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    Heterocyclic derivatives, process for their preparation and their therapeutic use
    4.
    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
    5.
    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。

    Compounds bearing sulphamoyl and amidino radicals, their preparation process and pharmaceutical compositions containing them
    7.
    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：US5714497A

    公开(公告)日：1998-02-03

    申请号：US478604

    申请日：1995-06-07

    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： A61K38/00 ,  C07K5/065 ,  C07K5/078 ,  A61K43/38 ,  C07D215/36 ,  C07D217/22 ,  C07D409/12 ,  A61K43/10

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

    摘要： The subject of the invention is the compounds of formula I ##STR1## in which Ar.sub.1 represents naphtyl, phenyl, quinolyl or isoquinolyl optionally substituted; Ar.sub.2 represents a 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; R.sub.1 represents nothing and N is attached 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 attached to Ar.sub.2 and represents a (C.sub.1 -C.sub.3)alkylene; R.sub.3 and R.sub.4, which are identical or different, represent H, (C.sub.1 -C.sub.4)alkyl or form, with the nitrogen atom to which they are attached, a (C.sub.5 -C.sub.7) saturated heterocycle selected from pyrrolidine, piperidine and hexahydroazepine; Z.sub.1 represents a (C.sub.1 -C.sub.12)alkylene, optionally interrupted or extended by a (C.sub.5 -C.sub.7)cycloalkyl or phenyl.

    摘要翻译： 本发明的主题是其中Ar 1表示任选取代的萘基，苯基，喹啉基或异喹啉的式I化合物（I） Ar2表示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; R1不表示，N与Ar2连接，任选地R 2和R'2形成双键; 或者R 1或R 2与Ar 2相连，表示（C1-C3）亚烷基; R3和R4相同或不同，代表H，（C1-C4）烷基或与其连接的氮原子一起形成选自吡咯烷，哌啶和六氢氮杂的（C5-C7）饱和杂环; Z1表示（C 1 -C 12）亚烷基，任选地被（C 5 -C 7）环烷基或苯基中断或延伸。