Patents Assigned to 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: 8362052
    Abstract: The present invention relates to a compound represented by formula (I): (wherein R, R2, R3 and R4 each independently represent a hydrogen or halogen atom; R5 and R6 each independently represent a hydrogen atom or lower alkyl or together represent oxo; X represents C(O) or the like; Y represents an oxygen atom or the like; Z represents a hydrogen atom or the like; R represents 5- or 6-membered heteroaryl having 1-3 hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms, contained within a ring, or the like) or to a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: January 29, 2013
    Assignee: MSD K.K.
    Inventors: Keisuke Arakawa, Teruyuki Nishimura, Yuichi Sugimoto, Hiroyuki Takahashi, Tadashi Shimamura
  • Patent number: 8344003
    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: October 23, 2009
    Date of Patent: January 1, 2013
    Assignee: MSD K. K.
    Inventors: Morihiro Mitsuya, Makoto Bamba, Fumiko Sakai, Hitomi Watanabe, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki
  • Patent number: 8338460
    Abstract: Compounds of a formula (I) and their pharmaceutically-acceptable salts are disclosed. The compounds have glucokinase-activating effect and are therefore useful for treatment of diabetes and obesity. R1 and R2 each independently represent a lower alkyl group; X1 represent a group of a formula (II-1): wherein: R11 and R12 each independently represent a hydrogen atom or a lower alkyl group, or taken together with the nitrogen atom to which they bond, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring (one carbon atom constituting the 4- to 7-membered nitrogen-containing aliphatic ring may be replaced by an oxygen atom), or taken together with a carbon atom in (CH2)m, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring; m indicates an integer of from 1 to 3.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: December 25, 2012
    Assignee: MSD K. K.
    Inventors: Noriaki Hashimoto, Yufu Sagara, Masanori Asai, Teruyuki Nishimura
  • Patent number: 8329711
    Abstract: The invention relates to compounds of general formula (I-0): wherein R1, R2, R3, R4, R5, R6, R7a, R8a, X, and Y are as defined herein. Compounds of the invention have, based on excellent Wee1 kinase-inhibitory effect, a cell growth-inhibitory effect and an additive/synergistic effect with any other anticancer agent, and are therefore useful in the field of medicine.
    Type: Grant
    Filed: October 20, 2008
    Date of Patent: December 11, 2012
    Assignee: MSD K.K.
    Inventors: Hidetomo Furuyama, Mikako Kawamura, Toshihiro Sakamoto, Fuyuki Yamamoto, Takashi Yoshizumi
  • Patent number: 8314094
    Abstract: [PROBLEMS] To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases. [MEANS FOR SOLVING PROBLEMS] The compound, which is for use as an active ingredient, is represented by the formula (I): [wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4) (wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents —O—, —NH—, etc.; and Y1, Y2, Y3, and Y4 each independently represents —CH—, —N—, etc.].
    Type: Grant
    Filed: October 2, 2008
    Date of Patent: November 20, 2012
    Assignee: MSD K.K
    Inventors: Shiho Ishikawa, Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi
  • Patent number: 8268842
    Abstract: The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: September 18, 2012
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
  • Patent number: 8263632
    Abstract: The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is 0 or CH2; 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 or OCH3; R10 is F or Cl; or a pharmaceutically acceptable salt or ester thereof
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: September 11, 2012
    Assignees: Vertex Pharmaceuticals Incoporated, MSD K.K.
    Inventors: Toshiharu Iwama, Nobuhiko Kawanishi, Michael Mortimore, Mitsuru Ohkubo, Tomoko Sunami
  • Patent number: 8232447
    Abstract: It is an object to provide a gene-modified non-human animal having inactivated MGAT2 gene and a gene-modified non-human animal cell, which are useful for the search of the function of MGAT2 in vivo. It is another object to provide a method for screening of a compound capable of inhibiting the activity of MGAT2 and a compound capable of inhibiting the activity of MGAT2. It is further another object to provide a method for detecting a disease induced by abnormal lipid metabolism based on the expression level or activity of MGAT2. A method for screening of a compound by using a gene-modified non-human mammal having the artificially inhibited expression of MGAT2 gene and a cell thereof enable to prevent or treat a disease induced by abnormal lipid metabolism. Also a screening of a compound capable of inhibiting or enhancing the function of MGAT2 enables to prevent or treat a disease induced by abnormal lipid metabolism.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: July 31, 2012
    Assignee: MSD K.K.
    Inventors: Katsumi Aragane, Katsuya Ohbuchi, Yoshitaka Tamai, Naomoto Harada, Naomi Murai, Yoshiki Ito, Jun Kusunoki, Yukina Tokushima, Takaharu Maruyama
  • Patent number: 8232284
    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: November 10, 2008
    Date of Patent: July 31, 2012
    Assignee: MSD K. K.
    Inventors: Tomoharu Iino, Akio Ohno, Norikazu Otake, Takuya Suga, Masanori Asai
  • Patent number: 8207169
    Abstract: The compounds of Formula D are of the class of triazolo-pyrido-pyrazines which are inhibitors of AKT useful for the treatment of cancer
    Type: Grant
    Filed: May 28, 2009
    Date of Patent: June 26, 2012
    Assignee: MSD K.K.
    Inventors: Hidetomo Furuyama, Yasuhiro Goto, Nobuhiko Kawanishi, Mark E. Layton, Takashi Mita, Akira Naya, Yoshio Ogino, Yu Onozaki, Kevin J. Rodzinak, Toshihiro Sakamoto, Philip E. Sanderson, Jiabing Wang
  • Patent number: 8188280
    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: February 4, 2009
    Date of Patent: May 29, 2012
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Patent number: 8163898
    Abstract: [PROBLEMS] To provide compounds useful as preventives or remedies for circulatory diseases, nervous diseases, metabolic diseases, reproductive system diseases, and digestive diseases. [MEANS FOR SOLVING PROBLEMS] Compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof: wherein R1 is C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 is phenyl, heteroaryl, or the like; Q is N or CH; and M1, M2, M3 and M4 are each independently hydrogen or C1-6 alkyl, or alternatively M1 together with M2 or M3 forms —CH2-CH2- or the like, or M4 together with M2 or M3 forms —CH2-CH2- or the like, with the proviso that M1, M2, M3, and M4 are such that one —CH2- or —CH2-CH2- group is formed thereamong.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: April 24, 2012
    Assignee: MSD K. K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Patent number: 8163770
    Abstract: Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof. This compound is useful for treatment of obesity, diabetes and the like. [In the formula (I), Ar represents a benzene ring or the like; X1 represents a nitrogen atom, a sulfur atom or the like; R1 represents an aryl group or the like; X2 represents a group represented by the following formula (II): (wherein R4 and R5 respectively represent a lower alkyl group or the like, and m represents a number of 2-4) or the like; one of X and Y represents an oxygen atom and the other represents a sulfanyl group or the like; and X3-X6 respectively represent —CH—, a nitrogen atom or the like.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: April 24, 2012
    Assignee: MSD. K. K.
    Inventors: Takashi Mizutani, Nagaaki Sato, Takahide Sasaki, Toshiyuki Takahashi
  • Patent number: 8158791
    Abstract: A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: [wherein X, Y, Z and W each independently represent a methine group or a nitrogen atom, provided that a case where all of X, Y, Z and W are methine group; A represents —O— or the like, B represents —C(O)— or the like, D represent —(CH2)m2-, —O— or the like, and m2 represents 0 or 1; Q represents a methine group or a nitrogen atom; and R represents a group represented by the following formula (II-1) (wherein R6, R7 and R8 independently represent a lower alkyl group or the like].
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: April 17, 2012
    Assignee: MSD K.K.
    Inventors: Makoto Jitsuoka, Nagaaki Sato, Daisuke Tsukahara
  • Patent number: 8158652
    Abstract: Compounds of a formula (I) [wherein, A represents formula (III-1) R3 is a hydrogen, lower alkyl et al; m is 0 or 1; R1 is a hydrogen atom, halogen atom et al, R2 is a hydrogen et al; p is 0 to 4; X is a carbon atom or nitrogen atom; and X1 to X4 is a lower alkyl et al], or pharmaceutical acceptable salts thereof. These have a potency antagonistic to binding to histamine H3 receptor, or have a potency inhibiting the constant activity of histamine H3 receptor, and are useful in the therapy of obesity, diabetes et al.
    Type: Grant
    Filed: November 30, 2005
    Date of Patent: April 17, 2012
    Assignee: MSD K.K.
    Inventors: Norikazu Ohtake, Takuya Suga, Shigeru Tokita
  • Patent number: 8138197
    Abstract: The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-a]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; 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 C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl 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; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; 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 n
    Type: Grant
    Filed: January 8, 2008
    Date of Patent: March 20, 2012
    Assignees: MSD K.K., Merck Sharp & Dohme Corp.
    Inventors: Tomoharu Iino, Hideki Jona, Hideki Kurihara, Masayuki Nakamura, Kenji Niiyama, Jun Shibata, Tadashi Shimamura, Hitomi Watanabe, Takeru Yamakawa, Lihu Yang
  • Patent number: 8138206
    Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.
    Type: Grant
    Filed: May 29, 2006
    Date of Patent: March 20, 2012
    Assignee: MSD. K.K.
    Inventors: Shiho Ishikawa, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi, Shigeru Tokita, Toshihiro Wada
  • Patent number: 8124807
    Abstract: [Problem] To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I): [wherein, Z represents formula (II-1), (II-2), or (II-3), wherein m and n are 0, 1, or 2, Y represents CR3 or N, R1 represents a C1-6 alkyl, C3-8 cycloalkyl, etc., R2 represents phenyl or a heteroaryl, etc., R3 and R4 each independently represent a hydrogen atom, a C1-6 alkyl, etc., M1, M2, M3, and M4 each independently represent a hydrogen atom, a C1-6 alkyl, etc.
    Type: Grant
    Filed: December 16, 2008
    Date of Patent: February 28, 2012
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Publication number: 20120035155
    Abstract: To provide an indole compound having a human QRFP receptor antagonistic activity and useful as a preventive or a remedy for various disorders. A compound of a formula (I) or a pharmaceutically-acceptable salt thereof is provided: [wherein, R1 represents a hydrogen atom, a halogen, a C1-6 alkyl, etc,; R2 represents a C1-6 alkyl, or a halo-C1-6 alkyl; R3 represents a hydrogen atom, a C1-6 alkyl, etc.; R4 represents a hydrogen atom, a C1-6 alkyl, a halo-C1-6 alkyl, etc.; or R3 and R4, taken together with the nitrogen atom to which they bond, form a 3- to 6-membered aliphatic nitrogen-containing hetero ring; or R3 and Y3, taken together, form —CH2—CH2—; Y1 and Y2 are both hydrogen atoms; or Y1 and Y2, taken together, form —CH2—CH2—; and Y3 represents a hydrogen atom; or Y3 and R3, taken together, form —CH2—CH2—].
    Type: Application
    Filed: April 17, 2010
    Publication date: February 9, 2012
    Applicant: MSD K.K.
    Inventors: Yuji Haga, Sayaka Mizutani, Nagaaki Sato