Exactly Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/303)
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Publication number: 20150065519Abstract: This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.Type: ApplicationFiled: August 28, 2014Publication date: March 5, 2015Inventors: Sarvajit Chakravarty, Roopa Rai, Son Minh Pham, Brahmam Pujala, Ramniwas Jangir, Rambabu Guguloth, Vijay Kumar Sharma
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Publication number: 20150065489Abstract: Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.Type: ApplicationFiled: October 30, 2014Publication date: March 5, 2015Inventors: Matthias HOFFMANN, Daniel BISCHOFF, Georg DAHMANN, Jasna KLICIC, Gerhard SCHAENZLE, Stefan Ludwig Michael WOLLIN, Serge Gaston CONVERS-REIGNIER, Stephen Peter EAST, Frederic Jacques MARLIN, Clive McCARTHY, John SCOTT
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Patent number: 8969376Abstract: The present invention relates to a compound represented by formula [I]: wherein: R1 is hydrogen, halogen, lower alkyl or cyano; Ring A is an optionally substituted heterocyclic group; Ring B is an optionally substituted 3 to 6-membered monocyclic group; and Y is optionally substituted amino, optionally substituted cyclic amino, optionally substituted aliphatic 3 to 6-membered monocyclyloxy, optionally substituted lower alkyl or optionally substituted lower alkyl-O—, or a pharmaceutically acceptable salt thereof, and to their use as PDE10 inhibitor.Type: GrantFiled: February 25, 2011Date of Patent: March 3, 2015Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Eiji Kawanishi, Mitsuya Hongu, Yoshihito Tanaka
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Patent number: 8969345Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.Type: GrantFiled: August 3, 2012Date of Patent: March 3, 2015Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
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Publication number: 20150057295Abstract: This invention relates to 6-alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification.Type: ApplicationFiled: August 20, 2014Publication date: February 26, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ulrich REISER, James MADDEN
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Publication number: 20150057309Abstract: The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them.Type: ApplicationFiled: February 27, 2013Publication date: February 26, 2015Inventors: Swaroop K. V. S. Vakkalanka, Dhanapalan Nagarathnam, Srikant Viswanadha, Meyyappan Muthuppalaniappan, Govindarajulu Babu, Prashant K. Bhavar
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Publication number: 20150057273Abstract: Disclosed are compounds having [1,2,4]triazolo[4,3-a]pyridine groups and pharmaceutically acceptable salts thereof. The compounds are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: ApplicationFiled: December 9, 2011Publication date: February 26, 2015Applicant: Chiesi Farmaceutici S.p.A.Inventors: Harry Finch, Monique Bodil Van Niel, Chi-Kit Woo
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Publication number: 20150057272Abstract: 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: August 1, 2014Publication date: February 26, 2015Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Patent number: 8962652Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.Type: GrantFiled: October 15, 2010Date of Patent: February 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Randall L. Halcomb, Paul Roethle
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Patent number: 8962620Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: November 4, 2013Date of Patent: February 24, 2015Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Publication number: 20150045360Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:Type: ApplicationFiled: August 21, 2014Publication date: February 12, 2015Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Publication number: 20150045368Abstract: Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: March 1, 2013Publication date: February 12, 2015Inventors: Howard Bregman, John L. Buchanan, Nagasree Chakka, Erin F. Dimauro, Hakan Gunaydin, Angel Guzman-Perez, Zihao Hua, Hongbing Huang, Xin Huang, Matthew W. Martin, Vinod F. Patel
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Publication number: 20150045332Abstract: The present invention relates to sphingosine-1-phosphate (S1P) receptors and compounds of the general formula: that are useful in the treatment and prevention of conditions associated with such receptors. More specifically, the present invention relates to the synthesis and use of sphingosine 1-phosphate receptor 2 (S1P2) antagonists that are useful in the treatment of cancer, atherosclerosis, diabetic retinopathy, and other inflammatory diseases. Among these inflammatory diseases that could be treated with these S1P2 antagonist are those characterized by fibrosis including chronic lung disease, chronic kidney and liver disease, chronic heart disease, and skin diseases such as sclerosis/scleroderma. The S1P2 antagonists can also be used in the treatment of glioblastoma multiforme (brain cancer), pediatric neuroblastoma, and other cancers.Type: ApplicationFiled: March 21, 2013Publication date: February 12, 2015Inventor: Rolf E. SWENSON
