Additional Hetero Ring Attached Directly Or Indirectly To The Four-membered Hetero Ring By Nonionic Bonding Patents (Class 514/210.18)
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Publication number: 20140171405Abstract: The present invention relates to fused pyrazole derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.Type: ApplicationFiled: December 18, 2013Publication date: June 19, 2014Applicant: Incyte CorporationInventors: Jincong Zhuo, Meizhong Xu, Ding-Quan Qian
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Publication number: 20140171403Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.Type: ApplicationFiled: March 15, 2013Publication date: June 19, 2014Applicant: Novartis AGInventors: Darren Mark Legrand, Vikki Furminger, Christopher Thomson, Owen Rhys Hughes, Emily Stanley
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Publication number: 20140171406Abstract: 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: 20140171404Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.Type: ApplicationFiled: December 17, 2013Publication date: June 19, 2014Applicant: NOVARTIS AGInventors: Vikki FURMINGER, Owen Rhys HUGHES, Darren Mark LEGRAND, Emily STANLEY, Christopher THOMSON
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Patent number: 8754071Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.Type: GrantFiled: September 19, 2013Date of Patent: June 17, 2014Inventors: Valentina Molenti, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh
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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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Publication number: 20140162983Abstract: The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.Type: ApplicationFiled: June 10, 2012Publication date: June 12, 2014Applicant: Merck Patent GmbHInventors: Brian L. Hodous, Lesley Liu-Bujalski, Reinaldo Jones, Donald Bankston, Theresa L. Johnson, Igor Mochalkin, Ngan Nguyen, Hui Qiu, Andreas Goutopoulos, Nadia Brugger
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Publication number: 20140163001Abstract: Provided is a heterocyclic compound having an ROR?t inhibitory activity.Type: ApplicationFiled: July 27, 2012Publication date: June 12, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Satoshi Yamamoto, Junya Shirai, Atsuko Ochida, Yoshiyuki Fukase, Yoshihide Tomata, Ayumu Sato, Shotaro Miura, Kazuko Yonemori, Ryokichi Koyama
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Publication number: 20140163002Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: August 6, 2012Publication date: June 12, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Patrick Y.S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
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Patent number: 8748417Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R1, and R2 are defined herein.Type: GrantFiled: March 13, 2013Date of Patent: June 10, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Yue-Mei Zhang, Peter J. Connolly, Shu-Chen Lin, Mark J. Macielag
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Publication number: 20140155374Abstract: Described herein are methods for using compounds that activate pyruvate kinase.Type: ApplicationFiled: May 3, 2012Publication date: June 5, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventor: Shin-San M. Su
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Publication number: 20140155373Abstract: Compounds of formula (I) described herein are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.Type: ApplicationFiled: December 5, 2013Publication date: June 5, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Elisabetta Armani, Gabriele Amari, Mauro Riccaboni, Charles Baker-Glenn
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Publication number: 20140155375Abstract: The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase enzymes.Type: ApplicationFiled: June 8, 2012Publication date: June 5, 2014Applicant: GlaxoSmithKline Interllectual Property LimitedInventors: Deborah W. Chen, Sarah Duncan, Nigel Paul King, Kiew Ching Lee, Sing Yeung Mak, Dean Andrew Rivers
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Publication number: 20140155377Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: February 6, 2014Publication date: June 5, 2014Applicant: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
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Publication number: 20140155372Abstract: The invention provides combinations comprising a) compound of formula I: (formula I), or a pharmaceutically acceptable salt thereof; and another agent selected from GDC-0973, PD-0325901, or a pharmaceutically acceptable salt thereof. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.Type: ApplicationFiled: March 30, 2012Publication date: June 5, 2014Applicant: GENENTECH, INC.Inventors: Brian Lee, Kui Lin, Michelle Nannini, Elizabeth Punnoose, Deepak Sampath
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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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Publication number: 20140155376Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R, R2, and R3 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: February 4, 2014Publication date: June 5, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Robert Than Hendricks, Johannes Hermann, Saul Jaime-Figueroa, Rama Kondru, Yan Lou, Stephen Lynch, Timothy D. Owens, Michael Soth, Calvin Yee
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Patent number: 8741887Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: December 18, 2012Date of Patent: June 3, 2014Assignee: Janssen Pharmaceutica, NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20140148432Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activation, including neuropsychiatric disorders, neurodegenerative diorders and other neurologic diseases, disorders and conditions including stroke, brain injury, epilepsy, neuropsychiatric disorders, mood disorders, chronic pain and related conditions.Type: ApplicationFiled: January 31, 2014Publication date: May 29, 2014Inventors: Ruppa Poornachary Kamalesh Babu, Scott James Myers
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Publication number: 20140148431Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: ApplicationFiled: August 24, 2012Publication date: May 29, 2014Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawsar, Sachin Bhagwat, Mohammed Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
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Patent number: 8735384Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).Type: GrantFiled: January 14, 2011Date of Patent: May 27, 2014Assignee: Amgen Inc.Inventors: Nick A. Paras, James Brown, Yuan Cheng, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Ana Elena Minatti, Thomas Nixey, Timothy Powers, Christopher M. Tegley, Qiufen Xue, Bryant Yang, Wenge Zhong
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Publication number: 20140142085Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: July 5, 2012Publication date: May 22, 2014Applicant: Gilead Sciences, Inc.Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-hung Chou, Randall L. Halcomb, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
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Publication number: 20140142084Abstract: Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.Type: ApplicationFiled: February 26, 2013Publication date: May 22, 2014Applicants: KOTOBUKI PHARMACEUTICAL CO., LTD., Astellas Pharma Inc.Inventors: Minoru Kameda, Ikumi Kuriwaki, Kazuhiko Iikubo, Hiroyuki Hisamichi, Yuichiro Kawamoto, Hiroyuki Moritomo, Tomoyuki Suzuki, Takashi Futami, Atsushi Suzuki, Kazuhisa Tsunoyama, Makoto Asaumi, Hiroshi Tomiyama, Atsushi Noda, Yoshinori Iwai, Kazuo Tokuzaki, Haruki Okada, Kozo Miyasaka
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Patent number: 8729063Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: December 20, 2012Date of Patent: May 20, 2014Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taishing Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
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Patent number: 8729064Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, W and are defined herein.Type: GrantFiled: March 19, 2013Date of Patent: May 20, 2014Assignee: Janssen Pharmaceutica NVInventors: Christopher M Flores, Marina I Nelen, Erica L Nulton, Stephen M Prouty, Matthew J Todd, Sui-Po Zhang
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Patent number: 8729062Abstract: The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: November 11, 2011Date of Patent: May 20, 2014Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
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Publication number: 20140135308Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: January 23, 2014Publication date: May 15, 2014Applicant: Genentech, Inc.Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
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Publication number: 20140135306Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.Type: ApplicationFiled: June 19, 2012Publication date: May 15, 2014Applicant: Novartis AGInventors: Nicole Buschmann, Pascal Furet, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
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Publication number: 20140135307Abstract: This invention relates to co-crystals and salts of CCR3 inhibitors of formula 1, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases related with the CCR3-receptor.Type: ApplicationFiled: January 22, 2014Publication date: May 15, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Markus FRANK, Hans HAEBERLE, Manuel HENRY, Thorsten PACHUR, Marco SANTAGOSTINO, Uwe STERTZ, Thomas TREBING, Ulrike WERTHMANN
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Patent number: 8722658Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: January 25, 2013Date of Patent: May 13, 2014Assignee: Janssen Pharmaceutica NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20140128366Abstract: The present invention relates to substituted 1,3,4-oxadiazoles-2-thio azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: November 4, 2013Publication date: May 8, 2014Applicant: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
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Publication number: 20140128367Abstract: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.Type: ApplicationFiled: June 14, 2012Publication date: May 8, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Xianhai Huang, Jason Brubaker, Scott L. Peterson, John W. Butcher, Joshua T. Close, Michelle Martinez, Rachel Nicola MacCoss, Joon O. Jung, Phieng Siliphaivanh, Hongjun Zhang, Robert G. Aslanian, Purakkattle Johny Biju, Li Dong, Ying Huang, Kevin D. McCormick, Anandan Palani, Ning Shao, Wei Zhou
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Publication number: 20140128369Abstract: The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: January 6, 2014Publication date: May 8, 2014Applicant: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Ken Chow, Evelyn G. Corpuz, Wha Bin Im
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Publication number: 20140128371Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.Type: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: ASTRAZENECA ABInventors: Kevin BARVIAN, Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU
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Publication number: 20140128370Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.Type: ApplicationFiled: January 9, 2014Publication date: May 8, 2014Applicant: NOVARTIS AGInventors: Nigel Graham COOKE, Frédéric ZECRI, Nicolas SOLDERMANN, Romain WOLF, Christina HEBACH, Klemens HOEGENAUER, Gregory John HOLLINGWORTH, Anette VON MATT, Ross Sinclair STRANG, Alexander Baxter SMITH, Paulo FERNANDES GOMES DOS SANTOS, Nadege GRAVELEAU, Frank STOWASSER, Nicola TUFILLI
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Publication number: 20140128368Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: June 11, 2012Publication date: May 8, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
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Publication number: 20140128365Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.Type: ApplicationFiled: November 2, 2012Publication date: May 8, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, Shung C. Wu, David S. Yoon
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Publication number: 20140121196Abstract: A compound that inhibits interaction between, murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.Type: ApplicationFiled: November 14, 2013Publication date: May 1, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
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Publication number: 20140121194Abstract: There is provided a method for controlling an animal ectoparasite having excellent controlling effects. The method for controlling an ectoparasite of dogs comprises orally administering an ectoparasite-controlling agent comprising as an active ingredient an isoxazoline compound represented by formula (I): wherein X1 represents a halogen atom or a C1-C3 haloalkyl, X2 represents a hydrogen atom, a halogen atom or a C1-C3 haloalkyl, X3 represents a hydrogen atom or a halogen atom, Q represents, for example, Q1, A1 represents R11—C(?O)—N(R12)—N(R13)—, R11—C(?O)—N(R12)—CH2— or R11—C(?O)—N(R12)—, and R10 represents a hydrogen atom, a halogen atom or a C1-C3 alkyl group, to a dog in a period from 30 minutes immediately before the start of feeding to 120 minutes after the end of feeding.Type: ApplicationFiled: October 17, 2013Publication date: May 1, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Kaori IKARI, Naonobu NISHIGUCHI
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Publication number: 20140121195Abstract: Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.Type: ApplicationFiled: October 17, 2013Publication date: May 1, 2014Applicant: ChemoCentryx, Inc.Inventors: Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jay Powers, Ju Yang
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Patent number: 8710043Abstract: 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: GrantFiled: June 21, 2012Date of Patent: April 29, 2014Assignee: Amgen Inc.Inventors: Jian J. Chen, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma
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Publication number: 20140113890Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.Type: ApplicationFiled: December 23, 2013Publication date: April 24, 2014Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
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Publication number: 20140107094Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 15, 2013Publication date: April 17, 2014Applicant: Janssen Pharmaceutica NVInventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Joan Pierce, Steven Goldberg, Anne Fourie, Xiaohua Xue
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Patent number: 8697888Abstract: In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: December 3, 2012Date of Patent: April 15, 2014Assignee: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Yiu-Yin Cheung
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Patent number: 8697683Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: March 18, 2013Date of Patent: April 15, 2014Assignee: Janssen Pharmaceutica NVInventors: Haiyan Bian, Kristen M. Chevalier, Jose Clemente, Peter J. Connolly, Christopher M. Flores, Shu-Chen Lin, Li Liu, John R. Mabus, Mark J. Macielag, Mark E. McDonnell, Philip M. Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Patent number: 8697684Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 29, 2013Date of Patent: April 15, 2014Assignee: Janssen Pharmaceutica NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20140100212Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.Type: ApplicationFiled: October 15, 2013Publication date: April 10, 2014Applicant: ALLERGAN, INC.Inventors: Xialing Guo, Zhen Zhu
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Publication number: 20140100215Abstract: The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.Type: ApplicationFiled: December 7, 2013Publication date: April 10, 2014Applicant: Exelixis, Inc.Inventors: Dana T. Aftab, A. Douglas Laird, Peter Lamb, Jean-Francois A. Martini
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Publication number: 20140100213Abstract: This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.Type: ApplicationFiled: November 4, 2013Publication date: April 10, 2014Applicant: GlaxoSmithKline LLCInventors: Nicholas David Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan Michael Chergurovich, Terence John Kiesow, Cynthia Ann Parrish, Alexander Joseph Reif, Kenneth Wiggall
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Publication number: 20140100214Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: December 6, 2013Publication date: April 10, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. CASTRO, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan