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    Delta opioid receptor antagonists
    4.
    发明授权
    Delta opioid receptor antagonists 失效
    Delta阿片受体拮抗剂

    公开(公告)号：US5578725A

    公开(公告)日：1996-11-26

    申请号：US380091

    申请日：1995-01-30

    Applicant: Philip S. Portoghese ,  Francine S. Farouz-Grant

    Inventor： Philip S. Portoghese ,  Francine S. Farouz-Grant

    IPC: C07D489/09 ,  C07D491/20 ,  C07D489/10

    CPC classification number: C07D491/20

    Abstract: Compounds are provided of the formula: ##STR1## wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.6 -C.sub.12)aralkyl, trans(C.sub.4 -C.sub.5)alkenyl, allyl or furan-2-ylalkyl, R.sup.2 is H, OH or O.sub.2 C(C.sub.1 -C.sub.5)alkyl; R.sup.3 is H, (C.sub.6 -C.sub.10)aralkyl, (C.sub.1 -C.sub.5)alky or (C.sub.1 -C.sub.5)alkylCO; X is O, S or NY, wherein Y is H, benzyl or (C.sub.1 -C.sub.5)alkyl; R is CH(Z)CO.sub.2 Y, wherein Z is H, CH.sub.2 CO.sub.2 Y or (CH.sub.2).sub.n N(R.sup.4)(R.sup.5), wherein n is 1-5 and R.sup.4 and R.sup.5 are individually H, (C.sub.1 -C.sub.4)alkyl, phenyl, (C.dbd.NH)NH.sub.2, benzyloxycarbonyl or (C.dbd.NHNO.sub.2); and the pharmaceutically acceptable salts thereof.

    Abstract translation: 化合物由下式提供：其中R1是（C1-C5）烷基，C3-C6（环烷基）烷基，C5-C7（环烯基）烷基，（C6-C12）芳基，（C6-C12）芳烷基， 反式（C 4 -C 5）烯基，烯丙基或呋喃-2-基烷基，R 2是H，OH或O 2 C（C 1 -C 5）烷基; R3是H，（C6-C10）芳烷基，（C1-C5）烷基或（C1-C5）烷基CO; X是O，S或NY，其中Y是H，苄基或（C1-C5）烷基; R是CH（Z）CO 2 Y，其中Z是H，CH 2 CO 2 Y或（CH 2）n N（R 4）（R 5），其中n是1-5，R 4和R 5分别是H，（C 1 -C 4）烷基，苯基，（ C = NH）NH 2，苄氧羰基或（C = NHNO 2）; 及其药学上可接受的盐。

    Opioid agonist compounds
    5.
    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：US5436249A

    公开(公告)日：1995-07-25

    申请号：US243661

    申请日：1994-05-16

    Applicant: Michael S. Dappen ,  Barnett S. Pitzele ,  Michael F. Rafferty

    Inventor： Michael S. Dappen ,  Barnett S. Pitzele ,  Michael F. Rafferty

    IPC: C07D489/09 ,  C07D491/20 ,  C07D495/20 ,  A61K31/44 ,  C07D491/12

    CPC classification number: C07D491/20 ,  C07D495/20

    Abstract: The present invention provides novel substituted opioid analgesic compounds of Formula I: ##STR1## which are opioid agonists, and 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.

    Abstract translation: 本发明提供式I的新颖的取代的阿片样物质镇痛化合物：作为阿片样物质激动剂的式I化合物，其可用作治疗疼痛的止痛剂，药物组合物包含治疗有效量的式I化合物 与药学上可接受的载体组合，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。

    Facile conversion of morphine to normorphine
    6.
    发明授权
    Facile conversion of morphine to normorphine 有权

    公开(公告)号：US11247999B1

    公开(公告)日：2022-02-15

    申请号：US17367251

    申请日：2021-07-02

    Applicant: Joseph DeGraw

    Inventor： Joseph DeGraw

    IPC: C07D489/09

    Abstract: There are provided methods of making an N-demethylated derivative of morphine namely, normorphine. The normorphine can be substituted at the N—H position with various ligands that may result in new useful morphine derivatives. These derivatives may have increased analgesic efficacy, have less addictive properties, and/or have effective anti-opiate properties capable of rescuing overdosed persons or lead to recovery from conditions caused by opiate drug abuse.

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