Tricyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 548/359.1)
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Patent number: 9012478Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: GrantFiled: July 3, 2013Date of Patent: April 21, 2015Assignee: Arena Pharmaceuticals, Inc.Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
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Publication number: 20150051177Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.Type: ApplicationFiled: October 31, 2014Publication date: February 19, 2015Inventor: Darren Orton
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Publication number: 20150005357Abstract: The present invention relates to the development of novel substituted 4,5-dihydro-2H-benzo[e]indazole-9-carboxylates, which can be used as therapeutic agents for the treatment and prevention of metabolic disorders, and a process of preparing said novel compounds. More particularly, the present invention relates to substituted 4,5-dihydro-2H-benzo[e]indazole-9-carboxylates and their related compounds, processes for preparing the said compounds and to their use in the treatment of diabetes and related metabolic disorders.Type: ApplicationFiled: January 29, 2013Publication date: January 1, 2015Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Atul Goel, Gaurav Taneja, Neha Rahuja, Arun Kumar Rawat, Natasha Jaiswal, Akhilesh Kumar Tamrakar, Arvind Kumar Srivastava
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Publication number: 20140343294Abstract: Compounds of formula (I): wherein: A, R, T, Q, L, Z, G, X and A? are as defined in the description. B and D, equal to or different from each other, are selected between heteroaryl and aryl, wherein at least one of the hydrogen atoms of said heteroaryl and aryl are substituted with groups selected from SO3?, SO3H, COO?, COOH, and one or more of the other hydrogen atoms of said heteroaryl and aryl are optionally substituted as reported in the description.Type: ApplicationFiled: April 10, 2014Publication date: November 20, 2014Inventors: Paolo LAZZARI, Matteo ZANDA, Monica SANI
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Publication number: 20140243307Abstract: The present invention relates to pyrazole azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 24, 2014Publication date: August 28, 2014Applicant: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, Ken Chow
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Publication number: 20140243287Abstract: The present invention relates to pyrazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 24, 2014Publication date: August 28, 2014Applicant: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, Ken Chow
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Patent number: 8778950Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.Type: GrantFiled: August 27, 2010Date of Patent: July 15, 2014Assignee: Arena Pharmaceuticals, Inc.Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
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Publication number: 20140171469Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: July 3, 2013Publication date: June 19, 2014Applicant: Arena Pharmaceuticals, Inc.Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
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Publication number: 20140051739Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.Type: ApplicationFiled: July 11, 2013Publication date: February 20, 2014Inventors: Eric ANDERSON, Gary L. BOLTON, Bradley CAPRATHE, Xin JIANG, Chitase LEE, William H. ROARK, Melean VISNICK
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Patent number: 8513436Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.Type: GrantFiled: December 19, 2011Date of Patent: August 20, 2013Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
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Publication number: 20130165412Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.Type: ApplicationFiled: September 14, 2012Publication date: June 27, 2013Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
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Publication number: 20130158024Abstract: The present invention features compounds, pharmaceutical compositions, and methods for treating trauma, ischemia, stroke, degenerative diseases associated with cellular necrosis, and other conditions. Screening assays for identifying compounds useful for treating these conditions are also described.Type: ApplicationFiled: October 31, 2012Publication date: June 20, 2013Inventors: Junying Yuan, Alexei Degterev, Junichi Hitomi, Gregory D. Cuny, Prakash Jagtap
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Patent number: 8420689Abstract: The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor.Type: GrantFiled: January 14, 2011Date of Patent: April 16, 2013Assignee: Glenmark Pharmaceuticals S.A.Inventors: Meyyappan Muthuppalaniappan, Gopalan Balasubramanian, Srinivas Gullapalli, Neelima Khairatkar Joshi, Shridhar Narayanan
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Publication number: 20130017149Abstract: Condensed tricyclic compounds having a condensed structure containing one phenyl and one pyrazole ring linked with each other by a central ring comprising from five to eight atoms, having affinity for the CB1 and/or CB2 receptors, with central nervous system and/or peripheral activity, of formula (I): wherein the various substituents are as defined in the description. The compounds show affinity for the CB1 and/or CB2 cannabinoidergic receptors.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
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Patent number: 8338472Abstract: The present invention is directed to hexahydrocyclopentylf]imidazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: February 16, 2009Date of Patent: December 25, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: William P. Dankulich, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
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Patent number: 8324262Abstract: The present invention features compounds, pharmaceutical compositions, and methods for treating trauma, ischemia, stroke, degenerative diseases associated with cellular necrosis, and other conditions. Screening assays for identifying compounds useful for treating these conditions are also described.Type: GrantFiled: December 20, 2006Date of Patent: December 4, 2012Assignees: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard CollegeInventors: Junying Yuan, Alexei Degterev, Junichi Hitomi, Gregory D. Cuny, Prakash Jagtap
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Patent number: 8299048Abstract: The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: February 24, 2009Date of Patent: October 30, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
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Patent number: 8258168Abstract: 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 invention, and methods of treatment using them.Type: GrantFiled: January 11, 2012Date of Patent: September 4, 2012Assignee: SanofiInventors: Laurent Dubois, Yannick Evanno, Christian Maloizel, Mireille Sevrin
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Publication number: 20120214766Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.Type: ApplicationFiled: August 27, 2010Publication date: August 23, 2012Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
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Publication number: 20120196880Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.Type: ApplicationFiled: December 19, 2011Publication date: August 2, 2012Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
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Publication number: 20120108584Abstract: 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 invention, and methods of treatment using them.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Applicant: SANOFI-AVENTISInventors: Laurent DUBOIS, Yannick Evanno, Christian Maloizel, Mireille Sevrin
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Publication number: 20120095055Abstract: 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 inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: May 24, 2010Publication date: April 19, 2012Applicant: Merck Sharp & Dohme, Corp.Inventors: Helen J. Mitchell, Danielle M. Hurzy, Mildred K. Kaufman
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Patent number: 8153819Abstract: Fungicidal mixtures, comprising as active components 1) at least one 1-methylpyrazol-4-ylcarboxanilides of the formula I where X=O or S, R1=C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, R3, R4 and R5=independently of one another cyano, nitro, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy or C1-C4-alkylthio; and 2) at least one active compound II, selected from the active compound groups A) to F): A) azoles; B) strobilurins; C) carboxamides; D) heterocyclic compounds; E) carbamates; F) other fungicides; in a synergistically effective amount, methods for controlling harmful fungi using mixtures of at least one compound I and at least one active compound II and the use of the compound(s) I with active compounds II for preparing such mixtures, and also compositions and seed comprising such mixtures.Type: GrantFiled: August 1, 2006Date of Patent: April 10, 2012Assignee: BASF SEInventors: Jochen Dietz, Markus Gewehr, Siegfried Strathmann, Reinhard Stierl, Frank Werner, Maria Scherer
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Patent number: 8119681Abstract: 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 or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: October 23, 2007Date of Patent: February 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Bungard, Jesse J. Manikowski, James J. Perkins, Robert Meissner
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Patent number: 8114899Abstract: 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 invention, and methods of treatment using them.Type: GrantFiled: January 27, 2009Date of Patent: February 14, 2012Assignee: Sanofi-AventisInventors: Laurent DuBois, Yannick Evanno, Christian Maloizel, Mireille Sevrin
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Publication number: 20120035131Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.Type: ApplicationFiled: October 20, 2011Publication date: February 9, 2012Inventors: Marvin J. Meyers, Graciela B. Arhancet, Xiangyang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
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Patent number: 8071589Abstract: The invention relates to benzoindazole derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: July 29, 2010Date of Patent: December 6, 2011Assignee: N. V. OrganonInventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen
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Publication number: 20110224262Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: November 24, 2009Publication date: September 15, 2011Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
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Publication number: 20110218225Abstract: 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 compositions of non-steroidal ligands of the glucocorticoid receptor for treating or preventing diseases (e.g., obesity, diabetes, depression, neurodegeneration or an inflammatory disease) associated with glucocorticoid binding to the glucocorticoid receptor.Type: ApplicationFiled: May 11, 2011Publication date: September 8, 2011Applicant: The Regents of the University of CaliforniaInventors: Thomas S. Scanlan, Nilesh Shah
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Patent number: 7947726Abstract: 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 compositions of non-steroidal ligands of the glucocorticoid receptor for treating or preventing diseases (e.g., obesity, diabetes, depression, neurodegeneration or an inflammatory disease) associated with glucocorticoid binding to the glucocorticoid receptor.Type: GrantFiled: February 3, 2009Date of Patent: May 24, 2011Assignee: The Regents of the University of CaliforniaInventors: Thomas S. Scanlan, Nilesh Shah
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Publication number: 20110112088Abstract: This invention relates to compounds of the formula: to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.Type: ApplicationFiled: January 13, 2011Publication date: May 12, 2011Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
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Publication number: 20110105440Abstract: The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: February 24, 2009Publication date: May 5, 2011Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
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Patent number: 7923465Abstract: The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenerative disorders, eating disorders, weight loss or control, and obesity).Type: GrantFiled: June 1, 2006Date of Patent: April 12, 2011Assignee: Glenmark Pharmaceuticals S.A.Inventors: Meyyappan Muthuppalaniappan, Gopalan Balasubramanian, Srinivas Gullapalli, Neelima Khairatkar Joshi, Shridhar Narayanan
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Patent number: 7897634Abstract: 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.Type: GrantFiled: January 30, 2007Date of Patent: March 1, 2011Assignee: Athersys, Inc.Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
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Publication number: 20110028451Abstract: The invention relates to benzoindazole derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: July 29, 2010Publication date: February 3, 2011Applicant: N.V. OrganonInventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen
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Publication number: 20110003797Abstract: The present invention is directed to hexahydrocyclopentyl[f]imidazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: February 16, 2009Publication date: January 6, 2011Inventors: William P. Dankulich, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
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Publication number: 20100311709Abstract: 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 or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: October 23, 2007Publication date: December 9, 2010Inventors: Christopher J. Bungard, Jesse J. Manikowski, James J. Perkins, Robert Meissner
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Publication number: 20100280016Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Inventors: Marvin J. Meyers, Graciela B. Arhancet, XiangYang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
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Publication number: 20100273791Abstract: The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.Type: ApplicationFiled: April 29, 2010Publication date: October 28, 2010Inventors: Braj Bhushan LOHRAY, Vidya Bhushan Lohray, Brijesh Srivastava
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Patent number: 7816390Abstract: 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-Bromo-phenylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol; or 3-[3-(2-Chloro-pyridin-4-ylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol, and N-oxides, pharmaceutically acceptable salts, solvates, tautomers and stereochemical isomers thereof and the uses of such compounds as inhibitors of tubulin polymerization and for the treatment of solid tumors. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.Type: GrantFiled: January 29, 2008Date of Patent: October 19, 2010Assignee: Janssen Pharmaceutica NVInventors: Robert A. Galemmo, Dana L. Johnson, Umar S. M. Maharoof, Jay M. Mei, Robert W. Tuman
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Publication number: 20100228036Abstract: The invention encompasses a process for making 2-[1-phenyl-5-hydroxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives, which are glucocorticoid receptor ligands, useful for the treatment of inflammatory and immunological diseases.Type: ApplicationFiled: October 20, 2008Publication date: September 9, 2010Inventors: Qinghao Chen, Shinji Fujimori, Jacob M. Janey, John Limanto, Rafik Naccache, Andrew F. Nolting, Zhigou J. Song, Neil Strotman, Lushi Tan, Mark Weisel
