Patents Assigned to MSD K.K.
  • Patent number: 8846700
    Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: September 30, 2014
    Assignee: MSD K.K.
    Inventors: Tomoharu Iino, Akio Ohno, Norikazu Otake, Takuya Suga, Masanori Asai
  • Patent number: 8791125
    Abstract: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
    Type: Grant
    Filed: March 22, 2011
    Date of Patent: July 29, 2014
    Assignee: MSD K.K.
    Inventors: Takeshi Sagara, Sachie Otsuki, Satoshi Sunami, Toshihiro Sakamoto, Kenji Niiyama, Fuyuki Yamamoto, Takashi Yoshizumi, Hidetomo Furuyama, Yasuhiro Goto, Makoto Bamba, Keiji Takahashi, Hiroshi Hirai, Toshihide Nishibata
  • Patent number: 8765789
    Abstract: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: July 1, 2014
    Assignee: MSD K.K.
    Inventors: Morihiro Mitsuya, Makoto Bamba, Fumiko Sakai, Hitomi Watanabe, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki
  • Publication number: 20140011801
    Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).
    Type: Application
    Filed: September 9, 2013
    Publication date: January 9, 2014
    Applicant: MSD K.K.
    Inventors: Tomoharu Iino, Aklo Ohno, Norikazu Otake, Takuya Suga, Masanori Asai
  • Patent number: 8614221
    Abstract: The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: March 10, 2010
    Date of Patent: December 24, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Weiming Fan, Thomas F. N. Haxell, Matthew G. Jenks, Nobuhiko Kawanishi, Shuliang Lee, Hao Liu, Michael J. Malaska, Joseph A. Moore, III, Yoshio Ogino, Yu Onozaki, Bharathi Pandi, Michael R. Peel, Toshihiro Sakamoto, Tony Siu
  • Patent number: 8609699
    Abstract: The present invention relates to compounds, which are useful for treatment and/or prevention of diabetes mellitus, diabetes mellitus complications or obesity, since the compounds have glucokinase-activating effects, and are presented in Formula (I): wherein R1 represents a carbamoyl group; R2 represents a lower alkyl group; both of X1 and X2 represent CH, or any one of X1 and X2 represents a nitrogen atom and the other represents CH; a group of represents a group selected from the group consisting of a pyridinyl, a pyrazinyl, a pyrazolyl, a thiadiazolyl, a triazolyl, an isoxazolyl and a thiazolyl group; and k is zero or 1, or relates to pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 3, 2009
    Date of Patent: December 17, 2013
    Assignee: MSD K.K.
    Inventors: Tomoharu Iino, Masanori Asai, Akio Ohno, Seiichi Inamura, Makoto Ishikawa, Norikazu Ohtake
  • Patent number: 8592428
    Abstract: The present invention relates to compounds, which are useful for treatment and/or prevention of diabetes mellitus, diabetes mellitus complications or obesity, since the compounds have glucokinase-activating effects, and are presented in Formula (I): wherein R1 represents a lower alkylsulfonyl group; R2 represents a hydrogen atom; R20 represents, e.g., a hydrogen atom; m represents an integer of from 1 to 3; and n represents zero or 1, or relates to a pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 3, 2009
    Date of Patent: November 26, 2013
    Assignee: MSD K. K.
    Inventors: Hideaki Imamura, Takuya Suga, Hiroyuki Takahashi, Hideki Jona, Etsuko Hirose, Norikazu Ohtake
  • Patent number: 8575179
    Abstract: The invention relates to compounds represented by the general formula (I) and the like. In the formula, Ar1 denotes an aryl or heteroaryl group which may have a substituent; R1 denotes a hydrogen atom, or denotes a C1-C6 alkyl, aryl, aralkyl or heteroaryl group which may have a substituent; R2 denotes an aralkyl group or a group represented by the formula (a); and R3 denotes a hydrogen atom or a C1-C6 alkyl group. The compounds of the invention have an excellent Wee1 kinase inhibitory effect, and therefore are useful in the field of medicine, especially in the field of treatment of various cancers.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: November 5, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Bamba, Satoshi Sunami
  • Patent number: 8536193
    Abstract: The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: September 17, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Hidetomo Furuyama, Yasuhiro Goto, Nobuhiko Kawanishi, Mark E. Layton, Takashi Mita, Yoshio Ogino, Yu Onozaki, Michael A. Rossi, Toshihiro Sakamoto, Philip E. Sanderson, Jiabing Wang
  • Patent number: 8524730
    Abstract: The invention relates to a compound of a general formula (I): wherein A represents a linking group; Ar1 represents a group formed from an aromatic ring; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; a C1-C6 alkyl group optionally having substituent(s); an aryl or heterocyclic group optionally having substituent(s); or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom, a sulfur atom or an imino group.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: September 3, 2013
    Assignee: MSD K.K.
    Inventors: Hideki Jona, Yoshihiro Shibata, Takeru Yamakawa
  • Patent number: 8519136
    Abstract: The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R2 is CO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: August 27, 2013
    Assignee: MSD K.K.
    Inventors: Tetsuya Kato, Nobuhiko Kawanishi, Takashi Mita, Katsumasa Nonoshita, Mitsuru Ohkubo
  • Patent number: 8507505
    Abstract: The present invention relates to a compound of General Formula (I) below, among others. In the Formula, Ar1 is an optionally substituted aryl or heteroaryl group; R1 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, or an optionally substituted aryl, aralkyl, or heteroaryl group; R2 is an optionally substituted aryl, aralkyl, or heteroaryl group; and R3 is a hydrogen atom or a C1-C6 alkyl group. A compound of the present invention has an excellent Wee1 kinase inhibiting effect, and is therefore useful in the filed of medicine, particularly in various types of cancer therapy.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: August 13, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Bamba, Hidetomo Furuyama, Toshihiro Sakamoto, Satoshi Sunami, Keiji Takahashi, Fuyuki Yamamoto, Takashi Yoshizumi
  • Patent number: 8492397
    Abstract: The present invention relates to a compound of Formula (I): wherein R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R10; R5 is H, hydroxy, C1-2 alkyl, or OCH3; and R10 is F or Cl, or a pharmaceutically acceptable salt or ester thereof.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: July 23, 2013
    Assignees: Vertex Pharmaceuticals Incorporated, MSD K.K.
    Inventors: Hayley Binch, Masaya Hashimoto, Toshiharu Iwama, Nobuhiko Kawanishi, Michael Mortimore, Mitsuru Ohkubo, Tomoko Sunami
  • Patent number: 8481503
    Abstract: The invention relates to combination anticancer therapy with certain Akt inhibitor and other anticancer agents such as anticancer antimetabolites, anticancer antibiotics, plant-derived anticancer agents, anticancer platinum-coordinated complex compounds, anticancer camptothecin derivatives and anticancer tyrosine kinase inhibitors.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: July 9, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Mark E. Layton, Hiroshi Hirai, Hidehito Kotani
  • Patent number: 8455477
    Abstract: The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: June 4, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Jason Katz, James Jewell, Joon Jung, Solomon Kattar, Yongquan Hou, Rachel MacCoss, Satoru Ito
  • Patent number: 8436004
    Abstract: The invention relates to a compound of a general formula (I): wherein A1 and A2 each mean a nitrogen atom or an optionally-substituted methine group; Ring B means a 5-membered to 7-membered aliphatic ring, or a spiro or bicyclo ring formed from the aliphatic ring and any other 3-membered to 7-membered aliphatic ring; R1 means a hydrogen atom, or an optionally-substituted C1-C6 alkyl group, or an optionally-substituted aryl, aralkyl or heteroaryl group; R2 means an optionally-substituted aryl, aralkyl or heteroaryl group; and X means a group of ?NH or ?O, etc. Based on its excellent Wee1 kinase-inhibitory effect, the compound of the invention has cell growth-inhibitory effect and has an additive/synergistic effect with any other anticancer agent, and is therefore useful in the field of medicine.
    Type: Grant
    Filed: June 12, 2008
    Date of Patent: May 7, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Bamba, Hidetomo Furuyama, Kenji Niiyama, Toshihiro Sakamoto, Satoshi Sunami, Keiji Takahashi, Fuyuki Yamamoto, Takashi Yoshizumi
  • Patent number: 8420823
    Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: April 16, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
  • Publication number: 20130085156
    Abstract: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 27, 2012
    Publication date: April 4, 2013
    Applicant: MSD K.K.
    Inventor: MSD K.K.
  • Patent number: 8367690
    Abstract: The present invention relates to a compound of Formula (I): wherein: R1 is H, —NHCOOR1a, C5-6 cycloalkyl, or phenyl; where the cycloalkyl and phenyl each independently may be substituted with one to three of the same or different substituents selected from R10; R1a is C1-3 alkyl which may be substituted with one to three of the same or different substituents selected from F and Cl; R2 is H, —COOH, —CH2 COOH, —COOR2a, or —CH2COOR2a; R2a is C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from halogen atoms; R3 is H, C1-6 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R11; R10 is F, Cl, CF3, or C1-2 alkyl; R11 is halogen atom, hydroxy, or cyano; W is selected from: W2a is H, halogen atom, cyano, C1-2 alkyl, or C3-5 cycloalkyl, or a pharmaceutically acceptable salt or ester thereof.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: February 5, 2013
    Assignees: Vertex Pharmaceuticals Inc., MSD K.K.
    Inventors: Hayley Binch, Masaya Hashimoto, Michael Mortimore, Mitsuru Ohkubo, Tomoko Sunami
  • Patent number: 8367698
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: February 5, 2013
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi