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    Benzamidine derivatives having anti-inflammatory and immunosuppressive activity
    2.
    发明授权
    Benzamidine derivatives having anti-inflammatory and immunosuppressive activity 有权
    具有抗炎和免疫抑制活性的苯甲脒衍生物

    公开(公告)号：US07202277B2

    公开(公告)日：2007-04-10

    申请号：US10467624

    申请日：2002-02-06

    申请人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    IPC分类号： A61K31/17

    CPC分类号： C07D213/40 ,  C07C257/14 ,  C07C279/18 ,  C07C279/36 ,  C07C335/20 ,  C07C2601/14 ,  C07C2603/74 ,  C07D209/14 ,  C07D209/40 ,  C07D277/48

    摘要： Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta position relative to the “-A-NH—” group.

    摘要翻译： 可以由通式（I）表示的化合物如下所示：

    Pyrrole derivatives with angiotensin II antagonist activity
    4.
    发明授权
    Pyrrole derivatives with angiotensin II antagonist activity 有权
    具有血管紧张素II拮抗剂活性的吡咯衍生物

    公开(公告)号：US07906501B2

    公开(公告)日：2011-03-15

    申请号：US11568362

    申请日：2005-04-27

    申请人： Francesco Makovec ,  Roberto Artusi ,  Antonio Giordani ,  Simona Zanzola ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Roberto Artusi ,  Antonio Giordani ,  Simona Zanzola ,  Lucio Claudio Rovati

    IPC分类号： A61K31/41 ,  C07D293/00 ,  C07D257/04 ,  C07D403/10 ,  C07D295/04

    CPC分类号： C07D403/10

    摘要： Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, —COOH, —CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.

    摘要翻译： 可以由下述通式（I）表示的化合物，其中：R 1是独立地选自：CHO，-COOH，-CH 2 OH的基团R 2是氢或直链或支链C 1 -C 6烷基R 3是氢 或选自Cl和Br R4中的卤素基团是直链或支链C 3 -C 5烷基及其药学上可接受的盐，例如钠盐或钾盐。 该化合物显示出有效和选择性的所有拮抗剂活性，并且可用于治疗其中AT1受体的全部或过表达的合成升高可能起主要病理学作用的任何障碍，如在动脉高血压，充血性心功能不全，血小板 与其相关的聚集和紊乱，例如心肌和脑梗死，肾缺血，静脉和动脉血栓形成，外周血管病变，肺动脉高压，糖尿病，糖尿病性神经病，青光眼和糖尿病性视网膜病变。

    Benzamidine derivatives having anti-inflammatory and immunosuppressive activity
    6.
    发明授权
    Benzamidine derivatives having anti-inflammatory and immunosuppressive activity 失效
    具有抗炎和免疫抑制活性的苯甲脒衍生物

    公开(公告)号：US07560591B2

    公开(公告)日：2009-07-14

    申请号：US12112299

    申请日：2008-04-30

    申请人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    IPC分类号： C07C335/16 ,  A61K31/17

    CPC分类号： C07D213/40 ,  C07C257/14 ,  C07C279/18 ,  C07C279/36 ,  C07C335/20 ,  C07C2601/14 ,  C07C2603/74 ,  C07D209/14 ,  C07D209/40 ,  C07D277/48

    摘要： Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta position relative to the “—A—NH—” group.

    摘要翻译： 可以由以下通式（I）表示的化合物：其中：A独立地选自甲酰胺基，硫代羧酰胺基和羰基，R 1选自具有1至3个碳的烷基 原子和氨基，未取代或被硝基或甲基取代，R 2独立地选自氢，具有1至4个碳原子的烷基，甲氧基，乙氧基，丙氧基，单 - ，双 - 或具有5至12个碳原子的三环环烷烃残基，未被取代或被甲基，甲氧基，羟基，氨基或卤素基团取代的金刚烷基，芳基，萘基或杂环基，R3和R4独立地选自氢和烷基 具有1至3个碳原子的基团，R 5表示独立地选自氢和甲基，甲氧基和羟基的一个或两个取代基，n为0至6的整数，并且脒基为t 他相对于“-A-NH-”组的对位或间位。

    Novel Benzamidine Derivatives Having Anti-Inflammatory and Immunosuppressive Activity
    7.
    发明申请
    Novel Benzamidine Derivatives Having Anti-Inflammatory and Immunosuppressive Activity 失效
    具有抗炎和免疫抑制活性的新型苯甲脒衍生物

    公开(公告)号：US20080207764A1

    公开(公告)日：2008-08-28

    申请号：US12112299

    申请日：2008-04-30

    申请人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    IPC分类号： A61K31/155 ,  C07C257/10

    CPC分类号： C07D213/40 ,  C07C257/14 ,  C07C279/18 ,  C07C279/36 ,  C07C335/20 ,  C07C2601/14 ,  C07C2603/74 ,  C07D209/14 ,  C07D209/40 ,  C07D277/48

    摘要： Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta position relative to the “-A-NH-” group.

    摘要翻译： 可以由以下通式（I）表示的化合物：其中：A独立地选自甲酰胺基，硫代羧酰胺基和羰基，R 1选自 具有1至3个碳原子的烷基和未被取代或被硝基或甲基取代的氨基，R 2独立地选自氢，具有1至4个碳的烷基 原子，甲氧基，乙氧基，丙氧基，具有5至12个碳原子的单环，双环或三环环烷烃残基，金刚烷基，芳基，萘基或杂环基，未取代或被甲基，甲氧基，羟基， 氨基或卤素基团，R 3和R 4独立地选自氢和具有1至3个碳原子的烷基，R 5， 代表独立地选自氢和甲基，甲氧基和羟基的一个或两个取代基，n是a 整数为0至6，脒基为相对于“-A-NH-”基的对位或间位。

    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
    9.
    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。