利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

70 条记录 (耗时 0.035 秒)

    6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands
    11.
    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。

    6-1H-IMIDAZO-QUINAZOLINE AND QUINOLINES DERIVATIVES, NEW MAO INHIBITORS AND IMIDAZOLINE RECEPTOR LIGANDS
    15.
    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。

    Use of Neboglamine (Cr 2249) as an Antipsychotic and Neuroprotective
    18.
    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。

    Method for the preparation of crystalline dexloxiglumide and products obtained
    19.
    发明申请
    Method for the preparation of crystalline dexloxiglumide and products obtained 失效
    制备结晶脱氧氟沙星和所得产品的方法

    公开(公告)号：US20060154987A1

    公开(公告)日：2006-07-13

    申请号：US10562013

    申请日：2004-06-21

    申请人： Francesco Makovec ,  Lucio Rovati

    发明人： Francesco Makovec ,  Lucio Rovati

    IPC分类号： A61K31/195 ,  C07C231/24

    CPC分类号： C07C237/22

    摘要： The present invention describes a novel method for the purification of dexloxiglumide by crystallization from isopropyl ether which permits the production, in a reproducible manner, of a product with morphological and particle-size characteristics such as to favour its use in the preparation of oral pharmaceutical forms on an industrial scale.

    摘要翻译： 本发明描述了一种通过从异丙醚中结晶来纯化脱氧氟沙星的新方法，其允许以可再现的方式产生具有形态和粒度特征的产物，例如有利于其用于制备口服药物形式 工业规模。

    Oxygenated-alkyl derivatives of glutamic and aspartic acids with antagonistic activity to bio-active polypeptides and a method for their preparation
    20.
    发明授权
    Oxygenated-alkyl derivatives of glutamic and aspartic acids with antagonistic activity to bio-active polypeptides and a method for their preparation 失效
    对生物活性多肽具有拮抗活性的谷氨酸和天冬氨酸的加氧烷基衍生物及其制备方法

    公开(公告)号：US4769389A

    公开(公告)日：1988-09-06

    申请号：US942751

    申请日：1986-12-17

    申请人： Francesco Makovec ,  Rolando Chiste' ,  Lucio Rovati ,  Luigi Rovati

    发明人： Francesco Makovec ,  Rolando Chiste' ,  Lucio Rovati ,  Luigi Rovati

    IPC分类号： A61K31/195 ,  A61P1/00 ,  A61P25/08 ,  C07C233/30 ,  C07C233/45 ,  C07C237/22 ,  C07C103/84

    CPC分类号： A61K31/195 ,  C07C233/30 ,  C07C233/45

    摘要： New Orginal derivates of D,L-glutamic acid and D,L-aspartic acid are described having the formula: ##STR1## where n is 1 or 2, R.sub.1 is a mono- or di-substituted phenyl group substituted with halogens such as chlorine and fluorine or with a methyl group in the 3 and 4 positions and in which R.sub.2 consists of a linear or branched alkyl group with 4 to 7 carbon atoms (preferably a pentyl group) and R.sub.3 is an alkyl group having 3 to 6 carbon atoms overall and containing an oxygen atom in the form of an either linkage, such as for example the groups 2-ethoxyethyl, 3-methoxypropyl, 3-ethoxypropyl etc. or in the form of a hydroxyl group such as for example 3-hydroxypropyl etc.The compounds have antagonistic activity towards bio-active polypeptides and are usable particularly in the treatment of illnesses of the digestive tract, of the central nervous system and anorexia and of all those affections (for example tumours) in which exogenic or endogenic bio-active polypeptides are involved.

    摘要翻译： 描述了具有下式的D，L-谷氨酸和D，L-天冬氨酸的新的原始衍生物：其中n是1或2，R1是被卤素如氯取代的单或二取代的苯基 和氟或在3和4位具有甲基，其中R 2由具有4至7个碳原子的直链或支链烷基（优选戊基）组成，并且R 3是总共具有3至6个碳原子的烷基 并且含有二键形式的氧原子，例如2-乙氧基乙基，3-甲氧基丙基，3-乙氧基丙基等，或以羟基形式例如3-羟基丙基等。 化合物对生物活性多肽具有拮抗活性，并且特别可用于治疗消化道，中枢神经系统和厌食症以及所有这些感染（例如肿瘤）的疾病，其中外源性或内源性生物活性多肽是 涉及。