Patents Examined by Erich A. Leeser
  • Patent number: 10407426
    Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.
    Type: Grant
    Filed: July 31, 2018
    Date of Patent: September 10, 2019
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Motoyuki Tanaka, Takashi Kondo, Yasuo Hirooka, Taihei Nishiyama, Atsushi Hiramatsu, Tomoyuki Koda, Sho Kouyama
  • Patent number: 10407407
    Abstract: Compounds of formula (I): wherein X, Y, R1 and R3-R11 are as herein defined, and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
    Type: Grant
    Filed: May 19, 2016
    Date of Patent: September 10, 2019
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Dominique Amans, Stephen John Atkinson, Michael David Barker, Matthew Campbell, Hawa Diallo, Clement Douault, Neil Stuart Garton, John Liddle, Jessica Fanny Renaux, Robert John Sheppard, Ann Louise Walker, Christopher Roland Wellaway, David Matthew Wilson
  • Patent number: 10398685
    Abstract: The present disclosure describes methods of treating pancreatic cancer and limiting over-expression of oncogenes, activating tumor suppressor genes or regulating signaling proteins in patients comprising administering compounds and pharmaceutical combinations as described herein.
    Type: Grant
    Filed: February 4, 2019
    Date of Patent: September 3, 2019
    Assignee: ChemoCentryx, Inc.
    Inventors: Petrus Bekker, Shichang Miao, Israel Charo, Tom Schall
  • Patent number: 10399960
    Abstract: A compound represented by formula (I) or formula (II): in formula (I), R3 represents an electron donating group, R4 represents a hydrogen atom, a substituted or unsubstituted aryl group or an electron donating group, L3 represents a substituted or unsubstituted heteroarylene group or a substituted or unsubstituted arylene group, L4 represents a single bond, a substituted or unsubstituted heteroarylene group or a substituted or unsubstituted arylene group, L3 and L4 may bond together to form a ring with the carbon atoms to which they are bonded, in formula (II), R5 represents an electron donating group, R6 represents a hydrogen atom, a substituted or unsubstituted aryl group or an electron donating group, L5 represents a substituted or unsubstituted heteroarylene group or a substituted or unsubstituted arylene group, L6 represents a single bond, a substituted or unsubstituted heteroarylene group or a substituted or unsubstituted arylene group.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: September 3, 2019
    Assignees: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION, NIPPON SODA CO., LTD.
    Inventors: Takuma Yasuda, In Seob Park, Yu Seok Yang, Hiroshi Sumiya, Yukio Fukushima
  • Patent number: 10392393
    Abstract: A compound with the formula I, wherein R2 is of formula II, where A is a C5-7 aryl group, X is selected from the group consisting of: OH, SH, CO2H, COH, N?C?O, NHNH2, CONHNH2, (III), (IV), and NHRN, wherein RN is selected from H and C1-4 alkyl, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH?CH—, and Q2 is a single bond; and its conjugates.
    Type: Grant
    Filed: January 26, 2017
    Date of Patent: August 27, 2019
    Assignee: Medimmune Limited
    Inventors: Philip Wilson Howard, Thaïs Cailleau
  • Patent number: 10391097
    Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-? or by PDE4, including but not limited to ulcerative colitis and Crohn's disease.
    Type: Grant
    Filed: August 27, 2018
    Date of Patent: August 27, 2019
    Assignee: vTv Therapeutics LLC
    Inventors: Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel
  • Patent number: 10392579
    Abstract: Photolabile pro-fragrances may include the ketones of Formula (I) Such compounds may be used in detergents, cleaning agents, cosmetic agents, air-care agents, and combinations thereof. The photolabile pro-fragrances may create a long-lasting fragrance on surfaces or in a room using the aforementioned pro-fragrances.
    Type: Grant
    Filed: September 14, 2016
    Date of Patent: August 27, 2019
    Assignee: HENKEL AG & CO. KGAA
    Inventors: Christian Kropf, Thomas Gerke, Ursula Huchel, Axel Griesbeck, Agnieszka Landes
  • Patent number: 10385052
    Abstract: Novel tricyclic compounds which have JAK inhibitory activities are useful for prevention, treatment or improvement of autoimmune diseases, inflammatory diseases and allergic diseases are provided. Novel tricyclic compound represented by the formula (I), the formula (II) or the formula (III) (wherein: each of A1, A2 and A3 is a cyclohexane-1,4-diyl group or the like; each of L1, L2 and L3 is a methylene group or the like; each of X1 and X3 is O or NH; each of R1 and R3 is a cyano C1-6 haloalkyl group or the like; and R2 is an aromatic heterocyclic group), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: August 20, 2019
    Assignee: Nissan Chemical Corporation
    Inventors: Tsuneo Watanabe, Keiji Takahashi, Keishi Hayashi, Takanori Nakamura, Masataka Minami, Kazunori Kurihara, Akio Yamamoto, Takuya Nishimura, Miyuki Uni, Toshihiko Kamiyama, Shunsuke Iwamoto
  • Patent number: 10385045
    Abstract: Provided is an EP2 agonist having excellent safety. A compound represented by general formula (I) (wherein all symbols are as defined in the description), a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has an EP2 agonist activity and is highly safe, and is therefore useful as a medicine, particularly a therapeutic agent for diseases associated with EP2 receptors, such as immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases and cartilage injury.
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: August 20, 2019
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Seiji Ogawa, Toshihide Watanabe, Isamu Sugimoto, Kousuke Tani, Kazumi Moriyuki, Yoshikazu Goto, Shinsaku Yamane
  • Patent number: 10385038
    Abstract: The present invention discloses a crystal of citrate salt of pyridine-substituted 2-aminopyridine-based protein kinase inhibitors, in particular, to crystal of 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4?-methoxy-6?-((S)-2-methylpiperazin-1-yl)-3,3?-bipyridin-6-amine citrate salt, a method for preparation thereof, a crystalline composition and a pharmaceutical composition comprising the crystal, and further discloses the use of crystals of citrate salt of the compound of Formula I in protein kinase-related diseases. The crystals of citrate salt according to the present invention are superior to 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4?-methoxy-6?-((S)-2-methylpiperazin-1-yl)-3,3?-bipyridin-6-amine or other salts of 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4?-methoxy-6?-((S)-2-methylpiperazin-1-yl)-3,3?-bipyridin-6-amine in at least one aspect of bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation, and the like.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: August 20, 2019
    Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD., CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Feng Gong, Xinlu Li, Rui Zhao, Xiquan Zhang, Xinhe Xu, Xijie Liu, Dengming Xiao, Yongxin Han
  • Patent number: 10370346
    Abstract: Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
    Type: Grant
    Filed: August 2, 2017
    Date of Patent: August 6, 2019
    Assignee: Imago Biosciences, Inc.
    Inventors: John M. McCall, Hugh Y. Rienhoff, Jr., Michael Clare
  • Patent number: 10370381
    Abstract: Provided are forms of 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one, compositions thereof, methods for their preparation, and methods for their use.
    Type: Grant
    Filed: February 23, 2018
    Date of Patent: August 6, 2019
    Assignee: Gilead Sciences, Inc.
    Inventor: Bing Shi
  • Patent number: 10370356
    Abstract: The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy
    Type: Grant
    Filed: September 20, 2016
    Date of Patent: August 6, 2019
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Stephen John Atkinson, Emmanuel Hubert Demont, Lee Andrew Harrison, Thomas George Christopher Hayhow, David House, Matthew J. Lindon, Alexander G. Preston, Jonathan Thomas Seal, Ian David Wall, Robert J. Watson, James Michael Woolven
  • Patent number: 10358427
    Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of HIV; including the prevention of the progression of AIDS and general immunosuppression.
    Type: Grant
    Filed: September 22, 2016
    Date of Patent: July 23, 2019
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Pek Yoke Chong, Martha Alicia De La Rosa, Hamilton D. Dickson, Wieslaw Mieczyslaw Kazmierski, Vicente Samano, Vincent Wing-Fai Tai
  • Patent number: 10351571
    Abstract: The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R5, R5?, R6, X1, X2, m, and n are described herein.
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: July 16, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell
  • Patent number: 10350206
    Abstract: Compounds of formula (I) as defined herein and their use as pharmaceuticals.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: July 16, 2019
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Anne Mengel, Hans-Georg Lerchen, Manfred Möwes, Thomas Müller, Lars Bärfacker, Marion Hitchcock, Arwed Cleve, Joachim Kuhnke, Hans Briem, Gerhard Siemeister, Wilhelm Bone, Amaury Ernesto Fernandez-Montalvan, Jens Schröder, Ursula Mönning, Simon Holton
  • Patent number: 10336747
    Abstract: Pyrimido[4,5-b]indole derivatives are provided. These compounds are useful to expand hematopoietic stem cell populations, particularly, human hematopoietic stem cell populations. The compounds are also useful in the medical treatment of diseases that involve hematopoietic stem cells.
    Type: Grant
    Filed: December 2, 2016
    Date of Patent: July 2, 2019
    Assignee: UNIVERSITÉ DE MONTRÉAL
    Inventors: Guy Sauvageau, Yves Gareau, Rejean Ruel, Stephane Gingras, Iman Fares
  • Patent number: 10336729
    Abstract: The invention relates to new benzonitrile derivatives of the formula (I) wherein R1 to R3 and A are as defined in the description and Claims, to their medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: March 3, 2016
    Date of Patent: July 2, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Andreas Blum, Stefan Peters
  • Patent number: 10336758
    Abstract: The invention is directed towards stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid and its hemisulfate salt as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: July 2, 2019
    Assignee: MERCK & CIE
    Inventors: Rudolf Moser, Viola Groehn, Thomas Egger, Thomas Ammann
  • Patent number: 10329282
    Abstract: The present invention relates to a Rho-associated protein kinase inhibitor of Formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and use thereof for the prevention or treatment of a disease mediated by the Rho-associated protein kinase (ROCK).
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: June 25, 2019
    Assignee: BEIJING TIDE PHARMACEUTICAL CO., LTD.
    Inventors: Yanping Zhao, Hongjun Wang, Gong Li, Yuanyuan Jiang, Xiang Li, Liying Zhou, Yanan Liu