Additional Hetero Ring Which Is Unsaturated Patents (Class 544/324)
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Publication number: 20140357614Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: ApplicationFiled: August 14, 2014Publication date: December 4, 2014Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xioahu Zhang
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Patent number: 8901146Abstract: Aminoalkylpyrimidine derivatives of formula I, wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.Type: GrantFiled: December 22, 2010Date of Patent: December 2, 2014Assignee: Medicis Pharmaceutical CorporationInventors: Elena Carceller Gonzalez, Marina Virgili Bernado, Robert Soliva Soliva, Carles Ferrer Costa
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Patent number: 8895575Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: GrantFiled: October 2, 2013Date of Patent: November 25, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
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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: 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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Publication number: 20140330007Abstract: 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: July 16, 2014Publication date: November 6, 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: 20140329842Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: March 7, 2014Publication date: November 6, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Sacha Holland, Rao Kolluri, Salvador Alvarez, Matthew Duncton, Rajinder Singh, Jing Zhang, Esteban Masuda
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Publication number: 20140323418Abstract: Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.Type: ApplicationFiled: November 23, 2012Publication date: October 30, 2014Applicant: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Brian Kane, Qing Xu, Shawn M. Bauer, Yonghong Song, Anjali Pandey, Ryan Dick
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Publication number: 20140323486Abstract: The present invention provides a compound of the following formula, racemates, enantiomers and salts thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.Type: ApplicationFiled: December 21, 2012Publication date: October 30, 2014Inventors: Edward Malcolm Tyndall, Lloyd George Czaplewski, Colin William Gordon Fishwick, Andrew Ian Yule, Jeffrey Peter Mitchell, Kelly Helen Anderson, Gary Robert William Pitt
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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: 8871778Abstract: Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).Type: GrantFiled: January 18, 2013Date of Patent: October 28, 2014Assignees: Genosco, Oscotec, Inc.Inventors: Jang-Sik Choi, Hae-Jun Hwang, Eunho Lee, Jaekyoo Lee, Ho-Juhn Song, Se Won Kim, Jung-Ho Kim, Jong Sung Koh, Tae-im Lee, Yung-geun Choi, Ik-hwan Han, Jaesang Lee, In Yong Lee, Dong Sik Jung
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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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Patent number: 8846908Abstract: The present disclosure relates to 2,4-pyrimidinediamines substituted with tricyclic carbamates and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, such as JAK2 or JAK3, is therapeutically useful.Type: GrantFiled: September 23, 2009Date of Patent: September 30, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Somasekhar Bhamidipati, Vadim Markovtsov
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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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Patent number: 8841287Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: June 11, 2009Date of Patent: September 23, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
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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: 20140275055Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Rajinder Singh, Matthew Duncton, Jing Zhang, Salvador Alvarez, Kin Tso, Sacha Holland, Rose Yen, Rao Kolluri, Thilo Heckrodt, Yan Chen, Esteban Masuda, Hui Li, Donald G. Payan
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Publication number: 20140273214Abstract: The present invention relates compounds for stabilizing cells and methods of their use.Type: ApplicationFiled: February 24, 2014Publication date: September 18, 2014Applicant: The Scripps Research InstituteInventors: Yue Xu, Sheng Ding
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Publication number: 20140275135Abstract: Solid forms of chemical compounds 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 PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, solid forms thereof, and pharmaceutical compositions thereof.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Daniel G. GENOV, Louis GRENIER, Andrew B. HAGUE, Alexander Redvers EBERLIN, Ludovic Sylvain Marc RENOU, Susana DEL RIO GANCEDO
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Patent number: 8835430Abstract: 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: GrantFiled: September 26, 2013Date of Patent: September 16, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
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Patent number: 8835420Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.Type: GrantFiled: July 8, 2013Date of Patent: September 16, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Edcon Chang, Wolfgang Reinhard Ludwig Notz, Michael B. Wallace
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Patent number: 8835432Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: GrantFiled: March 21, 2014Date of Patent: September 16, 2014Assignee: Amgen Inc.Inventors: Minna Bui, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Brian Lucas
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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: 20140249137Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis.Type: ApplicationFiled: October 31, 2013Publication date: September 4, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis, Harmon J. Zuccola
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Publication number: 20140249134Abstract: The present invention is directed to substituted triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 3, 2012Publication date: September 4, 2014Inventors: Christopher D. Cox, Vadim Y. Dudkin, June J. Kim, Scott D. Kuduk, Carol A. McVean, Thomas Reger, Justin T. Sheen, Thomas Steele
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Publication number: 20140242027Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.Type: ApplicationFiled: February 18, 2011Publication date: August 28, 2014Applicants: Southern Research Institute, Merck Sharp & Dohne Corp.Inventors: Ashok Arasappan, F. George Njoroge, Cecil D. Kwong, Subramaniam Ananthan, Frank Bennett, Francisco Velazquez, Vinay Girijavallabhan, Yuhua Huang, Hollis S. Kezer, Joseph Maddry, Robert C. REynold, Abhijit Roychowdhury, Anita T. Fowler, John A. Secrist, III, Ling Tong, Seong Heon Kim, Malcolm MacCoss, Srikanth Venkatraman, vishal Verma
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Patent number: 8815848Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.Type: GrantFiled: January 25, 2013Date of Patent: August 26, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
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Patent number: 8815882Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: GrantFiled: November 9, 2011Date of Patent: August 26, 2014Assignee: Genentech, Inc.Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Mark Chambers, Bryan K. Chan, Huifen Chen, Anthony Estrada, Zachary Kevin Sweeney
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Patent number: 8815877Abstract: Compounds having the formula I wherein A, R1a, R1b, R2, R3, R4, R5, R6, R7, R8, Ra, Rb, X1, X2, X3 and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: GrantFiled: December 21, 2012Date of Patent: August 26, 2014Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, James Crawford, Wendy Lee, Simon Mathieu, Joachim Rudolph
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Patent number: 8815885Abstract: Disclosed herein are, inter alia, compositions for modulating Ire1, Src, or Abl, methods for identifying modulating activity in test compounds, and methods for treating diseases caused by the activity or inactivity of Ire1, Src, or Abl.Type: GrantFiled: September 15, 2009Date of Patent: August 26, 2014Assignee: The Regents of the University of CaliforniaInventors: Peter Walter, Alexei Korennykh, Kevan M. Shokat, Chao Zhang, Janet Finer-Moore, Robert Stroud, Pascal Egea, Andrei Korostelev, Arvin Dar, Sebastian Bernales
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Publication number: 20140235620Abstract: The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined 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: September 26, 2012Publication date: August 21, 2014Applicant: NOVARTIS AGInventors: Thomas Raymond Caferro, Young Shin Cho, Abran Q. Costales, Huangshu Lei, Francois Lenoir, Julian Roy Levell, Gang Liu, Mark G. Palermo, Keith Bruce Pfister, Martin Sendzik, Cynthia Shafer, Michael David Shultz, Troy Smith, James Clifford Sutton, Bakary-Barry Toure, Fan Yang, Qian Zhao
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Publication number: 20140228322Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: February 7, 2014Publication date: August 14, 2014Applicant: Celgene Avilomics Research, Inc.Inventors: Nadia Haq, Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh, Zhendong Zhu
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Publication number: 20140227289Abstract: The present invention relates to a method of treating or preventing insulin resistance syndrome in an animal body by administering an inhibitor of protein kinase RNA-like endoplasmic reticulum kinase (PERK) gene, or a functional variant thereof, or an inhibitor of PERK protein or a functional variant thereof or a method of reducing activity of transcription factors of the FOXO family (Foxo 1, 3a, 4 and 6) by administering an inhibitor of protein kinase RNA-like endoplasmic reticulum kinase (PERK) gene, or a functional variant thereof, or an inhibitor of PERK protein or a functional variant thereof. The present invention also relates to different compounds and methods for using PERK gene or PERK protein.Type: ApplicationFiled: May 14, 2012Publication date: August 14, 2014Inventors: Stephen Michael Cohen, Wei Zhang
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Publication number: 20140221352Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: April 10, 2014Publication date: August 7, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
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Publication number: 20140221336Abstract: 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: February 5, 2014Publication date: August 7, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Francesco Salituro, Albert Pierce, Alex Aronov, Gabriel Martinez-Botella, Jian Wang, Luc Farmer, Mark Ledeboer, Tiansheng Wang, Randy Bethiel, Brian Ledford, Emilie Porter Huck
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Patent number: 8796296Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: GrantFiled: November 28, 2012Date of Patent: August 5, 2014Assignee: Genentech, Inc.Inventors: Charles Baker-Glenn, Mark Chambers, Bryan K. Chan, Anthony Estrada, Zachary Kevin Sweeney
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Publication number: 20140213574Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: April 16, 2014Publication date: July 31, 2014Applicant: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Patent number: 8785444Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: August 2, 2012Date of Patent: July 22, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Julian Golec, Christopher Davis, Daniel Robinson, John Studley
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Patent number: 8785630Abstract: The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.Type: GrantFiled: February 6, 2013Date of Patent: July 22, 2014Assignee: Vestaron CorporationInventors: Robert M. Kennedy, Bruce A. Steinbaugh
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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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Publication number: 20140187780Abstract: The present invention discloses compounds of formula I, II or X, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.Type: ApplicationFiled: December 24, 2013Publication date: July 3, 2014Applicant: Enanta Pharmaceuticals, Inc.Inventors: In Jong Kim, Tongzhu Liu, Jiang Long, Guoqiang Wang, Yao-Ling Qiu, Heejin Kim, Yanchun Wang, Ly Tam Phan, Yat Sun Or
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Publication number: 20140187772Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: ApplicationFiled: December 24, 2013Publication date: July 3, 2014Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Patent number: 8765939Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: August 16, 2012Date of Patent: July 1, 2014Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.Inventors: Nicholas J. Bennett, Thomas McInally, Tobias Mochel, Stephen Thom, Anna-Karin Tidén
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Publication number: 20140179664Abstract: The present invention relates to compounds of formula (I) wherein X1 to X5, Z1 to Z3, Y0, RY1, RY2 and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.Type: ApplicationFiled: July 24, 2012Publication date: June 26, 2014Applicant: Cellzome LimitedInventors: Jay Freeman, Valerie Reader, Glynn Addison, Nigel Ramsden, Jane Elizabeth Scanlon, Richard John Harrison
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Patent number: 8759365Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: GrantFiled: December 1, 2008Date of Patent: June 24, 2014Assignee: Novartis AGInventors: Muneto Mogi, Toshio Kawanami, Ken Yamada, Kayo Yasoshima, Hidetomo Imase, Takahiro Miyake, Osamu Ohmori
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Patent number: 8748412Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.Type: GrantFiled: February 2, 2011Date of Patent: June 10, 2014Assignee: Argusina Bioscience Inc.Inventors: Jiayu Liao, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
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Patent number: 8722884Abstract: The present invention relates to salts, solvates and substoichiometric solvates of N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide. The invention also provides pharmaceutical compositions comprising such complexes, as well as methods of treating abnormal cell growth by administering the complexes of the invention.Type: GrantFiled: November 20, 2006Date of Patent: May 13, 2014Assignee: Verastem, Inc.Inventors: John Charles Kath, Michael Joseph Luzzio, Susan La Greca, Nandini Chaturbhai Patel
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Publication number: 20140128387Abstract: Disclosed herein are protein kinase inhibitors, more particularly novel pyrimidine derivatives and pharmaceutical compositions thereof, and method of use thereof.Type: ApplicationFiled: November 5, 2013Publication date: May 8, 2014Applicants: SHANGHAI iNSTITUTE OF MATERIA MEDICA ACADEMY OF SCIENCES, SHANGHAI FOCHON PHARMACEUTICAL CO., LTD.Inventors: Weibo WANG, Meiyu Geng, Jian Ding, Xingdong Zhao, Jing Ai, Qiang Tian, Xia Peng, Weipeng Zhang, Hongbin Liu, Haohan Tan, Ling Chen
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Patent number: 8716290Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: GrantFiled: April 4, 2013Date of Patent: May 6, 2014Assignee: Amgen Inc.Inventors: Minna Bui, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Brian Lucas
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Patent number: 8710223Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: July 21, 2011Date of Patent: April 29, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Sacha Holland, Rao Kolluri, Salvador Alvarez, Matthew Duncton, Rajinder Singh, Jing Zhang, Esteban Masuda