PHOSPHONOACETIC ACID DERIVATIVE AND USE THEREOF FOR TREATING DEGENERATIVE JOINT DISORDER

Title:

PHOSPHONOACETIC ACID DERIVATIVE AND USE THEREOF FOR TREATING DEGENERATIVE JOINT DISORDER

Document Type and Number:

Japanese Patent JP3725600

Kind Code:

B2

Abstract:

PROBLEM TO BE SOLVED: To obtain a new compound having a proteoglycan synthesis-stimulating effect in cartilage and a substance P antagonistic action, and useful for the treatment and prophylaxis of degenerative joint disorders, rheumatic diseases accompanied by cartilage breakdown, inflammations, etc.
SOLUTION: This phosphonoacetic acid derivative is a compound of formula I {at least 2 of R1 to R3 exist and express each OH, a 1-12C alkoxy or the like; R5 is CN, CH2NHR9 [R9 is H, C(O)-2-3C alkyl] or the like; R6 and R7 are each H, a 1-6C alkyl or the like; (C-A-C) is (CH2-CH), (CH=C) or the like; provided that when R5 is CN, one of R1 to R3 is hydroxyl} or salt thereof and/or a stereoisomer thereof (except for compounds of formulae II and III), e.g. 3-(3,4-diacetoxyphenyl)-2-(diethoxyphosphinyl)propenic acid ethyl. The compound is obtained e.g. by reacting 3,4-diacetoxybenzaldehyde with phosphonoacetic acid triethyl in THF in the presence of TiCl4 and then reacting N-methylmorpholine therewith.

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Inventors:

Rolf Grave
Werner Tallwalt
Root rice
Klaus Ulrich Vuitman
Ciute Juan Miulner

Application Number:

JP2872596A

Publication Date:

December 14, 2005

Filing Date:

January 24, 1996

Export Citation:

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Assignee:

HOECHST AKTIENGESELLSCHAFT

International Classes:

A61K31/665; A61P9/00; A61P29/00; A61P43/00; B01J23/44; B01J25/02; B01J31/02; C07F9/38; C07F9/40; C07F9/58; C07F9/6533; C07F9/655; C07F9/6553; A61K31/66; C07F9/6571; C07F9/6574; C07F9/6596; (IPC1-7): C07F9/38; A61K31/66; A61K31/665; A61P9/00; A61P29/00; A61P43/00; B01J23/44; B01J25/02; B01J31/02; C07F9/58; C07F9/6533; C07F9/655; C07F9/6574

Domestic Patent References:

JP62236863A

Other References:

J.Hetero.Chem.,1985年,22(6),p.1713-1714
J.Hetero.Chem.,1987年,24(4),p.931-932

Attorney, Agent or Firm:

Chika Takagi
Tatsuo Sato
Kosuke Nishimura

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