US4619941A
Expired / Lapsed
US
⏱️ 0.0 years remaining
N-[(1H-imidazol-1-yl)alkyl]-1H-indolecarboxamides useful as thromboxane synthetase inhibitors and antihypertensive agents
Assignee: Wyeth Holdings LLC
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Filing: 1984-11-19
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Granted: 1986-10-28
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Expires: 2004-11-19
Abstract
Abstract This invention discloses novel N-[(1H-imidazol-1-yl)alkyl]-1H-indolecarboxamides which are useful as inhibitors of thromboxane synthetase and/or as antihypertensive agents in the treatment of hypertension and myocardial ischemia.
Inventors
- 👤 William B. Wright, Jr.
- 👤 Jeffery B. Press
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 21:50
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/02; C07D231/10; C07D231/12; C07D233/00; C07D233/54; C07D233/56; C07D249/00; C07D249/02; C07D249/08; C07D403/00; C07D403/02; C07D403/12
Claims Analysis
Total Claims: 37
Claim 1
Independent Claim
87 words
A compound of the formula: ##STR5## wherein R 1 is selected from the group consisting of hydrogen, halogen, alkyl(C 1 -C 3 ) and alkoxy (C 1 -C 3 ); R 2 is selected from the group consisting of hydrogen, alkyl (C 1 -C 3 ) and benzyl; n is an integer from 2 to 8 inclusive; R 3 and R 4 are each individually selected from the group consisting of hydrogen, alkyl (C 1 -C 3 ) and phenyl; or a pharmaceutically acceptable acid-addition salt thereof.
Claim 2
Dependent Claim
87 words
A compound of the formula: ##STR5## wherein R 1 is selected from the group consisting of hydrogen, halogen, alkyl(C 1 -C 3 ) and alkoxy (C 1 -C 3 ); R 2 is selected from the group consisting of hydrogen, alkyl (C 1 -C 3 ) and benzyl; n is an integer from 2 to 8 inclusive; R 3 and R 4 are each individually selected from the group consisting of hydrogen, alkyl (C 1 -C 3 ) and phenyl; or a pharmaceutically acceptable acid-addition salt thereof.
Claim 3
Dependent Claim
7 words
The compound according to claim 1; N-[3-(1H-imidazol-1-yl)propyl]-1-methyl-1H-indole-2-carboxamide.
Claim 4
Dependent Claim
7 words
The compound according to claim 1; N-[3-(1H-imidazol-1-yl)propyl]-5-methoxy-1H-indole-2-carboxamide.
Claim 5
Dependent Claim
7 words
The compound according to claim 1: N-[-3-1H-imidazol-1-yl)propyl]-1H-indole-2-carboxamide.
Claim 6
Dependent Claim
7 words
The compound according to claim 1; N-[-3-(1H-imidazol-1-yl)propyl]-1H-indole-5-carboximide.
Claim 7
Dependent Claim
7 words
The compound according to claim 1; 5-chloro-N-[3-(1Himidazol-1-yl)propyl]-1H-indole-2-carboxamide.
Claim 8
Dependent Claim
7 words
The compound according to claim 1; 1-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)proply]-1H-indole-2-carboxamide.
Claim 9
Dependent Claim
7 words
The compound according to claim 1; 5-chloro-N-[3-(4-methyl-1H-imidazol-1-yl)propyl]-1H-indole-2-carboxamide.
Claim 10
Dependent Claim
7 words
The compound according to claim 1; N-[4-(1H-imidazol-1-yl)butyl]-1H-indole-2-carboxamide.
Claim 11
Dependent Claim
7 words
The compound according to claim 1; 5-methoxy-N-[4-(1H-imidazol-1-yl)butyl]-1H-indole-2-carboxamide.
Claim 12
Dependent Claim
7 words
The compound according to claim 1; N-[3(2-methyl-1H-imidazol-1-yl)propyl]-1H-indole-2-carboximide.
Claim 13
Dependent Claim
8 words
The compound according to claim 1; 5-methoxy-N-[3-(2-methyl)-1H-imidazol-1-yl)propyl]-1H- indole-2-carboxamide.
Claim 14
Dependent Claim
7 words
The compound according to claim 1; N-[3-(2-methyl-1H-imidazol-1-yl)propyl]-1H-indole-5-carboxamide.
Claim 15
Dependent Claim
7 words
The compound according to claim 1; N-[3-(2-phenyl-1H-imidazol-1-yl)propyl]-1H-indole-2-carboxamide.
Claim 16
Dependent Claim
7 words
The compound according to claim 1; 1-methyl-N-[3-(2-methyl-1H-imidazol-1-yl)propyl]-1H-indole-2-carboxamide.
Claim 17
Dependent Claim
7 words
The compound according to claim 1; 5-chloro-N-[5-(1H-imidazol-1-yl)pentyl]-1H-indole-2-carboxamide.
Claim 18
Dependent Claim
7 words
The compound according to claim 1; 5-chloro-N-[4-(1H-imidazol-1-yl)butyl]-1H-indole-2-carboxamide.
Claim 19
Dependent Claim
7 words
The compound according to claim 1; 5-chloro-N-[8-(1H-imidazol-1-yl)octyl]-1H-indole-2-carboxamide.
Claim 20
Dependent Claim
7 words
The compound according to claim 1; N-[3-(4-methyl-1H-imidazol-1-yl)-propyl]-1H-indole-2-carboxamide.
Claim 21
Dependent Claim
7 words
The compound according to claim 1; N-[3-(1H-imidazol-1-yl)-propyl]-5-methyl-1H-indole-2-carboxamide.
Claim 22
Dependent Claim
7 words
The compound according to claim 1; 5-fluoro-N-[3-(1H-imidazol-1-yl)propyl]-1H-indole-2-carboxamide.
Claim 23
Dependent Claim
8 words
The compound according to claim 1; N-[3-(2-ethyl-1H-imidazol-1-yl)propyl]-1-methyl-1H-indole-2- carboxamide.
Claim 24
Dependent Claim
7 words
The compound according to claim 1; 1-benzyl-N-[4-(1H-imidazol-1-yl)butyl]-1H-indole-2-carboxamide.
Claim 25
Dependent Claim
7 words
The compound according to claim 1; 5-chloro-N-[6-(1H-imidazol-1-yl)hexyl]-1H-indole-2-carboxamide.
Claim 26
Dependent Claim
7 words
The compound according to claim 1; 5-bromo-1-methyl-N-[3-(2-methyl-1H-imidazol-1-yl)propyl]-1H-indole-2-carboxamide.
Claim 27
Dependent Claim
7 words
The compound according to claim 1; 5-chloro-N-[2-(1H-imidazol-1-yl)ethyl]-1H-indole-2-carboxamide.
Claim 28
Dependent Claim
7 words
The compound according to claim 1; N-[3-(2-phenyl-1H-imidazol-1-yl)propyl]-1H-indole-2-carboxamide.
Claim 29
Dependent Claim
7 words
The compound according to claim 1; N-[3-(4-phenyl-1H-imidazol-1-yl)propyl]-1H-indole-2-carboxamide.
Claim 30
Dependent Claim
8 words
The compound according to claim 1; 5-chloro-N-[3-(1H-imidazol-1-yl)-2-methylpropyl]-1H-indole-2- carboxamide.
Claim 31
Dependent Claim
7 words
The compound according to claim 1; 5-chloro-N-[3-(1H-imidazol-1-yl)-butyl]-1H-indole-2-carboxamide.
Claim 32
Dependent Claim
31 words
A method of inhibiting thromboxane synthetase enzyme in a mammal which comprises administering internally to said mammal an effective amount of a compound of the formula as recited in claim 1.
Claim 33
Dependent Claim
31 words
A method of lowering elevated blood pressure in a mammal which comprises administering internally to said mammal an effective amount of a compound of the formula as recited in claim 1.
Claim 34
Dependent Claim
35 words
A thromboxane synthetase enzyme inhibiting composition of matter in dosage unit form which comprises an effective amount of a compound of the formula as recited in claim 1 in association with a pharmaceutically acceptable carrier.
Claim 35
Dependent Claim
36 words
A thromboxane synthetase enzyme inhibiting composition of matter, as recited in claim 33, wherein the dosage unit comprises from about 10 mg to about 700 mg of the compound in association with the pharmaceutically acceptable carrier.
Claim 36
Dependent Claim
40 words
A therapeutic composition of matter in dosage unit form useful for lowering elevated blood pressure in mammals which comprises an effective amount of a compound of the formula as recited in claim 1 in association with a pharmaceutically acceptable carrier.
Claim 37
Dependent Claim
32 words
A therapeutic composition of matter as recited in claim 35 wherein the dosage unit comprises from about 10 mg to 700 mg of the compound in association with the pharmaceutically acceptable carrier.
References Cited (Backward Citations)
US4489089A
Cited
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| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1989-10-27 | 1990-04-28 | 1990-10-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-10-27 | 1994-04-28 | 1994-10-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-10-27 | 1998-04-28 | 1998-10-28 | $7700.00 | Window Closed / Lapsed |