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    CRYSTALLINE FORMS OF 6-(1H-IMIDAZOL-1-YL)-2-PHENYLQUINAZOLINE
    3.
    发明申请
    CRYSTALLINE FORMS OF 6-(1H-IMIDAZOL-1-YL)-2-PHENYLQUINAZOLINE 有权
    6-（1H-咪唑-1-基）-2-苯基喹唑啉的晶体形式

    公开(公告)号：US20120142713A1

    公开(公告)日：2012-06-07

    申请号：US13375816

    申请日：2010-06-04

    申请人： Antonio Giordani ,  Stefano Mandelli ,  Francesca Porta ,  Matteo Ghirri ,  Lucio Claudio Rovati

    发明人： Antonio Giordani ,  Stefano Mandelli ,  Francesca Porta ,  Matteo Ghirri ,  Lucio Claudio Rovati

    IPC分类号： A61K31/517 ,  A61P29/00 ,  C07D403/10

    CPC分类号： C07D403/04 ,  A01N43/54 ,  A61K31/517

    摘要： The present invention relates to the solid state of 6-(1H-imidazol-1-yl)-2-phenylquinazoline (I) and therefore to novel crystalline forms of the base and of pharmaceutically acceptable salts and solvates thereof, and also to methods for preparing them, to the respective pharmaceutical formulations and to their therapeutic use. Compound (I) may be obtained as the free base in five different crystalline forms, three polymorphic forms and two hydrates. Some pharmaceutically acceptable salts of (I) that have physicochemical characteristics acceptable for pharmaceutical development were obtained, and the respective polymorphic forms and/or hydrates were characterized.

    摘要翻译： 本发明涉及6-（1H-咪唑-1-基）-2-苯基喹唑啉（I）的固态，因此涉及碱的新型结晶形式及其药学上可接受的盐和溶剂合物，以及涉及 制备它们，各自的药物制剂及其治疗用途。 化合物（I）可以以五种不同的晶型，三种多晶型和两种水合物形式获得为游离碱。 获得了具有药物发育可接受的物理化学特性的（I）的一些药学上可接受的盐，并对其各自的多晶型和/或水合物进行了表征。

    Crystalline forms of 6-(1H-imidazol-1-yl)-2-phenylquinazoline
    4.
    发明授权
    Crystalline forms of 6-(1H-imidazol-1-yl)-2-phenylquinazoline 有权
    6-（1H-咪唑-1-基）-2-苯基喹唑啉的结晶形式

    公开(公告)号：US09174966B2

    公开(公告)日：2015-11-03

    申请号：US13375816

    申请日：2010-06-04

    申请人： Antonio Giordani ,  Stefano Mandelli ,  Francesca Porta ,  Matteo Ghirri ,  Lucio Claudio Rovati

    发明人： Antonio Giordani ,  Stefano Mandelli ,  Francesca Porta ,  Matteo Ghirri ,  Lucio Claudio Rovati

    IPC分类号： C07D403/04 ,  A61K31/517 ,  A01N43/54

    CPC分类号： C07D403/04 ,  A01N43/54 ,  A61K31/517

    摘要： The present invention relates to the solid state of 6-(1H-imidazol-1-yl)-2-phenylquinazoline (I) and therefore to novel crystalline forms of the base and of pharmaceutically acceptable salts and solvates thereof, and also to methods for preparing them, to the respective pharmaceutical formulations and to their therapeutic use. Compound (I) may be obtained as the free base in five different crystalline forms, three polymorphic forms and two hydrates. Some pharmaceutically acceptable salts of (I) that have physicochemical characteristics acceptable for pharmaceutical development were obtained, and the respective polymorphic forms and/or hydrates were characterized.

    摘要翻译： 本发明涉及6-（1H-咪唑-1-基）-2-苯基喹唑啉（I）的固态，因此涉及碱的新型结晶形式及其药学上可接受的盐和溶剂合物，以及涉及 制备它们，各自的药物制剂及其治疗用途。 化合物（I）可以以五种不同的晶型，三种多晶型和两种水合物形式获得为游离碱。 获得了具有药物发育可接受的物理化学特性的（I）的一些药学上可接受的盐，并对其各自的多晶型和/或水合物进行了表征。

    6-1H-IMIDAZO-QUINAZOLINE AND QUINOLINES DERIVATIVES, NEW MAO INHIBITORS AND IMIDAZOLINE RECEPTOR LIGANDS
    8.
    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
    10.
    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。