Ring Nitrogen In The Bicyclo Ring System Patents (Class 514/235.2)
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Publication number: 20140275077Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.Type: ApplicationFiled: May 13, 2014Publication date: September 18, 2014Applicant: Cephalon, Inc.Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
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Publication number: 20140275075Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.Type: ApplicationFiled: March 13, 2013Publication date: September 18, 2014Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENTInventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER
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Publication number: 20140275033Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff
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Publication number: 20140275078Abstract: The present invention relates to compositions comprising at least one MAPK pathway inhibitor including MEK and RAF inhibitors and at least one PI3K? inhibitor, and also to uses thereof for the treatment of cancer.Type: ApplicationFiled: September 14, 2012Publication date: September 18, 2014Applicant: SANOFIInventors: Carlos Garcia-Echeverria, Loïc Vincent, Angela Virone-Oddos
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Publication number: 20140275076Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R1 is optionally substituted heteroaryl etc.; R2 is hydrogen etc.; R3 and R4 are each independently hydrogen etc., R5 is the following group: (wherein Y is optionally substituted five membered heteroaryl etc., R9a is optionally substituted aryl etc., R9b and R9c are each dependently hydrogen etc., and m is the integral 0 etc.) etc.; R6 is hydrogen etc.; and R7 is hydrogen etc.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Katsunori Tsuboi, Yosuke Takanashi, Shingo Tojo, Tomohiro Kodama, Katsumi Kubota, Toshio Kanai
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Publication number: 20140274960Abstract: The present invention provides compounds of Formula (I) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.Type: ApplicationFiled: October 12, 2012Publication date: September 18, 2014Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
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Publication number: 20140256725Abstract: The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.Type: ApplicationFiled: September 14, 2012Publication date: September 11, 2014Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Matthijs Poulie, Cornelis Marius Timmers, Saskia Vertaik
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Publication number: 20140256658Abstract: The present invention describes antibiotic conjugates. These single drug entities are formed connecting one antibiotic with another antibiotic. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
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Publication number: 20140256724Abstract: The present application relates to cycloalkylpyridin-2-amines derivates of formula (1) or stereoisomers thereof or pharmaceutically acceptable salts thereof. The present application also relates to the process for the preparation of compounds of formula (I). The present application further describes the compounds of formula (1) as cholesteryl ester-transfer protein (CETP) inhibitors. The present application further relates to pharmaceutical compositions comprising compounds of formula (1) or stereoisomers thereof or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 17, 2012Publication date: September 11, 2014Applicant: DR. REDDY'S LABORATORIES LTD.Inventors: Anima Boruah, Shanavas Alikunju
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Publication number: 20140249144Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.Type: ApplicationFiled: May 12, 2014Publication date: September 4, 2014Applicant: KOWA COMPANY, LTD.Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
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Patent number: 8822462Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.Type: GrantFiled: January 28, 2010Date of Patent: September 2, 2014Assignee: Emory UniversityInventors: Stephen F. Traynelis, Dennis C. Liotta, Rose M. Santangelo, Ethel C. Garnier
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Patent number: 8822495Abstract: The invention relates to azacyclyl-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted aryldihydroisoquinolinone of the invention or its derivative, and the use of the azacyclyl-substituted aryldihydroisoquinolinones of the invention and their derivatives as MCH antagonists.Type: GrantFiled: August 14, 2008Date of Patent: September 2, 2014Assignee: SanofiInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig
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Patent number: 8822452Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.Type: GrantFiled: July 22, 2013Date of Patent: September 2, 2014Assignee: Laboratorios Salvat, S.A.Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Ester Monlleo Mas
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Publication number: 20140243314Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 24, 2012Publication date: August 28, 2014Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Publication number: 20140243333Abstract: A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.Type: ApplicationFiled: May 13, 2014Publication date: August 28, 2014Applicants: University of Kansas, University of North CarolinaInventors: Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski
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Publication number: 20140243332Abstract: Disclosed herein are methods of treating cancers characterized by aberrant ROS1 activity by administering an effective amount of foretinib (N1?-[3-fluoro-4-[[6-methoxy-7-(3-morpholinopropoxy)-4-quinolyl]oxy]phenyl]-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide), including methods of identifying mutations in the kinase domain of ROS1 that indicate resistance to crizotinib, but sensitivity to foretinib.Type: ApplicationFiled: February 26, 2014Publication date: August 28, 2014Applicant: Oregon Health & Science UniversityInventors: Monika A. Davare, Brian J. Druker
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Patent number: 8809326Abstract: Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.Type: GrantFiled: September 18, 2007Date of Patent: August 19, 2014Assignee: Aerie Pharmaceuticals, Inc.Inventors: Todd Bosanac, John David Ginn, Eugene Richard Hickey, Thomas Martin Kirrane, Jr., Weimin Liu, Anthony S. Prokopowicz, Sabine K. Schlyer, Cheng-Kon Shih, Roger John Snow, Michael Robert Turner, Frank Wu, Erick Richard Young
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Publication number: 20140228359Abstract: The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.Type: ApplicationFiled: July 20, 2012Publication date: August 14, 2014Applicant: UNIVERSITE JOSEPH FOURIERInventors: Jean-Noël Denis, Marcelle Claude Jolivalt, Louis Max Maurin, Nikolaevna Olga Burchak
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Publication number: 20140228343Abstract: 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: December 20, 2013Publication date: August 14, 2014Applicant: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
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Patent number: 8802671Abstract: Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (I) a pharmaceutically acceptable acid or base addition salt, a quaternary amine, a stereochemically isomeric form, a tautomeric form or a N-oxide form thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1 to 3; s is 0 to 4; R2 is hydrogen; halo; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 0 to 4; R4 and R5 each independently are hydrogen, alkyl or benzyl; or R4 and R5 may be taken together including the N to which they are attached; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl,Type: GrantFiled: July 31, 2006Date of Patent: August 12, 2014Assignee: Janssen Pharmaceutica NVInventors: Jérôme Emile Georges Guillemont, Elisabeth Thérèse Jeanne Pasquier, David Francis Alain Lançois, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul, Leo Jacobus Jozef Backx, Lieven Meerpoel
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Publication number: 20140221372Abstract: The present invention is directed to methods of administering foretinib or pharmaceutically acceptable salts or solvates thereof a c-Met inhibitor to a patient in need thereof comprising: determining whether said patient has less than 2 copies of the CAT haplotype in NR1I3 gene and/or the TT or CT genotype at the rs1045642 reference single nucleotide polymorphism in ABCB1 gene; and if said patient has less than 2 copies of the CAT haplotype in NR1I3 gene and/or the TT or CT genotype at the rs1045642 reference single nucleotide polymorphism in ABCB1 gene, administering to said patient a pharmaceutical composition comprising foretinib or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 6, 2014Publication date: August 7, 2014Applicant: GlaxoSmithKline Intellectual Property (NO 2.) LimitedInventors: Diptee Amit KULKARNI, Colin F Spraggs
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Publication number: 20140221345Abstract: 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: December 20, 2013Publication date: August 7, 2014Applicant: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
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Publication number: 20140221371Abstract: The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions.Type: ApplicationFiled: December 23, 2013Publication date: August 7, 2014Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Charles W. Hutchins, Franciso Javier Garcia-Ladona, Wolfgang Wernet
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Patent number: 8796268Abstract: This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: August 11, 2011Date of Patent: August 5, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Yongbo Hu, Todd B. Sells, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Publication number: 20140213586Abstract: The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.Type: ApplicationFiled: September 26, 2012Publication date: July 31, 2014Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. Leuven R&DInventors: Dorothee Bardiot, Gunter Carlens, Kai Dallmeier, Suzanne Kaptein, Michael McNaughton, Arnaud Marchand, Johan Neyts, Wim Smets, Mohamed Koukni
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Publication number: 20140213549Abstract: The present invention provides a substituted pyridine compound or a pharmacologically acceptable salt thereof which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a compound represented by a general formula (I), wherein R1 is H, optionally substituted alkyl, OH, optionally substituted alkoxy, alkylsulfonyl, optionally substituted amino, carboxy, optionally substituted carbonyl, CN, halogeno, optionally substituted phenyl, optionally substituted aromatic heterocyclyl, optionally substituted saturated heterocyclyl, optionally substituted saturated heterocyclyloxy or optionally substituted saturated heterocyclylcarbonyl, etc., and the like.Type: ApplicationFiled: July 8, 2011Publication date: July 31, 2014Applicants: UBE INDUSTRIES, LTD., DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsuyoshi Nakamura, Hidenori Namiki, Naoki Terasaka, Akiko Shima, Masahiko Hagihara, Noriaki Iwase, Katsunori Takata, Osamu Kikuchi, Kazunari Tsuboike, Hiroyuki Setoguchi, Kenji Yoneda, Hidetoshi Sunamoto, Koji Ito
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Publication number: 20140213582Abstract: 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: December 20, 2013Publication date: July 31, 2014Applicant: EPIZYME, INC.Inventors: KENNETH W. DUNCAN, RICHARD CHESWORTH, MICHAEL JOHN MUNCHHOF
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Patent number: 8791090Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.Type: GrantFiled: March 31, 2010Date of Patent: July 29, 2014Assignee: Kowa Company, Ltd.Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
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Publication number: 20140205537Abstract: Provided herein are compounds that inhibit or partially inhibit the activity of leucine rich repeat kinases. Also provided herein are methods of treatment of CNS disorders comprising administration of inhibitors of leucine rich repeat kinases.Type: ApplicationFiled: June 22, 2012Publication date: July 24, 2014Applicant: ZENOBIA THERAPEUTICS, INC.Inventors: Pierre-Yves Bounaud, Vicki Nienaber, Ruo W. Steensma, John A. Lowe, III
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Publication number: 20140206689Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: March 21, 2014Publication date: July 24, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Patent number: 8785489Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.Type: GrantFiled: October 13, 2009Date of Patent: July 22, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
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Publication number: 20140200197Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: September 9, 2013Publication date: July 17, 2014Inventors: JOHN A. MCCAULEY, CHRISTIAN BEAULIEU, DAVID J. BENNETT, CHRISTOPHER J. BUNGARD, RONALD K. CHANG, SHELDON CRANE, THOMAS J. GRESHOCK, LI HAO, KATE HOLLOWAY, JESSE J. MANIKOWSKI, DANIEL MCKAY, CARMELA MOLINARO, OSCAR MIGUEL MORADEI, PHILIPPE G. NANTERMET, CHRISTIAN NADEAU, TUMMANAPALLI SATYANARAYANA, WILLIAM SHIPE, SANJAY KUMAR SINGH, VOUY LINH TRUONG, SIVALENKA VIJAYARADHI, PETER D. WILLIAMS, CATHERINE M. WISCOUNT
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Publication number: 20140200216Abstract: The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: ApplicationFiled: January 14, 2014Publication date: July 17, 2014Applicant: INCYTE CORPORATIONInventors: Yun-Long Li, David M. Burns, Hao Feng, Chu-Biao Xue, Anlai Wang, Jun Pan
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Publication number: 20140199263Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: August 16, 2012Publication date: July 17, 2014Inventors: Casey Cameron McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
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Publication number: 20140194423Abstract: The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor.Type: ApplicationFiled: March 4, 2014Publication date: July 10, 2014Inventors: Baltazar Gomez-Mancilla, Fabrizio Gasparini
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Publication number: 20140194415Abstract: This invention relates to spirocyclic piperidines according to Formula (I) and the use of spirocyclic piperidines 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 spirocyclic piperidines in the treatment of cancer.Type: ApplicationFiled: August 16, 2012Publication date: July 10, 2014Applicant: GlaxoSmithKline Intellectual Property (No2) LimiteInventors: Jonathan Michael Ghergurovich, Michael Lee Moore, Cynthia Ann Parrish, Lance Howard Ridgers, Hongyi Lu
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Publication number: 20140194422Abstract: The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.Type: ApplicationFiled: June 12, 2012Publication date: July 10, 2014Applicant: EMORY UNIVERSITYInventors: Thota Ganesh, Aiming Sun, Susane M. Smith, John David Lambeth
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Patent number: 8771682Abstract: The present invention relates generally to methods and compositions for reducing Interleukin-4 or Interleukin-13 signaling, in particular to treat asthma and atopic dermatitis. The inventors have found that Rac/PAK mediated endocytosis of the ligand bound type I (IL-4R with the chains IL-4Ra and IL-2-Rg) and/or type II receptor (IL-13R with the chains IL-4Ra and IL-13Ra1) is needed for the IL-4 and/or IL-13 mediated activation of downstream signalling events including phosphorylation of Stat family transcrition factors. These discoveries enable new methods of screening compounds that modulate Interleukin-4 and Interleukin-13 signalling, as well as new methods for treating conditions characterized by increased Interleukin-4 and Interleukin-13 levels. These conditions include inflammatory conditions, asthma bronchiale, atopic dermatitis, allergies, atopic syndromes, allergic rhinitis, and th2-induced conditions.Type: GrantFiled: April 26, 2012Date of Patent: July 8, 2014Assignee: Technische Universtität DresdenInventors: Christian Bökel, Thomas Weidemann
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Patent number: 8772288Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: April 3, 2009Date of Patent: July 8, 2014Assignee: Almirall, S.A.Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
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Publication number: 20140187543Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6 and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivaties can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.Type: ApplicationFiled: September 25, 2013Publication date: July 3, 2014Inventors: Wilfried Lubisch, Wilfried Hornberger, Thorsten K. Oost, Daryl Richard Sauer, Liliane Unger, Wolfgang Wernet, Hervé Geneste
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Publication number: 20140187552Abstract: The invention comprises a method of treatment of aggression and similar behavioral syndromes, such as impulsivity and irritability, by a pharmaceutical agent exhibiting combined D2 and D5 antagonistic activity.Type: ApplicationFiled: July 26, 2013Publication date: July 3, 2014Applicant: Supernus Pharmaceuticals, Inc.Inventor: Christopher D. Breder
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Publication number: 20140187510Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.Type: ApplicationFiled: July 11, 2013Publication date: July 3, 2014Applicants: THE GENERAL HOSPITAL CORPORATION, MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR CENTER FOR COMMERCIALIZATIONInventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
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Publication number: 20140186407Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.Type: ApplicationFiled: July 18, 2011Publication date: July 3, 2014Applicant: Exelixis Inc.Inventor: Jo Ann Wilson
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Publication number: 20140187553Abstract: The invention relates to bicyclic compounds of formulas I and Ia, 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: ApplicationFiled: March 21, 2012Publication date: July 3, 2014Applicant: AMGEM INC.Inventors: Hui-Ling Wang, Victor J. Cee, Bradley J. Herberich, Claire L.M. Jackson, Brian Alan Lanman, Thomas Nixey, Liping H. Pettus, Anthony B. Reed, Bin Wu, Ryan Wurz, Andrew Tasker
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Publication number: 20140186280Abstract: 8-Hydroxy-quinoline derivatives and 8-ethers, 8-esters, 8-carbonates, 8-acyloxymethyl, 8-phosphates, (phosphoryloxy)methyl, and 8-carbamates derivatives thereof are described that exhibit iron chelation, neuroprotective, neurorestorative, apoptotic and/or selective MAO-AB inhibitory activities.Type: ApplicationFiled: March 4, 2014Publication date: July 3, 2014Inventors: Vincent R. ZURAWSKI, JR., David M. STOUT, Theodore J. NITZ, Moussa B.H. YOUDIM, Orly WEINREB
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Publication number: 20140179667Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.Type: ApplicationFiled: December 18, 2013Publication date: June 26, 2014Applicant: PFIZER INC.Inventors: Martin Paul EDWARDS, Robert Arnold KUMPF, Pei-Pei KUNG, Indrawan James MCAPLINE, Sacha NINKOVIC, Eugene Yuanjin RUI, Scott Channing SUTTON, John Howard TATLOCK, Martin James WYTHES, Luke Raymond Zehnder
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Publication number: 20140179675Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.Type: ApplicationFiled: February 28, 2014Publication date: June 26, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
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Publication number: 20140171363Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.Type: ApplicationFiled: February 24, 2014Publication date: June 19, 2014Applicant: NOVARTIS AGInventors: David Weninger BARNES, Gregory Raymond BEBERNITZ, Kevin CLAIRMONT, Scott Louis COHEN, Robert Edson DAMON, II, Robert Francis DAY, Stephanie Kay DODD, Christoph GAUL, Hatice Belgin GULGEZE EFTHYMIOU, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Kai LIN, Justin Yik Ching MAO, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, SU Liansheng
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Publication number: 20140163029Abstract: Compound of formula (I) and methods of treating disorders by administering a compound of formula (I) are described herein. Examples of disorders include neoplastic disorders, fat-cell related disorders, neurodegenerative disorders, and metabolic disorders.Type: ApplicationFiled: May 24, 2013Publication date: June 12, 2014Applicant: ELIXIR PHARMACEUTICALS, INC.Inventors: Andrew D. Napper, Peter DiStefano, Rory Curtis, Jeffrey Hixon, Thomas E. McDonagh, L. Julie Huber, Jonathan M. Solomon, Russel J. Thomas, Jean-francois Pons
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Patent number: 8748614Abstract: The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: GrantFiled: June 18, 2009Date of Patent: June 10, 2014Assignee: SanofiInventors: Oliver Plettenburg, Armin Hofmeister, Jochen Goerlitzer, Matthias Löhn