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    Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication
    11.
    发明授权
    Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication 有权

    公开(公告)号：US07355051B2

    公开(公告)日：2008-04-08

    申请号：US10596519

    申请日：2004-12-20

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

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

    IPC分类号： C07D401/106

    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, Ar2carbonyl, C1−4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1−4alkylcarbonyloxy, Ar2carbonyloxy, 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.

    PIPERIDINE-AMINO-BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    12.
    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
    13.
    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。

    Triazolobenzazepine derivatives
    14.
    发明授权
    Triazolobenzazepine derivatives 失效
    三唑并苯并吖嗪衍生物

    公开(公告)号：US5932569A

    公开(公告)日：1999-08-03

    申请号：US433388

    申请日：1996-05-08

    申请人： Frans Eduard Janssens ,  Jean Fernand Armand Lacrampe ,  Isabelle Noelle Constance Pilatte

    发明人： Frans Eduard Janssens ,  Jean Fernand Armand Lacrampe ,  Isabelle Noelle Constance Pilatte

    IPC分类号： A61K31/55 ,  A61P37/08 ,  C07D487/04 ,  C07D519/00 ,  C07D223/18

    CPC分类号： C07D487/04

    摘要： Antiallergic triazolobenzazepines of formula ##STR1## wherein each of the dotted lines independently represents an optional bond; R.sup.1 represents hydrogen, halo, C.sub.1-4 alkyl, hydroxy or C.sub.1-4 alkyloxy; R.sup.2 represents hydrogen, halo, C.sub.1-4 alkyl, hydroxy or C.sub.1-4 alkyloxy; R.sup.3 represents hydrogen, C.sub.1-4 alkyl or halo; --B.dbd.D-- is a bivalent radical of formula --C(R.sup.4).dbd.N--(a-1); or --N.dbd.C(R.sup.5)-- (a-2); R.sup.4 and R.sup.5 represent hydrogen, C.sub.1-4 alkyl, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl or hydroxycarbonyl; R.sup.5 also represents phenyl or pyridinyl; L represents hydrogen; C.sub.1-6 alkyl; substituted C.sub.1-6 alkyl, C.sub.3-6 alkenyl; C.sub.3-6 alkenyl substituted with aryl or, L represents a radical of formula -Alk-Y-Het.sup.1 (b-1), -Alk-NH--CO--Het.sup.2 (b-2) or --Alk-Het.sup.3 (b-3). Compositions comprising said compounds, processes of preparing the same, and intermediates in the preparation thereof.

    摘要翻译： PCT No.PCT / EP93 / 03320 Sec。 371日期1995年5月8日 102（e）日期1995年5月8日PCT提交1993年11月25日PCT公布。 公开号WO94 / 13671 日期1994年6月23日具有下式的抗变应性三唑并苯并吖嗪：其中每个虚线独立地表示任选的键; R 1表示氢，卤素，C 1-4烷基，羟基或C 1-4烷氧基; R 2表示氢，卤素，C 1-4烷基，羟基或C 1-4烷氧基; R3表示氢，C1-4烷基或卤素; -B = D-是式-C（R4）= N-（a-1）的二价基团; 或-N = C（R5） - （a-2）; R 4和R 5表示氢，C 1-4烷基，被羟基羰基或C 1-4烷氧基羰基取代的乙烯基，被羟基羰基或C 1-4烷氧基羰基取代的C 1-4烷基，羟基C 1-4烷基，甲酰基或羟基羰基; R5也表示苯基或吡啶基; L表示氢; C 1-6烷基; 取代的C 1-6烷基，C 3-6烯基; 由芳基取代的C 3-6链烯基，或L表示式-Alk-Y-Het1（b-1），-Alk-NH-CO-Het2（b-2）或-Alk-Het3（b-3）的基团。 包含所述化合物的组合物，其制备方法以及其制备中的中间体。

    Diaza-spiro--nonane derivatives as neurokinin (nk1) antagonists
    15.
    发明申请
    Diaza-spiro--nonane derivatives as neurokinin (nk1) antagonists 失效
    Diaza-spiro-壬烷衍生物作为神经激肽（nk1）拮抗剂

    公开(公告)号：US20090221641A1

    公开(公告)日：2009-09-03

    申请号：US11886175

    申请日：2006-03-03

    申请人： Frans Eduard Janssens ,  Sophie Coupa ,  Alain Phillippe Poncelet ,  Yvan Rene Ferdinand Simonnet ,  Bruno Schoentjes

    发明人： Frans Eduard Janssens ,  Sophie Coupa ,  Alain Phillippe Poncelet ,  Yvan Rene Ferdinand Simonnet ,  Bruno Schoentjes

    IPC分类号： A61K31/454 ,  C07D401/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P29/00 ,  A61P11/00 ,  A61P11/06

    CPC分类号： C07D487/08

    摘要： This invention concerns substituted diaza-spiro-[4.4]-nonane derivatives having neurokinin antagonistic activity, in particular NK1 antagonist ic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nocicept ion, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also 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.

    摘要翻译： 本发明涉及具有神经激肽拮抗活性的具有神经激肽拮抗活性的取代的二氮杂螺 - [4.4] - 壬烷衍生物，特别是NK1拮抗剂活性，其制备方法，包含它们的组合物及其作为药物的用途，特别是用于治疗和/或预防精神分裂症 呕吐，焦虑和抑郁症，肠易激综合征（IBS），昼夜节律紊乱，先兆子痫，伤痛感染，疼痛，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，慢性阻塞性肺病（COPD）和排尿 疾病如尿失禁。 根据本发明的化合物可以由通式（I）表示，并且还包括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-氧化物形式及其前药，其中所有取代基定义为 在权利要求1中。

    Diaza-spiro-{4,4}-nonane derivatives as neurokinin (NK1) antagonists
    17.
    发明授权
    Diaza-spiro-{4,4}-nonane derivatives as neurokinin (NK1) antagonists 失效
    Diaza-spiro- {4,4} - 壬烷衍生物作为神经激肽（NK1）拮抗剂

    公开(公告)号：US08604200B2

    公开(公告)日：2013-12-10

    申请号：US11886175

    申请日：2006-03-03

    申请人： Frans Eduard Janssens ,  Sophie Coupa ,  Alain Philippe Poncelet ,  Yvan Rene Ferdinand Simonnet ,  Bruno Schoentjes

    发明人： Frans Eduard Janssens ,  Sophie Coupa ,  Alain Philippe Poncelet ,  Yvan Rene Ferdinand Simonnet ,  Bruno Schoentjes

    IPC分类号： C07D215/00 ,  C07D217/00 ,  C07D219/00 ,  C07D221/00 ,  A01N43/42 ,  A61K31/44

    CPC分类号： C07D487/08

    摘要： This invention concerns substituted diaza-spiro-[4.4]-nonane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also 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.

    摘要翻译： 本发明涉及具有神经激肽拮抗活性的具有神经激肽拮抗活性的取代的二氮杂螺 - [4.4] - 壬烷衍生物，特别是NK1拮抗活性，其制备方法，包含它们的组合物及其作为药物的用途，特别是用于治疗和/或预防精神分裂症， 呕吐，焦虑和抑郁，肠易激综合征（IBS），昼夜节律紊乱，先兆子痫，伤害感受，疼痛，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，慢性阻塞性肺病（COPD）和排尿障碍 作为尿失禁。 根据本发明的化合物可以由通式（I）表示，并且还包括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-氧化物形式及其前药，其中所有取代基定义为 在权利要求1中。

    Substituted diaza-spiro-[4.5]-decane derivatives and their use as neurokinin antagonists
    18.
    发明授权
    Substituted diaza-spiro-[4.5]-decane derivatives and their use as neurokinin antagonists 失效
    取代的二氮 - 螺 - [4.5] - 癸烷衍生物及其作为神经激肽拮抗剂的用途

    公开(公告)号：US07612056B2

    公开(公告)日：2009-11-03

    申请号：US11547705

    申请日：2005-04-04

    申请人： Frans Eduard Janssens ,  Bruno Schoentjes ,  Sophie Coupa ,  Alain Philippe Poncelet ,  Yvan René Ferdinand Simonnet

    发明人： Frans Eduard Janssens ,  Bruno Schoentjes ,  Sophie Coupa ,  Alain Philippe Poncelet ,  Yvan René Ferdinand Simonnet

    IPC分类号： A61K31/44

    CPC分类号： C07D471/10

    摘要： This invention concerns substituted diaza-spiro-[4.5]-decane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence.The compounds according to the invention can be represented by general Formula (I) and comprises also 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.

    摘要翻译： 本发明涉及具有神经激肽拮抗活性，特别是NK1拮抗活性，组合NK1 / NK2拮抗活性，组合NK1 / NK3拮抗活性和组合NK1 / NK2 / NK3拮抗活性的取代的二氮 - 螺 - [4.5] - 癸烷衍生物 ，它们的制剂，包含它们的组合物及其作为药物的用途，特别是用于治疗和/或预防精神分裂症，呕吐，焦虑和抑郁，肠易激综合征（IBS），昼夜节律紊乱，先兆子痫，伤害感受，疼痛 ，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，慢性阻塞性肺病（COPD）和排尿障碍如尿失禁。 根据本发明的化合物可以由通式（I）表示，并且还包括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-氧化物形式及其前药，其中所有取代基定义为 在权利要求1中。