EP0230266A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Functionalized peptidyl aminodiols and -triols
Assignee: Abbott Laboratories
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Filing: 1987-01-15
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Granted: —
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Expires: 2007-01-15
Abstract
Abstract The invention relates to renin inhibiting compounds of the formula wherein A is hydrogen; loweralkyl; arylalkyl; OR₈ or SR₈ wherein R₈ is hydrogen, loweralkyl or aminoalkyl; NR₉R₁₀ wherein R₉ and R₁₀ are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; wherein B is NH, alkylamino, S, O, CH₂ or CHOH and R₁₁ is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, carboxylic acid-substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected) alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R₁ is loweralkyl, cycloalkylmethyl, benzyl, α-methylbenzyl, α, α-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R₁ is phenoxy, thiophenoxy or anilino, B is CH₂ or CHOH or A is hydrogen; R₃ is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R₄ is loweralkyl, cycloalkyl- methyl or benzyl; R₂, R₅ and R₆ are independently hydrogen or loweralkyl; X is O, NH or S; R₇ is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl. wherein R₁₂ and R₁₃ are independently hydrogen or loweralkyl, n is 0-2 and R₁₄ is substituted or unsubstituted penyl or heterocyclic; or XR₇ together are loweralkylsulfonyl, N₃ or Cl, and pharmaceutically acceptable salts thereof.
Inventors
- 👤 Saul Howard Rosenberg
- 👤 Jacob John Plattner
- 👤 Jay Richard Luly
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-08 13:14
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/14; C07D; C07D233/00; C07D233/54; C07D233/64; C07K5/00; C07K5/02; C07K5/0227; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06034; C07K5/06043; C07K5/06078; C07K5/08; C07K5/0802; C07K5/0804; C07K5/0806; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
191 words
A renin inhibiting compound of the formula: wherein A is hydrogen; loweralkyl; arylalkyl; OR₈ or SR₈ wherein R₈ is hydrogen, loweralkyl or aminoalkyl; NR₉R₁₀ wherein R₉ and R₁₀ are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; wherein B is NH, alkylamino, S, O, CH₂ or CHOH and R₁₁ is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, carboxylic acid- substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, (dihydroxyalkyl)(alkyl)amino, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected)- (alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R₁ is loweralkyl, cycloalkylmethyl, benzyl, α-methylbenzyl, α, α-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R₁ is phenoxy, thiophenoxy or anilino, B is CH₂ or CHOH or A is hydrogen; R₃ is loweralkyl, benzyl or heterocyclic ring substituted methyl; R₄ is loweralkyl, cycloalkylmethyl or benzyl; R₂, R₅ and R₆ are independently hydrogen or loweralkyl; X is O, NH or S; R₇ is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl, wherein R₁₂ and R₁₃ are independently hydrogen or loweralkyl, n is 0-2 and R₁₄ is substituted or unsubstituted phenyl or heterocyclic; or XR₇ together are loweralkylsulfonyl, N₃ or Cl, and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
191 words
A renin inhibiting compound of the formula: wherein A is hydrogen; loweralkyl; arylalkyl; OR₈ or SR₈ wherein R₈ is hydrogen, loweralkyl or aminoalkyl; NR₉R₁₀ wherein R₉ and R₁₀ are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; wherein B is NH, alkylamino, S, O, CH₂ or CHOH and R₁₁ is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, carboxylic acid- substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, (dihydroxyalkyl)(alkyl)amino, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected)- (alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R₁ is loweralkyl, cycloalkylmethyl, benzyl, α-methylbenzyl, α, α-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R₁ is phenoxy, thiophenoxy or anilino, B is CH₂ or CHOH or A is hydrogen; R₃ is loweralkyl, benzyl or heterocyclic ring substituted methyl; R₄ is loweralkyl, cycloalkylmethyl or benzyl; R₂, R₅ and R₆ are independently hydrogen or loweralkyl; X is O, NH or S; R₇ is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl, wherein R₁₂ and R₁₃ are independently hydrogen or loweralkyl, n is 0-2 and R₁₄ is substituted or unsubstituted phenyl or heterocyclic; or XR₇ together are loweralkylsulfonyl, N₃ or Cl, and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
35 words
The renin inhibiting compound of Claim 1 wherein B is NH, R₁ is benzyl, 4-methoxybenzyl or isobutyl; R₃ is loweralkyl, (4-imidazoyl)methyl or (3-pyrazoyl)methyl; R₄ is loweralkyl or cycloalkyl methyl and R₅ and R₆ are hydrogen.
Claim 4
Dependent Claim
24 words
The renin inhibiting compound of Claim 2 wherein A is BocNH; R₁ is benzyl; R₂ is (4-imidazoyl)methyl; R₄ is cyclohexylmethyl; and XR₇ is N₃.
Claim 5
Dependent Claim
24 words
The renin inhibiting compound of Claim 2 wherein A is BocNH; R₁ is 4-methoxybenzyl; R₃ is (4-imidazoyl)methyl; R₄ is cyclohexylmethyl and XR₇ is N₃.
Claim 6
Dependent Claim
24 words
The renin inhibiting compound of Claim 2 wherein A is BocNH; R₁ is benzyl; R₃ is (4-imidazoyl)methyl; R₄ is cyclohexylmethyl and R₇ is isopropyl.
Claim 7
Dependent Claim
11 words
The renin inhibiting compound of Claim 5 wherein X is S.
Claim 8
Dependent Claim
11 words
The renin inhibiting compound of Claim 5 wherein X is SO₂.
Claim 9
Dependent Claim
11 words
The renin inhibiting compound of Claim 5 wherein X is O.
Claim 10
Dependent Claim
23 words
The renin inhibiting compound of Claim 2 wherein A is ethoxycarbonylamino; R₁ and R₃ are isobutyl; R₄ is cyclohexylmethyl; and XR₇ is Cl.
Claim 11
Dependent Claim
204 words
A pharmaceutical composition for treating renin-associated hypertension, comprising a pharmaceutical carrier and a therapeutically effective amount of the compound of the formula: wherein A is hydrogen; loweralkyl; arylalkyl, OR₈ or SR₈ wherein R₈ is hydrogen, loweralkyl or aminoalkyl; NR₉R₁₀ wherein R₉ and R₁₀ are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; wherein B is NH, alkylamino, S, O, CH₂ or CHOH and R₁₁ is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, carboxylic acid-substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected)(alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R₁ is loweralkyl, cycloalkylmethyl benzyl, α-methylbenzyl, α, α-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiopenoxy or anilino; provided if R₁ is phenoxy, thiophenoxy or anilino, B is CH₂ or CHOH or A is hydrogen; R₃ is loweralkyl, benzyl or hetero cyclic ring-substituted methyl; R₄ is loweralkyl, cycloalkyl- methyl or benzyl; R₂, R₅ and R₆ are independently hydrogen or loweralkyl; X is O, NH or S; R₇ is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl, wherein R₁₂ and R₁₃ are independently hydrogen or loweralkyl, n is 0-2 and R₁₄ is substituted or unsubstituted phenyl or heterocyclic; or XR₇ together are loweralkylsulfonyl, N₃ or Cl, and pharmaceutically acceptable salts thereof.
Claim 12
Dependent Claim
204 words
A pharmaceutical composition for treating renin-associated hypertension, comprising a pharmaceutical carrier and a therapeutically effective amount of the compound of the formula: wherein A is hydrogen; loweralkyl; arylalkyl, OR₈ or SR₈ wherein R₈ is hydrogen, loweralkyl or aminoalkyl; NR₉R₁₀ wherein R₉ and R₁₀ are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; wherein B is NH, alkylamino, S, O, CH₂ or CHOH and R₁₁ is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, carboxylic acid-substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected)(alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R₁ is loweralkyl, cycloalkylmethyl benzyl, α-methylbenzyl, α, α-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiopenoxy or anilino; provided if R₁ is phenoxy, thiophenoxy or anilino, B is CH₂ or CHOH or A is hydrogen; R₃ is loweralkyl, benzyl or hetero cyclic ring-substituted methyl; R₄ is loweralkyl, cycloalkyl- methyl or benzyl; R₂, R₅ and R₆ are independently hydrogen or loweralkyl; X is O, NH or S; R₇ is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl, wherein R₁₂ and R₁₃ are independently hydrogen or loweralkyl, n is 0-2 and R₁₄ is substituted or unsubstituted phenyl or heterocyclic; or XR₇ together are loweralkylsulfonyl, N₃ or Cl, and pharmaceutically acceptable salts thereof.
References Cited (Backward Citations)
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