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    PIPERIDINE-AMINO-BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    2.
    发明申请
    PIPERIDINE-AMINO-BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开

    公开(公告)号：US20080146613A1

    公开(公告)日：2008-06-19

    申请号：US12030483

    申请日：2008-02-13

    申请人： Jean-Francois BONFANTI ,  Koenraad Jozef Lodewikjk Andries ,  Frans Eduard Janssens ,  Francois Maria Sommen ,  Jerome Emile Georges Guillemont ,  Jean Fernand Armand Lacrampe

    发明人： Jean-Francois BONFANTI ,  Koenraad Jozef Lodewikjk Andries ,  Frans Eduard Janssens ,  Francois Maria Sommen ,  Jerome Emile Georges Guillemont ,  Jean Fernand Armand Lacrampe

    IPC分类号： A61K31/4545 ,  A61P31/12

    CPC分类号： C07D401/14 ,  C07D417/14

    摘要： The present invention concerns piperidine-amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is C1-6alkyl optionally substituted with trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4alkyl-carbonyl, Ar2-carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2-carbonyloxy, Ar2(CH2)ncarbonyloxy, C1-4alkoxy-carbonyl(CH2)noxy, mono- or di(C1-4alkyl)aminocarbonyl, mono- or di(C1-4alkyl)-aminocarbonyloxy, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl or a heterocycles selected from the group consisting of pyrrolidinyl, pyrrolyl, dihydropyrrolyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, pyridyl and tetrahydropyridyl, wherein each of said heterocycle may optionally be substituted with oxo or C1-6alkyl; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R3a is C1-6alkyl and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen or C1-6alkyl, and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen or C1-6alkyl, and R2b is hydrogen; t is 1, 2 or 3; Ar1 is phenyl or substituted phenyl; and Ar2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.

    AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    5.
    发明申请
    AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
    氨基苯并咪唑衍生物作为呼吸道同发病毒复制的抑制剂

    公开(公告)号：US20090036466A1

    公开(公告)日：2009-02-05

    申请号：US10596500

    申请日：2004-12-20

    申请人： Jean-Francois Bonfanti ,  Koenraad Jozef Lodewijk Andries ,  Frans Eduard Janssens ,  Francois Maria Sommen ,  Jerome Emile Georges Guillemont ,  Jean Fernand Armand Lacrampe

    发明人： Jean-Francois Bonfanti ,  Koenraad Jozef Lodewijk Andries ,  Frans Eduard Janssens ,  Francois Maria Sommen ,  Jerome Emile Georges Guillemont ,  Jean Fernand Armand Lacrampe

    IPC分类号： A61K31/496 ,  C07D401/02 ,  A61K31/4439 ,  C07D401/14 ,  A61P31/12 ,  A61K31/4545 ,  C07D403/14

    CPC分类号： C07D405/14 ,  C07D401/06 ,  C07D401/14

    摘要： The present invention concerns amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is Ar1 or C1-6alkyl substituted with one or more substituents selected from trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4alkylcarbonyl, Ar2-carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2-carbonyloxy, Ar2(CH2)ncarbonyloxy, hydroxy-C2-4-alkyloxy, C1-4alkoxycarbonyl(CH2)noxy, mono- or di(C1-4alkyl)-aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyloxy, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, dioxolanyl optionally substituted with one or two C1-6alkyl radicals, and a heterocycle selected from pyrrolidinyl, pyrrolyl, dihydropyrrolyl, thiazolidinyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, pyridyl and tetrahydropyridyl, which each may optionally be substituted with oxo or C1-6alkyl; G is a direct bond or optionally substituted C1-10alkanediyl R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R3a is C1-6alkyl and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen or C1-6alkyl, and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen or C1-6alkyl, and R2b is hydrogen; Ar1 is phenyl or substituted phenyl and Ar2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.

    摘要翻译： 本发明涉及对呼吸道合胞病毒复制具有抑制活性的氨基苯并咪唑，其具有其前药，N-氧化物，加成盐，季胺，金属络合物和立体化学异构体形式，其中Q为Ar 1或C 1-6烷基取代 具有一个或多个选自三氟甲基，C 3-7环烷基，Ar 2，羟基，C 1-4烷氧基，C 1-4烷硫基，Ar 2 - 氧基 - ，Ar 2 - 硫基 - ，Ar 2（CH 2）n羟基，Ar 2（CH 2）n硫基，羟基羰基，氨基羰基 ，C 1-4烷基羰基，Ar 2 - 羰基，C 1-4烷氧基羰基，Ar 2（CH 2）n羰基，氨基羰基氧基，C 1-4烷基羰基氧基，Ar 2 - 羰基氧基，Ar 2（CH 2）n - 羰基氧基，羟基-C 2-4 4-烷氧基，C 1-4烷氧基羰基（CH 2） 一或二（C 1-4烷基） - 氨基羰基，一或二（C 1-4烷基）氨基羰基氧基，氨基磺酰基，一或二（C 1-4烷基）氨基磺酰基，任选被一个或两个C 1-6烷基取代的二氧戊环基， 选自吡咯烷基，吡咯基，二氢吡咯基，噻唑烷基的杂环 ，咪唑基，三唑基，哌啶基，高哌啶基，哌嗪基，吡啶基和四氢吡啶基，其各自可以任选被氧代或C 1-6烷基取代; G是直接键或任选取代的C 1-10烷二基R 1是Ar 1或单环或双环杂环; R2a和R3a之一是C1-6烷基，R2a和R3a中的另一个是氢; 在R2a不同于氢的情况下，则R2b为氢或C1-6烷基，R3b为氢; 在R3a不同于氢的情况下，R 3b是氢或C 1-6烷基，R 2b是氢; Ar 1是苯基或取代的苯基，Ar 2是苯基或取代的苯基。 它还涉及它们的制备方法和包含它们的组合物，以及它们作为药物的用途。

    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。

    Fused imidazole derivatives as multidrug resistance modulators
    7.
    发明授权
    Fused imidazole derivatives as multidrug resistance modulators 失效
    熔融咪唑衍生物作为多药耐药调节剂

    公开(公告)号：US06476018B1

    公开(公告)日：2002-11-05

    申请号：US09775524

    申请日：2001-02-02

    申请人： Frans Eduard Janssens ,  Joseph Elisabeth Leenaerts ,  Francois Maria Sommen ,  Dominique Louis Nestor Ghislaine Surleraux

    发明人： Frans Eduard Janssens ,  Joseph Elisabeth Leenaerts ,  Francois Maria Sommen ,  Dominique Louis Nestor Ghislaine Surleraux

    IPC分类号： A61K31437

    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 the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula —X—COOR5, —X—CONR6R7 or —X—COR10 wherein —X— is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is —CH2—, —CH2—CH2—, —CH═CH—, —CHOH—CH2—, —O—CH2—, —C(═O)—CH2— or —C(═NOH)—CH2—; —A—B— is a bivalent radical; A1 is a direct bond, optionally substituted C1-6alkanediyl, C1-6alkanediyl-oxy-C1-6alkanediyl, carbonyl, C1-6alkanediylcarbonyl, optionally substituted C1-6alkanediyloxy; A2 is a direct bond or C1-6alkanediyl; and Q is aryl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for inhibiting or reversing the effects of multidrug resistance.

    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，其中虚线是任选的键; n为1或2; R1是氢; 光环; 甲酰基 任选被羟基，C 1-4烷氧基，C 1-4烷基羰基氧基，咪唑基，噻唑基或恶唑基取代的C 1-4烷基; 或式-X-COOR5，-X-CONR6R7或-X-COR10基团，其中-X-是直接键，C1-4烷二基或C2-6亚烯基; R 5是氢，C 1-12烷基，Ar，Het，被C 1-4烷氧基，芳基或杂芳基取代的C 1-6烷基; R6和R7各自独立地为氢或C1-4烷基; R 2是氢，卤素，C 1-4烷基，羟基C 1-4烷基，C 1-4烷氧基羰基，羧基，甲酰基或苯基; R3是氢，C1-4烷基或C1-4烷氧基; R 4是氢，卤素，C 1-4烷基，C 1-4烷氧基或卤代C 1-4烷基; Z是-CH 2 - ， - CH 2 -CH 2 - ， - CH = CH-，-CHOH-CH 2 - ， - O-CH 2 - ， - C（= O）-CH 2 - 或-C（= NOH） -A-B-是二价基团; A1是直接键，任选取代的C 1-6烷二基，C 1-6烷二基 - 氧基-C 1-6烷二基，羰基，C 1-6烷二基羰基，任选取代的C 1-6烷二基氧基; A2是直接键或C1-6烷二基; Q为芳基。 公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于抑制或逆转多药耐药性的作用。