Plural Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 514/212.06)
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Publication number: 20130115313Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: November 9, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130115310Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: November 9, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130115314Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: November 9, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130115312Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: November 9, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130115311Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: November 9, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130095193Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: September 4, 2012Publication date: April 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, Somhairle MacCormick, Pierre-Henri Storck, Joanne Pinder, Michael Edward O'Donnell, Ronald Marcellus Alphonsus Knegtel, Stephen Clinton Young, Philip Michael Reaper, Steven John Durrant, Heather Clare Twin, Christopher John Davis
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Publication number: 20130053365Abstract: Provided are inhibitors of poly(ADP-ribose)polymerase according to Formula (M): where A, B, Y, Z, D, E, R1, R2, R3, and R4 are as defined herein. Also described are pharmaceutical compositions, methods of preparing, and methods of using a compound of Formula M to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: ApplicationFiled: August 29, 2012Publication date: February 28, 2013Applicant: BioMarin Pharmaceutical, Inc.Inventors: Bing Wang, Daniel Chu
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Publication number: 20130029972Abstract: The present invention provides a compound, or a pharmaceutically acceptable salt or hydrate, and a pharmaceutical composition containing said compound, or a pharmaceutically acceptable salt or hydrate, useful as a Notch pathway signaling inhibitor for the treatment of cancer.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicant: ELI LILLY AND COMPANYInventors: Philip Arthur HIPSKIND, Gregory Alan STEPHENSON
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Publication number: 20120316154Abstract: The present invention relates to certain lactam ring-containing compounds of the Formula (I) and pharmaceutically acceptable salts thereof, wherein D, E, X1, R1, R2, R3, R4, R9, and R10 are as herein described. In addition, the invention relates to pharmaceutically acceptable compositions comprising at least one such compound, and methods of using the compounds for treating or preventing various inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, asthma, and chronic obstructive pulmonary disorder.Type: ApplicationFiled: December 9, 2010Publication date: December 13, 2012Inventors: Dong Xiao, Anandan Palani, Robert G Aslanian, Sylvia Degrado, Xianhai Huang, Wei Zhou, Michael Sofolarides, Xiao Chen
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Patent number: 8329682Abstract: 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: GrantFiled: May 14, 2008Date of Patent: December 11, 2012Assignee: Shanghai Hengrui Pharmaceutical Co., Ltd.Inventors: Peng Cho Tang, Yidong Su, Yali Li, Lei Zhang, Fuqiang Zhao, Jialiang Yang, Ying Zhou, Pingyan Bie, Guangtao Qian, Minggang Ju
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Publication number: 20120309743Abstract: 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: August 9, 2012Publication date: December 6, 2012Applicant: 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: 8324204Abstract: 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: GrantFiled: June 4, 2007Date of Patent: December 4, 2012Assignee: UCB Pharma SAInventors: 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: 20120302550Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.Type: ApplicationFiled: February 10, 2011Publication date: November 29, 2012Applicant: Pfizer Inc.Inventors: Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
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Publication number: 20120302551Abstract: 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: August 9, 2012Publication date: November 29, 2012Applicant: 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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Publication number: 20120295887Abstract: Pharmaceutically acceptable salts of pyrrolo-nitrogenous heterocyclic derivatives, preparation method and medical use thereof are disclosed. More specifically, pharmaceutically acceptable salts of (R,Z)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-methylene)-5-(2-hydroxy-3-morpholinyl-4-yl-propyl)-3-methyl-5,6,7,8-tetrahydro-1H-pyrrolo[3,2-c]azepin-4-one presented by formula (I), the preparation method and the use thereof as therapeutic agents, especially as protein kinase inhibitors, are disclosed.Type: ApplicationFiled: January 7, 2011Publication date: November 22, 2012Applicants: SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD., JIANGSU HENGRUI MEDICINE CO., LTD.Inventor: Peng Cho Tang
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Patent number: 8304408Abstract: The invention provides dBHD-based compositions and dBHD analog compositions, and pharmaceutical compositions comprising them, e.g., in the form of liposomes and nanoparticles comprising them, and methods of making and using them. In one embodiment, these dBHD analogs are used to inhibit a dysfunctional stem cell and/or a cancer (tumor) stem cell.Type: GrantFiled: May 15, 2008Date of Patent: November 6, 2012Assignee: The Regents of the University of CaliforniaInventors: Wolfgang Wrasidlo, Catriona H. Jamieson, Dennis Carson, Tadeusz F. Molinski, Desheng Lu
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Publication number: 20120270857Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: June 30, 2010Publication date: October 25, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. Guzzo, David D. Manning, William Earley
