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    1-(1,2-Disubstituted piperidinyl)-4-substituted piperidine derivatives
    1.
    发明授权
    1-(1,2-Disubstituted piperidinyl)-4-substituted piperidine derivatives 失效
    1-（1,2-二取代哌啶基）-4-取代的哌啶衍生物

    公开(公告)号：US06169097A

    公开(公告)日：2001-01-02

    申请号：US09102295

    申请日：1998-06-22

    申请人： Frans Eduard Janssens ,  François Maria Sommen ,  Dominique Louis Nestor Ghislaine Surleraux ,  Yves Emiel Maria Van Roosbroeck

    发明人： Frans Eduard Janssens ,  François Maria Sommen ,  Dominique Louis Nestor Ghislaine Surleraux ,  Yves Emiel Maria Van Roosbroeck

    IPC分类号： A61K31445

    CPC分类号： C07D401/06 ,  C07D211/44 ,  C07D211/46 ,  C07D211/52 ,  C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/10 ,  C07D491/10

    摘要： The present invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 0, 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1; Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent of formula —O—CH2—CH2—O— or —O—CH2—CH2—CH2—O—; R2 is Ar2; Ar2C1-6alkyl; Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; R4 is hydrogen; C1-4alkyl; C1-4aklyloxyC1-4alkyl; hydroxyC1-4alkyl; carboxyl; C1-4aklyloxycarbonyl or Ar3; R5 is hydrogen; hydroxy; Ar3; Ar3C1-6alkyloxy; di(Ar3)C1-6alkyloxy; Ar3C1-6alkylthio; di(Ar3)C1-6alkylthio; Ar3C1-6alkylsulfoxy; di(Ar3)C1-6alkylsulfoxy; Ar3C1-6alkylsulfonyl; di(Ar3)C1-6alkylsulfonyl; —NR7R8; C1-6alkyl substituted with —NR7R8; or a radical of formula (a-1) or (a-2); R4 and R5 may also be taken together; R6 is hydrogen; hydroxy; C1-6alkyloxy; C1-6alkyl or Ar3C1-6alkyl; Ar1, Ar2 and Ar3 are phenyl or substituted phenyl; Ar2 is also naphtalenyl; and Het is an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物形式的化合物，其药学上可接受的加成盐和立体化学异构形式，其中n为0,1或2; m为1或2，条件是如果m为2，则n为1; p为0,1或2; = Q是= O或= NR3; X是共价键或式-O-，-S-，-NR 3 - 的二价基团; R1是Ar1; Ar 1 C 1-6烷基或二（Ar 1）C 1-6烷基，其中每个C 1-6烷基任选被羟基，C 1-4烷氧基，氧代或式-O-CH 2 -CH 2 -O-或-O-CH 2 -CH2-CH2-O-; R2是Ar2; Ar2C1-6烷基; Het或HetC 1-6烷基; R3是氢或C1-6烷基; R4是氢; C 1-4烷基; C 1-4烷氧基C 1-4烷基; 羟基C 1-4烷基; 羧基; C 1-4烷氧基羰基或Ar 3; R5是氢; 羟基; Ar3; Ar 3 C 1-6烷氧基; 二（Ar 3）C 1-6烷氧基; Ar 3 C 1-6烷硫基; 二（Ar 3）C 1-6烷硫基; Ar3C1-6烷基磺酰基; 二（Ar 3）C 1-6烷基亚磺酰基; Ar 3 C 1-6烷基磺酰基; 二（Ar 3）C 1-6烷基磺酰基; -NR7R8; 被-NR 7 R 8取代的C 1-6烷基; 或式（a-1）或（a-2）的基团; R4和R5也可以一起使用; R6是氢; 羟基; C 1-6烷氧基; C 1-6烷基或Ar 3 C 1-6烷基; Ar1，Ar2和Ar3是苯基或

    1-(1,2-disubstituted piperidinyl)-4-substituted piperazine derivatives
    3.
    发明授权
    1-(1,2-disubstituted piperidinyl)-4-substituted piperazine derivatives 有权
    1-（1,2-二取代的哌啶基）-4-取代的哌嗪衍生物

    公开(公告)号：US06521621B1

    公开(公告)日：2003-02-18

    申请号：US09745513

    申请日：2000-12-22

    申请人： Frans Eduard Janssens ,  François Maria Sommen ,  Dominique Louis Nestor Ghislaine Surleraux ,  Joseph Elisabeth Leenaerts ,  Yves Emiel Maria Van Roosbroeck

    发明人： Frans Eduard Janssens ,  François Maria Sommen ,  Dominique Louis Nestor Ghislaine Surleraux ,  Joseph Elisabeth Leenaerts ,  Yves Emiel Maria Van Roosbroeck

    IPC分类号： A61K31496

    CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D405/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  Y02P20/55

    摘要： This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent; R2 is Ar2, Ar2C1-6alkyl, Het1 or Het1C1-6alkyl; R3 is hydrogen or C1-6alkyl; L is hydrogen; Ar3; C1-6alkyl; C1-6alkyl substituted with 1 or 2 substituents selected from hydroxy, C1-6alkyloxy, Ar3, Ar3C1-6alkyloxy and Het2; C3-6alkenyl; Ar3C3-6alkenyl; di(Ar3)C3-6alkenyl or a radical of formula (a-1), (a-2), (a-3), (a-4) or (a-5); Ar1, Ar2 and Ar3 are each phenyl or substituted phenyl; Het1 and Het2 are each monocyclic or a bicyclic heterocycles; as substance-P antagonists; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物形式的化合物，其药学上可接受的加成盐和立体异构形式，其中n为0,1或2; m为1或2，条件是如果m为2，则n为1; p为1或2; = Q是= O或= NR3; X是共价键或式-O-，-S-，-NR 3 - 的二价基团; R 1是Ar 1，Ar 1 C 1-6烷基或二（Ar 1）C 1-6烷基，其中每个C 1-6烷基任选被羟基，C 1-4烷氧基，氧代或缩酮化的取代基取代; R2是Ar2，Ar2C1-6烷基，Het1或Het1C1-6烷基; R3是氢或C1-6烷基; L是氢; Ar3; C 1-6烷基; 被1或2个选自羟基，C 1-6烷氧基，Ar 3，Ar 3 C 1-6烷氧基和Het 2的取代基取代的C 1-6烷基; C 3-6烯基; Ar3C3-6烯基; 二（Ar 3）C 3-6烯基或式（a-1），（a-2），（a-3），（a-4）或（a-5）的基团。 Ar 1，Ar 2和Ar 3分别为苯基或取代的苯基; Het1和Het2分别是单环或双环杂环; 作为物质-P拮抗剂; 其制剂，含有它们的组合物及其作为药物的用途。

    1-(1,2-disubstituted pipeidinyl)-4-substituted piperidine derivatives
    4.
    发明授权
    1-(1,2-disubstituted pipeidinyl)-4-substituted piperidine derivatives 有权
    1-（1,2-二取代的管基）-4-取代的哌啶衍生物

    公开(公告)号：US06346540B1

    公开(公告)日：2002-02-12

    申请号：US09615523

    申请日：2000-07-13

    申请人： Frans Eduard Janssens ,  François Maria Sommen ,  Dominique Louis Nestor Ghislaine Surleraux ,  Yves Emiel Maria Van Roosbroeck

    发明人： Frans Eduard Janssens ,  François Maria Sommen ,  Dominique Louis Nestor Ghislaine Surleraux ,  Yves Emiel Maria Van Roosbroeck

    IPC分类号： A61K31454

    CPC分类号： C07D401/06 ,  C07D211/44 ,  C07D211/46 ,  C07D211/52 ,  C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/10 ,  C07D491/10

