Plural Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 514/212.06)
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Publication number: 20110039820Abstract: The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: ApplicationFiled: October 13, 2010Publication date: February 17, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Christopher F. Claiborne, Courtney A. Cullis, Natalie A. Dales, Michael Patane, Matthew Stirling, Omar Stradella, Gabriel S. Weatherhead
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Patent number: 7888344Abstract: A series of 5,6-dihydro-1,3-benzothiazol-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PD kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: GrantFiled: April 25, 2006Date of Patent: February 15, 2011Assignee: UCB Pharma S.A.Inventors: Rikki Peter Alexander, Pavandeep Aujla, Mark James Batchelor, Daniel Christopher Brookings, George Martin Buckley, Karen Viviane Lucile Crepy, Claire Louise Kulisa, James Petrie Turner
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Publication number: 20110034438Abstract: The invention relates to compounds of general formula (I), which can be used particularly as structural mimetics of proline-rich peptides and are therefore capable of binding PRM binding domains (proline-rich motif binding domains) of proteins. The invention also relates to the use of said compounds as pharmaceutical active agents and the use of these pharmaceutical active agents for treating bacterial diseases, neurodegenerative diseases and tumours.Type: ApplicationFiled: September 25, 2007Publication date: February 10, 2011Applicant: FORSCHUNGSVERBUND BERLIN E.V.Inventors: Ronald Kuehne, Hartmut Oschkinat, Christoph Brockmann, Hans-Guenther Schmalz
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Publication number: 20110028450Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: July 27, 2010Publication date: February 3, 2011Applicant: N.V. OrganonInventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
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Publication number: 20110003793Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 1, 2010Publication date: January 6, 2011Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. Guzzo, Matthew David Surman, James Francis Grabowski, JR., Emily Elizabeth Freeman
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Patent number: 7858612Abstract: The present invention relates to a method for maintaining the remission of or treating inflammatory bowel diseases, which comprises administering a maintenance therapeutically effective amount or a therapeutically effective amount of 7,8-dimethoxy-4(5H),10-dioxo-1H-1,2,3-triazolo[4,5-c][1]benzoazepine, a prodrug thereof, or a pharmaceutically acceptable salt thereof to a mammal, wherein the prodrug is 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzoazepine. The method according to the present invention is effective in the maintenance therapy and therapy of the inflammatory bowel diseases and has few side effects. Particularly, the method according to the present invention may exhibit strong maintenance therapeutic and therapeutic effects, even on severe cases having resistance to the conventional therapeutics.Type: GrantFiled: December 17, 2008Date of Patent: December 28, 2010Assignee: Meiji Seika Kaisha, Ltd.Inventors: Tomohisa Ninomiya, Takashi Shishikura, Mitsuhiro Uchida, Sho Takahata, Yukari Hoshina, Ken-ichi Kawano
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Publication number: 20100305066Abstract: A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: June 4, 2007Publication date: December 2, 2010Applicant: UCB PHARMA S.A.Inventors: Rikki Peter Alexander, Stuart Bailey, Stephen Brand, Daniel Christopher Brookings, Julien Alistair Brown, Alan Findlay Haughan, Natasha Kinsella, Christopher Lowe, Stephen Robert Mack, William Ross Pitt, Marianna Dilani Richard, Andrew Sharpe, Laura Jane Tait
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Publication number: 20100298292Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: ApplicationFiled: May 21, 2010Publication date: November 25, 2010Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
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Patent number: 7838517Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: May 15, 2009Date of Patent: November 23, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
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Publication number: 20100280004Abstract: This invention provides compounds of Formula I. The compounds are correctors of ?F508 CFTR trafficking. Also provided are uses of compounds of Formula I for treatment, as well as methods of treatment, of cystic fibrosis.Type: ApplicationFiled: July 3, 2008Publication date: November 4, 2010Inventors: Raymond Andersen, Robert Keyzers, Christopher Anthony Gray, David Y. Thomas, John W. Hanrahan, Graeme W. Carlile
