Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/210.21)
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Patent number: 9346782Abstract: 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: GrantFiled: October 14, 2014Date of Patent: May 24, 2016Assignee: 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, Maxwell D. Cummings
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Patent number: 9328095Abstract: 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: GrantFiled: October 15, 2013Date of Patent: May 3, 2016Inventors: 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, Maxwell D. Cummings
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Patent number: 9326985Abstract: Heteroaryl pyridone and aza-pyridone amide compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. 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: July 2, 2014Date of Patent: May 3, 2016Assignee: Genentech, Inc.Inventors: James John Crawford, Wendy Lee, Wendy B. Young
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Patent number: 9328112Abstract: Disclosed are compounds of Formula (Ia), and pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, R3A, R3B, and R4 are as described herein. The compounds may be used as agents in the treatment of diseases, including cancer. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula (Ia).Type: GrantFiled: December 12, 2014Date of Patent: May 3, 2016Assignee: AbbVie Inc.Inventors: Robin Frey, Jane Gong, Zhiqin Ji, Chunqiu Lai, Thomas Penning, Xiaohong Song, Andrew Souers, Yunsong Tong, Gui-Dong Zhu
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Patent number: 9284311Abstract: The present invention relates to the compound according to Formula I, and to its use in medicine, in particular in the treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. In particular, the compound inhibits JAK a family of tyrosine kinases, and more particularly JAK1. The present invention also provides pharmaceutical compositions comprising the compound, methods for the prophylaxis and/or treatment of diseases involving inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons by administering the compound.Type: GrantFiled: June 10, 2013Date of Patent: March 15, 2016Assignee: GALAPAGOS NVInventors: Gerben Albert Eleutherius van 't Klooster, Florence Sylvie Namour, Réginald Christophe Xavier Brys, Luc Juliaan Corina van Rompaey
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Patent number: 9266835Abstract: The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. For example, the compounds of the present invention are useful in the treatment of metabolic disorders.Type: GrantFiled: February 6, 2015Date of Patent: February 23, 2016Assignee: Janssen Pharmaceutica NVInventors: Bart DeCorte, Mark Macielag, Michael Greco, Yue-Mei Zhang, Christopher Teleha
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Patent number: 9266836Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: GrantFiled: December 5, 2014Date of Patent: February 23, 2016Assignee: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
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Patent number: 9242981Abstract: Disclosed are the ERK inhibitors of Formula (I): (Formula (I)) and the pharmaceutically acceptable salts thereof. All substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (I).Type: GrantFiled: September 12, 2011Date of Patent: January 26, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Gerald W. Shipps, Jr., Yongqi Deng, Alan B. Cooper, Xiaolei Gao, Binyuam Sun, James Wang, Liang Zhu
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Patent number: 9242924Abstract: The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabelled amino acids for use in in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor of the [18F]-1-amino-3-fluorocyclobutanecarboxylic acid ([18F] FACBC) PET agent, ensuring that the reaction efficiently goes to completion.Type: GrantFiled: March 7, 2012Date of Patent: January 26, 2016Assignee: GE Healthcare LimitedInventors: Steven Michael Fairway, Marit Rolandsgard
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Patent number: 9238652Abstract: Provided herein is a process for the preparation of an apoptosis-inducing agent, and chemical intermediates thereof. Also provided herein are novel chemical intermediates related to the process provided herein.Type: GrantFiled: March 4, 2015Date of Patent: January 19, 2016Assignee: AbbVie Inc.Inventors: Jufang Barkalow, Jean-Christophe Califano, Vincent S. Chan, Alan C. Christesen, Timothy A. Grieme, Yi-Yin Ku, Mathew M. Mulhern, Yu-Ming M. Pu
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Patent number: 9238655Abstract: Heteroaryl pyridone and aza-pyridone compounds 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 heteroaryl pyridone and aza-pyridone compounds 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: September 8, 2014Date of Patent: January 19, 2016Assignee: Genentech, Inc.Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
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Patent number: 9227976Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.Type: GrantFiled: March 8, 2013Date of Patent: January 5, 2016Assignee: Usher III Initiative, Inc.Inventors: Roland Werner Bürli, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E Harte
