Patent · US4400511A · A · US
2-Substituted octahydropyrrolo(1,2-A)-pyrazine-3-carboxylic acids
- (11) Publication number
- US4400511A
- (21) Application number
- US-37585882-A
- (22) Filing date
- 1982-05-07
- (30) Priority date
- 1982-05-07
- (43) Publication date
- 1983-08-23
- (45) Date of grant
- 1983-08-23
- (52) CPC
- C07D Heterocyclic compounds: 487/04
- (73) Assignee
- AMERICAN HOME PROD
- (54) Title
- 2-Substituted octahydropyrrolo(1,2-A)-pyrazine-3-carboxylic acids
- (57) Abstract
The compounds ##STR1## where R is hydrogen, alkyl, phenylalkyl or dialkylamino alkyl; R 1 is hydrogen, alkyl or phenyl; X is --S-- or --NH-- A is hydrogen, acyl, aroyl, alkyl or substituted alkyl in which the substituent is alkoxycarbonyl or phenylalkyl; n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof are antihypertensive agents of the ACE inhibitor type.
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Claims (6)
- A compound of the formula ##STR5## in which R is hydrogen, alkyl of 1 to 6 carbon atoms, phenylalkyl of 7 to 12 carbon atoms, or dialkylaminoalkyl where each alkyl group has 1 to 6 carbon atoms; R 1 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl; X is --S-- or --NH--; A is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxycarbonylalkyl in which each alkyl moiety has 1 to 6 carbon atoms, phenylalkyl of 7 to 12 carbon atoms, phenyl(alkoxycarbonyl)alkyl in which each alkyl group has 1 to 6 carbon atoms, alkanoyl of 2 to 7 carbon atoms, benzoyl or naphthoyl; and n is one of the integers 0, 1 or 2 or a pharmaceutically acceptable salt thereof.
- The compound of claim 1 which is 4-(3-benzoylthio-2-methylpropionyl)-1,4-diazabicyclo[4.3.0]nonane-3-carboxylic acid or a pharmaceutically acceptable salt thereof.
- The compound of claim 1 which is 4-(3-mercapto-2-methylpropionyl)-1,4-diazabicyclo[4.3.0]nonane-3-carboxylic acid or a pharmaceutically acceptable salt thereof.
- The compound of claim 1 which is 4-(3-benzoylthiopropionyl)-1,4-diazabicyclo[4.3.0]nonane-3-carboxylic acid or a pharmaceutically acceptable salt thereof.
- The compound of claim 1 which is 4-(3-mercaptopropionyl)-1,4-diazabicyclo[4.3.0]nonane-3-carboxylic acid or a pharmaceutically acceptable salt thereof.
- The compound of claim 1 which is 4-[2-[[1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]-1,4-diazabicyclo[4.3.0nonane-3-carboxylic acid or a pharmaceutically acceptable salt thereof.
Citations (4)
- JPS5088093A
- US3531485A
- US4291163A
- US4294832A
Record as JSON
{
"publication_number": "US4400511A",
"country": "US",
"kind": "A",
"title": "2-Substituted octahydropyrrolo(1,2-A)-pyrazine-3-carboxylic acids",
"abstract": "The compounds ##STR1## where R is hydrogen, alkyl, phenylalkyl or dialkylamino alkyl; R 1 is hydrogen, alkyl or phenyl; X is --S-- or --NH-- A is hydrogen, acyl, aroyl, alkyl or substituted alkyl in which the substituent is alkoxycarbonyl or phenylalkyl; n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof are antihypertensive agents of the ACE inhibitor type.",
"claims": [
"1. A compound of the formula ##STR5## in which R is hydrogen, alkyl of 1 to 6 carbon atoms, phenylalkyl of 7 to 12 carbon atoms, or dialkylaminoalkyl where each alkyl group has 1 to 6 carbon atoms; R 1 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl; X is --S-- or --NH--; A is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxycarbonylalkyl in which each alkyl moiety has 1 to 6 carbon atoms, phenylalkyl of 7 to 12 carbon atoms, phenyl(alkoxycarbonyl)alkyl in which each alkyl group has 1 to 6 carbon atoms, alkanoyl of 2 to 7 carbon atoms, benzoyl or naphthoyl; and n is one of the integers 0, 1 or 2 or a pharmaceutically acceptable salt thereof.",
"2. The compound of claim 1 which is 4-(3-benzoylthio-2-methylpropionyl)-1,4-diazabicyclo[4.3.0]nonane-3-carboxylic acid or a pharmaceutically acceptable salt thereof.",
"3. The compound of claim 1 which is 4-(3-mercapto-2-methylpropionyl)-1,4-diazabicyclo[4.3.0]nonane-3-carboxylic acid or a pharmaceutically acceptable salt thereof.",
"4. The compound of claim 1 which is 4-(3-benzoylthiopropionyl)-1,4-diazabicyclo[4.3.0]nonane-3-carboxylic acid or a pharmaceutically acceptable salt thereof.",
"5. The compound of claim 1 which is 4-(3-mercaptopropionyl)-1,4-diazabicyclo[4.3.0]nonane-3-carboxylic acid or a pharmaceutically acceptable salt thereof.",
"6. The compound of claim 1 which is 4-[2-[[1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]-1,4-diazabicyclo[4.3.0nonane-3-carboxylic acid or a pharmaceutically acceptable salt thereof."
],
"cpc": [
"C07D 487/04"
],
"assignees": [
"AMERICAN HOME PROD"
],
"filing_date": "1982-05-07",
"publication_date": "1983-08-23",
"grant_date": "1983-08-23",
"priority_date": "1982-05-07",
"application_number": "US-37585882-A",
"family_id": "23482660",
"citations": [
"JPS5088093A",
"US3531485A",
"US4291163A",
"US4294832A"
]
}
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