Title:
PDK4 INHIBITOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2014/103321
Kind Code:
A1
Abstract:
[Problem] The problem of the present invention is to provide a novel pyruvate dehydrogenase inhibitor. [Solution] Provided are a pyruvate dehydrogenase inhibitor comprising the compound represented by general formula (I) as the active ingredient (where in the formula, ring A is a six-member hydrocarbon ring having aromaticity that is optionally substituted by two to four substitution groups, R1 and R4 are the same or different and are, for instance, a hydrogen atom, hydroxyl group, or optionally substituted C1-6 alkyl group, and R2 and R3 are the same or different and are a hydrogen atom, carboxyl group, optionally substituted C1-6 alkyl group, C6-10 aryl group, or -C(=R9)-R10); a medical composition which comprises the pyruvate dehydrogenase kinase inhibitor as the active ingredient and which is for treating or preventing a disease or an impairment the development or deterioration of which is associated with pyruvate dehydrogenase kinase; and a cosmetic composition, and the like.
Inventors:
OMURA SATOSHI (JP)
NAKANO HIROFUMI (JP)
YAMAJI KENZABURO (JP)
YAMAMOTO TSUYOSHI (JP)
KIDO HIROSHI (JP)
YAMANE KAZUHIKO (JP)
SUNAZUKA TOSHIAKI (JP)
HIROSE TOMOYASU (JP)
NAKANO HIROFUMI (JP)
YAMAJI KENZABURO (JP)
YAMAMOTO TSUYOSHI (JP)
KIDO HIROSHI (JP)
YAMANE KAZUHIKO (JP)
SUNAZUKA TOSHIAKI (JP)
HIROSE TOMOYASU (JP)
Application Number:
PCT/JP2013/007649
Publication Date:
July 03, 2014
Filing Date:
December 26, 2013
Export Citation:
Assignee:
KITASATO INST (JP)
UNIV TOKUSHIMA (JP)
UNIV TOKUSHIMA (JP)
International Classes:
A61K31/122; A61K31/015; A61P1/14; A61P13/02; A61P31/16; A61P35/00; A61P43/00
Domestic Patent References:
| WO2006137190A1 | 2006-12-28 | |||
| WO2007111324A1 | 2007-10-04 |
Other References:
JUNJIAN WANG ET AL.: "Kaempferol is an estrogen-related receptor a and y inverse agonist", FEBS LETTERS, vol. 583, 2009, pages 643 - 647, XP025947014
CHEMICAL ABSTRACTS, 16 April 2012, Columbus, Ohio, US; abstract no. 1368910-17-1, "Chemical Catalog, Otava Chemicals" XP055270643
CHEMICAL ABSTRACTS, 15 April 2012, Columbus, Ohio, US; abstract no. 1368585-98-1, "Chemical Catalog, Otava Chemicals" XP055270645
WILLIAM R. MANN ET AL.: "Diverse mechanisms of inhibition of pyruvate dehydrogenase kinase by structurally distinct inhibitors", BIOCHIMICA ET BIOPHYSICA ACTA, vol. 1480, 2000, pages 283 - 292, XP027287959
JOSEPH J. BATENBURG ET AL.: "Regulation of Pyruvate Dehydrogenase by Fatty Acid in Isolated Rat Liver Mitochondria", THE JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 251, no. 5, 10 March 1976 (1976-03-10), pages 1364 - 1370, XP055267380
JOSEPH ESPINAL ET AL.: "Inhibition of Pyruvate Dehydrogenase Kinase by Halogenated Acetophenones", DRUG DEVELOPMENT RESEARCH, vol. 35, 1995, pages 130 - 136, XP000611456
INT. J. CANCER, vol. 128, 2011, pages 1001 - 1008
BIOCHEM. J., vol. 423, 2009, pages 243 - 252
J. BIOL CHEM., vol. 283, 2008, pages 25305 - 25315
MOL CELL BIOCHEM, vol. 299, 2007, pages 85 - 92
HUM MUTAT, vol. 29, 2008, pages 718 - 27
J. ANTIBIOTICS, vol. 62, 2009, pages 17 - 26
BERGE ET AL., J. PHARM. SCI., vol. 66, 1977, pages 1 - 19
See also references of EP 2939668A4
CHEMICAL ABSTRACTS, 16 April 2012, Columbus, Ohio, US; abstract no. 1368910-17-1, "Chemical Catalog, Otava Chemicals" XP055270643
CHEMICAL ABSTRACTS, 15 April 2012, Columbus, Ohio, US; abstract no. 1368585-98-1, "Chemical Catalog, Otava Chemicals" XP055270645
WILLIAM R. MANN ET AL.: "Diverse mechanisms of inhibition of pyruvate dehydrogenase kinase by structurally distinct inhibitors", BIOCHIMICA ET BIOPHYSICA ACTA, vol. 1480, 2000, pages 283 - 292, XP027287959
JOSEPH J. BATENBURG ET AL.: "Regulation of Pyruvate Dehydrogenase by Fatty Acid in Isolated Rat Liver Mitochondria", THE JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 251, no. 5, 10 March 1976 (1976-03-10), pages 1364 - 1370, XP055267380
JOSEPH ESPINAL ET AL.: "Inhibition of Pyruvate Dehydrogenase Kinase by Halogenated Acetophenones", DRUG DEVELOPMENT RESEARCH, vol. 35, 1995, pages 130 - 136, XP000611456
INT. J. CANCER, vol. 128, 2011, pages 1001 - 1008
BIOCHEM. J., vol. 423, 2009, pages 243 - 252
J. BIOL CHEM., vol. 283, 2008, pages 25305 - 25315
MOL CELL BIOCHEM, vol. 299, 2007, pages 85 - 92
HUM MUTAT, vol. 29, 2008, pages 718 - 27
J. ANTIBIOTICS, vol. 62, 2009, pages 17 - 26
BERGE ET AL., J. PHARM. SCI., vol. 66, 1977, pages 1 - 19
See also references of EP 2939668A4
Attorney, Agent or Firm:
HASEGAWA, Hiroshi et al. (JP)
Hiroshi Hasegawa (JP)
Hiroshi Hasegawa (JP)
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