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Class 548/244 - Nitrogen bonded directly to ring carbon of the oxazole ring


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which nitrogen is bonded directly to ring carbon
No. of patents: 78
Last issue date: 04/10/2007


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NumberTitleIssue Date
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
7084163Heterocyclic carboxamides and their use as fungicides
Compounds of general formula (I), in which Het represents a five or six membered saturated, partially unsaturated or aromatic ring containing between one and six heteroatoms of the group N, O, S, in which the heterocycle is substituted in an adjacent manner with -P-...
08/01/2006
7081538Substituted isoxazolines and their use as antibacterial agents
Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, X is O, S or NH; HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selecte...
07/25/2006
68358423-nitroisoxazoles and their use in the protection of materials
The 3-nitroisoxazoles of the formula (I) in which R1 and R2 are each as defined in the description, some of which are known, are highly suitable for use as biocides for pr...
12/28/2004
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
6746989Substituted benzoylpyrazoles as herbicides
The invention relates to novel substituted benzoylpyrazoles of the general formula (I), in which n represents the numbers 0, 1, 2 or 3, A represents a single bond or represents alkanediyl(alkylene), ...
06/08/2004
6420567N-heteroaryl aryl-substituted thienyl-furyl-and pyrrolyl-sulfonamides and derviatives thereof that modulate the activity of endothelin
Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, ...
07/16/2002
6387915Isoxazole-sulfonamide endothelin antagonists
Isoxazole-sulfonamide endothelin antagonists of formula (I) below having good affinity for endothelin receptors and selectivity for ETA over ETB are described herein. ##STR1## Such compounds are useful in the treatment of conditions ...
05/14/2002
6384066Sulphonyltriazol derivatives and their use for combating micro-organisms
Novel sulphonyltriazole derivatives of the formula ##STR1## in which Hal represents fluorine, chlorine or bromine, R1 represents hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkylaminocarbonyl, optionally substituted phenyl, optionally substituted ...
05/07/2002
6331637N-Alkyl, N-Alkenyl, N-Alkynyl, N-Aryl and N-fused bicyclo or tricyclo thienyl-, furyl-,and Pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
N-alkyl, N-alkenyl, N-alkynyl, N-aryl and N-fused bicyclo or tricyclo thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, (phenyl) and (phenoxy)th...
12/18/2001
6107320Phenyl sulfonamide endothelin antagonists
Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R1, R2 and R3 are each independently (a) hydrogen, except that R1 is other than hydrogen; (b) alkyl, alke...
08/22/2000
6080774Substituted biphenylsulfonamide endothelin antagonists
Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: ##STR2## R2 and R3 are each independently (a) hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, ...
06/27/2000
6057342Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof
The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH2 a...
05/02/2000
6022977Dynamic resolution of isoxazoline thioesters to isoxazoline carboxylic acids
The present invention relates generally to a novel method for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the ...
02/08/2000
6020354Halobenzimidazoles and their use as microbicides
New halogenobenzimidazoles of the formula in which A, R1, R2, R3, R4 and X have the meanings given in the description, and their acid addition salts and metal salt complexes, a process for their preparation and their use ...
02/01/2000
5962490Thienyl-, furyl- and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)-furylsulfonamides and N-(isoxazolyl)pyrrolyl...
10/05/1999
5939418Isoxazoline, isothiazoline and pyrazoline factor Xa inhibitors
Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders. ...
08/17/1999
5935973Heterocyclcarboxamide derivatives and their use as therapeutic agents
Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R1 is an optional substituent; U is an alkylene chain optionally substituted by one or more...
08/10/1999
5856507Methods for the preparation of biphenyl isoxazole sulfonamides
Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endo...
01/05/1999
56864343-aryl-2-isoxazolines as antiinflammatory agents
This invention relates to 3-aryl-2-isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDEIV). The 3-aryl-2-isoxazolines are useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulm...
11/11/1997
5621109Retroviral protease inhibiting compounds
A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein the terms R1, R2, R5, R6, Y, Y', m and n are herein defined....
04/15/1997
5599942Taxoid intermediates
Taxoids having a 1,3-oxazole containing moiety at the 13-position of the taxane nucleus....
02/04/1997
5594021Thienyl-, furyl- and pyrrolyl sulfonamides and derivatives thereof that modulate the activity of endothelin
Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolyls...
01/14/1997
5591761Thiophenyl-, furyl-and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
Thiophenyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, isoxazolyl-thiophenyl-sulfonamides, isoxazolyl-furyl-sulfonamides and isoxazolyl-pyrrolyl-s...
01/07/1997
5580894Isoxazolyl enaminones
An oxazolyl enaminone is provided having the formula: ##STR1## wherein R1 is selected from the group consisting of a branched or unbranched alkyl groups containing from 1 to 4 carbon atoms and R2 is selected from the group consi...
12/03/1996
5571821Sulfonamides and derivatives thereof that modulate the activity of endothelin
Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administeri...
11/05/1996
5571810Thiophene derivatives
This invention relates to new thiophene derivatives having antiinflammatory and analgesic activities and represented by the general formula [I]: ##STR1## wherein R1 is hydrogen, halogen, cyano, substituted lower alkyl, substituted or unsub...
11/05/1996
5523302Aromatic compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other thera...
06/04/1996
5514691N-(4-halo-isoxazolyl)-sulfonamides and derivatives thereof that modulate the activity of endothelin
N-(4-halo-isoxazolyl)sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(4-halo-3-isoxazolyl)sulfonamides and N-(4-halo-5-isoxazolyl)benzenesulfonamides and methods for inhi...
05/07/1996
5514696Phenyl sulfonamide endothelin antagonists
Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R1, R2 and R3 are each independently (a) hydrogen, except that R1 is other than hydrogen; (b) alkyl, alke...
05/07/1996
5464853N-(5-isoxazolyl)biphenylsulfonamides, N-(3-isoxazolyl)biphenylsulfonamides and derivatives thereof that modulate the activity of endothelin
N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazol...
11/07/1995
5378715Sulfonamide endothelin antagonists
Compounds of the formula ##STR1## inhibit endothelin, wherein: one of X and Y is N and the other is O; R is naphthyl or naphthyl substituted with R1, R2 and R3 ; R1, R2 and R3 are each inde...
01/03/1995
5318720Liquid crystal composition, liquid crystal device, display apparatus and display method
A mesomorphic compound represented by the following formula (I): ##STR1## wherein R1 and R2 respectively denote an alkyl group or alkoxy group each having 4-16 carbon atoms optionally substituted, halogen, --CN or --CF3.
06/07/1994
5292737N,N'-bis(sulfonamido)-2-amino-4-iminonaphthalen-1-ones and N,N'-bis(amido)-2-amino-4-iminonaphthalen-1-ones
N,N'-Bis(sulfonamido)-2-amino-4-iminonaphthalen-1-ones and N,N'-Bis(amido)-2-amino-4-iminonaphthalen-1-ones are disclosed. Methods of inhibiting protein kinase C activity which comprises contacting protein kinase C with an effective amount of an N,N'...
03/08/1994
52908023-substituted-2-oxindole derivatives
This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H
03/01/1994
52739893,5-disubstituted 2-isoxazolines and isoxazoles, agents containing them and their use
Novel 3,5-disubstituted 2-isoxazolines and isoxazoles and novel pharmaceuticals are described which are suitable, in particular, for the prophylaxis and/or treatment of pathological, neurodegenerative disorders in humans and animals. Processes for the pre...
12/28/1993
5256784Nonlineaphores and polymers incorporating such nonlineaphores
Nonlinear-optic (NLO) compositions containing functionalized merocyanine dyes, such that the molecules, comprising the NLO-active compositions have a functional group at each end of the molecule and each functional group differing in reactivity, thus perm...
10/26/1993
5245040Process for the preparation of nitroguanidine derivatives
A process for the preparation of 1,3-disubstituted 2-nitroguanidines of the formula I ##STR1## in which R1 is hydrogen or C1 -C4 alkyl, R2 is hydrogen, C1 -C6 alkyl, C3 -C
09/14/1993
5207816Cyclohexenone derivatives and their use for controlling undesirable plant growth
Cyclohexenone derivatives of the formula ##STR1## where R1 is alkyl, R2 is alkyl, unsubstituted or halogen-substituted alkenyl or alkynyl, X is a substituted or unsubstituted five-membered heteroaromatic radical, and Z is hydrog...
05/04/1993
5196541Process for the preparation of substituted 3-aminoacrylic esters
There is described a new process for the preparation of substituted 3-aminoacrylic esters of the general formula (I) ##STR1## in which R1, R2, R3, R4, X and n have the meaning given in the description. The ...
03/23/1993
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