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62 条记录 (耗时 0.036 秒)

    Opioid agonist compounds
    43.
    发明授权
    Opioid agonist compounds 失效
    阿片样物质激动剂化合物

    公开(公告)号：US5225417A

    公开(公告)日：1993-07-06

    申请号：US823221

    申请日：1992-01-21

    申请人： Michael S. Dappen ,  Barnett S. Pitzele ,  Michael F. Rafferty

    发明人： Michael S. Dappen ,  Barnett S. Pitzele ,  Michael F. Rafferty

    IPC分类号： C07D489/09 ,  C07D491/20 ,  C07D495/20

    CPC分类号： C07D491/20 ,  C07D495/20

    摘要： The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are opioid agonists which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

    摘要翻译： 本发明提供式I的取代的二苯并氮杂化合物：式I，其为可用作治疗疼痛的止痛剂的阿片样物质激动剂，药物组合物，其包含治疗有效量的式I化合物与 药学上可接受的载体，以及用于消除或改善动物疼痛的方法，包括向动物施用治疗有效量的式I化合物。

    Substituted dipeptide amides #3
    44.
    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。

    N-terminally substituted dipeptide amides
    45.
    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

    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 ,  C07C103/20

    CPC分类号： C07K5/06078 ,  A61K38/00

    摘要： 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.

    摘要翻译： 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。

    2-amino-3, 4 heptenoic compounds useful as nitric oxide synthase inhibitors
    47.
    发明授权
    2-amino-3, 4 heptenoic compounds useful as nitric oxide synthase inhibitors 失效
    可用作一氧化氮合酶抑制剂的2-氨基-3,4-庚烯化合物

    公开(公告)号：US06956131B2

    公开(公告)日：2005-10-18

    申请号：US09834815

    申请日：2001-04-13

    申请人： Barnett S. Pitzele ,  James A. Sikorski ,  Ronald Keith Webber

    发明人： Barnett S. Pitzele ,  James A. Sikorski ,  Ronald Keith Webber

    IPC分类号： C07C257/12 ,  C07C251/00

    CPC分类号： C07C257/12

    摘要： The present invention is directed to a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R2 is selected from the group consisting of H and methyl; and R2 is selected from the group consisting of H and methyl. The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，其中：R 2选自H和甲基; 和R 2选自H和甲基。 该化合物具有有用的一氧化氮合成酶抑制活性，并且预期可用于治疗或预防一氧化氮的合成或过度合成形成贡献部分的疾病或病症。

    2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors
    48.
    发明授权
    2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors 失效
    可用作一氧化氮合酶抑制剂的2-氨基-4,5-庚烯酸衍生物

    公开(公告)号：US06787668B2

    公开(公告)日：2004-09-07

    申请号：US09835196

    申请日：2001-04-13

    申请人： Barnett S. Pitzele ,  James A. Sikorski ,  Ronald Keith Webber

    发明人： Barnett S. Pitzele ,  James A. Sikorski ,  Ronald Keith Webber

    IPC分类号： C07C25700

    CPC分类号： C07C257/14

    摘要： The present invention is directed to a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R1 is selected from the group consisting of H and methyl; and R2 is selected from the group consisting of H and methyl. The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，其中：R 1选自H和甲基; 并且R 2选自H和甲基。化合物具有有效的一氧化氮合成酶抑制活性，并且预期可用于治疗或预防一氧化氮的合成或过度合成形成疾病或病症 贡献部分