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    .alpha.-Halomethyl derivatives of .alpha.-amino acids
    16.
    发明授权
    .alpha.-Halomethyl derivatives of .alpha.-amino acids 失效
    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。

    Novel enzyme inhibitors
    17.
    发明授权
    Novel enzyme inhibitors 失效
    新型酶抑制剂

    公开(公告)号：US4277395A

    公开(公告)日：1981-07-07

    申请号：US160111

    申请日：1980-06-16

    申请人： Philippe Bey ,  Brian W. Metcalf ,  Jeffrey S. Wiseman

    发明人： Philippe Bey ,  Brian W. Metcalf ,  Jeffrey S. Wiseman

    IPC分类号： C07D339/08 ,  C07K5/08 ,  C07C103/52 ,  C07D207/24

    CPC分类号： C07D339/08 ,  C07K5/0827

    摘要： Compounds of the following general formula are irreversible inhibitors of pancreatic elastase: ##STR1## wherein M is hydroxy, lower alkoxy, benzyloxy or --NY.sub.1 Y.sub.2 wherein each of R.sub.4 and R.sub.5 is hydrogen or lower alkyl; R is CF.sub.3, CHF.sub.2 or CH.sub.2 F; R.sub.1 is straight or branched lower alkyl; R.sub.2 is defined the same as R.sub.1 or is benzyl; R.sub.30 is CHO, carbobenzoxy, tert-butoxycarbonyl, benzoyl or lower alkanoyl; X is pro, ala or leu and Y and Z together form a single bond; or Y-X is ala-pro, ala-ala or ala-leu and Z forms a single bond; and Z-Y-X is ala-ala-pro, ala-ala-ala or pro-ala-leu.

    摘要翻译： 下列通式的化合物是胰弹性蛋白酶的不可逆抑制剂：其中M是羟基，低级烷氧基，苄氧基或-NY1Y2，其中R4和R5各自为氢或低级烷基; R是CF 3，CHF 2或CH 2 F; R1是直链或支链低级烷基; R2定义与R1相同或为苄基; R30为CHO，苄氧羰基，叔丁氧基羰基，苯甲酰基或低级烷酰基; X是pro，ala或leu，Y和Z一起形成单键; 或Y-X是ala-pro，ala-ala或ala-leu，Z形成单键; 和Z-Y-X是ala-ala-pro，ala-ala-ala或pro-ala-leu。

    Alpha-halomethyl derivatives of histamine and related compounds
    18.
    发明授权
    Alpha-halomethyl derivatives of histamine and related compounds 失效
    组胺和相关化合物的α-卤代甲基衍生物

    公开(公告)号：US4221914A

    公开(公告)日：1980-09-09

    申请号：US16640

    申请日：1979-03-01

    申请人： Philippe Bey ,  Michel Jung

    发明人： Philippe Bey ,  Michel Jung

    IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D233/66

    CPC分类号： C07D233/64

    摘要： Novel halomethyl derivatives of amines of the following general structure ##STR1## wherein Y is FCH.sub.2 --, F.sub.2 CH-- or F.sub.3 C--; 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.3 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; each of R.sub.1 and R.sub.2 is hydrogen, or a straight or branched lower alkyl group of from 1 to 4 carbon atoms and may be the same or different or R.sub.1 is hydrogen and R.sub.2 is fluorine; and pharmaceutically acceptable salts and individual optical isomers thereof.

    摘要翻译： 其中Y是FCH2-，F2CH-或F3C-的以下通式结构的胺的新型卤代甲基衍生物; 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或其中R3是氢，直链 或具有1至4个碳原子的支链低级烷基，苄基或对羟基苄基; R 1和R 2各自为氢或1至4个碳原子的直链或支链低级烷基，可以相同或不同，或者R 1为氢，R 2为氟; 及其药学上可接受的盐和单独的光学异构体。

    Peptidase inhibitors
    19.
    发明授权
    Peptidase inhibitors 失效
    肽酶抑制剂

    公开(公告)号：US5736520A

    公开(公告)日：1998-04-07

    申请号：US434959

    申请日：1995-05-04

    申请人： Philippe Bey ,  Michael R. Angelastro ,  Shujaath Mehdi

    发明人： Philippe Bey ,  Michael R. Angelastro ,  Shujaath Mehdi

    IPC分类号： A61K38/00 ,  C07K5/06 ,  A61K38/05

    CPC分类号： C07K5/06052 ,  C07K5/06026 ,  A61K38/00

    摘要： This invention relates to analogs of peptidase substrates in which the nitrogen atom of the scissile amide group of the substrate peptide has been replaced by H, an aldehyde, a substituted carbonyl or a substituted malonyl moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

    摘要翻译： 本发明涉及肽酶底物的类似物，其中底物肽的剪切酰胺基团的氮原子被H，醛，取代的羰基或取代的丙二酰部分替代。 肽酶底物的这些类似物为各种蛋白酶提供特异性酶抑制剂，其抑制将在各种疾病状态下具有有用的生理后果。