KR890002073A - Naphthothiazepine - Google Patents

Abstract

No content

Description

Naphthothiazepine

Since this is an open matter, no full text was included.

Claims (24)

Naphtho [1,2-b] -1,4-thiazepinone of the following general formula (I), and its pharmaceutically acceptable acid addition salt. Wherein R ₁ is phenyl substituted with 1 to 3 lower alkoxy groups or 1 to 3 halogen, R ₂ is hydroxy, lower alkoxy, lower alkanoyloxy, lower cycloalkylcarbonyloxy, Alkyl) or Alkyl), R ₃ and R ₄ are each independently lower alkyl or phenyl lower alkyl, or together form a piperidine or pyrrolidine ring, n is 2 to 4, and m is 1 or 2. The compound of claim 1 having a cis-configuration. The compound of claim 2 having a (+)-cis-configuration. The compound according to claim 1, wherein R ₁ is 4-lower alkoxyphenyl and R ₂ is hydroxy, lower alkoxy, lower cycloalkylcarbonyloxy, Alkyl) or Alkyl). The compound of any one of claims 1-3, wherein R ₁ is 4-lower alkoxyphenyl, R ₂ is lower alkanoyloxy, n is 2 or 3 and R ₃ and R ₄ are each independently lower alkyl. . The compound of claim 5, wherein R ₁ is 4-methoxyphenyl or 4-ethoxyphenyl, R ₂ is acetyloxy or propionyloxy, n is 2, and R ₃ and R ₄ are each methyl or ethyl. The compound of claim 6, wherein R ₁ is 4-methoxyphenyl, R ₂ is acetyloxy and R ₂ and R ₃ are each methyl. (±) -cis-5- [2- (dimethylamino) ethyl] -2,3-dihydro-3-highoxy-2- (4-methoxyphenyl) naphtho [1,2-b]- 1,4-thiazepin-4 (5H) -one. (±) -cis-3- (acetyloxy) -2,3-dihydro-2- (4-methoxyphenyl) -5- [2- (dimethylamino) ethyl] naphtho [1,2-b] -1,4-thiazepin-4 (5H) -one. (+)-Cis-2,3-dihydro-3-hydroxy-2- (4-methoxyphenyl) -5- [2- (dimethylamino) ethyl] naphtho [1,2-b] -1 , 4-thiazepin-4 (5H) -one. (+)-Cis-3- (acetoxy) -2,3-dihydro-2- (4-methoxyphenyl) -5- [2- (dimethylamino) ethyl] naphtho [1,2-b] -1,4-thiazepin-4 (5H) -one. (±) -cis-2,3-dihydro-3-methoxy-5- [2- (dimethylamino) ethyl] -2- (4-methoxyphenyl) naphtho [1,2-b] -1 , 4-thiazepin-4 (5H) -one: (±) -cis-2,3-dihydro-3- [4- (methoxyacetyl) oxy] -2- (4-methoxyphenyl) -5 -[2- (dimethylamino) ethyl] naphtho [1,2-b] -1,4-thiazepine-4 (5H) one: (±) -cis-3-[(ethoxycanonyl) oxy] -2,3-dihydro-2- (4-methoxyphenyl) -5- [2- (dimethylamino) ethyl] naphtho [1,2-b] -1,4-thiazepine-4 (5H) ON: (±) -cis-3-[(cyclopropylcarbonyl) oxy] -2,3-dihydro-5- [2- (dimethylamino) ethyl] -2- (4-methoxyphenyl) naphtho [1,2-b] -1,4-thiazepin-4 (5H) one: (±) -cis-5- [2- (diethylamino) ethyl] -2,3-dihydro-3-high Dooxy-2- (4-methoxyphenyl) naphtho [1,2-b] -1,4-thiazepin-4 (5H) one: (±) -cis-3- (acetyloxy) -5- [2- (diethylamino) ethyl] -2,3dihydro-2- (4-methoxyphenyl) naphtho [1,2-b] -1,4-thiazepin-4 (5H) -one: (±) -cis-2,3-dihydro-3-hydroxy-5- [3- ( Dimethylamino) -propyl] -2- (4-methoxyphenyl) naphtho [1,2-b] -1,4-thiazepin-4 (5H) -one: (±) -cis-3- (acetyl Oxy) -2,3-dihydro-5- [3- (dimethylamino) -propyl] -2- (4-methoxyphenyl) naphtho [1,2-b] -1,4-thiazepine-4 (5H) -one: (-)-cis-3- (acetyloxy) -2,3-dihydrodo-2- (4-methoxyphenyl) -5- [2- (dimethylamino) ethyl] naphtho [1,2-b] -1,4-thiazepin-4 (5H) -one: (-)-cis-2,3-dihydro-3-hydroxy-2- (4-methoxyphenyl)- 5- [2- (dimethylamino) ethyl] naphtho [1,2-b] -1,4-thiazepine-4 (5H) -one: (±) -trans-2,3-dihydro-3- Hydroxy-2- (4-methoxyphenyl) -5- [2- (dimethylamino) ethyl] niphtho [1,2-b] -1,4-thiazepin-4 (5H) -one: (± ) -Trans-3- (acetyloxy) -2,3-dihydro-2- (4-methoxyphenyl) -5- [2- (dimethylamino) ethyl] naphtho [1,2-b] -1 , 4-thiazepin-4 (5H) -one: (±) -cis-2,3-dihydro-3-hydroxy-2- (4-methoxyphenyl) -5- [2- [methyl (phenyl Methyl) amino] ethyl] naphtho [1,2-b] -1,4- Azepin-4 (5H) -one and (±) -cis-3- (acetyloxy) -2,3-dihydro-2- (4-methoxyphenyl) -5- [2- [methyl (phenylmethyl ) Amino] ethyl] naphtho [1,2-b] -1,4-thiazepin-4 (5H) -one. The compound of the following general formula (II). Wherein R ₁ is phenyl substituted with 1 to 3 lower alkoxy groups or 1 to 3 halogens. The compound according to any one of claims 1 to 12, used as therapeutically active substance. 13. A compound according to any one of claims 1 to 12 for use in the treatment or prevention of ischemia and hypertension. Reacting a compound of formula (II) with a compound of formula (III), optionally dividing the racemate of the obtained compound of formula (Ie) into its optically active enantiomer, or The alkali metal salt of the compound (Ie) is reacted with a lower alkylating agent, or the compound of formula (Ie) is lower alkanoic anhydride, lower alkanoyl halide, C ₁ -C ₅ -alkyl halo formate, C ₁ -C _3- The reaction of any of alkoxy acetyl or propionyl halides or lower cycloalkylcarboxylic acid halides or the conversion of the obtained compound of general formula (I) to pharmaceutically acceptable acid addition salts, Process for preparing a compound according to claim 1. In the line above, R ₁ , R ₃ , R ₄ and n are as defined above and Z is halogen. A medicament containing the compound according to any one of claims 1 to 12 and a therapeutically inert excipient. A therapeutic or prophylactic agent for ischemia and hypertension, comprising a compound according to any one of claims 1 to 12 and a therapeutically inert excipient. Use of a compound according to any one of claims 1 to 12 in the treatment or prevention of a disease. Use of a compound according to any one of claims 1 to 12 in the treatment or prevention of ischemia and / or hypertension. Use of a compound according to any one of claims 1 to 12 in the manufacture of a medicament for the treatment of ischemia and / or hypertension. The compound according to any one of claims 1 to 12, prepared according to the method as claimed in claim 16 or by an apparent compound equivalent method thereof. Invention as described above. A method for treating ischemia and / or hypertension of a patient, characterized in that the patient is administered an effective amount of the compound according to any one of claims 1 to 12. ※ Note: The disclosure is based on the initial application.