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Class 548/212 - Nitrogen attached directly to the thiazole ring by nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen is attached directly to the thiazole
No. of patents: 72
Last issue date: 12/25/2007


1    
NumberTitleIssue Date
7312211Pryanone compounds useful as reversible inhibitors of cysteine proteases
Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and othe...
12/25/2007
72207663-phenylpropionic acid derivatives
The invention relates to new compounds, 3-phenylpropionic acid derivatives of formula (I) wherein W represents COOH group or its bioisosters, or —COO—C1–C4-alkyl group; Y represents NH, N—C1–C10-alkyl, O, or S; X...
05/22/2007
7202257Anti-inflammatory medicaments
Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel com...
04/10/2007
7087611Preparation of an anhydrate form of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride (ziprasidone hydrochloride)
The present invention relates to new and useful processes for the preparation of the anhydrate form of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride. ...
08/08/2006
7041691Compounds for the modulation of PPARγ activity
Modulators of PPARγ activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity. ...
05/09/2006
6936606Cyanoamido-containing heterocyclic compounds useful as reversible inhibitors of cysteine proteases
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The co...
08/30/2005
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
6716841Nitrogen containing heterobicycles as factor Xa inhibitors
This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the s...
04/06/2004
6703347Isothiazole derivatives and their use as pesticides
A compound of formula (I), where A is optionally substituted alkylene, alkenylene, alkynylene, cycloalkylene, alkylenoxy, oxy(C1-6)alkylene, alkylenthio, thio(C1-6)alkylene, C1-6 alkylenamino, amino(C1-6)alkylen...
03/09/2004
6689770Aryl sulfonyls as factor Xa inhibitors
The present application describes aryl sulfonyls of formula I: ##STR1## or pharmaceutically acceptable salt or prodrug forms thereof, wherein D, E, and M are defined below, are effective factor Xa inhibitors....
02/10/2004
6670385଱-phenyl-ଲketosulfone
The present invention relates to novel aryl-substituted S(O)m cycles of the formula (I) ##STR1## in which F1, F2, G, V, W, X, Y, Z and m are each as defined in the description, to processes for their preparation and to the...
12/30/2003
6331537Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and pr...
12/18/2001
6245765Mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihyd ro-2(1H)-indol-2-one (=ziprasidone), its preparation and its use as dopamine D2 antagonist
The invention is directed to the mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydr o-2H-indol-2-one, pharmaceutical compositions containing said ziprasidone mesylate dihydrates, and methods of adminsiter...
06/12/2001
6156772Antagonists of gonadotropin releasing hormone
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both m...
12/05/2000
6124330N-[4-(Heteroarylmethyl)phenyl]-heteroarylamines
The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6 alkyl or a...
09/26/2000
5925766Substituted 3-(aminoalkylamino)-1, 2-benzisoxazoles and related compounds
This application relates to compounds of the formula ##STR1## wherein R1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof;...
07/20/1999
5843975Oxazolidinone derivatives, their preparation and therapeutical use
The present invention relates to isoindole derivatives, and more particularly to 5-(hydroxymethyl)oxazolidine-2-one derivatives which are substituted at the 3 position by an indazole, benzisoxazole or benzisothiazole ring system, to a process for their pr...
12/01/1998
5741799Heterocyclic thrombin inhibitors
Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R1, R2, R3, G, Gx, R6', Ra, Xa, R6, Rb, R3, p, Q, A and R4 are as defined...
04/21/1998
5256681[5(6)-(benzisoxa-,benzisothia-or indazol-3-yl)-1H-benzimidazol-2-yl]carbamates
[5(6)-(benzisoxa-, benzisothia- or indazol-3-yl)-1H-benzimidazol-2-yl]carbamates of formula (I) wherein R1 is hydrogen, C1-4 alkyl, halo, hydroxy or C1-4 alkyloxy; R2 is C1-4 alkyl; and X is O, S, SO,...
10/26/1993
5240923Sulfonamides useful as carbonic anhydrase inhibitors
Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed....
08/31/1993
5223517Heterocyclically substituted cycloalkano[b]-indolesulphonamides
Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydr...
06/29/1993
5169951Process for preparing nematicidal compositions
Nematicidal compositions which comprise as active ingredient compounds of formula I ##STR1## wherein R is nitro or halogen, and also processes for the preparation of the compounds of formula I, novel intermediates of the preparation process and ...
12/08/1992
5128267Naphthotriazolium salts
Naphthotriazolium salts which are chromogenic indicators for reducing substrate, such as NADH or NADPH....
07/07/1992
5099021Process for the preparation of pure, unsymmetrically disubstituted ureas
Process for the preparation of pure, unsymmetrically disubstituted ureas of the general formula ##STR1## in which R denotes a phenyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy, aryloxy...
03/24/1992
5091517Azo dyes containing a 4-aminopyrazolisothiazole diazo compound
The invention relates to novel azo dyes of the formula ##STR1## wherein R1 is an alkyl radical containing 1 to 12 carbon atoms, which is unsubstituted or substituted by hydroxy, alkoxy, cyano or phenyl, or is an aryl radical selected from ...
02/25/1992
5087288Herbicidal thioparaconic acid derivatives
A method of controlling plant growth is provided comprising applying to the plants or to a habitat thereof a herbicidally effective amount of a compound having the structure: ##STR1## wherein R1 is selected from the group consisting of car...
02/11/1992
50415452-hydroxybenzophenone hydrazides and derivatives thereof
Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R1, R2, R3, R4, R5, R6, X, Y...
08/20/1991
5037966Azo dyes containing a 3-aminobenzothienoisothiazole diazo component
Dyes of the formula ##STR1## where R and R1 are independently of the other hydrogen, halogen, nitro, alkyl or alkoxy and KK is the radical of a coupling component, which are particularly suitable for dyeing polyester fibers if no wate...
08/06/1991
5036082Insectidical nitro-substituted heterocyclic compounds
Nitro-substituted heterocyclic compounds of the formula (I) ##STR1## wherein R is hydrogen or alkyl, Z is an optionally substituted aryl or optionally substituted heterocyclic group containing at least one atom selected from N, O and S, A is optional...
07/30/1991
4996316Process for the preparation of tertiary N, N-dimethylamines
A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hy...
02/26/1991
4988711HMG-CoA reductare-inhibiting N-substituted N-amino-pyrroles
Inhibiting HMG-CoA reductase, as in treating hyperlipopproteinaemia, lipoproteinaemia and arteriosclerosis, with the new N-substituted N-amino-pyrroles of the formula ##STR1## in which R1 is an organic radical, R2 is an aryl or ...
01/29/1991
4960901Thermal imaging method
A thermal imaging method is provided which comprises heating imagewise a di- or triarylmethane compound possessing within its di- or triarylmethane structure an aryl group substituted in the ortho position to the meso carbon atom with a moiety ring-closed...
10/02/1990
48823425-alkylbenzimidazoles, method of use and pharmaceutical compositions
The present invention concerns new 5-alkylbenzimidazoles of the formula: ##STR1## wherein R1 is a phenyl ring of the formula: ##STR2## or R1 is naphthyl, heterocycle or a bicyclic heterocycle and R1 -R7
11/21/1989
4785116Aminoisothiazole compounds
Novel compounds of the general formula I ##STR1## where X and Y independently of one another are each carboxyl, a carboxylic ester group, cyano or an unsubstituted or substituted carbamyl or carboxylic hydrazide group and X and Y together form a radi...
11/15/1988
4777168Bicyclic benzo-oxy heterocyclic ethers and thioethers, pharmaceutical compositions and use
A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting parmacological activity, including anti-secretory and anti-ulcerogenic activity, pharaceutical compositions comprising these compounds, and methods for the treatment of ga...
10/11/1988
4772708Derivatives of alkyl-substituted 4-hydroxy-methyl-piperidine
Derivatives of 4-hydroxy-methyl-piperidine having general formula: ##STR1## wherein: R1, R2, R3 and R4 may be alkyl or may form, with the carbon they are bound to, a cycloalkyl group or the group ##STR2## ...
09/20/1988
4760076Benzisothiazole derivatives and their use as insecticides
The invention relates to the use of 3-acylaminobenzisothiazole-S,S-dioxides of the formula I ##STR1## wherein R1 is C1 -C10 alkyl, phenyl, or C1 -C10 alkyl which is substituted by halogen or C
07/26/1988
4748164Bicyclic benzonoid alkylene amino thieno [3,4-D] isothiazole ethers and thioethethers, pharmaceutical compositions and use
A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcero-genic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment o...
05/31/1988
4746746Mitomycin analogs
Novel methods for treatment of neoplastic disease states in animals, which methods comprise administering a therapeutically effective amount of a compound of the formula IIIa, ##STR1## wherein: Y is hydrogen or lower alkyl; and Z is an hydroxy substi...
05/24/1988
4715886Herbicidal pyrazole sulfonamides
Pyrazole sulfonamides are found to have utility as preemergent and/or postemergent herbicides or plant growth regulants....
12/29/1987
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