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    3-thiophene-substituted tyrosyl dipeptide amides
    61.
    发明授权
    3-thiophene-substituted tyrosyl dipeptide amides 失效
    3-噻吩取代的酪氨酰二肽酰胺

    公开(公告)号：US4758675A

    公开(公告)日：1988-07-19

    申请号：US14339

    申请日：1987-02-13

    Applicant: Donald W. Hansen, Jr. ,  Barnett S. Pitzele ,  Robert W. Hamilton ,  Michael Clare

    Inventor： Donald W. Hansen, Jr. ,  Barnett S. Pitzele ,  Robert W. Hamilton ,  Michael Clare

    IPC: A61K38/00 ,  C07K5/065 ,  C07D333/22

    CPC classification number: C07K5/06078 ,  A61K38/00

    Abstract: This invention relates to novel 3-thiophene-substituted tryosyl dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable addition salts thereof, wherein R.sup.1 is --OH, benzyloxy, or --OCH.sub.3 ; wherein R.sub.2 and R.sub.3 may be the same or different and represent lower alkyl of 1-6 carbon atoms; wherein R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl of 1-6 carbon atoms; wherein "v" represents an asymmetric carbon atom that may be racemic or that may have the D or L configuration; and wherein "w" represents an asymmetric carbon atom that has the D configuration. These compounds are useful as analgesic agents.

    Abstract translation: 本发明涉及下式的新型3-噻吩取代的甜蛋白二肽酰胺及其药学上可接受的加成盐，其中R1是-OH，苄氧基或-OCH3; 其中R2和R3可以相同或不同，代表1-6个碳原子的低级烷基; 其中R4，R5，R6，R7，R8和R9可以相同或不同，代表氢或1-6个碳原子的低级烷基; 其中“v”表示可以是外消旋的或可具有D或L构型的不对称碳原子; 并且其中“w”表示具有D构型的不对称碳原子。 这些化合物可用作止痛剂。

    Sulfide, sulfinyl and sulfone dipeptide amides
    62.
    发明授权
    Sulfide, sulfinyl and sulfone dipeptide amides 失效
    硫化物，亚磺酰基和砜二肽酰胺

    公开(公告)号：US4757153A

    公开(公告)日：1988-07-12

    申请号：US882796

    申请日：1986-07-14

    Applicant: Donald W. Hansen, Jr. ,  Daniel R. Pilipauskas ,  Michael Clare

    Inventor： Donald W. Hansen, Jr. ,  Daniel R. Pilipauskas ,  Michael Clare

    IPC: A61K38/00 ,  C07D333/20 ,  C07D333/38 ,  C07D333/48 ,  C07D335/02 ,  C07K5/065 ,  C07D337/00 ,  C07C103/00 ,  C07D331/04 ,  C07D333/36 ,  C07K7/12

    CPC classification number: C07D333/48 ,  C07D333/20 ,  C07D333/38 ,  C07D335/02 ,  C07K5/06078 ,  A61K38/00

    Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, lower alkoxy, --O(CH.sub.2).sub.n phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, and R.sup.9 may be the same or different and represent hydrogen, lower alkyl, cycloalkyl having 3 to 8 carbons, unsaturated lower alkyl, or --(CH.sub.2).sub.m cycloalkyl with the cycloalkyl having 3 to 8 carbons and m is 1 to 4; R.sup.10 is hydrogen or --(CH.sub.2).sub.p phenyl or with the phenyl optionally substituted with --NH.sub.2, --OH, halogen, --NO.sub.2, or lower alkyl or --(CH.sub.2).sub.p thienyl wherein p is 1 to 4; one of R.sup.7 or R.sup.8 is --(CH.sub.2).sub.f --S(O).sub.z --(CH.sub.2).sub.q --CH.sub.3 where f is 1 to 3 and q is 0 to 3, z is 0, 1 or 2 and the other is hydrogen or lower alkyl, or R.sup.7 and R.sup.8 together with carbon w is ##STR2## where x and y are independently 1 to 3 and z is 0, or 2. V represents an asymmetric carbon that may be recemic or have the D or L configuration; W represents an asymmetric carbon when R.sup.7 and R.sup.8 are not the same that may be recemic or have the D or L configuration.The compounds of this invention are useful as analgesic and/or antihypertensive agents.

    Abstract translation: 本发明涉及下式的新型取代的酪氨酸丙氨酸二肽酰胺及其药学上可接受的酸加成盐，其中R1是氢，低级烷基，羟基，低级烷氧基，-O（CH2）n-苯基，其中苯基任选被 卤素，-NO 2，-CN，-NH 2或低级烷基，其中n为1至4; R2和R3表示低级烷基，卤素或低级烷氧基，或R2或R3中的任一个为氢，另一个为低级烷基，低级烷氧基或卤素; R 4，R 5，R 6和R 9可以相同或不同，表示氢，低级烷基，具有3-8个碳原子的环烷基，不饱和低级烷基或 - （CH 2）m环烷基，环烷基具有3至8个碳原子，m是1 到4; R 10是氢或 - （CH 2）p苯基或与-NH 2，-OH，卤素，-NO 2或低级烷基或 - （CH 2）p噻吩基取代的苯基，其中p为1至4; R 7或R 8中的一个为 - （CH 2）f S（O）z - （CH 2）q -CH 3，其中f为1至3，q为0至3，z为0,1或2，而另一个为氢或低级烷基 或者R 7和R 8与碳w一起为，其中x和y独立地为1〜3，z为0或2.V表示可以是接受或具有D或L构型的不对称碳; 当R7和R8不相同时，W表示不对称碳，其可以是可接受的或具有D或L构型。 本发明的化合物可用作镇痛药和/或抗高血压药。

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