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Class 514/253.09 - Five-membered nitrogen hetero ring attached directly or indirectly to the piperazine ring by nonionic bonding


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the piperazine ring is attached directly
No. of patents: 428
Last issue date: 01/24/2012


1                      
NumberTitleIssue Date
81016181,4-substituted piperazine derivatives
A compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 represents a branched lower alkyl group having from 3 to 9 carbon atoms or ...
01/24/2012
80932502-aminocarbonyl-pyridine derivatives
The present invention relates to 2-aminocarbonyl-pyridine derivatives of Formula (I) and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of...
01/10/2012
8063052Wound healing
The present invention relates to the use of p38 MAP kinase inhibitors and p38 MAP kinase inhibition to promote wound healing. ...
11/22/2011
80534369-(piperazinylalkyl) carbazoles as bax-modulators
The present invention is related to piperazine derivatives of carbazole of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said piperazine derivatives of...
11/08/2011
8017616Heterocyclic substituted pyridine compounds with CXCR3 antagonist activity
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general s...
09/13/2011
7998963Arylpiperazine derivatives and uses thereof
Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein Ar is indolyl, indazolyl or dihydroindolyl, and R1, R2, R3 and R4 are as defined herein. Also provide...
08/16/2011
7956058Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate ...
06/07/2011
7951807Substituted oxindol derivatives and medicaments containing the same
The present invention relates to novel oxindole derivatives of the general formula (I), wherein the substituents A, B, R1, R2 and R3 are as defined in Claim 1, and medicaments contain...
05/31/2011
7910591Piperazine derivatives of alkyl oxindoles
The present invention is concerned with new indol-2-one derivatives of Formula (I), which have favorable activity profile for the prophylaxis and treatment of disorders in the central nervous or in the cadiovascular system. ...
03/22/2011
7884106Method of stabilizing lipid-rich plaque and method of preventing rupture thereof
A method of stabilizing lipid-rich plaques and method of preventing the rupture thereof, characterized in that an effective amount of 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide, its acid adduct salt or a ...
02/08/2011
78469334-imidazolin-2-one compounds
The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: w...
12/07/2010
7820672Indolylmaleimide derivatives
The compounds are indolylmaleimide derivatives comprising either a substituted pyridyl or indolyl residue. The compounds have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or ...
10/26/2010
7816361Immuno inhibitory pyrazolone compounds
Compounds of formula (IA) or (IB) are inhibitors of CD80 and useful in immunomodulation therapy: wherein Ar represents an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group having from 5 to 10 ring atoms; R1 and R2 i...
10/19/2010
7786124Heterocyclic substituted pyridine compounds with CXCR3 antagonist activity
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general s...
08/31/2010
7700598Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereome...
04/20/2010
7696209CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3, R4 and X are defined as in claim 1, the tautomers, the isomers, the diastereo...
04/13/2010
76830673-heterocyclyl-indole derivatives as inhibitors of glycogen synthase kinase-3 (GSK-3)
Compounds of formula Ia or Ib wherein P; R1; R2; m; and n are as defined in the application, salts thereof, processed for their preparation, new intermediates used therein, pharmaceutical formulations ...
03/23/2010
7659276Melanin concentrating hormone receptor antagonist
Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I wherein A, W, X, Z, R1-R3, and R8 are as defined in the specification, are provided. Also p...
02/09/2010
7659275Piperidinyl piperazine derivatives useful as inhibitors of chemokine receptors
In its many embodiments, the present invention provides a novel class of compounds of structural formula IA or IB where R1-R8 are as disclosed herein as inhibitors of the CCR5 receptors, methods of pre...
02/09/2010
7652015Kinase inhibitors
The present invention provides kinase inhibitors of Formula (I). Wherein R1, R2, X and Z are as described herein, or a pharmaceutically acceptable salt thereof. ...
01/26/2010
7638518Substituted pyrazole kinase inhibitors
The present invention is directed to novel substituted pyrazole compounds of Formula (I) or a form or composition thereof and the use thereof as inhibitors of ATP-protein kinase interactions. ...
12/29/2009
7592347Piperazine derivates and their use for the treatment of neurological and psychiatric diseases
The present invention relates to novel piperidine carbonyl piperazine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders. ...
09/22/2009
7544686Piperazinylalkylpyrazole derivatives useful as selective T-type calcium channel blockers and preparation method thereof
The present invention provides for novel piperazinylalkylpyrazole derivatives, the preparation method thereof and the selective T-type calcium channel blocking activity thereof. Particularly, it provides a piperazinylalkylpyrazole derivative as represented by the fo...
06/09/2009
7514438Melanin concentrating hormone receptor antagonist
Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I wherein A, W, X, Z, R1-R3, and R8 are as defined in the specification, are provided. Also p...
04/07/2009
74322551H-indol-5-yl-piperazin-1-yl-methanone derivatives
The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein in formula I is: wherein R1 to R4 are as defined in the description and claims. The compounds...
10/07/2008
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
7396830Piperazine amidines as antiviral agents
This disclosure provides compounds of Formula I as described herein having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with indole and a...
07/08/2008
7364740Molecular differences between species of the complex
Specific genetic deletion are identified in mycobacteria isolates, including variations in the M. tuberculosis genome sequence between isolates, and numerous deletion present in BCG as compared to M. tb. These deletions are used as markers to distinguish betw...
04/29/2008
7342015Indole derivatives
A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disord...
03/11/2008
7335658Pyridazine derivatives and their use as therapeutic agents
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): ...
02/26/2008
7300929Mediators of hedgehog signaling pathways, compositions and uses related thereto
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small ...
11/27/2007
7294627Chemical compounds
Compounds of formula (I) in which R1, R2, R3 and R4, have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorde...
11/13/2007
7291613Inhibitors of p38 kinase
The invention is directed to methods to inhibit p38-α kinase using compounds comprising saturated heterocycles coupled to a fused ring system. ...
11/06/2007
7291619Melanocortin receptor agonists
The present invention relates to melanocortin receptor agonists of formula (I), which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction ...
11/06/2007
7265118Regulation of substrate activity
A method for regulating substrate activity in vivo is useful for the treatment of medical disorders such as inflammation, arteriolosclerosis and angiogenesis. The method involves the administration of an effective amount of a DPP-IV inhibitor to a patient in need of...
09/04/2007
7247631Pegylated interferon alfa-CCR5 antagonist combination HIV therapy
Methods for treating treatment-naive as well as treatment-experienced adult and pediatric patients having HIV-1 infections as well as patients co-infected with HIV-1 and HCV involving administering a therapeutically effective amount of pegylated interferon-alfa, e.g...
07/24/2007
7241787Substituted N-cycloexylimidazolinones, process for their preparation and their use as medicaments
The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and to their use as medicaments. Compounds of the formula I,
07/10/2007
72417644(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders
Compounds of general formula:[Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions includin...
07/10/2007
72237642,4-bis (trifluoroethoxy)pyridine compound and drug containing the compound
The present invention is directed to a 2,4-bis(trifluoroethoxy)pyridine compound represented by formula (1): (wherein X1 represents a fluorine atom or a hydrogen atom) or a salt thereof, and to a drug ...
05/29/2007
7214679Piperidine/piperazine-type inhibitors of p38 kinase
Compounds of the formula: wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase. ...
05/08/2007
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