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Patent number: 9226930Abstract: 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: December 1, 2014Date of Patent: January 5, 2016Assignees: 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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Patent number: 9221813Abstract: The invention provides intermediates and processes of preparation thereof useful in the preparation of compounds that can be used as CHK1 inhibitors.Type: GrantFiled: April 22, 2013Date of Patent: December 29, 2015Assignee: Genentech, Inc.Inventor: Chong Han
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Patent number: 9200000Abstract: The present invention relates to compounds of the Formula and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.Type: GrantFiled: November 1, 2013Date of Patent: December 1, 2015Assignee: Pfizer Inc.Inventors: Christopher John Helal, Thomas Allen Chappie, John Michael Humphrey, Patrick Robert Verhoest, Eddie Yang
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Patent number: 9199949Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: GrantFiled: June 27, 2012Date of Patent: December 1, 2015Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.Inventors: Tong-Shuang Li, Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
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Patent number: 9187439Abstract: The invention disclosed herein is direct to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in treating neurodegenerative diseases and promoting the generation or survival of neurons in the mammalian brain. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to a method of promoting the generation or survival of neurons in a patient in need thereof in neurodegenerative and related diseases.Type: GrantFiled: September 19, 2012Date of Patent: November 17, 2015Assignee: Inception Orion, Inc.Inventors: Austin Chih-Yu Chen, Jill Melissa Baccei, Brian Andrew Stearns, Nicholas Simon Stock, Yen Pham Truong
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Patent number: 9187486Abstract: The invention relates to bicyclic compounds of formulas I and I?, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.Type: GrantFiled: April 19, 2012Date of Patent: November 17, 2015Assignee: AMGEN INC.Inventors: Derin C. D'amico, Bradley J. Herberich, Claire L. M. Jackson, Liping H. Pettus, Andrew Tasker, Hui-Ling Wang, Bin Wu, Ryan Wurz
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Patent number: 9162987Abstract: Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula (I): wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH2, NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions comprising a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions, comprising administering a safe and effective amount of a Formula I compound.Type: GrantFiled: September 24, 2010Date of Patent: October 20, 2015Assignees: University of Louisville Research Foundation, Inc., Advanced Cancer Therapeutics, LLCInventors: Robert A. Mitchell, John O. Trent, Pooran Chand, Gilles Hugues Tapolsky
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Patent number: 9145411Abstract: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts, prodrugs, and solvates thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.Type: GrantFiled: August 2, 2013Date of Patent: September 29, 2015Assignee: Asana Biosciences, LLCInventors: Roger Astbury Smith, Aranapakam Venkatesan, Mallesham Bejugam, Subramanya Hoshalli, Srinivas Nanduri
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Patent number: 9133219Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.Type: GrantFiled: November 25, 2014Date of Patent: September 15, 2015Assignee: BASILEA PHARMACEUTICA AGInventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
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Patent number: 9126957Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.Type: GrantFiled: August 10, 2012Date of Patent: September 8, 2015Assignees: MERCK SHARP & DOHME CORP., ALECTOS THERAPEUTICS, INC.Inventors: Harold G. Selnick, Kun Liu, Ernest J. McEachern, Yuanxi Zhou, Yongbao Zhu
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Patent number: 9126998Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: GrantFiled: March 7, 2013Date of Patent: September 8, 2015Assignee: BAYER PHARMA AGInventors: Alexandros Vakalopoulos, Markus Follmann, Ingo Hartung, Philipp Buchgraber, Rolf Jautelat, Jorma Haβfeld, Niels Lindner, Frank Wunder, Johannes-Peter Stasch, Gorden Redlich, Volkhart Min-Jian Li, Eva-Maria Becker, Andreas Knorr
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Patent number: 9127001Abstract: The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula (I) act on the TASK-1 potassium channel. The compounds are particularly suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.Type: GrantFiled: September 16, 2011Date of Patent: September 8, 2015Assignee: SanofiInventors: Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler, Josef Pernerstorfer, Joachim Brendel
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Patent number: 9115126Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: GrantFiled: January 13, 2011Date of Patent: August 25, 2015Assignee: Merck Sharp & Dohme B.V.Inventors: Jiaqiang Cai, David Jonathan Bennett, Philip Stephen Jones
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Patent number: 9107868Abstract: The present invention relates to the discovery of a novel molecular pathway involved in long-term hyperexcitability of sensory neurons, which, in higher animals, is associated with persistent pain. It is based on the discovery that, following injury to an axon of a neuron, an increase in nitric oxide synthase activity results in increased nitric oxide production, which, in turn, activates guanylyl cyclase, thereby increasing levels of cGMP. Increased cGMP results in activation of protein kinase G (“PKG”), which then is retrogradely transported along the axon to the neuron cell body, where it phosphorylates MAPKerk.Type: GrantFiled: August 8, 2012Date of Patent: August 18, 2015Assignee: The Trustees of Columbia University in the City of New YorkInventors: Richard Ambron, Ying-Ju Sung, Donald W. Landry, Shi-Xian Deng
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Patent number: 9102662Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: GrantFiled: November 6, 2014Date of Patent: August 11, 2015Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Patent number: 9085570Abstract: Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.Type: GrantFiled: October 10, 2011Date of Patent: July 21, 2015Assignees: The Board of Trustees of the Leland Stanford Junior University, Auckland UniServices Limited, Ruga CorporationInventors: Amato Giaccia, Edwin Lai, Olga Razorenova, Denise Chan, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Ray Tabibiazar, Po-wai Yuen
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Patent number: 9079902Abstract: The present invention provides compounds of Formula I or II, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: GrantFiled: August 16, 2012Date of Patent: July 14, 2015Assignee: AMGEN INC.Inventors: Thomas Dineen, Isaac E Marx, Hanh Nho Nguyen, Matthew Weiss
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Patent number: 9079886Abstract: The present invention is concerned with novel substituted triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 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: January 12, 2011Date of Patent: July 14, 2015Assignees: Janssen Pharmaceuticals, Inc., Cellzome LimitedInventors: Sven Franciscus Anna Van Brandt, Michel Anna Jozef De Cleyn, Henricus Jacobus Maria Gijsen, Didier Jean-Claude Berthelot, Michel Surkyn
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Patent number: 9073913Abstract: Imidazoquinolines of formula I that contain substituted amine or amide functionality at 1-position and that are effective as Toll like Receptor 7 activators are disclosed. These compounds are useful as anticancer agents.Type: GrantFiled: March 23, 2009Date of Patent: July 7, 2015Assignee: 4SC AGInventors: Volker Gekeler, Thomas Maier, Astrid Zimmermann, Hans-Peter Hofmann, Sanjeev A. Kulkarni, Anil P. Jagtap, Ganesh S. Chaure
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Patent number: 9067925Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.Type: GrantFiled: November 26, 2012Date of Patent: June 30, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
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Patent number: 9062045Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: GrantFiled: September 13, 2012Date of Patent: June 23, 2015Assignee: Novartis AGInventors: Chao Chen, Haibing Deng, Haibing Guo, Feng He, Lei Jiang, Fang Liang, Yuan Mi, Huixin Wan, Yao-Chang Xu, Hongping Yu, Ji Yue (Jeff) Zhang
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Patent number: 9050344Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof are disclosed. Also disclosed are 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: GrantFiled: January 9, 2014Date of Patent: June 9, 2015Assignee: Gilead Sciences, Inc.Inventors: Gediminas Brizgys, Chien-Hung Chou, Randall L. Halcomb, Yunfeng Eric Hu, Qi Liu, John R. Somoza, Winston C. Tse, Jennifer R. Zhang
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Publication number: 20150148332Abstract: The present invention provides compounds of formula (Ia) and (Ib) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.Type: ApplicationFiled: November 25, 2014Publication date: May 28, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Alexander Flohr, Katrin Groebke Zbinden, Bernd Kuhn, Christian Lerner, Markus Rudolph, Herve Schaffhauser
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Publication number: 20150148331Abstract: A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease.Type: ApplicationFiled: July 24, 2014Publication date: May 28, 2015Inventors: Esther Birtalan, Peter Hoelig, David J. Lindley, Yeshwant D. Sanzgiri, Ping Tong
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Publication number: 20150141402Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, G, ring A, ring B, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, and m are defined herein. The novel purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.Type: ApplicationFiled: November 20, 2014Publication date: May 21, 2015Applicant: PFIZER INC.Inventors: Douglas Carl Behenna, Hengmiao Cheng, Sujin Cho-Schultz, Theodore Otto Johnson, JR., John Charles Kath, Asako Nagata, Sajiv Krishnan Nair, Simon Paul Planken
