Hetero Ring Is Seven-membered Consisting Of Two Nitrogens And Five Carbon Atoms Patents (Class 514/218)
  • Patent number: 10683281
    Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
    Type: Grant
    Filed: August 8, 2019
    Date of Patent: June 16, 2020
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Scott W. Bagley, John M. Curto, David James Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Yajing Lian, Chris Limberakis, Allyn T. Londregan, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
  • Patent number: 10676468
    Abstract: Disclosed are novel N-(3-heteroarylaryl)-4-arylarylcarboxamides and analogs thereof, represented by the Formula I: wherein C cyclic group, D1-D4, Q1, Q2, R5 are defined herein. Compounds having Formula (I) are hedgehog pathway inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of hedgehog activity, such as cancer.
    Type: Grant
    Filed: July 19, 2013
    Date of Patent: June 9, 2020
    Assignee: Impact Therapeutics, Inc.
    Inventors: Suixiong Cai, Ye Edward Tian, Sishun Kang, Zheng Meng, Chengyun Gu, Feng Yin, Shengzhi Chen, Yang Zhang, Xiuyan Zhang, Hongqiang Fei, Dongmei Wang
  • Patent number: 10676465
    Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
    Type: Grant
    Filed: August 8, 2019
    Date of Patent: June 9, 2020
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Scott W. Bagley, John M. Curto, David James Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Yajing Lian, Chris Limberakis, Allyn T. Londregan, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
  • Patent number: 10654849
    Abstract: Compounds of formula (I): wherein R1, R2, J, K, L, n and W are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring pro-apoptotic and/or anti-proliferative agents.
    Type: Grant
    Filed: June 9, 2017
    Date of Patent: May 19, 2020
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: András Kotschy, Csaba Wéber, Attila Vasas, Balázs Molnár, árpád Kiss, Alba Macias, James Brooke Murray, Elodie Lewkowicz, Olivier Geneste, Mäia Chanrion, Didier Demarles, Lisa Ivanschitz
  • Patent number: 10654869
    Abstract: The present invention provides compounds as bacterial topoisomerase inhibitors with antibacterial activity. The present invention also provides pharmaceutical compositions comprising at least one of the compounds and methods of using the compounds and pharmaceutical compositions as antibacterial agents for treating infectious diseases.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: May 19, 2020
    Assignees: THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES, UNIVERSITY OF HAWAII
    Inventors: Yuk-Ching Tse-Dinh, Dianqing Sun
  • Patent number: 10632125
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: April 28, 2020
    Assignee: THOMAS HELLEDAYS STIFTELSE FOR MEDICINSK FORSKNING
    Inventors: Martin Scobie, Olov Wallner, Tobias Koolmeister, Karl Sven Axel Vallin, Carl Martin Henriksson, Evert Homan, Thomas Helleday, Sylvain Jacques, Roland Julius Yu Fiskesund
  • Patent number: 10632103
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Grant
    Filed: January 26, 2018
    Date of Patent: April 28, 2020
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • Patent number: 10603354
    Abstract: This invention concerns compositions and methods of treating or diagnosing inflammatory disorders and other disorders, as well as compositions and methods of treating HIV.
    Type: Grant
    Filed: January 30, 2019
    Date of Patent: March 31, 2020
    Assignees: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY, ACTINOBAC BIOMED, INC.
    Inventors: Scott C. Kachlany, Benjamin A. Belinka, Jr.
