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Class 546/274.4 - Chalcogen attached directly to the 1,3-diazole ring by nonionic bonding


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein chalcogen (i.e., oxygen, sulfur, selenium,
No. of patents: 231
Last issue date: 08/26/2008


1            
NumberTitleIssue Date
7417047Amino-5-(5-membered)hetero-arylimidazolone compounds and the use thereof for β-secretase modulation
The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and ...
08/26/2008
7390907Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascu...
06/24/2008
7354933Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use...
04/08/2008
7288559Carboxamide spirohydantoin CGRP receptor antagonists
The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pha...
10/30/2007
7226940Substituted heterocycles for the treatment of diabetes and other diseases
The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymph...
06/05/2007
7192954Monocyclic anilide spirohydantoin CGRP receptor antagonists
The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pha...
03/20/2007
7186727Pyridyl-substituted spiro-hydantoin compounds and use thereof
A class of substituted spiro-hydantoin compounds (II) having the formula: its pharmaceutically acceptable salts, enantiomers, solvates, or prodrugs thereof, wherein R16 is a substituted pyridinyl group...
03/06/2007
7129359Imidazolidinone compounds
This invention relates to compounds of the following formula: in which R1, R2, A1, A2, X, Y, m, n, p, x and y are as defined herein, pharmaceutical compositions compris...
10/31/2006
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
7078420Spiro-hydantoin compounds useful as anti-inflammatory agents
Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, whe...
07/18/2006
6995262Use of acylsulfonamido-substituted polymethine dyes as fluorescene dyes and/or markers
The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae ...
02/07/2006
6977267Spiro-hydantoin compounds useful as anti-inflammatory agents
Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, wherein L...
12/20/2005
6974826Imidazolidinedione derivatives for the treatment of diabetes and other diseases
The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymph...
12/13/2005
6884815High affinity small molecule C5a receptor modulators
This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as anta...
04/26/2005
6784298Hydantoin-containing glucokinase activators
Hydantoin compounds which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes. ...
08/31/2004
6784293Process for making Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils
The present invention provides a process for the efficient assembly of Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils via a one-pot solution phase or solid phase synthesis from readily available starting materials. ...
08/31/2004
6680333Imidazolidine derivatives, their preparation, their use and pharmaceutical preparations comprising them
The present invention relates to novel imidazolidine derivatives of formula I, ##STR1## wherein A, E, Z, R1, R2, R3, R4 and R5 have the meanings indicated in the claims. The compounds of formula I are...
01/20/2004
6620825Adenosine A3 receptor antagonists
A pharmaceutical composition for antagonizing adenosine at adenosine A3 receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophyla...
09/16/2003
6613908Method for carbamoylating alcohols
The present invention includes a method for carbamoylating an alcohol with sodium cyanate in the presence of methanesulfonic acid. The reaction can be conducted under anhydrous conditions. This method is suitable for carbamoylating a molecule including bo...
09/02/2003
66028895-heteroaryl substituted indoles
The present invention relates to compounds having general formula (I) as defined herein, or a pharmaceutically acceptable acid addition salt thereof. The compounds are selective 댑 -adrenoceptor ligands. ##STR1##...
08/05/2003
6583288Hydantoin-containing glucokinase activators
Hydantoin compounds which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes....
06/24/2003
6569873Azolidines as beta-3 adrenergic receptor agonists
This invention provides compounds of Formula I having the structure ##STR1## wherein, A, X, Y, Z, W, R1, R2, R3, R4, R5, and R6 are as defined hereinbefore or a pharmaceutically acceptable salt ...
05/27/2003
6562832Substituted imidazole compounds
Novel 1,4,5-subsituted imidazole compounds and compositions for use in therapy as cytokine inhibitors....
05/13/2003
6518293Anti-HIV imidazolone derivatives
The invention is concerned with novel imidazolone derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are inhibitors of the human immunodeficiency virus reverse ...
02/11/2003
6514993Serotonin 5-HT1A and dopamin D2 receptor ligands
The present invention relates to a novel series of 4-phenylpiperazines, 4-phenylpiperidines and 4-phenyl-1,2,3,6-tetrahydropyridines compounds of general formula (I) ##STR1## wherein A is alkylene, alkenylene, alkynylene, and C3-7 cycloalkylene...
02/04/2003
6492397N-arylheteroarylalkyl imidazol-2-one compounds for treatment of arteriosclerosis
A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of arteriosclerosis. Compounds of particular interest are angiotensin II antagonists of Formula I: ##STR1## wherein Ar is selected from ##STR2## wherein m is ...
12/10/2002
6462063C-proteinase inhibitors
The present invention relates to a novel class of N,N'-di substituted hydantoin hydroxamates capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatm...
10/08/2002
6455550N-alkanoylphenylalanine derivatives
Compounds of the formula: ##STR1## are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 ...
09/24/2002
6436966Adenosine A3 receptor antagonists
A pharmaceutical composition for antagonizing adenosine at adenosine A3 receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophyla...
08/20/2002
6420563Small molecule modulators of G protein-coupled receptor six
Disclosed herein are small molecule modulators of the G protein coupled receptor six, methods of making such compounds, and methods of using such compounds....
07/16/2002
6384061Hydantoin compounds and methods related thereto
The present invention relates to novel hydantoin compounds represented by formula (I) which shows an inhibitory activity against farnesyl transferase, and thus can be used as an anti-cancer agent, or pharmaceutically acceptable salts thereof, in which R
05/07/2002
6380134N-pyridyl herbicide compounds
Compounds of the formula I ##STR1## in which A is .dbd.N-- or ##STR2## R1 is hydrogen, fluorine, chlorine, bromine or methyl; R2 is C1 -C4 alkyl, C1 -C4 haloalkyl, halogen, R6 O...
04/30/2002
6355664Phenylpyrrolidines, phenylimidazolidines, 3-phenyl-1,3-oxizolidines and 3-phenyl-1,3-thiazolidines and their use in the treatment of inflammatory disease
A method treating or preventing inflammatory and immune cell-mediated diseases by the administration of certain novel and known small molecules. Exemplary of the novel compounds are those of the following structural formulas: ##STR1## ##STR2##...
03/12/2002
6350763Small molecules useful in the treatment of inflammation disease
Novel compounds of the formula I ##STR1## which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 1-acetyl-5-(R)-(4-bromobenzyl)-3-(2,6-dichloropyridin-4-yl)-5-methylimidazo line-2,4-dione; 5-(R)...
02/26/2002
6339158Process for the preparation of chiral nicotinic, quinolinic or benzoic acid imidazolinone herbicides
There is provided a stereospecific process for the preparation of essentially enantiomerically pure imidazolinone herbicides having the R-configuration via (R)2-amino-2,3-dimethylbutyronitrile....
01/15/2002
6331552Substituted imidazolidine derivatives, their preparation, their use and pharmaceutical preparations including them
Substituted imidazolidine derivatives of the formula I, ##STR1## in which B, E, W, Y, R, R2, R3, R30, e and h have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active com...
12/18/2001
6271249Diphenyl imidazoles as potassium channel modulators
Novel compounds of Formula 1 are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels: ##STR1## wherein "Het" is one of a select group of heterocyclic moieties; Z is independently for each occurrenc...
08/07/2001
6232321Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses
Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn -PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The ...
05/15/2001
6200991Imidazole derivatives, preparation and therapeutic application thereof
A compound of formula (I) ##STR1## the process of preparing compounds of formula (I), their pharmaceutical compositions, and the method of treating diseases associated with M3 muscarinic and/or S--HT4 serotoninergic receptors....
03/13/2001
6194438Derivatives of 2-(2-oxo-ethylidene)-imidazolidin-4-one, and compositions and methods for inhibiting abnormal cell growth comprising said derivatives
The present invention relates to compounds of the formula ##STR1## wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula I...
02/27/2001
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