1,3-diazine Ring Patents (Class 544/122)
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Patent number: 8921336Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.Type: GrantFiled: November 28, 2008Date of Patent: December 30, 2014Assignees: Dana-Farber Cancer Institute, Inc., The Scripps Research InstituteInventors: Nathanael Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang
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Publication number: 20140378450Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: Novartis AGInventors: Giorgio CARAVATTI, Robin Alec FAIRHURST, Pascal FURET, Clive MCCARTHY, Heinrich RUEEGER, Frank Hans SEILER, Frédéric STAUFFER
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Patent number: 8916554Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: July 22, 2013Date of Patent: December 23, 2014Assignee: Janssen Pharmaceutica, N.V.Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
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Patent number: 8916553Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.Type: GrantFiled: July 25, 2011Date of Patent: December 23, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Joel Francis Austin, Lisa S. Sharma, James Aaron Balog, Audris Huang, Upender Velaparthi, Chetan Padmakar Darne, Mark George Saulnier
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Publication number: 20140364398Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.Type: ApplicationFiled: August 27, 2014Publication date: December 11, 2014Applicant: PFIZER INC.Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
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Publication number: 20140363588Abstract: Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Qa, Qb, and Qc are a single bond or a divalent linking group. Ra, Rb, and Rc, are hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, cyano group, halogen group, or heterocyclic group. X2 is a single bond or a divalent linking group. X1 is a single bond or a predetermined divalent linking group.Type: ApplicationFiled: August 27, 2014Publication date: December 11, 2014Applicant: FUJIFILM CorporationInventors: Aiko YAMAMOTO, Satoshi TANAKA, Teruki NIORI, Masato NAGURA, Masaki NORO, Aiko YOSHIDA, Nobutaka FUKAGAWA, Yasukazu KUWAYAMA
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Patent number: 8906916Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: July 19, 2011Date of Patent: December 9, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Christina Esdar, Hartmut Greiner
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Patent number: 8906914Abstract: Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.Type: GrantFiled: August 17, 2010Date of Patent: December 9, 2014Assignee: Janssen Pharmaceutica NVInventors: Natalie A. Hawryluk, J. Guy Breitenbucher, William M. Jones, Alison L. Chambers, John M. Keith, Mark Seierstad
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Patent number: 8906902Abstract: The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.Type: GrantFiled: March 21, 2013Date of Patent: December 9, 2014Assignee: Biota Europe LimitedInventors: Christopher James Lunniss, James T. Palmer, Gary Robert William Pitt, David Davies, Lorraine Claire Axford
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Patent number: 8906906Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.Type: GrantFiled: August 5, 2010Date of Patent: December 9, 2014Assignee: Katholieke Universiteit LeuvenInventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
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Publication number: 20140357599Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.Type: ApplicationFiled: August 18, 2014Publication date: December 4, 2014Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
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Patent number: 8901120Abstract: In one aspect, the invention relates to substituted N-phenylpyrimidin-2-amine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of Axl kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the Axl kinase. 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: March 31, 2012Date of Patent: December 2, 2014Assignee: University of Utah Research FoundationInventors: David J. Bearss, Hariprasad Vankayalapati, Alexis Mollard, Steven L. Warner, Sunil Sharma
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Patent number: 8901119Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.Type: GrantFiled: March 9, 2012Date of Patent: December 2, 2014Assignee: GlaxoSmithKline Intellectual Property (No. 2) LimitedInventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
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Publication number: 20140343006Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,Type: ApplicationFiled: August 5, 2014Publication date: November 20, 2014Inventors: Jerome Emile Georges Guillemont, Patrice Palandijian, Marc Rene DeJonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desire Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
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Publication number: 20140343029Abstract: The invention provides novel imidazole amine compounds according to Formula (I) and Formula (II) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: September 12, 2012Publication date: November 20, 2014Applicant: MERCK PATENT GMBHInventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Lizbeth Celeste Deselm, Hui Qiu, Constantin Neagu, Donald Bankston, Christopher Charles Victor Jones
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Publication number: 20140336374Abstract: The present invention relates to a process for the production of novel antagonists for CCR2 (CC chemokine receptor 2) and intermediates thereof.Type: ApplicationFiled: July 29, 2014Publication date: November 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner EBEL, Sara FRATTINI, Riccardo GIOVANNINI, Christoph HOENKE, Thomas TRIESELMANN, Patrick TIELMANN
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Publication number: 20140336171Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: July 24, 2014Publication date: November 13, 2014Inventors: Luc Farmer, Gabriel Martinez-Botella, Albert Pierce, Francesco Salituro, Jian Wang, Marion W. Wannamaker, Tiansheng Wang
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Patent number: 8884006Abstract: A novel inhibitor of Rac activity based on the structure of the established Rac/Rac-GEF inhibitor NSC23766 is discloses. The compound EHop-016, with an IC50 of 1.1 ?M, is a 100-fold more efficient inhibitor of Rac activity than NSC23766. EHop-016 is specific for Rac1 and Rac3 at concentrations ?5 mM. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells, EHop-016 (?5 mM) inhibits the association of the Rac-GEF Vav2 with a nucleotide-free Rac1(G15A), which has a high affinity for activated GEFs. EHop-016 does not affect the association of the Rac-GEF Tiam-1 with Rac1(G15A) at similar concentrations. EHop-016 also inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation in both cell lines. EHop-016 decreases Rac-downstream effects of p21-activated kinase (PAK)1 activity and directed migration of metastatic cancer cells. At low concentrations (<5 ?M), EHop-016 does not affect cell viability.Type: GrantFiled: September 18, 2012Date of Patent: November 11, 2014Assignee: University of Puerto RicoInventors: Eliud Hernandez, Cornelis Vlaar, Suranganie Dharmawardhane
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Patent number: 8883785Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: GrantFiled: January 20, 2011Date of Patent: November 11, 2014Assignee: CHDI Foundation, Inc.Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Dirk Winkler, Frederick Brookfield, Paula C. De Aguiar Pena
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Publication number: 20140329795Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: August 28, 2012Publication date: November 6, 2014Inventors: Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson, Celia Dominguez, Leticia M. Toledo-Sherman, Ignacio Munoz
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Publication number: 20140329798Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119.Type: ApplicationFiled: November 9, 2012Publication date: November 6, 2014Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
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Publication number: 20140329816Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: July 26, 2012Publication date: November 6, 2014Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson
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Publication number: 20140328805Abstract: The present invention provides for compounds of Formula I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula all have the meaning as defined herein.Type: ApplicationFiled: May 1, 2014Publication date: November 6, 2014Applicant: GENENTECH, INC.Inventors: Anthony Estrada, Alan G. Olivero, Snahel Patel, Michael Siu
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Patent number: 8877761Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: GrantFiled: April 18, 2012Date of Patent: November 4, 2014Assignee: Pfizer Inc.Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
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Patent number: 8877745Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.Type: GrantFiled: May 10, 2011Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
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Patent number: 8877747Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.Type: GrantFiled: October 21, 2009Date of Patent: November 4, 2014Assignee: Korea Research Institute of Chemical TechnologyInventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
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Publication number: 20140323464Abstract: Provided herein are kinase inhibiting compounds and methods of using the same.Type: ApplicationFiled: May 16, 2012Publication date: October 30, 2014Inventors: John William Taunton, JR., Kenneth Albert Brameld, David Michael Goldstein, Jesse Mcfarland, Shyam Krishnan, Jonathan Choy
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Patent number: 8871314Abstract: Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Qa, Qb, and Qc are a single bond or a divalent linking group. Ra, Rb, and Rc, are hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, cyano group, halogen group, or heterocyclic group. X2 is a single bond or a divalent linking group. X1 is a single bond or a predetermined divalent linking group. R1 and R2 are a hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, or heterocyclic group.Type: GrantFiled: May 31, 2013Date of Patent: October 28, 2014Assignee: FUJIFILM CorporationInventors: Aiko Yamamoto, Satoshi Tanaka, Teruki Niori, Masato Nagura, Masaki Noro, Aiko Yoshida, Nobutaka Fukagawa, Yasukazu Kuwayama
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Publication number: 20140315882Abstract: The invention relates to new pyrrolidine derivatives of the formula wherein R1 to R3, Ar, L T and n are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: April 7, 2014Publication date: October 23, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Martin FLECK, Annekatrin HEIMANN, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
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Patent number: 8865894Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.Type: GrantFiled: February 22, 2013Date of Patent: October 21, 2014Assignee: Novartis AGInventors: Giorgio Caravatti, Robin Alec Fairhurst, Pascal Furet, Frédéric Stauffer, Frank Hans Seiler, Clive McCarthy, Heinrich Rueeger
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Publication number: 20140309210Abstract: A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein X, X1, X2, X3, R1, R2, R3, R4, R5 and R6 are described herein, compositions including the compounds and methods of making and using the compounds for the treatment of diseases.Type: ApplicationFiled: February 12, 2014Publication date: October 16, 2014Applicant: Genentech, Inc.Inventors: Jason Burch, Richard A. Goldsmith, Daniel Fred Ortwine, Richard Pastor, Zhonghua Pei
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Patent number: 8859538Abstract: The present invention provides a method of prophylaxis, treatment or inhibition of a cannabinoid receptor-associated disease, disorder or condition in a mammalian subject, the method comprising administering to the subject a compound having the structure of formula I or a pharmaceutically acceptable salt, acid salt, hydrate or stereoisomer thereof, wherein the cannabinoid receptor-associated disease, disorder or condition is pain or an inflammatory disease, disorder or condition, and wherein formula I is as follows: wherein Rb, Rc, Z, Y and m are defined in the specification.Type: GrantFiled: August 26, 2010Date of Patent: October 14, 2014Assignee: Cara Therapeutics, Inc.Inventors: R. Paul Beckett, Richard Foster, Christelle Henault, Janet L. Ralbovsky, Carla M. Gauss, Gary G. Gustafson, Zhiyong Luo, Ann-Marie Campbell, Tatiana E. Shelekhin
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Patent number: 8859574Abstract: The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or analplastic lymphoma kinase (ALK).Type: GrantFiled: July 23, 2013Date of Patent: October 14, 2014Assignee: IRM LLCInventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Christian Cho-Hua Lee, Songchun Jiang, Kunyong Yang
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Publication number: 20140303139Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.Type: ApplicationFiled: August 31, 2012Publication date: October 9, 2014Inventors: Chiyou Ni, Laykea Tafesse, Jiangcho Yao, Mark Youngman, Minnie Park, Bin Shao
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Publication number: 20140303154Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: June 19, 2014Publication date: October 9, 2014Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Publication number: 20140303163Abstract: The present invention discloses use of compounds of formula (I) in preventing and treating inflammatory disorder.Type: ApplicationFiled: March 24, 2011Publication date: October 9, 2014Inventor: Ying Luo
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Publication number: 20140296201Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.Type: ApplicationFiled: June 16, 2014Publication date: October 2, 2014Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
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Patent number: 8846675Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.Type: GrantFiled: May 3, 2012Date of Patent: September 30, 2014Assignee: Cymabay Therapeutics, Inc.Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
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Patent number: 8846947Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: July 2, 2009Date of Patent: September 30, 2014Assignee: GlaxoSmithKline LLCInventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Publication number: 20140288067Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: Epizyme, Inc.Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
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Publication number: 20140288072Abstract: The present application relates to a series of substituted pyra-zolopyridin-6-amines having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. Wherein R, R1, R2, Ra, Raa, Rb and n are as defined herein. The present invention further relates to pharmaceutical compositions comprising compounds of formula (I). The compounds of this application are useful as CETP inhibitors for increasing HDL cholesterol and decreasing LDL cholesterol in a patient.Type: ApplicationFiled: September 27, 2012Publication date: September 25, 2014Applicant: DR. REDDY'S LABORATORIES, LTD.Inventors: Anima Boruah, Shanavas Alikunju
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Publication number: 20140288044Abstract: The invention relates to compounds, pharmaceutical compositions and medicaments comprising such compounds, and the use of these compounds, compositions, and medicaments in methods of treating diseases and disorders.Type: ApplicationFiled: April 12, 2012Publication date: September 25, 2014Applicant: Alzheimer's Institute of America, Inc.Inventors: Ryan Holcomb, Paul R. Sebahar, Kazuyuki Suzuki, Donald A. McLeod, David M. Dastrup, Christophe Hoarau, Robert J. Halter, Matthew Gregory Bursavich, Mark D. Shenderovich, Burt Richards, Paul L. Bartel
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Publication number: 20140288048Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
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Publication number: 20140288043Abstract: A first aspect of the invention relates to a compound of formula (1A) or (1B), or a pharmaceutically acceptable salt thereof, Wherein R1 is a group selected from alkyl, monocyclic heterocycloalkyl, bicyclic heterocycloalkyl and cycloalkyl, each of which is optionally substituted, and wherein X1, X2, X3 and X4 are as defined herein. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (1A) and (1B).Type: ApplicationFiled: March 19, 2013Publication date: September 25, 2014Applicant: Genentech, Inc.Inventors: Bryan Chan, Anthony Estrada, Daniel Shore, Zachary Sweeney
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Publication number: 20140271543Abstract: New pyridin-2(1H)-one derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: July 23, 2012Publication date: September 18, 2014Applicant: ALMIRALL, S.A.Inventors: Paul Robert Eastwood, Jordi Bach Taña, Lluis Miquel Pages Santacana
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Publication number: 20140275087Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: March 17, 2014Publication date: September 18, 2014Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
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Publication number: 20140275024Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
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Publication number: 20140275083Abstract: The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: NOVARTIS AGInventors: Thomas Raymond CAFERRO, Zhuoliang CHEN, Young Shin CHO, Abran Q. COSTALES, Julian Roy LEVELL, Gang LIU, James R. MANNING, Martin SENDZIK, Cynthia SHAFER, Michael David SHULTZ, James SUTTON, Yaping WANG, Qian ZHAO
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Publication number: 20140275003Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Applicant: NOVARTIS AGInventors: Paul A. Barsanti, Matthew Burger, Yan Lou, Gisele Nishiguchi, Valery Polyakov, Savithri Ramurthy, Alice Rico, Lina Setti, Aaron Smith, Benjamin Taft, Huw Tanner, Alan DiPesa, Naeem Yusuff
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Publication number: 20140275086Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: March 17, 2014Publication date: September 18, 2014Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins