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Class 546/272.1 - 1,2-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: 369
Last issue date: 10/25/2011


1                    
NumberTitleIssue Date
8044208Imidazole derivatives as inhibitors of TAFIa
The present invention is directed to a compound of formula I: or any stereoisomeric form of the compound of the formula I or a mixture of these forms in any ratio or a physiologically acceptable salt of the compound of the ...
10/25/2011
7414061Aryl-isoxazol-4-yl-imidazole derivatives
The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I: wherein R1 to R6 are as defined in the specification and pharmaceutically acceptable acid add...
08/19/2008
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
73816873-heteroaryl substituted 5-methyloxymethyl isoxazolines used as herbicides
3-Heteroaryl-substituted isoxazolines of the formula I where: X is substituted 5-membered heteroaryl having one to four nitrogen atoms or one to three nitrogen atoms and one oxygen or sulfur atom or one oxygen ...
06/03/2008
7354919Isoxazole compositions useful as inhibitors of ERK
Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compo...
04/08/2008
7338967Substituted isoxazoles as fungicides
The present invention provides compounds of formula I: along with methods of making the same, compostions thereof, and methods of use thereof, particularly methods of use as fungicides. ...
03/04/2008
7332602Pyridyl substituted heterocycles useful for treating or preventing HCV infection
The present invention relates to pyridyl substituted heterocycles and hydro isomers thereof and pharmaceutical compositions thereof that inhibit replication and/or proliferation of HCV virus. The present invention also relates to the use of the pyridyl heterocycles ...
02/19/2008
7302347Method for creating specific, high affinity nuclear receptor pharmaceuticals
This invention pertains to agonists that activate nuclear receptors. These agonists include an extension that contacts a region of the nuclear receptor outside the native ligand binding pocket. Methods for producing, identifying and designing such agonists are inclu...
11/27/2007
7259175Peroxisome proliferator activated receptor modulators
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C
08/21/2007
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
7229999Pyridine-3-carboxamide derivatives as CB1 inverse agonists
The present invention relates to compounds of the formula wherein X and R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds ar...
06/12/2007
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
7211595Farnesyltransferase inhibitors
Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a p...
05/01/2007
7196103Indole derivatives as factor Xa inhibitors
The present invention is directed to the compound of formula I which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibit...
03/27/2007
7179804Tachykinin receptor antagonists
The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins ...
02/20/2007
7169798Inhibitors of c-Jun N terminal kinases (JNK) and other protein kinases
The present invention provides compounds of formula I: where R1 is H, CONH2, T(n)-R, or T(n)-Ar2, n may be zero or one, and G, XYZ, and Q are as described be...
01/30/2007
7125865Therapeutic compounds for treating dyslipidemic conditions
The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.
10/24/2006
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
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
7105549Aryl substituted pyridines and the use thereof
This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1–R4 are set in the specification. The in...
09/12/2006
RE39265Heteroarylpiperidines, 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
7091199Thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives useful as d antagonists
The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These condi...
08/15/2006
7087598Diamide invertebrate pest control agents containing a non-aromatic heterocyclic ring
This invention provides compounds of Formula I, their N-oxides and agriculturally suitable salts wherein A and B are independently O or S; J is an optionally substituted 5- or 6-memebered nonaromatic heterocyclic ring; K is taken together with the two contiguous lin...
08/08/2006
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
7078396Method of treating disorder related to high cholesterol concentration
A method of treating a disorder related to a high cholesterol concentration, comprising administering to a subject in need thereof a compound of formula (I): Also disclosed are methods, kits, combinations, and co...
07/18/2006
7067538MCP-1 receptor antagonists and methods of use thereof
The present invention relates to sulfones that are useful in the treatment of chemokine-mediated disorders. In certain embodiments, the present invention concerns the compounds that are MCP-1 receptor antagonists. ...
06/27/2006
7060710Isoxazole pyrazoloindane derivatives as cognition enhancing GABAα5 subtype ligands
The present invention provides compounds of formula I: in which: one of X and Y is a nitrogen atom substituted by a group R6′ and the other is a carbon atom substituted by an isoxazole group ...
06/13/2006
7056932Heterocyclyl substituted 1-alkoxy acetic acid amides
The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as ...
06/06/2006
70226504-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
7015236-heteroarylnicotinamide derivatives
An N-heteroaryl-4-(haloalkyl)nicotinamide derivative represented by formula (I): [wherein R represents a C1–C6 haloalkyl group; R1 represents a hydrogen atom, a C1–C6...
03/21/2006
6987189Short 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
6974826Imidazolidinedione derivatives 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...
12/13/2005
6964975Isoxazole and thiazole compounds and use thereof as medicine
The present invention relates to novel isoxazole and thiazole compounds having an excellent lysophosphatidic acid (LPA) receptor antagonistic activity represented by general formula [1] or salts thereof: wherein R1 and...
11/15/2005
69169334-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
6908923Compositions and methods for treating heart failure
Certain substituted benzamide derivatives of Formula I: selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including conges...
06/21/2005
6875871Oxazolidinone photoaffinity probes
Disclosed are novel compounds that are useful and effective as photoaffinity probes and methods of using oxazolidinone photoaffinity probes. ...
04/05/2005
6852745Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists
Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositi...
02/08/2005
6835741Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists
Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositi...
12/28/2004
6800642Antipsychotic aminomethyl derivatives of 7,8-dihydro-2,6,9-trioxa-3-aza-cyclopenta[a]naphthalene
Compounds of the formula: useful for treatment of disorders such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperpr...
10/05/2004
6790846Isoxazolone compounds useful in treating diseases associated with unwanted cytokine activity
Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Cr...
09/14/2004
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