Title:
PTP-1B INHIBITOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/013116
Kind Code:
A1
Abstract:
The present invention pertains to a compound represented by general formula (I) [each of the symbols in the formula is as set forth in the description] or a pharmacologically acceptable salt thereof, and to a pharmaceutical composition containing said compound as an active ingredient. Because the compound has PTP-1B inhibitory activity, the present invention can provide a pharmaceutical useful as an agent for treating diabetes, an agent for improving insulin resistance, an agent for improving glucose intolerance, an agent for treating diabetes complications, an anti-obesity agent, an anti-hyperglycemic agent, an agent for treating fatty liver, an anti-hyperlipidemic agent, an anti-arteriosclerosis agent, and an agent for preventing and/or treating metabolic syndrome.
Inventors:
SHOJI YOSHIMICHI (JP)
TAKEDA SHIGEMITSU (JP)
SHIRAHASE HIROAKI (JP)
TAKEDA SHIGEMITSU (JP)
SHIRAHASE HIROAKI (JP)
Application Number:
PCT/JP2019/026956
Publication Date:
January 16, 2020
Filing Date:
July 08, 2019
Export Citation:
Assignee:
KYOTO PHARMA IND (JP)
International Classes:
C07D217/26; A61K31/472; A61K31/4725; A61P3/00; A61P3/04; A61P3/06; A61P3/10; A61P9/10; A61P43/00; C07D405/06; C07D405/14; C07D409/14; C07D413/12; C07D417/06
Domestic Patent References:
| WO2002096880A1 | 2002-12-05 | |||
| WO2002096904A1 | 2002-12-05 | |||
| WO2004106542A1 | 2004-12-09 | |||
| WO2006095922A1 | 2006-09-14 |
Foreign References:
| JP2008540389A | 2008-11-20 | |||
| JPH10507174A | 1998-07-14 |
Other References:
OTAKE, KAZUYA ET AL.: "Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: Peroxisome proliferator-activated receptor y selective agonists with protein-tyrosine phosphatase 1B inhibition", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 20, no. 2, 2012, pages 1060 - 1075, XP028442343, ISSN: 0968-0896, DOI: 10.1016/j.bmc.2011.11.035
OTAKE, KAZUYA ET AL.: "Novel 2,7-substituted (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor y partial agonists with protein-tyrosine phosphatase IB inhibition", CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 63, no. 12, 2015, pages 998 - 1014, XP055674585, ISSN: 0009-2363
KLOPFENSTEIN, SEAN R. ET AL.: "1, 2, 3, 4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 16, no. 6, 2006, pages 1574 - 1578, XP028755069, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2005.12.051
ANDROVIC, LADISLAV ET AL.: "Synthesis and characterization of N-substituted (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxamides and thioamides as organocatalysts for asymmetric aldol reaction", HETEROCYCLES, vol. 89, no. 8, 2014, pages 1844 - 1859, ISSN: 0385-5414
5 March 2018 (2018-03-05)
MORISHITA, KO ET AL.: "2-Acyl-3-carboxyl-tetrahydroisoquinoline derivatives: mixed-type PTP1B inhibitors without PPARy activation", CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 66, no. 12, 27 September 2018 (2018-09-27), pages 1131 - 1152, XP055674590, ISSN: 0009-2363
OTAKE, KAZUYA ET AL.: "Novel 2,7-substituted (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor y partial agonists with protein-tyrosine phosphatase IB inhibition", CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 63, no. 12, 2015, pages 998 - 1014, XP055674585, ISSN: 0009-2363
KLOPFENSTEIN, SEAN R. ET AL.: "1, 2, 3, 4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 16, no. 6, 2006, pages 1574 - 1578, XP028755069, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2005.12.051
ANDROVIC, LADISLAV ET AL.: "Synthesis and characterization of N-substituted (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxamides and thioamides as organocatalysts for asymmetric aldol reaction", HETEROCYCLES, vol. 89, no. 8, 2014, pages 1844 - 1859, ISSN: 0385-5414
5 March 2018 (2018-03-05)
MORISHITA, KO ET AL.: "2-Acyl-3-carboxyl-tetrahydroisoquinoline derivatives: mixed-type PTP1B inhibitors without PPARy activation", CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 66, no. 12, 27 September 2018 (2018-09-27), pages 1131 - 1152, XP055674590, ISSN: 0009-2363
Attorney, Agent or Firm:
TAKASHIMA, Hajime (JP)
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