Bicyclo Ring System Having The Diazole Ring As One Of The Cyclos (e.g., 2, 4-dichloro-5-nitrophenyl-4,5,6,7-tetrahydro-2h-indazole, Etc.) Patents (Class 548/360.1)
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Patent number: 8163743Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity.Type: GrantFiled: June 3, 2009Date of Patent: April 24, 2012Assignee: GlaxoGroupLimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Katherine Louise Jones, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Christian Alan Paul Smethurst, Yoshiaki Washio
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Patent number: 8153663Abstract: This invention relates to novel indazole derivatives of formula I: wherein R1 to R7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be used as medicaments.Type: GrantFiled: September 21, 2009Date of Patent: April 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Gregory Martin Benson, Konrad Bleicher, Song Feng, Uwe Grether, Bernd Kuhn, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Markus Rudolph, Sven Taylor
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Patent number: 8138208Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, W, X, R1-R5 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: GrantFiled: July 6, 2009Date of Patent: March 20, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun, Zhenshan Zhang
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Publication number: 20110306599Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: November 24, 2010Publication date: December 15, 2011Applicant: JAPAN TOBACCO INC.Inventors: Teruhiko INOUE, Tetsudo KAYA, Shinichi KIKUCHI, Koji MATSUMURA, Ritsuki MASUO, Motoya SUZUKI, Michihide MAEKAWA
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Patent number: 8071782Abstract: This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.Type: GrantFiled: October 2, 2008Date of Patent: December 6, 2011Assignee: Janssen Pharmaceutica NVInventors: Xiaohu Deng, Neelakandha S. Mani
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Patent number: 8063091Abstract: 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 the compounds.Type: GrantFiled: July 22, 2009Date of Patent: November 22, 2011Assignee: Abbott LaboratoriesInventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
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Patent number: 8017601Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: June 30, 2006Date of Patent: September 13, 2011Assignee: Amgen Inc.Inventors: Tae-Seong Kim, Jean-Christophe Harmange, Steven Bellon, Shon Booker, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Timothy S. Harvey, Joseph L. Kim, Matthew Lee, Longbin Liu, Vinod F. Patel, Andrew Tasker
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Patent number: 8008505Abstract: This invention relates to novel indazole or 4,5,6,7-tetrahydro-indazole derivatives of formula I wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be used as medicaments.Type: GrantFiled: September 21, 2009Date of Patent: August 30, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Bernd Kuhn, Hans Richter, Sven Taylor
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Patent number: 7981918Abstract: The present invention discloses novel compounds of Formula (I): having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I), as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: GrantFiled: April 5, 2007Date of Patent: July 19, 2011Assignee: Eli Lilly and CompanyInventors: Thomas Daniel Aicher, Peter Biagio Anzeveno, Renhua Li, Alexei Pavlovych Krasutsky, Thomas Edward Mabry, Ashraf Saeed, Nancy June Snyder, Hongqi Tian, Owen Brendan Wallace, Leonard Larry Winneroski, Yanping Xu
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Patent number: 7943652Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, Y, Z, and are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: GrantFiled: March 26, 2009Date of Patent: May 17, 2011Assignee: Novartis AGInventors: Michael D. Shultz, Christine Hiu-Tung Chen, Young Shin Cho, Lei Jiang, Jianmei Fan, Gang Liu, Dyuti Majumdar, Jianke Li
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Patent number: 7928135Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: GrantFiled: October 19, 2010Date of Patent: April 19, 2011Assignee: Serenex, Inc.Inventors: Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
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Patent number: 7919517Abstract: The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents aType: GrantFiled: November 21, 2008Date of Patent: April 5, 2011Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Yoshihisa Ohta, Fumihiko Kanai, Shinji Nara, Yutaka Kanda, Hiroshi Umehara, Yukimasa Shiotsu, Tomoki Naoe, Hitoshi Kiyoi, Keiko Kawashima, Hiromi Ando, Motoki Miyama
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Patent number: 7897619Abstract: The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: GrantFiled: July 16, 2008Date of Patent: March 1, 2011Assignee: Amgen Inc.Inventors: Qingping Zeng, Dawei Zhang, Guomin Yao, George E. Wohlhieter, Xianghong Wang, James Rider, Andreas Reichelt, Holger Monenschein, Fang-Tsao Hong, James R. Falsey, Celia Dominguez, Matthew P. Bourbeau, John G. Allen
