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    Macrolide antibiotics
    6.
    发明授权
    Macrolide antibiotics 失效
    大环内酯抗生素

    公开(公告)号：US06900183B2

    公开(公告)日：2005-05-31

    申请号：US10450886

    申请日：2001-12-20

    申请人： Daniele Andreotti ,  Stefano Biondi ,  Sergio Lociuro

    发明人： Daniele Andreotti ,  Stefano Biondi ,  Sergio Lociuro

    IPC分类号： A01N25/34 ,  A01N43/22 ,  A01N63/02 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  A61K31/70

    CPC分类号： C07H17/08 ,  A61K9/0019 ,  A61K9/2018

    摘要： 11,12 γ lactone ketolides of the following formula: and pharmaceutically acceptable salts and solvates thereof, wherein R, R1, R2, and R3 are as described herein. The disclosure also relates to processes for the preparation of such compounds, to compositions containing them, and to their use in the therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.

    摘要翻译： 具有下式的11,12个γ-内酯酮内酯及其药学上可接受的盐和溶剂合物，其中R 1，R 2，R 2和R 3， SUB>如本文所述。 本公开还涉及制备这些化合物的方法，含有它们的组合物及其在治疗或预防人或动物体内的全身或局部细菌感染中的用途。

    Condensed n-heterocyclic compounds and their use as crf receptor antagonists
    9.
    发明申请
    Condensed n-heterocyclic compounds and their use as crf receptor antagonists 有权
    缩合的N-杂环化合物及其作为crf受体拮抗剂的用途

    公开(公告)号：US20070004708A1

    公开(公告)日：2007-01-04

    申请号：US10552493

    申请日：2004-04-07

    申请人： Daniele Andreotti ,  Giovannie Bernasconi ,  Emiliano Castiglioni ,  Stefania Contini ,  Romano Di Fabio ,  Elettra Fazzolari ,  Aldo Feriani ,  Gabriella Gentile ,  Mario Mattioli ,  Anna Mingardi ,  Fabio Sabbatini ,  Yves St-Denis

    发明人： Daniele Andreotti ,  Giovannie Bernasconi ,  Emiliano Castiglioni ,  Stefania Contini ,  Romano Di Fabio ,  Elettra Fazzolari ,  Aldo Feriani ,  Gabriella Gentile ,  Mario Mattioli ,  Anna Mingardi ,  Fabio Sabbatini ,  Yves St-Denis

    IPC分类号： A61K31/549 ,  A61K31/519 ,  A61K31/496 ,  A61K31/501 ,  A61K31/4745 ,  C07D487/02 ,  C07D471/02

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： 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).

    摘要翻译： 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。