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US4147786A
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1-Indolylalkyl-3-or 4-trimethyleneurido-piperidines
Assignee: Novartis Corp
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Filing: 1977-05-16
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Granted: 1979-04-03
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Expires: 1997-05-16
Abstract
Abstract 1-(Indolyl-3-alkyl)-3 or 4-(ureido or guanidino)-piperidines, e.g. those of the formula ##STR1## acyl derivatives and salts thereof are antihypertensive agents.
Inventors
- 👤 Charles F. Huebner
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 16:53
CPC Classifications
C; C07; C07D; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07D209/14; C07D209/30; C07D209/32; C07D209/34; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/56; C07D211/58
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
128 words
A compound of the formula ##STR14## wherein Ph is unsubstituted 1,2-phenylene or 1,2-phenylene substituted by one member selected from lower alkyl, hydroxy, mercapto, lower alkoxy, lower alkenedioxy having 1 or 2 carbon atoms, benzyloxy, lower alkylmercapto, halogeno, triflouromethyl, nitro and amino; each of R 1 and R 2 is hydrogen or lower alkyl; (R 3 +R 4 ) is lower alkylene separating both nitrogens by 3 carbon atoms; R 5 is hydrogen, lower alkyl or phenyl unsubstituted or substituted in the positions 3 to 6 as defined for Ph above; X is oxygen, sulfur, imino or lower alkylimino; m is an integer from 1 to 7; each of p and q is an integer from 1 to 3, but (p+q)=4; or a therapeutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
128 words
A compound of the formula ##STR14## wherein Ph is unsubstituted 1,2-phenylene or 1,2-phenylene substituted by one member selected from lower alkyl, hydroxy, mercapto, lower alkoxy, lower alkenedioxy having 1 or 2 carbon atoms, benzyloxy, lower alkylmercapto, halogeno, triflouromethyl, nitro and amino; each of R 1 and R 2 is hydrogen or lower alkyl; (R 3 +R 4 ) is lower alkylene separating both nitrogens by 3 carbon atoms; R 5 is hydrogen, lower alkyl or phenyl unsubstituted or substituted in the positions 3 to 6 as defined for Ph above; X is oxygen, sulfur, imino or lower alkylimino; m is an integer from 1 to 7; each of p and q is an integer from 1 to 3, but (p+q)=4; or a therapeutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
120 words
A compound as claimed in claim 1, in which formula Ph is 1,2-phenylene unsubstituted or monosubstituted by lower alkyl, hydroxy, mercapto, lower alkoxy, lower alkylenedioxy, benzyloxy, lower alkylmercapto, halogeno, trifluoromethyl, nitro or amino; each of R 1 and R 2 is hydrogen or lower alkyl; (R 3 +R 4 ) is lower alkylene separating both nitrogenes by 3 carbon atoms; R 5 is hydrogen, lower alkyl or phenyl unsubstituted or monosubstituted in the positions 3 to 6 as defined for Ph above; X is oxygen, sulfur, imino or lower alkylimino; m is an integer from 1 to 4; each of p and q is an integer from 1 to 3, but (p+q)=4; or a therapeutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
109 words
A compound as claimed in claim 1, in which formula Ph is 1,2-phenylene unsubstituted or substituted by hydroxy, mercapto or, alkyl, alkoxy or alkylmercapto each with up to 4 carbon atoms, benzyloxy, halogeno, trifluoromethyl, nitro or amino; each of R 1 , R 2 and R 5 is hydrogen or alkyl with up to 4 carbon atoms (R 3 +R 4 ) is alkylene with 3 to 4 carbon atoms separating both nitrogens by 3 carbon atoms; X is oxygen, nitrogen or imino; m is an integer from 1 to 4 and each of p and q is the integer 2; or a therapeutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
64 words
A compound as claimed in claim 3 and corresponding to the formula ##STR15## wherein R is hydrogen, hydroxy, mercapto or, alkyl, alkoxy or alkylmercapto each with up to 4 carbon atoms, benzyloxy, halogeno, trifluoromethyl, nitro or amino; m is an integer from 1 to 4; n is the integer 3 and X is oxygen, sulfur or imino; or therapeutically acceptable acid addition salts thereof.
Claim 6
Dependent Claim
54 words
A compound as claimed in claim 4, in which formula R is hydrogen, methyl, hydroxy, mercapto, methoxy, benzyloxy, methylmercapto, fluoro, chloro, bromo, trifluoromethyl, nitro or amino; m is an integer from 1 to 4; n is the integer 3 and X is oxygen, sulfur or imino; or a therapeutically acceptable acid addition salt thereof.
Claim 7
Dependent Claim
11 words
A compound as claimed in claim 4 and being the 1-(2-indolyl-3-ethyl)-4-(1,3-propyleneureido)-piperidine.
Claim 8
Dependent Claim
21 words
A hypotensive pharmaceutical composition comprising a pharmacologically effective amount of a compound claimed in claim 1, together with a pharmaceutical excipient.
Claim 9
Dependent Claim
27 words
A method for reducing the blood pressure in mammals, which comprises administering to them enterally or parenterally an effective amount of a composition claimed in claim 7.
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) | 1982-04-02 | 1982-10-02 | 1983-04-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-04-02 | 1986-10-02 | 1987-04-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-04-02 | 1990-10-02 | 1991-04-03 | $7700.00 | Window Closed / Lapsed |