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Publication number: 20100256115Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: ApplicationFiled: March 18, 2010Publication date: October 7, 2010Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20100249102Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: ApplicationFiled: April 6, 2010Publication date: September 30, 2010Applicant: ALANTOS PHARMACEUTICALS HOLDINGS, INC.Inventors: Christian Gege, Carine Chevrier, Matthias Schneider, Harald Bluhm, Matthias Hochgürtel, Hongbo Deng, Brian M. Gallagher, JR., Irving Sucholeiki, Arthur Taveras
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Patent number: 7803793Abstract: This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.Type: GrantFiled: September 21, 2007Date of Patent: September 28, 2010Assignee: Janssen Pharmaceutica NVInventors: Yue-Mei Zhang, Bangping Xiang, Shyh-Ming Yang, Kenneth Rhodes, Robert Scannevin, Paul Jackson, Davraj Chakravarty, Xiaodong Fan, Lawrence J. Wilson, Prabha Karnachi
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Publication number: 20100222320Abstract: Compounds of formula I: Selectively attenuate production of A?(1-42) and hence find use in treatment or prevention of diseases associated with deposition of A? in the brain, in particular Alzheimer's disease.Type: ApplicationFiled: June 9, 2008Publication date: September 2, 2010Inventors: Christian Fischer, Ben Munoz, Susan Zultanski, Joey Methot, Hua Zhou, W. Colby Brown
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Publication number: 20100190773Abstract: Heterocyclic compounds and analogues thereof and their use as inhibitors of Mitogen-Activated Protein Kinase-Activated Protein kinase-2 (MAPKAP-k2), and also to a method for preventing or treating a disease or disorder that can be treated or prevented by modulating the activity of MAPKAP-K2 in a subject and to pharmaceutical compositions and kits that include these MAPKAP-K2 inhibitors.Type: ApplicationFiled: March 19, 2010Publication date: July 29, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha ABEYWARDANE, Craig Andrew MILLER, Tina Marie MORWICK, Neil MOSS, Matthew Russell NETHERTON, Roger John SNOW, Ji WANG, Jiang-Ping WU, Zhaoming XIONG
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Publication number: 20100179126Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: December 4, 2009Publication date: July 15, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Indu T. Bharathan, Matthew Duffey, Amy Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
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Patent number: 7732436Abstract: The synthesis and biological activity of indoloazepines and acid amine salts thereof which are structurally related to naturally-occurring hymenialdisine is disclosed. Naturally-occurring hymenialdisine obtained from the sponge is a potent inhibitor of production of cytokines interleukin-2 (IL-2) and tumor necrosis factor-? (TNF-?). The chemically-synthesized indoloazepines of the invention also inhibit production of IL-2 and TNF-?. The indoloazepines are useful for treating inflammatory diseases, particularly diseases associated with kinases NF-?B or GSK-3? activation or NF-?B activated gene expression products. The indoloazepines are useful for the treatment of cancer by the inhibition of kinases CHK1 and CHK2.Type: GrantFiled: August 9, 2006Date of Patent: June 8, 2010Assignee: Board Of Trustees Of Michigan State UniversityInventor: Jetze J. Tepe
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Publication number: 20100137283Abstract: The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIV”) integrase enzyme.Type: ApplicationFiled: February 1, 2010Publication date: June 3, 2010Inventors: Klaus Ruprecht Dress, Qiyue Hu, Ted William Johnson, Michael Bruno Plewe, Steven Paul Tanis, Huichun Zhu, Junhu Zhang
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Publication number: 20100130475Abstract: The present invention relates to a pharmaceutical composition for preventing or treating inflammatory bowel diseases, which comprises 7,8-dimethoxy-4(5H),10-dioxo-1H-1,2,3-triazolo[4,5-c][1]benzoazepine, a prodrug thereof, preferably 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzoazepine as a prodrug, or a pharmaceutically acceptable salt thereof. The pharmaceutical composition according to the present invention is effective in the prophylaxis and therapy of the inflammatory bowel diseases and has few side effects. Particularly, the pharmaceutical composition according to the present invention may exhibit strong prophylactic and therapeutic effects even on severe cases having resistance to the conventional therapeutics.Type: ApplicationFiled: December 17, 2008Publication date: May 27, 2010Inventors: Tomohisa Ninomiya, Takashi Shishikura, Mitsuhiro Uchida, Sho Takahata, Yukari Hoshina, Ken-ichi Kawano