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Publication number: 20120258955Abstract: The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.Type: ApplicationFiled: December 16, 2010Publication date: October 11, 2012Applicant: JANSSEN PHARMACEUTICA NVInventors: Gregor James MacDonald, Andrés Avelino Trabanco-Suárez, Susana Conde-Ceide, Gary John Tresadern, José Manuel Bartolomé-Nebreda, Joaquin Pastor-Fernández
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Publication number: 20120251491Abstract: The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.Type: ApplicationFiled: May 12, 2010Publication date: October 4, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge, Craig A. Coburn
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Publication number: 20120219641Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: February 14, 2012Publication date: August 30, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: David D. Manning, Christopher Lawrence Cioffi
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Publication number: 20120214794Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: October 13, 2011Publication date: August 23, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
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Publication number: 20120207769Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: April 26, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: 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: 8242105Abstract: 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 tumors.Type: GrantFiled: September 25, 2007Date of Patent: August 14, 2012Assignee: Forschungsverbund Berlin E.V.Inventors: Ronald Kuehne, Hartmut Oschkinat, Christoph Brockmann, Hans-Guenther Schmalz, Jan Zaminer
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Publication number: 20120202750Abstract: 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: January 23, 2012Publication date: August 9, 2012Applicant: Genentech, Inc.Inventors: 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: 20120195985Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT-1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: March 21, 2012Publication date: August 2, 2012Applicant: Amgen Inc.Inventors: Stephen Hitchcock, Albert Amegadzie, Wenyuan Qian, Xiaoyang Xia, Scott S. Harried
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Publication number: 20120184519Abstract: The invention includes compositions and methods for regulating PI3K p110 delta as an anti-retroviral therapy. The invention includes inhibiting p110 delta, a component of PI3K p110 delta signaling pathway, or any combination thereof in a cell as an anti-retroviral therapeutic approach for treating a retroviral infection, for example HIV. The invention includes a method of modulating PI3K p110 delta in a cell infected with a retrovirus by contacting the cell with an effective amount of a composition comprising an inhibitor of PI3K p110 delta.Type: ApplicationFiled: March 12, 2012Publication date: July 19, 2012Inventors: Peter D. Katsikis, Alina C. Boesteanu, Martin Turner
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Publication number: 20120184530Abstract: 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: March 27, 2012Publication date: July 19, 2012Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventor: Stephen M. CONDON
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Publication number: 20120178739Abstract: 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: March 14, 2012Publication date: July 12, 2012Applicant: 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: 20120172348Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 22, 2010Publication date: July 5, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
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Publication number: 20120070409Abstract: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: ApplicationFiled: February 3, 2011Publication date: March 22, 2012Applicant: Japan Tobacco Inc.Inventors: Takahiro Oka, Kazutaka Ikegashira, Shintaro Hirashima, Hiroshi Yamanaka, Satoru Noji, Yasushi Niwa, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yukihiro Nomura
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Publication number: 20120065190Abstract: Compounds of formula I: (wherein variables A1, m, R1, R2, R3, R4 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: December 14, 2007Publication date: March 15, 2012Inventors: Ian M. Bell, Harold G. Selnick
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Patent number: 8124600Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: GrantFiled: May 28, 2009Date of Patent: February 28, 2012Assignee: Albany Molecular Research, Inc.Inventors: David D. Manning, Christopher Lawrence Cioffi
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Publication number: 20120046242Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.Type: ApplicationFiled: December 21, 2009Publication date: February 23, 2012Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Travis L. BIechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
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Patent number: 8110568Abstract: 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: GrantFiled: March 18, 2010Date of Patent: February 7, 2012Assignee: Genentech, Inc.Inventors: 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: 20120010178Abstract: Methods, compounds and compositions for promoting motor neuron survival and the treatment of a neurodegenerative disorders such as Spinal Muscular Atrophy (SMA) are described herein.Type: ApplicationFiled: October 21, 2009Publication date: January 12, 2012Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Lee Rubin, Amy Sinor, Nina Ruslanovna Makhortova, Yin Miranda Yang, Monica Hayhurst Bennett
