Pyridomorphinans, pyridazinomorphinans and use thereof
    5.
    发明授权
    Pyridomorphinans, pyridazinomorphinans and use thereof 有权
    吡哆醇,哒嗪吗啡喃及其用途

    公开(公告)号:US07541364B2

    公开(公告)日:2009-06-02

    申请号:US11718565

    申请日:2004-08-27

    IPC分类号: A61K31/4748 C07D491/12

    CPC分类号: C07D491/18

    摘要: Compounds represented by the formula: wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R′ is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence to μ agonists.

    摘要翻译: 由下式表示的化合物:其中R是C 1-6烷基; C4-6环烷基烷基; 或C 3-6烯基; R'是H或C 1-6烷基; X是H或OH; Y是烷基,环烷基,芳基,杂芳基,芳基烷基或芳酰基; Z为CH或N; 条件是X为H,当Z为CH且R为C 4环烷基烷基或C 4链烯基时; 其前药; 及其药学上可接受的盐。 上述化合物可用作治疗疼痛的止痛剂; 作为免疫调节剂,调节滥用药物的行为效应,调节对mu激动剂的耐受性和依赖性的发展。

    Nonpeptide Inhibitors of Matrix Metalloproteinases
    6.
    发明申请
    Nonpeptide Inhibitors of Matrix Metalloproteinases 失效
    基质金属蛋白酶的非肽抑制剂

    公开(公告)号:US20080312329A1

    公开(公告)日:2008-12-18

    申请号:US10593748

    申请日:2005-03-21

    摘要: Disclosed are selective inhibitors of matrix metalloproteinases represented by the following formula (I). wherein X is (CH2)nO, (CH2)nS, (CH2)nNR1, (CH2)n(CH2), or CH═CH, wherein n=0, 1, or 2; R and R1 are, independently, a substituted or unsubstitued alkyl, alkenyl, alkynyl, aryl, heteroaryl group, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl; and Z is NH or CH2; or a pharmaceutically acceptable salt thereof. Also disclosed are methods of making such compounds and methods of using such compounds to inhibit tumor progression and to treat diseases such as arthritis.

    摘要翻译: 公开了由下式(I)表示的基质金属蛋白酶的选择性抑制剂。 其中X是(CH 2)n O,(CH 2)n S,(CH 2)n NR1,(CH 2)n(CH 2)或CH-CH,其中n = 0,1或2; R和R 1独立地是取代或未取代的烷基,烯基,炔基,芳基,杂芳基,环烷基,杂环烷基,环烯基或杂环烯基; Z为NH或CH 2; 或其药学上可接受的盐。 还公开了制备这些化合物的方法和使用这些化合物抑制肿瘤进展和治疗疾病如关节炎的方法。

    Pyridomorphinans, thienomorphinans and use thereof
    7.
    发明授权
    Pyridomorphinans, thienomorphinans and use thereof 有权
    吡哆醇,噻吩吗啡喃及其用途

    公开(公告)号:US07105675B2

    公开(公告)日:2006-09-12

    申请号:US11259073

    申请日:2005-10-27

    IPC分类号: C07D498/20

    CPC分类号: C07D491/20 C07D495/20

    摘要: Compounds represented by the formulae: wherein each of Y, X and R individually is selected from the group consisting of hydrogen, hydroxy, halo, CF3, NO2, CN, NH2, COR1 and CO2R2 wherein R1 is selected from the group consisting of alkyl, aryl, alkaryl, and NH2, and R2 is selected from the group consisting of alkyl, aryl and aralkyl, and provided that at least one of Y, X and R is other than H; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain, as immunomodulators and for treating drug abuse.

    摘要翻译: 由下式表示的化合物:其中Y,X和R各自独立地选自氢,羟基,卤素,CF 3,NO 2,CN, 选择其中R 1,R 2,R 2,R 1,R 2,R 2,R 2, 由烷基,芳基,烷芳基和NH 2 2组成的组,R 2选自烷基,芳基和芳烷基,并且至少 Y,X和R之一不是H; 及其药学上可接受的盐。 上述式的化合物可用作治疗疼痛的止痛剂,作为免疫调节剂和用于治疗药物滥用。