公开(公告)号：EP1339691A1

公开(公告)日：2003-09-03

申请号：EP01998541.5

申请日：2001-11-26

申请人： GlaxoSmithKline S.p.A. ,  Laboratoire Glaxosmithkline S.A.S.

发明人： FARINA, Carlo,c/o Nikem Research srl ,  GIARDINA, Giuseppe,c/o Nikem Research srl ,  GRUGNI, Mario,c/o Nikem Research srl ,  NADLER, G. M. ,c/o Laboratoire GlaxoSmithKline

IPC分类号： C07D215/52 ,  C07D401/06 ,  C07D401/14 ,  A61K31/47 ,  A61P11/00

CPC分类号： C07D401/06 ,  C07D401/14

摘要： Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof, wherein R1 is H or alkyl; R2 is R8R9; R8 is a single bond or alkyl, optionally substituted one or more times by hydroxy; R9 is aryl or cycloalkyl or heteroaryl, optionally substituted one or more times by hydroxy, alkoxy ou alkoxyalkyl; R3 is H or alkyl or cycloalkyl or cycloalkylalkyl, optionally substituted one or more times by hydroxy or by one or more fluorines; R4 is NR10R11; R10 and R11 Are independently selected from H or alkyl, or R10 and R11 together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring comprising 3-8 ring menbers, which heterocyclic ring is unsubstituted or is substituted one or more times by one or more substituents R12; R12 is oxo or R13R14R15, wherein R13 Is a single bond or alkyl, R14 is OC(O) or C(O)O, and R15 is H or alkyl; R5 is an alkyl, cycloalkyl, cycloalkylalkyl, aryl or single or fused ring aromatic heterocyclic group, which group is unsubstituted or is substituted one or more times by one or more substituents selected from halo such as fluoro, alkyl or haloalkyl such as fluoroalkyl; R6 represents H or up to three substituents independently selected from the list consisting of: alkyl, alkenyl, aryl, alkoxy or a hydroxylated derivative thereof, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, alkoxycarbonyl, haloalkyl such as trifluoromethyl, acyloxy, amino, mono- or di- alkylamino, alkoxyamido, alkoxycarboxylate or an esterified derivative thereof; R7 is H or halo; a is 1-6; and any of R1, R3, R5, R8, R10, R11 and R12 May optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy or oxo; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.

摘要翻译： 某些下式（I）化合物或其药学上可接受的盐或水合物，其中R1是H或烷基; R2是R8R9; R8是单键或烷基，任选被羟基取代一次或多次; R9为芳基或环烷基或杂芳基，任选被羟基，烷氧基或烷氧基烷基取代一次或多次; R3是H或烷基或环烷基或环烷基烷基，任选被羟基或一个或多个氟取代一次或多次; R4是NR10R11; R10和R11独立地选自H或烷基，或者R10和R11与它们所连接的氮原子一起形成包含3-8个环的饱和或不饱和杂环，该杂环是未取代的或被一个或多个 时间被一个或多个取代基R12取代; R12是氧代或R13R14R15，其中R13是单键或烷基，R14是OC（O）或C（O）O，并且R15是H或烷基; R5是烷基，环烷基，环烷基烷基，芳基或单或稠环芳族杂环基，该基团未被取代或被一个或多个选自以下的取代基取代一次或多次：卤素如氟，烷基或卤代烷基如氟烷基; R6代表H或至多三个独立地选自下列的取代基：烷基，烯基，芳基，烷氧基或其羟基化衍生物，羟基，卤素，硝基，氰基，羧基，甲酰氨基，磺酰氨基，烷氧羰基，卤代烷基如三氟甲基， 酰氧基，氨基，单 - 或二 - 烷基氨基，烷氧基酰氨基，烷氧基羧酸酯或其酯化衍生物; R7是H或卤素; a是1-6; 并且R 1，R 3，R 5，R 8，R 10，R 11和R 12中的任何一个可以任选被卤素，羟基，氨基，氰基，硝基，羧基或氧代取代一次或多次; 制备这些化合物的方法，包含这些化合物的药物组合物以及这些化合物和组合物在药物中的用途。