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Publication number: 20120003318Abstract: Methods of treating atrial arrhythmia include administering an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof, such that the at least one antiarrhythmic pharmaceutical agent first enters the heart through the pulmonary vein to the left atrium. Other methods of treating atrial arrhythmia include administering by inhalation an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof. An amount of the at least one antiarrhythmic pharmaceutical agent may peak in the coronary sinus of the heart at a time ranging from 10 seconds to 30 minutes from initiation of the administering. Unit doses, aerosols, and kits are also contemplated.Type: ApplicationFiled: March 18, 2010Publication date: January 5, 2012Inventors: Carlos A. Schuler, Rangachari Narasimhan
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Publication number: 20110257157Abstract: 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: June 30, 2011Publication date: October 20, 2011Applicant: 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: 7998952Abstract: 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: GrantFiled: December 4, 2009Date of Patent: August 16, 2011Assignee: 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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Publication number: 20110178163Abstract: The present disclosure provides methods of determining the levels of BRCA1 in a cell, altering the levels of BRCA1 in a cell, determining the likelihood of developing cancer, and determining the prognosis of a patient with cancer using miR-182 and analogs thereof. Importantly, the invention also provides methods of determining whether a patient should be treated with PARP inhibitors, improving PARP therapy in cancer, as well as methods for selecting and improving genotoxic therapies. Also featured are methods of treating patients with cancers based on the expression levels of miR-182. The invention also features compositions comprising miR-182 and analogs thereof, antagomirs of mIR-182 and analogs thereof, in combination with PARP inhibitors and genotoxic agents.Type: ApplicationFiled: January 13, 2011Publication date: July 21, 2011Inventor: Dipanjan Chowdhury
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Patent number: 7968535Abstract: This invention relates to the use of azapaullones, particularly in combination with immunomodulating agents, in the prevention, and/or treatment of pancreatic autoimmune disorders, e.g. type I diabetes or LADA and neurodegenerative disorders.Type: GrantFiled: May 4, 2006Date of Patent: June 28, 2011Assignees: Develogen Atkiengesellschaft, Technische Universitaet Carolo-Wilhelmina Zu BraunschweigInventors: Rainer Mussmann, Conrad Peter Kunick, Hendrik Stukenbrock, Marcus Geese, Simone Kegel, Ulrike Burk
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Patent number: 7968536Abstract: The present invention provides compounds useful as inhibitors of protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: GrantFiled: June 30, 2008Date of Patent: June 28, 2011Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.Inventors: 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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Publication number: 20110136788Abstract: [Problem] The present invention aims to provide an agent for the prophylaxis or treatment of irritable bowel syndrome. [Solving Means] An agent for the prophylaxis or treatment of irritable bowel syndrome, containing a compound having a TGR5 receptor agonist activity, a fused ring compound represented by the formula wherein ring A is an optionally substituted aromatic ring, and ring B? is a 5- to 9-membered ring having one or more substituents, or a salt thereof as an active ingredient.Type: ApplicationFiled: August 6, 2009Publication date: June 9, 2011Inventor: Minoru Maruyama
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Patent number: 7951795Abstract: Compounds of formula I: (wherein variables A1, A2, A3, G1, G2, G3, J, m, n, p, R1, R2, R3, R4 and Y 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: GrantFiled: December 5, 2007Date of Patent: May 31, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Harold G. Selnick
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Patent number: 7947677Abstract: 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, J, K, 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: GrantFiled: November 14, 2006Date of Patent: May 24, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman, Harold G. Selnick
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Publication number: 20110118231Abstract: 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: November 19, 2010Publication date: May 19, 2011Applicants: 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: 7935694Abstract: 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: September 4, 2008Date of Patent: May 3, 2011Assignee: 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: 20110086834Abstract: Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. 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, inflammation and the like.Type: ApplicationFiled: June 26, 2009Publication date: April 14, 2011Applicant: AMGEN INC.Inventors: Guoqing Chen, Timothy D. Cushing, Paul Faulder, Benjamin Fisher, Xiao He, Kexue Li, Zhihong Li, Wen Liu, Lawrence R. Mcgee, Vatee Pattaropong, Jennifer L. Seganish, Youngshook Shin, Zhulun Wang
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Publication number: 20110053911Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.Type: ApplicationFiled: March 13, 2009Publication date: March 3, 2011Inventors: Raffaele Ingenito, Philip Jones, Laura Llauger Bufi, Jesus Maria Ontoria Ontoria, Rita Scarpelli
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Publication number: 20110053910Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: ApplicationFiled: July 3, 2006Publication date: March 3, 2011Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Patent number: 7897595Abstract: The present invention relates to pyridoazepine derivatives that act as 5-HT ligands, e.g., 5-HT2 C. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: GrantFiled: May 23, 2007Date of Patent: March 1, 2011Assignee: Forest Laboratories Holdings LimitedInventors: Gian-Luca Araldi, Alexander Bischoff, Nhut K. Diep