Plural Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/234.5)
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Patent number: 8258145Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to the use of these compounds in treating brain cancer.Type: GrantFiled: July 3, 2007Date of Patent: September 4, 2012Assignee: Myrexis, Inc.Inventors: Sui Xiong Cai, Mark B. Anderson, Adam Willardsen, Nilantha Sudath Sirisoma
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Publication number: 20120220570Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.Type: ApplicationFiled: August 25, 2010Publication date: August 30, 2012Applicant: Takeda Pharmaceutical Company LimitedInventors: Satoshi Sasaki, Yuta Tanaka
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Publication number: 20120220587Abstract: Compounds of the formula (I), in which X1, X2, L, Y, R2, R3, R4, R5, R6, R7, R8, R9, R10 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.Type: ApplicationFiled: September 6, 2010Publication date: August 30, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Ulrich Emde, Hans Peter Buchstaller, Markus Klein, Christina Esdar, Joerg Bomke
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Publication number: 20120220588Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, and methods of making and using the same.Type: ApplicationFiled: November 1, 2010Publication date: August 30, 2012Inventors: Lara S. Kallander, Brian Griffin Lawhorn, Joanne Philp
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Patent number: 8252790Abstract: Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HT2B receptor. The compound and salt are useful for treatment or prevention of various diseases and conditions associated with a 5-HT2B receptor.Type: GrantFiled: November 24, 2009Date of Patent: August 28, 2012Assignee: Raqualia Pharma Inc.Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Tadashi Inoue, Yuji Shishido, Hiroaki Ito
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Patent number: 8252793Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: GrantFiled: August 17, 2011Date of Patent: August 28, 2012Assignees: Alcon Research, Ltd., Astellas Pharma Inc.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
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Patent number: 8252792Abstract: Thienopyrimidines of formula (Ia) or (Ib): wherein R1-R3 have any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase, in particular the p110 delta subtype, such as immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.Type: GrantFiled: April 25, 2007Date of Patent: August 28, 2012Assignee: F. Hoffman-La Roche AGInventors: Stewart James Baker, Paul John Goldsmith, Timothy Colin Hancox, Neil Anthony Pegg, Stephen Price, Stephen Joseph Shuttleworth, Sukhjit Sohal
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Publication number: 20120214762Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: March 15, 2012Publication date: August 23, 2012Applicant: Genentech, Inc.Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A.G.N. Montalbetti
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Patent number: 8247423Abstract: Described herein are compositions and methods for using these compositions in the treatment of cancer, tumors, and tumor-related disorders in a subject.Type: GrantFiled: July 11, 2008Date of Patent: August 21, 2012Assignee: Tragara Pharmaceuticals, Inc.Inventors: Thomas M. Estok, Sara L. Zaknoen, Robert K. Mansfield, Tracy Lawhon
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Publication number: 20120208811Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.Type: ApplicationFiled: August 5, 2010Publication date: August 16, 2012Applicants: F. HOFFMANN-LA ROCHE AG, CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
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Publication number: 20120208812Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: October 21, 2010Publication date: August 16, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode-Johnson, Emily M. Stocking, Devin M. Swanson
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Publication number: 20120207751Abstract: The invention relates to a combination comprising compounds of formula (I) and one or more other antiproliferative compounds, hormones or radiation, pharmaceutical preparations comprising the combination thereof, and the application thereof in a process for the treatment of tumors.Type: ApplicationFiled: April 23, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: Carlos Garcia-Echeverria, Frédéric Stauffer, Pascal Furet
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Publication number: 20120208794Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.Type: ApplicationFiled: August 25, 2010Publication date: August 16, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Satoshi Sasaki, Yuta Tanaka
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Publication number: 20120202784Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. 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.Type: ApplicationFiled: January 13, 2012Publication date: August 9, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, JR., Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Suganthini S. Nanthakumar, Jingrong Cao, Upul Keerthi Bandarage, Anne-Laure Grillot
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Publication number: 20120202793Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2, which may be selective for ROCK2, and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and/or ROCK2. Also provided are treatments combining inhibitors of ROCK1 and/or ROCK2 with statins.Type: ApplicationFiled: March 9, 2010Publication date: August 9, 2012Inventors: Paul Sweetnam, Alessandra Bartolozzi, Anthony Stewart Campbell, Bridget Cole, Hope Foudoulakis, Brian Kirk, Hemalatha Seshadri, Siya Ram
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Publication number: 20120196856Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 26, 2010Publication date: August 2, 2012Inventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
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Publication number: 20120196851Abstract: The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: ApplicationFiled: October 6, 2010Publication date: August 2, 2012Applicant: SIENA BIOTECH S.P.A.Inventors: Maurizio Varrone, Arianna Nencini, Joanna Margaret Quinn, Andrea Caricasole, Annette Cornelia Bakker, Giovanni Gaviraghi, Massimilano Salerno
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Publication number: 20120190680Abstract: Compounds, pharmaceutical compositions, and methods of use are disclosed for heteroaryl amide analogues of formula Ia and/or Ib: In certain embodiments, the heteroaryl amide analogues are agonists and/or ligands of dopamine receptors and may be useful, inter alia, for the treatment of a condition responsive to P2X7 receptor modulation, for example, pain, inflammation, a neurological or neurodegenerative disorder, a cardiovascular disorder, an ocular disorder or an immune system disorder.Type: ApplicationFiled: August 11, 2008Publication date: July 26, 2012Applicant: H. LUNDBECK A/SInventors: Rajagopal Bakthavatchalam, David C. Ihle, Scott M. Capitosti, David J. Wustrow, Jun Yuan
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Publication number: 20120190673Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.Type: ApplicationFiled: December 19, 2011Publication date: July 26, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio BERDINI, Maria Grazia CARR, Adrian Liam GILL, Steven HOWARD, Eva Figueroa NAVARRO, Gary TREWARTHA, David Charles REES, Mladen VINKOVIC, Paul Graham WYATT
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Publication number: 20120184522Abstract: A subject-matter of the present invention is the use of compounds of formula (I) in the base, hydrate or solvate form or in the form of their mixtures, as medicaments or for the preparation of medicaments intended for the treatment of at least one cardiovascular disease and/or to prevent the appearance of at least one cardiovascular disease.Type: ApplicationFiled: October 7, 2011Publication date: July 19, 2012Applicant: SANOFIInventors: Philip JANIAK, Gilbert MARCINIAK, Jean-Francois NAVE, Fabrice VIVIANI
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Publication number: 20120184535Abstract: A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.Type: ApplicationFiled: December 28, 2011Publication date: July 19, 2012Applicant: SELVITA S.A.Inventors: Krzysztof BRZÓZKA, Wojciech CZARDYBON, Aleksandra SABINIARZ, Mariusz MILLIK, Renata WINDAK, Adrian ZAREBSKI, Nicolas BEUZEN
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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: 20120184523Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: March 22, 2012Publication date: July 19, 2012Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takbuchi, Yong Wang, Wei Xu
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Patent number: 8221737Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 15, 2010Date of Patent: July 17, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Publication number: 20120178723Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 11, 2011Publication date: July 12, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Publication number: 20120177641Abstract: Disclosed is the identification, provision and use of a panel of biomarkers that predict sensitivity or resistance to EGFR inhibitors, and products and processes related thereto. In one embodiment, a method is described for selecting a cancer patient who is predicted to benefit from therapeutic administration of an EGFR inhibitor, an agonist thereof, or a drug having substantially similar biological activity as EGFR inhibitor. Also described is a method to identify molecules that interact with the EGFR pathway to allow or enhance responsiveness to EGFR inhibitors, as well as a plurality of polynucleotides or antibodies for detection of the expression of genes that are indicative of sensitivity or resistance to EGFR inhibitors, an agonist thereof, or a drug having substantially similar biological activity as EGFR inhibitors. A method to identify a compound with the potential to enhance the efficacy of EGFR inhibitors is also described.Type: ApplicationFiled: March 12, 2012Publication date: July 12, 2012Inventors: Paul A. BUNN, Christopher D. COLDREN, Wilbur A. FRANKLIN, Mark W. GERACI, Barbara A. HELFRICH, Fred R. HIRSCH, Razvan LAPADAT, Michio SUGITA, Samir E. WITTA
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Patent number: 8217037Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.Type: GrantFiled: April 5, 2007Date of Patent: July 10, 2012Assignees: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, B.V. Patel Pharmaceutical Education & Research Development (PERD)Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Swapnil G. Yerande, Gajanan S. Inamdar, Vasudevan Sudarsanam
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Publication number: 20120171245Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.Type: ApplicationFiled: December 15, 2011Publication date: July 5, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann
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Publication number: 20120172345Abstract: This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 11, 2011Publication date: July 5, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Yongbo Hu, Todd B. Sells, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Publication number: 20120165305Abstract: The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases.Type: ApplicationFiled: December 21, 2011Publication date: June 28, 2012Inventors: Wenqing YAO, Colin ZHANG, Meizhong XU, Jincong ZHUO, Chunhong HE
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Publication number: 20120165307Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. 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.Type: ApplicationFiled: March 1, 2012Publication date: June 28, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Luc Farmer, Gabriel Matinez-Botella, Albert Pierce, Francesco Salituro, Jian Wang, Marion Wannamaker, Tiansheng Wang
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Publication number: 20120165309Abstract: [Object] A novel and excellent method for preventing or treating rejection in the transplantation of various organs, allergy diseases, autoimmune diseases, hematologic tumor, or the like, based on a PI3K?-selective inhibitory action and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), is provided [Means for Solution] It was found that a 3-substituted triazine or 3-substituted pyrimidine derivative exhibits a PI3K?-selective inhibitory action, and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), and can be an agent for preventing or treating rejection in the transplantation of various organs, allergy diseases (asthma, atopic dermatitis, etc.), autoimmune diseases (rheumatoid arthritis, psoriasis, ulcerative colitis, Crohn's disease, systemic lupus erythematosus, etc.), hematologic tumor (leukemia etc.Type: ApplicationFiled: February 10, 2010Publication date: June 28, 2012Applicant: Astellas Pharma Inc.Inventors: Fumie Takahashi, Sunao Imada, Masahiko Shiwaku, Yasumasa Shiwaku, Atsuko Shiwaku, Koji Kato, Hidehiko Fukahori
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Publication number: 20120165330Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: December 22, 2010Publication date: June 28, 2012Applicant: Sirtris Pharmaceuticals, Inc.Inventor: Chi B. Vu
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Publication number: 20120156197Abstract: Provided is a method of treating a proliferative disease, condition, or disorder in a subject by administering a combination of an inhibitor of p53 and MDM2 binding and an EGFR inhibitor. Various embodiments of the disclosed methods provide a synergistic anti-proliferative or anti-apoptotic effect compared to administration of one agent alone.Type: ApplicationFiled: July 21, 2011Publication date: June 21, 2012Inventors: Joseph P. Errico, Benjamin Mugrage, Ignatius Turchi, Matthew Sills, Jane Ong, John Allocco, Pam Wines
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Publication number: 20120157412Abstract: The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.Type: ApplicationFiled: February 28, 2012Publication date: June 21, 2012Inventors: Kathleen A. Battista, Gilles C. Bignan, Guozhang Xu, Lily Lee, Terry V. Hughes, Steven K. Wetter, Peter J. Connolly, Marta C. Abad, Stuart L. Emanuel, Prabha S. Karnachi, Steven A. Middleton
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Publication number: 20120156228Abstract: The invention features methods, kits, and compositions for generating new hair follicles and growing hair on a subject.Type: ApplicationFiled: September 9, 2011Publication date: June 21, 2012Applicants: Follica, Inc., The Trustees Of The University of PennsylvaniaInventors: David Steinberg, Kevin Pojasek, Stephen Prouty, George Cotsarelis, Mayumi Ito
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Publication number: 20120149686Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.Type: ApplicationFiled: April 6, 2010Publication date: June 14, 2012Applicant: University Health NetworksInventors: Peter B. Sampson, Yong liu, Sze-Wan Le, Brian T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
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Publication number: 20120149676Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: June 14, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Alexander HEIM-RIETHER, Raimund KUELZER, Roland PFAU, Klaus RUDOLF, Dirk STENKAMP
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Publication number: 20120148678Abstract: We have disclosed an implantable sustained release composition comprising, a biocompatible, biodegradable polymer, a cyclodextrin inclusion complex of a poorly water soluble pharmaceutical agent present, and a plasticizer, where the polymer is the minority phase of the formulation. Furthermore, The we disclose an implantable sustained release composition that provides a detectable plasma level of an otherwise poorly soluble drug for at least 28 days.Type: ApplicationFiled: December 8, 2010Publication date: June 14, 2012Applicant: Advanced Technologies and Regenerative Medicine, LLC.Inventors: Deborah M. Schachter, Qiang Zhang, Peter Van Remoortere, Yufu Li
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Publication number: 20120148534Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.Type: ApplicationFiled: March 16, 2010Publication date: June 14, 2012Inventors: Jeffrey S. Glenn, Wenjin Yang, Ingrid C. Choong
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Patent number: 8198273Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer.Type: GrantFiled: May 4, 2010Date of Patent: June 12, 2012Assignee: Plexxikon Inc.Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Guoxian Wu
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Publication number: 20120142686Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:Type: ApplicationFiled: October 20, 2011Publication date: June 7, 2012Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
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Publication number: 20120141472Abstract: Disclosed herein are methods of predicting prognosis of a neoplastic disease (such as lung cancer, for example NSCLC), including determining the IGF1R gene copy number in a biological sample from a patient having a neoplastic disease; wherein an increase in IGF1R copy number predicts a good prognosis of the neoplastic disease in the patient. Also disclosed herein are methods of scoring copy number of a gene of interest in a biological sample. The method includes identifying individual cells in the sample having highest number of signals for the gene of interest detected by in situ hybridization, counting the number of signals for the gene of interest in the identified individual cells and determining an average number of signals per cell.Type: ApplicationFiled: May 28, 2010Publication date: June 7, 2012Inventors: Shalini Singh, Fabien Gaire, James Ranger-Moore
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Publication number: 20120142685Abstract: The present invention provides a compound formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: April 4, 2008Publication date: June 7, 2012Inventors: Markus Rolf Dobler, Charles Francis Jewell, JR., Erik Meredith, Lauren G. Monovich, Sarah Siska, Anette Von Matt, Maurice Van Eis, Taeyoung Yoon, Christoph Gaul, Michael Paul Capparelli
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Patent number: 8193177Abstract: Methods are provided for treating fibrotic connective tissue diseases such as scleroderma and conditions such as surgically-induced adhesions using compounds that activate the signaling pathways of hepatocyte growth factor.Type: GrantFiled: November 13, 2008Date of Patent: June 5, 2012Assignee: Angion Biomedica Corp.Inventor: Latha Paka
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Publication number: 20120135990Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: ApplicationFiled: May 27, 2010Publication date: May 31, 2012Applicant: TETRALOGIC PHARMACEUTICALS CORP.Inventors: Stephen M. Condon, Yijun Deng, Matthew D. Alexander, Matthew G. Laporte
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Publication number: 20120135989Abstract: The present invention provides a (di)azaindole derivative represented by the formula (I). A compound of the present invention inhibits a Cdc7 protein kinase activity and suppresses cell proliferation.Type: ApplicationFiled: June 29, 2011Publication date: May 31, 2012Applicants: CRYSTALGENOMICS, INC., SBI BIOTECH CO., LTD.Inventors: Yoko Funakoshi, Chika Tanaka, Choul Hong Park, Seong Gu Ro
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Publication number: 20120135953Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: ApplicationFiled: August 6, 2010Publication date: May 31, 2012Applicant: Tibotec PharmaceuticalsInventors: David Mc Gowan, Samuel Dominique Demin, Stefaan Julien Last, Koen Vandyck, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20120129851Abstract: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.Type: ApplicationFiled: October 31, 2011Publication date: May 24, 2012Applicant: Endo Pharmaceuticals Inc.Inventors: Roger Astbury Smith, Scott Kevin Thompson, Subramanya Hosahalli, Mallesham Bejugam, Srinivas Nanduri, Sunil Kumar Panigrahi, Natarajan Mahalingam
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Publication number: 20120129854Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the yield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: April 27, 2010Publication date: May 24, 2012Applicant: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens