| 摘要 |
1466295 Derivatives of mercaptomethylpyridine MERCK & CO Inc 12 June 1974 [15 June 1973 16 May 1974] 26178/74 Heading C2C The invention comprises (with certain exceptions) compounds of formula (= Q-S-R 32 ) and their pharmaceutically acceptable salts, wherein m is 0 or 1; R is C 1-5 alkyl; each R 31 is H, -COO (alkyl or alkenyl, #C 5 ) or -CONH 2 , or both R 31 groups form together O=C< or (C 1-3 alkyl) 2 C<; and R 32 is H, -COO (alkyl or alkenyl, #C 5 ), -S-Q or (m=O)-CO-S-Q. In examples, these compounds are prepared by standard methods for (a) the formation of thiol, disulphide, carbonate, mono- and di-thiocarbonate groups, or (b) the scission of a cyclic ketal. Intermediates for which preparative details are given are 5-X-2,2,8-trimethyl-4H-m-dioxino- [4,5-c] pyridine, where X is CH 2 Cl or CH 2 SC(S)OEt; and 5-Y-3 - carbamyloxy - 4 - carbamyloxymethyl-2-methylpyridine, where Y is CH 2 Cl or CH 2 S 2 O 3 H (presumably as the Na salt). Therapeutic compositions having anti-rheumatoid arthritis activity comprise compounds (A), and may be administered orally, parenterally, rectally, topically, or by inhalation spray.
|