  • Patent number: 10570137
    Abstract: The present invention relates to compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein R1 is C1-C3alkyl optionally substituted with F, C3-C6cycloalkyl, C1-C3alkoxy; X represents a bond or C1-C3alkylene optionally substituted with OH, ONO, ONO2; R2 is H, OH, ONO, ONO2, C(O)OH, C(O)OC1-C3alkyl, CHO, CN, C1-C3alkoxy, OC(O)H, OC(O)—C1-C3alkyl, C(O)N(R6)OR7, OC1-C3alkylene-C(O)OH, OC1-C3alkylene-C(O)OC1-C3alkyl, OC1-C3alkylene-C(O)N(R6)OR7, S(O0-2)C1-C3alkyl, CR8?N—OR9, CR8?N—NR10R11, CR8?NR12 or CR8?N—ONO2; R3 is C1-C6alkyl optionally substituted with F, OH, ONO, ONO2, C1-C3alkoxy, C3-C6cycloalkyl; C3-C6cycloalkyl, C2-C6alkenyl, C2-C6alkynyl; R4 is C1-C6alkyl optionally substituted with C3-C6cycloalkyl, C1-C6alkoxy, F, ONO, ONO2; C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl; R5 is H, SO2NR13R14, NHSO2NR13R14; R6 is H or C1-C3alkyl; R7 is H, C1-C3alkyl, C1-C3alkoxy, C1-C3alkyl substituted with phenyl, benzyl or a heterocyclic ring, wherein said phenyl, benzyl or
    Type: Grant
    Filed: November 15, 2016
    Date of Patent: February 25, 2020
    Assignee: TOPADUR PHARMA AG
    Inventors: Reto Naef, Hermann Tenor
  • Patent number: 10548899
    Abstract: The present invention provides a compound which has a cholinergic muscarinic M1 receptor positive allosteric modulator activity and may be useful as a medicament such as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, Lewy body dementia and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. In the formula (I), each symbol is as described in the attached specification.
    Type: Grant
    Filed: October 19, 2016
    Date of Patent: February 4, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiro Sugimoto, Shinkichi Suzuki, Hiroki Sakamoto, Masami Yamada, Minoru Nakamura, Makoto Kamata, Kenichiro Shimokawa, Masaki Ogino, Eiji Kimura, Masataka Murakami, Takuto Kojima, Jinichi Yonemori
  • Patent number: 10478430
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase and combination therapies thereof. 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: wherein the variables are as defined herein.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: November 19, 2019
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: John Robert Pollard, Philip Michael Reaper, Mohammed Asmal
  • Patent number: 10449192
    Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
    Type: Grant
    Filed: February 26, 2018
    Date of Patent: October 22, 2019
    Assignee: KUDO PHARMACEUTICALS LIMITED
    Inventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
  • Patent number: 10426783
    Abstract: Disclosed herein is a prophylactic or therapeutic agent for ocular fundus disease, especially diabetic retinopathy or age-related macular degeneration. The prophylactic or therapeutic agent for ocular fundus disease comprising: (S)-(?)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, a salt thereof, or a solvate thereof, as an active ingredient.
    Type: Grant
    Filed: December 21, 2016
    Date of Patent: October 1, 2019
    Assignees: KYUSHU UNIVERSITY, NAT'L UNIVERSITY CORPORATION, KOWA COMPANY, LTD.
    Inventors: Tatsuro Ishibashi, Shintaro Nakao, Ryoichi Arita, Ken Mizuno, Akifumi Tsuchiura
  • Patent number: 10407376
    Abstract: The present invention is directed to a method for preparing a final phenolic product from biomass comprising the steps of providing a furanic compound obtainable from biomass; reacting the furanic compound with a dienophile to obtain a phenolic compound; reacting the phenolic compound further to obtain the final phenolic product.
    Type: Grant
    Filed: January 18, 2016
    Date of Patent: September 10, 2019
    Assignee: Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TNO
    Inventors: Marc Crockatt, Jan Harm Urbanus, Paul Mathijs Konst, Martijn Constantijn De Koning
  • Patent number: 10369128
    Abstract: A method for treating a proliferative disease, disorder, or condition comprising administering a cis-diamine platinum(II) thione complex. A cis-diamine platinum(II) thione complex and compositions containing it.
