Ring Nitrogen Is Shared By The Two Cyclos Patents (Class 544/281)
  • Patent number: 11339165
    Abstract: The invention concerns compounds having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection. Formula (Ia).
    Type: Grant
    Filed: November 28, 2018
    Date of Patent: May 24, 2022
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: David Francis Alain Lançois, Jérôme Émile Georges Guillemont, Pierre Jean-Marie Bernard Raboisson, Dirk André Emmy Roymans, Peter Rigaux, Antoine Benjamin Michaut, Guillaume Jean Maurice Mercey
  • Patent number: 11155557
    Abstract: Compounds of Formula (IA), or a pharmaceutically acceptable salt thereof, and methods of use as Janus kinase inhibitors are described herein.
    Type: Grant
    Filed: June 25, 2019
    Date of Patent: October 26, 2021
    Assignee: Genentech, Inc.
    Inventors: F. Anthony Romero, Mark Zak, Guiling Zhao, Paul Gibbons, Wei Li, Yun-Xing Cheng, Po-Wai Yuen, Limin Cheng
  • Patent number: 11130758
    Abstract: Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
    Type: Grant
    Filed: April 10, 2020
    Date of Patent: September 28, 2021
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Roch Boivin, Eric Carlson, Atsushi Endo, Hans Hansen, Lynn D. Hawkins, Sally Ishizaka, Matthew Mackey, Sridhar Narayan, Takashi Satoh, Shawn Schiller
  • Patent number: 11059827
    Abstract: This invention relates to inhibitors of NTRK that are active against wild-type NTRK and its resistant mutants.
    Type: Grant
    Filed: July 31, 2019
    Date of Patent: July 13, 2021
    Assignee: Blueprint Medicines Corporation
    Inventors: Steven Mark Wenglowsky, Chandrasekhar V. Miduturu, Neil Bifulco, Joseph L. Kim
  • Patent number: 11001590
    Abstract: The present invention covers Pyrazolopyrimidine compounds of general formula (I): in which n, o, X, Y, R, Q, R1, R2, R3 and R4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: January 29, 2020
    Date of Patent: May 11, 2021
    Assignee: BAYER ANIMAL HEALTH GMBH
    Inventors: Hans-Georg Schwarz, Adeline Köhler, Nils Griebenow, Wei Zhuang
  • Patent number: 10934301
    Abstract: The present invention covers Pyrazolopyrimidine compounds of general formula (I): in which n, o, X, Y, R, Q, R1, R2, R3 and R4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: January 29, 2020
    Date of Patent: March 2, 2021
    Assignee: BAYER ANIMAL HEALTH GMBH
    Inventors: Ulrich Görgens, Claudia Welz, Daniel Kulke, Claudia Böhm
  • Patent number: 10676479
    Abstract: A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R3, R4, R6, and R7 are as defined herein.
    Type: Grant
    Filed: June 9, 2017
    Date of Patent: June 9, 2020
    Assignee: Novartis AG
    Inventors: Ho Man Chan, Xingnian Fu, Xiang-Ju Justin Gu, Ying Huang, Ling Li, Yuan Mi, Wei Qi, Martin Sendzik, Yongfeng Sun, Long Wang, Zhengtian Yu, Hailong Zhang, Ji Yue Zhang, Man Zhang, Qiong Zhang, Kehao Zhao
  • Patent number: 10640500
    Abstract: Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
    Type: Grant
    Filed: December 14, 2017
    Date of Patent: May 5, 2020
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Roch Boivin, Eric Carlson, Atsushi Endo, Hans Hansen, Lynn D. Hawkins, Sally Ishizaka, Matthew Mackey, Sridhar Narayan, Takashi Satoh, Shawn Schiller
  • Patent number: 10617690
    Abstract: The present invention discloses a series of JAK inhibitors, and particularly discloses a compound of formula (I) or a pharmaceutically acceptable salt thereof and the use thereof in preparation of drugs for treating diseases related to JAK.
