Patents Represented by Attorney, Agent or Law Firm Richard C. Billups
  • Patent number: 7968589
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: June 28, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John E. Stelmach, Emma R. Parmee, James R. Tata, Keith G. Rosauer, Ronald M. Kim, Amy R. Bittner, Jiang Chang, Christopher Joseph Sinz
  • 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
  • Patent number: 7803951
    Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: March 24, 2006
    Date of Patent: September 28, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Rui Liang, Emma R. Parmee
  • Patent number: 7799818
    Abstract: Pyrazoles having a naphthyl group attached are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: September 21, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Emma R. Parmee, Yusheng Xiong, Jian Guo, Rui Liang, Linda Brockunier
  • Patent number: 7799820
    Abstract: Disclosed is a compound represented by the formula (I) below, which has a glucokinase-activating effect and is thus useful for treatment of diabetes or obesity, or a pharmaceutically acceptable salt thereof. In the formula, R1 represents an aryl or the like; R11 represents an aryl or the like; R2 represents a formyl or the like, R3 represents a C1-6 alkyl or the like; R3 represents a hydrogen atom or the like; Z1 represents —O— or the like; Z2 represents —O— or the like; Y1-Y4 respectively represent a carbon atom or a nitrogen atom; ring A represents a heteroaryl group; X represents a carbon atom or the like; m represents an integer of 0-2; and q represents an integer of 0-2.
    Type: Grant
    Filed: September 29, 2006
    Date of Patent: September 21, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Keiji Takahashi, Yoshio Ogino, Teruyuki Nishimura
  • Patent number: 7767881
    Abstract: To clarify histamine receptor H3 protein function in vivo, the present inventors constructed a nonhuman higher animal in which the expression of a histamine receptor H3 gene was artificially inhibited. As a result, the present inventors found that this nonhuman higher animal showed increased body weight, food intake, blood insulin level, or blood leptin level compared with a control. Thus, the present inventors found that abnormalities in the histamine receptor H3 protein relate to diseases characterized by changes in body weight or food intake, and this has made it possible to screen drugs for treatment or prevention of these diseases, and to examine these diseases.
    Type: Grant
    Filed: June 28, 2002
    Date of Patent: August 3, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hidehito Kotani, Kazuhiko Takahashi, Hiroaki Suwa
  • Patent number: 7754743
    Abstract: Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): [wherein X1 represents oxygen, etc., X2 represents oxygen, etc., R1 represents a group on Ring A such as alkylsulfonyl, etc., R2 represents C3-7 cyclic alkyl optionally substituted with a halogen, etc., R3 represents a substituent on Ring B such as lower alkyl, etc., formula (II): [Chemical Formula 1] represents 6- to 10-membered aryl, etc., and formula (III): [Formula 1] represents monocyclic or bicyclic heteroaryl optionally having on Ring B a substituent represented by R3 above, wherein the carbon atom of Ring B which is bonded to the nitrogen atom of the amide group of formula (I) forms a C?N bond with the nitrogen atom of the ring], as well as their pharmaceutically acceptable salts.
    Type: Grant
    Filed: September 5, 2008
    Date of Patent: July 13, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Tomoharu Iino, Noriaki Hashimoto, Hiroshi Nakashima, Keiji Takahashi, Teruyuki Nishimura, Jun-ichi Eiki
  • Patent number: 7728025
    Abstract: A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided. A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R1 represents an aryl, etc.; R2 represents a hydroxy, etc.; R3 represents a —C1-6 alkyl, etc.; R4 represents a —C1-6 alkyl, etc.; X5 represents —O—, etc.
    Type: Grant
    Filed: December 28, 2004
    Date of Patent: June 1, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Katsumasa Nonoshita, Makoto Ishikawa, Hiroshi Nakashima, Daisuke Tsukahara, Yoshio Ogino, Fumiko Sakai, Yoshikazu Nagae, Keisuke Arakawa, Teruyuki Nishimura
  • Patent number: 7709658
    Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.
    Type: Grant
    Filed: July 21, 2006
    Date of Patent: May 4, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lushi Tan, James Christopher McWilliams, Frederick W. Hartner, Naoki Yoshikawa, Wenji Li
  • Patent number: 7687534
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: March 30, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John E. Stelmach, Emma R. Parmee, James R. Tata, Keith G. Rosauer, Ronald M. Kim, Amy R. Bittner, Jiang Chang, Christopher Joseph Sinz
  • Patent number: 7687502
    Abstract: The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R1 is an optionally substituted five to six-membered heteroaryl group, etc.; R2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 23, 2005
    Date of Patent: March 30, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Morihiro Mitsuya, Makoto Bamba, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki, Keisuke Arakawa
  • Patent number: 7683218
    Abstract: Disclosed is an efficient and widely-applicable method for commercially producing a thioether compound or a thiol compound which is useful as a pharmaceutical compound or a production intermediate of it. Specifically disclosed is a method for producing a thioether compound represented by the general formula [I] below or a salt thereof. This method is characterized in that a compound represented by the following general formula [III]: [III] (wherein X represents a bromine atom, a chlorine atom or a trifluoromethylsulfonyloxy group, and ring A represents an aryl group or a heteroaryl ring group) or a salt thereof is reacted with a thiol compound represented by the following general formula [II]: [II] or a salt thereof in the presence of a palladium compound such as Pd2(dba)3, a base such as i-Pr2NEt and a phosphorus compound represented by the following formula [AA].
    Type: Grant
    Filed: October 7, 2005
    Date of Patent: March 23, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takahiro Itoh, Toshiaki Mase, Atsushi Akao
  • Patent number: 7683092
    Abstract: Novel crystalline forms of two indole compounds connected to phenoxyalkylcarboxylic acid groups are selective PPAR gamma partial agonists that are useful in the treatment of type 2 diabetes, hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. The novel crystal forms include a crystalline free acid dihydrate and crystalline free acid anhydrate of one compound and several crystalline forms of the free acid and the sodium salt of the second compound. The invention also relates to pharmaceutical compositions comprising these novel crystal forms, processes to prepare the crystal forms and their pharmaceutical compositions, and uses of the crystal forms in the treatment of type 2 diabetes and other PPAR gamma modulated diseases.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: March 23, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dalian Zhao, Jean-Francois Marcoux, David Boardman, Aquiles E. Leyes
  • Patent number: 7649009
    Abstract: Pyrazole amides are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: January 19, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Teresa Beeson, Linda Brockunier, Emma R. Parmee, Subharekha Raghavan
  • Patent number: 7629362
    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: February 13, 2004
    Date of Patent: December 8, 2009
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Morihiro Mitsuya, Makoto Bamba, Fumiko Sakai, Hitomi Watanabe, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki
  • Patent number: 7625938
    Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.
    Type: Grant
    Filed: July 19, 2005
    Date of Patent: December 1, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Linda Brockunier, Jian Guo, Rui Liang, Emma R. Parmee, Subharekha Raghavan, George Scott Tria, Yusheng Xiong
  • Patent number: 7625933
    Abstract: Indoles of Formula I having —X-aryl-(CH2)x-oxazolidinedione and —X-heteroaryl-(CH2)x-oxazolidinedione substituents on the N atom of the indole ring, where x is 0 or 1, and —X— is a bond or —CH2—, and their thiazolidinedione analogs, are PPAR gamma agonists or partial agonists and are useful in the treatment and control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
    Type: Grant
    Filed: June 28, 2005
    Date of Patent: December 1, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Kun Liu, Peter T. Meinke, Harold B. Wood
  • Patent number: 7598398
    Abstract: The present invention relates to substituted indoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus and related conditions.
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: October 6, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Ronald M. Kim, Amy R. Bittner, Christopher Joseph Sinz, Emma R. Parmee
  • Patent number: 7598285
    Abstract: Pyrazoles having a naphthyl group attached are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: October 6, 2009
    Assignee: Merck & Co., Inc
    Inventors: Emma R. Parmee, Yusheng Xiong, Jian Guo, Rui Liang, Linda Brockunier
  • Patent number: 7572922
    Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.
    Type: Grant
    Filed: January 23, 2004
    Date of Patent: August 11, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Emma Parmee, Subharekha Raghavan, Teresa Beeson, Dong-Ming Shen