发明公开
EP0144804A3 New 2,5-diaryl tetrahydrofurans and analogs thereof as paf-antagonists
失效
新的2,5-DIARYL四氢呋喃和其类似物作为PAF拮抗剂
- 专利标题： New 2,5-diaryl tetrahydrofurans and analogs thereof as paf-antagonists
- 专利标题（中）： 新的2,5-DIARYL四氢呋喃和其类似物作为PAF拮抗剂
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申请号： EP84113600申请日： 1984-11-12
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公开(公告)号： EP0144804A3公开(公告)日： 1986-01-08
- 发明人: Biftu, Tesfaye , Hwang, San-Bao , Doebber, Thomas W. , Beattie, Thomas R. , Shen, Tsung-Ying
- 申请人： MERCK & CO. INC.
- 专利权人： MERCK & CO. INC.
- 当前专利权人： MERCK & CO. INC.
- 优先权： US551666 19831114
- 主分类号： C07D307/12
- IPC分类号： C07D307/12 ; C07D307/18 ; C07D307/20 ; A61K31/34
摘要：
Compounds of formula:
are disclosed wherein R and R' independently are
(a) hydrogen; (b) haloloweralkyl; (c) halo; (d) CONR 2 R 3 wherein R 2 and R 3 independently represent C 1-6 alkyl and hydrogen; (e) loweralkenyl; (f) -COR 2 (g) -CH 2 OR 2 ; (h) loweralkynyl; (i) -CH 2 -NR 2 R 3 ; (j) -CH 2 SR 2 ; (k) =0; or (I) -OR 2 ; Ar and Ar' are the same or different from each other and are (a) phenyl or substituted phenyl of formula
where R 4 -R 8 independently represent H, RO-, R 2 S-, 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 , -C0 2 R 2 , -NR 2 SO 2 R 3 , COR 2 , N0 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 or substituted pyrryl; (c) furyl or substituted furyl; (d) pyridyl or substituted pyridyl; or (e) thiophene or substituted thiophene. These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby are useful in the treatment of varous diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.
are disclosed wherein R and R' independently are
(a) hydrogen; (b) haloloweralkyl; (c) halo; (d) CONR 2 R 3 wherein R 2 and R 3 independently represent C 1-6 alkyl and hydrogen; (e) loweralkenyl; (f) -COR 2 (g) -CH 2 OR 2 ; (h) loweralkynyl; (i) -CH 2 -NR 2 R 3 ; (j) -CH 2 SR 2 ; (k) =0; or (I) -OR 2 ; Ar and Ar' are the same or different from each other and are (a) phenyl or substituted phenyl of formula
where R 4 -R 8 independently represent H, RO-, R 2 S-, 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 , -C0 2 R 2 , -NR 2 SO 2 R 3 , COR 2 , N0 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 or substituted pyrryl; (c) furyl or substituted furyl; (d) pyridyl or substituted pyridyl; or (e) thiophene or substituted thiophene. These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby are useful in the treatment of varous diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.
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