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    Substituted dipeptide amides #3
    78.
    发明授权
    Substituted dipeptide amides #3 失效
    取代的二肽酰胺＃3

    公开(公告)号：US4880829A

    公开(公告)日：1989-11-14

    申请号：US146006

    申请日：1988-01-20

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

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

    IPC: A61K38/00 ,  C07K5/065

    CPC classification number: 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, --OCO.sub.2 lower alkyl, 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, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.10 is selected from the group consisting of--(ALK)Xwhere ALK represents alkylene, thioalkylene, oxyalkylene, having 1 to 5 carbon atoms; alkenylene and alkynylene having 2 to 4 carbon atoms; and X represents pyridyl, pyrimidinyl, 9H-fluoren-9-yl, diphenylmethyl, thienyl, carboxy, lower alkoxy carbonyl, substituted phenyl wherein the phenyl substituent is amino, hydroxy, halogen, nitro, methylenedioxy, lower alkyl, carboxy, lower alkoxycarbonyl, lower alkoxy, carboxamide, diloweralkylamino or X represents phenyl when ALK is not alkylene; or R.sup.10 is ##STR2## where p and q are independently 1 to 4; or R.sup.9 and R.sup.10 together with N is ##STR3## where r and t are independently 1 to 4;v represents an asymmetric carbon that may be racemic 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 racemic or have the D or L configuration.These compounds are useful as analgesic and/or antihypertensive compounds.

    Abstract translation: 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R 1是氢，低级烷基，羟基，-OCO 2低级烷基，低级烷氧基，-O（CH 2）n - 苯基，其中任选被卤素取代的苯基，-NO 2，-CN，-NH 2或其中n为1至4的低级烷基; 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，R 7，R 8和R 9可以相同或不同，表示氢或低级烷基; R 10选自 - （ALK）X，其中ALK表示亚烷基，硫代亚烷基，氧化烯，具有1至5个碳原子; 具有2至4个碳原子的亚烯基和亚炔基; 羟基，卤素，硝基，亚甲二氧基，低级烷基，羧基，低级烷氧基羰基，低级烷氧基羰基，低级烷氧基羰基， 低级烷氧基，甲酰胺，二低级烷基氨基或X代表苯基，当ALK不是亚烷基时; 或R10为，其中p和q独立地为1至4; 或R 9和R 10与N一起为，其中r和t独立地为1至4; v表示可以是外消旋或具有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，可以是外消旋的或具有D或L构型。 这些化合物可用作镇痛和/或抗高血压化合物。

    Substituted tyrosyl methionyl dipeptide amides
    79.
    发明授权
    Substituted tyrosyl methionyl dipeptide amides 失效
    取代的酪氨酰甲硫氨酰二肽酰胺

    公开(公告)号：US4767744A

    公开(公告)日：1988-08-30

    申请号：US14329

    申请日：1987-02-13

    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 ,  A61K37/02 ,  C07C103/20 ,  C07D207/00 ,  C07K5/06

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

    Abstract: This invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable addition salts thereof, wherein R.sup.1 is --OH, --OCH.sub.3 or lower alkoxy of 1-6 carbon atoms; wherein R.sup.2 and R.sup.3 may be the same or different and represent straight or branched chain lower alkyl of 1-6 carbon atoms; wherein R.sup.4, R.sup.5 R.sup.9 may be the same or different and represent hydrogen or straight or branched chain lower alkyl having 1-6 carbon atoms; wherein R.sup.6 represents hydrogen, or straight or branched chain lower alkyl of 1-6 carbon atoms, or R.sup.6 may act together with N.sup.6, C.sup.w and either R.sup.7 R.sup.8 to form a cycloamine of the formula: ##STR2## such that between R.sup.7 and R.sup.8, when one acts to form said cycloamine, the other is hydrogen, or straight or branched chain lower alkyl of 1-6 carbon atoms; wherein when neither R.sup.7 nor R.sup.8 is acting to form said cycloamine, R.sup.7 R.sup.8 act together with C.sup.w to form a cycloalkyl of the formula: ##STR3## where n=3, 4, 5; wherein C.sup.w represents an asymmetric carbon atom when R.sup.7 and R.sup.8 are not the same and may be racemic or have the D or L configuration; and wherein C.sup.v represents an asymmetric carbon atom that may be racemic or that may hve the D or L configuration.These compounds are useful because they possess analgesic activity in mammals.

