← Back to Patent Explorer
EP0161801A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Perhydrothiazepine derivatives, their preparation and their therapeutic use

Assignee: Sankyo Co Ltd
•
Filing: 1985-04-10
•
Granted: —
•
Expires: 2005-04-10
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

Abstract

Abstract Compounds of formula (I): (wherein: R 1 represents an optionally substituted alkyl, cycloalkyl, aryl, partially hydrogenated aryl or heterocyclic group; R 2 , R 3 , R 4 and R 5 represent hydrogen or an optionally substituted alkyl, cycloalkyl, aralkyl, aryl, heterocyclic or heterocyclic-alkyl group or any adjacent pair thereof form a cyclic structure, at least one not being hydrogen; A represents a bond, or a methylene, ethylene, oxymethyl or thiomethyl group; B represents an alkylene, alkylidene, cycloalkylene or cycloalkylidene group; and n is 0, 1 or 2) and salts and esters thereof are hypotensive agents.

Inventors

  • 👤 Hiroaki Sankyo Chemical Research Lab. Yanagisawa
  • 👤 Sadao Sankyo Chemical Research Lab. Ishihara
  • 👤 Akiko Sankyo Chemical Research Lab. Ando
  • 👤 Takuro Sankyo Chemical Research Lab. Kanazaki
  • 👤 Hiroyuki Sankyo Biological Research Lab. Koike
  • 👤 Yoshio Sankyo Fermentation Research Lab. Tsujita

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-06 10:52
CPC Classifications
C; C07; C07D; C07D281/00; C07D281/02; C07D281/04; C07D281/06; C07D209/00; C07D209/02; C07D209/44; C07D209/48; A; A61; A61P; A61P9/00; A61P9/12; C07D307/00; C07D307/02; C07D307/34; C07D307/38; C07D307/52; C07D333/00; C07D333/02; C07D333/04; C07D333/06; C07D333/14; C07D333/18; C07D333/20; C07D405/00; C07D405/02; C07D405/12; C07D409/00; C07D409/02; C07D409/12; C07D417/00; C07D417/02; C07D417/04; C07D417/14; C07K; C07K5/00; C07K5/02; C07K5/022; C07K5/0222; A61K; A61K38/00

Claims Analysis

Total Claims: 58
Claim 1
Independent Claim 627 words
Compounds of formula (I): wherein: R represents a C 1 -C 10 alkyl group, a C 3 -C 8 cycloalkyl group, a carbocyclic aryl group having from 6 to 14 ring carbon atoms, a partially hydrogenated carbocyclic aryl group having from 6 to 14 ring carbon atoms or a heterocyclic group having from 5 to 14 ring atoms, of which from 1 to 5 are nitrogen, sulphur or oxygen hetero-atoms, said groups represented by R 1 being unsubstituted or having at least one substituent selected from the group consisting of: (a) oxo groups, C 1 -C 6 alkyl groups, C 6 -C 10 carbocyclic aryl groups, aralkyl groups wherein the alkyl part is C 1 -C 6 alkyl and the aryl part is C 6 -C 10 carbocyclic aryl, hydroxy groups, C 1 -C 6 alkoxy groups, alkoxyalkoxy groups where each alkoxy part is C 1 -C 6 , aralkyloxy groups, wherein the alkoxy part is C 1 -C 6 alkoxy and the aryl part is C 6 -C 10 carbocyclic aryl, aryloxy groups wherein the aryl part is C 6 -C 10 carbocyclic aryl, halogen atoms, nitro groups, cyano groups, carboxy groups, alkoxycarbonyl groups wherein the alkoxy part is C 1 -C 6 alkoxy, amino groups, C 1 -C 6 alkylamino groups, dialkylamino groups wherein each alkyl part is C 1 -C 6 alkyl, aliphatic or carbocyclic aromatic carboxylic acylamino groups, carbamoyl groups, alkylcarbamoyl groups where the alkyl part is C 1 -C 6 alkyl, dialkylcarbamoyl groups where each alkyl part is C 1 -C 6 alkyl, C 1 -C 6 alkylthio groups, C 6 -C 10 carbocyclic arylthio groups, C 1 -C 6 alkylsulphonyl groups and C 6 -C 10 carbocyclic arylsulphonyl groups wherein the aryl part is unsubstituted or has from 1 to 3 C 1 -C 6 alkyl substituents; R 2 , R 3 , R 4 and R 5 are the same or different and each represents a hydrogen atom, a C 1 -C 10 alkyl group, a C 3 -C 8 cycloalkyl group, an aralkyl group wherein the alkyl part is C 1 -C 6 alkyl and the aryl part is C 6 -C 10 carbocyclic aryl, a C 6 -C 14 carbocyclic aryl group, a C 1 -C 6 alkyl group having a heterocyclic substituent wherein the heterocyclic part has from 5 to 10 ring atoms of which from 1 to 5 are nitrogen, sulphur or oxygen hetero-atoms, or a heterocyclic group having from 5 to 14 ring atoms of which from 1 to 5 are nitrogen, sulphur or oxygen hetero-atoms, provided that R 2 , R 3 , R 4 and R 5 do not all represent hydrogen atoms, said groups represented by R 2 , R 3 , R 4 and R 5 being unsubstituted or having at least one substituent selected from the group consisting of the substituents defined in (a) above, or R 2 and R 3 , R 4 and R 5 or R 2 and R 4 together form a saturated carbocyclic or heterocyclic ring having from 3 to 6 ring atoms, of which, in said heterocyclic ring, from 1 to 3 are nitrogen, sulphur or oxygen hetero-atoms, or R 2 and R 3 , R 4 and R or R 2 and R 4 together form a saturated carbocyclic ring having 5 or 6 ring atoms, which ring is fused with a C 6 - C 10 carbocyclic aryl system; A represents a direct carbon-carbon bond, a methylene group, an ethylene group, an oxymethyl group or a thiomethyl group; B represents a C 1 -C 4 alkylene or alkylidene group or a C 3 -C 6 cycloalkylene or cycloalkylidene group n is 0, 1 or 2; and pharmaceutically acceptable salts and esters thereof.
Claim 2
Dependent Claim 627 words
Compounds of formula (I): wherein: R represents a C 1 -C 10 alkyl group, a C 3 -C 8 cycloalkyl group, a carbocyclic aryl group having from 6 to 14 ring carbon atoms, a partially hydrogenated carbocyclic aryl group having from 6 to 14 ring carbon atoms or a heterocyclic group having from 5 to 14 ring atoms, of which from 1 to 5 are nitrogen, sulphur or oxygen hetero-atoms, said groups represented by R 1 being unsubstituted or having at least one substituent selected from the group consisting of: (a) oxo groups, C 1 -C 6 alkyl groups, C 6 -C 10 carbocyclic aryl groups, aralkyl groups wherein the alkyl part is C 1 -C 6 alkyl and the aryl part is C 6 -C 10 carbocyclic aryl, hydroxy groups, C 1 -C 6 alkoxy groups, alkoxyalkoxy groups where each alkoxy part is C 1 -C 6 , aralkyloxy groups, wherein the alkoxy part is C 1 -C 6 alkoxy and the aryl part is C 6 -C 10 carbocyclic aryl, aryloxy groups wherein the aryl part is C 6 -C 10 carbocyclic aryl, halogen atoms, nitro groups, cyano groups, carboxy groups, alkoxycarbonyl groups wherein the alkoxy part is C 1 -C 6 alkoxy, amino groups, C 1 -C 6 alkylamino groups, dialkylamino groups wherein each alkyl part is C 1 -C 6 alkyl, aliphatic or carbocyclic aromatic carboxylic acylamino groups, carbamoyl groups, alkylcarbamoyl groups where the alkyl part is C 1 -C 6 alkyl, dialkylcarbamoyl groups where each alkyl part is C 1 -C 6 alkyl, C 1 -C 6 alkylthio groups, C 6 -C 10 carbocyclic arylthio groups, C 1 -C 6 alkylsulphonyl groups and C 6 -C 10 carbocyclic arylsulphonyl groups wherein the aryl part is unsubstituted or has from 1 to 3 C 1 -C 6 alkyl substituents; R 2 , R 3 , R 4 and R 5 are the same or different and each represents a hydrogen atom, a C 1 -C 10 alkyl group, a C 3 -C 8 cycloalkyl group, an aralkyl group wherein the alkyl part is C 1 -C 6 alkyl and the aryl part is C 6 -C 10 carbocyclic aryl, a C 6 -C 14 carbocyclic aryl group, a C 1 -C 6 alkyl group having a heterocyclic substituent wherein the heterocyclic part has from 5 to 10 ring atoms of which from 1 to 5 are nitrogen, sulphur or oxygen hetero-atoms, or a heterocyclic group having from 5 to 14 ring atoms of which from 1 to 5 are nitrogen, sulphur or oxygen hetero-atoms, provided that R 2 , R 3 , R 4 and R 5 do not all represent hydrogen atoms, said groups represented by R 2 , R 3 , R 4 and R 5 being unsubstituted or having at least one substituent selected from the group consisting of the substituents defined in (a) above, or R 2 and R 3 , R 4 and R 5 or R 2 and R 4 together form a saturated carbocyclic or heterocyclic ring having from 3 to 6 ring atoms, of which, in said heterocyclic ring, from 1 to 3 are nitrogen, sulphur or oxygen hetero-atoms, or R 2 and R 3 , R 4 and R or R 2 and R 4 together form a saturated carbocyclic ring having 5 or 6 ring atoms, which ring is fused with a C 6 - C 10 carbocyclic aryl system; A represents a direct carbon-carbon bond, a methylene group, an ethylene group, an oxymethyl group or a thiomethyl group; B represents a C 1 -C 4 alkylene or alkylidene group or a C 3 -C 6 cycloalkylene or cycloalkylidene group n is 0, 1 or 2; and pharmaceutically acceptable salts and esters thereof.
Claim 3
Dependent Claim 49 words
Compounds as claimed in Claim 1, represented by the formula (Ia): (wherein R 1 -R 5 , A, B and n are as defined in Claim 1 and R 6 and R 7 , which are the same or different, each represents a hydrogen atom or a carboxy-protecting group).
Claim 4
Dependent Claim 290 words
Compounds as claimed in Claim 2, wherein R 6 and R 7 are the same or different and each represents a C 1 -C 10 alkyl group, an aralkyl group in which the aryl part is a C 6 -C 10 carbocyclic aryl group which is unsubstituted or substituted as defined in (b) below and the alkyl part is C 1 -C 6 alkyl, a C 6 -C 14 carbocyclic aryl group, a partially hydrogenated C 6 -C 14 carbocyclic aryl group, a phthalidyl group or a trialkylsilyl group where each alkyl part is C 1 -C 6 alkyl, said groups represented by R 6 and R 7 being unsubstituted or having at least one substituent selected from the group consisting of: (b) halogen atoms, hydroxy groups, C 1 -C 6 alkox y groups, (C 1 -C 6 alkoxy)-(C 1 -C 3 alkoxy) groups, aliphatic and carbocyclic aromatic carboxylic acyloxy groups, oxo groups, carboxy groups, alkoxycarbonyl groups where the alkoxy part is C 1 -C 6 alkoxy, alkoxycarbonyloxy groups where the alkoxy part is C 1 -C 6 alkoxy, aliphatic and carbocyclic aromatic carboxylic acylamino groups, nitro groups, cyano groups, amino groups, C 1 -C 6 alkylamino groups, dialkylamino groups where each alkyl part is C I -C 6 alkyl, C 6 -C 10 carbocyclic arylamino groups, C 1 -C 6 alkylthio groups, C 6 -C 10 carbocyclic arylthio groups, C 1 -C 6 alkylsulphonyl groups, C 6 -C 10 carbocyclic arylsulphonyl groups and heterocyclic groups having from 5 to 14 ring atoms, of which from 1 to 5 are nitrogen, sulphur or oxygen hetero-atoms, said heterocyclic groups being unsubstituted or having at least one substituent selected from the group consisting of the substituents defined in (a) of Claim 1.
