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Class 546/162 - Nitrogen attached indirectly to the six-membered hetero ring through the directly attached nitrogen by nonionic bonding


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen is attached indirectly to the
No. of patents: 213
Last issue date: 11/29/2011


1            
NumberTitleIssue Date
80676011-[2-(4-benzyl-4-hydroxy-piperidin-1 -yl )-ethyl]-3-(2-methyl-quinolin- 4-yl)- urea as crystalline sulfate salt
The invention relates to 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt and a process for its preparation. Further, the present invention relates to the us...
11/29/2011
7964731Isotopically marked quinoline derivatives as adenosin A3 receptor ligands
The invention relates to adenozin A3 receptor ligands labeled with iodine isotops of mass number 125, within those favorably to antagonists and their isomers, to the experimental materials containing them, to a process for the preparation of the compounds...
06/21/2011
7868174Form of a benzenesulfonamide derivative
The present disclosure relates to an improved process for the preparation of enantiomerically enriched alcohols of Formula (I), from the corresponding ketone of Formula (II),
01/11/2011
7368573Triamide-substituted heterobicyclic compounds
This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1-R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the ...
05/06/2008
7365081Indole derivatives and their use as medicaments
The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors ...
04/29/2008
RE40278Heterocyclic amines having central nervous system activity
Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: and pharmaceutically acceptable salts thereof wherein R1 ...
04/29/2008
7332504Heterocyclic substituted aminoazacycles useful as central nervous system agents
Heterocyclic substituted aminoazacyclic compounds of formula I Z-R3I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions ...
02/19/2008
7314939Compositions and methods for inhibiting TGF-β
The present invention provides compounds of the formula: and pharmaceutically acceptable isomers, salts, hydrates, solvates, and prodrug derivatives thereof, wherein R1, R6, R7, R...
01/01/2008
7312230Carboxylic acid derivatives as IP antagonists
This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 ...
12/25/2007
7309715Compound
A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl...
12/18/2007
73040832-iminoimidazole derivatives (2)
A 2-iminoimidazole derivative represented by the formula: {wherein R1, R2 and R3 represent hydrogen, optionally substituted C1-6 alkyl, etc.; R6 represents h...
12/04/2007
7183414Processes for the preparation of benzoimidazole derivatives
The present invention relates to a process for preparing a compound of the formula I or a pharmaceutically acceptable salt, prodrug, hydrate or solvate thereof, wherein R1, R2, R3
02/27/2007
7183413Aminoquinoline compounds
This invention relates to treating inflammatory and immune diseases with certain aminoquinoline compounds that bind to CXCR3 receptors. The aminoquinoline compounds are covered by the formula (I) shown below. Each variable is defined in the specification.
02/27/2007
7151110Pyrazole compounds as transforming growth factor (TGF) inhibitors
Novel pyrazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming gro...
12/19/2006
7148227Fungicidal triazolopyrimidines, methods for producing the same, use thereof for combating harmful fungi and agents containing said substances
The invention relates to triazolopyrimidines of formula (I), in which the substituents are defined as follows: L1 represents cyano, S(═O)nA1 or C(═O)A2, wherein A1 stands for hydrogen, hydroxy, alkyl, alkyla...
12/12/2006
70841562-Aminoquinoline compounds
The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-...
08/01/2006
7060834N-type calcium channel antagonists for the treatment of pain
Compounds useful for the treatment of pain in accord with the following structural diagram, wherein A, R1, b, R4, R5, R6, R7 and R8 are any of a n...
06/13/2006
6995175Chemical derivatives and their application as antitelomerase agent
The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans. ...
02/07/2006
69893922-Aminoquinolines as melanin concentrating hormone receptor antagonists
The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, which antagonize the effects of melanin-concentrating hormone (MCH) through the melanin concentrating ...
01/24/2006
6962930Compounds, compositions and method suitable for amelioration of withdrawal syndromes and withdrawal-induced brain damage
Compounds, composition and method for ameliorating alcohol or drug dependency withdrawal syndromes and withdrawal-induced brain damage are disclosed. In particular, a series of N-substituted-4-uredo-5,7-dihalo-2-carboxy quinoline compounds are disclosed having combi...
11/08/2005
6946473Preparation and use of acetylenic ortho-sulfonamido and phosphinic acid amido bicyclic heteroaryl hydroxamic acids as TACE inhibitors
Compounds of the formula which are useful in disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative c...
09/20/2005
6930185Melanin-concentrating hormone antagonist
A melanin-concentrating hormone antagonist comprising a compound of the formula (I): wherein Ar1 is a cyclic group which may be substituted; X and Y are the same or different and are a spacer having a main c...
08/16/2005
6903104Indol-3-YL-2-oxoacetamide compounds and methods of use thereof
The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following formula. In this formul...
06/07/2005
6903094Amide derivatives and nociceptin antagonists
The present invention relates to a compound of the formula [1′]   wherein R2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the lik...
06/07/2005
6894167Method of preparation of (s)-n-tert-butyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
A new method is described here for the synthesis of (S)-N-tert-butyl-1,2,3,4-tetrahydroiso-quinoline-3-carboxamide comprising the following steps: a) (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is reacted with formic acid...
05/17/2005
6881753Potassium channel inhibitors and method
Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure: where A, B, D, Q, X1, R, R1, X2 and R2 are as defined...
04/19/2005
6875769Substituted6,6-hetero-bicyclicderivatives
This invention relates to compounds of the formula wherein A, B, D, E, K, G, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds. ...
04/05/2005
6875768Phthalamide derivatives, intermediates in the production thereof, and agricultural/horticultural insecticides and method for using the same
Heterocyclic amine derivatives represented by general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Q represents an optio...
04/05/2005
68614361-glyoxylamide indolizines for treating cancer
Disclosed is a compound represented by Structural Formula (I): Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z1 and Z2 are...
03/01/2005
6841673N-heterocyclic derivatives as nos inhibitors
N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using the...
01/11/2005
6833370Heterocycle substituted aminoazacycles useful as central nervous system agents
Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3  I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said comp...
12/21/2004
6825352Preparation and use of ortho-sulfonamido arylhydroxamic acids as matrix metalloproteinase inhibitors
Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs. ...
11/30/2004
6818772Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in repro...
11/16/2004
6800650Pyridine and quinoline derivatives
The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compou...
10/05/2004
6784189Potassium channel inhibitors and method
Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure where A, B, D, Q, X1, R, R1, X2 and R2 are as defined he...
08/31/2004
6720427Thiazole derivatives
The invention provides compounds of formula 1 wherein R1, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inh...
04/13/2004
6706699Quinolines and uses thereof
This invention relates to compounds of the general formula: in which RA, RB, RC and RD are as defined herein, and to their preparation and use. ...
03/16/2004
6699879Phenyl urea and phenyl thiourea derivatives as orexin receptor antagonists
The present invention provides phenyl urea and phenyl thiourea derivatives which are non-peptide antagonists of human orexin receptors, in particular orexin-1 receptors, of formula (I) ##STR1## in which: Z represents oxygen or sulfur; and R1
03/02/2004
6696467Quinoline derivatives
Compounds of general formula I ##STR1## as well as pharmaceutically acceptable salts and esters thereof, are potent inhibitors of neuropeptide Y and can be used in the form of pharmaceutical preparations for the treatment or prevention of various disease ...
02/24/2004
6653321Naphthylsulfonic acids and related compounds as glucose uptake agonists
Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptabl...
11/25/2003
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