1,5-benzothiazepine derivatives and their pharmaceutical use

Claim 2

A 1,5-benzothiazepine of the formula: ##STR48## wherein R 1 is lower alkyl or lower alkoxy, R 2 is lower alkanoyl, each one of R 3 and R 4 is lower alkyl, Ring A is a substituted benzene ring of the formula: ##STR49## R a is lower alkyl or lower alkoxy, and each one of R b and R c is lower alkyl or a pharmaceutically acceptable acid addition salt thereof.

Claim 3

A compound according to claim 1, in which R 1 is methyl or methoxy.

Claim 4

A compound according to claim 2, in which R a is methyl or methoxy, and R b and R c are methyl.

Claim 5

A compound according to claim 2, in which Ring A is a substituted benzene ring of the formula: ##STR50## wherein R a is methyl or methoxy.

Claim 6

A compound according to claim 3, in which R 2 is acetyl, and R 3 and R 4 are methyl.

Claim 7

A cis isomer of a compound claimed in any one of claims 1 through 5.

Claim 8

A (+)-cis isomer of a compound claimed in any one of claims 1 through 5.

Claim 9

A compound according to claim 5, which is selected from (±)-cis-2-(4-methylphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methoxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (±)-cis-2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (±)-cis-2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-7-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (±)-cis-2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-7-methoxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (±)-cis-2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methoxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (±)-cis-2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-6-methoxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (+)-cis-2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (+)-cis-2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-7-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (+)-cis-2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methoxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (±)-cis-2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-7,8-dimethyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (+)-cis-2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-7,8-dimethyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (±)-cis-2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-6,7-dimethyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, or a pharmaceutically acceptable acid addition salt thereof.

Claim 10

A 1,5-benzothiazepine of the formula: ##STR51## wherein R 1 is lower alkyl or lower alkoxy, R 2 is hydrogen atom or lower alkanoyl and Ring A is a substituted benzene ring of the formula: ##STR52## R a is lower alkyl or lower alkoxy and each one of R b and R c is lower alkyl, or a salt thereof.

Claim 11

A 1,5-benzothiazepine of the formula: ##STR51## wherein R 1 is lower alkyl or lower alkoxy, R 2 is hydrogen atom or lower alkanoyl and Ring A is a substituted benzene ring of the formula: ##STR52## R a is lower alkyl or lower alkoxy and each one of R b and R c is lower alkyl, or a salt thereof.

Claim 12

A 1,5-benzothiazepine of the formula: ##STR53## wherein R 1 is lower alkyl or lower alkoxy, each one of R 3 and R 4 is lower alkyl, Ring A is a substituted benzene ring of the formula: ##STR54## wherein R a is lower alkyl or lower alkoxy and each one of R b and R c is lower alkyl, or a salt thereof.

Claim 13

A 1,5-benzothiazepine of the formula: ##STR53## wherein R 1 is lower alkyl or lower alkoxy, each one of R 3 and R 4 is lower alkyl, Ring A is a substituted benzene ring of the formula: ##STR54## wherein R a is lower alkyl or lower alkoxy and each one of R b and R c is lower alkyl, or a salt thereof.

Claim 14

A compound according to claim 1 which is: ±cis-2-(4 methoxyphenyl)-3-acetoxy-5-[-2-(dimethylamino)ethyl]-6-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one or its pharmaceutically acceptable salt.

Claim 15

A pharmaceutical composition possessing hypotensive, cerebral vasodilating or coronary vasodilating activity which comprises a therapeutically effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier therefor.

Claim 16

A method of producing a hypotensive effect on a warm-blooded animal comprising administering to said warm-blooded animal an effective amount of a compound claimed in claim 1.

Claim 17

A method of producing a cerebral vasodilating effect on a warm-blooded animal comprising administering to said warm-blooded animal an effective amount of a compound claimed in claim 1.

Claim 18

A method of producing a coronary vasodilating effect on a warm-blooded animal comprising administering to said warm-blooded animal an effective amount of a compound claimed in claim 1.