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1. (WO1985004658) 1,5-BENZOXATHIEPINE DERIVATIVES AND THEIR PREPARATION
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1985/004658 International Application No.: PCT/JP1984/000168
Publication Date: 24.10.1985 International Filing Date: 04.04.1984
IPC:
C07D 327/02 (2006.01) ,C07D 411/06 (2006.01) ,C07D 411/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
327
Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms
02
one oxygen atom and one sulfur atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
411
Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
411
Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
Applicants:
TAKEDA CHEMICAL INDUSTRIES, LTD. [JP/JP]; 27, Doshomachi 2-chome Higashi-ku, Osaka-shi Osaka 541, JP
Inventors:
SUGIHARA, Hirosada; JP
HIRATA, Minoru; JP
Agent:
AMAI, Sakuji; Osaka Plant of Takeda Chemical Industries, Ltd. 17-85, Jusohonmachi 2-chome Yodogawa-ku, Osaka-shi Osaka 532, JP
Priority Data:
Title (EN) 1,5-BENZOXATHIEPINE DERIVATIVES AND THEIR PREPARATION
(FR) DERIVES DE 1,5 BENZOXATHIEPINE ET LEUR PREPARATION
Abstract:
(EN) Novel 1,5-benzoxathiepine derivatives represented by formula (I), wherein R1 and R2 each represents hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy, R3 and R4 each represents hydrogen, lower alkyl or optionally substituted cycloalkyl or aralkyl or, when taken together, R3 and R4 form a ring together with the adjacent nitrogen atom, X represents hydrogen, optionally substituted lower alkyl, optionally substituted aryl, or optionally esterified or amidated carboxyl, Y represents > C=O or > CH-OR5 (wherein R5 represents hydrogen, acyl, or optionally substituted amido), m represents an integer of 0 to 2, and n represents and integer of 1 to 6, and salts thereof show the effect of blocking serotonin S receptor, calcium-competitive effect, diuretic effect, and anti-thrombotic effect, and are useful for prophylaxis and treatment of ischemic heart disease, thrombosis, and hypertension.
(FR) Nouveaux dérivés de 1,5 benzoxathiépines de formule (I) où R1 et R2 représentent chacun un hydrogène, un halogène, un hydroxy, un alkyle inférieur ou un alkoxy inférieur, R3 et R4 représentent chacun un hydrogène, un alkyle inférieur ou un aralkyle ou un cycloalkyle facultativement substitué ou, pris ensemble, R3 et R4 forment un cycle avec l'atome d'azote voisin, X représente un hydrogène, un alkyle inférieur facultativement substitué, un aryle facultativement substitué ou un carboxyle facultativement estérifié ou amidé, Y représente > C=O ou > CH-OR5 (où R5 représente un hydrogène, un acyle ou un amido facultativement substitué), m est un nombre entier de 0 à 2 et n un nombre entier de 1 à 6; ces dérivés et leurs sels ont un effet de blocage du récepteur S de sérotonine, un effet concurrent au calcium, un effet diurétique et un effet antithrombotique et sont utiles pour la prophylaxie et le traitement de l'affection cardiaque ischémique, de la thrombose et de l'hypertension.
Designated States: MC
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)