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    Substituted tyrosyl alanine dipeptide amides
    5.
    发明授权
    Substituted tyrosyl alanine dipeptide amides 失效
    取代的酪氨酰丙氨酸二肽酰胺

    公开(公告)号：US4727189A

    公开(公告)日：1988-02-23

    申请号：US851834

    申请日：1986-04-14

    申请人： Donald W. Hansen, Jr. ,  Robert H. Mazur ,  Daniel R. Pilipauskas

    发明人： Donald W. Hansen, Jr. ,  Robert H. Mazur ,  Daniel R. Pilipauskas

    IPC分类号： A61K38/00 ,  C07K5/065 ,  C07C103/20 ,  C07C68/00

    CPC分类号： C07K5/06078 ,  A61K38/00

    摘要： The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sub.1 represents straight or branched lower alkyl having 1 to 4 carbons;R.sub.2 represents hydrogen, hydroxy, --OCO.sub.2 R.sub.1 substituent or lower alkyl having 1 to 4 carbons;R.sub.3 represents a hydrogen or lower alkyl having 1 to 6 carbons;R.sub.4 and R.sub.5 may be the same or different and represent hydrogen or lower alkyl having 1 to 6 carbons;n is 1 to 6;X represents a hydrogen, hydroxy or OCO.sub.2 R.sub.1 substituent;A represents a cyclohexyl, phenyl or phenyl substituted with one or more lower alkyls containing 1 to 6 carbons, one or more amino, hydroxy, halogen, nitro or lower alkoxy substituent having 1 to 6 carbons;V represents the asymmetric carbon that may be racemic or have the D or L configuration;W represents the asymmetric carbon when R.sub.4 and R.sub.5 are not the same that may optionally be racemic or have the D or L configuration.These compounds are useful as analgesic and/or antihypertensive agents.

    摘要翻译： 本发明涉及下式的新型取代的酪氨酰丙氨酸二肽酰胺及其药学上可接受的酸加成盐，其中R1代表具有1-4个碳原子的直链或支链低级烷基; R2代表氢，羟基，-OCO2R1取代基或具有1至4个碳原子的低级烷基; R3表示氢或具有1至6个碳的低级烷基; R 4和R 5可以相同或不同，表示氢或具有1至6个碳的低级烷基; n为1至6; X表示氢，羟基或OCO 2 R 1取代基; A表示被一个或多个含有1至6个碳的低级烷基，一个或多个具有1-6个碳原子的氨基，羟基，卤素，硝基或低级烷氧基取代基取代的苯基或苯基; V表示可以是外消旋或具有D或L构型的不对称碳; 当R4和R5不相同时，W表示不对称碳，其可任选地是外消旋的或具有D或L构型。 这些化合物可用作止痛剂和/或抗高血压药物。

    Substituted tyrosyl alanine dipeptide amides
    7.
    发明授权
    Substituted tyrosyl alanine dipeptide amides 失效

    公开(公告)号：US4599325A

    公开(公告)日：1986-07-08

    申请号：US692611

    申请日：1985-01-22

    申请人： Donald W. Hansen, Jr. ,  Robert H. Mazur ,  Daniel R. Pilipauskas

    发明人： Donald W. Hansen, Jr. ,  Robert H. Mazur ,  Daniel R. Pilipauskas

    IPC分类号： A61K38/00 ,  C07K5/065 ,  A61K37/24 ,  C07K7/12

    CPC分类号： C07K5/06078 ,  A61K38/00 ,  Y10S514/809

    摘要： The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sub.1 represents straight or branched lower alkyl having 1 to 4 carbons;R.sub.2 represents hydrogen, hydroxy, --OCO.sub.2 R.sub.1 substituent or lower alkyl having 1 to 4 carbons;R.sub.3 represents a hydrogen or lower alkyl having 1 to 6 carbons;R.sub.4 and R.sub.5 may be the same or different and represent hydrogen or lower alkyl having 1 to 6 carbons;n is 1 to 6;X represents a hydrogen, hydroxy or OCO.sub.2 R.sub.1 substituent;A represents a cyclohexyl, phenyl or phenyl substituted with one or more lower alkyls containing 1 to 6 carbons, one or more amino, hydroxy, halogen, nitro or lower alkoxy substituent having 1 to 6 carbons;V represents the asymmetric carbon that may be racemic or have the D or L configuration;W represents the asymmetric carbon when R.sub.4 and R.sub.5 are not the same that may optionally be racemic or have the D or L configuration. These compounds are useful as analgesic and/or antihypertensive agents.

    N-Adamantane-substituted tetrapeptide amides
    8.
    发明授权
    N-Adamantane-substituted tetrapeptide amides 失效
    N-金刚烷取代的四肽酰胺

    公开(公告)号：US4273704A

    公开(公告)日：1981-06-16

    申请号：US099765

    申请日：1979-12-03

    申请人： Robert H. Mazur

    发明人： Robert H. Mazur

    IPC分类号： C07K5/10 ,  A61K38/00 ,  A61P25/04 ,  C07K5/02 ,  C07K5/06 ,  C07K5/103 ,  C07K5/107 ,  C07K7/02 ,  C07K14/575 ,  C07K14/655 ,  C07C103/52

    CPC分类号： C07K5/06026 ,  C07K5/0205 ,  C07K5/1005 ,  C07K5/1016 ,  C07K7/02 ,  A61K38/00

    摘要： N-Adamantane-substituted tetrapeptide amides and the pharmacologically acceptable salts thereof are disclosed herein. These compounds are analogs of enkephalin wherein the methionine or leucine of position 5 has been substituted by an adamantyl amide and the glycine of position 2 has been substituted by various amino acid residues. Optionally the tyrosine of position 1 and the phenylalanine of position 4 may be substituted by various amino acid residues. These compounds exhibit agonist activity at opiate receptor sites and are useful as analgesics.

    摘要翻译： 本文公开了N-金刚烷取代的四肽酰胺及其药理学上可接受的盐。 这些化合物是脑啡肽的类似物，其中位置5的甲硫氨酸或亮氨酸已经被金刚烷基酰胺取代，并且位置2的甘氨酸被各种氨基酸残基取代。 任选地，位置1的酪氨酸和位置4的苯丙氨酸可以被各种氨基酸残基取代。 这些化合物在阿片受体位点表现出激动剂活性，可用作镇痛药。

    Cyclohexyl and phenyl substituted enkephalins
    10.
    发明授权
    Cyclohexyl and phenyl substituted enkephalins 失效
    环己基和苯基取代的脑啡肽

    公开(公告)号：US4407746A

    公开(公告)日：1983-10-04

    申请号：US330614

    申请日：1981-12-14

    申请人： Robert H. Mazur ,  David A. Tyner ,  Eleanor A. Hallinan

    发明人： Robert H. Mazur ,  David A. Tyner ,  Eleanor A. Hallinan

    IPC分类号： C07K14/655 ,  A61K38/00 ,  A61K38/22 ,  A61P25/04 ,  C07K5/10 ,  C07K5/107 ,  C07K14/575 ,  C07K14/70 ,  C07C103/52 ,  A61K37/00

    CPC分类号： C07K5/1016

    摘要： The invention discloses cyclohexyl and phenyl substituted enkephalin derivatives of the formula: ##STR1## Where R.sub.1, R.sub.2, R.sub.4, and R.sub.8 is hydrogen or alkyl of R.sub.3 is alkylthioalkyl or alkylsulfinylalkyl, X is: ##STR2## R.sub.5 is cyclohexylmethyl, phenylmethyl, optionally substituted by --NO.sub.2, R.sub.6 is cyclohexyl or phenyl optionally substituted by R.sub.7 and R.sub.7 is hydrogen, an alkyl ester of carboxylic acid or hydroxyalkyl and the pharmaceutically acceptable salts, which are useful as analgesic agents.

    摘要翻译： 本发明公开了下式的环己基和苯基取代的脑啡肽衍生物：其中R1，R2，R4和R8是氢或R3的烷基是烷硫基烷基或烷基亚磺酰基烷基，X是：环己基甲基，苯甲基， 通过-NO 2，R 6是任选被R 7取代的环己基或苯基，R 7是氢，羧酸或羟烷基的烷基酯和药学上可接受的盐，其可用作止痛剂。