Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
    3.
    发明授权
    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof 有权
    哌嗪酰基哌啶衍生物,其制备和治疗用途

    公开(公告)号:US07294628B2

    公开(公告)日:2007-11-13

    申请号:US10516808

    申请日:2003-06-05

    CPC分类号: C07D417/14 C07D401/14

    摘要: The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4) alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents the aromatic group 1,3-thiazol-2-yl of formula: Preparation process and therapeutic application.

    摘要翻译: 本发明涉及通式(I)的取代的1-哌嗪基酰基哌啶衍生物,其中n为1或2; R 1表示卤素原子; 三氟甲基; (C 1 -C 4 -C 4)烷基; (C 1 -C 4 -C 4)烷氧基; 三氟甲氧基; R 2表示氢原子或卤素原子; R 3代表氢原子; 一个基团-OR 5; 基团-CH 2或OR 5; 基团-NR 6 R 7; 基团-NR 8 COR 9; 基团-NR 8 CONR 10 R 11; 基团-CH 2 NR 12 R 13; 基团-CH 2 NR 8 CONR 14 R 15 15; (C 1 -C 4 -C 4)烷氧基羰基; 基团-CONR 16 R 17 R 17; 或者R 3 3在其所连接的碳原子和哌啶环的相邻碳原子之间构成双键; R 4代表下式的芳族基团1,3-噻唑-2-基:制备方法和治疗应用。

    Heterocyclic derivatives, process for their preparation and their
therapeutic use
    7.
    发明授权
    Heterocyclic derivatives, process for their preparation and their therapeutic use 失效
    杂环衍生物,其制备方法及其治疗用途

    公开(公告)号:US06057318A

    公开(公告)日:2000-05-02

    申请号:US81782

    申请日:1998-05-20

    摘要: The invention relates to compounds of formula: ##STR1## in which: A is selected from O or S; B is selected from C or N;Z.sub.1 is selected from C.sub.1 -C.sub.4 alkylene or phenylene;Z.sub.2 is C.sub.1 -C.sub.4 alkylene; W is NR.sub.1 R.sub.2, in which R.sub.1 is selected from H or C.sub.1 -C.sub.4 alkyl and R.sub.2 is selected from H, C.sub.1 -C.sub.4 alkyl, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2 in which Q.sub.1 and Q.sub.2 are independently selected from H or C.sub.1 -C.sub.4 alkyl, SO.sub.2 Q.sub.3 or COQ.sub.3 in which Q.sub.3 is C.sub.1 -C.sub.4 alkyl, COOQ.sub.4 in which Q.sub.4 is selected from C.sub.1 -C.sub.4 alkyl or benzyl, or R.sub.1 and R.sub.2 taken together with N form a saturated heterocycle, or W is selected from C.sub.1 -C.sub.4 alkoxy or thioalkoxy, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2, pyridyl, imidazolyl or COOQ.sub.5 in which Q.sub.5 is C.sub.1 -C.sub.5 alkyl; R.sub.3 is not present when B is N, or is H, C.sub.1 -C.sub.8 alkyl or halogen; Ar.sub.1 is selected from optionally substituted phenyl, thienyl, furyl, indolyl, naphthyl or benzyl or Ar.sub.1 and R.sub.3 taken together form a phenylalkylene group; Ar.sub.2 is selected from pyrimidinyl, quinolyl, isoquinolyl, indolyl, isoindolyl or pyridyl, optionally substituted; as well as their salts.Use as medicines.

    摘要翻译: 本发明涉及下式的化合物:其中:A选自O或S; B选自C或N; Z1选自C1-C4亚烷基或亚苯基; Z2是C1-C4亚烷基; W是NR1R2,其中R1选自H或C1-C4烷基,R2选自H,C1-C4烷基,CONQ1Q2或CSNQ1Q2,其中Q1和Q2独立地选自H或C1-C4烷基,SO2Q3或COQ3 其中Q3是C1-C4烷基,其中Q4选自C1-C4烷基或苄基的COOQ4,或与N一起形成的R 1和R 2形成饱和杂环,或W选自C 1 -C 4烷氧基或硫代烷氧基,CONQ 1 Q 2或 CSNQ1Q2,吡啶基,咪唑基或COOQ5,其中Q5是C1-C5烷基; 当B为N时,R 3不存在,或为H,C 1 -C 8烷基或卤素; Ar1选自任选取代的苯基,噻吩基,呋喃基,吲哚基,萘基或苄基或Ar1和R3一起形成苯基亚烷基; Ar2选自嘧啶基,喹啉基,异喹啉基,吲哚基,异吲哚基或吡啶基,任选取代; 以及它们的盐。 用作药物。

    Heterocyclic derivatives process for their preparation and their
therapeutic use
    9.
    发明授权
    Heterocyclic derivatives process for their preparation and their therapeutic use 失效
    杂环衍生物制备方法及其治疗用途

    公开(公告)号:US5891894A

    公开(公告)日:1999-04-06

    申请号:US081783

    申请日:1998-05-20

    摘要: The invention relates to compounds of formula: ##STR1## in which: A is selected from 0 or S; B is selected from C or N; Z.sub.1 is selected from C.sub.1 -C.sub.4 alkylene or phenylene; Z.sub.2 is C.sub.1 -C.sub.4 alkylene; W is NR.sub.1 R.sub.2, in which R.sub.1 is selected from H or C.sub.1 -C.sub.4 alkyl and R.sub.2 is selected from H, C.sub.1 -C.sub.4 alkyl, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2 in which Q.sub.1 and Q.sub.2 are independently selected from H or C.sub.1 -C.sub.4 alkyl, SO.sub.2 Q.sub.3 or COQ.sub.3 in which Q.sub.3 is C.sub.1 -C.sub.4 alkyl, COOQ.sub.4 in which Q.sub.4 is selected from C.sub.1 -C.sub.4 alkyl or benzyl, or R.sub.1 and R.sub.2 taken together with N form a saturated heterocycle, or W is selected from C.sub.1 -C.sub.4 alkoxy or thioalkoxy, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2, pyridyl, imidazolyl or COOQ.sub.5 in which Q.sub.5 is C.sub.1 -C.sub.5 alkyl; R.sub.3 is not present when B is N, or is H, C.sub.1 -C.sub.8 alkyl or halogen; Ar.sub.1 is selected from optionally substituted phenyl, thienyl, furyl, indolyl, naphthyl or benzyl or Ar.sub.1 and R.sub.3 taken together form a phenylalkylene group; Ar.sub.2 is selected from pyrimidinyl, quinolyl, isoquinolyl, indolyl, isoindolyl or pyridyl, optionally substituted; as well as their salts.

    摘要翻译: 本发明涉及下式的化合物:其中:A选自0或S; B选自C或N; Z1选自C1-C4亚烷基或亚苯基; Z2是C1-C4亚烷基; W是NR1R2,其中R1选自H或C1-C4烷基,R2选自H,C1-C4烷基,CONQ1Q2或CSNQ1Q2,其中Q1和Q2独立地选自H或C1-C4烷基,SO2Q3或COQ3 其中Q3是C1-C4烷基,其中Q4选自C1-C4烷基或苄基的COOQ4,或与N一起形成的R 1和R 2形成饱和杂环,或W选自C 1 -C 4烷氧基或硫代烷氧基,CONQ 1 Q 2或 CSNQ1Q2,吡啶基,咪唑基或COOQ5,其中Q5是C1-C5烷基; 当B为N时,R 3不存在,或为H,C 1 -C 8烷基或卤素; Ar1选自任选取代的苯基,噻吩基,呋喃基,吲哚基,萘基或苄基或Ar1和R3一起形成苯基亚烷基; Ar2选自嘧啶基,喹啉基,异喹啉基,吲哚基,异吲哚基或吡啶基,任选取代; 以及它们的盐。