Title:
MORPHOLINE AND THIOMORPHOLINE TACHYKININ RECEPTOR ANTAGONIST
Document Type and Number:
Japanese Patent JP2634372
Kind Code:
B2
Abstract:
PURPOSE: To provide a novel compd. useful for treatment for inflammation diseases, aches, migraine, asthma, angina, hypertension, ischemia, etc.
CONSTITUTION: This compsn. is expressed by formula I. In formula I, R1 is H, hydroxy, oxo, 1 to 6C alkoxy group, etc., R2 and R3 are each H, hydroxy, oxo, 1 to 6C alkoxy, phenyl group, etc., X is O, S, SO or SO2, R4 is expressed by formula II (R6 to R8 are each H, hydroxy, 1 to 6C alkoxy, phenyl group, etc., T is a single bond, O, S, CO, CH2, etc., Z is H, 1 to 4C alkyl, etc.), etc., R5 is a (substd.) phenyl group, 3 to 7C cycloalkyl group, etc., and for example, the compsn. is 2-(3,5-bis(trifluoromethyl)benzyloxy-3-phenyl-morpholine. The compd. is obtd. by, for example, bringing a compd. expressed by formula III (R11 to R12 are the same as R6, etc.), into contact with an org. acid such as toluene sulfonic acid in a aprotic solvent such as toluene at 0°C to the refluxing temp. of the solvent.
Inventors:
KONRATSUDO PII DOON
JEFURII JEI HOORU
MARUKOMU MATSUKOSU
SANDAA JII MIRUZU
TAMARA RATSUDOWAHETSUTEI
SHURENITSUKU KEI SHAA
JEFURII JEI HOORU
MARUKOMU MATSUKOSU
SANDAA JII MIRUZU
TAMARA RATSUDOWAHETSUTEI
SHURENITSUKU KEI SHAA
Application Number:
JP21204593A
Publication Date:
July 23, 1997
Filing Date:
June 29, 1993
Export Citation:
Assignee:
MERUKU ENDO CO INC
International Classes:
A61K31/5355; A61K31/5375; A61K31/54; A61P9/00; A61K31/535; A61P9/10; A61P9/12; A61P11/00; A61P11/06; A61P25/04; A61P25/06; A61P29/00; C01B15/013; C07D265/30; C07D265/32; C07D279/12; C07D413/04; C07D413/06; C07D413/14; C07D417/04; A61K38/00; C07D; C07K7/00; (IPC1-7): C07D265/30; C07D265/32; C07D413/06; C07D417/06
Foreign References:
| US4476311A |
Attorney, Agent or Firm:
Yoshio Kawaguchi (2 outside)
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