Title:
PREVENTION AND/OR THERAPEUTIC AGENT FOR FIBROMYALGIA
Document Type and Number:
WIPO Patent Application WO/2016/111357
Kind Code:
A1
Abstract:
The present invention is directed to the compound (1S)-2-acetyl-1-(4-chloro-2-methoxyphenyl)-5-fluoro-1,2,3,9-tetrahydrospiro[ß-carboline-4,1'-cyclopropane] represented by the formula. This compound, when compared to conventionally-known TSPO antagonists, markedly suppresses a drop in pain threshold, making it possible to form excellent prevention and/or therapeutic agent for fibromyalgia.
Inventors:
KATSUMATA SEISHI (JP)
MITSUI KATSUKUNI (JP)
EZAKI YUYA (JP)
MITSUI KATSUKUNI (JP)
EZAKI YUYA (JP)
Application Number:
PCT/JP2016/050527
Publication Date:
July 14, 2016
Filing Date:
January 08, 2016
Export Citation:
Assignee:
ONO PHARMACEUTICAL CO (JP)
International Classes:
A61K31/438; A61K31/381; A61K31/405; A61K31/5513; A61K31/616; A61P1/00; A61P1/02; A61P1/10; A61P1/12; A61P3/04; A61P7/10; A61P9/00; A61P11/00; A61P13/10; A61P15/00; A61P17/00; A61P17/04; A61P19/02; A61P19/04; A61P19/08; A61P21/00; A61P25/00; A61P25/02; A61P25/04; A61P25/22; A61P25/24; A61P27/02; A61P27/16; A61P29/00; A61P37/06
Domestic Patent References:
| WO2009025091A1 | 2009-02-26 |
Foreign References:
| JP4997976B2 | 2012-08-15 | |||
| JP2002541097A | 2002-12-03 | |||
| JP2008260728A | 2008-10-30 |
Other References:
BAZZICHI L. ET AL.: "Peripheral benzodiazepine receptors on platelets of fibromyalgic patients", CLINICAL BIOCHEMISTRY, vol. 39, no. 9, 2006, pages 867 - 872, XP005650573, DOI: doi:10.1016/j.clinbiochem.2006.06.002
FAGGIOLI P. ET AL.: "Increase in peripheral benzodiazepine receptors on monocytes in fibromyalgia", RHEUMATOLOGY, vol. 43, no. 10, 2004, pages 1224 - 1225, XP003032465
KATSUHIRO TODA ET AL.: "Sen'i Kintsusho", THE JAPANESE JOURNAL OF PSYCHIATRY, vol. 11, no. 1, 2006, pages 65 - 73, XP008185717
TAKAKO MIYAMAE ET AL.: "Wagakuni ni Okeru Sen'i Kintsusho no Jittai to Rinshozo", THE JOURNAL OF THE JAPAN PEDIATRIC SOCIETY, vol. 112, no. 12, 2008, pages 1769 - 1777, XP008185609
KUSUKI NISHIOKA: "Totsu Model kara Itami o Miru 2 Sen'i Kintsusho Model", BIOMEDICINE & THERAPEUTICS, vol. 39, no. 8, 2005, pages 806 - 809, XP008185611
HIROSHI KIYAMA: "CNS-mediated disintegration of homeostasis by chronic stress", FOLIA PHARMACOLOGICA JAPONICA, vol. 142, no. 5, 2013, pages 210 - 214, XP003032466
KOICHI OTA: "Sen'i Kintsusho ni Gappei suru Restless Legs Shokogun ni Taisuru Pramipexole, Gabapentin enacarbil Heiyo Chiryo no Koka", PAIN CLINIC, vol. 34, no. 12, 2013, pages 1671 - 1677, XP008185610
FAGGIOLI P. ET AL.: "Increase in peripheral benzodiazepine receptors on monocytes in fibromyalgia", RHEUMATOLOGY, vol. 43, no. 10, 2004, pages 1224 - 1225, XP003032465
KATSUHIRO TODA ET AL.: "Sen'i Kintsusho", THE JAPANESE JOURNAL OF PSYCHIATRY, vol. 11, no. 1, 2006, pages 65 - 73, XP008185717
TAKAKO MIYAMAE ET AL.: "Wagakuni ni Okeru Sen'i Kintsusho no Jittai to Rinshozo", THE JOURNAL OF THE JAPAN PEDIATRIC SOCIETY, vol. 112, no. 12, 2008, pages 1769 - 1777, XP008185609
KUSUKI NISHIOKA: "Totsu Model kara Itami o Miru 2 Sen'i Kintsusho Model", BIOMEDICINE & THERAPEUTICS, vol. 39, no. 8, 2005, pages 806 - 809, XP008185611
HIROSHI KIYAMA: "CNS-mediated disintegration of homeostasis by chronic stress", FOLIA PHARMACOLOGICA JAPONICA, vol. 142, no. 5, 2013, pages 210 - 214, XP003032466
KOICHI OTA: "Sen'i Kintsusho ni Gappei suru Restless Legs Shokogun ni Taisuru Pramipexole, Gabapentin enacarbil Heiyo Chiryo no Koka", PAIN CLINIC, vol. 34, no. 12, 2013, pages 1671 - 1677, XP008185610
Attorney, Agent or Firm:
AOKI, Atsushi et al. (JP)
Aoki 篤 (JP)
Aoki 篤 (JP)
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