Additional Hetero Ring Which Is Unsaturated Patents (Class 544/324)
  • Patent number: 10370361
    Abstract: The present disclosure relates to crystalline polymorph and amorphous forms of 2-methyl-2-(3-methyl-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-1H-pyrazol-1-yl)propanenitrile or solvates, tautomers, and pharmaceutically acceptable salts or cocrystals thereof, and processes for their preparation.
    Type: Grant
    Filed: November 20, 2018
    Date of Patent: August 6, 2019
    Assignee: Denali Therapeutics Inc.
    Inventors: Travis Remarchuk, Anantha Sudhakar
  • Patent number: 10023562
    Abstract: Compounds having the following formula: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R2 is a monocyclic heteroaryl group, and R1, R3, R4, R5 and R6 are as defined herein, are useful as kinase modulators, including IRAK-4 inhibition.
    Type: Grant
    Filed: April 6, 2017
    Date of Patent: July 17, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Rajeev S. Bhide, John V. Duncia, John Hynes, Satheesh K. Nair, William J. Pitts, Sreekantha R. Kumar, Daniel S. Gardner, Natesan Murugesan, Venkatram Reddy Paidi, Joseph B. Santella, Ramesh Sistla, Hong Wu
  • Patent number: 9993491
    Abstract: The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: June 12, 2018
    Assignee: SOCPRA—SCIENCES ET GÉNIE S.E.C.
    Inventors: Jerome Mulhbacher, Daniel Lafontaine, Francois Malouin, Marianne Allard, Eric Marsault
  • Patent number: 9926298
    Abstract: Heterocyclic compounds of Formula (I) shown herein. Also disclosed are pharmaceutical compositions containing the heterocyclic compounds and methods of using the heterocyclic compounds to mobilize hematopoietic stem cells and endothelial progenitor cells into the peripheral circulation. Further provided are methods for treating tissue injury, cancer, inflammatory disease, and autoimmune disease with the heterocyclic compounds.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: March 27, 2018
    Assignee: National Health Research Institutes
    Inventors: Kak-Shan Shia, Jiing-Jyh Jan, Lun Kelvin Tsou, Chiung-Tong Chen, Yu-Sheng Chao
  • Patent number: 9447095
    Abstract: The present invention relates to novel pyrimidine derivatives of formula (I) as inhibitors of the enzyme phosphodiesterase 10 (PDE-10), pharmaceutical compositions comprising an effective amount of these compounds and the use of the compounds for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by inhibition of the enzyme Phosphodiesterase 10 such as neurological, psychiatric, respiratory or metabolic diseases.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: September 20, 2016
    Assignee: PALOBIOFARMA S.L.
    Inventors: Juan Camacho Gómez, Julio Castro Palomino Laria
  • Patent number: 9428492
    Abstract: The present invention is directed to secondary alcohol substituted triazole 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: Grant
    Filed: November 11, 2013
    Date of Patent: August 30, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Christopher D. Cox, Vadim Y. Dudkin, Carol A. McVean, Thomas S. Reger, Justin T. Steen
  • Patent number: 9359348
    Abstract: The present invention is directed to substituted cyclopropyl imidazopyridine 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: Grant
    Filed: November 11, 2013
    Date of Patent: June 7, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Thomas S. Reger
  • Patent number: 9284302
    Abstract: The present invention is directed to substituted cyclobutyl benzimidazole 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: Grant
    Filed: November 11, 2013
    Date of Patent: March 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Casey C. McComas, Thomas S. Reger
  • Publication number: 20150126504
    Abstract: 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: Application
    Filed: January 12, 2015
    Publication date: May 7, 2015
    Applicant: 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
  • Patent number: 9018224
    Abstract: 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. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: 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
  • Publication number: 20150111883
    Abstract: 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: Application
    Filed: October 21, 2014
    Publication date: April 23, 2015
    Inventors: Jaekyoo Lee, Jang-Sik Choi, Hae-Jun Hwang, Ho-Juhn Song, Jung-Ho Kim, Se-Won Kim, Jong Sung Koh, Jaesang Lee, Tae-Im Lee, Yung-Geun Choi, Sung-Ho Park, In Yong Lee, Byung-Chul Suh, Paresh Devidas Salgaonkar, Dong-Sik Jung
  • Patent number: 9006243
    Abstract: HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R6 and R7 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 and R5 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; cyano; —S(?O)rR9; —NH—S(?O)2R9; —NHC(?O)H; —C(?O)NHNH2; —NHC(?O)R9; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is pyridyl, —C(?O)NR5aR5b; —CH(OR5c)R5d; —CH2—NR5eR5f; —CH?NOR5a; —CH2—O—C2-6alkenyl; —CH2—O—P(?O)(OR5g)2; —CH2—O—C(?O)—NH2; —C(?O)—R5d; X is —NR1—, —O—, —CH2—, —S—; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compou
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: April 14, 2015
    Assignee: Janssen R&D Ireland
    Inventors: Jerôme Emile Georges Guillemont, Céline Isabelle Mordant
  • Publication number: 20150099743
    Abstract: 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 disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Hui LI, Seiji NUKUI, Stephanie Anne SCALES, Min TENG, Chunfeng YIN
  • Publication number: 20150099875
    Abstract: The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Jean-Damien Charrier, Michael Edward O'Donnell
  • Publication number: 20150099770
    Abstract: The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof: (I) wherein the variable groups X, R1, R2, R3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer.
    Type: Application
    Filed: May 17, 2013
    Publication date: April 9, 2015
    Inventors: Seiji Hori, Futoshi Hasegawa, Daisuke Urabe, Hirotaka Kurebayashi
  • Publication number: 20150099749
    Abstract: This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno François Marie Delest
  • Publication number: 20150094298
    Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
    Type: Application
    Filed: December 5, 2014
    Publication date: April 2, 2015
    Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Yonghong Song, Qing Xu, Wolin Huang, Chandrasekar Venkataramani, Jack W. Rose, Anjali Pandey
  • Publication number: 20150094296
    Abstract: The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: March 27, 2013
    Publication date: April 2, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Tetsuya Tsukamoto, Yusuke Ohba, Takafumi Yukawa, Hiroyuki Nagamiya, Taku Kamei, Norihito Tokunaga, Morihisa Saitoh, Atsutoshi Okabe
  • Publication number: 20150080368
    Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Applicant: VERASTEM, INC.
    Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
  • Publication number: 20150065533
    Abstract: The present application relates to novel benzyl-substituted carbamates, 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, especially for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: November 3, 2011
    Publication date: March 5, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Niels Lindner, Frank Wunder, Volkhart Min-Jian Li
  • Patent number: 8962643
    Abstract: The invention encompasses compounds having formula I 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, are therapeutically useful.
    Type: Grant
    Filed: February 23, 2007
    Date of Patent: February 24, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Ankush Argade, Kin Tso, Sambaiah Thota, David Carroll, Arvinder Sran, Robin Cooper, Rajinder Singh, Somasekhar Bhamidipati, Vanessa Taylor, Esteban Masuda
  • Patent number: 8962622
    Abstract: Compounds of formula I modulate jnk and cdk: or a pharmaceutically acceptable salt thereof, where R, R1, R2, R3, and m are defined herein.
    Type: Grant
    Filed: September 7, 2007
    Date of Patent: February 24, 2015
    Assignee: Roche Palo Alto LLC
    Inventors: David Michael Goldstein, Levi Gong, Christophe Michoud, Wylie Solang Palmer, Achyutharao Sidduri
  • Publication number: 20150051238
    Abstract: Pyrazole compounds that are modulators of LRRK2, methods of making the compounds, and methods for using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 19, 2015
    Applicant: GENENTECH, INC.
    Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Bryan K. Chan, Mark Chambers, Huifen Chen, Anthony Estrada, Zachary Kevin Sweeney
  • Publication number: 20150051201
    Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3 and A 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: Application
    Filed: November 3, 2014
    Publication date: February 19, 2015
    Applicant: Genentech, Inc.
    Inventors: Charles Baker-Glenn, Bryan K. Chan, Jennafer Dotson, Anthony Estrada, Timothy Heffron, Joseph Lyssikatos, Zachary Sweeney
  • Patent number: 8957081
    Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: February 17, 2015
    Assignee: IRM LLC
    Inventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
  • Patent number: 8957068
    Abstract: 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: Grant
    Filed: September 26, 2012
    Date of Patent: February 17, 2015
    Assignee: Novartis AG
    Inventors: 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
  • Publication number: 20150045339
    Abstract: The object is to provide an Fms-like tyrosine kinase 3 (FLT3) inhibitor useful as a therapeutic agent for acute myeloid leukemia (AML). A novel nitrogen-containing heterocyclic compound represented by the general formula [1] or a salt thereof is provided. The compound or a salt thereof of the present invention can be used as an active ingredient of a pharmaceutical composition for a treatment of a disease or condition relating to FLT3, such as acute myeloid leukemia (AML) and acute promyelocytic leukemia (APL).
    Type: Application
    Filed: October 16, 2014
    Publication date: February 12, 2015
    Applicant: FUJIFILM CORPORATION
    Inventors: Masaru TAKASAKI, Toshiaki TSUJINO, Shintarou TANABE, Megumi OOKUBO, Kimihiko SATO, Atsushi HIRAI, Daisuke TERADA, Shinsuke INUKI, Shinsuke MIZUMOTO
  • Publication number: 20150038481
    Abstract: Described are compounds of Formula I or Formula II: wherein: ring A is a 5- or 6-membered heteroaryl group; dashed lines are optional double bonds; X is N or O; Y is a carbon atom or an S or N heteroatom in ring A in any suitable location; and substituents are as given herein. Compositions containing the same and methods of using the same in treating cancers such as acute lymphoblastic leukemia are also described.
    Type: Application
    Filed: May 21, 2013
    Publication date: February 5, 2015
    Inventors: Xiaodong Wang, Weihe Zhang, Dmitri Kireev, Dehui Zhang, Andrew Mclver
  • Publication number: 20150038460
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Application
    Filed: October 16, 2014
    Publication date: February 5, 2015
    Applicant: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A.G.N. Montalbetti
  • Publication number: 20150025095
    Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit RSV infection and/or replication; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: February 15, 2013
    Publication date: January 22, 2015
    Inventors: Tatyana Dekhtyar, Arthur Gomtsyan, M-Akhteruzzaman Molla, Anil Vasudevan, Teresa (lok Chan) Ng, Mikhail Shafeev
  • Publication number: 20150023930
    Abstract: Described herein are aminoquinoline and aminoacridine based hybrids, pharmaceutical compositions and medicaments that include such aminoquinoline and aminoacridine based hybrids, and methods of using such compounds for diagnosing and/or treating infections, neurodegerative diseases or disorders, inflammation, inflammation associated diseases and disorders, and/or diseases or disorders that are treatable with dopamine agonists such as the restless leg syndrome.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 22, 2015
    Applicant: The McLean Hospital Corporation
    Inventors: Diwan S. Rawat, Sunny Manohar, Ummadisetty Chinna Rajesh, Deepak Kumar, Anuj Thakur, Mohit Tripathi, Panyala Linga Reddy, Shamseer Kulangara Kandi, Satyapavan Vardhineni, Kwang-Soo Kim, Chun-Hyung Kim
  • Patent number: 8927547
    Abstract: The invention provides novel pyrimidine derivatives of formula I, to methods of preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for using such compounds in treatment of diseases including cancer; wherein R1, R2, R3, R4, R5, L, A, D, E, Z, and Y are as defined in the specification.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: January 6, 2015
    Assignee: Noviga Research AB
    Inventors: Marita Högberg, Tommy Johansson, Emma Dahlstedt, Olof Smitt
  • Publication number: 20150005302
    Abstract: The present invention directs a compound represented by formula (I).
    Type: Application
    Filed: December 21, 2012
    Publication date: January 1, 2015
    Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Joel R. Walker, Raymond Huntley
  • Publication number: 20150005297
    Abstract: 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: Application
    Filed: September 12, 2014
    Publication date: January 1, 2015
    Applicant: 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
  • Publication number: 20150005293
    Abstract: 5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: September 9, 2014
    Publication date: January 1, 2015
    Inventors: Hongbin Li, Jun Yuan, Rajagopal Bakthavatchalam, Kevin J. Hodgetts, Qin Guo, Scott M. Capitosti, Jianmin Mao, David J. Wustrow
  • Publication number: 20150005281
    Abstract: The present invention relates to compounds of formula (I) wherein X, R, Y0, T0A, T0B 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 and their use as medicaments.
    Type: Application
    Filed: December 20, 2012
    Publication date: January 1, 2015
    Inventors: Andrew Hobson, Glynn Addison, Nigel Ramsden, John Harrison
  • Publication number: 20140378488
    Abstract: Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.
    Type: Application
    Filed: September 5, 2011
    Publication date: December 25, 2014
    Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.
    Inventors: Yili Ding, Xuan Yang, Qingyan Yan, Hua Bai, Lifeng Cai, Kenneth Smith, Jian Chai
  • Patent number: 8916554
    Abstract: 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: Grant
    Filed: July 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Publication number: 20140363588
    Abstract: 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: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Aiko YAMAMOTO, Satoshi TANAKA, Teruki NIORI, Masato NAGURA, Masaki NORO, Aiko YOSHIDA, Nobutaka FUKAGAWA, Yasukazu KUWAYAMA
  • Publication number: 20140357614
    Abstract: 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: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    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, Xioahu Zhang
  • Patent number: 8901146
    Abstract: 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: Grant
    Filed: December 22, 2010
    Date of Patent: December 2, 2014
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Elena Carceller Gonzalez, Marina Virgili Bernado, Robert Soliva Soliva, Carles Ferrer Costa
  • Patent number: 8895575
    Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.
    Type: Grant
    Filed: October 2, 2013
    Date of Patent: November 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
  • Publication number: 20140343006
    Abstract: 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: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Inventors: 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
  • Publication number: 20140329842
    Abstract: 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: Application
    Filed: March 7, 2014
    Publication date: November 6, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Sacha Holland, Rao Kolluri, Salvador Alvarez, Matthew Duncton, Rajinder Singh, Jing Zhang, Esteban Masuda
  • Publication number: 20140330007
    Abstract: 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: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Applicant: 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
  • Publication number: 20140328805
    Abstract: 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: Application
    Filed: May 1, 2014
    Publication date: November 6, 2014
    Applicant: GENENTECH, INC.
    Inventors: Anthony Estrada, Alan G. Olivero, Snahel Patel, Michael Siu
  • Publication number: 20140323418
    Abstract: 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: Application
    Filed: November 23, 2012
    Publication date: October 30, 2014
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Zhaozhong J. Jia, Brian Kane, Qing Xu, Shawn M. Bauer, Yonghong Song, Anjali Pandey, Ryan Dick
  • Publication number: 20140323486
    Abstract: 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: Application
    Filed: December 21, 2012
    Publication date: October 30, 2014
    Inventors: Edward Malcolm Tyndall, Lloyd George Czaplewski, Colin William Gordon Fishwick, Andrew Ian Yule, Jeffrey Peter Mitchell, Kelly Helen Anderson, Gary Robert William Pitt
  • Publication number: 20140323464
    Abstract: Provided herein are kinase inhibiting compounds and methods of using the same.
    Type: Application
    Filed: May 16, 2012
    Publication date: October 30, 2014
    Inventors: John William Taunton, JR., Kenneth Albert Brameld, David Michael Goldstein, Jesse Mcfarland, Shyam Krishnan, Jonathan Choy
  • Patent number: 8871778
    Abstract: 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: Grant
    Filed: January 18, 2013
    Date of Patent: October 28, 2014
    Assignees: 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