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US4663347A Expired / Lapsed US ⏱️ 0.0 years remaining

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
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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 02:36
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

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