Trans-4-(2-thiaoxo-1-pyrrolidinyl or piperidinyl)-2H-benzo[b]pyran-3-ol derivatives useful in treating hypertension
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/445
A61K-031/40
C07D-405/04
출원번호
US-0592115
(1984-03-22)
우선권정보
GB-0008064 (1983-03-24)
발명자
/ 주소
Evans John M. (Roydon GB2) Buckingham Robin E. (Welwyn Garden City GB2) Willcocks Kenneth (Harlow GB2)
출원인 / 주소
Beecham Group p.l.c. (GB2 03)
인용정보
피인용 횟수 :
7인용 특허 :
4
초록▼
A compound of formula (I): [Figure] (I) wherein: either one of R1 and R2 is hydrogen and the other is selected from the class of C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, C
A compound of formula (I): [Figure] (I) wherein: either one of R1 and R2 is hydrogen and the other is selected from the class of C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, C1-6 alkoxysulphinyl, C1-6 alkoxysulphonyl, C1-6 alkylcarbonylamino, C1-6 alkoxycarbonylamino, C1-6 alkyl-thiocarbonyl, C1-6 alkoxy-thiocarbonyl, C1-6 alkyl-thiocarbonyloxy, 1-mercapto-C2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C1-6 alkyl groups, or C1-6 alkysulphinylamino, C1-6 alkylsulphonylamino C1-6 alkoxysulphinylamino or C1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C1-6 alkylcarbonyl, nitro or cyano, or -C(C1-6 alkyl)NOH or -C(C1-6 alkyl)NNH2, or one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C1-6 alkyl groups or by C2-7 alkanoyl; one of R3 and R4 is hydrogen or C1-4 alkyl and the other is C1-4 alkyl or R3 and R4 together are C2-5 polymethylene. R5 is hydrogen, C1-3 alkyl or C1-8 acyl; and n is 1 or 2; the thiolactam group being trans to the OR5 group; or, when one or the other of R1 and R2 is an amino or an amino-containing group capable of forming an acid addition salt, a pharmaceutically acceptable salt thereof, having useful pharmacological activity, a process for preparing them, pharmaceutical compositions containing them, and their use in the treatment of mammals.
대표청구항▼
A compound of formula (I): [Figure] (I) wherein: either one of R1 and R2 is hydrogen and the other is C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, C1-6 alkoxysulphinyl, C1-6 a
A compound of formula (I): [Figure] (I) wherein: either one of R1 and R2 is hydrogen and the other is C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, C1-6 alkoxysulphinyl, C1-6 alkoxysulphonyl, C1-6 alkylcarbonylamino, C1-6 alkoxycarbonylamino, C1-6 alkyl-thiocarbonyl, C1-6 alkoxy-thiocarbonyl, C1-6 alkyl-thiocarbonyloxy, 1-mercapto-C2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C1-6 alkyl groups, or C1-6 alkylsulphinylamino, C1-6 alkylsulphonylamino C1-6 alkoxysulphinylamino or C1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C1-6 alkylcarbonyl, nitro or cyano, or -C(C1-6 alkyl)NOH or -C(C1-6 alkyl)NNH2, or one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C1-6 alkyl groups or by C2-7 alkanoyl; one of R3 and R4 is hydrogen or C1-4 alkyl and the other is C1-4 alkyl or R3 and R4 together are C2-5 polymethylene; R5 is hydrogen, C1-3 alkyl or C1-8 acyl; n is 1 or 2; the thiolactam group being trans to the OR5 group; or, when one of R1 and R2 is an amino or an amino-containing group capable of forming an acid addition salt, a pharmaceutically acceptable salt thereof.
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이 특허에 인용된 특허 (4)
Evans John M. (Roydon GB2) Showell Graham A. (Harlow GB2) Fake Charles S. (Harlow GB2), Anti-hypertensive chromanol derivatives.
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