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Publication number: 20100215741Abstract: Condensed tricyclic compounds having a condensed structure containing one phenyl and one pyrazole ring linked with each other by a central ring comprising from five to eight atoms, having affinity for the CB1 and/or CB2 receptors, with central nervous system and/or peripheral activity, of formula (I): wherein the various substituents are as defined in the description. The compounds show affinity for the CB1 and/or CB2 cannabinoidergic receptors.Type: ApplicationFiled: February 25, 2010Publication date: August 26, 2010Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
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Publication number: 20100216785Abstract: Microemulsions of pharmaceutical compositions comprising, the following components (% by weight), the sum of the components being 100%: S) from 0.01 to 95% of one or more compounds selected from surfactants, polymers, forming organized structures as: aggregates, micelles, liquid crystals, vesicles, in the liquid in which they are solubilized, O) from 0.01 to 95% of one or more oils selected from esters of C4-C32 acids or C4-C32 acids, PA) from 0.001 to 90% of compounds having affinity for the CB1 and/or CB2 cannabinoidergic receptors of formula A?: AD) from 0 to 60% by weight of one or more compounds selected from modifiers of the water and/or oil polarity, modifiers of the film curvature of component S), co-surfactants, water or a saline aqueous solution the difference to 100%, wherein the ratio by weight S)/PA) is lower than that of microemulsions wherein component O) is absent.Type: ApplicationFiled: February 25, 2010Publication date: August 26, 2010Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni LORIGA, Ilaria MANCA, Gerard Aime PINNA, Luca PANI
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Patent number: 7781428Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.Type: GrantFiled: October 24, 2007Date of Patent: August 24, 2010Assignee: Pfizer Inc.Inventors: Marvin J. Meyers, Graciela B. Arhancet, Xiangyang Chen, Susan Hockerman, David B. Reitz, Joseph G. Rico
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Patent number: 7776791Abstract: The invention relates to novel N-heterocyclylphenyl-substituted cyclic ketoenols of the formula (I) in which CKE, W, X, Y and Z are as defined in the disclosure, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides. The invention further relates to selective herbicidal compositions comprising firstly the N-heterocyclylphenyl-substituted cyclic ketoenols and secondly a compound which improves crop plant tolerance.Type: GrantFiled: June 7, 2004Date of Patent: August 17, 2010Assignee: Bayer CropScience AGInventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Stefan Lehr, Klaus Kunz, Jörg Konze, Olga Malsam, Mark Wilhelm Drewes, Dieter Feucht, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann, Wahed Ahmed Moradi, Guido Bojack, Thomas Auler, Martin Hills, Heinz Kehne
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Publication number: 20100190836Abstract: The present invention features compounds, pharmaceutical compositions, and methods for treating trauma, ischemia, stroke, degenerative diseases associated with cellular necrosis, and other conditions. Screening assays for identifying compounds useful for treating these conditions are also described.Type: ApplicationFiled: December 20, 2006Publication date: July 29, 2010Inventors: Junying Yuan, Alexei Degterev, Junichi Hitomi, Gregory D. Cuny, Prakash Jagtap
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Publication number: 20100104659Abstract: Compounds of a certain formula I, in which Ra, Rb and Rc have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: July 12, 2007Publication date: April 29, 2010Inventors: Matthias Vennemann, Thomas Bär, Thomas Maier, Andreas Lindenmaier, Jürgen Braunger, Markus Boehm, Astrid Zimmermann, Volker Gekeler
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Patent number: 7662846Abstract: The present invention encompasses compounds of Formula (I) and Formula (II) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: April 19, 2004Date of Patent: February 16, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, James M. Balkovec, Richard Beresis, Steven L. Colletti, Donald W. Graham, Gool F. Patel, Cameron J. Smith
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Publication number: 20100010038Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom, a halogen atom, a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or mercapto optionally having a substituent, Xa, Xb, Xc and Xd are each a carbon atom or a nitrogen atom, provided that any one or two of Xa, Xb, Xc and Xd is/are nitrogen atom(s), m is 0 to 2, and rings A to C are each a ring optionally having substituent(s), or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.Type: ApplicationFiled: December 27, 2007Publication date: January 14, 2010Inventors: Osamu Uchikawa, Tatsuki Koike, Takafumi Takai, Yasutaka Hoashi
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Patent number: 7645885Abstract: The invention provides non-steroidal ligands for the androgen receptor, methods for making non-steroidal ligands of the androgen receptor, compositions of non-steroidal ligands of the androgen receptor and methods of using non-steroidal ligands and compositions of non-steroidal ligands of the androgen receptor for treating or preventing diseases (e.g., prostate cancer) associated with androgen binding to the androgen receptor.Type: GrantFiled: August 28, 2006Date of Patent: January 12, 2010Assignee: The Regents of the University of CaliforniaInventors: Thomas S. Scanlan, Dmitry V. Kadnikov