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    SPIRO AMINIC COMPOUNDS WITH NK1 ANTAGONIST ACTIVITY
    2.
    发明申请
    SPIRO AMINIC COMPOUNDS WITH NK1 ANTAGONIST ACTIVITY 审中-公开
    具有NK1拮抗剂活性的SPIRO氨基化合物

    公开(公告)号：US20130310400A1

    公开(公告)日：2013-11-21

    申请号：US13982035

    申请日：2012-02-02

    申请人： Luigi Piero Stasi ,  Lucio Rovati

    发明人： Luigi Piero Stasi ,  Lucio Rovati

    IPC分类号： C07D401/14

    CPC分类号： A61K31/506 ,  A61K31/444 ,  C07D401/12 ,  C07D401/14

    摘要： The invention concerns a spiro-amino compound of Formula (I), wherein A is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring containing 1 to 3 nitrogen atom; X is a substituent selected from the group consisting of (C1-C3)alkyl and halogen, Y is a substituent selected from the group consisting of halogen and trifluoromethyl or a pharmaceutically acceptable salt thereof for use in the treatment of pathologies which require an antagonist of the NK1 receptor.

    摘要翻译： 本发明涉及式（I）的螺 - 氨基化合物，其中A选自5或6元芳环和含有1至3个氮原子的5或6元杂芳环; X是选自（C 1 -C 3）烷基和卤素的取代基，Y是选自卤素和三氟甲基的取代基或其药学上可接受的盐，其用于治疗需要拮抗剂 NK1受体。

    Use of Neboglamine (Cr 2249) as an Antipsychotic and Neuroprotective
    5.
    发明申请
    Use of Neboglamine (Cr 2249) as an Antipsychotic and Neuroprotective 失效
    使用神经酰胺（Cr 2249）作为抗精神病药和神经保护剂

    公开(公告)号：US20070249715A1

    公开(公告)日：2007-10-25

    申请号：US11569545

    申请日：2005-05-23

    申请人： Francesco Makovec ,  Lucio Rovati

    发明人： Francesco Makovec ,  Lucio Rovati

    IPC分类号： A61K31/195 ,  A61P25/18

    CPC分类号： A61K31/196 ,  A61K31/13

    摘要： Use of neboglamine, (S)-4-amino-N-(4,4-dimethylcyclohexyl)glutamic acid (CR 2249) (CAS Registry Number 163000-63-3), of the racemate thereof or of a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment of schizophrenia.

    摘要翻译： 在其外消旋物或其药学上可接受的盐中使用神经酰胺，（S）-4-氨基-N-（4,4-二甲基环己基）谷氨酸（CR 2249）（CAS登记号163000-63-3） 制备用于治疗精神分裂症的药物。

    CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR AGONISTS
    6.
    发明申请
    CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR AGONISTS 有权
    循环胺衍生物作为EP4受体激动剂

    公开(公告)号：US20140243373A1

    公开(公告)日：2014-08-28

    申请号：US14127474

    申请日：2011-07-04

    申请人： Manuela Borriello ,  Sabrina Pucci ,  Luigi Piero Stasi ,  Lucio Rovati

    发明人： Manuela Borriello ,  Sabrina Pucci ,  Luigi Piero Stasi ,  Lucio Rovati

    IPC分类号： C07F1/02

    CPC分类号： C07F1/02 ,  C07D207/16 ,  C07D211/60

    摘要： There is described a group of novel cyclic amine derivative compounds having an EP4 receptor agonistic activity.Specifically, the compounds according to the invention are provided with analgesic, antinflammatory, antiglaucoma activity, and also with anti-osteoporosis and antiulcerative activity.The present invention therefore relates to novel cyclic amine derivative compounds, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as pain, glaucoma, ulcerative colitis and osteoporosis.

    摘要翻译： 描述了一组具有EP4受体激动活性的新型环胺衍生物化合物。 具体地说，根据本发明的化合物具有镇痛，抗炎，抗青光眼活性，并具有抗骨质疏松和抗溃疡活性。 因此，本发明涉及新型环胺衍生物化合物，其制备方法，含有它们的药物组合物及其作为药物的用途，特别是用于治疗或缓解前列腺素E介导的疾病如疼痛，青光眼，溃疡性结肠炎和骨质疏松症。

    Use of neboglamine in the treatment of toxicodependency
    8.
    发明申请
    Use of neboglamine in the treatment of toxicodependency 失效
    使用奈格列胺治疗毒性依赖性

    公开(公告)号：US20110288173A1

    公开(公告)日：2011-11-24

    申请号：US13192071

    申请日：2011-07-27

    申请人： Francesco MAKOVEC ,  Gianfranco CASELLI ,  Lucio Claudio ROVATI ,  Antonio GIORDANI

    发明人： Francesco MAKOVEC ,  Gianfranco CASELLI ,  Lucio Claudio ROVATI ,  Antonio GIORDANI

    IPC分类号： A61K31/195 ,  A61P25/36 ,  A61P25/30

    CPC分类号： A61K31/16

    摘要： Use of neboglamine, (S)-4-amino-N(4,4-dimethyl-cyclohexyl)glutamic acid (CR 2249) (CAS Registry Number 163000-63-3), the racemic mixture thereof or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in the treatment of toxicodependency induced by drugs such as CNS sedatives such as opiates, barbiturates, benzodiazepines, alcohol, stimulants such as amphetamines and cocaine, and hallucinogens such as LSD, mescalin, cannabis (marijuana) or fencyclidine.

    摘要翻译： 使用奈格列胺，（S）-4-氨基-N-（4,4-二甲基 - 环己基）谷氨酸（CR 2249）（CAS登记号163000-63-3），其外消旋混合物或其药学上可接受的盐， 用于制备用于治疗由诸如阿片类药物，巴比妥类，苯并二氮杂类，酒精，兴奋剂如苯丙胺和可卡因的CNS镇静剂等药物诱导的毒性依赖性药物，以及迷幻药如LSD，mescalin，大麻（大麻）或 芬太尼

    6-1H-IMIDAZO-QUINAZOLINE AND QUINOLINES DERIVATIVES, NEW MAO INHIBITORS AND IMIDAZOLINE RECEPTOR LIGANDS
    9.
    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。