Diphenyl-pyrazolopyridine derivatives, preparation thereof, and use thereof as nuclear receptor not modulators
    2.
    发明授权
    Diphenyl-pyrazolopyridine derivatives, preparation thereof, and use thereof as nuclear receptor not modulators 有权
    二苯基 - 吡唑并吡啶衍生物,其制备方法及其作为核受体而不是调节剂的用途

    公开(公告)号:US08680096B2

    公开(公告)日:2014-03-25

    申请号:US13513497

    申请日:2010-12-03

    CPC分类号: C07D471/04

    摘要: The invention relates to a formula (I), in which R is a hydrogen or halogen atom or a (C1-C6)alkyl group; X is one or more substituents selected from a hydrogen or halogen atom, a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, hydroxy, or hydroxy(C1-C6)alkyl group; Y is a hydrogen or halogen atom or a (C1-C6)alkyl group; R1 is an NR2R3 or OR4 group; R2 and R3 independently are a hydrogen atom, a (C1-C6)alkyl, hydroxy(C1-C6)alkyl or oxo(C1-C6)alkyl group or R2 and R3, together with the nitrogen atom supporting the same, form a heterocycle optionally substituted by a (C1-C6)alkyl, hydroxy or oxo group; and R4 is a (C1-C6)alkyl, hydroxy(C1-C6)alkyl, or oxo(C1-C6)alkyl group, in the base or acid addition salt state. Said formula can be used therapeutically for treating or preventing diseases linked to the nuclear receptors Nurr-1, also known as NR4A2, NOT, TINUR, RNR-1, and HZF3.

    摘要翻译: 本发明涉及式(I),其中R是氢或卤原子或(C1-C6)烷基; X是一个或多个选自氢或卤素原子,(C 1 -C 6)烷基,卤代(C 1 -C 6)烷基,(C 1 -C 6)烷氧基,卤代(C 1 -C 6)烷氧基,氰基,羟基或 羟基(C 1 -C 6)烷基; Y是氢或卤素原子或(C1-C6)烷基; R1是NR2R3或OR4基团; R2和R3独立地是氢原子,(C1-C6)烷基,羟基(C1-C6)烷基或氧代(C1-C6)烷基或R2和R3与支持它的氮原子一起形成杂环 任选被(C 1 -C 6)烷基,羟基或氧代基取代; 并且R 4是在碱或酸加成盐状态下的(C 1 -C 6)烷基,羟基(C 1 -C 6)烷基或氧代(C 1 -C 6)烷基。 所述配方可用于治疗或预防与核受体Nurr-1(也称为NR4A2,NOT,TINUR,RNR-1和HZF3)相关的疾病。

    Acetylene derivatives of 5-phenyl-pyrazolopyridine, preparation thereof, and therapeutic use thereof
    4.
    发明授权
    Acetylene derivatives of 5-phenyl-pyrazolopyridine, preparation thereof, and therapeutic use thereof 有权
    5-苯基 - 吡唑并吡啶的乙炔衍生物,其制备及其治疗用途

    公开(公告)号:US08546424B2

    公开(公告)日:2013-10-01

    申请号:US13395819

    申请日:2010-09-17

    CPC分类号: C07D471/04

    摘要: Compounds of formula (I): in which: R1 and R2 represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl group, R3 represents one or more hydrogen or halogen atoms, X represents from 1 to 4 substituents, identical to or different from one another, chosen from hydrogen, halogen or (C1-C6)alkyl, in the form of the base or of an addition salt with an acid. Therapeutic use and synthetic process.

    摘要翻译: 式(I)化合物:其中:R1和R2彼此独立地表示氢原子或(C1-C6)烷基,R3表示一个或多个氢或卤素原子,X表示1至4个取代基 ,彼此相同或不同,选自氢,卤素或(C1-C6)烷基,其为碱的形式或与酸的加成盐。 治疗用途和合成过程。

    5-PHENYLPYRAZOLOPYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF

    公开(公告)号:US20130023554A1

    公开(公告)日:2013-01-24

    申请号:US13496118

    申请日:2010-09-17

    CPC分类号: C07D471/06

    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.

    DIPHENYL-PYRAZOLOPYRIDINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF AS NUCLEAR RECEPTOR NOT MODULATORS
    6.
    发明申请
    DIPHENYL-PYRAZOLOPYRIDINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF AS NUCLEAR RECEPTOR NOT MODULATORS 有权
    二苯基吡唑并吡啶衍生物,其制备方法及其作为核受体而不是调节剂

    公开(公告)号:US20120245164A1

    公开(公告)日:2012-09-27

    申请号:US13513497

    申请日:2010-12-03

    CPC分类号: C07D471/04

    摘要: The invention relates to a formula (I), in which R is a hydrogen or halogen atom or a (C1-C6)alkyl group; X is one or more substituents selected from a hydrogen or halogen atom, a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, hydroxy, or hydroxy(C1-C6)alkyl group; Y is a hydrogen or halogen atom or a (C1-C6)alkyl group; R1 is an NR2R3 or OR4 group; R2 and R3 independently are a hydrogen atom, a (C1-C6)alkyl, hydroxy(C1-C6)alkyl or oxo(C1-C6)alkyl group or R2 and R3, together with the nitrogen atom supporting the same, form a heterocycle optionally substituted by a (C1-C6)alkyl, hydroxy or oxo group; and R4 is a (C1-C6)alkyl, hydroxy(C1-C6)alkyl, or oxo(C1-C6)alkyl group, in the base or acid addition salt state. Said formula can be used therapeutically for treating or preventing diseases linked to the nuclear receptors Nurr-1, also known as NR4A2, NOT, TINUR, RNR-1, and HZF3.

    摘要翻译: 本发明涉及式(I),其中R是氢或卤原子或(C1-C6)烷基; X是一个或多个选自氢或卤素原子,(C 1 -C 6)烷基,卤代(C 1 -C 6)烷基,(C 1 -C 6)烷氧基,卤代(C 1 -C 6)烷氧基,氰基,羟基或 羟基(C 1 -C 6)烷基; Y是氢或卤素原子或(C1-C6)烷基; R1是NR2R3或OR4基团; R2和R3独立地是氢原子,(C1-C6)烷基,羟基(C1-C6)烷基或氧代(C1-C6)烷基或R2和R3与支持它的氮原子一起形成杂环 任选被(C 1 -C 6)烷基,羟基或氧代基取代; 并且R 4是在碱或酸加成盐状态下的(C 1 -C 6)烷基,羟基(C 1 -C 6)烷基或氧代(C 1 -C 6)烷基。 所述配方可用于治疗或预防与核受体Nurr-1(也称为NR4A2,NOT,TINUR,RNR-1和HZF3)相关的疾病。