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Class 514/405 - Polycyclo ring system having the diazole ring as one of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the 1,2-diazole ring is one of the
No. of patents: 159
Last issue date: 01/24/2012


1        
NumberTitleIssue Date
8101644Pyrrolinone derivative and pharmaceutical composition comprising the same
The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the des...
01/24/2012
80844856-(aminoalkyl)indazoles
6-(Aminoalkyl)indazoles of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, and renal, cardiac and vascular protecting medicinally active ingredients. ...
12/27/2011
8063091Indazole, benzisoxazole, and benzisothiazole kinase inhibitors
Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using th...
11/22/2011
8053459Selenolopyrazole derivatives and use thereof as anticancer agents
The present invention synthesizes a series of selenolo[3,2-c]pyrazole and selenolo[2,3-c]pyrazole derivatives, and discovers their anticancer activity. ...
11/08/2011
7968583Substituted pyrrolo-pyrazole derivatives active as kinase inhibitors
Substituted pyrrolo-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...
06/28/2011
7846959Raf modulators and methods of use
The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell...
12/07/2010
7842712Indazolinone compositions useful as kinase inhibitors
The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK...
11/30/2010
7820707Heterocyclic derivatives
The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention...
10/26/2010
7816390N-substituted tricyclic 3-aminopyrazoles as anti-mitotic tubulin polymerization inhibitors
The invention is directed to compounds having the following structures: N-(3-ethoxyphenyl)-1,4-dihydro-6-ethoxy-7-(3-hydroxypropoxy)-1-methylindeno[1,2-c]pyrazole-3-amine; 3-[3-(3...
10/19/2010
78038303-amino-1-arylpropyl indoles and AZA-substituted indoles and uses thereof
The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb...
09/28/2010
7772268Diacyl indazole derivatives as lipase and phospholipase inhibitors
The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of t...
08/10/2010
7767705Compounds that inhibit TRPV1 and uses thereof
Compounds of formula (I) wherein R3, R7, R9 and L are defined in the description are TRPV1 antagonists that exhibit low inhibitory activity against CYP3A4. Compositions comprising such compo...
08/03/2010
76259371H-benzo[F]indazol-5-YL derivatives as selective glucocorticoid receptor modulators
The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and infl...
12/01/2009
7622492Pyrazolones as inhibitors of 11β-hydroxysteroid dehydrogenase
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...
11/24/2009
7612106Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof
The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor.
11/03/2009
7582669Aminoindazole 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 heteroaryl fused to a (1-10C) cycloalkyl...
09/01/2009
75413761H-indazole compounds
The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Whe...
06/02/2009
7517901p38 MAP kinase inhibitors and methods for using the same
Compounds of formula Ia or Ib: wherein X and Y are nitrogen or CRe, and R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the...
04/14/2009
7514463Lonidamine analogues and their use in male contraception and cancer treatment
Novel compounds useful for inhibiting spermatogenesis and cancer treatment, and in particular as inhibitors of heat shock proteins and/or elongation factor 1 alpha. ...
04/07/2009
7473701Substituted indazoles, compositions containing them, method of production and use
Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particular in oncology. ...
01/06/2009
7449488Pyrazolopyrimidines as protein kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, me...
11/11/2008
7425572Use 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
7407950-(heteroaryl)-1-indole-2-carboxamide derivatives and their use as vanilloid TRPV1 receptor ligands
The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein.
08/05/2008
7390797Fused indazole compounds
The present invention provides a novel fused indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. ...
06/24/2008
7354928Small molecule inhibitors targeted at Bcl-2
The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bin...
04/08/2008
7354944Thiadiazole compounds and methods of use
The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnorm...
04/08/2008
7342046Gossypol co-crystals and the use thereof
This invention relates to compositions comprising co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co-crystals of (...
03/11/2008
7338972Substituted 1-alkylamino-1H-indazoles for the treatment of glaucoma
Substituted 1-alkylamino-1H-indazoles for lowering intraocular pressure and treating glaucoma are disclosed. ...
03/04/2008
7312239Medicament for prevention and/or therapy of arterial wall disorder
An object of the present invention is to provide a medicament and method which is useful for prevention and/or therapy of arterial wall injury. According to the present invention, there is provided a method for prevention and/or therapy of arterial wall injury which...
12/25/2007
7300950Pyrazole derivatives, their preparation and their use in pharmaceuticals
The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: in which X, R1, R1a, R2, R3, R4 a...
11/27/2007
7291612Immunomodulatory compounds
The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthri...
11/06/2007
7285553Serotonergic 5HTreceptor compounds for treating ocular and CNS disorders
Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for...
10/23/2007
7262200Indazolinone compositions useful as kinase inhibitors
The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK...
08/28/2007
7259183Indole, indazole and indoline derivatives as CETP inhibitors
The present invention relates to compounds of formula (I): wherein —X—Y—, R1 to R11 and n are as defined in the description and claims, and pharmaceutically acceptable salts thereof. T...
08/21/2007
7241792Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof
The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor.
07/10/2007
7226941Compound for treating angiogenesis
The present invention provides methods and pharmaceutical compositions for inhibiting expressions of HIF and HIF regulated genes, inhibiting angiogenesis, inducing cell cycle arrest in tumor cells, and treating cell proliferating diseases or conditions. ...
06/05/2007
7214699Indazole derivatives as CRF antagonists
This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein R3 is optionally substituted aryl or heteroaryl, R1...
05/08/2007
7211597Substituted pyrazolyl compounds for the treatment of inflammation
The present invention relates to compounds of Formula I: wherein A is (CH2)m-Q-(CH2)n, wherein each CH2 may be independently substituted with one or more substitut...
05/01/2007
7208512Benzodifuranimidazoline and benzofuranimidazoline derivatives and their use for the treatment of glaucoma
The present invention provides benzodifuran imidazoline derivatives and benzofuran imidazoline derivatives for lowering intraocular pressure and providing ocular neuroprotection. ...
04/24/2007
7199147Rho kinase inhibitors
A compound represented by the formula (1): wherein R1—X— indicates that 1 to 4 R1—X— groups are present which may be the same or different, the rin...
04/03/2007
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