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Patent number: 7713958Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activity of CDK1, CDK2, CDK4, CDK5, GSK3?, Bcr-abl, Flt-3, c-Kit, PDGFR?, Src, Mek1 and CK1.Type: GrantFiled: August 6, 2008Date of Patent: May 11, 2010Assignee: IRM LLCInventors: Yongqin Wan, Nathanael S. Gray
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Publication number: 20100075952Abstract: The invention provides new pyrrolo-nitrogenous heterocyclic derivatives represented by formula (I) or their salts, the preparation thereof, pharmaceutical compositions containing such derivatives and the use of such derivatives as therapeutic agents, especially as protein kinase inhibitors, wherein each substituent in formula (I) is same as defined in the description.Type: ApplicationFiled: May 14, 2008Publication date: March 25, 2010Inventors: Peng Cho ChoTang, Yidong Su, Yali Li, Lei Zhang, Fuqiang Zhao, Jialiang Yang, Ying Zhou, Pingyan Bie, Guangtao Qian, Minggang Ju
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Publication number: 20100069360Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1, R2, R3, R7 and X are as defined in the specification.Type: ApplicationFiled: August 28, 2007Publication date: March 18, 2010Inventors: Laszlo Revesz, Achim Schlapbach, Rudolf Walchli
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Publication number: 20100056495Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.Type: ApplicationFiled: July 24, 2007Publication date: March 4, 2010Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventor: Stephen M. Condon
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Publication number: 20090306045Abstract: The present invention relates to the use of glycogen synthase kinase 3(GSK3) inhibitors, especially inhibitors of GSK-3?, GSK-3? and GSK-3?2, preferably, inhibitors of GSK-3?, in patients having autoimmune diseases and/or immune dysfunction/dysregulation to induce immune tolerance. Inhibition of GSK leads to activation of a pathway of dendritic cell maturation which leads to a dendritic phenotype which attenuates, rather than induces, immune responses. The immune responses and mature dendritic cells produced by the method of the present invention redirect or attenuate the immune response in individuals, thus leading to effective therapies for a number of autoimmune diseases and/or diseases of immune dysfunction/dysregulation (immune inflammatory diseases), including systemic lupus erythematosus (SLE), autoimmune diabetes (type I diabetes mellitus), asthma, rheumatoid arthritis, inflammatory bowel disease, among numerous others.Type: ApplicationFiled: December 22, 2006Publication date: December 10, 2009Inventors: Ira Mellman, Aimin Jiang
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Publication number: 20090291941Abstract: The present invention relates to pyrido[3,2-c]benzazocinone derivatives and related compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: October 18, 2006Publication date: November 26, 2009Inventors: Christopher J. Dinsmore, Jongwon Lim, Alan B. Northrup
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Publication number: 20090281082Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: May 15, 2009Publication date: November 12, 2009Applicant: Vertex Pharmaceuticals IncorporatedInventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
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Publication number: 20090281080Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, R6, T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: ApplicationFiled: November 14, 2006Publication date: November 12, 2009Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman
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Publication number: 20090281081Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.Type: ApplicationFiled: May 6, 2009Publication date: November 12, 2009Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C. B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
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Publication number: 20090264411Abstract: A series of 4,5,6,7-tetrahydrothieno[2,3-c]azepin-8-one derivatives, and analogues thereof, which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.Type: ApplicationFiled: February 13, 2009Publication date: October 22, 2009Applicant: UCB Pharma S.A.Inventors: Victoria Elizabeth Laing, Daniel Christopher Brookings, Rachel Jane Carbery, Jose Miguel Gascon Simorte, Martin Clive Hutchings, Barry John Langham, Martin Alexander Lowe
