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171 条记录 (耗时 0.018 秒)

    QUINAZOLINE DERIVATIVES
    135.
    发明申请
    QUINAZOLINE DERIVATIVES 审中-公开

    公开(公告)号：US20160207938A1

    公开(公告)日：2016-07-21

    申请号：US15003124

    申请日：2016-01-21

    申请人： Janssen Pharmaceutica NV

    发明人： Eddy Jean Edgard FREYNE ,  Timothy Pietro Suren PERERA ,  Peter Jacobus Johannes Antonius BUIJNSTERS ,  Marc WILLEMS ,  Gaston Stanislas Marcella DIELS ,  Werner Constant Johan EMBRECHTS ,  Peter TEN HOLTE ,  Frederik Jan Rita ROMBOUTS ,  Carsten SCHULTZ-FADEMRECHT

    IPC分类号： C07D498/06 ,  C07C229/40 ,  C07D239/94

    CPC分类号： C07D498/06 ,  C07C229/16 ,  C07C229/40 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94

    摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —O—N═CH— or —C1-2alkyl-; R1 and R2 each independently represents hydrogen or halo; R3 represents hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 each independently represents hydrogen or C1-4alkyl; R14 and R15 represents hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 each independently represent hydrogen or C1-4alkyl optionally substituted with phenyl or hydroxy; R20 and R21 each independently represent hydrogen or C1-4alkyl optionally substituted with C1-4alkyloxy; Het20, Het21 and Het22 each independently represent a heterocycle selected from the group consisting pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted with hydroxy.

    COMPOSITIONS AND METHODS FOR THE TREATMENT OF RESPIRATORY DISORDERS
    137.
    发明申请
    COMPOSITIONS AND METHODS FOR THE TREATMENT OF RESPIRATORY DISORDERS 有权
    用于治疗呼吸道疾病的组合物和方法

    公开(公告)号：US20150133407A1

    公开(公告)日：2015-05-14

    申请号：US14399181

    申请日：2013-05-14

    申请人： Mahesh Kandula

    发明人： Mahesh Kandula

    IPC分类号： C07D473/04 ,  C07D213/66 ,  C07C237/40 ,  C07C237/20 ,  C07D339/04 ,  C07C229/40

    CPC分类号： C07D473/04 ,  A61K47/48038 ,  A61K47/481 ,  A61K47/48107 ,  A61K47/542 ,  A61K47/55 ,  A61K47/551 ,  C07C229/40 ,  C07C237/20 ,  C07C237/40 ,  C07C239/20 ,  C07C275/40 ,  C07C2601/14 ,  C07D213/66 ,  C07D339/04

    摘要： The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of respiratory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of viscid or excessive mucus, cough, inflammation, redness in sore throat, infection in the throat, sore throat, abnormal mucus secretion, impaired mucus transport, allergic rhinitis, asthma, COPD, respiratory muscular disorders and pain in acute sore throat.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，以及其多晶型物，溶剂合物，对映体，立体异构体和水合物。 包含有效量的式I化合物和用于治疗呼吸系统疾病的方法的药物组合物可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射。 这些组合物可用于治疗粘稠或过度粘液，咳嗽，炎症，喉咙发红，咽喉感染，喉咙痛，粘液分泌异常，粘液运输受损，过敏性鼻炎，哮喘，COPD，呼吸肌肉疾病和疼痛 在喉咙痛。

    QUINAZOLINE DERIVATIVES
    139.
    发明申请
    QUINAZOLINE DERIVATIVES 审中-公开
    喹诺酮衍生物

    公开(公告)号：US20130178624A1

    公开(公告)日：2013-07-11

    申请号：US13744878

    申请日：2013-01-18

    申请人： Janssen Pharmaceutica N.V.

    发明人： Eddy Jean Edgard FREYNE ,  Timothy Pietro Suren Perera ,  Peter Jacobus Johannes Antonius Buijnsters ,  Marc Willems ,  Gaston Stanislas Marcella Diels ,  Werner Constant Johan Embrechts ,  Peter Ten Holte ,  Frederik Jan Rita Rombouts ,  Carsten Schultz-Fademrecht

    IPC分类号： C07D239/94 ,  C07C229/40 ,  C07C229/16

    CPC分类号： C07D498/06 ,  C07C229/16 ,  C07C229/40 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94

    摘要： The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl, —O—N═CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-4alkyl optionally substituted with phenyl or hydroxy; R20 and R21 are hydrogen or C1-4alkyl optionally substituted with C1-4alkyloxy; Het20, Het21 and Het22 are a heterocycle selected from the group consisting pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted with hydroxy.

    摘要翻译： 本发明涉及下式的化合物其中Z代表NH; Y代表任选被氨基，一或二（C 1-4烷基）氨基或C 1-4烷氧基羰基氨基 - ， - C 3-7烯基-CO-的氨基取代的-C 3-9烷基 - ， - C 2-9烯基 - ， - 氨基，一或二（C 1-4烷基）氨基 - 或C 1-4烷氧基羰基氨基 - ，C 1-5烷基-NR 13 -C 1-5烷基 - ， - C 1-5烷基-NR 14 -CO-C 1-5烷基 - C 1-6烷基-CO-NH - ， - C 1-5烷基-CO NR 15 -C 1-5烷基 - ， - C 1-3烷基-NH-CO-Het 20 - ， - C 1-2烷基-CO-Het 21 -CO-， - C 1-2烷基 -NH-CO-CR16R17-NH-，-C1-2烷基-CO-NH-CR18R19-CO-，-C1-2烷基-CO-NR20-C1-3烷基-CO-或-NR22-CO-C1-3烷基 - NH-; X1表示直接键，O或-O-C 1-2烷基 - ; X 2代表直接键，-CO-C 1-2烷基 - ，NR 12，-NR 12 -C 1-2烷基，-O-N = CH-或-C 1-2烷基 - ; R1和R2是氢或卤素; R3是氢; R4表示氢或C1-4烷氧基; R 12和R 13是氢或C 1-4烷基; R14和R15是氢; R 16和R 17各自独立地表示氢或C 1-4烷基; R 18和R 19是氢或任选被苯基或羟基取代的C 1-4烷基; R 20和R 21是氢或任选被C 1-4烷氧基取代的C 1-4烷基; Het20，Het21和Het22是选自吡咯烷基，2-吡咯烷基或任选被羟基取代的哌啶基的杂环。