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    Pyridyl and pyrimidinyl substituted tyrosyl dipeptide amides
    34.
    发明授权
    Pyridyl and pyrimidinyl substituted tyrosyl dipeptide amides 失效
    吡啶基和嘧啶基取代的酪氨酰二肽酰胺

    公开(公告)号：US4933325A

    公开(公告)日：1990-06-12

    申请号：US145953

    申请日：1988-01-20

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

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

    IPC分类号： A61K38/00 ,  C07K5/065

    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.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 gorup 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.

    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; R10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。

    Fluorenyl substituted tyrosyl dipeptide amides which are useful in treating pain
    35.
    发明授权
    Fluorenyl substituted tyrosyl dipeptide amides which are useful in treating pain 失效
    可用于治疗疼痛的芴基取代的酪氨酰二肽酰胺

    公开(公告)号：US4847241A

    公开(公告)日：1989-07-11

    申请号：US145954

    申请日：1988-01-20

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

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

    IPC分类号： A61K38/00 ,  C07K5/065

    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.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 substitutent 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 symmetric 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.

    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。

    Phenyl substituted dipeptide amides
    36.
    发明授权
    Phenyl substituted dipeptide amides 失效
    苯取代二肽酰胺

    公开(公告)号：US4822775A

    公开(公告)日：1989-04-18

    申请号：US882794

    申请日：1986-07-14

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

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

    IPC分类号： A61K38/00 ,  C07K5/065 ,  A61K31/34 ,  C07D317/54 ,  C07D317/58 ,  C07K5/06

    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.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.

    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， 当ALK不是亚烷基时，低级烷氧基，羧酰胺，二低级烷基氨基或X代表苯基; 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。

    O-substituted tyrosyl dipeptide amides
    37.
    发明授权
    O-substituted tyrosyl dipeptide amides 失效
    N-末端取代的酪氨酰丙氨酸

    公开(公告)号：US4797470A

    公开(公告)日：1989-01-10

    申请号：US14340

    申请日：1987-02-13

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

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

    IPC分类号： A61K38/00 ,  C07K5/065 ,  C07K5/08

    CPC分类号： C07K5/06078 ,  A61K38/00

    摘要： This invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is ##STR2## where X is oxygen or sulfur, Y is oxygen or nitrogen, and R.sup.11 represents straight or branched chain lower alkenyl having 2-6 carbon atoms, or phenyl, benzyl, and their equivalents such as nitro, halogen, or lower alkyl or lower alkoxy substituted phenyl or benzyl; wherein R.sup.2 and R.sup.3 may be the same or different and represent straight or branched chain lower alkyl having 1-6 carbon atoms, wherein R.sup.4 -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 C.sub.w is 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 is an asymmetric carbon atom and may be racemic or may have the D or L configuration.The compounds of this invention are useful because they possess analgesic activity in mammals.

    摘要翻译： 本发明涉及下式的化合物及其药学上可接受的酸加成盐，其中R 1为X，其中X为氧或硫，Y为氧或氮，R11为直链或支链低级烯基，其具有2 -6个碳原子，或苯基，苄基及其等同物如硝基，卤素或低级烷基或低级烷氧基取代的苯基或苄基; 其中R2和R3可以相同或不同，表示具有1-6个碳原子的直链或支链低级烷基，其中R4-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 碳原子 其中当R 7和R 8不相同时，C w是不对称碳原子，并且可以是外消旋的或具有D或L构型; 并且其中Cv是不对称碳原子并且可以是外消旋的或可以具有D或L构型。 本发明的化合物是有用的，因为它们在哺乳动物中具有止痛活性。

    Substituted dipeptide amides #3
    40.
    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

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

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

    IPC分类号： A61K38/00 ,  C07K5/065

    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.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.

    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。