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1. 发明授权

US4560795A .alpha.-Halomethyl derivatives of .alpha.-amino acids 失效
标题翻译： α-氨基酸的α-甲基甲基衍生物
公开(公告)号：US4560795A
公开(公告)日：1985-12-24
申请号：US577116
申请日：1984-02-06
申请人： Philippe Bey , Michel Jung
发明人： Philippe Bey , Michel Jung
IPC分类号： A61K31/16 , A61K31/195 , A61K38/00 , C07D211/74 , C07D211/76 , C07D223/08 , C07H19/02 , C07H19/16 , C07K5/06 , C07C101/24
CPC分类号： C07H19/16 , A61K31/16 , A61K31/195 , C07D211/74 , C07D211/76 , C07D223/08 , C07H19/02 , C07K5/06191 , A61K38/00
摘要： Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is F.sub.2 CH--, F.sub.3 C--, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR2## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR3## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms, or ##STR4## wherein R.sub.3 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and the lactams thereof when Z is R.sub.a HN(CH.sub.2).sub.n -- and each of R.sub.a and R.sub.b is hydrogen; with the provisos that when Z is .gamma.-guanidinopropyl or .beta.-methylthioethyl, Y is FCH.sub.2 --, F.sub.2 CH-- or F.sub.3 C--; when Z is .gamma.-guanidinopropyl, R.sub.1 is hydroxy; and when Z is .beta.-thioethyl, .beta.-benzylthioethyl, S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl or ##STR5## Y and Y.sub.2 are FCH.sub.2 --, F.sub.2 CH--, or F.sub.3 C-- and are the same, each of R.sub.a and R.sub.b is hydrogen and R.sub.1 is hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof.
摘要翻译：以下通式结构的α-氨基酸的新型卤代甲基衍生物：其中Y为F 2 CH - ，F 3 C - ，Cl 2 CH-; Z是β-甲硫基乙基，β-硫乙基，β-苄硫基乙基; S-（5'-脱氧腺苷酸-5'-基）-S-甲硫基乙基，γ-胍基丙基，RaHN（CH2）n-，其中n为整数3或4，或其中Y2为F2CH-或F3C-; R a和R b中的每一个可以相同或不同，并且是氢，烷基部分具有1至4个碳原子并且是直链或支链的烷氧基羰基，其中烷氧基部分具有1至4个碳原子并且是直链或支链或者其中R 2是氢，1至4个碳原子的直链或支链低级烷基，苄基或对羟基苄基; R1是羟基，1至8个碳原子的直链或支链烷氧基，-NR4R5，其中R4和R5各自是氢或1-4个碳原子的低级烷基，或者其中R3是氢， 1至4个碳原子的直链或支链低级烷基，苄基或对羟基苄基; 当Z为RaHN（CH2）n-且其各自的R a和R b为氢时，其内酰胺; 条件是当Z是γ-胍基丙基或β-甲硫基乙基时，Y是FCH 2 - ，F 2 CH-或F 3 C-; 当Z是γ-胍基丙基时，R 1是羟基; 当Z是β-硫代乙基时，β-苄基硫代乙基，S-（5'-脱氧腺苷-5'-基）-S-甲硫基乙基Y和Y 2是FCH 2 - ， - - - R a和R b各自为氢，R 1为羟基; 及其药学上可接受的盐和单独的光学异构体。

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