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Class 540/524 - Additional hetero ring containing


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain at least two hetero rings.
No. of patents: 252
Last issue date: 06/28/2011


1              
NumberTitleIssue Date
7968708Azepans and methods for making and using same
Disclosed are compounds having the formula: wherein Z1 is an alkylene moiety; Q is a carboxylic acid derivative; and R1 and R2 are the same or different and are selected from the group consi...
06/28/2011
7951940Substituted indole compounds having NOS inhibitory activity
The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other p...
05/31/2011
7939657N-substituted benzene sulfonamides
Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R3′,...
05/10/2011
7829699Process for the preparation of CGRP antagonist
An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1 -carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifl...
11/09/2010
7390798Carboxamide spirolactam CGRP receptor antagonists
The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in...
06/24/2008
7375219Substituted indole compounds having NOS inhibitory activity
The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other p...
05/20/2008
7368566Process and intermediates for preparing benzazepines
Disclosed is a new process and intermediates for preparing benzazepines of Formula (I): wherein R1 and R2 are as defined herein. ...
05/06/2008
7342022Compounds in the treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3
The present invention relates to new compounds of formula I wherein R1, R2, R3, n, m are defined as in claim 1, a process for their preparation and new intermediates used in the preparation thereof, pharmaceutical formulations contai...
03/11/2008
7329652Diaminotriazole 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 invention, processes for preparing the compounds and methods of using...
02/12/2008
7291612Immunomodulatory compounds
The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthri...
11/06/2007
7279468Integrin ligands
The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the αvβ3 integrin receptor, their use, and pharmaceutical preparations comprising these compoun...
10/09/2007
7253158Sulfonamides
The invention relates to compounds of the general formula in which R1, R2, R3, R4, R2′, R3′, R4′, R5, and X is —CHR— are as defined in t...
08/07/2007
7253159Methods and compositions for immunomodulation using CD1 antigens
The invention relates to novel CD1a-presented antigens. These antigens can be used as antigens, adjuvants or as immunomodulatory agents in a variety of diagnostic, therapeutic and prophylactic applications. ...
08/07/2007
7235545CGRP receptor antagonists
The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, ...
06/26/2007
7208488N-substituted benzene sulfonamides
Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R
04/24/2007
7208487Compounds, compositions and methods
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed. ...
04/24/2007
7205309Quinazoline derivatives
Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3 and A have the significance given in the specification are provided. The...
04/17/2007
7205292CGRP receptor antagonists
The present invention is directed to compounds of Formula I and Formula II: (where variables R1, R2, R3, R4, R6, A, B, G, J, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the ...
04/17/2007
7199117Phenyl-substituted imidazopyridines
The invention features pharmaceutically-active imidazopyridines and derivatives that are substituted with phenyl, methods of making them, and methods of using them. ...
04/03/2007
7173032Methods and compositions of novel triazine compounds
The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced...
02/06/2007
7157447Bicyclic heterocycles as HIV integrase inhibitors
The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharm...
01/02/2007
7125865Therapeutic compounds for treating dyslipidemic conditions
The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.
10/24/2006
7115644Heterocyclic compounds
Disclosed are benzimidazolone compounds of formulas (I) & (II): wherein R1, R2, R3, R4, R5, X, L, m, n and t are defined herein. The compounds inhibit production of cytokines involved in inflammatory proc...
10/03/2006
70911982,5-disubstituted pyrimidine derivatives
The present invention relates to novel 2,5-disubstituted pyrimidine derivatives which stimulate soluble guanylate cyclase, to processes for the preparation thereof, and to the use thereof for producing medicaments, in particular medicaments for the treatment of cent...
08/15/2006
7087597Pyrimidine 5-carboxamide compounds, process for producing the same and use thereof
Compounds of the formula wherein R1, R2, R3, R4, X and Y are as defined, which have a superior cGMP specific phosphodiesterase (PDE) inhibitory activity, and can be use...
08/08/2006
7084196Flame retardant compositions
Polymeric substrates, for example polyolefins such as polypropylene, can be made flame retardant by the incorporation therein of a synergistic mixture of (i.) at least one compound selected from the group consisting of nitroxyl stabilizers, hydroxylamine stabilizers...
08/01/2006
7081456Immunomodulatory compounds
The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthri...
07/25/2006
RE39112Purine 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 compound represented by the formula (I), its pharmacologically...
05/30/2006
7026310Heteroaryl derivatives and their use as medicaments
The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors. ...
04/11/2006
7022390Polyester and polyamide compositions of low residual aldehyde content
A mixture of a polyester, such as poly(ethylene terephthalate) PET, or a polyamide, and a suitable stabilizer selected from the group consisting of hydroxylamine stabilizers, substituted hydroxylamine stabilizers, nitrone stabilizers and amine oxide stabilizers, whe...
04/04/2006
7015320Process for the manufacture of optically active 3-substituted lactams by asymmetric hydrogenation of 3-alkylidenelactams
The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) process, comprising: contacting a compound of formula (II): ...
03/21/2006
7001899Interleukin converting enzyme inhibitors
The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula: wherein each X is independently selected from: i) —C(W)2...
02/21/2006
6992044Substituted phenyluracils
The invention relates to novel substituted phenyl uracils of the formula (I) in which R1 represents hydrogen, amino or in each case optionally substituted alkyl, alkenyl or alkynyl, ...
01/31/2006
6958329Lactams substituted by cyclic succinates as inhibitors of A-β protein production
This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more spec...
10/25/2005
6953789Thiol compounds, their production and use
The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1
10/11/2005
69537883-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase
The present invention relates to certain novel 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase. Pharmaceutical compositions containing said compounds as well as methods of treating various disease state...
10/11/2005
6953790CGRP receptor antagonists
The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T...
10/11/2005
6924292Furoisoquinoline derivatives, process for producing the same and use thereof
A compound having a partial structure represented by Formula: or a salt thereof has an excellent phosphodiesterase (PDE) IV-inhibiting effect, and is useful as a prophylactic or therapeutic agent against inflammatory d...
08/02/2005
6908650Polyester and polyamide compositions of low residual aldehyde content
A mixture of a polyester, such as poly(ethylene terephthalate) PET, or a polyamide, and a suitable stabilizer selected from the group consisting of hydroxylamine stabilizers, substituted hydroxylamine stabilizers, nitrone stabilizers and amine oxide stabilizers, whe...
06/21/2005
6903089Lactam-substituted pyrazolopyridine derivatives
The invention relates to novel pyrazolopyridine derivatives of formula (I) wherein R1 represents NH2 or NHCO-C1-6-alkyl, and R2 represents a radical of formula R3N...
06/07/2005
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