    摘要： The present invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 0, 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1; Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent of formula —O—CH2—CH2—O— or —O—CH2—CH2—CH2—O—; R2 is Ar2; Ar2C1-6alkyl; Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; R4 is hydrogen; C1-4alkyl; C1-4alkyloxyC1-4alkyl; hydroxyC1-4alkyl; carboxyl; C1-4alkyloxycarbonyl or Ar3; R5 is hydrogen; hydroxy; Ar3; Ar3C1-6alkyloxy; di(Ar3)C1-6alkyloxy; Ar3C1-6alkylthio; di(Ar3)C1-6alkylthio; Ar3C1-6alkylsulfoxy; di(Ar3)C1-6alkylsulfoxy; Ar3C1-6alkylsulfonyl; di(Ar3)C1-6alkylsulfonyl; —NR7R8; C1-6alkyl substituted with —NR7R8; or a radical of formula (a-1) or (a-2); R4 and R5 may also be taken together; R6 is hydroxy; C1-6alkyloxy; C1-6alkyl or Ar3C1-6alkyl; Ar1, Ar2 and Ar3 are phenyl or substituted phenyl; Ar2 is also naphtalenyl; and Het is an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物形式的化合物，其药学上可接受的加成盐和立体化学异构形式，其中n为0,1或2; m为1或2，条件是如果m为2，则n为1; p为0,1或2; = Q是= O或= NR3; X是共价键或式-O-，-S-，-NR 3 - 的二价基团; R1是Ar1; Ar 1 C 1-6烷基或二（Ar 1）C 1-6烷基，其中每个C 1-6烷基任选被羟基，C 1-4烷氧基，氧代或式-O-CH 2 -CH 2 -O-或-O-CH 2 -CH2-CH2-O-; R2是Ar2; Ar2C1-6烷基; Het或HetC 1-6烷基; R3是氢或C1-6烷基; R4是氢; C 1-4烷基; C 1-4烷氧基C 1-4烷基; 羟基C 1-4烷基; 羧基; C 1-4烷氧基羰基或Ar 3; R5是氢; 羟基; Ar3; Ar 3 C 1-6烷氧基; 二（Ar 3）C 1-6烷氧基; Ar 3 C 1-6烷硫基; 二（Ar 3）C 1-6烷硫基; Ar3C1-6烷基磺酰基; 二（Ar 3）C 1-6烷基亚磺酰基; Ar 3 C 1-6烷基磺酰基; 二（Ar 3）C 1-6烷基磺酰基; -NR7R8; 被-NR 7 R 8取代的C 1-6烷基; 或式（a-1）或（a-2）的基团; R4和R5也可以一起使用; R6是羟基; C 1-6烷氧基; C 1-6烷基或Ar 3 C 1-6烷基; Ar1，Ar2和Ar3是苯基或取代基

    Novel Formulations For Opioid-Based Treatments Of Pain Comprising 1-(1,2-Disubstituted Piperidinyl)-4-Substituted Piperazine Derivatives
    6.
    发明申请
    Novel Formulations For Opioid-Based Treatments Of Pain Comprising 1-(1,2-Disubstituted Piperidinyl)-4-Substituted Piperazine Derivatives 审中-公开
    用于基于阿片样物质治疗包含1-（1,2-二取代的哌啶基）-4-取代的哌嗪衍生物的疼痛的新型制剂

    公开(公告)号：US20080070924A1

    公开(公告)日：2008-03-20

    申请号：US10560482

    申请日：2004-06-07

    申请人： Frans Eduard Janssens ,  Francois Maria Sommen ,  Joseph Elisabeth Leenaerts ,  Yves Emiel Maria Van Roosbroeck ,  Theo Frans Meert

    发明人： Frans Eduard Janssens ,  Francois Maria Sommen ,  Joseph Elisabeth Leenaerts ,  Yves Emiel Maria Van Roosbroeck ,  Theo Frans Meert

    IPC分类号： A61K31/496 ,  A61P25/04

    CPC分类号： A61K31/4468 ,  A61K31/485 ,  A61K31/496 ,  A61K2300/00

    摘要： This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1-(1,2-disubstituted piperidinyl)-4-substituted piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in acute and chronic pain treatments, more in particular in inflammatory, post-operative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NK1-receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression and tolerance in opioid-based treatments of pain.The pharmaceutical formulations according to the invention comprise NK1-antagonists according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.The pharmaceutical composition according to the invention reduces to a large extent a number of unwanted side-effects associated with opioid analgesics, in particular respiratory depression and tolerance, thereby increasing the total tolerability of said opioids in pain treatment.

    摘要翻译： 本发明涉及用于基于阿片样物质治疗疼痛和/或伤害感受的新型制剂，其包含阿片样镇痛药和具有神经激肽拮抗活性的1-（1,2-二取代哌啶基）-4-取代的哌嗪衍生物，特别是NK < 所述制剂用于制备用于预防和/或治疗呕吐，疼痛和/或伤害感受的药物，特别是在急性和慢性疼痛治疗中，特别是在炎性，术后， 急诊室（ER），突破性，神经病理性和癌症疼痛治疗，以及使用NK1受体拮抗剂制备用于预防和/或治疗阿片样物质的呼吸抑制和耐受性的药物 的治疗疼痛。 根据本发明的药物制剂包含根据通式（I）的NK 1 - 拮抗剂，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式和 其中所有取代基如权利要求1中所定义。根据本发明的药物组合物在很大程度上降低了与阿片类镇痛药相关的许多不想要的副作用，特别是呼吸抑制和耐受性，从而增加了 所述阿片类药物在疼痛治疗中。

    1-(1,2-disubstituted piperidinyl)-4 (fused imidazole)-piperidine derivatives
    7.
    发明授权
    1-(1,2-disubstituted piperidinyl)-4 (fused imidazole)-piperidine derivatives 失效
    1-（1,2-二取代的哌啶基）-4（稠合咪唑） - 哌啶衍生物

    公开(公告)号：US06251894B1

    公开(公告)日：2001-06-26

    申请号：US09102136

    申请日：1998-06-22

    申请人： Frans Eduard Janssens ,  Joseph Elisabeth Leenaerts ,  Yves Emiel Maria Van Roosbroeck

    发明人： Frans Eduard Janssens ,  Joseph Elisabeth Leenaerts ,  Yves Emiel Maria Van Roosbroeck

    IPC分类号： A01N4346

    CPC分类号： C07D487/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/14

    摘要： This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; ═Q is ═O or ═NR3; X is a covalent bond or —O—, —S—, —NR3—; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted; R2 is Ar2, Ar2C1-6alkyl, Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; L is a piperidine derivative of formula (a-1) or a spiro piperidine derivative of formula (a-2); Ar1 is phenyl or substituted phenyl; Ar2 is naphtalenyl; phenyl or substituted phenyl; and Het is a monocyclic or bicyclic heterocycle; each monocyclic and bicyclic heterocycle may optionally be substituted on a carbon atom; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物形式的化合物，其药学上可接受的加成盐及其立体化学异构形式，其中n为0,1或2; m为1或2，条件是如果m为2，则n为1; = Q是= O或= NR3; X是共价键或-O - ， - S - ， - NR 3 - ; R 1是Ar 1，Ar 1 C 1-6烷基或二（Ar 1）C 1-6烷基，其中每个C 1-6烷基任选被取代; R2是Ar2，Ar2C1-6烷基，Het或HetC1-6烷基; R3是氢或C1-6烷基; L是式（a-1）的哌啶衍生物或式（a-2）的螺哌啶衍生物; Ar 1是苯基或取代的苯基; Ar2是萘基; 苯基或取代的苯基; Het是单环或双环杂环; 每个单环和双环杂环可任选地在碳原子上取代; 作为P物质拮抗剂; 其制剂，含有它们的组合物及其作为药物的用途。