The Other Cyclo In The Bicyclo Ring System Is A Pyrrole Ring (including Hydrogenated) (e.g., Pyrrolo[3,2-d]pyrimidine, Etc.) Patents (Class 514/265.1)
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Publication number: 20130225556Abstract: The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.Type: ApplicationFiled: March 29, 2013Publication date: August 29, 2013Applicant: Incyte CorporationInventor: Incyte Corporation
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Publication number: 20130225577Abstract: The instant invention provides compounds of formula I which are Jak inhibitors, and as such are useful for the treatment of Jak-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: October 17, 2011Publication date: August 29, 2013Inventors: David Joseph Guerin, Jason D. Brubaker, Michelle Martinez, Joon O. Jung, Neville J. Anthony, Mark E. Scott, Carolyn Michele Cammarano, Dawn Marie Mampreian Hoffman, Hyun Chong Woo, Christopher J. Dinsmore, Philip Jones
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Publication number: 20130217682Abstract: Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.Type: ApplicationFiled: February 14, 2013Publication date: August 22, 2013Applicant: Millennium Pharmaceuticals, Inc.Inventor: Millennium Pharmaceuticals, Inc.
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Publication number: 20130209543Abstract: The present invention provides for methods and pharmaceutical compositions comprising inhibitors of mTorC1 and/or mTorC2. In some aspects, the invention provides for treatment regimens resulting in enhanced treatment efficacy and better tolerability.Type: ApplicationFiled: November 21, 2012Publication date: August 15, 2013Applicant: Intellikine LLCInventor: Intellikine LLC
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Publication number: 20130210831Abstract: The present disclosure provides pyrrolopyrimidine compounds and methods of use therefor. For example, the disclosure provides certain pyrrolopyrimidine compounds capable of inhibiting JAK kinases. The disclosure further provides the pharmaceutical compositions containing these pyrrolopyrimidine compounds, and use of these pyrrolopyrimidine compounds in the treatment of disorders or diseases, such as inflammatory diseases and cancer.Type: ApplicationFiled: August 18, 2011Publication date: August 15, 2013Inventors: Wei-Guo Su, Wei Deng, Jinshui Li, Jianguo Ji
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Patent number: 8507508Abstract: There is provided polymorphs and amorphous form of pemetrexed or its pharmaceutical acceptable salts and process for making thereof.Type: GrantFiled: April 4, 2008Date of Patent: August 13, 2013Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Raghavendracharyulu Venkata Palle, Sekhar Munaswamy Nariyam, Vijay Bhailalbhai Patel, Raghupati Rama Subrahmanyam Vinjamuri, Surya Narayana Devarakonda, Sesha Reddy Yarraguntla, Vamsi Krishna Mudapaka, Venu Nalivela
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Publication number: 20130203786Abstract: The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: May 16, 2011Publication date: August 8, 2013Inventors: Jacqueline D. Hicks, Tesfaye Biftu, Ping Chen, Xiaoxia Qian, Robert R. Wilkening
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Patent number: 8501753Abstract: The present disclosure provides novel hemi- and mono-salts of 7-[(3R,4R)-3-Hydroxy-4-hydroxymethyl-pyrrolidin-1-ylmethyl]-3,5-dihydro-pyrrolo[3,2-d]pyrimidin-4-one (Compound 1) with various organic and inorganic acids. In one embodiment, the organic acid is a C4 organic diacids. The present disclosure further provides novel methods for preparing these salts. The novel monohydrates hemisalts of the C4 organic diacids are isostructural and can be prepared with different properties. Multiple acids can be used simultaneously and the proportion of acids can be varied offering the opportunity to select hemi-salts of compound 1 with desired properties.Type: GrantFiled: March 24, 2010Date of Patent: August 6, 2013Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Gary Bartley, Thomas Cleary, John Lang
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Patent number: 8501752Abstract: The present invention provides methods for treating cancer and other pathological proliferating conditions by inhibiting mitosis using at least one pyrrolo[2,3-d]pyrimidine having the general formula (16): where X is selected from the group consisting of lower alkyls, heteroalkyls, substituted or unsubstituted aryls or heteroaryls, arylalkyls, and heteroarylalkyls; where R1 is selected from the group consisting of hydrogen, lower alkyls, heteroalkyls, substituted or unsubstituted aryls or heteroaryls, arylalkyls, and heteroarylalkyls; where R2 is selected from the group consisting of hydrogen, lower alkyls, heteroalkyls, alkoxys, substituted or unsubstituted aryls or heteroaryls; where R3 is selected from the group consisting of zero, lower alkyls, heteroalkyls, alkenyls, and heteroalkenyls; and where R4 is selected from the group consisting of substituted or unsubstituted aryls or heteroaryls, arylalkyls, heteroarylalkyls, and hydrogen.Type: GrantFiled: September 1, 2011Date of Patent: August 6, 2013Assignee: Duquesne University of the Holy GhostInventor: Aleem Gangjee
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Publication number: 20130197016Abstract: The use of vascular endothelial growth factor receptor 2 inhibitors or a pharmaceutically acceptable salt thereof for the treatment of ocular vascular disease is provided. Dosing regimes, including once weekly administration, of certain VEGF-R2 inhibitors are provided which deliver therapeutically effective concentrations of the VEGF-R2 compounds in ocular tissues for at least one week for the treatment of ocular vascular disease.Type: ApplicationFiled: October 25, 2011Publication date: August 1, 2013Inventors: Mitchell Brigell, Peter End, Vinayak Hosagrahara, Bruce D. Jaffee, Erik Meredith, Ronald Keith Newton, Stephen Poor, Yubin Qiu
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Publication number: 20130195954Abstract: Described herein are compounds and processes that can be used to prepare polymer-based films, particles, gels and related compositions, and processes for delivery of agents, and other uses.Type: ApplicationFiled: November 8, 2012Publication date: August 1, 2013Applicants: THE TRUSTEES OF THE BOSTON UNIVERSITY, THE BRIGHAM AND WOMEN'S HOSPITALInventors: The Brigham and Women's Hospital, The Trustees of the Boston University
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Publication number: 20130190320Abstract: The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.Type: ApplicationFiled: January 12, 2013Publication date: July 25, 2013Applicant: ACEA BIOSCIENCES, INC.Inventor: ACEA Biosciences, Inc.
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Publication number: 20130190334Abstract: The invention provides a compound of Formula (I) Z N N O N O A1R2 R1 R3R 3 L A2 (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3,Z, A1, L and A 5 2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: ApplicationFiled: September 20, 2011Publication date: July 25, 2013Applicant: PFIZER INC.Inventors: Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith
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Publication number: 20130183268Abstract: The present invention relates to drug combinations and pharmaceutical compositions for treating hyperproliferative disorders such as cancer including non-small cell lung carcinoma, said drug combination comprising (1) a fluoro-substituted-diaryl urea of Formula (I), (2) at least one antifolate and optionally (3) at least one platinum complex antineoplastic nucleic acid binding agent, where any of these components can be present in the form of a pharmaceutically acceptable salt or other derivative thereof.Type: ApplicationFiled: July 19, 2011Publication date: July 18, 2013Applicant: BAYER HEALTHCARE LLCInventors: Olaf Christensen, Iris Kuss
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Patent number: 8486902Abstract: The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile.Type: GrantFiled: October 8, 2010Date of Patent: July 16, 2013Assignee: Incyte CorporationInventors: James D. Rodgers, Adam Shilling, Argyrios G. Arvanitis, Stacey Shepard, Laurine G. Galya, Mei Li, Frank M. Nedza
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Publication number: 20130178486Abstract: Compounds having the formula I wherein A, R1a, R1b, R2, R3, R4, R5, R6, R7, R8, Ra, Rb, X1, X2, X3 and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: ApplicationFiled: December 21, 2012Publication date: July 11, 2013Applicant: Genentech, Inc.Inventor: Genentech, Inc.
