membered aromatic rings; Ar2 is 5- or 6-membe...
12/18/2007
7288652Method for preparing oltipraz
Provided is a method for preparing oltipraz. The method includes reacting methyl 2-methyl-3-(pyrazin-2-yl)-3oxopropionate with phosphorus pentasulfide in the presence of a mixed solvent of toluene and xylene, followed by recrystallization. ...
10/30/2007
7285551Fused-ring compounds and use thereof as drugs
The present invention provides a fused ring compound of the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for he...
10/23/2007
7285554Pyrazole derivative
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors conta...
10/23/2007
7282501Modulators of peroxisome proliferator activated receptors (PPAR)
The present invention is directed to a compound of formula I, and pharmaceutically acceptable salts, solvates, hydrates or stereoisomer thereof, which are useful in treating Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hyperte...
10/16/2007
7282502CCR9 inhibitors and methods of use thereof
The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compound...
10/16/2007
7279472Compounds useful as reversible inhibitors of cysteine proteases
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds
10/09/2007
7276602Isothiazole derivatives useful as anticancer agents
The invention relates to compounds of the formula 1 or pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof, wherein wherein X, R1, and R2 are as defined herein. The inv...
10/02/2007
7273868Pyrazine derivatives
1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, ...
09/25/2007
7262196Tri(cyclo) substituted amide glucokinase activator compounds
Compounds of Formula (I): or pharmaceutically acceptable salts or N-oxides thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes. ...
08/28/2007
7259175Peroxisome proliferator activated receptor modulators
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C
08/21/2007
7256192Aromatic diamide derivatives, chemicals for agricultural or horticultural use and usage thereof
The present invention relates to an aromatic diamide derivative represented by the general formula (I): [A1 is optionally substituted (C1-C8)alkylene grou...
08/14/2007
7253188Aminobenzamide derivative
This invention relates to a novel compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is —S(O)p-A, ...
08/07/2007
7253197Aminothiazole derivatives
Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4 have the significance given in the specification, and the compounds, salts and esters...
08/07/2007
7250418Compounds as CRFreceptor antagonists
The present invention relates to compounds of Formula I, or a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a prodrug thereof. The compounds of the inventions are CRF1 receptor a...
07/31/2007
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