1,3-diazine Ring Patents (Class 544/122)
  • Patent number: 10377725
    Abstract: The present invention relates to a phenyl amino pyrimidine compound or a polymorph of a salt thereof, specifically, to N-(cyanomethyl)-4-(2-((4-(2?,2?,6?,6?-d4-morpholino)phenyl)amino)pyrimidin-4-yl)benzamide, or a pharmaceutically acceptable salt thereof, or a polymorph of a solvate thereof, that is, a compound shown in formula I or salt thereof, or a polymorph of a solvate thereof. The polymorph is suitable for preparing a pharmaceutical composition for suppressing non-receptor tyrosine kinases (such as JAK kinase).
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: August 13, 2019
    Assignee: Suzhou Zelgen Biopharmaceuticals Co., Ltd.
    Inventors: Binhua Lv, Chengwei Li, Dan Xiao
  • Patent number: 10266548
    Abstract: Compounds of formula (I) which are inhibitors of Bub 1 kinase, processes for their production and their use as pharmaceuticals.
    Type: Grant
    Filed: February 21, 2017
    Date of Patent: April 23, 2019
    Assignees: Bayer Intellectual Property GmbH, Bayer Pharma Aktiengesellschaft
    Inventors: Marion Hitchcock, Anne Mengel, Vera Pütter, Gerhard Siemeister, Antje Margret Wengner, Hans Briem, Knut Eis, Volker Schulze, Amaury Ernesto Fernandez-Montalvan, Stefan Prechtl, Simon Holton, Jörg Fanghänel, Philip Lienau, Cornelia Preusse, Mark Jean Gnoth
  • Patent number: 10252984
    Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: April 9, 2019
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
  • Patent number: 10112931
    Abstract: 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: Grant
    Filed: April 27, 2017
    Date of Patent: October 30, 2018
    Assignee: NOVARTIS AG
    Inventors: 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 Clifford Sutton, Yaping Wang, Qian Zhao
  • Patent number: 10098889
    Abstract: This invention relates to L-tartaric acid complexes, acid addition salts, base addition salts of the compound named (S)-4-(((R)-6-(2-chloro-4-fluorophenyl)-5-(methoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl) morpholine-3-carboxylic acid or tautomer thereof and pharmaceutical compositions thereof, and further relates to use of the compounds or the pharmaceutical compositions in the manufacture of a medicament, especially for use in preventing, managing, treating or lessening a HBV infection. The complex, acid addition salt or base addition salt of the present invention is crystalline form, substantially crystalline form, polymorphism, amorphism, hydrate or solvate.
    Type: Grant
    Filed: February 1, 2016
    Date of Patent: October 16, 2018
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Qingyun Ren, Liang Chen, Xinchang Liu, Jinsheng Liang, Chenliang Wu, Zhifu Zou, Guanghua Yan, Desheng Huangfu, Siegfried Goldmann, Yingjun Zhang
  • Patent number: 10035803
    Abstract: The present invention relates to a novel method of preparing copanlisib, and copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: July 31, 2018
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Jan-Georg Peters, Jürgen Stiehl, Kai Lovis
  • Patent number: 10035779
    Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: July 31, 2018
    Assignee: GlaxoSmithKline, LLC
    Inventors: Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
  • Patent number: 10023593
    Abstract: An ALK kinase inhibitor compound as represented by Formula I, pharmaceutical composition containing the compound, and preparation method and use thereof in the preparation of drugs serving as an ALK inhibitor for treating cancer.
    Type: Grant
    Filed: May 29, 2015
    Date of Patent: July 17, 2018
    Assignee: Beijing Pearl Biotechnology Limited Liability Company
    Inventors: Jiaqiang Dong, Boyu Zhong, Hongbin Yuan, Chuan Shih, Shaosong Chu, Deyi Zhang, Ruihao Zhang
  • Patent number: 10005737
    Abstract: The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.
