Tricyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 548/359.1)
  • Patent number: 9012478
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: April 21, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Publication number: 20150051177
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Inventor: Darren Orton
  • Publication number: 20150005357
    Abstract: 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: Application
    Filed: January 29, 2013
    Publication date: January 1, 2015
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Atul Goel, Gaurav Taneja, Neha Rahuja, Arun Kumar Rawat, Natasha Jaiswal, Akhilesh Kumar Tamrakar, Arvind Kumar Srivastava
  • Publication number: 20140343294
    Abstract: 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: Application
    Filed: April 10, 2014
    Publication date: November 20, 2014
    Inventors: Paolo LAZZARI, Matteo ZANDA, Monica SANI
  • Publication number: 20140243287
    Abstract: 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: Application
    Filed: February 24, 2014
    Publication date: August 28, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, Ken Chow
  • Publication number: 20140243307
    Abstract: 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: Application
    Filed: February 24, 2014
    Publication date: August 28, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, Ken Chow
  • Patent number: 8778950
    Abstract: 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: Grant
    Filed: August 27, 2010
    Date of Patent: July 15, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
  • Publication number: 20140171469
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: July 3, 2013
    Publication date: June 19, 2014
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Publication number: 20140051739
    Abstract: 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: Application
    Filed: July 11, 2013
    Publication date: February 20, 2014
    Inventors: Eric ANDERSON, Gary L. BOLTON, Bradley CAPRATHE, Xin JIANG, Chitase LEE, William H. ROARK, Melean VISNICK
  • Patent number: 8513436
    Abstract: 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: Grant
    Filed: December 19, 2011
    Date of Patent: August 20, 2013
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
  • Publication number: 20130165412
    Abstract: 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: Application
    Filed: September 14, 2012
    Publication date: June 27, 2013
    Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
  • Publication number: 20130158024
    Abstract: 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: Application
    Filed: October 31, 2012
    Publication date: June 20, 2013
    Inventors: Junying Yuan, Alexei Degterev, Junichi Hitomi, Gregory D. Cuny, Prakash Jagtap
  • Patent number: 8420689
    Abstract: 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: Grant
    Filed: January 14, 2011
    Date of Patent: April 16, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Meyyappan Muthuppalaniappan, Gopalan Balasubramanian, Srinivas Gullapalli, Neelima Khairatkar Joshi, Shridhar Narayanan
  • Publication number: 20130017149
    Abstract: 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: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
  • Patent number: 8338472
    Abstract: 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: Grant
    Filed: February 16, 2009
    Date of Patent: December 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William P. Dankulich, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
  • Patent number: 8324262
    Abstract: 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: Grant
    Filed: December 20, 2006
    Date of Patent: December 4, 2012
    Assignees: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard College
    Inventors: Junying Yuan, Alexei Degterev, Junichi Hitomi, Gregory D. Cuny, Prakash Jagtap
  • Patent number: 8299048
    Abstract: 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: Grant
    Filed: February 24, 2009
    Date of Patent: October 30, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
  • Patent number: 8258168
    Abstract: 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: Grant
    Filed: January 11, 2012
    Date of Patent: September 4, 2012
    Assignee: Sanofi
    Inventors: Laurent Dubois, Yannick Evanno, Christian Maloizel, Mireille Sevrin
  • Publication number: 20120214766
    Abstract: 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: Application
    Filed: August 27, 2010
    Publication date: August 23, 2012
    Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
  • Publication number: 20120196880
    Abstract: 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: Application
    Filed: December 19, 2011
    Publication date: August 2, 2012
    Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
  • Publication number: 20120108584
    Abstract: 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: Application
    Filed: January 11, 2012
    Publication date: May 3, 2012
    Applicant: SANOFI-AVENTIS
    Inventors: Laurent DUBOIS, Yannick Evanno, Christian Maloizel, Mireille Sevrin
  • Publication number: 20120095055
    Abstract: 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: Application
    Filed: May 24, 2010
    Publication date: April 19, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Helen J. Mitchell, Danielle M. Hurzy, Mildred K. Kaufman
  • Patent number: 8153819
    Abstract: 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: Grant
    Filed: August 1, 2006
    Date of Patent: April 10, 2012
    Assignee: BASF SE
    Inventors: Jochen Dietz, Markus Gewehr, Siegfried Strathmann, Reinhard Stierl, Frank Werner, Maria Scherer
  • Patent number: 8119681
    Abstract: 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: Grant
    Filed: October 23, 2007
    Date of Patent: February 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher J. Bungard, Jesse J. Manikowski, James J. Perkins, Robert Meissner
  • Patent number: 8114899
    Abstract: 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: Grant
    Filed: January 27, 2009
    Date of Patent: February 14, 2012
    Assignee: Sanofi-Aventis
    Inventors: Laurent DuBois, Yannick Evanno, Christian Maloizel, Mireille Sevrin
  • Publication number: 20120035131
    Abstract: 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: Application
    Filed: October 20, 2011
    Publication date: February 9, 2012
    Inventors: Marvin J. Meyers, Graciela B. Arhancet, Xiangyang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
  • Patent number: 8071589
    Abstract: 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: Grant
    Filed: July 29, 2010
    Date of Patent: December 6, 2011
    Assignee: N. V. Organon
    Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen
  • Publication number: 20110224262
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: November 24, 2009
    Publication date: September 15, 2011
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Publication number: 20110218225
    Abstract: 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: Application
    Filed: May 11, 2011
    Publication date: September 8, 2011
    Applicant: The Regents of the University of California
    Inventors: Thomas S. Scanlan, Nilesh Shah
  • Patent number: 7947726
    Abstract: 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: Grant
    Filed: February 3, 2009
    Date of Patent: May 24, 2011
    Assignee: The Regents of the University of California
    Inventors: Thomas S. Scanlan, Nilesh Shah
  • Publication number: 20110112088
    Abstract: This invention relates to compounds of the formula: to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.
    Type: Application
    Filed: January 13, 2011
    Publication date: May 12, 2011
    Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
  • Publication number: 20110105440
    Abstract: 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: Application
    Filed: February 24, 2009
    Publication date: May 5, 2011
    Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
  • Patent number: 7923465
    Abstract: 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: Grant
    Filed: June 1, 2006
    Date of Patent: April 12, 2011
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Meyyappan Muthuppalaniappan, Gopalan Balasubramanian, Srinivas Gullapalli, Neelima Khairatkar Joshi, Shridhar Narayanan
  • Patent number: 7897634
    Abstract: 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: Grant
    Filed: January 30, 2007
    Date of Patent: March 1, 2011
    Assignee: Athersys, Inc.
    Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
  • Publication number: 20110028451
    Abstract: 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: Application
    Filed: July 29, 2010
    Publication date: February 3, 2011
    Applicant: N.V. Organon
    Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen
  • Publication number: 20110003797
    Abstract: 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: Application
    Filed: February 16, 2009
    Publication date: January 6, 2011
    Inventors: William P. Dankulich, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
  • Publication number: 20100311709
    Abstract: 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: Application
    Filed: October 23, 2007
    Publication date: December 9, 2010
    Inventors: Christopher J. Bungard, Jesse J. Manikowski, James J. Perkins, Robert Meissner
  • Publication number: 20100280016
    Abstract: 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: Application
    Filed: July 12, 2010
    Publication date: November 4, 2010
    Inventors: Marvin J. Meyers, Graciela B. Arhancet, XiangYang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
  • Publication number: 20100273791
    Abstract: 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: Application
    Filed: April 29, 2010
    Publication date: October 28, 2010
    Inventors: Braj Bhushan LOHRAY, Vidya Bhushan Lohray, Brijesh Srivastava
  • Patent number: 7816390
    Abstract: 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: Grant
    Filed: January 29, 2008
    Date of Patent: October 19, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Robert A. Galemmo, Dana L. Johnson, Umar S. M. Maharoof, Jay M. Mei, Robert W. Tuman
  • Publication number: 20100228036
    Abstract: 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: Application
    Filed: October 20, 2008
    Publication date: September 9, 2010
    Inventors: Qinghao Chen, Shinji Fujimori, Jacob M. Janey, John Limanto, Rafik Naccache, Andrew F. Nolting, Zhigou J. Song, Neil Strotman, Lushi Tan, Mark Weisel
  • Publication number: 20100215741
    Abstract: 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: Application
    Filed: February 25, 2010
    Publication date: August 26, 2010
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
  • Publication number: 20100216785
    Abstract: 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: Application
    Filed: February 25, 2010
    Publication date: August 26, 2010
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni LORIGA, Ilaria MANCA, Gerard Aime PINNA, Luca PANI
  • Patent number: 7781428
    Abstract: 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: Grant
    Filed: October 24, 2007
    Date of Patent: August 24, 2010
    Assignee: Pfizer Inc.
    Inventors: Marvin J. Meyers, Graciela B. Arhancet, Xiangyang Chen, Susan Hockerman, David B. Reitz, Joseph G. Rico
  • Patent number: 7776791
    Abstract: 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: Grant
    Filed: June 7, 2004
    Date of Patent: August 17, 2010
    Assignee: Bayer CropScience AG
    Inventors: 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
  • Publication number: 20100190836
    Abstract: 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: Application
    Filed: December 20, 2006
    Publication date: July 29, 2010
    Inventors: Junying Yuan, Alexei Degterev, Junichi Hitomi, Gregory D. Cuny, Prakash Jagtap
  • Publication number: 20100104659
    Abstract: 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: Application
    Filed: July 12, 2007
    Publication date: April 29, 2010
    Inventors: Matthias Vennemann, Thomas Bär, Thomas Maier, Andreas Lindenmaier, Jürgen Braunger, Markus Boehm, Astrid Zimmermann, Volker Gekeler
  • Patent number: 7662846
    Abstract: 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: Grant
    Filed: April 19, 2004
    Date of Patent: February 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, James M. Balkovec, Richard Beresis, Steven L. Colletti, Donald W. Graham, Gool F. Patel, Cameron J. Smith
  • Publication number: 20100010038
    Abstract: 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: Application
    Filed: December 27, 2007
    Publication date: January 14, 2010
    Inventors: Osamu Uchikawa, Tatsuki Koike, Takafumi Takai, Yasutaka Hoashi
  • Patent number: 7645885
    Abstract: 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: Grant
    Filed: August 28, 2006
    Date of Patent: January 12, 2010
    Assignee: The Regents of the University of California
    Inventors: Thomas S. Scanlan, Dmitry V. Kadnikov