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Class 540/603 - Plural hetero atoms in the additional hetero ring


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero atoms.
No. of patents: 383
Last issue date: 09/30/2008


1                    
NumberTitleIssue Date
74296075-HTreceptor antagonists
The present invention relates to compounds of formula I: wherein one of R1 and R4 is selected from the group consisting of H, and optionally substituted C1-6 alkyl, C3-7 cycloalky...
09/30/2008
74140484,5-dihydro-isoxazole derivatives and their pharmaceutical use
The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A1=A2-A3=A4- is a pyridinylidene, p...
08/19/2008
7405209Protease inhibitors
The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such co...
07/29/2008
7393842Pyrazole analogs acting on cannabinoid receptors
One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the i...
07/01/2008
7323456Carboxylic acid derivatives compounds and agents comprising the compounds as active ingredient
A compound of formula (I) (wherein all symbols are as defined in the specification) and a salt thereof, and peroxisome proliferator activated receptor regulator comprising thereof as active ingredient. Because a ...
01/29/2008
7304052Substituted homopiperidinyl benzimidazole analogues as fundic relaxants
The present invention relates to compounds of formula (I) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- repres...
12/04/2007
7304048Indole-type derivatives as inhibitors of p38 kinase
The invention is directed to methods to inhibit p38-α kinase using compounds containing an aromatic system coupled through a 7-membered heterocycle to an indole-type system. ...
12/04/2007
7273857Benzimidazolidinone derivatives as muscarinic agents
Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the s...
09/25/2007
7265103Substituted amino isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart o...
09/04/2007
7241901Process for preparing thiazole derivative and the intermediate compounds for preparing the same
The present invention provides a process for preparing thiazole derivatives of formula (XI), that activate the delta subtype of the human Peroxisome Proliferator Activated Receptor (hPPARδ), and also provides processes for compounds of formula (VI), (VII), (VIII) a...
07/10/2007
7238696Heterocyclyl-3-sulfonylindazoles as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor ...
07/03/2007
72327923-heterocyclyl-substituted benzoyl derivatives
Benzoyl derivatives of the formula I where the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio...
06/19/2007
7229987Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes
The present invention relates to a melanin concentrating hormone antagonist compound of formula I: (I); or a pharmaceutically acceptable salt, solvate, enantiomer or prodrug thereof useful in the treatment, prevention or amelioration of symptoms associated with obes...
06/12/2007
7151175Propenecarboxylic acid amidoxime derivatives, a process for the preparation thereof, and pharmaceutical compositions containing the same
The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suit...
12/19/2006
7125877Benzimidazole derivatives
This invention provides compounds which are represented by a general formula [I] [in which X stands for hydrogen or halogen; B stands for halogen, cyano or optionally fluorine-substituted lower alkyl; D stands fo...
10/24/2006
7105556Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2
09/12/2006
7087593Benzimidazolidinone derivatives as muscarinic agents
Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the s...
08/08/2006
7071182Antagonists 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...
07/04/2006
7071184Protease inhibitors
The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel int...
07/04/2006
7049307Antagonists 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...
05/23/2006
70340291-aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor ...
04/25/2006
7030150Benzimidazole compounds and antiviral uses thereof
The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or o...
04/18/2006
7008957Bicyclic cyanoheterocycles, process for their preparation and their use as medicaments
The invention relates to compounds of the formula I in which the radicals have the stated meanings, their stereoisomeric forms and their physiologically tolerated salts and process for their preparation. The com...
03/07/2006
7001901Tetrazolylpropionamides as inhibitors of Aβ protein production
This invention relates to novel tetrazolyl-propionamides in which the amide group comprises an aminoazepinone, and related structures, of Formula (I): or pharmaceutically acceptable salt or prod...
02/21/2006
6982259N-heterocyclic derivatives as NOS inhibitors
N-Heterocyclic derivatives of the following formula: where m, n, p, A1, R1, R2, R3 and R4 are described herein, as well as other N-heterocyclic derivatives, are us...
01/03/2006
6953793Substituted pyrazoles
Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described. ...
10/11/2005
6936570Tetrazolinone derivatives
The invention relates to novel tetrazolinone derivatives of general formula (I) wherein R1 represents halogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylsulfonyl, C1-4
08/30/2005
6919329N-Aryl-2-oxazolidinone-5-carboxamides and their derivatives
The present invention provides antibacterial agents having the formulae I, II, and III described herein. ...
07/19/2005
6906090Compositions and methods for treating mycobacterial diseases
The invention provides the use of certain isatin and oxindole derivatives in the preparation of a medicament for use in the treatment of mycobacterial disease. ...
06/14/2005
6887864Azepane derivatives
This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their ...
05/03/2005
6887865N-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...
05/03/2005
6861432Piperazine derivatives that destabilize androgen receptors
This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R′, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the inventio...
03/01/2005
6833375N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C
12/21/2004
68283151-Amino triazoloc4,3-a! quinazoline-5-ones and/or -5-thiones inhibiting phosphodiesterase IV
The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutical...
12/07/2004
6767912Heterocyclylindazole and -azaindazole compounds as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor. ...
07/27/2004
6696437Heterocyclically substituted benzimidazoles, the production and application thereof
The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs....
02/24/2004
6680314Azacyclooctane and heptane derivatives, their preparation and use in therapy
Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: ##STR1## wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 ...
01/20/2004
6667303Aryl substituted 1,4-diazepanes and method of use thereof
Aryl substituted 1,4-diazepanes are provided such as derivatives of 6-(1,4-diazepan-1-yl)benzo[cd]indol-2(1H)-one, 6-(1,4-diazepan-1-yl)acenaphthylen-1(2H)-one and 5-(1,4-diazepan-1-yl)-2H-naphtho[1,8-cd]isothiazole-1,1-dioxide. Also provided are pha...
12/23/2003
66276265-heterocyclo-pyrazoles
The present invention relates to 5-heterocyclo-pyrazoles of the formula I: ##STR1## wherein ring W, m, n, and R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal us...
09/30/2003
6627624Aryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined here...
09/30/2003
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