    Type: Grant
    Filed: November 22, 2016
    Date of Patent: June 26, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Michael Edward O'Donnell
  • Patent number: 9987276
    Abstract: The present invention provides 2,4-diaminopyrimidines, and/or pharmaceutically acceptable compositions thereof, as kinase inhibitors.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: June 5, 2018
    Assignee: Celgene CAR LLC
    Inventors: Juswinder Singh, Russell C. Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
  • Patent number: 9732063
    Abstract: In compounds of formula I: R1 to R5, Ar and X1 to X3 have defined meanings. The compounds have anti-inflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: August 15, 2017
    Assignees: RESPIVERT LIMITED, TOPIVERT PHARMA LIMITED
    Inventors: Fritz-Frieder Frickel, Matthew Colin Thor Fyfe, Premji Meghani, Stephen Malcolm Thom
  • Patent number: 9688672
    Abstract: 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: Grant
    Filed: July 13, 2016
    Date of Patent: June 27, 2017
    Assignee: NOVARTIS AG
    Inventors: 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 Clifford Sutton, Yaping Wang, Qian Zhao
  • Patent number: 9682974
    Abstract: Compounds of formula (I), processes for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: October 27, 2014
    Date of Patent: June 20, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Anne Mengel, Anja Richter, Marion Hitchcock, Hans Briem, Gerhard Siemeister, Wilhelm Bone, Amaury Ernesto Fernandez-Montalvan, Jens Schröder, Simon Holton, Cornelia Preuβe, Ursula Mönning
  • Patent number: 9527859
    Abstract: The present invention relates to novel amidopyridine derivatives. More specifically, the present invention provides a medicinal agent which is useful as a prophylactic or therapeutic agent for diseases based on the production of cytokines from T cells, comprising as the active ingredient an amidopyridine derivative or a pharmacologically acceptable salt thereof. Provided are an amidopyridine derivative of the following general formula (I): wherein each symbol has the same meaning as defined in the description, or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: December 27, 2016
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Masayuki Watanabe, Hiroyuki Furukawa, Maiko Hamada, Naoto Fujie, Hiroyuki Ushio, Tooru Takashima
  • Patent number: 9458177
    Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: October 4, 2016
    Assignee: NOVARTIS AG
    Inventors: Giorgio Caravatti, Robin Alec Fairhurst, Pascal Furet, Clive McCarthy, Heinrich Rueeger, Frank Hans Seiler, Frédéric Stauffer
  • Patent number: 9434719
    Abstract: 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: Grant
    Filed: March 12, 2014
    Date of Patent: September 6, 2016
    Assignee: NOVARTIS AG
    Inventors: 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
  • Patent number: 9415055
    Abstract: The present invention is directed to novel cyclic amines which inhibit the P2X7 receptor.
    Type: Grant
    Filed: July 8, 2015
    Date of Patent: August 16, 2016
    Assignee: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohamed Eldemenky, Bin Chen, Yu Jiang
  • Patent number: 9394260
    Abstract: The present invention provides compounds of Formula (I): (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Grant
    Filed: April 1, 2013
    Date of Patent: July 19, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Hui Hu, Jennifer X. Qiao, Tammy C. Wang
  • Patent number: 9353066
    Abstract: The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: May 31, 2016
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Andrew M. Haidle, Jason Burch, Daniel Guay, Jacques Yves Gauthier, Joel Robichaud, Jean Francois Fournier, John Michael Ellis, Matthew Christopher, Solomon D. Kattar, Graham F. Smith, Alan B. Northrup
  • Patent number: 9278956
    Abstract: A novel inhibitor of Rac activity based on the structure of the established Rac/Rac-GEF inhibitor NSC23766 is discloses. The compound EHop-016, with an IC50 of 1.1 ?M, is a 100-fold more efficient inhibitor of Rac activity than NSC23766. EHop-016 is specific for Rac1 and Rac3 at concentrations ?5 mM. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells, EHop-016 (?5 mM) inhibits the association of the Rac-GEF Vav2 with a nucleotide-free Rac1(G15A), which has a high affinity for activated GEFs. EHop-016 does not affect the association of the Rac-GEF Tiam-1 with Rac1(G15A) at similar concentrations. EHop-016 also inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation in both cell lines. EHop-016 decreases Rac-downstream effects of p21-activated kinase (PAK)1 activity and directed migration of metastatic cancer cells. At low concentrations (<5 ?M), EHop-016 does not affect cell viability.
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: March 8, 2016
    Assignee: University of Puerto Rico
    Inventors: Eliud Hernandez, Cornelis Vlaar, Suranganie Dharmawardhane
  • Patent number: 9265763
    Abstract: Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: February 23, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marion Hitchcock, Anne Mengel, Vera Pütter, Gerhard Siemeister, Antje Margret Wengner, Hans Briem, Knut Eis, Volker Schulze, Amaury Ernesto Fernandez-Montalvan, Stefan Prechtl, Simon Holton, Jörg Fanghänel, Philip Lienau, Cornelia Preusse, Mark Jean Gnoth
  • Patent number: 9227959
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or CH R1 is fluoro or chloro R2 is hydrogen or methyl or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: January 5, 2016
    Assignee: Hoffman-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Patent number: 9187453
    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: Grant
    Filed: March 27, 2013
    Date of Patent: November 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tetsuya Tsukamoto, Yusuke Ohba, Takafumi Yukawa, Hiroyuki Nagamiya, Taku Kamei, Norihito Tokunaga, Morihisa Saitoh
  • Patent number: 9133204
    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: Grant
    Filed: September 9, 2014
    Date of Patent: September 15, 2015
    Assignee: H. Lundbeck A/S
    Inventors: Hongbin Li, Jun Yuan, Rajagopal Bakthavatchalam, Kevin J Hodgetts, Qin Guo, Scott M. Capitosti, Jianmin Mao, David J. Wustrow
  • Patent number: 9133168
    Abstract: The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: September 15, 2015
    Assignee: SANOFI
    Inventors: Maurice Brollo, Jean-Christophe Carry, Victor Certal, Eric Didier, Gilles Doerflinger, Youssef El Ahmad, Frank Halley, Karl Andreas Karlsson
  • Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • Patent number: 9040529
    Abstract: The invention relates compounds of general formula (I) and pharmaceutically acceptable salts and solvates thereof wherein R1 is halogen, vinylene-aryl, substituted aryl, heteroaryl or a benzo[1,3]dioxolil group, W is a group of formula —NH—SO2—R2 or heteroaryl group or NHR3 group where R3 is hydrogen or heteroaryl; and n is 1, 2, 3 or 4. Furthermore, the present invention is directed to pharmaceutical composition containing at least one compound of general formula (I) and/or pharmaceutically acceptable salts or solvates thereof and for the use of them for the preparation of pharmaceutical compositions for the prophylaxis and/or the treatment of protein kinase related, especially CDK9-related diseases e.g. cell proliferative disease, infectious disease, pain, cardiovascular disease and inflammation.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: May 26, 2015
    Assignee: Vichem Chemie Kutató Kft.
    Inventors: Zoltán Greff, Zoltán Varga, György Kéri, Gábor Németh, László Örfi, Csaba Szántai Kis
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Publication number: 20150141428
    Abstract: The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 21, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Melissa Egbertson, Edward Brnardic, Kristen G. Jones, John M. Sanders, Darrell Henze
  • Publication number: 20150141427
    Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150141396
    Abstract: The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases.
    Type: Application
    Filed: July 3, 2013
    Publication date: May 21, 2015
    Applicant: Ares Trading S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Patrick Gerber, Mathilde Muzerelle
  • Publication number: 20150141372
    Abstract: Compounds of formula (I), processes for their production and their use as Bub1 kinase inhibitors for the treatment of hyperproliferative diseases and/or disorders responsive to induction of cell death.
    Type: Application
    Filed: May 8, 2013
    Publication date: May 21, 2015
    Inventors: Marion Hitchcock, Christoph-Stephan Hilger, Anne Mengel, Hans Briem, Simon Holton, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernández-Montalván, Christian Stegmann, Cornelia Preuße, Mark Jean Gnoth
  • 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
  • Publication number: 20150119394
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 30, 2015
    Inventors: Abhijit Roychowdhury, Rajiv Sharma, Malcolm Mascarenhas, Chandrika B-Rao, Shashikant M. Patil, Sambhaji Chavan, Nitin Lad, Smriti Khanna, Christopher J. Dinsmore
  • Publication number: 20150111891
    Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
    Type: Application
    Filed: January 3, 2013
    Publication date: April 23, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongyan Guo, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Randall W. Vivian, Lianhong Xu, Hong Yang
  • Publication number: 20150111871
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 23, 2015
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Publication number: 20150111866
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.
    Type: Application
    Filed: April 26, 2013
    Publication date: April 23, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John J. Acton, III, Feng Ye, Petr Vachal, Deyou Sha, James F. Dropinski, Lin Chu, Debra Ondeyka, Alexander J. Kim, Vincent J. Colandrea, Yi Zang, Fengqi Zhang, Guizhen Dong
  • Publication number: 20150105370
    Abstract: Embodiments of the disclosure relate to selectively substituted quinoline 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: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Inventors: ERIC CARLSON, HANS HANSEN, LYNN HAWKINS, SALLY ISHIZAKA, MATTHEW MACKEY, SHAWN SCHILLER, CHIKAKO OGAWA, HEATHER DAVIS
  • 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: 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: 20150099748
    Abstract: Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).
    Type: Application
    Filed: September 29, 2014
    Publication date: April 9, 2015
    Inventors: Gregory W. Endres, Pil Heui Lee, Kirk Lang Olson, James Bernard Kramer, Fred Lawrence Ciske, Stephen Douglas Barrett
  • 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: 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: 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
  • Patent number: 8993567
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: March 31, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Publication number: 20150087827
    Abstract: The present invention relates to a process for preparing 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-ol (I—enol form) or 2-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one (I—keto form) and sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-olate (II) from 1,2,3-triazole (III), methyl bromoacetate (IV-Me-Br) or ethyl bromoacetate (IV-Et-Br), 4,6-dichloropyrimidine (VIII), morpholine (IX) and hydrazine (XII).
    Type: Application
    Filed: May 6, 2013
    Publication date: March 26, 2015
    Applicant: BAYER PHARMA AKTIENGESELLSCAFT
    Inventors: Hans-Christian Militzer, Johannes Eggert
  • Publication number: 20150087646
    Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Application
    Filed: June 10, 2013
    Publication date: March 26, 2015
    Applicant: GLENMARK PHARMACEUTICALS S.A.
    Inventors: Laxmikant Atmaram Gharat, Nagarajan Muthukaman, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Publication number: 20150087585
    Abstract: Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H-imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
    Type: Application
    Filed: March 26, 2013
    Publication date: March 26, 2015
    Applicant: PFIZER INC.
    Inventors: Kay Ahn, Markus Boehm, Shawn Cabral, Philip A. Carpino, Kentaro Futatsugi, David Hepworth, Daniel W. Kung, Suvi Orr, Jian Wang
  • Patent number: 8987250
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Publication number: 20150080396
    Abstract: The invention concerns compounds of Formula (I): wherein L1, R1, R2, R3, R4 and X are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of disease, for example cancer.
    Type: Application
    Filed: August 26, 2014
    Publication date: March 19, 2015
    Applicants: DAINIPPON SUMITOMO PHARMA CO., LTD., ASTRAZENECA AB
    Inventors: Nicholas James Bennett, Stephen Thom, Thomas McInally