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US4410539A
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Heterocyclic thromboxane synthetase inhibitors and pharmaceutical compositions containing them
Assignee: Pfizer Inc
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Filing: 1981-10-20
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Granted: 1983-10-18
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Expires: 2001-10-20
Abstract
Abstract Heterocyclic thromboxane synthetase inhibitors of the formula <IMAGE> (I) wherein R1, which is attached to the 2-, 3- or 4-position, is hydrogen, halogen, C1-C4 alkyl, hydroxy or C1-C4 alkoxy; Y, which is attached to the 2- or 3-position, is -COOH, -COO(C1-C4 alkyl) or -CONH2; X is O, S, NH, N(C1-C4 alkyl) or N(benzyl); and R, which is attached to the 5-, 6- or 7-position, is a group of the formula <IMAGE> or (3- or 4-pyridyl)-Z2- wherein Z1 is -CH2-, -CH2CH2- or -CH2CH2O- and Z2 is -CH2-, -CH2CH2-, -CH=CH-, -CH2O- or -OCH2-; and their pharmaceutically acceptable salts; processes for their preparation, and pharmaceutical compositions containing them.
Inventors
- 👤 Peter E. Cross
- 👤 Roger P. Dickinson
- 👤 Geoffrey N. Thomas
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 04:02
CPC Classifications
C; C07; C07D; C07D333/00; C07D333/50; C07D333/52; C07D333/54; A; A61; A61P; A61P25/00; A61P25/28; A61P3/00; A61P3/08; A61P3/10; A61P35/00; A61P43/00; A61P7/00; A61P7/02; C07D209/00; C07D209/02; C07D209/04; C07D209/30; C07D209/42; C07D231/00; C07D231/02; C07D231/10; C07D231/12; C07D233/00; C07D233/54; C07D233/56; C07D249/00; C07D249/02; C07D249/08; C07D307/00; C07D307/77; C07D307/78; C07D307/82; C07D307/84; C07D307/85; C07D333/62; C07D333/68; C07D333/70
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
103 words
A compound of the formula: ##STR88## wherein R 1 , which is attached to the 2-, 3- or 4-position, is hydrogen, halogen, C 1 -C 4 alkyl, hydroxy, or C 1 -C 4 alkoxy; Y, which is attached to the 2- or 3-position, is --COOH, --COO(C 1 -C 4 alkyl) or --CONH 2 ; X is O, S, NH or N(benzyl); and R, which is attached to the 5-, 6- or 7-position, is a group of the formula: ##STR89## wherein Z 1 is --CH 2 --, --CH 2 CH 2 -- or --CH 2 CH 2 O--; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
103 words
A compound of the formula: ##STR88## wherein R 1 , which is attached to the 2-, 3- or 4-position, is hydrogen, halogen, C 1 -C 4 alkyl, hydroxy, or C 1 -C 4 alkoxy; Y, which is attached to the 2- or 3-position, is --COOH, --COO(C 1 -C 4 alkyl) or --CONH 2 ; X is O, S, NH or N(benzyl); and R, which is attached to the 5-, 6- or 7-position, is a group of the formula: ##STR89## wherein Z 1 is --CH 2 --, --CH 2 CH 2 -- or --CH 2 CH 2 O--; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
29 words
A compound according to claim 1 wherein X is O; R is (1-imidazolyl)methyl; R 1 is hydrogen or 3-methyl; and Y is --COOH, --COOCH 3 or --CONH 2 .
Claim 4
Dependent Claim
54 words
A compound according to claim 1 wherein R 1 is attached to the 2- or 3-position and is hydrogen, halogen, C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and R is a group of the formula: ##STR90## wherein n is 1 or 2; or a pharmaceutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
27 words
A compound according to claim 3 wherein X is S; R 1 is hydrogen, methyl or methoxy; Y is --COOH; and R is attached to the 6-position.
Claim 6
Dependent Claim
18 words
The compound according to claim 4 wherein R 1 is 3-methyl; Y is 2-COOH; and R is ##STR91##
Claim 7
Dependent Claim
37 words
A compound according to claim 1 in which X is S; Y is --COOH, --COOCH 3 , --COOC 2 H 5 or --CONH 2 ; and R 1 is hydrogen, 3-chloro, 2- or 3-methyl, 4-methoxy or 4-hydroxy.
Claim 8
Dependent Claim
23 words
A compound according to claim 6 wherein Y is --COOH; R 1 is hydrogen, 2- or 3-methyl, or 4-methoxy; and R is (1-imidazolyl)methyl.
Claim 9
Dependent Claim
28 words
A compound according to claim 1 in which X is NH or N(benzyl); R 1 is hydrogen; R is (1-imidazolyl)methyl; and Y is --COOH or --COOCH 3 .
Claim 10
Dependent Claim
25 words
A pharmaceutical composition comprising a thromboxane synthetase enzyme inhibiting amount of a compound according to claim 1 together with a pharmaceutically acceptable diluent or carrier.
Claim 11
Dependent Claim
44 words
A method for treating an animal having a condition characterized by an imbalance of the prostacyclin:thromboxane A 2 ratio which comprises administering to said animal a sufficient amount of a compound according to claim 1 restore the prostacyclin:thromboxane A 2 balance in said animal.
References Cited (Backward Citations)
EP0003560A2
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1986-10-17 | 1987-04-18 | 1987-10-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-10-17 | 1991-04-18 | 1991-10-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-10-17 | 1995-04-18 | 1995-10-18 | $7700.00 | Window Closed / Lapsed |