Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
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Publication number: 20140147411Abstract: In certain embodiments, the disclosure relates to methods of treating cancer comprising administering an effective amount a tyrosine kinase inhibitor in combination with an immunotherapy to a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating cancer comprising: i) analyzing both chromosomes in a cell from a subject for the a V600E mutation of BRAF; and ii) determining if both of the chromosomes contain the V600E mutation, then treating the subject comprising the step of administering an effective amount a tyrosine kinase inhibitor in combination with an immunotherapy to the subject.Type: ApplicationFiled: November 12, 2013Publication date: May 29, 2014Applicants: U.S. GOVERNMENT represented by the UNITED STATES DEPARTMENT OF VETERANS AFFAIRS, EMORY UNIVERSITYInventors: Brian Paul Pollack, Bishu Sapkota, Charles E. Hill
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Publication number: 20140148461Abstract: The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: November 22, 2013Publication date: May 29, 2014Inventors: Hervé GENESTE, Sean Colm TURNER, Michael OCHSE, Karla DRESCHER, Lawrence A. BLACK, Katja JANTOS
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Publication number: 20140148478Abstract: The invention relates to substituted heteroquinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: November 27, 2013Publication date: May 29, 2014Applicant: GRÜNENTHAL GMBHInventors: Sven KÜHNERT, Simon LUCAS, Gregor BAHRENBERG, Wolfgang SCHRÖDER
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Publication number: 20140148467Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: February 3, 2014Publication date: May 29, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Publication number: 20140148430Abstract: Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: November 26, 2012Publication date: May 29, 2014Applicant: Gilead Connecticut, Inc.Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao
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Publication number: 20140148438Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.Type: ApplicationFiled: September 22, 2011Publication date: May 29, 2014Inventor: Michael Farber
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Publication number: 20140148465Abstract: The invention describes methods and compositions for alleviating medical afflictions for which anxiety may cause or exacerbate the affliction. A subject suffering from the affliction is treated with a combination of a pharmaceutical compound that enhances learning, and a second pharmaceutical recognized to be useful for treatment of the affliction, wherein D-cycloserine is the pharmaceutical compound that enhances learning. Representative afflictions include pain, mood disorders, anxiety disorders including performance anxiety, insomnia, female sexual dysfunction, chronic fatigue, autism spectrum disorders, fibromyalgia, and attention deficit-hyperactivity disorder.Type: ApplicationFiled: January 31, 2014Publication date: May 29, 2014Inventors: Jason P. McDevitt, Michael Davis
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Patent number: 8735424Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: GrantFiled: August 31, 2009Date of Patent: May 27, 2014Assignee: Novartis AGInventors: Matthew Burger, Mika Lindvall
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Patent number: 8735398Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: GrantFiled: November 7, 2012Date of Patent: May 27, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
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Publication number: 20140142135Abstract: The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 and R6 may have the meanings as described in claim 1, as well as medicaments which contain these compounds. Further, the invention relates to methods of treating a disease selected from asthma, COPD, allergic rhinitis, adult respiratory distress syndrome, bronchitis, allergic dermatitis, contact dermatitis, idiopathic thrombocytopenic purpura, rheumatoid arthritis and allergic rhinoconjunctivitis by administrating an appropriate amount of a compound of formula 1 to a patient in need thereof.Type: ApplicationFiled: November 4, 2013Publication date: May 22, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dennis FIEGEN, Sandra HANDSCHUH, Silke HOBBIE, Matthias HOFFMANN, Takeshi KONO, Yayoi SATO, Andreas SCHNAPP, Annette SCHULER-METZ
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Publication number: 20140142108Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 30, 2013Publication date: May 22, 2014Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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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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Patent number: 8729074Abstract: The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: GrantFiled: March 19, 2010Date of Patent: May 20, 2014Assignee: Amgen Inc.Inventors: Yunxin Y. Bo, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Aaron C. Siegmund, Nuria A. Tamayo, Kevin C. Yang
