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    6-1H-IMIDAZO-QUINAZOLINE AND QUINOLINES DERIVATIVES, NEW MAO INHIBITORS AND IMIDAZOLINE RECEPTOR LIGANDS
    1.
    发明申请
    6-1H-IMIDAZO-QUINAZOLINE AND QUINOLINES DERIVATIVES, NEW MAO INHIBITORS AND IMIDAZOLINE RECEPTOR LIGANDS 有权
    6-1H-咪唑 - 喹唑啉和喹啉衍生物，新的MAO抑制剂和咪唑啉受体配体

    公开(公告)号：US20110118289A1

    公开(公告)日：2011-05-19

    申请号：US12999862

    申请日：2008-06-20

    申请人： Antonio Giordani ,  Marco Lanza ,  Gianfranco Caselli ,  Stefano Mandelli ,  Simona Zanzola ,  Francesco Makovec ,  Lucio Claudio Rovati

    发明人： Antonio Giordani ,  Marco Lanza ,  Gianfranco Caselli ,  Stefano Mandelli ,  Simona Zanzola ,  Francesco Makovec ,  Lucio Claudio Rovati

    IPC分类号： A61K31/517 ,  C07D401/10 ,  A61K31/4709 ,  C07D405/14 ,  C07D403/10 ,  A61P25/36

    CPC分类号： A61K31/517 ,  A61K31/4178 ,  A61K31/485 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  A61K2300/00

    摘要： The present invention is directed to 6-(1H-imidazo-1-yl)-2-aryl and 2-heteroaryl quinazoline and quinolines derivatives, compounds of formula (I), their pharmaceutical acceptable salts and solvates and corresponding pharmaceutical compositions, that acts as Monoamine Oxidase (MAO) inhibitors and Imidazoline Receptor ligands: wherein: X is independently selected from —CH group or a nitrogen atom (—N), W is independently selected from an aryl group, an heteroaryl group, or a benzocondensed heteroaryl group such as 1,3-benzodioxole, benzofuran, 2,3-dihydrobenzofuran, benzothiophene, 2,3-dihydrobenzothiophene, indole, 2,3-dihydroindole, benzimidazole, benzoxazole, benzothiazole, 2H-3,4-dihydrobenzopyran, [1,4]-benzodioxine, 2,3-dihydro-[1,4]-benzodioxine (1,4-benzodioxan). R1 is independently selected from hydrogen (—H), C1-C4 alkyl, hydroxymethyl (—CH2OH), aminomethyl (—CH2NH2), alkylaminomethyl [CH2NH(R2)], or di-alkylaminomethyl [CH2N(R2)2], trifluoromethyl (—CF3).Compounds of formula (I) elicited a pharmacological profile suitable for the clinical treatment of depression and related disorders, Parkinson disease, drug abuse, and morphine tolerance and dependence.

    摘要翻译： 本发明涉及6-（1H-咪唑-1-基）-2-芳基和2-杂芳基喹唑啉和喹啉衍生物，式（I）化合物，其药学上可接受的盐和溶剂化物以及相应的药物组合物，其作用 作为单胺氧化酶（MAO）抑制剂和咪唑啉受体配体：其中：X独立地选自-CH基或氮原子（-N），W独立地选自芳基，杂芳基或苯并稠合的杂芳基，例如 作为1,3-苯并间二氧杂环戊烯，苯并呋喃，2,3-二氢苯并呋喃，苯并噻吩，2,3-二氢苯并噻吩，吲哚，2,3-二氢吲哚，苯并咪唑，苯并恶唑，苯并噻唑，2H-3,4-二氢苯并吡喃，[1,4] 苯并二恶英，2,3-二氢 - [1,4] - 苯并二恶英（1,4-苯并二恶烷）。 R 1独立地选自氢（-H），C 1 -C 4烷基，羟甲基（-CH 2 OH），氨基甲基（-CH 2 NH 2），烷基氨基甲基[CH 2 NH（R 2）]或二烷基氨基甲基[ -CF 3）。 式（I）化合物引发适于临床治疗抑郁症和相关疾病，帕金森病，药物滥用和吗啡耐受性和依赖性的药理学特征。

    6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands
    2.
    发明授权
    6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands 有权
    6-1H-咪唑并喹唑啉和喹啉衍生物，新的MAO抑制剂和咪唑啉受体配体

    公开(公告)号：US08633208B2

    公开(公告)日：2014-01-21

    申请号：US12999862

    申请日：2008-06-20

    申请人： Antonio Giordani ,  Marco Lanza ,  Gianfranco Caselli ,  Stefano Mandelli ,  Simona Zanzola ,  Francesco Makovec ,  Lucio Claudio Rovati

    发明人： Antonio Giordani ,  Marco Lanza ,  Gianfranco Caselli ,  Stefano Mandelli ,  Simona Zanzola ,  Francesco Makovec ,  Lucio Claudio Rovati

    IPC分类号： A01N43/54 ,  A01N43/42 ,  A61K31/517 ,  A61K31/44 ,  C07D239/72 ,  C07D401/00 ,  C07D403/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D233/00

    CPC分类号： A61K31/517 ,  A61K31/4178 ,  A61K31/485 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  A61K2300/00

    摘要： The present invention is directed to 6-(1H-imidazo-1-yl)-2-aryl and 2-heteroaryl quinazoline and quinolines derivatives, compounds of formula (I), their pharmaceutical acceptable salts and solvates and corresponding pharmaceutical compositions, that acts as Monoamine Oxidase (MAO) inhibitors and Imidazoline Receptor ligands: wherein: X is independently selected from —CH group or a nitrogen atom (—N), W is independently selected from an aryl group, an heteroaryl group, or a benzocondensed heteroaryl group such as 1,3-benzodioxole, benzofuran, 2,3-dihydrobenzofuran, benzothiophene, 2,3-dihydrobenzothiophene, indole, 2,3-dihydroindole, benzimidazole, benzoxazole, benzothiazole, 2H-3,4-dihydrobenzopyran, [1,4]-benzodioxine, 2,3-dihydro-[1,4]-benzodioxine (1,4-benzodioxan). R1 is independently selected from hydrogen (—H), C1-C4 alkyl, hydroxymethyl (—CH2OH), aminomethyl (—CH2NH2), alkylaminomethyl [CH2NH(R2)], or di-alkylaminomethyl [CH2N(R2)2], trifluoromethyl (—CF3). Compounds of formula (I) elicited a pharmacological profile suitable for the clinical treatment of depression and related disorders, Parkinson disease, drug abuse, and morphine tolerance and dependence.

    摘要翻译： 本发明涉及6-（1H-咪唑-1-基）-2-芳基和2-杂芳基喹唑啉和喹啉衍生物，式（I）化合物，其药学上可接受的盐和溶剂化物以及相应的药物组合物，其作用 作为单胺氧化酶（MAO）抑制剂和咪唑啉受体配体：其中：X独立地选自-CH基或氮原子（-N），W独立地选自芳基，杂芳基或苯并稠合的杂芳基，例如 作为1,3-苯并间二氧杂环戊烯，苯并呋喃，2,3-二氢苯并呋喃，苯并噻吩，2,3-二氢苯并噻吩，吲哚，2,3-二氢吲哚，苯并咪唑，苯并恶唑，苯并噻唑，2H-3,4-二氢苯并吡喃，[1,4] 苯并二恶英，2,3-二氢 - [1,4] - 苯并二恶英（1,4-苯并二恶烷）。 R 1独立地选自氢（-H），C 1 -C 4烷基，羟甲基（-CH 2 OH），氨基甲基（-CH 2 NH 2），烷基氨基甲基[CH 2 NH（R 2）]或二烷基氨基甲基[ -CF 3）。 式（I）化合物引发适于临床治疗抑郁症和相关疾病，帕金森病，药物滥用和吗啡耐受性和依赖性的药理学特征。