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Class 546/271.4 - 1,3-oxazoles (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 oxygen
No. of patents: 619
Last issue date: 05/15/2012


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NumberTitleIssue Date
8178683Antimicrobial ortho-fluorophenyl oxazolidinones for treatment of bacterial infections
The present invention provides certain ortho-fluorophenyl oxazolidinones of the following formula I: or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions contai...
05/15/2012
8158801Violet laser excitable dyes and their method of use
The present invention provides dye compounds optimally excited at about 400 nm and have a Stokes shift of at least about 80 nm. These dyes find use in detection of analyte in a sample and the preparation of dye-conjugates. ...
04/17/2012
8124778Tricyclic inhibitors of fatty acid amide hydrolase
A series of substituted oxazole compounds having an alpha keto side chain at the 2 position and an aromatic, heteroaromatic or heterocycle substituent at the 5 position are disclosed. These compounds exhibit inhibition of fatty acid amid hydrolase and arc useful for...
02/28/2012
7994331Heterocycle-substituted benzimidazole derivative
A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein X1 to X4 independently represent a carbon atom or the like; the ring A represents a 5- to 6-membered heteroaryl having 1 to 4 heteroatoms indep...
08/09/2011
7449583Process for the preparation of 4-(8-chloro-5 6-dihydro-11h-benzo-(5 6)-cyclohepta-(1 2b)-pyridin-11-ylidene-1-piperidiniecarboxylic acid ethyl ester (loratadine)
A process and new oxazolinic intermediates for the preparation of 4-(8-chloro-5,6-dihydro-11H-benzo-[5,6]-cyclohepta-[1,2-b]-pyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester (loratadine) is described. The process starts from 2-(4,4-dimethyl-4,5-dihydrooxa...
11/11/2008
7442486Radiation-sensitive compositions comprising oxazole derivatives and imageable elements based thereon
Radiation-sensitive element comprising: (a) one or more types of monomers each comprising at least one ethylenically unsaturated group accessible to a free-radical polymerization, (b) at least one sensitizer, (c) at least one coinitiator capable of forming free radi...
10/28/2008
7420055Aryl sulfonamides
Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful...
09/02/2008
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
7282501Modulators of peroxisome proliferator activated receptors (PPAR)
The present invention is directed to a compound of formula I, and pharmaceutically acceptable salts, solvates, hydrates or stereoisomer thereof, which are useful in treating Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hyperte...
10/16/2007
7273936Oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors
Novel oxazole and thiazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of tran...
09/25/2007
7253187Heterocyclic 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
7238716Alkanoic acid derivatives process for their production and use thereof
An alkanoic acid derivative useful as a prophylactic or therapeutic agent of diabetes mellitus, hyperlipidemia, impaired glucose tolerance and the like can be provided by a compound represented by the formula whe...
07/03/2007
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
7214678Arylsulfanyl 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
7214693Heterocyclic selective androgen receptor modulators and methods of use thereof
This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and a...
05/08/2007
7211591Carboxylic acid derivative and a pharmaceutical composition containing the derivative as active ingredient
A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate there...
05/01/2007
7199124JNK inhibitor
The present invention relates to a c-Jun N-terminal kinase inhibitor containing an azole compound (I) substituted by a nitrogen-containing aromatic group having substituent(s)(except a compound represented by the formula: ...
04/03/2007
7192974Hydroxymethyl substituted dihydroisoxazole derivatives useful as antibiotic agents
Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, (I) R1a is NH(C═W)R5 or (a); W is O or S; R2 and R3 are for example H or F; R1 is for example hydrogen, or ha...
03/20/2007
71897121,3-Oxazole compounds for the treatment of cancer
Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
03/13/2007
7186738Antibacterial oxalidinones
Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted with: T is for example selected from (TAa1 to TAa12) such...
03/06/2007
7183278Picolinamide derivative and harmful organism control agent comprising said picolinamide derivative as active component
Disclosed are novel compounds useful for the control of harmful organisms, harmful organism control agents using the same, and processes for producing the novel compounds. The useful novel compounds according to the present invention include compounds represented by...
02/27/2007
7173048Indolyl derivatives as liver-X-receptor (LXR) modulators
The invention relates to compounds of formula (I): and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, wherein R1, R2, R3, R4, R5...
02/06/2007
7157456Substituted oxazolidinones and their use in the field of blood coagulation
The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxi...
01/02/2007
7148219Biaryl heterocyclic compounds and methods of making and using the same
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety th...
12/12/2006
7144900Pharmaceutical composition
Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis ...
12/05/2006
7141583Oxazolidinone derivatives with antibiotic activity
Compounds of the formula (I), or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein HET is an N-linked 5-membered heteroaryl ring, optionally substituted on a C atom by an ox...
11/28/2006
7129259Halogenated biaryl heterocyclic compounds and methods of making and using the same
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having at least one halogenated hydrocarbon moiety, a biaryl moiet...
10/31/2006
7122666Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses
Compounds having activity against production of an inflammatory cytokine of formula (I)′: A′ is pyrrole; R1′ is phenyl or naphthyl; R2′ is pyridyl or pyrimidinyl; R3′ is...
10/17/2006
7119104Activator of peroxisome proliferator-activated receptor delta
A compound represented by the formula (I) or a salt of the compound, and a PPAR-δ activator which contains the compound or salt as the active ingredient: (wherein A represents O or S; B
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
7105547Antimicrobial 1-aryl dihydropyridone compounds
The present invention provides antibacterial agents of formula I, or a pharmaceutically acceptable salt thereof. ...
09/12/2006
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
7091360Process for preparing heteroaryl and unsaturated heterocycloalkylmagnesium reagents and uses thereof
The present invention is directed to a novel process for preparing heteroaryl and unsaturated heterocycloalkylmagnesium reagents that are useful in the synthesis of a variety of pharmaceuticals, in particular certain cysteine protease inhibitors. ...
08/15/2006
RE39140Heterocyclic compounds
Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by...
06/20/2006
RE39131Heterocyclic compounds
Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atoms or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted b...
06/13/2006
RE39130Heterocyclic compounds
Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by...
06/13/2006
RE39129Heterocyclic compounds
Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by...
06/13/2006
RE39127Heterocyclic compounds
Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by...
06/13/2006
7056933Heterocyclo-alkylsulfonyl pyrazoles
The present invention relates to heterocyclo alkylsulfonyl pyrazoles of the formula I: wherein the ring of the formula (R5)—A—(SOmR4), m, X, R1 through R5
06/06/2006
7049271Phenyl-substituted 2-enamino-ketonitriles
The present invention relates to novel phenyl-substituted 2-enamino-ketonitriles of the formula (I): in which Ar, X, Z, Y and K are each as defined in the description, to a plurality of pro...
05/23/2006
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