Claim 5
Dependent Claim 103 words
Compounds as claimed in Claim 2, in which: R represents a phenyl group or a C 2 -C 7 alkyl group; R 2 and R 4 are the same or different and each represents a hydrogen atom, a C 1 -C 10 alkyl group, a phenyl group, a naphthyl group, a C 3 -C 8 cycloalkyl group or a heterocyclic group having from 5 to 10 ring atoms, of which from 1 to 3 are nitrogen, oxygen or sulphur hetero-atoms; R 3 and R 5 both represent hydrogen atoms; A represents an ethylene group; B represents a methylene group; and n is O.
Claim 6
Dependent Claim 66 words
Compounds as claimed in Claim 4, in which: R 2 and R 4 are the same or different and each represents a hydrogen atom, a C 1 -C 10 alkyl group, a phenyl group, a naphthyl group, a C 3 -C 8 cycloalkyl group or a heterocyclic group having 5 or 6 ring atoms, of which from 1 to 3 are nitrogen, oxygen or sulphur hetero-atoms.
Claim 7
Dependent Claim 51 words
Compounds as claimed in Claim 4 in which R 6 represents a hydrogen atom, a C 1 -C 10 alkyl group or an aralkyl group in which the aryl part is a C 6 -C 10 carbocyclic aryl group and the alkyl part is a C 1 -C 6 alkyl group.
Claim 8
Dependent Claim 198 words
Compounds as claimed in Claim 2, in which: R represents a phenyl group or a C 2 -C 7 alkyl group; R 2 represents a C 1 -C 10 alkyl group, a phenyl group, a naphthyl group, a C 3 -C 8 cycloalkyl group or a heterocyclic group having 5 or 6 ring atoms of which from 1 to 3 are nitrogen, oxygen or sulphur hetero-atoms; R 3 , R 4 and R 5 all represent hydrogen atoms; R 6 represents a hydrogen atom, a C 1 -C 10 alkyl group or an aralkyl group of which the aryl part is a C 6 -C 10 carbocyclic aryl group and the alkyl part is a C 1 -C 6 alkyl group; R 7 represents a hydrogen atom, a (C 1 -C 4 alkoxy)carbonyloxy(C 1 -C 4 alkyl) group, a (C 2 - C 5 alkanoyl)oxy(C 1 -C 4 alkyl) group, a (5-alkyl-2-oxo-l,3-dioxolen-4-yl)alkyl group in which each alkyl group has from 1 to 4 carbon atoms, a (5-phenyl-2-oxo-1,3-dioxolen-4-yl)alkyl group in which the alkyl part has from 1 to 4 carbon atoms, or a phthalidyl group; A represents an ethylene group; B represents a methylene group; and n is 0.
Claim 9
Dependent Claim 176 words
Compounds as claimed in Claim 2, in which: R represents a phenyl group or a C 2 -C 7 alkyl groups; R 2 represents a heterocyclic group having 5 or 6 ring atoms of which from 1 to 3 are nitrogen, oxygen or sulphur hetero-atoms; R 3 , R 4 and R 5 all represent hydrogen atoms; R 6 represents a hydrogen atom, a C 1 -C 6 alkyl group or an aralkyl group of which the aryl part is a C 6 -C 10 carbocyclic aryl group and the alkyl part is a C 1 -C 4 alkyl group; R 7 represents a hydrogen atom, a (C 1 -C 4 alkoxy)carbonyloxy(C 1 -C 4 alkyl) group, a (C 2 -C 5 alkanoyl)oxy(C 1 -C 4 alkyl) group, a (5-alkyl-2-oxo-1,3-dioxolen-4-yl)alkyl group in which each alkyl part has from 1 to 4 carbon atoms, a (5-phenyl-2-oxo-l,3-dioxolen-4-yl)alkyl group in which the alkyl part has from 1 to 4 carbon atoms or a phthalidyl group; A represents an ethylene group; B represents a methylene group; and n is 0.
Claim 10
Dependent Claim 175 words
Compounds as claimed in Claim 2, in which: R 1 represents a phenyl group or a C 2 -C 7 alkyl group; R 2 represents a heterocyclic group having 5 ring atoms, of which from 1 to 3 are nitrogen, oxygen or sulphur hetero-atoms; R 3 , R 4 and R 5 all represent hydrogen atoms; R 6 represents a hydrogen atom, a C 1 -C 6 alkyl group or an aralkyl group of which the aryl part is a C 6 -C 10 carbocyclic aryl group and the alkyl part is a C 1 -C 4 alkyl group; R 7 represents a hydrogen atom, a (C 1 -C 4 alkoxy)carbonyloxy(C 1 -C 4 alkyl) group, a (C 2 -C 5 alkanoyl)oxy(C 1 -C 4 alkyl) group, a (5-alkyl-2-oxo-1,3-dioxolen-4-yl)alkyl group in which each alkyl part has from 1 to 4 carbon atoms, a (5-phenyl-2-oxo-1,3-dioxolen-4-yl)alkyl group in which the alkyl part has from 1 to 4 carbon atoms or a phthalidyl group; A represents an ethylene group; B represents a methylene group; and n is 0.
