Class 546/211 - 1,2-diazole (including hydrogenated)

Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring consists of
No. of patents: 271
Last issue date: 12/20/2011

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Number	Title	Issue Date
8080666	3,4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinase and glycogen synthase kinase-3 modulators The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3....	12/20/2011
8013163	4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide acid addition salts as kinase inhibitors The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. Also pr...	09/06/2011
7608718	4,5-dihydro-1H-pyrazole derivatives having potent CB-antagonistic activity The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have...	10/27/2009
7576218	4-phenylpiperdine-pyrazole CCR1 antagonists Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-me...	08/18/2009
7521562	Filters for electronic display devices The present invention provides a filter for electronic display devices, comprising a squarylium compound represented by General Formula (I): [wherein R1 and R2 may be the same or different and each rep...	04/21/2009
7432379	Substituted pyrazole derivatives and related compounds as bradykinin Breceptor antagonists Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds ...	10/07/2008
7429581	Pyrazole-derivatives as factor Xa inhibitors The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is...	09/30/2008
7423052	Piperidine compounds for use as orexin receptor antagoinst A invention relates to N aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists. ...	09/09/2008
7407972	Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thro...	08/05/2008
7396929	Synthesis of 3-amino-4-substituted pyrazole derivatives This application discloses a novel process to synthesize 3-amino-4-substituted pyrazole derivatives, which may be used, for example, as intermediates to prepare compounds having, for example, pharmaceutical utility. ...	07/08/2008
7393842	Pyrazole analogs acting on cannabinoid receptors One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the i...	07/01/2008
7381721	Substituted piperidine compounds 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as anta...	06/03/2008
7332508	Substituted homopiperidine, piperidine or pyrrolidine derivatives A novel class of substituted homopiperidine, piperidine and pyrrolidine derivatives, methods for their preparation, pharmaceutical compositions comprising them and use thereof in the treatment of disorders related to the histamine H3 receptor. More particularly, the...	02/19/2008
7326705	Heterocyclic sodium/proton exchange inhibitors and method Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, al...	02/05/2008
7312218	Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or hetero...	12/25/2007
7291632	Substituted 2-carbonylamino-6-piperidinaminopyridines and substituted 1-carbonylamino-3-piperidinaminobenzenes as 5-HT agonists The present invention relates to compounds of formula I: (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is C(R3c═ or N═; R1 is C2–C6 alkyl, substituted C2–C6 alkyl, ...	11/06/2007
7285554	Pyrazole derivative Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors conta...	10/23/2007
7259157	N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain. ...	08/21/2007
7253186	N-substituted piperidine derivatives as serotonin receptor agents Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contac...	08/07/2007
7253170	Pyrazole-amine compounds useful as kinase inhibitors The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5...	08/07/2007
7247635	Pyrazole derivative Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors conta...	07/24/2007
7217714	CCR5 modulators Compounds of Formula 1 [Region α]−[Region β]−[Region γ]−[Region δ] (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...	05/15/2007
7189679	Herbicidal 3-amino-2-thiomethylbenzoylpyrazoles 3-Amino-2-thiomethylbenzoylpyrazoles of the formula (I) and their use as herbicides are described. In this formula (I) R1 to R9 are various radicals. ...	03/13/2007
7157472	Neuropeptide Y Y5 receptor antagonists The present invention discloses compounds which, are receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as me...	01/02/2007
7153868	N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a c...	12/26/2006
7141585	Pyrazole derivatives This invention relates to the use of pyrazole derivatives of the formula and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain ...	11/28/2006
7119108	Pyrazole derivatives as cannabinoid receptor antagonists Novel cannabimimetic pyrazole derivatives are presented which have preferentially high affinities for both of the cannabinoid CB1 or CB2 receptor sites. The improved receptor affinity makes these analogs useful as experimental tools for cannabinoid receptor studies ...	10/10/2006
7115635	Benzylpiperidine compound The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following ben...	10/03/2006
7105556	Conformationally 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
7091350	Diaminopyrazole derivatives and their use for oxidation dyeing of keratinous fibres The invention relates to diaminopyrazole derivatives having the following structure (I), wherein R1 represents an alkyl or alkenyl radical bearing at least one substituent selected from among OR, NRR′, SR, SOR, SO2R, COOR, CONRR′, PO(OH)	08/15/2006
7067656	Sulfamoyl compounds and agricultural and horticultural fungicides A sulfamoyl compound of the general formulae (1): wherein R1 and R2 are each independently C1-4 alkyl, or R1 and R2 togeth...	06/27/2006
7034049	3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents Compounds which are 3-amino-pyrazole derivatives represented by formula (I) wherein R is C3–C6 cycloalkyl group optionally substituted by a straight or branched C1–C6 alkyl or arylalkyl group; R1 is a straig...	04/25/2006
7009056	Blockade of voltage dependent sodium channels Compounds of formula (I), and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis. ...	03/07/2006
6974810	4,5-Dihydro-1H-pyrazole derivatives having potent CB1-antagonistic activity The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have...	12/13/2005
6958339	Pyrazole derivative The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal co...	10/25/2005
6958350	Chemical compounds The invention provides a compound of formula (I): wherein R1, R2, R3, R4, R5, N, X and Y are as defined in the specification, processes, for their preparation, pharmaceutical compositions containing them, and th...	10/25/2005
6953793	Substituted pyrazoles Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described. ...	10/11/2005
6894173	Intermediates useful for synthesis of heteroaryl-substituted urea compounds, and processes of making same Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic co...	05/17/2005
6890928	Aromatic sulfone hydroxamic acids and their use as protease inhibitors This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This inventi...	05/10/2005
6864249	Piperidine and azetidine thrombin inhibitors The present invention relates to a compound having formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of the class of thrombin inhib...	03/08/2005

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Class 546/211 - 1,2-diazole (including hydrogenated)