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Class 514/406 - Pyrazoles


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the 1,2-diazole ring is pyrazole
No. of patents: 1098
Last issue date: 05/29/2012


1                      
NumberTitleIssue Date
8188135Compounds as cannabinoid receptor ligands
Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and met...
05/29/2012
8178573Compounds
The present invention provides compounds of formula (I): pharmaceutical compositions comprising the compounds and the use of the compounds for the manufacture of a medicament, particularly for the treatment of inflammation ...
05/15/2012
8148417Primary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in th...
04/03/2012
8148416Treatment of inflammatory, cancer, and thrombosis disorders
A pharmaceutical composition and a method of treating inflammation in a mammal. The method administers the therapeutic composition to the mammal. The therapeutic composition includes: a standard therapeutic dose of a COX2 inhibitor consisting of celecoxib or rofecox...
04/03/2012
8148418Ethers, secondary amines and derivatives thereof as modulators of the 5-HTserotonin receptor useful for the treatment of disorders related thereto
The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment...
04/03/2012
8143302Methods and compositions for diagnostic and therapeutic targeting of COX-2
The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell an...
03/27/2012
81382171H-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors
Thieno[2,3-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful...
03/20/2012
8124641Aminotetrahydroindazoloacetic acids
The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, R1-R3 and n are defined in the detailed description and claims. In addition, the present inven...
02/28/2012
8119682Iodopyrazolyl carboxanilides
This invention relates to novel intermediates used in the preparation of iodopyrazolylcarboxanilides of the formula (I) in which R1, R2, R3, R4, R5, R6 and Z...
02/21/2012
81196812-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta [ƒ]indazole-5-YL]ethyl phenyl derivatives as glucocorticoid receptor ligands
The present invention is directed to 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases ...
02/21/2012
81148992H- or 3H-benzo[e]indazol-1-yl carbamate derivatives, the preparation and therapeutic use thereof
Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the inve...
02/14/2012
8097641Heterocyclyl substituted tetrahydronaphthalene derivatives as 5-HT7 receptor ligands
The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen compounds of general formula (I), methods for their preparation, and compositions comprising these compounds as well as their use for the treatment or prophylaxis of various disorders in...
01/17/2012
8088814Methods and compositions for the treatment of psychiatric disorders
A method for the prevention, treatment, or inhibition of a psychiatric disorder, in particular schizophrenia, is described which comprises administering a COX-2 inhibitor or prodrug thereof to a subject. Moreover, a method for the prevention, treatment, or inhibitio...
01/03/2012
8084486Substituted arylpyrazoles
This invention relates to a combination product comprising a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7 and R9 are as ...
12/27/2011
8080574PDK-1/Akt signaling inhibitors
Use of a new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I for inducing apoptosis in unwanted rapidly proliferating cells, for treating, inhibiting, or delaying the onset of cancer, and for preventing restenosis in a subject that has u...
12/20/2011
8044083Kinase inhibitors and methods of use thereof
The compound of Formula (I) and pharmaceutically acceptable salts and prodrugs thereof are useful in the treatment and prevention of various disorders mediated by kinases. ...
10/25/2011
8039502Anti-infective agents against intracellular pathogens
A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from
10/18/2011
7998996Substituted pyrazoline compounds for reducing triglycerides in blood
The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal. ...
08/16/2011
7981917Methods and compositions for including apoptosis by stimulating ER stress
The present invention provides a method for inducing apoptosis in selected cells by aggravating ER-stress. The aggravation of ER-stress is achieved in a specific manner by inhibiting SERCA (sarcoplasmic/endoplasmic reticulum calcium ATPase), leading to elevated leve...
07/19/2011
7981918Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I...
07/19/2011
7977368Pyrazolopyrrolidines as inhibitors of gamma secretase
The invention provides compounds of Formula I wherein A, Y, R1, R1a, R2, and R2a are as described in the specification. Compounds of Formula I are useful in treating and/or preven...
07/12/2011
7968584Substituted arylpyrazoles
This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthes...
06/28/2011
7960426Substituted arylpyrazoles
This invention relates to a combination product comprising a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7 and R9 are as ...
06/14/2011
7960425Pyrazole compounds and thrombopoietin receptor activators
A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
06/14/2011
7951831Use of inhibitors of soluble epoxide hydrolase to synergize activity of COX and 5-LOX inhibitors
The invention relates to methods, compositions, and uses of those compositions for making medicaments, for potentiating the beneficial effects of inhibitors of COX-1, COX-2, and 5-LOX, and reducing adverse effects, by also administering inhibitors of soluble epoxide...
05/31/2011
7951832Pyrazole derivatives as kinase inhibitors
The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: wherein X is a six-member ring selected from phenyl, pyridine, or pyrimidine; Y is H, an alkenyl, a sub...
05/31/2011
7951833Crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]Benzoic acid 471
New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described. ...
05/31/2011
7947728Indole and indazole analogs as glycogen synthase activators
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositi...
05/24/2011
7947727Compounds
The present invention provides compounds of formula (I): a process for their preparation, pharmaceutical compositions comprising the compounds and the preparation of said compositions, intermediates and use of the compounds...
05/24/2011
7947726Non-steroidal ligands for the glucocorticoid receptor, and compositions thereof
The invention provides non-steroidal ligands for the glucocorticoid receptor, methods for making non-steroidal ligands of the glucocorticoid receptor, compositions of non-steroidal ligands of the glucocorticoid receptor and methods of using non-steroidal ligands and...
05/24/2011
7943653Substituted 5-vinylphenyl-1-phenyl-pyrazole cannabinoid modulators
This invention is directed to a cannabinoid modulator compound of formula (I): or a form thereof, and methods for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
05/17/2011
7932283Fungicide N-cyclopropyl-sulfonylamide derivatives
The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods fo...
04/26/2011
7919517Indazole derivatives
The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each repres...
04/05/2011
79195181-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40
The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present i...
04/05/2011
7897634Pyrazoles for the treatment of obesity and other CNS disorders
This invention relates to compounds of the formulas (1), (2) and (3) having pharmacological activity, to compositions containing these compounds, and to methods of treatment employing the compounds and compositions. ...
03/01/2011
7893098Pyrrole and pyrazole DAAO inhibitors
Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss ...
02/22/2011
7893099Cyclopentane derivatives
The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. ...
02/22/2011
7888381Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity, and use thereof
Non-steroidal compounds are provided 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 the structure of formula (I)
02/15/2011
7879897Pesticidal 5-substituted-oxyalkylamino-1-arylpyrazole derivatives
The invention relates to 5-sub-stituted-oxyalkylaminopyrazole derivatives of the formula or salts thereof wherein the various symbols are as defined in the description, to processes for their preparation, to compositions th...
02/01/2011
7879898Hepatocyte growth factor pathway activators in chronic obstructive pulmonary disease
Methods are provided for treating chronic obstructive pulmonary diseases such as emphysema using compounds that activate the signaling pathways of hepatocyte growth factor. ...
02/01/2011
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