Patent US4595693A successfully refreshed from Google Patents.
US4595693A
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Method of use of 2,5-diaryl tetrahydrofurans and analogs thereof as PAF-antagonists
Assignee: Merck and Co Inc
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Filing: 1984-06-04
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Granted: 1986-06-17
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Expires: 2004-06-04
Abstract
Abstract Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared. These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.
Inventors
- 👤 Tesfaye Biftu
- 👤 Thomas W. Doebber
- 👤 San-Bao Hwang
- 👤 Thomas R. Beattie
- 👤 Tsung-Ying Shen
- 👤 Robert Stevenson
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 23:33
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/335; A61K31/34; C; C07; C07D; C07D307/00; C07D307/02; C07D307/04; C07D307/10; C07D307/12
Claims Analysis
Total Claims: 4
Claim 1
Independent Claim
241 words
A method for the treatment of a disease or a disorder mediated by PAF comprising administering to a mammalian species in need of the treatment a therapeutically effective amount of a compound of formula: ##STR8## wherein R is: (a) hydrogen; (b) lower alkyl of 1-6 carbon atoms; (c) haloloweralkyl; (d) halo; (e) COOH; (f) CONR 2 R 3 wherein R 2 and R 3 independently represent C 1-6 alkyl and hydrogen; (g) COOR° wherein R° is C 1-6 alkyl; (h) loweralkenyl; (i) --COR 2 ; (j) --CH 2 OR 2 ; (k) loweralkynyl; (l) --CH 2 NR 2 R 3 ; (m) --CH 2 SR 2 ; (n) ═O; or (o) --OR 2 ; R 1 is lower alkyl; --COOH; or --COOR°; Ar and Ar 1 are the same or different from each other and are (a) phenyl of formula ##STR9## where R 4 -R 8 independently represent H, RO--, R 2 S, R 2 SO, R 2 SO 2 --, CF 3 O--, CF 3 S--, R 2 R 3 N--, --OCH 2 CO 2 R 2 , --SO 2 NR 2 R 3 , --CO 2 R 2 , --NR 2 SO 2 R 3 , COR 2 , NO 2 , or CN or R 4 -R 5 , R 5 -R 6 , R 6 -R 7 and R 7 -R 8 are joined together forming a bridge; (b) pyrryl; (c) furyl; (d) pyridyl; or (e) thiophene.
Claim 2
Independent Claim
241 words
A method for the treatment of a disease or a disorder mediated by PAF comprising administering to a mammalian species in need of the treatment a therapeutically effective amount of a compound of formula: ##STR8## wherein R is: (a) hydrogen; (b) lower alkyl of 1-6 carbon atoms; (c) haloloweralkyl; (d) halo; (e) COOH; (f) CONR 2 R 3 wherein R 2 and R 3 independently represent C 1-6 alkyl and hydrogen; (g) COOR° wherein R° is C 1-6 alkyl; (h) loweralkenyl; (i) --COR 2 ; (j) --CH 2 OR 2 ; (k) loweralkynyl; (l) --CH 2 NR 2 R 3 ; (m) --CH 2 SR 2 ; (n) ═O; or (o) --OR 2 ; R 1 is lower alkyl; --COOH; or --COOR°; Ar and Ar 1 are the same or different from each other and are (a) phenyl of formula ##STR9## where R 4 -R 8 independently represent H, RO--, R 2 S, R 2 SO, R 2 SO 2 --, CF 3 O--, CF 3 S--, R 2 R 3 N--, --OCH 2 CO 2 R 2 , --SO 2 NR 2 R 3 , --CO 2 R 2 , --NR 2 SO 2 R 3 , COR 2 , NO 2 , or CN or R 4 -R 5 , R 5 -R 6 , R 6 -R 7 and R 7 -R 8 are joined together forming a bridge; (b) pyrryl; (c) furyl; (d) pyridyl; or (e) thiophene.
Claim 3
Dependent Claim
18 words
The method of claim 1 wherein the compound is a stereoisomer of formula (4), (1) or (3): ##STR10##
Claim 4
Dependent Claim
11 words
The method of claim 1 wherein the active compound is cis-3,4-dimethyl-2,5-bis(3,4-dimethoxyphenyl)tetrahydrofuran.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1989-06-16 | 1989-12-16 | 1990-06-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-06-16 | 1993-12-16 | 1994-06-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-06-16 | 1997-12-16 | 1998-06-17 | $7700.00 | Window Closed / Lapsed |