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Patent number: 8729096Abstract: The present invention relates to novel imidazolidine-2,4-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2 (FPR2).Type: GrantFiled: February 12, 2013Date of Patent: May 20, 2014Assignee: Allergan, Inc.Inventors: Richard L. Beard, Vidyasagar Vuligonda, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 8729081Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.Type: GrantFiled: October 12, 2009Date of Patent: May 20, 2014Assignee: VM Discovery Inc.Inventor: Jay Jie-Qiang Wu
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Patent number: 8729095Abstract: A compound of the general formula (I): [wherein, R1 represents a halogen atom, or the like, R2 represents a hydrogen atom, or the like, R3 and R4, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, R5 represents a hydrogen atom, a halogen atom, or the like, R6 represents a hydrogen atom, a halogen atom, or the like, R7 and R8, each independently, represent a hydrogen atom, a halogen atom, or the like, R9 and R10, each independently, represent a hydrogen atom, a C1-4 alkyl group, R11 and R12, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, X represents an oxygen atom, a group —CH2—, or the like, Y represents a nitrogen atom, a group ?CH—, or the like, and Z represents a nitrogen atom, or the like] or a pharmacologically acceptable salt thereof, which has an excellent suppressive action on platelet aggregation, and is useful for prevention and/or treatment of thromboembolism.Type: GrantFiled: August 27, 2010Date of Patent: May 20, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Tatsuya Nishi, Masashi Hasegawa, Yumi Nakamoto, Yuichi Ochiai, Ryoko Kitazawa, Hiroshi Susaki
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Publication number: 20140134133Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: November 10, 2013Publication date: May 15, 2014Applicants: Calitor Sciences, LLCInventor: Ning Xi
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Publication number: 20140135328Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
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Publication number: 20140135218Abstract: This document discloses molecules having the following formula (Formula One) and processes related thereto.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: DOW AGROSCIENCES LLCInventors: Negar Garizi, Maurice C. Yap, Tony K. Trullinger, CaSandra L. McLeod, Paul R. LePlae, JR., Timothy C. Johnson, Ricky Hunter, John F. Daeuble, SR., Ann M. Buysse
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Publication number: 20140135325Abstract: The invention encompasses compound and pharmaceutical composition comprising the compound of the following Formula (I): or pharmaceutically acceptable salts or prodrugs thereof, that are useful for inhibiting ezrin protein in a cell or for inhibiting the growth of a cancer cell.Type: ApplicationFiled: October 7, 2013Publication date: May 15, 2014Applicant: GEORGETOWN UNIVERSITYInventors: Milton L. Brown, Mikell Paige, Jeffrey A. Torestsky, Aykut Uren, George Kosturko, Gullay Bulut
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Patent number: 8722677Abstract: Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), wherein the dashed lines, X, Y and R1 through R5 are as defined in the specification. The compounds are useful in the prophylaxis or treatment of viral infections.Type: GrantFiled: June 22, 2012Date of Patent: May 13, 2014Assignees: Gilead Sciences, Inc., K.U. Leuven Research & DevelopmentInventors: Steven S. Bondy, David A. Oare, Gerhard Puerstinger
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Patent number: 8722687Abstract: The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: April 15, 2010Date of Patent: May 13, 2014Assignee: Astex Therapeutics LtdInventors: Gordon Saxty, Valerio Berdini, Christopher William Murray, Eddy Jean Edgard Freyne, Yannick Aimé Eddy Ligny, Pascal Ghislain André Bonnet, Berthold Wroblowski, Alexandra Papanikos
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Patent number: 8722702Abstract: Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.Type: GrantFiled: February 25, 2013Date of Patent: May 13, 2014Assignee: Plexxikon Inc.Inventors: Jiazhong Zhang, Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Guoxian Wu, Marika Nespi, Chao Zhang
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Patent number: 8722708Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6?R7?); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7? are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.Type: GrantFiled: June 12, 2006Date of Patent: May 13, 2014Assignees: Merck Sharp & Dohme Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Andrew Stamford, Guoqing Li, William Greenlee, Zhaoning Zhu, Brian McKittrick, Robert Mazzola, Ying Huang, Tao Guo, Thuy X. H. Le, Gang Qian, Yuefei Shao
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Publication number: 20140128374Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.Type: ApplicationFiled: November 5, 2013Publication date: May 8, 2014Applicant: PFIZER INCInventors: JENNIFER ELIZABETH DAVOREN, AMY BETH DOUNAY, IVAN VIKTOROVICH EFREMOV, DAVID LAWRENCE FIRMAN GRAY, SCOT RICHARD MENTE, STEVEN VICTOR O'NEIL, BRUCE NELSEN ROGERS, CHAKRAPANI SUBRAMANYAM, LEI ZHANG
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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: 20140128426Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: ApplicationFiled: May 9, 2013Publication date: May 8, 2014Applicant: Siga Technologies Inc.Inventor: Siga Technologies Inc.
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Publication number: 20140128424Abstract: 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: ApplicationFiled: March 7, 2013Publication date: May 8, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventor: BAYER PHARMA AKTIENGESELLSCHAFT
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Publication number: 20140128372Abstract: 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: ApplicationFiled: March 7, 2013Publication date: May 8, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Alexandros VAKALOPOULOS, Markus FOLLMANN, Ingo HARTUNG, Philipp BUCHGRABER, Rolf JAUTELAT, Jorma HAßFELD, Niels LINDNER, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva-Maria BECKER, Andreas KNORR
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Publication number: 20140128425Abstract: 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: ApplicationFiled: March 7, 2013Publication date: May 8, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Alexandros VAKALOPOULOS, Ingo HARTUNG, Markus FOLLMANN, Rolf JAUTELAT, Niels LINDNER, Dirk SCHNEIDER, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI
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Publication number: 20140128373Abstract: Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: February 1, 2012Publication date: May 8, 2014Inventors: Prabha N. Ibrahim, Chao Zhang, Wayne Spevak, Jiazhong Zhang, Guoxian Wu, Jack Lin, Hanna Cho, Marika Nespi, Songyuan Shi, Todd Ewing, Ying Zhang
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Publication number: 20140128335Abstract: The present invention relates to the use of polyaminoisoprenyl derivatives in antibiotic or antiseptic treatment of bacteria including those presenting multiple drug resistance (MDR), in particular as efflux pump inhibitors. It also relates to novel polyaminoisoprenyl derivatives, compositions comprising the same, process for preparing the same, and use thereof in antibiotic or antiseptic treatment.Type: ApplicationFiled: February 23, 2012Publication date: May 8, 2014Applicants: UNIVERSITE D'AIX-MARSEILLE, UNIVERSITE DE CORSE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Jean-Michel Bolla, Jean Michel Brunel, Joseph Pierre Felix Casanova, Vannina Lorenzi, Liliane Berti
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Publication number: 20140128386Abstract: 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: ApplicationFiled: November 4, 2013Publication date: May 8, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Alexandros VAKALOPOULOS, Ingo HARTUNG, Markus FOLLMANN, Rolf JAUTELAT, Alexander STRAUB, Jorma HAßFELD, Niels LINDNER, Dirk SCHNEIDER, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva Maria BECKER-PELSTER, Andreas KNORR
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Patent number: 8716273Abstract: The invention relates to compounds of the general formula (I): Wherein X, Y, Z, Z1, Z2, Z3, Z4 and n are as defined herein. The invention also relates to a method for making the same and to the use thereof in therapy.Type: GrantFiled: February 10, 2012Date of Patent: May 6, 2014Assignee: SANOFIInventors: Laurent Dubois, Yannick Evanno, Catherine Gille, David Machnik, Andre Malanda
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Patent number: 8716272Abstract: The invention relates to compounds of the general formula (I): Wherein X, Y, Z, Z1, Z2, Z3, Z4 and n are as defined herein. The invention also relates to a method for making the same and to the use thereof in therapy.Type: GrantFiled: February 10, 2012Date of Patent: May 6, 2014Assignee: SanofiInventors: Laurent Dubois, Yannick Evanno, Catherine Gille, David Machnik, Andre Malanda
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Publication number: 20140121235Abstract: Disclosed herein are methods for treating an S6K-overexpressing cancer, comprising administering a therapeutically effective amount of leflunomide to a subject in need thereof.Type: ApplicationFiled: October 25, 2013Publication date: May 1, 2014Applicant: Rush University Medical CenterInventor: Xiulong Xu
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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: 20140121203Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to imidazo[1,2-a]pyridine containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities (HDAC).Type: ApplicationFiled: January 3, 2014Publication date: May 1, 2014Applicant: MEI Pharma, Inc.Inventors: Ken Chi Lik Lee, Eric T. Sun, Haishan Wang
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Publication number: 20140120083Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating cancers or hematologic disorders.Type: ApplicationFiled: March 15, 2013Publication date: May 1, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Howard M. STERN, Jeffery L. KUTOK
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Publication number: 20140121236Abstract: Disclosed is a compound for treatment of Myotonic Dystrophy type 1 having the formula: Wherein X is selected from the group consisting of O, N, C, or S, Y is a homo- or heteroatomic 5-membered ring comprising one or more atoms selected from the group consisting of N, O, S, and C, Z is an optionally substituted aryl group or optionally substituted heteroaryl, including but not limited to halogenated benzenes, pyridines, substituted benzene, substituted pyridine, R2=hydroxy, acyl, alkoxyl, esters, ethers, cyclic ethers, and lactones, R3=H, alkyl, an optionally substituted alkyl, aliphatic ether, ester, cyclic unsaturated and aromatic ring groups, and R1, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, and alkoxyl or a pharmaceutically or cosmetically acceptable salt, solvate, or hydrate thereof.Type: ApplicationFiled: November 19, 2013Publication date: May 1, 2014Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Sita REDDY, Lucio COMAI, Nouri NEAMATI
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Publication number: 20140120111Abstract: The present invention provides novel methods for treating Th2-mediated immune disorders and enhancing Th1-mediated immune responses in a subject comprising administering to the subject, a pharmaceutical composition comprising a serum-glucocorticoid regulated kinase 1 (SGK1) inhibitor and a pharmaceutically acceptable carrier. Methods for treating a wide range of autoimmune diseases are also taught. The present invention also provides methods for augmenting the treatment of subjects having viral or parasitic infections, or which have cancerous tumors.Type: ApplicationFiled: May 17, 2012Publication date: May 1, 2014Inventors: Jonathan David Powell, Emily Beth Heikamp
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Patent number: 8709419Abstract: The present invention relates to a combination therapy of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide, or a pharmaceutically acceptable salt thereof, and an EGFR inhibitor for treating a patient suffering from a proliferative disorder, in particular a solid tumor, for example, colorectal cancer, melanoma, and thyroid cancer.Type: GrantFiled: August 10, 2011Date of Patent: April 29, 2014Assignee: Hoffmann-La Roche, Inc.Inventors: Kapil Dhingra, Brian Higgins, Kenneth Kolinsky, Richard J. Lee, Brian Lestini, Kathryn Packman, Fei Su
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Patent number: 8710074Abstract: In one aspect, the invention relates to dihydronaphthyridinyl(organo)methanone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate 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: January 12, 2012Date of Patent: April 29, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Jason Manka, Jon Jacobs, Ya Zhou, José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Susana Conde-Ceide, Eric S. Dawson
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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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Patent number: 8710073Abstract: The present invention relates to bi-substrate inhibitor molecules combining (i) a pyridine, pyridinium or dihydropyridine-type structure allied to active metabolites of isoniazide, or related structures, and (ii) a hydrophobic substituent. The invention also relates to the method for preparing said molecules, to the pharmaceutical compositions containing said molecules, and to the use thereof as inhibitors of enoyl reductase for the preparation of a drug, especially an anti-infective drug for the treatment of tuberculosis.Type: GrantFiled: February 6, 2009Date of Patent: April 29, 2014Assignees: Centre National de la Recherche Scientifique (C.N.R.S.), Universite Paul Sabatier Toulouse IIIInventors: Jean Bernadou, Vania Bernardes-Genisson, Tamara Delaine, Annaïck Quemard
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Publication number: 20140113892Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4-P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: ApplicationFiled: May 10, 2013Publication date: April 24, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
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Publication number: 20140113898Abstract: The invention relates to bisarylsulfone and dialkylarylsulfone compounds (e.g., compounds according to any of Formulas (I)-(IX) or compounds (1)-(227) of Tables 4 and 5) useful in treating conditions associated with calcium channel function, and particularly conditions associated with N-type calcium channel activity. The invention also relates to pharmaceutical compositions that include these bisarylsulfone compounds, as well methods for the treatment of conditions such as cardiovascular disease, epilepsy, cancer and pain.Type: ApplicationFiled: November 4, 2011Publication date: April 24, 2014Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan A. Pajouhesh, Richard Holland, Yuanxi Zhou, Yongbao Zhu, Michael Edward Grimwood, Navjot Chahal
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Publication number: 20140113917Abstract: The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2 antagonistic activity, wherein L, Y1, Y2, Y3, Y4, Y5, Z, R1, R2, R3 and n have one of the meanings as indicated in the specification and claims, to their use as medicaments, to pharmaceutical compositions containing said compounds and to pharmaceutical compositions containing said compounds in combination with one or more active substances.Type: ApplicationFiled: March 15, 2012Publication date: April 24, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Boehringer Ingelheim International GmbH
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Publication number: 20140113931Abstract: Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.Type: ApplicationFiled: March 15, 2013Publication date: April 24, 2014Applicant: Portola Pharmaceuticals, Inc.Inventor: Portola Pharmaceuticals, Inc.
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Patent number: 8703165Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.Type: GrantFiled: November 30, 2010Date of Patent: April 22, 2014Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer