发明申请
- 专利标题: 5-PHENYLPYRAZOLOPYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
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申请号: US13496118申请日: 2010-09-17
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公开(公告)号: US20130023554A1公开(公告)日: 2013-01-24
- 发明人: Florian Auger , Danielle De Peretti , Luc Even
- 申请人: Florian Auger , Danielle De Peretti , Luc Even
- 申请人地址: FR Paris
- 专利权人: SANOFI
- 当前专利权人: SANOFI
- 当前专利权人地址: FR Paris
- 优先权: FR0956444 20090918
- 国际申请: PCT/FR10/51932 WO 20100917
- 主分类号: C07D471/04
- IPC分类号: C07D471/04 ; C07F5/02 ; A61P25/28 ; A61P25/08 ; A61P29/00 ; A61P25/30 ; A61P19/10 ; A61P35/00 ; A61P25/16 ; A61P25/18 ; A61P25/24 ; A61K31/437 ; A61P25/00
摘要:
Compounds of formula (I): in which:R1 represents a phenyl group or naphthyl group, optionally substituted by one or more atoms or groups chosen, independently of one another, from: halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, (C1-C6)thioalkyl, —S(O)(C1-C6)alkyl, —S(O)2(C1-C6)alkyl, hydroxyl, hydroxy(C1-C6)alkylene, CHO, COOH, (C1-C6)alkoxy(C1-C6)alkyleneoxy, NRaRb, CONRaRb, SO2NRaRb, NRcCORd, OC(O)NRaRb, OCO(C1-C6)alkyl, NRcC(O)ORe or NRcSO2Re; X represents from 1 to 4 substituents which are identical to or different from one another and which are chosen from hydrogen, halogen, (C1-C6)alkyl or (C1-C6)alkoxy, it being possible for the (C1-C6)alkyl to be optionally substituted by one or more groups chosen from a halogen, (C1-C6)alkoxy or hydroxyl; R2 and R3 represent, independently of one another, a hydrogen atom, a (C1-C6)alkyl group optionally substituted by an Rf group, or a CHO or COOH group; X and R3 can together form, with the carbon atoms which carry them, a carbocycle of 5 to 7 carbon atoms; R4 represents a hydrogen atom or a (C1-C6)alkyl group; Ra and Rb represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl, aryl(C1-C6)alkylene or aryl group; or Ra and Rb together form, with the nitrogen atom which carries them, an azetidine, pyrrolidine, piperidine, azepine, morpholine, thiomorpholine, piperazine or homopiperazine group, this group being optionally substituted by a (C1-C6)alkyl, aryl or aryl(C1-C6)alkylene group; Rc and Rd represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl, aryl(C1-C6)alkylene or aryl group; or Rc and Rd together form a (C2-C5)alkylene group; Re represents a (C1-C6)alkyl, aryl(C1-C6)alkylene or aryl group; or Rc and Re together form a (C2-C5)alkylene group; Rf represents a hydroxyl, oxo, CHO or COOH group, in the form of the base or of an addition salt with an acid.Therapeutic use and synthetic process.
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