Indole, azaindole and related heterocyclic amidopiperazine derivatives
    1.
    发明授权
    Indole, azaindole and related heterocyclic amidopiperazine derivatives 有权
    吲哚,氮杂吲哚和相关的杂环酰胺基哌嗪衍生物

    公开(公告)号:US06825201B2

    公开(公告)日:2004-11-30

    申请号:US10127256

    申请日:2002-04-22

    IPC分类号: A61K31496

    摘要: The invention comprises substituted indole, azaindole and related heterocyclic amidopiperazine derivatives of general Formula I wherein: Q is —may represent a bond; A is selected from the group consisting of C1-6alkoxy, C1-6alkyl, C3-7cycloalkyl, phenyl, and heteroaryl; wherein said heteroaryl may be monocyclic or bicyclic and may be comprised of three to eleven atoms selected from the group consisting of C, N, NR9, O, and S, and wherein each ring of said phenyl and heteroaryl is optionally substituted with one to five same or different substituents selected from the group consisting of R19-R23; T is U is NR7, O, or S; V is C(H)kR1, O or N(R7′)k; W is CR3 or NR10; X is CR4 or NR10; Y is CR5 or NR10; Z is CR6 or NR10; k is 0 or 1; and m, n, and p are each independently 0, 1, or 2 provided that the sum of m, n, and p must equal 1 or 2; compositions thereof and their use as antiviral agents, particularly for treating HIV infection.

    摘要翻译: 本发明包括取代的吲哚,氮杂吲哚和通式I的相关杂环酰胺基哌嗪衍生物,其中Q可以表示键; A选自C1-6烷氧基,C1-6烷基,C3-7环烷基,苯基和杂芳基; 其中所述杂芳基可以是单环或双环的,并且可以由选自C,N,NR 9,O和S的三至十一个原子组成,并且其中所述苯基和杂芳基的每个环任选被 一至五个相同或不同的选自R 19 -R 23的取代基; T是U是NR 7,O或S; V是C(H)k R 1,O或N (R 7')k; W是CR 3或NR 10; X是CR 4或NR 10; Y是CR 5或NR 10; Z是CR 6 >或NR 10; k为0或1; m,n和p各自独立地为0,1或2,条件是m,n和p之和必须等于1或2;其组成及其组成 用作抗病毒剂,特别是用于治疗HIV感染。

    Piperazine-containing compounds useful in the treatment of pain
    3.
    发明授权
    Piperazine-containing compounds useful in the treatment of pain 失效
    可用于治疗疼痛的含有哌嗪的化合物

    公开(公告)号:US06784181B2

    公开(公告)日:2004-08-31

    申请号:US10149911

    申请日:2002-10-21

    IPC分类号: A61K31496

    摘要: The present invention is directed to a compound of general formula (I), wherein R1 is selected from phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl; each phenyl ring and heteroaromatic ring optionally and independently being further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo, as well as their pharmaceutically acceptable salts. The invention includes pharmaceutical compositions comprising these compounds and the use of the compounds in therapy, in particular in the management of pain.

    摘要翻译: 本发明涉及通式(I)的化合物,其中R 1选自苯基,吡啶基,噻吩基,呋喃基,咪唑基; 每个苯环和杂芳环任选和独立地被1,2或3个选自直链和支链C 1 -C 6烷基,NO 2,CF 3,C 1 -C 6烷氧基,氯,氟,溴和碘的取代基取代,以及 其药学上可接受的盐。 本发明包括包含这些化合物的药物组合物和化合物在治疗中的用途,特别是用于治疗疼痛。

    Use of 2-amino-thiazoline derivatives as inhibitors of inducible NO-synthase
    6.
    发明授权
    Use of 2-amino-thiazoline derivatives as inhibitors of inducible NO-synthase 失效
    使用2-氨基 - 噻唑啉衍生物作为诱导型NO合成酶的抑制剂

    公开(公告)号:US06699867B2

    公开(公告)日:2004-03-02

    申请号:US10291084

    申请日:2002-11-08

    IPC分类号: A61K31496

    摘要: The present invention relates to the use of 2-amino-thiazoline derivatives of formula (I): in which either Y is a methylene (CH2) and X is chosen from the following groups: O, NH, (C1-C4) N-Alkyl, N-Bn, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 or CHPh; or Y is a carbonyl (C═O) and X is chosen from the following groups: NH, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl or N-5-pyrimidyl or pharmaceutically acceptable salts thereof as inhibitors of inducible NO-synthase.

    摘要翻译: 本发明涉及式(I)的2-氨基 - 噻唑啉衍生物的用途:其中Y是亚甲基(CH 2),X选自下列基团:O,NH,(C 1 -C 4) 烷基,N-Bn,N-Ph,N-(2-Py),N-(3-Py),N-(4-Py),N-2-嘧啶基,N-5-嘧啶基, SO2,CH2或CHPh; 或者Y是羰基(C = O),X选自下列基团:NH,N-Ph,N-(2-Py),N-(3-Py),N-(4-Py),N -2-嘧啶基或N-5-嘧啶基或其药学上可接受的盐作为诱导型NO合成酶的抑制剂。