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    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
    1.
    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

    申请人： Françoise Bono ,  Michaël Bosch ,  Victor Dos Santos ,  Jean-Marc Herbert ,  Dino Nisato ,  Bernard Tonnerre ,  Jean Wagnon

    发明人： Françoise Bono ,  Michaël Bosch ,  Victor Dos Santos ,  Jean-Marc Herbert ,  Dino Nisato ,  Bernard Tonnerre ,  Jean Wagnon

    IPC分类号： A61K31/497 ,  A61K31/4965 ,  C07D241/04 ,  C07D295/00

    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。

    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
    2.
    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：US07468368B2

    公开(公告)日：2008-12-23

    申请号：US10516704

    申请日：2003-06-05

    申请人： Françoise Bono ,  Michaël Bosch ,  Victor Dos Santos ,  Jean-Marc Herbert ,  Dino Nisato ,  Bernard Tonnerre ,  Jean Wagnon

    发明人： Françoise Bono ,  Michaël Bosch ,  Victor Dos Santos ,  Jean-Marc Herbert ,  Dino Nisato ,  Bernard Tonnerre ,  Jean Wagnon

    IPC分类号： A61K31/50 ,  A61K31/501 ,  C07D241/04 ,  C07D401/00 ,  C07D403/00

    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; p 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 an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; 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; p为1或2; R1表示卤素原子; 三氟甲基; （C1-C4）烷基; （C 1 -C 4）烷氧基; 三氟甲氧基; R2表示氢原子或卤素原子; R3表示氢原子; 一组-OR5; 基团-CH 2 OR 5; 基团-NR 6 R 7; 一个-NR8COR9基团; 一组-NR8CONR10R11; 基团-CH 2 NR 12 R 13; 基团-CH2NR8CONR14R15; （C1-C4）烷氧基羰基; 一组-CONR16R17; 或者R 3构成与其连接的碳原子和哌啶环的相邻碳原子之间的双键; R 4表示选自以下的芳族基团：所述芳族基团是未取代的或被独立地选自卤素原子的取代基单取代或二取代; （C1-C4）烷基; （C 1 -C 4）烷氧基; 三氟甲基; 制备工艺及治疗应用。

    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
    4.
    发明申请
    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：US20060167007A1

    公开(公告)日：2006-07-27

    申请号：US10516808

    申请日：2003-06-05

    申请人： Francoise Bono ,  Michael Bosch ,  Victor Dos Santos ,  Jean-Marc Herbert ,  Dino Nisato ,  Bernard Tonnerre ,  Jean Wagnon

    发明人： Francoise Bono ,  Michael Bosch ,  Victor Dos Santos ,  Jean-Marc Herbert ,  Dino Nisato ,  Bernard Tonnerre ,  Jean Wagnon

    IPC分类号： A61K31/496 ,  C07D417/14 ,  C07D403/02

    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表示氢原子; 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
    9.
    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

    申请人： Andre Bernat ,  Jean-Marc Herbert ,  Gerard Valette

    发明人： Andre Bernat ,  Jean-Marc Herbert ,  Gerard Valette

    IPC分类号： A61K31/40 ,  A61K31/41 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/427 ,  A61K31/44 ,  A61K31/47 ,  A61K31/495 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P11/14 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D521/00 ,  A61K31/497 ,  A61K31/535

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    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
    10.
    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

    申请人： Andre Bernat ,  Jean-Marc Herbert ,  Gerard Valette

    发明人： Andre Bernat ,  Jean-Marc Herbert ,  Gerard Valette

    IPC分类号： A61K31/40 ,  A61K31/41 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/427 ,  A61K31/44 ,  A61K31/47 ,  A61K31/495 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P11/14 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D521/00 ,  C07D401/02

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    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。