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    Compounds bearing sulphamoyl and amidino radicals, their preparation process and pharmaceutical compositions containing them
    5.
    发明授权
    Compounds bearing sulphamoyl and amidino radicals, their preparation process and pharmaceutical compositions containing them 失效
    带有氨磺酰基和脒基的化合物，其制备方法和含有它们的药物组合物

    公开(公告)号：US5674890A

    公开(公告)日：1997-10-07

    申请号：US582887

    申请日：1996-01-04

    申请人： Bernard Christophe ,  Loic Foulon ,  Alain Pellet ,  Claudine Serradeil-Le Gal ,  Gerard Valette

    发明人： Bernard Christophe ,  Loic Foulon ,  Alain Pellet ,  Claudine Serradeil-Le Gal ,  Gerard Valette

    IPC分类号： A61K31/16 ,  A61K31/155 ,  A61K31/18 ,  A61K38/00 ,  A61P9/00 ,  A61P25/00 ,  C07C311/18 ,  C07D215/36 ,  C07K1/113 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07D333/22 ,  A61K31/38 ,  C07D409/12 ,  C07D413/12

    CPC分类号： C07K5/06078 ,  C07K5/06139 ,  A61K38/00

    摘要： A compound of formula I ##STR1## in which Ar.sub.1 is naphthyl and phenyl, quinolyl or isoquinolyl optionally substituted; Ar.sub.2 is phenyl or thienyl optionally substituted; R.sub.1, R.sub.2 and R'.sub.2 are independently of each other H or (C.sub.1 -C.sub.4)alkyl or R.sub.1 represents a bond and N is covalently bonded to Ar.sub.2, and optionally R.sub.2 and R'.sub.2 form a double bond, or R.sub.1 or R.sub.2 is covalently bonded to Ar.sub.2 and represents a (C.sub.1 -C.sub.3 )alkylene; R.sub.3 and R.sub.4 are independently of each other H or (C.sub.1 -C.sub.4)alkyl or form, with the nitrogen atom to which they are attached pyrrolidine, ppiperidine, or hexahydroazepine; Z.sub.1 represents (C.sub.1 -C.sub.12)alkylene, optionally interrupted by a radical selected from the group consisting of (C.sub.5 -C.sub.7)cycloalkyl and phenyl or substituted with a radical selected from the group consisting of (C.sub.5 -C.sub.7)cycloalkyl and phenyl; Q.sub.1 is selected from the group consisting of methyl, amino, (C.sub.1 -C.sub.4)alkoxycarbonylamino, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1 -C.sub.4)-alkylamino, pyrrolidinyl, piperidino, morpholino, piperazinyl, 4-(C.sub.1 -C.sub.4)alkylpiperazinyl, amidino, (C.sub.1 -C.sub.4)-alkylamidino, guanidino, (C.sub.1 -C.sub.4)alkylguanidino, pyridyl, imidazolyl, pyrimidinyl, indolyl, hydroxy,(C.sub.1 -C.sub.4)alkoxy,(C.sub.2 -C.sub.8)alkoxycarbonyl,N-�amino(C.sub.1 -C.sub.4)alkyl!-N-�(C.sub.1 -C.sub.4)alkyl!amino, carbamoyl, phenyl and phenyl substituted by a radical selected from the group consisting of Cl, F, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and hydroxyle; Q.sub.2 is selected from the group consisting of H and (C.sub.1 -C.sub.4)alkyl; Q.sub.3 is selected from the group consisting of H and (C.sub.1 -C.sub.4)alkyl or Q.sub.1 and Q.sub.3 are attached to form a heterocycle and together represent (C.sub.2 -C.sub.3)alkylene, whereas Z.sub.1 represents a bond, in the form of pure enantiomer or mixture thereof in any proportions as well as its salt with acid.

    摘要翻译： 其中Ar1是萘基和苯基，任选取代的喹啉基或异喹啉的式I化合物（I） Ar 2是任选取代的苯基或噻吩基; R 1，R 2和R'2彼此独立地为H或（C 1 -C 4）烷基或R 1表示键，并且N与Ar 2共价连接，并且任选地R 2和R'2形成双键，或者R 1或R 2为 共价结合Ar2，代表（C1-C3）亚烷基; R3和R4彼此独立地为H或（C1-C4）烷基或与其连接的氮原子形成吡咯烷，哌啶或六氢氮杂; Z1代表（C1-C12）亚烷基，任选被选自（C 5 -C 7）环烷基和苯基的基团或被选自（C 5 -C 7）环烷基和苯基的基团取代的基团间隔; Q1选自甲基，氨基，（C1-C4）烷氧基羰基氨基，（C1-C4）烷基氨基，二（C1-C4） - 烷基氨基，吡咯烷基，哌啶子基，吗啉代，哌嗪基，4-（C1-C4） 烷基脒基，胍基，（C1-C4）烷基胍基，吡啶基，咪唑基，嘧啶基，吲哚基，羟基，（C1-C4）烷氧基，（C2-C8）烷氧基羰基，N- [ C 1 -C 4烷基] -N - [（C 1 -C 4）烷基]氨基，氨基甲酰基，苯基和被选自Cl，F，（C 1 -C 4）烷基，（C 1 -C 4） 烷氧基和羟基; Q2选自H和（C1-C4）烷基; Q3选自H和（C1-C4）烷基或Q1和Q3连接形成杂环，并且一起代表（C 2 -C 3）亚烷基，而Z 1表示以纯对映异构体或混合物形式的键 以及其与酸的盐。

    Heterocyclic derivatives, process for their preparation and their therapeutic use
    8.
    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
    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

    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。