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    • 35. 再颁专利
    • Olefinic derivatives of amino acids
    • 氨基酸的烯烃衍生物
    • USRE31980E
    • 1985-09-03
    • US458116
    • 1983-01-14
    • Brian W. MetcalfMichel Jung
    • Brian W. MetcalfMichel Jung
    • C07C237/00
    • C07C237/00
    • Novel compounds of the following general formula are useful pharmacologic agents: ##STR1## R is .[.selected from.]. hydrogen.[., alkylcarbonyl wherein the alkyl moiety contains from 1 to 4 carbon atoms, alkoxycarbonyl wherein the alkoxy moiety contains from 1 to 4 carbon atoms and may be straight or branched, and ##STR2## wherein R.sub.10 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl.].; R.sub.2 is .[.selected from.]. hydroxy.[., a straight or branched alkoxy group of from 1 to 8 carbon atoms, a lower alkylamino group wherein the alkyl moiety contains from 1 to 4 carbon atoms, and ##STR3## wherein R.sub.4 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl, and p-hydroxybenzyl.].; R.sub.3 is .[.selected from.]. hydrogen.[., chlorine, bromine, and iodine.].; [A] is .[.selected from.]. ##STR4## .[.and --CH.dbd.CH--.]. wherein R.sub.1 is .[.selected from.]. hydrogen.[., lower alkyl of from 1 to 4 carbon atoms, phenyl and substituted phenyl wherein the substituents on the substituted phenyl may be attached at the ortho, meta or para positions of the phenyl ring and are selected from halogen, lower alkoxy of from 1 to 4 carbon atoms, and lower alkyl of from 1 to 4 carbon atoms; n is an integer of from 1 to 5; and the lactams of said compounds wherein [A] represents ##STR5## R and R.sub.1 represent hydrogen.]. and n is the integer 2 .[.or 3.]. and pharmaceutically acceptable salts and individual optical isomers thereof.
    • 37. 发明授权
    • Derivatives of amines and amino acids
    • 胺和氨基酸的衍生物
    • US4267374A
    • 1981-05-12
    • US52035
    • 1979-06-25
    • Brian W. MetcalfMichel JungCharles Danzin
    • Brian W. MetcalfMichel JungCharles Danzin
    • A61K31/205C07C271/06C07C87/24C07C103/28C07C103/44C07C125/06
    • A61K31/205C07C271/06
    • Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R 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 straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## 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 ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.b can be the same or different; with the provisos that when R.sub.2 is hydrogen, R.sub.1 is --C.tbd.H; when A is ethylidene, R.sub.2 is hydrogen; and when R.sub.a is ##STR6## A is methylene; and pharmaceutically acceptable salts and individual optical isomers thereof.
    • 新颖的式(Ⅰ)化合物,其中A是亚甲基,亚乙基或亚乙基; R1是-C3BCH或-CH = CH2; R2是氢或COR,其中R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分别是氢或1-4个碳原子的直链或支链低级烷基或 其中R 6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; R a是氢,其中烷基部分具有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其中R7被选定 由氢,1至4个碳原子的直链或支链低级烷基,苄基和对羟基苄基; 并且Rb具有与Ra所定义的相同的含义,不同之处在于Rb不是< IMAGE>并且Ra和Rb可以相同或不同; 条件是当R 2是氢时,R 1是-C 3 H H; 当A为亚乙基时,R 2为氢; 而当Ra为亚甲基时, 及其药学上可接受的盐和单独的光学异构体。
    • 38. 发明授权
    • .alpha.-Acetylenic derivatives of .alpha.-amino acids
    • α-氨基酸的α-乙酸衍生物
    • US4260823A
    • 1981-04-07
    • US54167
    • 1979-07-02
    • Patrick J. CasaraMichel JungBrian W. Metcalf
    • Patrick J. CasaraMichel JungBrian W. Metcalf
    • C07C101/20C07C101/26C07C101/28C07C101/72
    • C07C237/12
    • Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein R 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 ##STR2## is hydrogen, a straight or branched lower alkyl group of 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; each R.sub.1 is the same and is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.3 R.sub.4 wherein each of R.sub.3 and R.sub.4 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms and can be the same or different, or ##STR3## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; and pharmaceutically acceptable salts and individual optical isomers thereof.
    • 具有以下一般结构的α-氨基酸的新型炔属衍生物:其中R是氢,其中烷基部分具有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 碳原子是直链或支链的,或者是氢,1-4个碳原子的直链或支链低级烷基,苄基或对羟基苄基; 每个R 1相同,为羟基,具有1至8个碳原子的直链或支链烷氧基,-NR 3 R 4,其中R 3和R 4各自为氢或1至4个碳原子的低级烷基并且可以相同 或不同的,或其中R5是氢,1-4个碳原子的直链或支链低级烷基,苄基或对羟基苄基; 及其药学上可接受的盐和单独的光学异构体。
    • 40. 发明授权
    • .alpha.-Acetylenic derivatives of .alpha.-amino acids
    • α-氨基酸的α-乙酸衍生物
    • US4182891A
    • 1980-01-08
    • US812067
    • 1977-07-01
    • Brian W. MetcalfMichel Jung
    • Brian W. MetcalfMichel Jung
    • A61K31/195A61K31/16A61K31/165A61K31/215A61K31/22A61K31/27A61K38/55A61P3/00A61P17/00A61P25/00A61P33/00A61P35/00A61P37/00C07C67/00C07C229/30C07C233/47C07C237/12C07C237/16C07C237/20C07C237/22C07C239/00C07C279/14C07C313/00C07C323/58C07C323/60C07D211/76C07H19/16C07K1/113C07K5/06C07D211/72C07C101/24C07D223/10
    • C07H19/16C07D211/76
    • Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Z is .beta.-methylthioethyl, .beta.-benzylthioethyl, S-(5'-desoxyadenosin-5' -yl)-S-methylthioethyl, .gamma.-guanidinopropyl, or RHN(CH.sub.2).sub.n --; n is the integer 3 or 4; each R 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 ##STR2## 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 ##STR3## 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 RHN(CH.sub.2).sub.n -- and each R is hydrogen; with the provisos that when Z is .beta.-benzylthioethyl or S-(5'-desoxyadenosin-5' -yl)-S-methyl-thioethyl, R is hydrogen and R.sub.1 is hydroxy, when Z is .gamma.-guanidinopropyl, R is hydrogen and R.sub.1 is hydroxy or a straight or branched lower alkoxy group of from 1 to 8 carbon atoms, and when Z is RHN(CH.sub.2).sub.n -- both R groups are the same; and pharmaceutically acceptable salts and individual optical isomers thereof.
    • 下列通式结构的α-氨基酸的新型炔属衍生物:其中Z是β-甲硫基乙基,β-苄硫基乙基,S-(5'-脱氧腺苷-5'-基)-S-甲硫基乙基,γ-胍基丙基, 或RHN(CH 2)n - n是3或4的整数; 每个R是氢,其中烷基部分具有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的,或其中R2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RHN(CH 2)n - 且每个R为氢时,其内酰胺; 条件是当Z是β-苄基硫代乙基或S-(5'-脱氧腺苷-5'-基)-S-甲基 - 硫代乙基时,R是氢并且R 1是羟基,当Z是γ-胍基丙基时,R是氢和 R 1是羟基或1至8个碳原子的直链或支链低级烷氧基,当Z是RHN(CH2)n-时,两个R基都相同; 及其药学上可接受的盐和单独的光学异构体。