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Publication number: 20150141403Abstract: 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: ApplicationFiled: December 1, 2014Publication date: May 21, 2015Inventors: 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: 20150141401Abstract: A diazabicyclooctane compound, which is a beta-lactame inhibitor, represented by the following formula (I): wherein A represents Ra(Rb)N— or RcO—; B represents NH or NC1-6 alkyl; C represents benzyl, H or SO3M, wherein M represents H, an inorganic or an organic cation; Ra and Rb represent H, C1-6 alkyl or acyl; Rc represents C1-6 alkyl or a heterocyclyl; A is unsubstituted or substituted with 0 to 4 substituents Fn1, wherein Fn1 represents C1-6 alkyl, O?, or Rg-(CH2)0-3—, wherein Rg represents a heterocyclyl, phenyl, heteroaryl, acyl, RdO2S—, Re(Rf)N—, Re(Rf)NCO—, ReO—, ReOCO— or a protective group, wherein Rd represents C1-6 alkyl or MO—; Re and Rf represent H or C1-6 alkyl, and a heterocycle having at least one nitrogen atom may be formed between Ra and Rb, between Rc and B, or between Re and Rf.Type: ApplicationFiled: May 30, 2013Publication date: May 21, 2015Applicant: MEIJI SEIKA PHARMA CO., LTD.Inventors: Takao Abe, Takeshi Furuuchi, Yoshiaki Sakamaki, Seiichi Inamura, Akihiro Morinaka
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Publication number: 20150141400Abstract: The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 24, 2013Publication date: May 21, 2015Inventors: Takeshi Murata, Hatsuo Kawada, Satoshi Niizuma, Sousuke Hara, Kihito Hada, Hideaki Shimada, Hiroshi Tanaka, Toshiyuki Mio
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Patent number: 9034884Abstract: The present invention provides heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines of Formula I: wherein X, Y, Z, L, A, R5, n, m, and r are defined above, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: GrantFiled: November 18, 2011Date of Patent: May 19, 2015Assignee: Incyte CorporationInventors: James D. Rodgers, Wenyu Zhu, Joseph Glenn
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Publication number: 20150133422Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.Type: ApplicationFiled: November 8, 2013Publication date: May 14, 2015Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose
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Publication number: 20150133428Abstract: The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: November 14, 2014Publication date: May 14, 2015Inventors: Upender Velaparthi, Chetan Padmakar Darne, Peiying Liu, Mark D. Wittman, Bradley C. Pearce, Erika M. V. Araujo, Bireshwar Dasgupta, Jalathi Surendran Nair, Sakthi Kumaran Janakiraman, Chandrasekhar Reddy Rachamreddy, Mettu Mallikarjuna Rao, Arul Mozhi Selvan Subbiah Karuppiah, Bandreddy Subba Reddy, Pulicharla Nagalakshmi, Rajesh Onkardas Bora, Shilpa Holehatti Maheshwarappa, Selvakumar Kumaravel, Dibakar Mullick, Ramesh Sistla
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Publication number: 20150133427Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: ApplicationFiled: October 15, 2014Publication date: May 14, 2015Applicant: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
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Patent number: 9029357Abstract: The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.Type: GrantFiled: June 27, 2014Date of Patent: May 12, 2015Assignee: BioprojetInventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Denis Danvy, Stéphane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
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Patent number: 9029356Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: GrantFiled: March 14, 2014Date of Patent: May 12, 2015Assignee: Nerviano Medical Sciences S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Publication number: 20150126488Abstract: [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.Type: ApplicationFiled: April 17, 2013Publication date: May 7, 2015Applicant: ASTELLAS PHARMA INCInventors: Yutaka Nakajima, Sunao Imada, Yuji Takasuna, Naohiro Aoyama, Takahiro Nigawara, Shohei Shirakami, Fumiyuki Shirai, Junji Sato, Keita Nakanishi, Kaori Kubo
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Publication number: 20150126492Abstract: The present invention provides a compound of formula I a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitor of the complement alternative pathway and particularly as inhibitor of Factor B for the treatment of e.g. age-related macular degeneration and diabetic retinopathy. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 19, 2013Publication date: May 7, 2015Applicant: NOVARTIS AGInventors: Michael Dechantsreiter, Jonathan E. Grob, Aengus Macsweeney, Wolfgang Miltz, Stefan Andreas Randl, Richard Sedrani, Holger Sellner, Finton Sirockin, Eric Valeur
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Patent number: 9023840Abstract: The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: GrantFiled: February 21, 2014Date of Patent: May 5, 2015Assignee: Incyte CorporationInventors: Wenqing Yao, David M Burns, Jincong Zhuo
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Patent number: 9023839Abstract: 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: April 22, 2014Date of Patent: May 5, 2015Assignee: IRM LLCInventors: Valentina Molteni, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh