Patents Assigned to MSD K.K.
  • Publication number: 20120028970
    Abstract: The present invention relates to a compound represented by a formula (I): wherein X is a group represented by or the like; Y is a group represented by or the like; and Ar1 is a group represented by or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 27, 2010
    Publication date: February 2, 2012
    Applicant: MSD K.K.
    Inventors: Minoru Kameda, Kensuke Kobayashi, Chisato Nakama, Makoto Ando, Nagaaki Sato
  • Publication number: 20120029041
    Abstract: 2-Aryl imidazoline derivatives are provided that are useful as anti-obesity agents or the like. A compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 each independently represent a hydrogen atom, halogen, C1-6alkyl, or the like; R3a, R3b, R4a and R4b each independently represent a hydrogen atom, C1-6alkyl, or haloC1-6alkyl; and Ar represents aryl, wherein the aryl may be substituted with 1 to 3 substituents such as halogen, cyano, C1-6alkyl, haloC1-6alkyl, C1-6alkyloxy, haloC1-6alkyloxy, hydroxy, amino, monoC1-6alkylamino, diC1-6alkylamino, and C1-6alkyloxy-carbonyl.
    Type: Application
    Filed: April 21, 2010
    Publication date: February 2, 2012
    Applicant: MSD K.K.
    Inventors: Yuji Haga, Minoru Moriya, Toshiyuki Takahashi
  • Patent number: 8106086
    Abstract: A compound represented by the general formula (I-a): [wherein R1a and R2a each means hydrogen, lower cycloalkyl, lower alkyl, etc.; R3a means hydrogen, lower cycloalkyl, lower alkyl, etc.; R4a and R5a each means lower alkyl, lower cycloalkyl, etc. or R4a and R5a are bonded to each other to form lower cycloalkylidene; and R6a means lower alkyl, lower haloalkyl, etc.]. This compound functions as an LCE inhibitor and is useful as a therapeutic agent for various circulatory diseases, nervous diseases, metabolic diseases, reproductive diseases, digestive tract diseases, neoplasm, infectious diseases, etc.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: January 31, 2012
    Assignee: MSD K.K.
    Inventors: Toshiyuki Takahashi, Tsuyoshi Nagase, Nagaaki Sato
  • Publication number: 20120022078
    Abstract: A novel aryl indole derivative is provided that is effective as a preventive or remedy for various diseases. A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1 is a hydrogen atom, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkyloxy, or haloC1-6alkyloxy; R2 represents C1-6alkyl or haloC1-6alkyl; R3 represents a hydrogen atom, C1-6alkyl, or haloC1-6alkyl; and Ar represents an aryl or heteroaryl, wherein the aryl or the heteroaryl may be substituted with 1 to 3 substituents such as halogen, C1-6alkyl, haloC1-6alkyl, and C1-6alkyloxy.
    Type: Application
    Filed: April 7, 2010
    Publication date: January 26, 2012
    Applicant: MSD K.K.
    Inventors: Hiroyuki Kishino, Sayaka Mizutani, Shunji Sakuraba, Nagaaki Sato
  • Patent number: 8101618
    Abstract: A compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 represents a branched lower alkyl group having from 3 to 9 carbon atoms or the like; R2 represents a 6-membered heteroaryl group having 1 or 2 nitrogen atoms or the like; R3 represents a hydrogen atom, an alkanoylamino group or the like; R4 represents a hydrogen atom, a lower alkyl group or the like; X1 represents an oxygen atom or a sulfur atom; X2 represents an oxygen atom or a single bond; and m indicates an integer of from 0 to 4. This compound has a metabotropic glutamate receptor 1 inhibitory effect, and therefore is useful for the treatment of a brain disorder such as convulsion, acute pain, inflammatory pain, chronic pain, cerebral infraction or transient cerebral ischemic attack, a mental dysfunction such as schizophrenia, and a disease such as anxiety and drug addition.
    Type: Grant
    Filed: April 5, 2006
    Date of Patent: January 24, 2012
    Assignee: MSD K.K.
    Inventors: Hiroshi Kawamoto, Toshifumi Kimura, Hisashi Ohta, Akio Sato, Atsushi Satoh, Gentaroh Suzuki
  • Patent number: 8101621
    Abstract: The present invention relates to a compound of general formula I: wherein: n1 and n2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; Re is hydrogen atom or lower alkyl; two groups selected from four groups consisting of (i) either one of Ra1 and Ra1?, (ii) either one of Ra2 and Ra2?, (iii) either one of Rb1 and Rb1?, and (iv) either one of Rb2 and Rb2?, are combined to form —(CH2)n— where n is 1, 2 or 3; and among Ra1, Ra1?, Ra2, Ra2?, Rb1, Rb1?, Rb2 and Rb2?, the groups which do not form —(CH2)n— are each independently hydrogen atom, etc.; X1, X2, X3 and X4 are each independently CH, N, etc.; Y1, Y2, Y3 and Y4 are the same or different and are CH or N, etc.; W is a 5-membered aromatic heterocyclic group, or a pharmaceutically acceptable salt or ester thereof.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: January 24, 2012
    Assignee: MSD K.K.
    Inventors: Tetsuya Kato, Nobuhiko Kawanishi, Takashi Mita, Keita Nagai, Katsumasa Nonoshita, Mitsuru Ohkubo
  • Publication number: 20120015938
    Abstract: The present invention relates to a compound represented by a formula (I): wherein R1 represents a halogen atom or the like; R2 represents a hydrogen atom or the like; R3 and R4 each independently represents lower alkyl; R5 represents phenyl or the like; R6 represents a halogen atom or the like; m is an integer of from 0 to 2; p is an integer of from 1 to 4; and q is an integer of from 1 to 5 as an inhibitor of DGAT1 and its use for the treatment of hyperlipidemia etc.
    Type: Application
    Filed: February 12, 2010
    Publication date: January 19, 2012
    Applicant: MSD K.K.
    Inventors: Masanori Asai, Tasuku Haketa, Seiichi Inamura, Hideki Kurihara, Teruyuki Nishimura, Tadashi Shimamura
  • Patent number: 8093389
    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 indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R1 and R2 each 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; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R3 and R4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-C
    Type: Grant
    Filed: January 8, 2008
    Date of Patent: January 10, 2012
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Tomoharu Iino, Hideki Jona, Jun Shibata, Tadashi Shimamura, Takeru Yamakawa, Lihu Yang
  • Publication number: 20110319396
    Abstract: The present invention relates to a compound represented by the formula (I): wherein R1 represents a hydrogen atom or the like; R2 represents lower alkyl or the like; R3 and R4 represent lower alkyl or the like; R5 represents phenyl or the like; R6 represents a hydrogen atom or the like; m is an integer of from 0 to 2; p is an integer of from 1 to 4; and q is an integer of from 1 to 5, or a pharmaceutical acceptable salt thereof, and a DGAT 1 inhibitor comprising the compound.
    Type: Application
    Filed: January 19, 2010
    Publication date: December 29, 2011
    Applicant: MSD K.K.
    Inventors: Masanori Asai, Tasuku Haketa, Seiichi Inamura, Makoto Ishikawa, Hideki Jona, Hiroshi Kawamoto, Hideki Kurihara, Jun Shibata, Tadashi Shimamura, Takuya Suga, Hitomi Watanabe
  • Publication number: 20110312976
    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: Application
    Filed: March 9, 2010
    Publication date: December 22, 2011
    Applicant: MSD K.K.
    Inventors: Keisuke Arakawa, Teruyuki Nishimura, Yuichi Sugimoto, Hiroyuki Takahashi, Tadashi Shimamura
  • Publication number: 20110275647
    Abstract: The present invention relates to a compound represented by a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 represents lower alkyl or the like; R2 represents phenyl or the like; R represents a halogen atom or the like; X represents an oxygen atom or the like; Y1, Y2, Y3 and Y4 represent CH or the like; l represents an integer of from 0 to 3; m and n each represent an integer of 1 or 2; p represents an integer of from 0 to 2; and q represents an integer of from 1 to 3.
    Type: Application
    Filed: February 22, 2010
    Publication date: November 10, 2011
    Applicant: MSD K.K.
    Inventors: Keisuke Arakawa, Yoshiki Ito, Hiroshi Kawamoto, Junichi Sakaki, Tadashi Shimamura
  • Patent number: 8044070
    Abstract: Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II): or the following formula (III): Y represents a group of a formula (IV): The compounds have a histamine-H3 receptor antagonistic or inverse-agonistic activity and are useful for remedy and/or prevention of obesity, diabetes, hormone secretion disorders, sleep disorders, etc.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: October 25, 2011
    Assignee: MSD K.K.
    Inventors: Norikazu Ohtake, Akira Naya, Yuji Haga, Makoto Jitsuoka, Takuya Suga, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani
  • Patent number: 7994331
    Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein X1 to X4 independently represent a carbon atom or the like; the ring A represents a 5- to 6-membered heteroaryl having 1 to 4 heteroatoms independently selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom; X5 represents an oxygen atom or the like; X represents a carbon atom or the like; Het represents a 5- or 6-membered aliphatic heterocycle; R1 represents an aryl or the like; R2 represents a formyl group or the like; and R3 represents a —C1-6 alkyl or the like. The compound or salt has a glucokinase activation effect and is useful as a therapeutic agent for diabetes.
    Type: Grant
    Filed: July 12, 2006
    Date of Patent: August 9, 2011
    Assignee: MSD K.K.
    Inventors: Yoshio Ogino, Katsumasa Nonoshita, Teruyuki Nishimura, Jun-ichi Eiki
  • Patent number: 7935712
    Abstract: The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.
    Type: Grant
    Filed: July 14, 2006
    Date of Patent: May 3, 2011
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Takeru Yamakawa, Hideki Jona, Kenji Niiyama, Koji Yamada, Tomoharu Iino, Mitsuru Ohkubo, Hideaki Imamura, Jun Shibata, Jun Kusunoki, Lihu Yang
  • Patent number: 7935708
    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: April 25, 2007
    Date of Patent: May 3, 2011
    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: 7932394
    Abstract: A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided. The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.
    Type: Grant
    Filed: November 1, 2005
    Date of Patent: April 26, 2011
    Assignee: MSD K.K.
    Inventors: Noriaki Hashimoto, Keiji Takahashi, Chisato Nakama, Yoshio Ogino, Fumiko Sakai, Teruyuki Nishimura, Jun-ichi Eiki