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    • 2. 发明申请
    • Condensed n-heterocyclic compounds and their use as crf receptor antagonists
    • 缩合的N-杂环化合物及其作为crf受体拮抗剂的用途
    • US20070004708A1
    • 2007-01-04
    • US10552493
    • 2004-04-07
    • Daniele AndreottiGiovannie BernasconiEmiliano CastiglioniStefania ContiniRomano Di FabioElettra FazzolariAldo FerianiGabriella GentileMario MattioliAnna MingardiFabio SabbatiniYves St-Denis
    • Daniele AndreottiGiovannie BernasconiEmiliano CastiglioniStefania ContiniRomano Di FabioElettra FazzolariAldo FerianiGabriella GentileMario MattioliAnna MingardiFabio SabbatiniYves St-Denis
    • A61K31/549A61K31/519A61K31/496A61K31/501A61K31/4745C07D487/02C07D471/02
    • C07D471/04C07D487/04
    • The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof (Formula (I)) wherein the dashed line may represent a double bond; R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 lkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R2, nitro, hydroxy, —NR3R4, cyano and or a group Z; R1 is hydrogen, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; D, G is —C— optionally substituted; X is carbon or nitrogen; Y is nitrogen or —C— optionally substituted; W is a 4-8 membered ring, which may be saturated or may contain one to three double bonds, and in which:—one carbon atom is replaced by a carbonyl or S(O)m; and—one to four carbon atoms may optionally be replaced by oxygen, nitrogen or NR12, S(O)m, carbonyl, and such ring may be further substituted by 1 to 8 substituents; Z is a 5-6 membered heterocycle, which may be substituted by 1 to 8 R5 groups or a phenyl ring, which may be substituted by 1 to 4 substituents; m is an integer from 0 to 2. to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
    • 本发明提供了包含立体异构体,前体药物和药学上可接受的盐或溶剂合物(式(I))的式(I)化合物,其中虚线可以表示双键; R是芳基或杂芳基,其各自可以被1-4个选自以下的基团取代:卤素,C 1 -C 6烷基,C 1 -C 6烷氧基,卤代C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基,卤素 C 1 -C 6烷氧基,-C(O)R 2,硝基,羟基,-NR 3 R 4,氰基和/或Z ; R 1是氢,C 3 -C 7环烷基,C 1 -C 6烷基,C 1 -C 6烷氧基,C 1 -C 6硫代烷基,C 2 -C 6烯基,C 2 -C 6炔基,卤代C 1 -C 6烷基,卤代C 1 -C 6烷氧基,卤素,NR 3 R 4或氰基; D,G是-C-任选取代的; X是碳或氮; Y是氮或-C-任选取代的; W是4-8元环,其可以是饱和的或可以含有一至三个双键,并且其中: - 一个碳原子被羰基或S(O)m取代; 一至四个碳原子可以任选地被氧,氮或NR 12,S(O)m H,羰基取代,并且这种环可进一步被1 至8个取代基; Z是5-6元杂环,其可被1至8个R 5取代基或可被1至4个取代基取代的苯环; m为0至2的整数。其制备方法,含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子(CRF)介导的病症的用途。