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US4075208A
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1-Substituted-4-(2-oxo-hexahydro-1-pyrimidinyl)-piperidine
Assignee: Novartis Corp
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Filing: 1976-01-28
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Granted: 1978-02-21
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Expires: 1996-01-28
Abstract
Abstract Piperidines of the formula <IMAGE> in which R1 stands for optionally substituted aryl, R2 for hydrogen, lower alkyl, lower alkenyl, acyl or alpha -aryl-lower alkyl, R3 for a free or substituted hydroxyl group, alk for lower alkylene which separates the two nitrogen atoms by 2 or 3 carbon atoms, R4 represents hydrogen or lower alkyl and n represents an integer from 1 to 4, and their salts as well as processes for their manufacture and pharmaceutical compositions comprising such compounds, and a process for lowering the blood pressure wherein such compositions are administered to a warm-blooded host.
Inventors
- 👤 Max Wilhelm
- 👤 Kurt Eichenberger
- 👤 Herbert Schroter
- 👤 Franz Ostermayer
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 07:24
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/72; C07D213/75; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/445; A61K31/495; A61K31/63; A61K31/635
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
139 words
A piperidine compound having the formula ##STR14## wherein R 1 is phenyl, naphthyl, 5,6,7-tetrahydro-1-naphthyl or 5,6,7,8-tetrahydro-2-naphthyl, or phenyl, naphthyl, 5,6,7-tetrahydro-1-naphthyl or 5,6,7-tetrahydro-2-naphthyl which are monosubstituted or disubstituted by lower alkyl, lower alkoxy, lower alkenyl, lower alkenyloxy, halogen, halogen-lower alkyl, carbamoyl, lower alkyl-substituted carbamoyl, lower alkoxycarbonylamino-lower alkyl, lower alkoxy-lower alkoxy, lower alkanoylaminoethenyl, lower akylthio-lower alkoxy, hydroxyl, lower alkanoyl, lower alkoxy-lower alkyl, lower alkynyl, lower alkylthio-lower alkyl, hydroxy-lower alkyl, lower alkanoyloxy, lower alkylthio, lower alkanoyl amino, cyano, amino, nitro, ureido, lower alkylated ureido, phenyl-lower alkoxy, and/or lower alkynyloxy, R 2 is hydrogen, lower alkyl, lower alkenyl, α-phenyl-lower alkyl or lower alkanoyl, R 3 is hydroxyl, a lower alkanoyloxy or a lower alkoxy, R 4 is hydrogen or lower alkyl, n is an integer from 0 to 4, and alk is trimethylene or mono-lower alkylated trimethylene or a therapeutically acceptable salt thereof.
Claim 2
Dependent Claim
139 words
A piperidine compound having the formula ##STR14## wherein R 1 is phenyl, naphthyl, 5,6,7-tetrahydro-1-naphthyl or 5,6,7,8-tetrahydro-2-naphthyl, or phenyl, naphthyl, 5,6,7-tetrahydro-1-naphthyl or 5,6,7-tetrahydro-2-naphthyl which are monosubstituted or disubstituted by lower alkyl, lower alkoxy, lower alkenyl, lower alkenyloxy, halogen, halogen-lower alkyl, carbamoyl, lower alkyl-substituted carbamoyl, lower alkoxycarbonylamino-lower alkyl, lower alkoxy-lower alkoxy, lower alkanoylaminoethenyl, lower akylthio-lower alkoxy, hydroxyl, lower alkanoyl, lower alkoxy-lower alkyl, lower alkynyl, lower alkylthio-lower alkyl, hydroxy-lower alkyl, lower alkanoyloxy, lower alkylthio, lower alkanoyl amino, cyano, amino, nitro, ureido, lower alkylated ureido, phenyl-lower alkoxy, and/or lower alkynyloxy, R 2 is hydrogen, lower alkyl, lower alkenyl, α-phenyl-lower alkyl or lower alkanoyl, R 3 is hydroxyl, a lower alkanoyloxy or a lower alkoxy, R 4 is hydrogen or lower alkyl, n is an integer from 0 to 4, and alk is trimethylene or mono-lower alkylated trimethylene or a therapeutically acceptable salt thereof.
Claim 3
Dependent Claim
62 words
The compound of claim 1, wherein R 1 is a phenyl or phenyl mono- or di-substituted by lower alkyl, lower alkoxy, lower alkenyl, lower alkenyloxy, lower alkanoyl, lower alkanoylamino, hydroxyl, benzyloxy, N-lower alkylcarbamoyl or halogen, R 2 is hydrogen or lower alkyl, R 3 is hydroxyl, R 4 is hydrogen or methyl, n is 1 and alk is trimethylene or monomethylated trimethylene.
Claim 4
Dependent Claim
38 words
The compound of claim 1, wherein R 1 is phenyl monosubstituted by methyl, methoxy, allyl, allyloxy, hydroxyl, acetylamino, propionyl, N-methyl-carbamoyl or chlorine, R 2 is hydrogen, R 3 is hydroxyl, R 4 is hydrogen and alk is trimethylene.
Claim 5
Dependent Claim
44 words
The compound of claim 1, wherein the compound has the formula ##STR15## in which R' stands for halogen, lower alkyl or lower alkoxy, R" for lower alkyl or hydrogen, R'" for methyl or hydrogen and alk' for trimethylene or a therapeutically acceptable salt thereof.
Claim 6
Dependent Claim
32 words
The compounds of claim 1, wherein the compound has the formula ##STR16## in which R' stands for lower alkyl or lower alkoxy and alk' for trimethylene or a therapeutically acceptable salt thereof.
Claim 7
Dependent Claim
15 words
A compound as claimed in claim 1, being 1-[3-(o-chlorophenoxy)-2-hydroxypropyl]-4-(2-oxo-hexahydro-1-pyrimidinyl)-piperidine or a therapeutically acceptable salt thereof.
Claim 8
Dependent Claim
14 words
A 3as claimed in claim 1, being 1-[3-(o-methylphenoxy)-2-hydroxypropyl]-4-(2-oxo-hexahydro-1-pyrimidinyl)piperidine or a therapeutically acceptable salt thereof.
Claim 9
Dependent Claim
15 words
A compound as claimed in claim 1, being 1-[3-(o-methoxyphenoxy)-2-hydroxypropyl]-4-(2-oxo-hexahydro-1-pyrimidinyl)-piperidine or a therapeutically acceptable salt thereof.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-02-20 | 1981-08-22 | 1982-02-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-02-20 | 1985-08-22 | 1986-02-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-02-20 | 1989-08-22 | 1990-02-21 | $7700.00 | Window Closed / Lapsed |