    Type: Grant
    Filed: January 19, 2016
    Date of Patent: April 14, 2020
    Assignee: WUXI FORTUNE PHARMACEUTICAL CO., LTD
    Inventors: Hao Wu, Weiwei Mao, Lili Fan, Charles Z. Ding, Shuhui Chen, Fei Wang, Guoping Hu, Jian Li
  • Patent number: 10604525
    Abstract: The present invention covers Pyrazolopyrimidine compounds of general formula (I), in which n, o, X, Y, R, Q, R1, R2, R3 and R4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: April 10, 2017
    Date of Patent: March 31, 2020
    Assignee: BAYAL ANIMAL HEALTH GMBH
    Inventors: Adeline Köhler, Claudia Welz, Kirsten Börngen, Daniel Kulke, Thomas Ilg, Johannes Köbberling, Walter Hübsch, Hans-Georg Schwarz, Ulrich Görgens, Ulrich Ebbinghaus-Kintscher, Maike Hink, Dirk Nennstiel, Klaus Raming, Martin Adamczewski, Claudia Böhm, Nils Griebenow, Wei Zhuang
  • Patent number: 10570139
    Abstract: The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
    Type: Grant
    Filed: May 3, 2018
    Date of Patent: February 25, 2020
    Assignee: BEIGENE SWITZERLAND GMBH
    Inventors: Zhiwei Wang, Yunhang Guo
  • Patent number: 10414772
    Abstract: Certain pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds that inhibit cycline dependent kinase (CDK) (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.) are disclosed. Pharmaceutical compositions comprising these compounds, and the use of these compounds and compositions to inhibit CDK; to treat disorders associated with CDK such as those arising from an inappropriate activity, mutation, overexpression, or upstream pathway activation of CDK; or disorders that are ameliorated by the inhibition of CDK; proliferative disorders; cancer; viral infections; neurodegenerative disorders; ischaemia; renal diseases; and cardiovascular disorders are also disclosed. Optionally, the treatment further comprises simultaneous or sequential treatment with a further active agent, e.g., an aromatase inhibitor, an anti-estrogen, a Her2 blocker, a cytotoxic chemotherapeutic agent, etc.
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: September 17, 2019
    Assignees: Imperial Innovations Limited, Emory University, Cancer Research Technology Limited
    Inventors: Alexander Bondke, Sebastian Kroll, Anthony Barrett, Matthew Fuchter, Brian Slafer, Simak Ali, Charles Coombes, James Patrick Snyder
  • Patent number: 10307426
    Abstract: Compounds and salts thereof that are useful as JAK kinse inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
    Type: Grant
    Filed: May 21, 2018
    Date of Patent: June 4, 2019
    Assignee: Genentech, Inc.
    Inventors: Mark Zak, F. Anthony Romero, Yun-Xing Cheng
  • Patent number: 10233191
    Abstract: The invention relates to fused piperidine amides useful as inhibitors of ion channels for the treatment of pain. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: March 19, 2019
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Paul Deninno, Corey Anderson, Erica Lynn Conroy, Bryan A. Frieman, Peter Diederik Jan Grootenhuis, Sara Sabina Hadida-Ruah, Dennis James Hurley, Fabrice Jean Denis Pierre, Alina Silina, Johnny Uy, Jinglan Zhou
  • Patent number: 10227344
    Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. For Formula (I) compounds R1, R2, R3, Ar and Z are as defined in the specification. The inventive Formula (I) compounds are inhibitors of CK2 and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer, inflammation and immunological disorders.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: March 12, 2019
    Assignee: Polaris Pharmaceuticals, Inc.
    Inventors: Stephen E. Webber, Xueliang Tao, Elena Brin
  • Patent number: 10005782
    Abstract: The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: June 26, 2018
    Assignee: BEIGENE, LTD.