    Abstract translation: 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加成盐，其中R1是-OH，-OCH3或1-6个碳原子的低级烷氧基; 其中R2和R3可以相同或不同，表示1-6个碳原子的直链或支链的低级烷基; 其中R4，R5 R9可以相同或不同，表示氢或具有1-6个碳原子的直链或支链低级烷基; 其中R6表示氢或1-6个碳原子的直链或支链低级烷基，或R6可以与N6，Cw和R7R8一起起作用以形成下式的环胺：使得在R 7和R 8之间， 当一个作用形成所述环胺时，另一个是氢或1-6个碳原子的直链或支链的低级烷基; 其中当R7和R8都不起作用形成所述环胺时，R 7 R8与Cw一起作用以形成下式的环烷基：其中n = 3,4,5; 其中当R 7和R 8不相同时，Cw表示不对称碳原子，可以是外消旋的或具有D或L构型; 并且其中Cv表示可以是外消旋的或可以是D或L构型的不对称碳原子。 这些化合物是有用的，因为它们在哺乳动物中具有止痛活性。

    N-terminally substituted dipeptide amides
    80.
    发明授权
    N-terminally substituted dipeptide amides 失效
    N-末端取代的二肽酰胺

    公开(公告)号：US4760180A

    公开(公告)日：1988-07-26

    申请号：US882795

    申请日：1986-07-14

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

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

    IPC: A61K38/00 ,  C07K5/065 ,  C07C103/20

    CPC classification number: C07K5/06078 ,  A61K38/00

    Abstract: This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is lower alkoxy or --O--(CH.sub.2).sub.n -phenyl where the phenyl may be optionally substituted with 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, lower alkoxy or 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.7, R.sup.8, and R.sup.9 represent hydrogen or lower alkyl, R.sup.6 represents hydrogen, lower alkyl, lower alkenyl, or --(CH.sub.2).sub.m -cycloalkyl wherein m is 1 to 4 and the cycloalkyl has 3 to 8 carbon atoms; R.sup.10 is --(CH.sub.2).sub.p -phenyl wherein p is 1 to 4; and v represents an asymmetric carbon that may be racemic 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 racemic or have the D or L configuration. This invention also encompasses compounds where R.sup.1 is hydroxy, provided at least one of R.sup.4, R.sup.5, R.sup.6 or R.sup.9 is lower alkyl. The compounds of this invention are useful analgesic agents.

    Abstract translation: 本发明包括式IMA的化合物及其药学上可接受的酸加成盐，其中R 1是低级烷氧基或-O-（CH 2）n - 苯基，其中苯基可以任选地被卤素，-NO 2，-CN， NH 2或其中n为1至4的低级烷基; R2和R3表示低级烷基，卤素，低级烷氧基或R2或R3中的一个为氢，另一个为低级烷基，低级烷氧基或卤素; R 4，R 5，R 7，R 8和R 9表示氢或低级烷基，R 6表示氢，低级烷基，低级烯基或 - （CH 2）m - 环烷基，其中m为1至4，环烷基具有3至8个碳原子; R 10为 - （CH 2）p - 苯基，其中p为1至4; v表示可以是外消旋的或具有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，可以是外消旋的或具有D或L构型。 本发明还包括R1为羟基的化合物，只要R4，R5，R6或R9中的至少一个为低级烷基。 本发明的化合物是有用的止痛剂。

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