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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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Patent number: 7893098Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5;Type: GrantFiled: September 25, 2009Date of Patent: February 22, 2011Assignee: Sepracor Inc.Inventors: Q. Kevin Fang, Seth Hopkins, Michele Heffernan, Milan Chytil
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Patent number: 7888381Abstract: Non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or an enantiomer, a diastereomer, a pharmaceutically acceptable salt, or hydrate thereof, where J is selected from NR1 or C(R4)(R4a); K is selected from NR2 or C(R5)(R5a); L is selected from NR3 or C(R6)(R6a); and A, X, Y, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R8, R10, R11, and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.Type: GrantFiled: June 13, 2006Date of Patent: February 15, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Zhonghui Lu, David S. Weinstein, Bin Jiang
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Publication number: 20110034529Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: October 19, 2010Publication date: February 10, 2011Applicant: Serenex, Inc.Inventors: Kenneth He Huang, Jeron Eaves, Gunnar J. Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
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Patent number: 7858809Abstract: Intermediates useful for the synthesis of pyrazole-fused ring derivatives, such as 7-phenylpyrazolo [1,5-a]pyridine derivatives, and method for producing the same. Method for producing compound represented by the general formula (II), wherein Z1 and Z2 each independently represents a methine group or a nitrogen atom; Rl represents an ethyl group or the like; R5 represents a hydrogen atom or the like; R2 and R3 each independently represents a C1-6 alkyl group or the like, salts thereof, or solvates of both, comprising the step of: reacting a compound represented by the general formula (I), wherein Z1, Z2, R5, R1, R2 and R3 each has the same definition as described above, with an organometallic reagent; and then reacting the resulting product with pentafluoroiodobenzene.Type: GrantFiled: April 8, 2005Date of Patent: December 28, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Shigeto Negi, Toshikazu Shimizu, Hiroshi Kuroda, Naoyuki Shimomura, Manabu Sasho, Yorihisa Hoshino, Manabu Kuboto
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Patent number: 7851498Abstract: This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: September 22, 2006Date of Patent: December 14, 2010Assignee: Janssen Pharmaceutica NVInventors: Mingde Xia, Fina Liotta, Huajun Lu, Meng Pan, Michael P. Wachter
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Patent number: 7846959Abstract: 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 death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.Type: GrantFiled: March 25, 2005Date of Patent: December 7, 2010Assignee: Exelixis, Inc.Inventors: Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Larisa Dubenko, Abigail R. Kennedy, Steven Charles Defina, Angie I. Kim, Jean-Claire L. Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Anagha Abhijit Joshi
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Patent number: 7829559Abstract: The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to pyrazole derivatives of formula (I) and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy and prophylaxis, in particular for the treatment of psychosis or pain.Type: GrantFiled: August 29, 2005Date of Patent: November 9, 2010Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Jordi Corbera Arjona, Maria Rosa Cuberes-Altisent, Joerg Holenz, Daniel MartĂnez-Olmo, David Vaño-Domenech
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Patent number: 7825151Abstract: This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: March 20, 2007Date of Patent: November 2, 2010Assignee: Janssen Pharmaceutica NVInventors: Mingde Xia, Fina Liotta, Huajun Lu, Meng Pan, Michael P. Wachter, Mark J. Macielag
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Patent number: 7820673Abstract: The present invention provides a urea derivative or a salt thereof, which is useful as a therapeutic agent for thrombosis.Type: GrantFiled: December 15, 2004Date of Patent: October 26, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Keiji Kubo, Yasuhiro Imaeda
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Patent number: 7795266Abstract: Compositions comprising tetrahydroindolone derivatives in which the tetrahydroindolone moiety is covalently linked to a substituted arylpiperazine moiety and methods for treating neurological and psychiatric conditions using such compositions are disclosed.Type: GrantFiled: September 27, 2004Date of Patent: September 14, 2010Inventors: David R. Helton, David B. Fick, Jason P. Sharp, Ernest H. Pfadenhauer
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Patent number: 7790718Abstract: This invention is directed to a tetrahydro-cyclopentyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: September 22, 2006Date of Patent: September 7, 2010Assignee: Janssen Pharmaceutica NVInventors: Fina Liotta, Mingde Xia, Michael P. Wachter, Scott A. Beers
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Patent number: 7750021Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.Type: GrantFiled: July 25, 2008Date of Patent: July 6, 2010Assignee: IRM LLCInventors: Yuan Mi, Shifeng Pan, Nathanael Schiander Gray, Wenqi Gao, Yi Fan, Tao Jiang
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Publication number: 20100152125Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.Type: ApplicationFiled: March 20, 2008Publication date: June 17, 2010Applicant: Brandeis UniversityInventors: Jeffrey N. Agar, Gregory A. Petsko, Dagmar Ringe, Walter R.P. Novak
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Patent number: 7728030Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments.Type: GrantFiled: December 20, 2007Date of Patent: June 1, 2010Assignees: AstraZeneca AB, Bayer Schering Pharma AktiengesellschaftInventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrecher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
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Publication number: 20100125090Abstract: The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.Type: ApplicationFiled: August 14, 2009Publication date: May 20, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Mark Miller, Ashvani Singh, Matthew Hamilton, Peter D.J. Grootenhuis
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Publication number: 20100076026Abstract: This invention relates to novel indazole derivatives of formula I: wherein R1 to R7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be used as medicaments.Type: ApplicationFiled: September 21, 2009Publication date: March 25, 2010Inventors: Gregory Martin Benson, Konrad Bleicher, Song Feng, Uwe Grether, Bernd Kuhn, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Markus Rudolph, Sven Taylor
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Publication number: 20100016369Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, W, X, R1-R5 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: ApplicationFiled: July 6, 2009Publication date: January 21, 2010Inventors: Li Chen, Fariboz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun, Zhenshan Zhang
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Publication number: 20100016397Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5;Type: ApplicationFiled: September 25, 2009Publication date: January 21, 2010Applicant: Sepracor Inc.Inventors: Q. Kevin Fang, Seth Hopkins, Michele Heffernan, Milan Chytil
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Patent number: 7622493Abstract: The present invention is directed to compounds of formula (I) wherein variables X1, X2, Y, R1a, R1b, R2a, R2b, A1, A2, A3, and A4 are as defined in the description, and methods of use to treat pain, neuropathic pain, allodynia, pain associated with inflammation or an inflammatory disease, inflammatory hyperalgesia, bladder overactivity, and urinary incontinence.Type: GrantFiled: April 13, 2007Date of Patent: November 24, 2009Assignee: Abbott LaboratoriesInventors: Brian S. Brown, John R. Koenig, Arthur R. Gomtsyan, Chih-Hung Lee
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Publication number: 20090281131Abstract: The present invention relates to novel heterocyclic compounds that are useful as phosphodiesterase inhibitors (PDEs) in particular phosphodiesterase type 4 (PDE IV) inhibitors and phosphodiesterase type 10 (PDE 10) inhibitors, processes for their preparation, pharmaceutical compositions containing them and their use in treating allergic and inflammatory diseases as well as for inhibiting the production of Tumor Necrosis Factor (TNF-?).Type: ApplicationFiled: September 10, 2007Publication date: November 12, 2009Inventors: Balasubramanian Gopalan, Dhamjewar Ravi, Shrikant Havale, Swamy Keshavapura Hosamane Sreedhara
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Patent number: 7595320Abstract: The present invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles of formula (I): wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and their use for the treatment of pathological conditions, in particular as anticancer agents.Type: GrantFiled: August 29, 2007Date of Patent: September 29, 2009Assignee: Aventis Pharma S.A.Inventors: Claude Barberis, Jean-Christophe Carry, Gilles Doerflinger, Dominique Barbalat-Damour, Francois Clerc, Herve Minoux
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Publication number: 20090215850Abstract: The present invention is directed to a method for treating, ameliorating or preventing CB2 receptor mediated pain in a subject in need thereof comprising administering to the subject an effective amount of a compound of formula (I): or a form thereof, wherein X1R1, X2R2, X3R3, X4R4 and X5R5 are as defined herein.Type: ApplicationFiled: February 27, 2008Publication date: August 27, 2009Inventors: Mingde Xia, Mark J. Macielag, Christopher M. Flores, Kevin Paul Pavlick
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Patent number: 7576087Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: GrantFiled: June 19, 2007Date of Patent: August 18, 2009Assignee: WyethInventors: Ronald Charles Bernotas, Yinfa Yan
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Patent number: 7572823Abstract: Compounds of formula I their manufacture, pharmaceutical compositions containing them and their use as medicaments.Type: GrantFiled: January 26, 2007Date of Patent: August 11, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Aurelia Conte, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
