Title:
G-PROTEIN-CONJUGATED RECEPTOR AGONIST
Document Type and Number:
WIPO Patent Application WO/2008/139987
Kind Code:
A1
Abstract:
Disclosed is a novel aralkyl carboxylic acid compound which has an agonistic
activity on GPR-120 and/or GPR-40, particularly GPR-120, and is therefore useful
as an appetite regulator, an anti-obesity agent, a therapeutic agent for diabetes,
a pancreatic beta differentiating cell growth enhancer, a therapeutic agent
for metabolic syndrome, a therapeutic agent for a gastrointestinal disease,
a therapeutic agent for a neuropathy, a therapeutic agent for a mental disorder,
a therapeutic agent for a pulmonary disease, a therapeutic agent for a pituitary
hormone secretion disorder or a lipid flavoring/seasoning agent. The aralkyl
carboxylic acid compound is represented by the general formula (I). (I)
wherein the ring Q represents a pyridyl or the like; R1 represents
a C1-6 alkyl group or the like; R2 represents a hydrogen atom,
a C1-4 alkyl group or a C1-4 alkoxy group; m and n independently
represent an integer of 1 to 5; and X represents an oxygen atom, a sulfur atom or
-NR3- [wherein R3 represents a hydrogen atom or a C1-4
alkyl group].
Inventors:
TSUJIMOTO GOZOH (JP)
HIRASAWA AKIRA (JP)
MIYATA NAOKI (JP)
SUZUKI TAKAYOSHI (JP)
TAKAHARA YOSHIYUKI (JP)
ISHIGURO MASAJI (JP)
HATA YOSHIE (JP)
HIRASAWA AKIRA (JP)
MIYATA NAOKI (JP)
SUZUKI TAKAYOSHI (JP)
TAKAHARA YOSHIYUKI (JP)
ISHIGURO MASAJI (JP)
HATA YOSHIE (JP)
Application Number:
PCT/JP2008/058457
Publication Date:
November 20, 2008
Filing Date:
April 25, 2008
Export Citation:
Assignee:
JAPAN SCIENCE & TECH AGENCY (JP)
UNIV KYOTO (JP)
UNIV NAGOYA CITY (JP)
PHARMA FRONTIER CO LTD (JP)
TSUJIMOTO GOZOH (JP)
HIRASAWA AKIRA (JP)
MIYATA NAOKI (JP)
SUZUKI TAKAYOSHI (JP)
TAKAHARA YOSHIYUKI (JP)
ISHIGURO MASAJI (JP)
HATA YOSHIE (JP)
UNIV KYOTO (JP)
UNIV NAGOYA CITY (JP)
PHARMA FRONTIER CO LTD (JP)
TSUJIMOTO GOZOH (JP)
HIRASAWA AKIRA (JP)
MIYATA NAOKI (JP)
SUZUKI TAKAYOSHI (JP)
TAKAHARA YOSHIYUKI (JP)
ISHIGURO MASAJI (JP)
HATA YOSHIE (JP)
International Classes:
A61K31/18; A61K31/196; A61K31/41; A61K31/4402; A61K31/47; A61P1/00; A61P1/18; A61P3/00; A61P3/04; A61P3/10; A61P5/06; A61P11/00; A61P25/00; A61P25/18; A61P43/00; C07C217/22; C07C311/51; C07D213/74; C07D215/12; C07D257/04
Domestic Patent References:
| WO2005087710A1 | 2005-09-22 | |||
| WO1989003819A1 | 1989-05-05 | |||
| WO2000000611A2 | 2000-01-06 | |||
| WO2000050596A2 | 2000-08-31 | |||
| WO2002067868A2 | 2002-09-06 | |||
| WO2003068959A1 | 2003-08-21 | |||
| WO2004065960A1 | 2004-08-05 |
Foreign References:
| JP2005015461A | 2005-01-20 | |||
| US4218475A | 1980-08-19 | |||
| JP2005015358A | 2005-01-20 |
Other References:
MCKEOWN S.C. ET AL.: "SOLID PHASE SYNTHESIS AND SAR OF SMALL MOLECULE AGONISTS FOR THE GPR40 RECEPTOR", BIOORG. MED. CHEM. LETT., vol. 17, no. 6, 15 March 2007 (2007-03-15), pages 1584 - 1589, XP005895369
BRISCOE C.P. ET AL.: "PHARMACOLOGICAL REGULATION OF INSULIN SECRETION IN MIN6 CELLS THROUGH THE FATTY ACID RECEPTOR GRP40: IDENTIFICATION OF AGONIST AND ANTAGONIST SMALL MOLECULES", BR. J. PHARMACOL., vol. 148, no. 5, 2006, pages 619 - 628, XP002576562
GARRIDO D.M. ET AL.: "SYNTHESIS AND ACTIVITY OF SMALL MOLECULE GPR40 AGONISTS", BIOORG. MED. CHEM. LETT., vol. 16, no. 7, 2006, pages 1840 - 1845, XP025106979
USUI S. ET AL.: "IDENTIFICATION OF NOVEL PPARgamma LIGANDS BY THE STRUCTURAL MODIFICATION OF A PPARgamma LIGAND", BIOORG. MED. CHEM. LETT., vol. 16, no. 12, 15 June 2006 (2006-06-15), pages 3249 - 3254, XP025106220
USUI S. ET AL.: "DESIGN, SYNTHESIS, AND BIOLOGICAL ACTIVITY OF NOVEL PPARgamma LIGANDS BASED ON RISOGLITAZONE AND 15D-PGJ2", BIOORG. MED. CHEM. LETT., vol. 15, no. 6, 2005, pages 1547 - 1551, XP025313562
See also references of EP 2151236A4
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 15, no. 6, 2005, pages 1547 - 1551
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 16, no. 12, 2006, pages 3249 - 3254
BR J PHARMACOL., vol. 148, no. 5, July 2006 (2006-07-01), pages 619 - 628
NATURE MEDICINE, vol. 11, no. 1, 2005, pages 90 - 94
NUTRITION, vol. 17, no. 3, 2001, pages 230 - 5
BEST PRACT RES CLIN ENDOCRINOL METAB, vol. 18, no. 4, 2004, pages 569 - 86
DIG DIS SCI., vol. 49, no. 3, 2004, pages 361 - 9
ENDOCRINOLOGY, vol. 145, no. 6, 2004, pages 2653 - 9
PHARMACOL TOXICOL, vol. 91, no. 6, 2002, pages 375 - 81
GASTROENTEROLOGY, vol. 127, no. 3, 2004, pages 957 - 69
MED RES REV., vol. 23, no. 5, 2003, pages 559 - 605
HORM METAB RES, vol. 36, no. 11-12, 2004, pages 842 - 5
AM J PHYUSIOL ENDOCRINOL METAB, vol. 287, no. 6, 2004, pages 1209 - 15
DIG DIS SCI, vol. 43, no. 4, 1998, pages 799 - 805
PHYSIOL BEHAV., vol. 83, no. 4, 2004, pages 617 - 21
BEST PRACT RES CLI ENDOCRINOL METAB., vol. 18, no. 4, 2004, pages 569 - 86
TRENDS ENDOCRINOL METAB., vol. 15, no. 6, 2004, pages 259 - 63
CURR DRUG TARGET CNS NEUROL DISORD, vol. 3, no. 5, 2004, pages 379 - 88
DIABETOLOGY, vol. 48, no. 9, 2005, pages 1700 - 13
DIABETES, vol. 53, no. 3, 2004, pages 225 - 32
HORMONE METAB RES., no. 11-12, 2004, pages 766 - 70
HORMONE METAB RES., vol. 36, no. 11-12, 2004, pages 846 - 51
CURR DRUG TARGET CNS NEUROL DISORD, vol. 1, no. 5, 2002, pages 495 - 510
CURR DRUG TARGETS., vol. 5, no. 69, 2004, pages 565 - 71
CURR ALZHEIMER RES, vol. 2, no. 3, 2005, pages 377 - 85
DRUG, vol. 63, no. 12, 2003, pages 1785 - 97
BR J PHARMACOL., vol. 141, no. 8, 2004, pages 1275 - 84
ENDOCRINOLOGY., vol. 139, no. 5, 1998, pages 2363 - 8
AM J RESPIR CRIT CARE MED., vol. 163, no. 4, 2001, pages 840 - 6
BRISCOE C.P. ET AL.: "PHARMACOLOGICAL REGULATION OF INSULIN SECRETION IN MIN6 CELLS THROUGH THE FATTY ACID RECEPTOR GRP40: IDENTIFICATION OF AGONIST AND ANTAGONIST SMALL MOLECULES", BR. J. PHARMACOL., vol. 148, no. 5, 2006, pages 619 - 628, XP002576562
GARRIDO D.M. ET AL.: "SYNTHESIS AND ACTIVITY OF SMALL MOLECULE GPR40 AGONISTS", BIOORG. MED. CHEM. LETT., vol. 16, no. 7, 2006, pages 1840 - 1845, XP025106979
USUI S. ET AL.: "IDENTIFICATION OF NOVEL PPARgamma LIGANDS BY THE STRUCTURAL MODIFICATION OF A PPARgamma LIGAND", BIOORG. MED. CHEM. LETT., vol. 16, no. 12, 15 June 2006 (2006-06-15), pages 3249 - 3254, XP025106220
USUI S. ET AL.: "DESIGN, SYNTHESIS, AND BIOLOGICAL ACTIVITY OF NOVEL PPARgamma LIGANDS BASED ON RISOGLITAZONE AND 15D-PGJ2", BIOORG. MED. CHEM. LETT., vol. 15, no. 6, 2005, pages 1547 - 1551, XP025313562
See also references of EP 2151236A4
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 15, no. 6, 2005, pages 1547 - 1551
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 16, no. 12, 2006, pages 3249 - 3254
BR J PHARMACOL., vol. 148, no. 5, July 2006 (2006-07-01), pages 619 - 628
NATURE MEDICINE, vol. 11, no. 1, 2005, pages 90 - 94
NUTRITION, vol. 17, no. 3, 2001, pages 230 - 5
BEST PRACT RES CLIN ENDOCRINOL METAB, vol. 18, no. 4, 2004, pages 569 - 86
DIG DIS SCI., vol. 49, no. 3, 2004, pages 361 - 9
ENDOCRINOLOGY, vol. 145, no. 6, 2004, pages 2653 - 9
PHARMACOL TOXICOL, vol. 91, no. 6, 2002, pages 375 - 81
GASTROENTEROLOGY, vol. 127, no. 3, 2004, pages 957 - 69
MED RES REV., vol. 23, no. 5, 2003, pages 559 - 605
HORM METAB RES, vol. 36, no. 11-12, 2004, pages 842 - 5
AM J PHYUSIOL ENDOCRINOL METAB, vol. 287, no. 6, 2004, pages 1209 - 15
DIG DIS SCI, vol. 43, no. 4, 1998, pages 799 - 805
PHYSIOL BEHAV., vol. 83, no. 4, 2004, pages 617 - 21
BEST PRACT RES CLI ENDOCRINOL METAB., vol. 18, no. 4, 2004, pages 569 - 86
TRENDS ENDOCRINOL METAB., vol. 15, no. 6, 2004, pages 259 - 63
CURR DRUG TARGET CNS NEUROL DISORD, vol. 3, no. 5, 2004, pages 379 - 88
DIABETOLOGY, vol. 48, no. 9, 2005, pages 1700 - 13
DIABETES, vol. 53, no. 3, 2004, pages 225 - 32
HORMONE METAB RES., no. 11-12, 2004, pages 766 - 70
HORMONE METAB RES., vol. 36, no. 11-12, 2004, pages 846 - 51
CURR DRUG TARGET CNS NEUROL DISORD, vol. 1, no. 5, 2002, pages 495 - 510
CURR DRUG TARGETS., vol. 5, no. 69, 2004, pages 565 - 71
CURR ALZHEIMER RES, vol. 2, no. 3, 2005, pages 377 - 85
DRUG, vol. 63, no. 12, 2003, pages 1785 - 97
BR J PHARMACOL., vol. 141, no. 8, 2004, pages 1275 - 84
ENDOCRINOLOGY., vol. 139, no. 5, 1998, pages 2363 - 8
AM J RESPIR CRIT CARE MED., vol. 163, no. 4, 2001, pages 840 - 6
Attorney, Agent or Firm:
DAITO, Teruo (17-12 Takanawa 2-chome, Minato-ku, Tokyo 74, JP)
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