Indole-2-alkanoic acids and their use as prostaglandin antagonists |
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| 申请号 | EP85304468 | 申请日 | 1985-06-24 | 公开(公告)号 | EP0166591A3 | 公开(公告)日 | 1986-06-25 |
| 申请人 | MERCK FROSST CANADA INC.; | 发明人 | Guindon, Yvan; Gillard, John W.; Yoakim, Christiane; Jones, Thomas R.; Fortin, Rejean; | ||||
| 摘要 | Compounds of the formula I where R 1 is H or alkyl of 1 to 6 carbons or R 1 and R 8 taken together form a group (CH 2 ) v wherein v is 1 to 7; R 2 is where each R 8 is independently H, OH, C 1 to C 4 -O-alkyl or alkyl of 1 to 4 carbons; or an R 1 and an R 8 taken together form a group (CH 2 ) v wherein v is 1 to 7, R 9 is COOR 1 ; CH 2 OH; CHO; tetrazole; NHSO 2 R 10 wherein R 10 is OH, alkyl or alkoxy of 1 to 6 carbons, perhaloalkyl of 1 to 6 carbons, phenyl or phenyl substituted by alkyl or alkoxy groups of 1 to 3 carbons, halogen, hydroxy, COOH, CN, formyl or acyl of 1 to 6 carbons; CONHSO 2 R 10 ; hydroxymethylketone; CN; or CON(R 8 ) 2 ; X is O; S; SO; S0 2 ; NR 11 wherein R 11 is H, alkyl of 1 to 6 carbons, acyl of 1 to 6 carbons, CN; CR 1 R 8 ; or the unit wherein the dotted line represents an optical triple bond and in which the R 1 and R 8 substituents are absent when a triple bond is present; r and q are each independently 0 to 5 and p is 0 or 1 provided that the total of p, q and r is 2 to 6; R 3 is H, alkyl of 1 to 6 carbons; phenyl or phenyl substituted by R 4 ; or C 1 to C 4 alkylphenyl or C 1 to C 4 alkylphenyl in which the phenyl is substituted by R 4 ; R 4 , R 5 , R 6 and R 7 are each independently selected from: (1) hydrogen; (2) alkyl having 1 to 6 carbon atoms; (3) alkenyl having 2 to 6 carbon atoms; (4) -(CH 2 ) n M wherein n is 0 to 3 and M is a) OR 12 ; b) halogen; c) CF 3 ; d) SR 12 ; e) phenyl or substituted phenyl wherein substituted phenyl is as defined below in the definition of R 12 ; f ) COOR 13 ; g) h) tetrazole; i) wherein R 15 is C 1 to C 6 alkyl, benzyl or phenyl; j) -NR 13 R 13 ; k) -NHSO 2 R 16 wherein R 16 is C 1 to C 6 alkyl, phenyl, or CF 3 ; I) m) -SOR 12 ; n) -CON 13 R 13 ; o) -SO 2 NR 13 R 13 ; p) -SO 2 R 12 ; q) N0 2 ; r) s) t) u) CN; each R 12 independently is H; C 1 to C 6 alkyl; benzyl; phenyl or substituted phenyl wherein the substituents are C 1 to C 3 alkyl, halogen, CN, CF 3 , COOR 13 , CH 2 COOR 13 , C 1 to C 3 alkoxy, or C 1 to C 4 perfluoroalkyl; each R 13 is independently H, phenyl or C 1 to C 6 alkyl; and, each R 14 independently is H, (CH 2 ) n COOR 13 wherein n is 0 to 4, C 1 to C 6 alkyl, CF 3 , phenyl, or substituted phenyl wherein substituted phenyl is as defined above in the definition of R 12 ; and their pharmaceutically acceptable salts are useful as prostaglandin antagonists and are made into pharmaceutical compositions. Certain of the compounds are novel. |
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