    Inventors: Zhiwei Wang, Yunhang Guo
  • Patent number: 9815842
    Abstract: The present invention describes new pyrazolo-pyrimidine derivatives which are generally interacting with MALT1 proteolytic and/or autoproteolytic activity, and in particular which may inhibit said activity. The present invention further describes the synthesis of said new pyrazolo-pyrimidine derivatives, their use as a medicament, especially by interacting with MALT1 proteolytic and/or autoproteolytic activity.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: November 14, 2017
    Assignee: Novartis AG
    Inventors: Carole Pissot Soldermann, Jean Quancard, Achim Schlapbach, Oliver Simic, Marina Tintelnot-Blomley, Thomas Zoller
  • Patent number: 9682982
    Abstract: The adaptor associated kinase 1 (AAK1) inhibitor 3-methyloxetan-3-yl-4-(3-(2-methoxypyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine-1-carboxylate: and pharmaceutically acceptable salts and solid forms thereof are disclosed. Compositions comprising the compound and methods of their use to treat, manage and/or prevent diseases and disorders mediated by mediated by AAK1 activity are also disclosed.
    Type: Grant
    Filed: March 16, 2015
    Date of Patent: June 20, 2017
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Yingzhi Bi, Godwin Kumi
  • Patent number: 9604984
    Abstract: Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.
    Type: Grant
    Filed: April 26, 2016
    Date of Patent: March 28, 2017
    Assignee: Genentech, Inc.
    Inventors: Mark Edward Zak, Nicholas Charles Ray, Simon Charles Goodacre, Rohan Mendonca, Terry Kellar, Yun-Xing Cheng, Wei Li, Po-Wei Yuen
  • Patent number: 9458161
    Abstract: Embodiments of the present invention relates to compounds of the following formula: as well as compositions, methods of imaging and methods of treating subjects comprising the use of the compound, wherein the variables are defined herein.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: October 4, 2016
    Assignee: Vanderblit University
    Inventors: H. Charles Manning, Jason R. Buck, Dewei Tang
  • Patent number: 9447099
    Abstract: The present invention provides methods for preparing 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine (compound A), which is useful for the treatment of depression and other CNS disorders. The present methods are useful for preparing compound A on large scale in manufacturing facilities.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: September 20, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephan Bachmann, Daniel Bailey, Jodie Brice, Miall Cedilote, Zhiming Dong, Stefan Hildbrand, Doreen Miller, Paul Spurr, Amit Srivastava, Juergen Wichmann, Thomas Woltering, Jason Yang, Pingsheng Zhang
  • Patent number: 9365827
    Abstract: Methods and composition for the production of cardiomyocytes from differentiation of pluripotent stem cells are provided. For example, in certain aspects methods including differentiating pluripotent stem cells in a large volume of suspension culture in the presence of ROCK inhibitors are described. In further aspects, methods for differentiation of stem cells into cardiomyocytes that overcome variability between different stem cell clones and different batch of culture medium are provided.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: June 14, 2016
    Assignee: Cellular Dynamics International, Inc.
    Inventors: Casey Stankewicz, Matt Riley, Nathaniel Beardsley, Wen Bo Wang, Peter Fuhrken, Steven Kattman
  • Patent number: 9238653
    Abstract: Inhibitors of parasitic dihydroorotate dehydrogenase enzyme (DHOD) are candidate therapeutics for treating malaria. Illustrative of such therapeutic agents include the compound: and a triazolopyrimidine class of compounds that conform to Formula IX: and their solvates, stereoisomers, tautomers and pharmaceutically acceptable salts.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: January 19, 2016
    Assignees: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM, MMV MEDICINES FOR MALARIA VENTURE, UNIVERSITY OF WASHINGTON
    Inventors: Pradipsinh K. Rathod, David Floyd, Jeremy Burrows, Alka Marwaha, Ramesh Gujjar, Jose Coteron-Lopez, Margaret Phillips, Susan A. Charman, David Matthews
  • Patent number: 9040694
    Abstract: The presently-disclosed subject matter relates to compounds of the formula: and methods for use thereof. The presently-disclosed subject matter relates methods of selectively differentiating a stem cell, and methods of screening for compounds useful for enhancing terminal differentiation of committed cardiac progenitor cells.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: May 26, 2015
    Assignee: Vanderbilt University
    Inventors: Charles C. Hong, Corey R. Hopkins, Antonis K. Hatzopoulos, Craig W. Lindsley, Jijun Hao
  • Patent number: 9034882
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: May 19, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Annapurna Pendri, David R. Langley, Samuel Gerritz, Guo Li, Weixu Zhai, Stanley D'Andrea, Manoj Patel, B. Narasimhulu Naidu, Kevin Peese, Zhongyu Wang
  • Publication number: 20150133429
    Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 14, 2015
    Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
  • Patent number: 9029377
    Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Publication number: 20150126530
    Abstract: The present invention relates to novel substituted imidazo[1,2-a]pyrimidine compounds of formula (I), their pharmaceutically acceptable salts, and their isomers, stereoisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further” relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals. (Formula I).
    Type: Application
    Filed: October 15, 2012
    Publication date: May 7, 2015
    Applicant: Torrent Pharmaceuticals Limited
    Inventors: Chaitanya Dutt, Vijay Chauthaiwale, Ramesh Chandra Gupta, Sameer Ghalsasi, Davinder Tuli, Shailesh Deshpande, Anita Chaudhari, Shitalkumar Zambad
  • Publication number: 20150126506
    Abstract: 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 PI3 kinase activity, are described herein.
    Type: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Inventors: 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
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Patent number: 9023844
    Abstract: Heterocyclylpyri(mi)dinylpyrazole of the formula (I) in which R1 to R5, X1, U, Q, W, Y, n, a, b have the meanings given in the description, and agrochemically active salts, to their use and to methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants and for reducing mycotoxins in plants and parts of the plants, to processes for preparing such compounds and compositions and treated seed and also to their use for controlling phytopathogenic harmful fungi in agriculture, horticulture, forestry, in animal husbandry, in the protection of materials, in the domestic and hygiene field and for the reduction of mycotoxins in plants and parts of the plants.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: May 5, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stefan Hillebrand, Amos Mattes, Alexander Sudau, Pierre Wasnaire, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann, Haruko Sawada, Philippe Desbordes, Anne-Sophie Rebstock, Stéphane Brunet, Hélène Lachaise, Philippe Rinolfi
  • Publication number: 20150119380
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
    Type: Application
    Filed: December 28, 2012
    Publication date: April 30, 2015
    Inventors: Matthew G. Woll, Guangming Chen, Soongyu Choi, Amal Dakka, Song Huang, Gary Mitchell Karp, Chang-Sun Lee, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Sergey Paushkin, Hongyan Qi, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Emmanuel Pinard, Hasane Ratni
  • Publication number: 20150111874
    Abstract: 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 PI3 kinase activity, are described herein.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 23, 2015
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Martin R. TREMBLAY
  • Patent number: 9012042
    Abstract: A condensed-cyclic compound represented by Formula 1 below, an organic light-emitting device including the same, and a flat panel display apparatus including the organic light-emitting device: X1, Ar1, Ar2, Ar3, Ar4, Ar5, Ar6, Ar7, Ar8, Ar9, Ar10, Ar11, and Ar12 being described in the detailed description of the invention. The organic light-emitting device including an organic layer including the compound above has low driving voltage and high emission efficiency.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: April 21, 2015
    Assignee: Samsung Display Co., Ltd.
    Inventors: Hee-Yeon Kim, Seung-Gak Yang, Jeoung-In Yi, Jae-Yong Lee
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Publication number: 20150105374
    Abstract: The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.
    Type: Application
    Filed: September 19, 2014
    Publication date: April 16, 2015
    Inventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Nils GRIEBENOW, Dieter LANG, Frank WUNDER, Walter HÜBSCH, Niels LINDNER, Alexandros VAKALOPOULOS, Adrian TERSTEEGEN
  • Patent number: 9006235
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: April 14, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Zhizhen Barbara Zheng, Stanley D'Andrea, David R. Langley, B. Narasimhulu Naidu
  • Patent number: 8999998
    Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: April 7, 2015
    Assignee: Genentech, Inc.
    Inventors: Paul Gibbons, Emily Hanan, Wendy Liu, Joseph P. Lyssikatos, Steven R. Magnuson, Rohan Mendonca, Richard Pastor, Thomas E. Rawson, Michael Siu, Mark Zak, Aihe Zhou, Bing-Yan Zhu
  • Publication number: 20150094275
    Abstract: The present invention provides novel heteroaryl compounds 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: Application
    Filed: November 13, 2014
    Publication date: April 2, 2015
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. GRAY, Jianming ZHANG, Barun OKRAM, Xianming DENG, Jae Won CHANG, Amy WOJCIECHOWSKI
  • Publication number: 20150080372
    Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line.
    Type: Application
    Filed: October 14, 2014
    Publication date: March 19, 2015
    Inventors: Prabha N. Ibrahim, Guoxian Wu, Jack Lin, Wayne Spevak, Hanna Cho, Todd Ewing, Chao Zhang
  • Patent number: 8980878
    Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Grant
    Filed: April 17, 2013
    Date of Patent: March 17, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Dustin Siegel, David Sperandio, Hai Yang, Michael Sangi, Jay P. Parrish, Hon Chung Hui
  • Patent number: 8975264
    Abstract: Disclosed is a novel compound acting as a cannabinoid receptor 1 inhibitor, the compound being a pyrazolo[1,5-a]pyrimidine derivative, a prodrug thereof, an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof. The novel compound or the like is useful for preventing or treating diseases mediated by the cannabinoid receptor-1.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: March 10, 2015
    Assignee: Amorepacific Corporation
    Inventors: Song Seok Shin, Yong Deog Hong, Kyoung Hee Byoun, Mi Young Park, Jin Kyu Choi, Yang Hui Park, Il Hong Bae, Yung Hyup Joo, Kyung Min Lim, Young Ho Park
  • Patent number: 8975254
    Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: March 10, 2015
    Assignee: Orion Corporation
    Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
  • Patent number: 8975400
    Abstract: Disclosed are 2,3-dihydroimiazo[1,2-c]pyrimidin-5(IH)-one compounds that inhibit Lp-PLA2,processes for their preparation, compositions containing them and their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: March 10, 2015
    Assignee: Glaxo Group Limited
    Inventors: Zehong Wan, Kai Long, Yingxia Sang, Xiaobo Su
  • Publication number: 20150065482
    Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Application
    Filed: August 22, 2014
    Publication date: March 5, 2015
    Applicant: GENENTECH, INC.
    Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Jason Burch
  • Publication number: 20150065497
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: March 5, 2015
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
  • Publication number: 20150065522
    Abstract: The present invention relates to compounds formula (I): and to salts thereof, wherein R1-R4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: September 4, 2014
    Publication date: March 5, 2015
    Inventors: Brian K. Albrecht, Steven F. Bellon, Victor S. Gehling, Jean-Christophe Harmange, Yves LeBlanc, Jun Liang, Steven Magnuson, Vicki Tsui, Birong Zhang
  • Patent number: 8969360
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables R1, R2, R3, and R4 are as defined herein.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: March 3, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Chris Davis, Steven Durrant, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Michael O'Donnell, Francoise Pierard, Joanne Pinder, Pierre-Henri Storck, Heather Twin
  • Patent number: 8969341
    Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: March 3, 2015
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Patent number: 8962627
    Abstract: The present invention provides new oxime derivatives of the general formula (I), pharmaceutical compositions containing them and their use for the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. This invention further provides new oxime derivatives of the general formula (I) consisting of modulators of nervous system receptors sensitive to glutamate, which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. In particular embodiments, the new oxime derivatives of the invention are modulators of metabotropic glutamate receptors (mGluRs). The invention further provides positive allosteric modulators of mGluRs and more specifically positive alSosteric modulators of mGluR4.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: February 24, 2015
    Assignee: Prestwick Chemical, Inc.
    Inventors: Stephan Schann, Stanislas Mayer, Christophe Morice, Bruno Giethlen