Claim 11
Dependent Claim 136 words
Compounds as claimed in Claim 2, in which: R 1 represents a phenyl group or a C 2 -C 7 alkyl group; R 2 represents a thienyl group or furyl group; R 3 , R 4 and R 5 all represent hydrogen atoms; R 6 represents a hydrogen atom, a C 1 -C 4 alkyl group, a benzyl group or phenylethyl group; R 7 represents a hydrogen atom, a (C 2 -C 5 alkanoyl)oxy(C 1 -C 3 alkyl) group, a (C 1 -C 4 alkoxy)carbonyloxy(C 1 -C 3 alkyl) group, a (2-oxo-l,3-dioxolen-4-yl)alkyl group in which the alkyl is C 1 -C 3 alkyl and which has a C 1 -C 4 alkyl or phenyl substituent at the 5-position, or a phthalidyl group; A represents an ethylene group; B represents a methylene group; and n is 0.
Claim 12
Dependent Claim 112 words
Compounds as claimed in Claim 2, in which: R represents a phenyl group or a C 2 -C 7 alkyl group; R 2 represents a 2-thienyl group, a 3-thienyl group or a 2-furyl group; R 3 , R 4 and R 5 all represent hydrogen atoms; R 6 represents a hydrogen atom, a C 1 -C 4 alkyl group or a benzyl group; R 7 represents a hydrogen atom, a (C 2 -C 5 alkanoyl)oxy(C 1 -C 3 alkyl) group, a (C 1 -C 4 alkoxy)carbonyloxy(C 1 -C 2 alkyl) group, a (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl group or a (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methyl group; A represents an ethylene group; B represents a methylene group; and n is 0.
Claim 13
Dependent Claim 157 words
Compounds as claimed in Claim 2, in which: R represents a phenyl group or a C 2 -C 7 alkyl group; R 2 represents a phenyl group, a naphthyl group, a C 1 -C 6 alkyl group or a C 3 -C 8 cycloalkyl group; R 3 , R 4 and R 5 all represent hydrogen atoms; R 6 represents a hydrogen atom, a C 1 -C 6 alkyl group or an aralkyl group of which the aryl part is a C 6 -C 10 carbocyclic aryl group and the alkyl part is a C 1 -C 4 alkyl group; R 7 represents a hydrogen atom, an acyloxyalkyl group, an alkoxycarbonyloxyalkyl group, a (2-oxo-l,3-dioxolen-4-yl)alkyl group where the alkyl group is C 1 -C 4 and which has a C 1 -C 4 alkyl or phenyl substituent at the 5-position, or a phthalidyl group; A represents an ethylene group; B represents a methylene group; and n is 0.
Claim 14
Dependent Claim 140 words
Compounds as claimed in Claim 2, in which: R 1 represents a phenyl group or a C 2 -C 7 alkyl group; R 2 represents a naphthyl group; R 3 , R 4 and R 5 all represent hydrogen atoms; R 6 represents a hydrogen atom, a C 1 -C 6 alkyl group or an aralkyl group of which the aryl part is a C 6 -C 10 carbocyclic aryl group and the alkyl part is a C 1 -C 4 alkyl group; R 7 represents a hydrogen atom, an acyloxyalkyl group, an alkoxycarbonyloxyalkyl group, a (2-oxo-l,3-dioxolen-4-yl)alkyl group where the alkyl group is C 1 -C 4 and which has a C 1 -C 4 alkyl or phenyl substituent at the 5-position, or a phthalidyl group; A represents an ethylene group; B represents a methylene group; and n is 0.
Claim 15
Dependent Claim 136 words
Compounds as claimed in Claim 2, in which: R 1 represents a phenyl group or a C 2 -C 7 alkyl group; R 2 , R 3 and R 5 all represent hydrogen atoms; R 4 represents a heterocyclic group having 5 or 6 ring atoms, of which from 1 to 3 are nitrogen, oxygen or sulphur hetero-atoms; R 6 represents a hydrogen atom, a C 1 -C 4 alkyl group, a benzyl group or a phenylethyl group; R 7 represents a hydrogen atom, an acyloxyalkyl group, an alkoxycarbonyloxyalkyl group, a (5-alkyl-2-oxo- l,3-dioxolen-4-yl)alkyl group in which each alkyl group is C 1 -C 4 , a (5-phenyl-2-oxo-1,3-dioxolen-4-yl)alkyl group in which the alkyl part is C 1 -C 4 or a phthalidyl group; A represents an ethylene group; B represents a methylene group; and n is 0.
