Class 544/140 - 1,2-Diazole ring (including hydrogenated)

Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the five-membered hetero ring has ringnitrogens
No. of patents: 250
Last issue date: 07/12/2011

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Number	Title	Issue Date
7977477	Benzimidazole derivatives and their use as protein kinase inhibitors The invention provides compounds of the formula (I): The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Auroa kinases and are therefore useful to treat cancer and viral diseases. ...	07/12/2011
7652135	Compositions useful as inhibitors of protein kinases The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein A, B, Q, R1, and R2 are as described in the specification. These compounds are inhibi...	01/26/2010
7511136	Aminoindazole derivatives active as kinase inhibitors Compounds which are 3-aminoindazole derivatives or pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or compositions are useful in the treatment of diseases caused by and/or associated...	03/31/2009
7425572	Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma Novel dioxinoindazole compounds and dioxoloindazole compounds are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions of one or more of...	09/16/2008
7348427	Antipathogenic benzamide compounds Antipathogenic benzamide compounds having the formula wherein at least one of the R1 groups is F, Cl, CN or CF3 and R2, R3, Y, Z, m, and n are as defined herein. ...	03/25/2008
7342037	Anti-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...	03/11/2008
7329657	Indazolyl-substituted pyrroline compounds as kinase inhibitors The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or am...	02/12/2008
7304060	Indazolyl-substituted pyrroline compounds as kinase inhibitors The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or am...	12/04/2007
7282498	Substituted fused pyrroleoximes and fused pyrazoleoximes Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, ant...	10/16/2007
7282499	Sigma receptor inhibitors The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to some pyrazole derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy...	10/16/2007
7279476	Pyrazole-derived kinase inhibitors and uses thereof Described herein are compounds that are useful as protein kinase inhibitors having the formula: where B, R1, n, R3, Q, and R4 are described in the specification. The compounds are...	10/09/2007
7247628	Cannabinoid receptor ligands and uses thereof Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment diseases, conditions and/or disorders herein. ...	07/24/2007
7196082	Ophthalmic compositions for treating ocular hypertension This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the us...	03/27/2007
7196109	Aminoindazole derivatives as medicaments and pharmaceutical compositions including them The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl...	03/27/2007
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
7179804	Tachykinin 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
7166629	Aminoindazole derivatives as medicaments and pharmaceutical compositions including them The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or h...	01/23/2007
7144911	Anti-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...	12/05/2006
7141568	Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them Pyrrolo[3,4-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 usefu...	11/28/2006
7091340	Polymorphs Disclosed are polymorphs of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea and processes from making the same. ...	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
7064123	Compounds and compositions as cathepsin inhibitors The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making. ...	06/20/2006
7041669	1,4-benzofused urea compounds useful in treating cytokine mediated diseases Disclosed are 1,4-disubstituted benzo-fused urea compounds of formula (I): wherein Ar, X, A, L, and Q of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes an...	05/09/2006
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
6979685	Cycloalkyl amine compounds and uses thereof Aminocycloalkyl compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of a...	12/27/2005
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
6964975	Isoxazole 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
6956036	6-hydroxy-indazole derivatives for treating glaucoma Substituted 1-(α-alkyl-ethylamino)-1H-indazol-6-ols useful for lowering and controlling IOP and treating glaucoma are disclosed ...	10/18/2005
6949579	Aminoindazole derivatives and intermediates, preparation thereof, and pharmaceutical compositions thereof The present invention relates to the novel indazole derivatives of general formula (I): in which: R is either O, S or NH; R3 is an alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, aryl, heterocycle, cycloalkyl, alk...	09/27/2005
6916924	Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents This invention relates to novel processes for preparing heteroaryl-substituted urea compounds of formula (I): which are useful for treating diseases and pathological conditions involving inflammation such as chronic in...	07/12/2005
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
6875789	Pyrazole-derived kinase inhibitors and uses thereof Described herein are compounds that are useful as protein kinase inhibitors having the formula: where B, R1, n, R3, Q, and R4 are described in the specification. The compounds are usefu...	04/05/2005
6852717	Compounds useful as anti-inflammatory agents Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds. ...	02/08/2005
6774233	Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents 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 c...	08/10/2004
6753426	Polymorph and process for preparing same Disclosed are processes, polymorph and 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 com...	06/22/2004
6753329	Inhibitors of cyclin-dependent kinases, compositions and uses related thereto The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and conse...	06/22/2004
6730671	Compounds useful as reversible inhibitors of cathespin S Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.	05/04/2004
6727246	1-(aminoalkyl)-3-sulfonylindole-and-indazole derivatives as 5-hydroxytryptamine-6 ligands The present invention provides compounds of formula I and the use thereof for the treatment of central nervous system disorders related to or affected by the 5-HT6 receptor. ...	04/27/2004
6720317	Inhibitors of factor Xa Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders. ...	04/13/2004
6716841	Nitrogen containing heterobicycles as factor Xa inhibitors This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the s...	04/06/2004

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Class 544/140 - 1,2-Diazole ring (including hydrogenated)