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Patent number: 7601710Abstract: The synthesis and biological activity of indoloazepines and acid amine salts thereof which are structurally related to naturally-occurring hymenialdisine is disclosed. Naturally-occurring hymenialdisine obtained from the sponge is a potent inhibitor of production of cytokines interleukin-2 (IL-2) and tumor necrosis factor-? (TNF-?). The chemically-synthesized indoloazepines of the invention also inhibit production of IL-2 and TNF-?. The indoloazepines are useful for treating inflammatory diseases, particularly diseases associated with kinases NF-?B or GSK-3? activation or NF-?B activated gene expression products. The indoloazepines are useful for the treatment of cancer by the inhibition of kinases CHK1 and CHK2.Type: GrantFiled: August 9, 2006Date of Patent: October 13, 2009Assignee: Board of Trustees of Michigan State UniversityInventor: Jetze J. Tepe
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Publication number: 20090156578Abstract: In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.Type: ApplicationFiled: December 1, 2006Publication date: June 18, 2009Inventors: Henry Pauls, Judd M. Berman
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Publication number: 20090137555Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activity of CDK1, CDK2, CDK4, CDK5, GSK3?, Bcr-abl, Flt-3, c-Kit, PDGFR?, Src, Mek1 and CK1.Type: ApplicationFiled: August 6, 2008Publication date: May 28, 2009Applicant: IRM LLCInventors: Yongqin Wan, Nathanael S. Gray
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Patent number: 7531530Abstract: The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments.Type: GrantFiled: July 23, 2004Date of Patent: May 12, 2009Assignees: Cancer Research Technology Limited, PfizerInventors: Thomas Helleday, Nicola Curtin
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Publication number: 20090105213Abstract: The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: ApplicationFiled: September 4, 2008Publication date: April 23, 2009Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Christopher F. Claiborne, Courtney A. Cullis, Natalie A. Dales, Michael Patane, Matthew Stirling, Omar Stradella, Gabriel S. Weatherhead
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Publication number: 20090062255Abstract: The invention relates to a method for evaluating a chemotherapeutic potential of a candidate molecule. In evaluating the candidate molecule, the candidate molecule is tested for its ability to inhibit the in vitro growth of a cancer cell; to bind a cellular receptor produced by a cancer cell, wherein said receptor, such as a peripheral benzodiazepine receptor, is produced in a greater amount by said cancer cell than by a normal cell; and to inhibit the activity of at least one protein member of the MAPK pathway. The invention further relates to dibenzodiazepinone analogues and derivatives thereof.Type: ApplicationFiled: August 15, 2008Publication date: March 5, 2009Applicant: THALLION PHARMACEUTICALS INC.Inventors: Henriette GOURDEAU, Pierre FALARDEAU, My-Anh WIOLAND, Nadia BOUFAIED, James B. MCALPINE, Mustapha AOUIDATE, Thierry BERTOMEU, Ashraf IBRAHIM
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Patent number: 7491713Abstract: Compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, D, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, pharmaceutical compositions comprising these compounds, use of these compounds and compositions to prevent or treat diseases involving CGRP.Type: GrantFiled: January 25, 2005Date of Patent: February 17, 2009Assignee: Merck + Co., Inc.Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W Shaw, Craig A. Stump, Theresa M. Williams
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Publication number: 20090005359Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: ApplicationFiled: June 30, 2008Publication date: January 1, 2009Applicant: Sunesis Pharmaceuticals, IncInventors: Jennifer Cossrow, Bing Guan, Alexey Ishchenko, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
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Patent number: 7470680Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: May 1, 2007Date of Patent: December 30, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Stephen E. Mercer, Haiquan Fang, Xiaojun Han, Guanglin Luo, Gene M. Dubowchik, Graham S. Poindexter
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Patent number: 7470679Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: May 1, 2007Date of Patent: December 30, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Stephen E. Mercer, Prasad V. Chaturvedula
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Publication number: 20080312211Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described: formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: December 19, 2006Publication date: December 18, 2008Applicant: ASTRAZENECA ABInventors: Gregory Basarab, Haihong Ni, Brian Sherer, Fei Zhou
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Patent number: 7459448Abstract: The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: GrantFiled: October 3, 2005Date of Patent: December 2, 2008Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Christopher F. Claiborne, Courtney A. Cullis, Natalie A. Dales, Michael Patane, Matthew Stirling, Omar Stradella, Gabriel S. Weatherhead
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Publication number: 20080287422Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: ApplicationFiled: April 18, 2008Publication date: November 20, 2008Inventors: Prasad V. Chaturvedula, Stephen E. Mercer, Haiquan Fang
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Publication number: 20080255090Abstract: Antimitotic compounds and salts are provided in which the compound has the structure (formula (I)): wherein X and Y are substituted or unsubstituted and are selected from carbon atoms and atoms of groups 15 and 16 of the periodic table; Z is selected from N—R, O and S; U is selected from CR1, N, NH, NR, S and O, R1, R2, and R3 are independently selected from H, NH2, NHR, NR2, SH, SR, SiR3, OH, OR, F, CI, Br, I, ?O, ?S and R; W is selected from O, S, and H2; R4 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NR2 and halide; R is selected from H, substituted or unsubstituted aryl, and substituted or unsubstituted 1 to 20 carbon linear, branched, or cyclic, saturated or unsaturated alkyl, in which alkyl carbon atoms are replaced by 0 to 10 oxygen, 0 to 10 sulphur, and 0 to 10 N atoms; and wherein bonds to carbon atoms or to any of X, Y, Z and U are saturated or unsaturated; and providing that when W is H2, R4 is not H, OH, or unsubstituted phenyl.Type: ApplicationFiled: September 15, 2004Publication date: October 16, 2008Applicant: THE UNIVERSITY OF BRITISH COLUMBIAInventors: Raymond J. Andersen, Michel Roberge, Emiliano Manzo
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Publication number: 20080242658Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula IType: ApplicationFiled: April 6, 2005Publication date: October 2, 2008Inventors: Mark G Palermo, Sushil Kumar Sharma, Christopher Straub, Run-Ming Wang, Leigh Zawel, Yanlin Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
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Patent number: 7423031Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activity of CDK1, CDK2, CDK4, CDK5, GSK3?, Bcr-ab1, Flt-3, c-Kit, PDGFR?, Src, Mek1 and CK1.Type: GrantFiled: April 30, 2004Date of Patent: September 9, 2008Assignee: IRM LLCInventors: Yongqin Wan, Nathanael Schiander Gray
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Patent number: 7419967Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: August 25, 2005Date of Patent: September 2, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R Hale, Clarence W Andrews, III, Eric S Furfine, Ronald G Sherrill, Andrew Spaltenstein, Gregory T Lowen
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Publication number: 20080188457Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of one or more biguanides in combination with one or more GSK3-? agents, to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: February 1, 2008Publication date: August 7, 2008Applicant: BrainCells, Inc.Inventors: Carrolee Barlow, Todd Carter, Andrew Morse, Kai Treuner, Kym I. Lorrain
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Patent number: 7384930Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: October 11, 2005Date of Patent: June 10, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Stephen E. Mercer, Haiquan Fang
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Patent number: 7384931Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptorsType: GrantFiled: May 3, 2006Date of Patent: June 10, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Stephen E. Mercer, Haiquan Fang
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Patent number: 7378411Abstract: The present invention relates to thienopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: December 2, 2002Date of Patent: May 27, 2008Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, George D. Hartman, William F. Hoffman