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Publication number: 20090197886Abstract: This invention is directed to a hexahydro-cycloheptapyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: ApplicationFiled: April 7, 2009Publication date: August 6, 2009Inventors: Fina Liotta, Mingde Xia, Huajun Lu, Meng Pan, Michael P. Wachter
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Publication number: 20090111800Abstract: The present invention discloses novel compounds of Formula (I): having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I), as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: ApplicationFiled: April 5, 2007Publication date: April 30, 2009Inventors: Thomas Daniel Aicher, Peter Biagio Anzeveno, Renhua Li, Alexei Pavlovych Krasutsky, Thomas Edward Mabry, Ashraf Saeed, Nancy June Snyder, Gregory Alan Stephenson, Hongqi Tian, Owen Brendan Wallace, Leonard Larry Winneroski, JR., Yanping Xu
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Patent number: 7517902Abstract: Disclosed are novel substituted indazole compounds, pharmaceutical compositions comprising such compounds, and methods of treatment comprising such compounds.Type: GrantFiled: December 4, 2006Date of Patent: April 14, 2009Assignee: Aventis Pharma S.A.Inventors: Frank Halley, Michel Tabart, Hervé Bouchard, Catherine Souaille, Alain Le Brun, Fabrice Viviani, Laurence Gauzy-Lazo, Pascal Desmazeau, Odile Angouillant-Boniface, Bruno Filoche-Romme
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Publication number: 20090093637Abstract: This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.Type: ApplicationFiled: October 2, 2008Publication date: April 9, 2009Inventors: Xiaohu Deng, Neelakandha S. Mani
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Publication number: 20090093452Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein RQ, R7, n, Q2, Q3, Y, and X1-X3 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: August 24, 2007Publication date: April 9, 2009Inventors: Kenneth He Huang, Steven E. Hall, James Veal
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Patent number: 7511046Abstract: The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.Type: GrantFiled: July 21, 2006Date of Patent: March 31, 2009Assignee: Aventis Hoklings Inc.Inventors: David M Fink, Brian S Freed, Nicholas J Hrib, Raymond W Kosley, George E Lee, Gregory H Merriman, Barbara S Rauckman
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Publication number: 20090054423Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: April 7, 2006Publication date: February 26, 2009Inventors: Jason E. Imbriglio, Steven L. Colletti, James R. Tata, Rui Liang, Subharekha Raghavan, Darby R. Schmidt, Abigail L. Smenton, Sook Yee Chan
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Publication number: 20090042961Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.Type: ApplicationFiled: May 8, 2008Publication date: February 12, 2009Inventors: Varghese John, Michel Maillard, Barbara Jagodzinska, Jose Aquino, Gary Probst, Jay Tung
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Patent number: 7479357Abstract: An organophotoreceptor that includes: (a) a charge transport material having the formula wherein A is selected from heterocyclic groups, naphthyl group, alkylsulfonylphenyl, stilbenyl or the group X, wherein X is represented by the formula B is selected from hydrogen, alkyl group, and an aryl group, with the proviso that when A is naphthyl, B is naphthyl; or where R1 is selected from the group consisting of N-pyrrolyl, N-pyrazolyl, N-tetrazolyl, N-indolyl, N-carbazolyl, N-triazolyl, N-imidazolyl, N-benzimidazolyl, N-indazolyl, and N-benzotriazolyl group, and R3 is a 9-fluorenone group. (b) a charge generating compound; and (c) an electrically conductive substrate.Type: GrantFiled: September 13, 2002Date of Patent: January 20, 2009Assignee: Samsung Electronics Co., Ltd.Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katritzky, Ritu Jain, Rexiat Maimait, Anatoliy V. Vakulenko
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Patent number: 7473701Abstract: 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.Type: GrantFiled: October 13, 2004Date of Patent: January 6, 2009Assignee: Aventis Pharma S.A.Inventors: Dominique Damour, Jean-Christophe Carry, Patrick Nemecek, Corinne Terrier, Frederico Nardi, Bruno Filoche-Romme, Marie-Pierre Cherrier, Daniel Bezard
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Patent number: 7470717Abstract: The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents aType: GrantFiled: July 30, 2004Date of Patent: December 30, 2008Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoshihisa Ohta, Fumihiko Kanai, Shinji Nara, Yutaka Kanda, Hiroshi Umehara, Yukimasa Shiotsu, Tomoki Naoe, Hitoshi Kiyoi, Keiko Kawashima, Hiromi Ando, Motoki Miyama
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Patent number: 7452997Abstract: This invention is directed to a tetrahydro-indazole cannabinoid modulator compound of formula I: and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: March 23, 2005Date of Patent: November 18, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Bharat Lagu, Fina Liotta, Meng Pan, Michael P. Wachter, Mingde Xia Xia