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Patent number: 8481550Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.Type: GrantFiled: August 24, 2011Date of Patent: July 9, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher F. Claiborne, Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
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Publication number: 20130172372Abstract: The present application relates to novel fused 4-aminopyrimidines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: July 5, 2011Publication date: July 4, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li
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Publication number: 20130172314Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: ApplicationFiled: September 14, 2012Publication date: July 4, 2013Applicant: Pharmacyclics, Inc.Inventors: Wei CHEN, David J. Loury
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Publication number: 20130171102Abstract: The invention is related to anti-viral compounds of formula (A) as defined in the claims, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: May 20, 2011Publication date: July 4, 2013Applicant: Gilead Sciences, Inc.Inventors: Kyla Bjornson, Steven S. Bondy, You-chul Choi, Chien-Hung Chou, Ruchika Mishra, James D. Trenkle, Winston C. Tse, Randall W. Vivian, James G. Taylor
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Patent number: 8476282Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. For example, the invention provides compounds of Formula: Also provided in the present invention are methods of using such compounds or compositions, and methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications such as treatment of cancer.Type: GrantFiled: September 17, 2009Date of Patent: July 2, 2013Assignee: Intellikine LLCInventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
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Publication number: 20130165457Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.Type: ApplicationFiled: June 19, 2012Publication date: June 27, 2013Applicant: Millennium Pharmaceuticals, Inc.Inventors: Steven P. Langston, Edward J. Olhava, Stepan Vyskocil
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Patent number: 8470850Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.Type: GrantFiled: May 6, 2010Date of Patent: June 25, 2013Assignee: MethylGene Inc.Inventors: Arkadii Vaisburg, Stephen William Claridge, Franck Raeppel, Oscar Mario Saavedra, Noemy Berstein, Marie-Claude Granger, Lijie Zhan, Amal Wahhab, David Liewellyn
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Publication number: 20130157996Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: June 21, 2012Publication date: June 20, 2013Applicant: Amgen Inc.Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
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Publication number: 20130158028Abstract: The present invention relates to the novel use of stimulators and activators of soluble guanylate cyclase for the treatment of sickle cell anemia and for the preservation of blood substitutes. The present invention furthermore relates to the use of stimulators and activators of soluble guanylate cyclase in combination with PDE5 inhibitors for the treatment of sickle cell anemia and for the preservation of blood substitutes.Type: ApplicationFiled: June 21, 2011Publication date: June 20, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Johannes-Peter Stasch, Eva-Maria Becker, Hubert Trübel, Herbert Himmel
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Publication number: 20130158025Abstract: Disclosed is a novel compound acting as a cannabinoid receptor 1 inhibitor, a prodrug thereof, an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof. The novel compound or the like is useful for preventing or treating diseases mediated by the cannabinoid receptor-1.Type: ApplicationFiled: August 31, 2011Publication date: June 20, 2013Applicant: AMOREPACIFIC CORPORATIONInventors: Song Seok Shin, Yong Deog Hong, Kyoung Hee Byoun, Mi Young Park, Jin Kyu Choi, Yang Hui Park, Il Hong Bae, Yung Hyup Joo, Kyung Min Lim, Young Ho Park
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Publication number: 20130158040Abstract: Disclosed are compounds of Formula (I): useful for treatment of autoimmune and inflammatory diseases associated with IL-2 inhibition via modulation of calcium release-activated calcium (CRAC) channels. Also disclosed are methods of making and using the compounds for treatment of diseases associated with CRAC channels.Type: ApplicationFiled: December 17, 2012Publication date: June 20, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130149392Abstract: The present invention is a method for treating non-small cell lung cancer in a subject in need thereof, comprising administering to the subject an effective amount of a bis(thiohydrazideamide) compound of formula (I): wherein the variables are defined herein. Furthermore, pharmaceutical compositions, combination therapies, and uses thereof are also provided in the present application.Type: ApplicationFiled: December 12, 2011Publication date: June 13, 2013Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Wei Guo, Vojo Vukovic
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Publication number: 20130150342Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: February 17, 2011Publication date: June 13, 2013Applicant: NOVARTIS AGInventors: Christopher Thomas Brain, Young Shin Cho, John William Giraldes, Bharat Lagu, Julian Roy Levell, Michael J. Luzzio, Lawrence Blas Perez, Yaping Wang, Fan Yang
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Patent number: 8461165Abstract: The invention relates to the compounds of formula I, their preparation and the pharmaceutical compositions containing the compounds. The invention also relates to the use of the compounds of formula I in preparing medicines, which can treat sexual dysfunction of animals including human (male and female), especially erectile dysfunction of male and the diseases in which the function of phospholipase 5 (cGMP PDE5) is involved.Type: GrantFiled: January 11, 2010Date of Patent: June 11, 2013Assignees: Yangtze River Pharmaceutical (Group) Co., Ltd, Tianjin North Pharma Sci-Tech Co., LtdInventors: Yongfeng Wang, Kejun Zhao
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Patent number: 8455505Abstract: The compound of formula (I) is an inhibitor of human neutrophil elastase, useful for inhalation treatment of pulmonary inflammation.Type: GrantFiled: January 22, 2010Date of Patent: June 4, 2013Assignee: Chiesi Farmaceutici S.p.A.Inventors: Christine Edwards, Janus Kulagowski, Harry Finch
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Publication number: 20130137709Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.Type: ApplicationFiled: May 5, 2011Publication date: May 30, 2013Inventors: Nathanael S. Gray, Wenjun Zhou
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Publication number: 20130137681Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: January 30, 2013Publication date: May 30, 2013Applicant: INCYTE CORPORATIONInventor: INCYTE CORPORATION
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Patent number: 8450332Abstract: Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use.Type: GrantFiled: June 1, 2012Date of Patent: May 28, 2013Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Hugh Alfred Burgoon, Nicole Cathleen Goodwin, Bryce Alden Harrison, Jason Patrick Healy, Ying Liu, Ross Mabon, Brett Marinelli, David Brent Rawlins, Dennis Stewart Rice, Norris Andrew Whitlock
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Patent number: 8450331Abstract: In its many embodiments, the present invention provides certain thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds (or tautomers or a pharmaceutically acceptable salts thereof) having the structural Formula (III): wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's Disease, are also disclosed.Type: GrantFiled: April 21, 2009Date of Patent: May 28, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Zhaoning Zhu, Andrew Stamford, Mihirbaran Mandal, Xiaoxiang Liu
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Patent number: 8450329Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. For example, the invention provides compounds of Formula: Also provided in the present invention are methods of using such compounds or compositions, and methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications such as treatment of cancer.Type: GrantFiled: September 17, 2009Date of Patent: May 28, 2013Assignee: Intellikine LLCInventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
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Patent number: 8445501Abstract: The compounds of Formula (I), in which R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the N-oxides of the compounds and the salts thereof and the stereoisomers of the compounds, the salts, the N-oxides of the compounds and the N-oxides of the salts thereof are effective inhibitors of the type 5 phosphodiesterase.Type: GrantFiled: February 25, 2009Date of Patent: May 21, 2013Assignee: Takeda GmbHInventors: Josef Stadlwieser, Beate Schmidt, Heiko Bernsmann, Alexander Sudau, Torsten Dunkern, Degenhard Marx, Jörg Diefenbach
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Publication number: 20130123284Abstract: Provided herein are compounds useful for kinase inhibition.Type: ApplicationFiled: March 24, 2011Publication date: May 16, 2013Applicant: AMITECH THERAPEUTIC SOLUTIONS INCInventors: Lee Daniel Arnold, Eric A. Murphy
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Patent number: 8440689Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.Type: GrantFiled: December 17, 2010Date of Patent: May 14, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Yasuyoshi Arikawa, Qing Dong, Victoria Feher, Benjamin Jones, Betty Lam, Zhe Nie, Christopher Smith, Masashi Takahashi
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Publication number: 20130116260Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.Type: ApplicationFiled: December 17, 2010Publication date: May 9, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yasuyoshi Arikawa, Benjamin Jones, Betty Lam, Zhe Nie, Christopher Smith, Masashi Takahashi, Qing Dong, Victoria Feher
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Publication number: 20130116268Abstract: Disclosed herein are methods and materials for improving vision. Particularly exemplified herein are pyrimidine compounds that serve to proliferate retinal stem cells.Type: ApplicationFiled: September 25, 2012Publication date: May 9, 2013Inventors: Kiminobu Sugaya, Tingyu Qu
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Publication number: 20130101680Abstract: The present invention relates to a method of treating pancreatic cancer in a subject in need thereof by administering an effective amount of a composition containing (A) tegafur and (B) gimeracil in conjunction with radiotherapy.Type: ApplicationFiled: December 17, 2012Publication date: April 25, 2013Inventor: Masakazu FUKUSHIMA
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Patent number: 8426428Abstract: Provided herein are electrophilically enhanced kinase inhibitors of Formula I. Also provided herein are methods of making and utilizing the same.Type: GrantFiled: December 5, 2008Date of Patent: April 23, 2013Assignee: Principia Biopharma, Inc.Inventor: Richard Miller
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Publication number: 20130096141Abstract: Compounds of structural formula I: are GPR119 agonists and are useful for the treatment, control or prevention of disorders responsive to agonism of GPR119, such as metabolic-related disorders such as type I diabetes, type II diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia or syndrome X. The compounds are also reported as being useful for controlling weight gain, controlling food intake, and inducing satiety in mammals.Type: ApplicationFiled: June 14, 2011Publication date: April 18, 2013Inventors: Bernard R. Neustadt, Hong Liu
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Publication number: 20130096144Abstract: The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases.Type: ApplicationFiled: October 12, 2012Publication date: April 18, 2013Applicant: Incyte CorporationInventor: Incyte Corporation
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Patent number: 8420657Abstract: The invention relates to compounds of formula I and salts thereof wherein the substituens are as defined in the specification, processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.Type: GrantFiled: February 5, 2009Date of Patent: April 16, 2013Assignee: Novartis AGInventors: Christoph Gaul, Marc Gerspacher, Philipp Holzer, Carole Pissot Soldermann
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Patent number: 8415362Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines of Formula I: that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: June 12, 2008Date of Patent: April 9, 2013Assignee: Incyte CorporationInventors: James D. Rodgers, Stacey Shepard, Thomas P. Maduskuie, Haisheng Wang, Nikoo Falahatpisheh, Maria Rafalski, Argyrios G. Arvanitis, Louis Storace, Ravi Kumar Jalluri
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Patent number: 8410089Abstract: A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: wherein P: substituted 6-membered aromatic ring, Q: (substituted) 6-membered aromatic ring, A1: CR4aR4b, NR4c, O, S, SO or SO2 {R4a-4c: H etc.}, L1: (substituted) C1-5 alkylene, L2: a bond or (substituted) C1-3 alkylene, L3-4: (substituted) C1-3 alkylene, R1: H, X, CN, (substituted) hydrocarbon, (substituted) heterocycle or (substituted) OH, or (substituted) 4- to 8-membered (heterocyclic) ring together with A1, R2: H, CN, (substituted) hydrocarbon, and R3a: —COSRA1, (substituted) 5- or 6-membered aromatic ring {RA1: (substituted) hydrocarbon or (substituted) heterocycle}.Type: GrantFiled: February 17, 2010Date of Patent: April 2, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Kentaro Rikimaru, Hiroshi Imoto, Masahiro Kamaura
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Publication number: 20130079323Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.Type: ApplicationFiled: September 10, 2010Publication date: March 28, 2013Applicant: TRIUS THERAPEUTICS, INC.Inventors: Christopher J. Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
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Publication number: 20130079324Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.Type: ApplicationFiled: September 14, 2012Publication date: March 28, 2013Inventors: Hengmiao Cheng, Theodore Otto Johnson, JR., John Charles Kath, Kevin Kun-Chin Liu, Elizabeth Ann Lunney, Asako Nagata, Sajiv Krishnan Nair, Simon Paul Planken, Scott Channing Sutton