Class 546/271.1 - 1,2-thiazoles (including hydrogenated)

Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the five-membered hetero ring has sulfur
No. of patents: 260
Last issue date: 09/30/2008

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Number	Title	Issue Date
7429667	Phenylamino isothiazole carboxamidines as MEK inhibitors The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones. ...	09/30/2008
7390907	Vanilloid 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
7276602	Isothiazole derivatives useful as anticancer agents The invention relates to compounds of the formula 1 or pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof, wherein wherein X, R1, and R2 are as defined herein. The inv...	10/02/2007
7256291	Labeling reagents comprising aphenylic analogs of rhodamine dyes This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful ...	08/14/2007
7253187	Heterocyclic inhibitors of ERK2 and uses thereof Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1...	08/07/2007
7226740	Aza-benzazolium containing cyanine dyes Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. The subject d...	06/05/2007
7214678	Arylsulfanyl and heteroarylsulfanyl derivatives for treating pain According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.	05/08/2007
7183303	Gamma-secretase inhibitors Compounds of formula I: inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease. ...	02/27/2007
7141596	Inhibitors of proteins that bind phosphorylated molecules The present invention provides compounds that can modulate the activity of a target protein, such as a phosphatase, that selectively binds phosphorylated peptides or proteins. The present compounds can be useful in treating diseases or disorders, including, for exam...	11/28/2006
7132425	5-substituted-six-membered heteroaromatic glucokinase activators The present invention provides a compound according to formula I where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula I are ...	11/07/2006
7105556	Conformationally 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
RE39265	Heteroarylpiperidines, and their use as antipsychotics and analgetics Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compound...	09/05/2006
7022650	4-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines A description is given of 4-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines of formula (I) and of their use as herbicides. In this formula (I) R1, R2, R3 and R4	04/04/2006
6989398	Benzanilides as potassium channel openers Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided. ...	01/24/2006
6987189	Short synthesis of pyridine-based pharmaceutical intermediates A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1–C4 alkyl, C1–C4 alkoxy,...	01/17/2006
6987184	Isothiazoloanthrones, isoxazoloanthrones, isoindolanthrones and derivatives thereof as JNK inhibitors and compositions and methods related Isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof having the general formula: and pharmaceutically acceptable salts thereof, wherein R0 is —CH2—, —SO—, ...	01/17/2006
6939882	Fungicides Use of compounds of general formula (I) or salts thereof as phytopathogenic fungicides wherein the various radicals and substituents are as defined in the description, pesticidal compositions containing them and method for combatting pests which comprises applying t...	09/06/2005
6927216	Cyclic sulfonyl compounds as inhibitors of metalloproteases The present application describes novel cyclic sulfonyl derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms select...	08/09/2005
6924298	2-(3,5-Disubstituted-4-pyridyl)-4-(thienyl, thiazolyl or arylphenyl)-1,3-oxazoline compounds Oxazoline compounds having a 3,5-disubstituted-4-pyridyl group in the 2-position and a thienyl, thiazolyl or an arylphenyl group in the 4-position are effective in controlling aphids, insects and mites. ...	08/02/2005
6916933	4-pyridinyl-n-acyl-l-phenylalanines Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4. ...	07/12/2005
6855825	Short synthesis of pyridine-based pharmaceutical intermediates A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1-C4 alkyl, C1-C4 alkoxy, ar...	02/15/2005
6821992	Fungicides The invention relates to compounds of general formula I, where A1, R1, R2 and Y are as defined in the description; and to their use as phytopathogenic fungicides. ...	11/23/2004
6800760	Quinolinone derivatives Organic compounds having the formulas I and II are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and...	10/05/2004
6777410	Isoindole derivatives This invention relates to compounds represented by the general formula [I] wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 ...	08/17/2004
6730792	β3 adrenergic agonists The present invention relates to a β3 adrenergic receptor agonist of formula (I) or a pharmaceutical salt thereof, which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type II diabetes and/or obe...	05/04/2004
6720425	Alkyl or aryl substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity. ...	04/13/2004
6689888	Processes and intermediates useful in preparing 댣-adrenergic receptor agonists The present invention provides processes useful in the preparation of certain 댣 -adrenergic receptor agonists of the structural formula ##STR1## the pharmaceutically acceptable salts thereof, and the hydrates of said pharmaceuticall...	02/10/2004
6677341	(R)-Chiral halogenated substituted heteroaryl benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and m...	01/13/2004
6667326	Pesticidal aminoheterocyclamide compounds The invention relates to compounds of the general formula ##STR1## wherein R1, R2, R3, R4, R5, X1, X2, X3, m and n have the significances given in claim 1, and optionally ...	12/23/2003
6664047	Aza-benzazolium containing cyanine dyes Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. Th...	12/16/2003
6620831	Indazoles substituted with 1,1-dioxoisothiazolidine useful as inhibitors of cell proliferation The present invention relates to an indazole derivative, pharmaceutically acceptable salt, solvated product and isomer thereof substituted with 1,1-dioxoisothiazolidine which are useful as inhibitors for Cyclin Dependent Kinase(CDK). The present invention...	09/16/2003
6605725	Benzanilides as potassium channel openers Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided....	08/12/2003
6593349	Bisarylamines as potassium channel openers Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions...	07/15/2003
6525076	Selective factor Xa inhibitors Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders....	02/25/2003
6492397	N-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
6489344	Inhibitors of glycogen synthase kinase 3 New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the in...	12/03/2002
6486308	Covalently linked oligonucleotide minor groove binder conjugates Minor groove binding molecules are covalently bound to oligonucleotides which in their base sequence are complementary to a target sequence of single stranded or double stranded DNA, RNA or hybrids thereof. The covalently bound oligonucleotide minor groov...	11/26/2002
6458950	Compounds and pharmaceutical compositions containing the same A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen,...	10/01/2002
6303639	Propanolamine derivatives substituted by heterocyclic radicals, processes for their preparation, pharmaceuticals comprising these compounds and their use Substituted propanolamine derivatives and pharmaceutically tolerated salts and physiologically functional derivatives thereof are described. Also described are compounds of formula (I), ##STR1## in which the radicals have the meanings given in the specificatio...	10/16/2001
6271236	Diaminopyridine-containing thiourea inhibitors of herpes virus Compounds of the formula ##STR1## wherein R1 -R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl ...	08/07/2001

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Class 546/271.1 - 1,2-thiazoles (including hydrogenated)