Title:
NOVEL LIGANDS OF NUCLEAR RECEPTOR SUPERFAMILY, PROCESS FOR PRODUCING THE SAME AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2002/074725
Kind Code:
A1
Abstract:
Aldehyde residues in ascochlorin, analogs thereof and derivatives of the same can be selectively oxidized into carboxylic acids. All of phenolic hydroxyl groups of ascochlorin, analogs thereof and derivatives of the same are protected by alkylation or acylation and aromatic aldehyde groups thereof are selectively oxidized to thereby give the corresponding carboxylic acids. The thus synthesized carboxylic acids are ligands activating nuclear receptor super family including retinoid receptor, retinoid orphan receptor, peroxisome proliferation activator receptor (PPAR$g(a)) and steroid receptor (PXR) and having therapeutic effects on life style-related diseases, chronic inflammation, cancer, etc.
Inventors:
TAMURA GAKUZO (JP)
KUWAHARA SHIGEFUMI (JP)
ANDO KUNIO (JP)
HOSOKAWA TOMOYOSHI (JP)
KUWAHARA SHIGEFUMI (JP)
ANDO KUNIO (JP)
HOSOKAWA TOMOYOSHI (JP)
Application Number:
PCT/JP2002/002487
Publication Date:
September 26, 2002
Filing Date:
March 15, 2002
Export Citation:
Assignee:
ARIGEN INC (JP)
NUCLEAR RECEPTOR RES LTD (JP)
TAMURA GAKUZO (JP)
KUWAHARA SHIGEFUMI (JP)
ANDO KUNIO (JP)
HOSOKAWA TOMOYOSHI (JP)
NUCLEAR RECEPTOR RES LTD (JP)
TAMURA GAKUZO (JP)
KUWAHARA SHIGEFUMI (JP)
ANDO KUNIO (JP)
HOSOKAWA TOMOYOSHI (JP)
International Classes:
A61P3/06; A61K31/192; A61P3/10; A61P3/14; A61P5/14; A61P9/10; A61P19/00; A61P29/00; A61P35/00; A61P37/02; A61P37/06; A61P43/00; C07C51/29; C07C65/40; C07C67/29; C07C69/63; (IPC1-7): C07C51/29; A61K31/122; A61P3/10; A61P3/14; A61P5/14; A61P9/10; A61P29/00; A61P35/00; A61P37/06; C07C65/40; C07C67/29; C07C69/63
Foreign References:
| JPS6176441A | 1986-04-18 | |||
| JPH09157286A | 1997-06-17 |
Other References:
GRUNEIRO E.M. ET AL.: "Some derivatives of O-orsellinic acid", AN. ASOC. QUIM. ARGENT., vol. 59, no. 3-4, 1971, pages 259 - 264, XP002952738
SOLLADIE G. ET AL.: "Asymmetric synthesis of orsellinic acid type macrolides: The example of lasiodiplodin", TETRAHEDRON: ASYMMETRY, vol. 1, no. 3, 1990, pages 187 - 198, XP002952739
SOLLADIE G. ET AL.: "Asymmetric synthesis of orsellinic acid type macrolides: The example of lasiodiplodin", TETRAHEDRON: ASYMMETRY, vol. 1, no. 3, 1990, pages 187 - 198, XP002952739
Attorney, Agent or Firm:
Shamoto, Ichio (Section 206 New Ohtemachi Bldg., 2-1,
Ohtemachi 2-chom, Chiyoda-ku Tokyo, JP)
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