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Class 548/233 - 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 wherein nitro- is bonded directly to ring carbon
No. of patents: 277
Last issue date: 12/20/2011


1              
NumberTitleIssue Date
8080669Process for the synthesis of 2-aminoxazole compounds
The present invention relates to a process for synthesizing in good yield substituted 2-aminoaryloxazole compounds of formula I which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit, bcr-abl, Flt-3 and mutant forms thereof.
12/20/2011
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
7396838Use of 1H-indol-3-yl-2-oxoacetamide compounds
A method of treating cancer including administering to a subject in need thereof an effective amount of a compound of the formula 1: wherein R1, R2, R3, R4, and n are as defined h...
07/08/2008
7368578Five-membered heterocyclic compounds
The present invention provides a compound represented by the formula: wherein R1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom...
05/06/2008
7361654Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory- and immune-associated disea...
04/22/2008
7317030Compounds as inhibitors of cell proliferation and viral infections
The present invention relates to novel compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Z is NH, or ...
01/08/2008
7317024Heterocyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
The invention relates to a class of novel non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have th...
01/08/2008
7307095Inhibitors of cathepsin S
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides m...
12/11/2007
7279582Retroviral protease inhibiting compounds
A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed. ...
10/09/2007
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
7173051Inhibitors of cathepsin S
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides m...
02/06/2007
7126005Process for preparing florfenicol
The present invention is directed to a new process of preparing highly pure Florfenicol. The invention is further directed to new oxazolidine derivatives useful in making Florfenicol and processes of making these derivatives. Examples of such intermediates include (...
10/24/2006
7119113Oxazoles as mGluR1 enhancers
The invention relates to carboxamide derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as mGluR1 enhancers in the treatment and prevention of neurological disor...
10/10/2006
7112599Oxazole compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula wherein R3, R5, R6, R7, and Z, and other variables enumerated under one or more of R3, R5
09/26/2006
7109224Acyl guanidine compounds and use thereof
Acyl guanidine compounds of the following Formula wherein R1, R2, R3, R4 and L are described herein, and pharmaceutical compositions thereof, are useful in treating leu...
09/19/2006
7078422Activator for peroxisome proliferator-activated receptor
A phenylacetic acid derivative represented by the general formula (II) (wherein R11 and R12 each represents hydrogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkyl substituted by one to three halogen atoms, an optionally ...
07/18/2006
6995181Modulators of the glucocorticoid receptor and method
Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the s...
02/07/2006
6972292Certain substituted polyketides, pharmaceutical compositions containing them and their use in treating tumors
The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds ...
12/06/2005
69583483-glyoxylamideindoles for treating cancer
Disclosed is an anti-cancer compound represented by Structural Formula (I): The variables in Structural Formula (I) are described hereinbelow. Also disclosed is a pharmaceutical composition comprising a pharmaceuticall...
10/25/2005
6949567Compounds for the treatment of protozoal diseases
The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C═O, C═S, C═NH, (C═O)2 or SO2; and to pro...
09/27/2005
6924300Oxyiminoalkanoic acid derivatives
To provide a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolera...
08/02/2005
6864254Inhibitor for 20-hete-yielding enzyme
An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular dis...
03/08/2005
6846838Ureido-substituted aniline compounds useful as serine protease inhibitors
Compounds having the formula (I), or pharmaceutically-acceptable salts, hydrates or prodrugs thereof, are effective as inhibitors of Factor VIIa. ...
01/25/2005
6818775Alkyl 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. ...
11/16/2004
6762200Oxa(thia)zolidine derivative and anti-inflammatory drug
The present invention provides medicinal compositions characterized by containing as the active ingredient either a compound represented by a general formula (1) or a pharmaceutically acceptable composite thereof, [where...
07/13/2004
6716881Carbanilides used as pesticides
The present invention provides carbanilides of formula (I), wherein A, Q, R, X, Z and m are as defined herein. A plurality of processes for preparing these compounds is provided, along with methods of using the compounds...
04/06/2004
6706920Antistatic composition
An antistatic composition comprises (a) at least one ionic salt consisting of a nonpolymeric nitrogen onium cation and a weakly coordinating fluoroorganic anion, the conjugate acid of the anion being a superacid; and (b) at least one thermoplastic polymer. The compo...
03/16/2004
6686476Substituted 1-aryl-3-heteroaryl-thioureas and substituted 1-aryl-3-heteroaryl-isothioureas as antiatherosclerotic agents
Antiatherosclerotic agents are provided which are represented by Formulas I or II: ##STR1## wherein R is ##STR2## wherein R9, R10, R11, R12, R13, and R14 are each, independently, hydro...
02/03/2004
6680337Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents
The present invention provides cyclopentane heptanoic acid, 2 heteroaryl alkyl or alkenyl derivatives which may be substituted in the 1-position with hydroxyl, alkyloxy, amino and amido groups, e.g. 1-OH cyclopentane heptanoic acid, 2 heteroarylalkenyl de...
01/20/2004
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
6677360Biphenyl and biphenyl-analogous compounds as integrin antagonists
The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophyl...
01/13/2004
6677353Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating...
01/13/2004
6653330Amide-type triazole compounds
A compound of formula (I) or a pharmacologically acceptable prodrug or salt thereof which exhibits excellent antifungal activity: ##STR1## wherein Ar1 represents a phenyl group or the like; Ar2 represents a phenylene group or the lik...
11/25/2003
6653321Naphthylsulfonic acids and related compounds as glucose uptake agonists
Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptabl...
11/25/2003
6653483Alkyl or aryl substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity....
11/25/2003
6620963TRICYCLO[6.2.202,7]DODECA-2(7),3,5-TRIEN-4-CARBONYLAMINO-PHENYL AND TRICYCLO[6.2.202,7]DODECA-2(7),3,5-TRIEN-4-CARBONYLAMINO-HETEROARYL AND RELATED COMPOUNDS HAVING RAR଱ RECEPTOR SELECTIVE BIOLOGICAL ACTIVITY
Compounds of the formula ##STR1## where the variables have the meaning defined in the specification, which bind specifically or selectively to to RAR଱ retinoid receptors....
09/16/2003
6605629Neurotrophin production secretion promoting agent
A neurotrophin production/secretion promoting agent which comprises an azole derivative of the formula: ##STR1## wherein R1 represents a halogen atom, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionall...
08/12/2003
6596747Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
Compounds having the formula (I), ##STR1## are effective as inhibitors of IMPDH enzyme and/or serine protease Factor VIIa, wherein B is a monocyclic or bicyclic carbocyclic or heterocyclic ring, D is a monocyclic or bicyclic carbocyclic or heterocyclic ri...
07/22/2003
6596743Carbamic acid derivatives
The present invention is a compound of formula: ##STR1## wherein R1, R2, R2', X, A1 /A2 and B are as defined in the specification. These compounds may be used in the control or prevention of acute and/or ...
07/22/2003
6586433Substituted N-heteroaryl-N-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating...
07/01/2003
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