Claim 16
Dependent Claim 151 words
Compounds as claimed in Claim 2, in which: R represents a phenyl group or a C 2 -C 7 alkyl group; R 2 , R 3 and R 5 all represent hydrogen atoms; R 4 represents a C 1 -C 6 alkyl group, a phenyl group, a naphthyl group or a C 3 -C 8 cycloalkyl group; R 6 represents a hydrogen atom, a C 1 -C 4 alkyl group, a benzyl group or a phenylethyl group; R 7 represents a hydrogen atom, a (C 2 - C 5 alkanoyl)oxy(C 1 -C 3 alkyl) group, a (C 1 -C 4 alkoxy)carbonyloxy(C 1 -C 3 alkyl) group, a (5-alkyl-2-oxo-1,3-dioxolen-4-yl)alkyl group in which each alkyl part is C 1 -C 3 , a (5-phenyl-2-oxo-l,3-dioxolen-4-yl)alkyl group in which the alkyl part is C 1 -C 3 or a phthalidyl group; A represents an ethylene group; B represents a methylene group; and n is 0,
Claim 17
Dependent Claim 9 words
α-[6-(1-carboxy-3-phenylpropylamino)-5-oxo-2-(2-thienyl)perhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 18
Dependent Claim 9 words
α-[6-(1-carboxy-3-phenylpropylamino)-5-oxo-2-(2-thienyl)perhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 19
Dependent Claim 9 words
α-[6-(1-ethoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(2-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 20
Dependent Claim 9 words
α-[6-(1-ethoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(2-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 21
Dependent Claim 9 words
α-[6-(1-butoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(2-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 22
Dependent Claim 9 words
α-[6-(1-butoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(2-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 23
Dependent Claim 9 words
α-[6-(1-carboxy-3-phenylpropylamino)-5-oxo-2-(3-thienyl)perhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 24
Dependent Claim 9 words
α-[6-(1-carboxy-3-phenylpropylamino)-5-oxo-2-(3-thienyl)perhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 25
Dependent Claim 9 words
α-[6-(1-ethoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(3-thienyl)perhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 26
Dependent Claim 9 words
α-[6-(1-ethoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(3-thienyl)perhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 27
Dependent Claim 9 words
α-[6-(1-butoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(3-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 28
Dependent Claim 9 words
α-[6-(1-butoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(3-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 29
Dependent Claim 9 words
α-[6-(1-carboxy-3-phenylpropylamino)-2-(2-furyl)-5-oxoperhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 30
Dependent Claim 9 words
α-[6-(1-carboxy-3-phenylpropylamino)-2-(2-furyl)-5-oxoperhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 31
Dependent Claim 9 words
α-[6-(1-ethoxycarbonyl-3-phenylpropylamino)-2-(2-furyl)-5-oxoperhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 32
Dependent Claim 9 words
α-[6-(1-ethoxycarbonyl-3-phenylpropylamino)-2-(2-furyl)-5-oxoperhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 33
Dependent Claim 9 words
α-[6-(1-butoxycarbonyl-3-phenylpropylamino)-2-(2-furyl)-5-oxoperhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 34
Dependent Claim 9 words
α-[6-(1-butoxycarbonyl-3-phenylpropylamino)-2-(2-furyl)-5-oxoperhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 35
Dependent Claim 9 words
α-[6-(1-carboxy-3-phenylpropylamino)-2-(3-furyl)-5-oxoperhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 36
Dependent Claim 9 words
α-[6-(1-carboxy-3-phenylpropylamino)-2-(3-furyl)-5-oxoperhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 37
Dependent Claim 9 words
α-[6-(1-ethoxycarbonyl-3-phenylpropylamino)-2-(3-furyl)-5-oxoperhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 38
Dependent Claim 9 words
α-[6-(1-ethoxycarbonyl-3-phenylpropylamino)-2-(3-furyl)-5-oxoperhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 39
Dependent Claim 9 words
α-[6-(1-butoxycarbonyl-3-phenylpropylamino)-2-(3-furyl)-5-oxoperhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 40
Dependent Claim 9 words
α-[6-(1-butoxycarbonyl-3-phenylpropylamino)-2-(3-furyl)-5-oxoperhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 41
Dependent Claim 9 words
α-[6-(1-carboxy-3-phenylpropylamino)-5-oxo-2-(1,3-thiazol-4-yl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 42
Dependent Claim 9 words
α-[6-(1-carboxy-3-phenylpropylamino)-5-oxo-2-(1,3-thiazol-4-yl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 43
Dependent Claim 9 words
α-[6-(1-ethoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(1,3-thiazol-4-yl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 44
Dependent Claim 9 words
α-[6-(1-ethoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(1,3-thiazol-4-yl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 45
Dependent Claim 9 words
α-[6-(1-butoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(1,3-thiazol-4-yl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 46
Dependent Claim 9 words
α-[6-(1-butoxycarbonyl-3-phenylpropylamino)-5-oxo-2-(1,3-thiazol-4-yl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 47
Dependent Claim 9 words
α-[6-(1-carboxynonylamino)-5-oxo-2-(2-thienyl)-perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 48
Dependent Claim 9 words
α-[6-(1-carboxynonylamino)-5-oxo-2-(2-thienyl)-perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 49
Dependent Claim 9 words
α-[6-(1-ethoxycarbonylnonylamino)-5-oxo-2-(2-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 50
Dependent Claim 9 words
α-[6-(1-ethoxycarbonylnonylamino)-5-oxo-2-(2-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 51
Dependent Claim 9 words
α-[6-(1-ethoxycarbonylnonylamino)-5-oxo-2-(3-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 52
Dependent Claim 9 words
α-[6-(1-ethoxycarbonylnonylamino)-5-oxo-2-(3-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 53
Dependent Claim 10 words
α-[6-(1-ethoxycarbonyl-3-phenylpropyl- amino)-2-(3-methyl-2-thienyl)-5-oxoperhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 54
Dependent Claim 10 words
α-[6-(1-ethoxycarbonyl-3-phenylpropyl- amino)-2-(3-methyl-2-thienyl)-5-oxoperhydro-1,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 55
Dependent Claim 10 words
α-[6-(1-ethoxycarbonyl-3-phenylpropyl- amino)-2-(5-methyl-2-thienyl)-5-oxoperhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 56
Dependent Claim 10 words
α-[6-(1-ethoxycarbonyl-3-phenylpropyl- amino)-2-(5-methyl-2-thienyl)-5-oxoperhydro-l,4-thiazepin-4-yl]acetic acid and pharmaceutically acceptable salts and esters thereof.
Claim 57
Dependent Claim 43 words
A pharmaceutical composition for the treatment of angiotensin-induced hypertension, which composition comprises a hypotensive agent in admixture with a pharmaceutically acceptable carrier or diluent, wherein said hypotensive agent is at least one compound as claimed in any one of Claims 1 to 35.
Claim 58
Dependent Claim 140 words
A process for preparing a compound as claimed in any one of Claims 1 to 35, which process comprises: condensing a compound of formula (II): (in which R 2 , R 3 , R 4 , R 5 , B and n are as defined in Claim 1 and R 7 represents a hydrogen atom or a carboxy-protecting group) with a compound of formula (III): (in which R 1 and A are as defined in Claim 1, X represents a halogen atom or a sulphonyloxy group and R 6 represents a hydrogen atom or a carboxy-protecting group) or, under reductive conditions, with a compound of formula (IV): (in which R 1 , R 6 and A are as defined above) and optionally thereafter subjecting the product to one or more of the reactions: oxidation, deprotection, esterification, group interchange or salification.

References Cited (Backward Citations)

No citation records indexed.

USPTO Annuity & Maintenance Windows

Maintenance schedule is calculated for granted US utility patents.

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag