Ring Nitrogen Is Shared By The Two Cyclos Patents (Class 544/281)
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Publication number: 20140239269Abstract: A pyrene-based compound, and an organic light-emitting diode including the pyrene-based compound are provided.Type: ApplicationFiled: August 5, 2013Publication date: August 28, 2014Inventors: Eun-Jae Jeong, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jun-Ha Park, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Soo-Yon Kim, Jong-Hyuk Lee
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Publication number: 20140234254Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: February 15, 2014Publication date: August 21, 2014Applicants: SUNSHINE LAKE PHARMA CO., LTD., CALITOR SCIENCES, LLCInventor: Ning Xi
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Publication number: 20140228368Abstract: The present invention is directed to pyrimidine 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: August 20, 2012Publication date: August 14, 2014Inventors: Christopher D. Cox, Vadim Y. Dudkin, Jeffrey Kern, Mark E. Layton, Izzat T. Raheem
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Publication number: 20140228349Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.Type: ApplicationFiled: October 9, 2012Publication date: August 14, 2014Inventors: Mark Laurence Boys, Laurence E. Burgess, C. Todd Eary, Robert Groneberg, Bruno P. Hache, Darren Harvey, Erik James Hicken, Christopher F. Kraser, Ellen Laird, David A. Moreno, Mark C. Munson, Li Ren, John E. Robinson, Stephen T. Schlachter
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Patent number: 8796294Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: GrantFiled: June 4, 2012Date of Patent: August 5, 2014Assignee: Exelixis Patent Company LLCInventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
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Patent number: 8796285Abstract: The present invention provides new pyrazol-[1,5-a]-pyrimidone derivates and pharmaceutical compositions comprising said compounds and one or more pharmaceutically acceptable carriers or diluents. The uses of the compounds for the manufacture of potassium channel openers, anti-epilepsy medicaments, anti-anxiety medicaments and analgesic medicaments are also provided in the present invention.Type: GrantFiled: June 3, 2010Date of Patent: August 5, 2014Assignees: Hebei Medical University, Peking UniversityInventors: Hailin Zhang, Jinlong Qi, Diqun Zhang, Kewei Wang, Fan Zhang, Yan Fu, Yi Mi, Wen Xu, Xiaona Du, Yibing Wu, Qingzhong Jia, Shuangge Yang
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Publication number: 20140213599Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.Type: ApplicationFiled: January 23, 2014Publication date: July 31, 2014Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Zehong WAN, Yingxia Sang, Qing Zhang
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Publication number: 20140213554Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.Type: ApplicationFiled: December 20, 2013Publication date: July 31, 2014Inventors: Guoxian Wu, Katrina Chan, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Marika Nespi, Wayne Spevak, Ying Zhang
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Patent number: 8791108Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: GrantFiled: August 9, 2012Date of Patent: July 29, 2014Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Manoj Patel
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Patent number: 8791123Abstract: Compounds of Formula (I) and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.Type: GrantFiled: July 9, 2010Date of Patent: July 29, 2014Assignee: Array Biopharma, Inc.Inventors: Shelley Allen, Steven Wade Andrews, Kevin Ronald Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Jeongbeob Seo
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Publication number: 20140206673Abstract: Provided are compounds of formula (I), wherein X, Y, Z, W, V, R2, R3 and m are defined as in the description. Their pharmaceutical compositions and their uses for treating cancers are also provided.Type: ApplicationFiled: June 18, 2012Publication date: July 24, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
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Publication number: 20140206536Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; A is O, S, NR3e or C(R3c)?C(R3d); Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 1, 2 or 3; and R1, R2, R3a-R3e, R4, R5, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: March 19, 2014Publication date: July 24, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: WENMING ZHANG, CALEB WILLIAM HOLYOKE, JR., KENNETH ANDREW HUGHES, GEORGE PHILIP LAHM, THOMAS FRANCIS PAHUTSKI, JR., MY-HANH THI TONG, MING XU
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Publication number: 20140194622Abstract: The present invention provides methods for the synthesis of polycyclic guanidine compounds. In certain embodiments, provided methods include the step of contacting a described reagent with a triamine compound to provide a polycyclic guanidine compound.Type: ApplicationFiled: January 6, 2014Publication date: July 10, 2014Applicant: Novomer, Inc.Inventor: Alexei Gridnev
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Publication number: 20140194404Abstract: This invention relates to amidopyrazole compounds that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment of cellular proliferative diseases, for example, cancer, hyperplasia, restenosis, cardiac hypertrophy, immune disorders and inflammation.Type: ApplicationFiled: March 21, 2012Publication date: July 10, 2014Inventors: William T. McElroy, Guoqing Li, Ginny Dai Ho, Zheng Tan, Sunil Paliwal, William Michael Seganish, Deen Tulshian, John Lampe, Joey L. Methot, Hua Zhou, Michael D. Altman, Liang Zhu
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Publication number: 20140194418Abstract: Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1˜X5, R1˜R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.Type: ApplicationFiled: January 20, 2012Publication date: July 10, 2014Applicant: ABBVIE INC.Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Fengchun Wu, Yan Shen, Cuihua Liu, Zhenguang Zou, Marina Pliushchev
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Patent number: 8771665Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: GrantFiled: December 16, 2011Date of Patent: July 8, 2014Assignee: Cocrystal Discovery, Inc.Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Publication number: 20140187545Abstract: PI3K? selective compounds having the structureType: ApplicationFiled: June 29, 2012Publication date: July 3, 2014Applicant: GlaxoSmithKline LLCInventors: Hong Lin, Juan Luengo, Michael Lee Moore, Junya Qu, Ralph A. Rivero, Rosanna Tedesco, Hongyi Yu
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Publication number: 20140179715Abstract: Disclosed are 2,3-dihydroimidazo[1,2-c]pyrimidin-5(1H)-one compounds that inhibit Lp-PLA2, processes for their preparation, compositions containing them and their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.Type: ApplicationFiled: July 25, 2012Publication date: June 26, 2014Applicant: Glaxo Group LimitedInventors: Zehong Wan, Kai Long, Yingxia Sang, Xiaobo Su
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Publication number: 20140171639Abstract: 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: February 24, 2014Publication date: June 19, 2014Applicant: 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: 20140167007Abstract: A pyrene-based compound and an organic light-emitting diode including the pyrene-based compound are provided.Type: ApplicationFiled: October 8, 2013Publication date: June 19, 2014Applicant: SAMSUNG DISPLAY CO., LTD.Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jun-Ha Park, Eun-Young Lee, Chang-Ho Lee, Jong-Hyuk Lee
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Publication number: 20140163008Abstract: 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: ApplicationFiled: August 3, 2011Publication date: June 12, 2014Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
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Publication number: 20140163000Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: ApplicationFiled: December 6, 2013Publication date: June 12, 2014Inventors: Nadia Ahmad, Dean Boyall, Jean-Damien Charrier, Chris Davis, Rebecca Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Donald Middleton, Michael O'Donnell, Maninder Panesar, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
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Patent number: 8748435Abstract: The present invention relates to pyrazolo pyrimidine derivatives, to methods of preparing these, to combinations and pharmaceutical composition comprising these, and to their use in the treatment of diseases and disorders which may for example involve autoimmune diseases, angiogenesis, pain, and/or inflammatory diseases.Type: GrantFiled: March 26, 2012Date of Patent: June 10, 2014Assignee: Novartis AGInventors: Wolfgang Miltz, Berndt Oberhauser, Andrea Vaupel, Juraj Velcicky, Klaus Weigand, Rajender Reddy Leleti, Yugang Liu, Zhengming Du
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Publication number: 20140155416Abstract: There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.Type: ApplicationFiled: November 25, 2013Publication date: June 5, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tsuneo Yasuma, Akira Mori, Masahiro Kawase, Hiroyuki Kimura, Masato Yoshida, Albert Charles Gyorkos, Scott Alan Pratt, Christopher Peter Corrette
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Publication number: 20140154240Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.Type: ApplicationFiled: May 30, 2013Publication date: June 5, 2014Inventors: Kerim Babaoglu, Constantine G. Boojamra, Eugene J. Eisenberg, Hon Chung Hui, Richard L. Mackman, Jay P. Parrish, Michael Sangi, Oliver L. Saunders, Dustin Siegel, David Sperandio, Hai Yang
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Patent number: 8729264Abstract: Provided is an agent for the prevention and/or treatment of a skin disease containing, as an active ingredient, a pyrazolopyrimidine derivative represented by the formula (I) (wherein each symbol is as defined in the specification), or a pharmacologically acceptable salt thereof, and the like.Type: GrantFiled: September 26, 2008Date of Patent: May 20, 2014Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Keisuke Yamamoto, Seiji Aratake, Daisuke Nakashima, Kimihisa Ueno, Mirai Mizutani, Daisuke Harada, Katsuya Kobayashi, Kazuki Hemmi
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Patent number: 8729074Abstract: The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: GrantFiled: March 19, 2010Date of Patent: May 20, 2014Assignee: Amgen Inc.Inventors: Yunxin Y. Bo, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Aaron C. Siegmund, Nuria A. Tamayo, Kevin C. Yang
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Patent number: 8722708Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6?R7?); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7? are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.Type: GrantFiled: June 12, 2006Date of Patent: May 13, 2014Assignees: Merck Sharp & Dohme Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Andrew Stamford, Guoqing Li, William Greenlee, Zhaoning Zhu, Brian McKittrick, Robert Mazzola, Ying Huang, Tao Guo, Thuy X. H. Le, Gang Qian, Yuefei Shao
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Patent number: 8722676Abstract: Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: November 2, 2012Date of Patent: May 13, 2014Assignee: Genentech, Inc.Inventors: James John Crawford, Daniel Fred Ortwine, Wendy B. Young
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Publication number: 20140114068Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.Type: ApplicationFiled: June 18, 2012Publication date: April 24, 2014Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
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Publication number: 20140107099Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.Type: ApplicationFiled: December 19, 2013Publication date: April 17, 2014Applicant: Genentech, Inc.Inventors: Jeffrey Blaney, Paul A. Gibbons, Emily Hanan, Joseph P. Lyssikatos, Steven R. Magnuson, Richard Pastor, Thomas E. Rawson, Aihe Zhou, Bing-Yan Zhu
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Patent number: 8691825Abstract: The instant invention provides for substituted fused pyrimidine compounds of Formula A that inhibit Akt activity: In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: March 29, 2010Date of Patent: April 8, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Qi Chen, Mingxiang Cui, Bin Hu, Shuangxi Hu, Zhifa Pu, Philip E. Sanderson, Richard Soll, Xue Tang, Jiabing Wang, Yongjin Yan, Jinfeng Yao, Hongjie Zhang
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Publication number: 20140094466Abstract: In alternative embodiments, the invention provides compositions that inhibit the polypeptide SSH-2, or SlingSHot-2, a phosphatase enzyme that regulates actin filaments, and methods for making and using them, including methods comprising administering compositions of the invention to regulate or modify actin filament polymerization by inhibiting SSH-2, where in one embodiment compositions of the invention slow or inhibit F-actin depolymerization and severing. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit cell motility and/or internal remodeling. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit, or reverse, or ameliorate the progression of a cancer or a metastasis or other uncontrolled or unregulated cell growth, and/or Alzheimer's disease.Type: ApplicationFiled: March 15, 2012Publication date: April 3, 2014Inventors: Jason H. Haga, Shu Chien, Matt Mui, Marshall J. Levesque, Phillip D. Pham
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Publication number: 20140094474Abstract: Compounds of formula (I) or (II) wherein Rx, Rz, R9, R10, R14, R14?, R15, R15?, A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.Type: ApplicationFiled: April 20, 2012Publication date: April 3, 2014Applicant: ORION CORPORATIONInventors: Olli Törmakängas, Gerd Wohlfahrt, Harri Salo, Rathna Durga Ramasurbamanian, Pranab Kumar Patra, Arputharaj Ebenezer Martin, Terhi Heikkinen, Anniina Vesalainen, Anu Moilanen, Arja Karjalainen
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Publication number: 20140088110Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.Type: ApplicationFiled: November 26, 2013Publication date: March 27, 2014Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Swen HÖLDER, Armin ZÜLCH, Thomas BÄR, Thomas MAIER, Astrid ZIMMERMANN, Thomas BECKERS, Volker GEKELER, Hemant JOSHI, Yogesh MUNOT, Umesh BHISE, Sunil CHAVAN, Sachin SHIVATARE, Sarvesh PATEL, Vikas GORE
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Publication number: 20140088096Abstract: 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: March 27, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Roushan Afroze, Indu T. Bharathan, Jeffrey P. Ciavarri, Paul E. Fleming, Jeffrey L. Gaulin, Mario Girard, Steven P. Langston, Francois Soucy, Tzu-Tshin Wong, Yingchun Ye
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Patent number: 8680113Abstract: Compounds having Formula I: wherein the variables Ar1, Ar2, R1, R2 and R3 are defined herein, pharmaceutical compositions, and methods of using such compounds or compositions for inhibiting Bmi-1 expression.Type: GrantFiled: July 1, 2009Date of Patent: March 25, 2014Assignee: PTC Therapeutics, Inc.Inventors: Young-Choon Moon, Nadiya Sydorenko, Thomas Davis, Liangxian Cao, Daniel J. Medina, Marites A. Rafanan
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Patent number: 8673924Abstract: In its many embodiments, the present invention provides a method of inhibiting one or more cyclin dependent kinases in a patient comprising administering to said patient a therapeutically effective amount of at least one pyrazolo[1,5-a]pyrimidine compound or a pharmaceutical composition comprising such compound, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: April 20, 2007Date of Patent: March 18, 2014Assignees: Merck Sharp & Dohme Corp., Pharmacopeia, LLCInventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Alan Mallams, Carmen S. Alvarez, Kartik M. Keertikar, Jocelyn Rivera, Tin-Yau Chan, Vincent S. Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhenmin He, Ray Anthony James, Haengsoon Park, Vidyadhar M. Paradkar, Douglas Walsh Hobbs, Paul Kirschmeier, Rajat Bannerji
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Publication number: 20140073638Abstract: 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: ApplicationFiled: October 16, 2013Publication date: March 13, 2014Applicant: 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: 20140057894Abstract: Disclosed herein is a compound of Formula I: wherein X, R1, R2, and R3 are as defend herein, or a pharmaceutically acceptable salt thereof to allow the drug to penetrate the cell membrane; or a prodrug, or the compound is labeled with a detectable label or an affinity tag thereof. Also disclosed is a pharmaceutical composition, a method of treating a disorder mediated by melanocortin-4 receptors, and a method of treating obesity using the compounds described.Type: ApplicationFiled: January 26, 2012Publication date: February 27, 2014Applicant: Universite De MontrealInventors: Michel Bouvier, Anne Marinier, Rejean Ruel, Patricia René, Yves Chantigny, Philippe Dagneau, Stéphane Gingras
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Publication number: 20140046056Abstract: Provided is a novel compound represented by the following formula wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor ? agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.Type: ApplicationFiled: October 22, 2013Publication date: February 13, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Tsuyoshi Maekawa, Hideyuki Igawa
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Publication number: 20140045779Abstract: This invention relates with anti-tumor activities of new compounds containing an adamantyl group or analogs thereof.Type: ApplicationFiled: August 29, 2011Publication date: February 13, 2014Inventor: Lifeng Xu
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Publication number: 20140038941Abstract: A ring-fused heterocyclic derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof having a T-type calcium channel regulatory effect and useful as a pruritus therapeutic and/or preventive agent, and the like are provided. In the general formula (I), R1 represents optionally substituted lower alkyl, and the like; R2 represents an optionally substituted cycloalkyl, and the like; Q represents a hydrogen atom, and the like; R3 represents —C(?O)NR8R9 (wherein R8 and R9 may be the same or different, and each represents a hydrogen atom, and the like), and the like; L1 represents —CR11AR11B— (wherein R11A and R11B may be the same or different, and each represents a hydrogen atom, and the like), and the like; and W1 and W2 may be the same or different, and each represents C—R12 (wherein R12 represents a hydrogen atom, and the like), and the like.Type: ApplicationFiled: February 1, 2012Publication date: February 6, 2014Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Takashi Sawada, Tomohiro Danjo, Keiichi Motosawa, Takayuki Furuta, Maki Ichioka, Masamori Sugawara, Noriaki Uesaka
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Publication number: 20140038989Abstract: A compound of Formula (I) or a pharmaceutically acceptable salt thereof: wherein: R1 represents a group selected from: i) phenyl optionally substituted with one or two substituents independently selected from Me, OMe, CF3, F, Cl and NMe2; furanyl, thiophenyl, pyrrolyl, pyridyl, cyclohexyl or naphthyl, each of which is optionally substituted with one or two substituents independently selected from Me, OMe, CF3, F, Cl and NMe2; and iii) benzo[1,3]dioxo5-yl or 2,3-dihydrobenzo[1,4]dioxin-6-yl; R2 represents CF3, C1-4alkyl, or CHF2; when R1 represents optionally substituted furanyl, thiophenyl, pyrrolyl, pyridyl or naphthyl, R3 represents Et; when R1 represents optionally substituted cyclohexyl, R3 represents Et or Me; otherwise R3 represents Et, Me, Br or OMe, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided, together with certain novel compounds.Type: ApplicationFiled: April 20, 2012Publication date: February 6, 2014Applicant: Glaxo Group LimitedInventors: Emilio Alvarez-Ruiz, Luis Ballell-Pages, Julia Castro Pichel, Lourdes Encinas, Jorge Esquivias, Franscisco Gamo-Benito, Maria Cruz Garcia-Palancar, Modesto Jesus Remuinan-Blanco
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Patent number: 8637526Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.Type: GrantFiled: May 2, 2011Date of Patent: January 28, 2014Assignee: Genentech, Inc.Inventors: Jeffrey Blaney, Paul A. Gibbons, Emily Hanan, Joseph P. Lyssikatos, Steven R. Magnuson, Richard Pastor, Thomas E. Rawson, Aihe Zhou, Bing-Yan Zhu
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Publication number: 20140024659Abstract: The invention relates to N-substituted hetero-bicyclic compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic compounds. The N-substituted hetero-bicyclic compounds of the present invention are defined by the following formula I: wherein A, B, X, Het, R1, R2, W1, W2, W3 and W4 are defined as in the description.Type: ApplicationFiled: April 5, 2012Publication date: January 23, 2014Applicant: BASF SEInventors: Ralph Paulini, Carsten Beyer, Henricus Maria Martinus Bastiaans, Nancy B. Rankl
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Patent number: 8633200Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: GrantFiled: September 2, 2011Date of Patent: January 21, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Annapurna Pendri, Guo Li, Samuel Gerritz, David R. Langley, George L. Trainor, Nicholas A. Meanwell
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Publication number: 20140014925Abstract: A compound represented by Formula 1 below and an organic light-emitting device including the compound are provided: Substituents in Formula 1 are the same as defined in the specification.Type: ApplicationFiled: June 21, 2013Publication date: January 16, 2014Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jun-Ha Park, Eun-Young Lee, Chang-Ho Lee, Jong-Hyuk Lee
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Publication number: 20140011810Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.Type: ApplicationFiled: September 11, 2013Publication date: January 9, 2014Applicant: Gatekeeper Pharmaceuticals, Inc.Inventors: Nathanael S. Gray, Wenjun Zhou
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Patent number: 8618114Abstract: The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HT6 receptor antagonists and pharmaceutical compositions, and also to method for prophylaxis and treatment of various diseases of central nervous system at humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors, in particular, Alzheimer's disease, Parkinson's disease, Huntington's disease, schizophrenia, and other neurodegenerative diseases, cognitive disorders and obesity.Type: GrantFiled: October 6, 2009Date of Patent: December 31, 2013Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko, Yan Lavrovsky, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva