Patent US4663347A successfully refreshed from Google Patents.
US4663347A
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Benzofuran 2-carboxylic acid esters useful as inhibitors of leukotriene biosynthesis
Assignee: Merck Frosst Canada and Co
•
Filing: 1985-04-19
•
Granted: 1987-05-05
•
Expires: 2005-04-19
Abstract
Abstract Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
Inventors
- 👤 Joseph G. Atkinson
- 👤 Yvan Guindon
- 👤 Cheuk K. Lau
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 03:32
CPC Classifications
C; C07; C07D; C07D307/00; C07D307/77; C07D307/78; C07D307/82; C07D307/84; C07D307/85; A; A61; A61P; A61P1/00; A61P11/00; A61P29/00; A61P37/00; A61P37/08; A61P43/00; C07C; C07C2603/00; C07C2603/02; C07C2603/04; C07C2603/06; C07C2603/10; C07C2603/12; C07C2603/16
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
166 words
A compound of Formula I: ##STR149## wherein the compound is selected from the following group: ______________________________________
Com-
pound R.sub.1
R.sub.2 R.sub.3 R.sub.4 R
______________________________________
172 CH.sub.3
OC(CH.sub.3).sub.3
4-OH H H
216 Me OEt 4-OH 5-CH.sub.2 OH
H
217 Me OEt 5-OAc H H
218 Me OEt 4-OH 5-CH.sub.2 OEt
H
226 Me OEt
##STR150##
H H
227 Me
##STR151##
4-OAc H H
230 Me OMe
##STR152##
5-CH.sub.2 CHCH.sub.2
H
231 Me OEt
##STR153##
5-Pr H
241 Me OEt 5-OH 4-CH.sub.2 CHCH.sub.2
H
242 Me OEt 4-OH 5-CH.sub.2 CHCH.sub.2
H
245 Ph OEt 6-OH H H
246 Me OEt 5-NHAc H H
250 Pr OEt 4-OH H H
252 Me OEt 4-OH 5-Pr H
253 Ph OEt 4-OH H H
254 Ph OEt 4-OH
##STR154##
H
259 Me
##STR155##
4-OH H H
261 CH.sub.3
OH 4-OH 5-Pr H
263 Me
##STR156##
4-OH H H
288 CH.sub.3
OEt
##STR157##
H H
366 CH.sub.3
OEt 4-OH 5-CH.sub.2 CH.sub.2 CH.sub.3
7-F
367 CH.sub.3
OEt 4-OH 5-CH.sub.2 CH.sub.2 CH.sub.3
7-Cl
______________________________________
Claim 2
Dependent Claim
166 words
A compound of Formula I: ##STR149## wherein the compound is selected from the following group: ______________________________________
Com-
pound R.sub.1
R.sub.2 R.sub.3 R.sub.4 R
______________________________________
172 CH.sub.3
OC(CH.sub.3).sub.3
4-OH H H
216 Me OEt 4-OH 5-CH.sub.2 OH
H
217 Me OEt 5-OAc H H
218 Me OEt 4-OH 5-CH.sub.2 OEt
H
226 Me OEt
##STR150##
H H
227 Me
##STR151##
4-OAc H H
230 Me OMe
##STR152##
5-CH.sub.2 CHCH.sub.2
H
231 Me OEt
##STR153##
5-Pr H
241 Me OEt 5-OH 4-CH.sub.2 CHCH.sub.2
H
242 Me OEt 4-OH 5-CH.sub.2 CHCH.sub.2
H
245 Ph OEt 6-OH H H
246 Me OEt 5-NHAc H H
250 Pr OEt 4-OH H H
252 Me OEt 4-OH 5-Pr H
253 Ph OEt 4-OH H H
254 Ph OEt 4-OH
##STR154##
H
259 Me
##STR155##
4-OH H H
261 CH.sub.3
OH 4-OH 5-Pr H
263 Me
##STR156##
4-OH H H
288 CH.sub.3
OEt
##STR157##
H H
366 CH.sub.3
OEt 4-OH 5-CH.sub.2 CH.sub.2 CH.sub.3
7-F
367 CH.sub.3
OEt 4-OH 5-CH.sub.2 CH.sub.2 CH.sub.3
7-Cl
______________________________________
Claim 3
Dependent Claim
13 words
A compound of claim 1 which is: 172, 231, 288, 366, or 367.
Claim 4
Dependent Claim
12 words
A compound of claim 1 which is: 231, 288, 366, or 367.
Claim 5
Dependent Claim
25 words
A method of inhibiting mammalian leukotriene biosynthesis or action which comprises administering to a mammal a pharmaceutically effective amount of a compound of claim 1.
Claim 6
Dependent Claim
25 words
A method of inhibiting human leukotriene biosynthesis or action which comprises administering to a human a pharmaceutically effective amount of a compound of claim 1.
Claim 7
Dependent Claim
33 words
A method of treating pulmonary conditions, inflammation, cardiovascular conditions, or skin conditions which comprises administering to a human in need of such treatment a pharmaceutically effective amount of a compound of claim 1.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-05-04 | 1990-11-03 | 1991-05-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-05-04 | 1994-11-03 | 1995-05-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-05-04 | 1998-11-03 | 1999-05-05 | $7700.00 | Window Closed / Lapsed |