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Publication number: 20150045355Abstract: Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.Type: ApplicationFiled: December 31, 2011Publication date: February 12, 2015Inventors: Changyou Zhou, Shaohui Wang, Guoliang Zhang
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Publication number: 20150045361Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: October 22, 2014Publication date: February 12, 2015Inventors: Yi CHEN, Timothy D. CUSHING, Jason A. DUQUETTE, Felix GONZALEZ LOPEZ DE TURISO, Xiaolin HAO, Xiao HE, Brian S. LUCAS, Lawrence R. MCGEE, Andreas REICHELT, Robert M. RZASA, Jennifer L. SEGANISH, Youngsook SHIN, Dawei ZHANG
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Publication number: 20150045349Abstract: The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: February 19, 2013Publication date: February 12, 2015Inventors: Hiroyuki Nagamiya, Masato Yoshida, Masaki Seto, Shogo Marui, Tsuneo Oda, Yuji Ishichi, Hideo Suzuki, Tomokazu Kusumoto, Takatoshi Yogo, Chul Yun Rhim, Cheolhwan Yoon, Gil Nam Lee, Hyun Bin Kang, Kwang Ok Kim, Hye Sun Jeon
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Publication number: 20150045379Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: July 17, 2014Publication date: February 12, 2015Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
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Publication number: 20150045327Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.Type: ApplicationFiled: August 5, 2014Publication date: February 12, 2015Inventors: Steven Emiel VAN DER PLAS, Hans KELGTERMANS, Sébastien Jean Jacques Cédric DROPSIT MONTOVER, Sébastien Laurent Xavier MARTINA, Martin James Inglis ANDREWS
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Patent number: 8952162Abstract: The present invention relates to a compound according to formula I, wherein R1, R2 and A are as defined herein, which exhibit PDE4 inhibitory activity and may be used in the treatment of inflammatory diseases or autoimmune diseases, in particular inflammatory or proliferative dermal diseases.Type: GrantFiled: December 18, 2009Date of Patent: February 10, 2015Assignee: Leo Pharma A/SInventors: Simon Feldbæk Nielsen, Thomas Vifian, Anne Marie Horneman, Jesper Færgemann Lau
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Patent number: 8952004Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: January 5, 2011Date of Patent: February 10, 2015Assignee: Boehringer Ingelheim International GmbHInventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
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Patent number: 8952058Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: GrantFiled: October 12, 2012Date of Patent: February 10, 2015Assignee: Ambit Biosciences CorporationInventors: Michael J. Hadd, Michael D. Hocker, Mark W. Holladay, Gang Liu, Martin W. Rowbottom, Shimin Xu
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Patent number: 8952034Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: July 26, 2010Date of Patent: February 10, 2015Assignee: Gilead Sciences, Inc.Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
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Publication number: 20150038488Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.Type: ApplicationFiled: July 31, 2014Publication date: February 5, 2015Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
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Publication number: 20150038509Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).Type: ApplicationFiled: June 12, 2014Publication date: February 5, 2015Inventors: Gary J. Bridger, Renato T. Skerlj, Al Kaller, Curtis Harwig, David Earl Bogucki, Trevor R. Wilson, Jason B. Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosario DiFluri
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Patent number: 8946257Abstract: N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors.Type: GrantFiled: June 28, 2013Date of Patent: February 3, 2015Assignee: Vectura LimitedInventor: Jorge Salas Solana
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Patent number: 8946205Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: GrantFiled: May 11, 2010Date of Patent: February 3, 2015Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma, S.A.Inventors: Jose Maria Cid-Nunez, Ana Isabel De Lucas Olivares, Andres Avelino Trabanco-Suarez, Gregor James MacDonald
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Patent number: 8946426Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: GrantFiled: February 2, 2010Date of Patent: February 3, 2015Assignees: Janssen Pharmaceuticals, Inc., Cellzome LimitedInventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
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Publication number: 20150031681Abstract: A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): wherein A is CR1E or a nitrogen atom, X—Y—Z is N—CO—NR3AR3B and the like, R1A to R1E are each independently a hydrogen atom and the like, R2A to R2D are each independently a hydrogen atom and the like, R3A and R3B are each independently an optionally-substituted C3-10 cycloalkyl and the like, and n is 1 or 2 or a pharmaceutically acceptable salt thereof, which exhibits potent modulatory-effects on the activity of ?7 nicotinic acetylcholine receptor (?7 nAChR).Type: ApplicationFiled: April 9, 2013Publication date: January 29, 2015Inventors: Shinya Usui, Hiroki Yamaguchi, Yoko Nakai
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Publication number: 20150030588Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.Type: ApplicationFiled: November 12, 2012Publication date: January 29, 2015Inventors: Katayoun Jessen, Xin Guo, Pingda Ren, Christian Rommel, Yi Liu
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Patent number: 8940761Abstract: The present invention relates to novel [1,2,4]triazolopyridine compounds with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.Type: GrantFiled: December 19, 2012Date of Patent: January 27, 2015Assignee: Leo Pharma A/SInventors: Simon Feldbæk Nielsen, Jens Christian Højland Larsen
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Patent number: 8940760Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: GrantFiled: July 5, 2013Date of Patent: January 27, 2015Assignee: Genkyotex SAInventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
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Patent number: 8940758Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.Type: GrantFiled: July 17, 2013Date of Patent: January 27, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Ando
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Publication number: 20150025081Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: ApplicationFiled: September 17, 2014Publication date: January 22, 2015Inventors: Andreas Ritzen, Morten Langgard, Jan Kehler, Jacob Nielsen, John Paul Kilburn, Mohamed M. Farah
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Publication number: 20150025065Abstract: The present invention relates to compounds of general formula I, wherein the group R1, R2, X and Y are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: July 15, 2014Publication date: January 22, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Elke LANGKOPF, Holger WAGNER
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Publication number: 20150023916Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: ApplicationFiled: February 14, 2013Publication date: January 22, 2015Applicant: SIGA TECHNOLOGIES INC.Inventors: Dongcheng Dai, James R. Burgeson, Sean M. Amberg, Dennis E. Hruby
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Patent number: 8937060Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: GrantFiled: May 11, 2010Date of Patent: January 20, 2015Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma, SAInventors: Jose Maria Cid-Nunez, Daniel Oehlrich, Andres Avelino Trabanco-Suarez, Gary John Tresadern, Juan Antonio Vega Ramiro, Gregor James MacDonald
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Publication number: 20150018385Abstract: The present invention relates to the use of compounds with fused amino pyridine core for the treatment of malignancies associated with brain and lung. The oral administration of compounds of the instant application results in effective brain penetration and provides for non-intrusive treatment of brain and lung tumors.Type: ApplicationFiled: May 12, 2014Publication date: January 15, 2015Inventors: Xiong Cai, Changgeng Qian
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Publication number: 20150018351Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.Type: ApplicationFiled: July 10, 2014Publication date: January 15, 2015Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
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Publication number: 20150018371Abstract: Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.Type: ApplicationFiled: March 6, 2013Publication date: January 15, 2015Inventors: Roger D. Cone, Julien A. Sebag, Jacques Pantel, Savannah Y. Williams, David C. Weaver, Gary A. Sulikowski, Craig W. Lindsley, Padma S. Portonova, Chao Zhang
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Publication number: 20150018386Abstract: The present invention discloses an amorphous form of apixaban, process of preparation and compositions thereof.Type: ApplicationFiled: March 5, 2013Publication date: January 15, 2015Inventors: Shriprakash Dhar Dwivedi, Kamlesh Kumar Singh, Jitendra Maganbhai Gajera, Nitin Tandon, Digambar Ware
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Publication number: 20150018388Abstract: The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.Type: ApplicationFiled: December 11, 2013Publication date: January 15, 2015Inventors: Richard B. Silverman, Yinan Zhang
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Publication number: 20150018381Abstract: Although it can be farnesylated, the mutant lamin A protein expressed in Hutchinson Gilford Progeria Syndrome (HGPS) cannot be defarnesylated because the characteristic mutation causes deletion of a cleavage site necessary for binding the protease ZMPSTE24 and effecting defarnesylation. The result is an aberrant farnesylated protein (called “progerin”) that alters normal lamin A function as a dominant negative, as well as assuming its own aberrant function through its association with the nuclear membrane. The retention of farnesylation, and potentially other abnormal properties of progerin and other abnormal lamin gene protein products, produces disease. Farnesyltransferase inhibitors (FTIs) (both direct effectors and indirect inhibitors) will inhibit the formation of progerin, cause a decrease in lamin A protein, and/or an increase prelamin A protein. Decreasing the amount of aberrant protein improves cellular effects caused by and progerin expression.Type: ApplicationFiled: July 21, 2014Publication date: January 15, 2015Inventors: Leslie B. GORDON, Francis S. COLLINS, Thomas GLOVER, Michael W. GLYNN, Brian C. CAPELL, Adrienne D. COX, Channing J. DER
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Publication number: 20150018337Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 29, 2014Publication date: January 15, 2015Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Patent number: 8933095Abstract: Compounds of Formula I: wherein X, Y, Z, R1, R2, R3, R4 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.Type: GrantFiled: October 31, 2013Date of Patent: January 13, 2015Assignee: Pfizer Inc.Inventors: Amy Beth Dounay, Laura Ann McAllister, Vinod Dipak Parikh, Suobao Rong, Patrick Robert Verhoest
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Patent number: 8933094Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.Type: GrantFiled: October 16, 2013Date of Patent: January 13, 2015Assignee: Hoffmann-La Roche Inc.Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20150011545Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.Type: ApplicationFiled: July 15, 2014Publication date: January 8, 2015Applicant: AstraZeneca ABInventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle Laurae LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
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Publication number: 20150011557Abstract: The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.Type: ApplicationFiled: September 7, 2012Publication date: January 8, 2015Applicant: Merck Patent GmbHInventors: Kai Schiemann, Wolfgang Staehle, Michael Busch, Dirk Wienke, Oliver Poeschke, Christa Burger
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Publication number: 20150011548Abstract: A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.Type: ApplicationFiled: October 9, 2012Publication date: January 8, 2015Inventors: Tero Linnanen, Gerd Wohlfahrt, Srinivas Nanduri, Ravi Ujjinamatada, Srinivasan Rajagopalan, Subhendu Mukherjee
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Crystal form I of salt of a dipeptidyl peptidase-IV inhibitor and preparation method and use thereof
Patent number: 8927572Abstract: The present invention relates to the crystal form I of salt of a dipeptidyl peptidase-IV inhibitor, and the preparation method and use thereof. In particular, it relates to the crystal form I of dihydrochloride salt of the compound (R)-2-[[7-(3-aminopiperidin-1-yl)-3,5-dimethyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl]methyl]benzonitrile represented by formula (1), which is a dipeptidyl peptidase-IV inhibitor, and the preparation method and use thereof. The crystal form I of dihydrochloride salt of the dipeptidyl peptidase-IV inhibitor represented by formula (1) is characterized in that it has characteristic peaks at 8.7±0.2°, 19.4±0.2°, 23.5±0.2° and 27.2±0.2° in X-ray powder diffraction indicated by an angle 2? (°) using Cu—K? irradiation.Type: GrantFiled: July 6, 2012Date of Patent: January 6, 2015Assignee: Xuanzhu Pharma Co., Ltd.Inventor: Chutian Su -
Patent number: 8927720Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: January 6, 2015Assignee: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville