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31. 发明公开

EP0493642A1 Novel sulfonyl derivatives 失效
标题翻译：新磺酰化
公开(公告)号：EP0493642A1
公开(公告)日：1992-07-08
申请号：EP91100035.4
申请日：1991-01-02
申请人： Takayanagi, Takeo, Dr.
发明人： Takayanagi, Takeo, Dr.
IPC分类号： C07C335/42 , A61K31/63 , C07D203/12 , C07F3/02 , C07F1/08 , C07C311/48 , C07C309/76 , C07C311/53 , C07C309/88 , C07F3/10
CPC分类号： C07D203/08 , C07C309/76 , C07C309/88 , C07C311/49 , C07C311/53 , C07C335/42 , C07D239/69 , C07D473/38 , C07F1/005 , C07F3/003 , C07H19/16
摘要： The present invention relates to novel sulfonyl compounds

wherein R' and R'' are the same or different and are each hydrogen, -COCHR⁴, -COC(R⁴)₃ -SO₂CH₃, -COOCH₂CH₃, -CH₂-CH₂-R⁴, -CONH-CH₂CH₂R⁴, -CONHCH₂COOCH₂CH₃, -CH₂CH₂OCONH₂, and R₄ is Cl or a residue selected from

-NHCOCH₂CH₂OH, -NHCOCH₂CH₃, -NHOH, -NHCH₃, and

R¹ and R² are the same or different and are each selected from

6-mercaptopurinyl, 5-fluorouracily, prednisolyl, salicyl-. hydrazidyl, 1-allyl-2-thiouracilyl, hydroxylamine, isoamidyl, or is an inorganic group consisting of -OH, -SH, -F, -J, -CCl₃, or an organic group consisting of -O-CH₃, -O-CH₂CH₃, -O-CH=CH₂, -O-C₆H₅ or benzhydrol; or an aminoehtyl residue, or an ether group forming oxonium salts consisting of ClCH₂OCH₂Cl, CH₃OCH₂CH₂OCH₃, CH₂ClCH₂OCH₂CH₂Cl, C₄H₉OCH₃, (C₆H₅)₂O,

(CH₂=CHCH₂)₂O, CH₂=CHOCH=CH₂, C₄H₉OC₄H₉, C₆H₅OCH₃, CH₃-O-CHCl₂, ClCH₂-O-C₂H₅, OHCH₂CH₂-O-CH₂CH₂Cl, ClCH₂CHCl-C₂H, and Mt as a metal atom; and wherein the

residue can optionally be changed to a linear, branched or cyclic alkyl having 1 to 6 carbon atoms, halogen or a Hg:N-(C₁-C₆) alkyl group.
The invention further relates to a process for the preparation of the novel sulfonyl compounds and derivatives thereof, as well as for a process for manufacturing a pharmaceutical composition containing the novel sulfonyl compound as an active ingredient. Such novel sulfonyl compound are for example capable in the use for inhibitung tissue growth.
摘要翻译：本发明涉及新的磺酰化合物，其中R'和R“相同或不同，各自为氢，-COCHR 4，-COC（R 4）3 -SO 2 CH 3，-COOCH 2 CH 3， CH 2 -CH 2 -CH 2 R 4，-CONH-CH 2 CH 2 R 4，-CONHCH 2 COOCH 2 CH 3，-CH 2 CH 2 OCONH 2和R 4是Cl或选自下列的残基：CHCO 2 -NHCOCH 2 CH 2 OH，-NHCOCH 2 CH 3，-NHOH，-NHCH 3和CHEM R 1和R 2相同或不同，各自选自6-巯基嘌呤，5-氟尿苷，泼尼松
林，水杨酰基。或者是由-OH，-SH，-F，-J，-CCl 3或由-O-CH 3，-O-（C 1 -C 3）组成的有机基团的无机基团， CH 2 CH 3，-O-CH = CH 2，-O-C 6 H 5或二苯基甲醇; 或C 6 H 9 OCH 3，（C 6 H 5）2 O，CH CH 2（CH 2 = CHCH 2）2 O，CH 2 = CHOCH = CH 2，C 4 H 9 OC 4 H 9，C 6 H 5 OCH 3，CH 3 -O（CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2） -CHCl 2，ClCH 2 -O-C 2 H 5，OHCH 2 CH 2 -O-CH 2 CH 2 Cl，ClCH 2 CHCl-C 2 H和Mt作为金属原子; 并且其中所述残基可任选地改变为具有1至6个碳原子的直链，支链或环状烷基，卤素或Hg：N-（C 1 -C 6）烷基。本发明还涉及制备新的磺酰基化合物及其衍生物的方法，以及制备含有新型磺酰化合物作为活性成分的药物组合物的方法。这样的新型磺酰化合物例如能够用于抑制组织生长。

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