    Type: Grant
    Filed: February 12, 2019
    Date of Patent: August 6, 2019
    Assignee: King Fahd University of Petroleum and Minerals
    Inventors: Mohammed Yagoub Jomaa, Anvarhusein A. Isab
  • Patent number: 10364234
    Abstract: Pyridinecarboxamide derivatives, preparation methods, and a pharmaceutical uses thereof are provided. In particular, pyridinecarboxamide derivatives represented by general formula (I), wherein the substituents of the formula (I) are defined in the specification are provided. Also provided are a preparation method for the pyridinecarboxamide derivatives of formula (I), a pharmaceutical composition containing the pyridinecarboxamide derivatives, and uses of the pyridinecarboxamide derivatives as therapeutic agents, especially as inhibitors of the Renal Outer Medullary Potassium channel (ROMK) and in the preparation of medicaments for treating and/or preventing hypertension and heart failure.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: July 30, 2019
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Xin Li, Qing Dong, Piaoyang Sun
  • Patent number: 10363244
    Abstract: The present invention provides uses of a glucokinase activator in combination with metformin. Uses include treating type 2 diabetes, lowering blood glucose, improving insulin sensitivity, enhancing phosphorylation of glucose, and improving the therapeutic effectiveness of metformin. The invention also provides pharmaceutical compositions that comprise a GK activator and metformin. The invention also provides a salt formed between metformin and a GK activator.
    Type: Grant
    Filed: August 8, 2018
    Date of Patent: July 30, 2019
    Assignee: vTv Therapeutics LLC
    Inventors: Adnan M. M. Mjalli, Maria Carmen Valcarce Lopez
  • Patent number: 10357473
    Abstract: A method for treating a proliferative disease, disorder, or condition comprising administering a cis-diamine platinum(II) thione complex. A cis-diamine platinum(II) thione complex and compositions containing it.
    Type: Grant
    Filed: February 12, 2019
    Date of Patent: July 23, 2019
    Assignee: King Fahd University of Petroleum and Minerals
    Inventors: Mohammed Yagoub Jomaa, Anvarhusein A. Isab
  • Patent number: 10357503
    Abstract: This invention relates to a method for the prevention of cardiovascular disease, a formulation for the prevention of cardiovascular disease, the use of specified active principals for the manufacture of such a formulation for use in the method and to a method of preparing said formulation. The formulation of the present invention is a combination of active principals for use in the prevention of cardiovascular disease, notably ischaemic heart disease (including heart attacks) and stroke among the general adult population.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: July 23, 2019
    Inventors: Nicholas J Wald, Malcolm R Law
  • Patent number: 10351535
    Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opioid receptor and more particularly to piperazine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: July 16, 2019
    Assignee: ESTEVE PHARMACEUTICALS, S.A.
    Inventors: Félix Cuevas-Cordobés, Carmen Almansa-Rosales, Monica Garcia Lopez
  • Patent number: 10329270
    Abstract: The present invention relates to pyridine, pyrimidine, pyrazine, and pyridazine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
    Type: Grant
    Filed: October 21, 2014
    Date of Patent: June 25, 2019
    Assignee: Merck Patent GmbH
    Inventors: Hui Qiu, Richard D. Caldwell, Constantin Neagu, Igor Mochalkin, Lesley Liu-Bujalski, Reinaldo Jones, Devon Tate, Theresa L. Johnson, Anna Gardberg
  • Patent number: 10292968
    Abstract: The present application relates to substituted heterocycles compound of Formula I and pharmaceutical compositions thereof useful for the inhibition of BET protein function by binding to bromodomains (Formula I).
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: May 21, 2019
    Assignee: Zenith Epigenetics Ltd.
    Inventors: Samuel David Brown, Craig Alan Coburn, Olesya Kharenko
  • Patent number: 10292990
    Abstract: A nanoparticulate composition of abiraterone acetate that allows treatment at a lower dose than convention abiraterone acetate formulations is described as in a method of treating prostate cancer by administering the composition together with a glucocorticoid.
    Type: Grant
    Filed: November 7, 2016
    Date of Patent: May 21, 2019
    Assignee: SUN PHARMA GLOBAL FZE
    Inventors: Paul Nemeth, Matt Callahan, H. William Bosch, Marck Norret
  • Patent number: 10278944
    Abstract: A method for treating a proliferative disease, disorder, or condition comprising administering a cis-diamine platinum(II) thione complex. A cis-diamine platinum(II) thione complex and compositions containing it.
    Type: Grant
    Filed: October 26, 2017
    Date of Patent: May 7, 2019
    Assignee: King Fahd University of Petroleum and Minerals
    Inventors: Mohammed Yagoub Jomaa, Anvarhusein A. Isab
  • Patent number: 10280184
    Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: May 7, 2019
    Assignee: AbbVie Inc.
    Inventors: Michael M. Friedman, Philip Cox, Kristine E. Frank, Michael Z. Hoemann, Augustine Osuma, Noel S. Wilson, Xiangdong Xu, Kevin Cusack, Raymond Huntley, J. Martin Herold
  • Patent number: 10273225
    Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.
    Type: Grant
    Filed: May 14, 2018
    Date of Patent: April 30, 2019
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Mark E. Adams, Jason W. Brown, Stephen Hitchcock, Maria Hopkins, Shota Kikuchi, Betty Lam, Holger Monenschein, Holly Reichard, Huikai Sun
  • Patent number: 10273228
    Abstract: Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: April 30, 2019
    Assignees: Indiana University Research and Technology Corporation, Assembly Biosciences, Inc.
    Inventors: Lee Daniel Arnold, Hans Maag, William W. Turner, Jr.
  • Patent number: 10220036
    Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein R1, R2, R3, R4, R5, and n are as defined herein.
    Type: Grant
    Filed: December 21, 2015
    Date of Patent: March 5, 2019
    Assignee: Novartis AG
    Inventors: Ho Man Chan, Xiang-Ju Justin Gu, Ying Huang, Ling Li, Yuan Mi, Wei Qi, Martin Sendzik, Yongfeng Sun, Long Wang, Zhengtian Yu, Hailong Zhang, Ji Yue (Jeff) Zhang, Man Zhang, Qiong Zhang, Kehao Zhao
  • Patent number: 10220043
    Abstract: A technique is provided for suppressing the crystal precipitation of an aqueous composition containing a halogenated isoquinoline derivative during low-temperature preservation. An aqueous composition comprising a compound represented by Formula (1): wherein x represents a halogen atom, or a salt thereof, or a solvate of the compound or the salt thereof, and brimonidine or a salt thereof.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: March 5, 2019
    Assignee: KOWA COMPANY, LTD.
    Inventor: Isamu Sawai
  • Patent number: 10206997
    Abstract: Provided herein is a vaccine that combines a vaccine facilitator and a DNA construct encoding an antigen to elicit antigen-specific antibody responses, wherein the vaccine facilitator is a Na/K pump inhibitor. Cellular entry of the DNA is accelerated as compared to other vaccines that do not contain the vaccine facilitator.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: February 19, 2019
    Inventors: Bin Wang, Shuang Geng
  • Patent number: 10179777
    Abstract: Compounds of the formula I in which W, R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of ALK1, AL2 and ALK5, and can be employed for the treatment of diseases such as cancer.
    Type: Grant
    Filed: March 22, 2016
    Date of Patent: January 15, 2019
    Assignee: MERCK PATENT GMBH
    Inventors: Dieter Dorsch, Alfred Jonczyk, Mireille Krier
  • Patent number: 10172830
    Abstract: Pyrazolone derivatives of formula (I) defined herein exhibit human neutrophil elastase inhibitory properties and are useful for the treatment of diseases or conditions in which HNE is implicated.
    Type: Grant
    Filed: May 26, 2017
    Date of Patent: January 8, 2019
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Jonathan Mark Sutton, Robert Andrew Heald, Andrew Stephen Robert Jennings, Carmelida Capaldi, Elisabetta Armani
  • Patent number: 10174011
    Abstract: The present invention provides a heterocyclic compound represented by the formula (I), its stereoisomers, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and their use in preparing a medicament for the prevention and/or treatment of central nervous system disease.
    Type: Grant
    Filed: March 9, 2015
    Date of Patent: January 8, 2019
    Assignees: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, SUZHOU VIGONVITA LIFE SCIENCES CO., LTD., TOPHARMAN SHANDONG CO., LTD.
    Inventors: Hualiang Jiang, Zhen Wang, Jianfeng Li, Rongxia Zhang, Yang He, Yongjian Liu, Minghao Bi, Zheng Liu, Guanghui Tian, Weiming Chen, Feipu Yang, Chunhui Wu, Yu Wang, Xiangrui Jiang, Jingjing Yin, Guan Wang, Jingshan Shen
  • Patent number: 10155761
    Abstract: The compounds of formula (I) are antagonists of the CXCR4 receptor Wherein R1, X, Y and R2 are as defined in the claims.
    Type: Grant
    Filed: April 26, 2017
    Date of Patent: December 18, 2018
    Assignee: PROXIMAGEN, LLC
    Inventors: Edward Daniel Savory, Alison Stewart, Allison Carley, Giles Brown, Iain Simpson, Kathryn Oliver, Lee Patient, Michael Higginbottom, Andrew Graham Cole
  • Patent number: 10106507
    Abstract: Disclosed herein are compounds that are inhibitors of BRD4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BRD4 are also disclosed. In certain aspects, disclosed are compounds of Formula I-IV.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: October 23, 2018
    Assignee: H. Lee Moffitt Cancer Center and Research Insitute, Inc.
    Inventors: Ernst Shönbrunn, Nicholas J. Lawrence, Harshani R. Lawrence
  • Patent number: 10093684
    Abstract: Certain imidazopyrazines of Formula I and pharmaceutical compositions thereof are provided herein: Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: January 11, 2017
    Date of Patent: October 9, 2018
    Assignee: Gilead Connecticut, Inc.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Douglas G. Stafford, Jianjun Xu
  • Patent number: 10064869
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: September 4, 2018
    Assignee: THOMAS HELLEDAYS STIFTELSE FOR MEDICINSK FORSKNING
    Inventors: Martin Scobie, Olov Wallner, Tobias Koolmeister, Karl Sven Axel Vallin, Carl Martin Henriksson, Evert Homan, Thomas Helleday, Sylvain Jacques, Matthieu Desroses, Marie-Caroline Jacques-Cordonnier, Roland Julius Yu Fiskesund
  • Patent number: 10065960
    Abstract: The present invention is directed to novel compounds of formula I and their use as therapeutic compounds.
    Type: Grant
    Filed: July 14, 2015
    Date of Patent: September 4, 2018
    Assignee: Ogeda SA
    Inventors: Hamid R. Hoveyda, Marie-Odile Roy, Graeme L. Fraser, Guillaume Dutheuil
  • Patent number: 10034885
    Abstract: The present invention provides a novel corneal thickness modulating agent. The present invention pertains to a corneal thickness modulating agent containing 1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof or a solvate thereof.
    Type: Grant
    Filed: September 24, 2015
    Date of Patent: July 31, 2018
    Assignee: KOWA COMPANY, LTD.
    Inventors: Hiroyuki Takahashi, Kiyoshi Toya, Akifumi Tsuchiura
  • Patent number: 10030017
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer, melanoma, and the like.
    Type: Grant
    Filed: March 15, 2016
    Date of Patent: July 24, 2018
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Amogh Boloor, Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 10022382
    Abstract: Provided are novel compounds which are capable of inhibiting an activity of RNA polymerase I, and uses thereof in treating diseases or disorders modulated by RNA polymerase I, preferably autoimmune diseases such as multiple sclerosis and proliferative diseases.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: July 17, 2018
    Assignee: Tel HaShomer Medical Research Infrastructure and Services Ltd.
    Inventors: Anat Achiron, Roi Mashiach, Michael Gurevich
  • Patent number: 10000499
    Abstract: The present invention is directed to methyl diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: November 20, 2015
    Date of Patent: June 19, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Thomas S. Reger, Jason W. Skudlarek
  • Patent number: 9981969
    Abstract: The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.
    Type: Grant
    Filed: June 2, 2014
    Date of Patent: May 29, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Milana Maletic, Yunfu Luo, Zhiqi Qi, Chunsing Li, Tingting Yu, Richard Soll
  • Patent number: 9980972
    Abstract: The invention relates to a new use of a known Rho kinase inhibitor, fasudil or a fasudil derivative selected from hydroy-fasudil or dimethylfasudil, in the treatment of amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: May 29, 2018
    Assignee: GEORG-AUGUST-UNIVERSITÄT GÖTTINGEN STIFTUNG ÖFFENTLICHEN RECHTS, UNIVERSITÄTSMEDIZIN
    Inventors: Paul Lingor, Lars Tönges
  • Patent number: 9969725
    Abstract: The invention is directed to pharmaceutically acceptable salts of suvorexant, which is an antagonist of orexin receptors. The pharmaceutically acceptable salts of suvorexant are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is further directed to pharmaceutical compositions comprising pharmaceutically acceptable salts of suvorexant.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: May 15, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael McNevin, Sachin Lohani
  • Patent number: 9957282
    Abstract: The present invention includes crystalline forms of 2-(4-Methyl-[1,4]diazepan-1-yl)-5-oxo-5H-7-thia-1,11b-diaza-benzo[c]fluorene-6-carboxylic acid (5-methyl-pyrazin-2-ylmethyl)-amide and crystalline forms of salts and/or solvates of 2-(4-Methyl-[1,4]diazepan-1-yl)-5-oxo-5H-7-thia-1,11b-diaza-benzo[c]fluorene-6-carboxylic acid (5-methyl-pyrazin-2-ylmethyl)-amide. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms and the compositions thereof.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: May 1, 2018
    Assignee: SENHWA BIOSCIENCES, INC.
    Inventors: David M. Ryckman, Iching Grace Yu, Hshiou-ting Liu
  • Patent number: 9938245
    Abstract: The present invention provides, inter alia, compounds having the structure of formula (I): Compositions containing such compounds are also provided. Methods for using such compounds or compositions for treating or ameliorating the effects of a cancer having a cell that harbors an oncogenic RAS mutation, for modulating a lipoxygenase in a ferroptosis cell death pathway, and for depleting reduced glutathione (GSH) in a cell harboring an oncogenic RAS mutation are further provided.
    Type: Grant
    Filed: January 14, 2015
    Date of Patent: April 10, 2018
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Brent R. Stockwell, Wan Seok Yang, Marie-Helene Larraufie
  • Patent number: 9931336
    Abstract: Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt.
    Type: Grant
    Filed: August 15, 2016
    Date of Patent: April 3, 2018
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Casey Kopczynski, Cheng-Wen Lin, Jill Marie Sturdivant, Mitchell A. deLong
  • Patent number: 9855251
    Abstract: The present invention provides uses of a glucokinase activator in combination with metformin. Uses include treating type 2 diabetes, lowering blood glucose, improving insulin sensitivity, enhancing phosphorylation of glucose, and improving the therapeutic effectiveness of metformin. The invention also provides pharmaceutical compositions that comprise a GK activator and metformin. The invention also provides a salt formed between metformin and a GK activator.
    Type: Grant
    Filed: February 11, 2016
    Date of Patent: January 2, 2018
    Assignee: vTv Therapeutics LLC
    Inventors: Adnan M. M. Mjalli, Maria Carmen Valcarce Lopez
  • Patent number: 9845328
    Abstract: The method of synthesizing vardenafil base, in anhydrous conditions, by chlorosulfonation of 2-(2-etoxy-phenyl)-5 -methyl-7-propyl-iH-imidazo[5,1-fJ[1,2,4]triazin-4-one in a mixture of thionyl chloride and sulfurochloridic acid followed by amidation of the product, 4-etoxy-3-(5-methyl-4-oxo-7-propyl-3,4-dihydroimidazo[5,1-f][1,2,4]triazin-2-yl)benzene-sulfonic acid chloride with N-ethylpiperazine, in an aprotic solvent, in the presence of an inorganic base and the method of conversion the product, vardenafil base, to yield vardenafil monohydrochloride trihydrate having a melting point of 234° C. by contacting with water of the anhydrous modification V of vardenafil monohydrochloride in an organic solvent. The subject of the invention is also the anhydrous modification V of vardenafil monohydrochloride and its use in the preparation of vardenafil monohydrochloride trihydrate having a melting point of 234° C.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: December 19, 2017
    Assignee: ZAKLADY FARMACEUTYCZNE POLPHARMA S.A.
    Inventors: Roman Szramka, Jerzy Drygas, Marcin Szulc, Robert Rynkiewicz