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    N-imidazolyl derivatives of substituted alkoxyimino tetrahydronaphthalenes and chromans having antithromboxane A.sub.2 activity
    1.
    发明授权
    N-imidazolyl derivatives of substituted alkoxyimino tetrahydronaphthalenes and chromans having antithromboxane A.sub.2 activity 失效
    取代的烷氧基亚氨基四氢萘酮的N-咪唑衍生物和具有抗恶唑酮A2活性的色素

    公开(公告)号：US5246956A

    公开(公告)日：1993-09-21

    申请号：US830876

    申请日：1992-02-04

    申请人： Paolo Cozzi ,  Antonio Giordani ,  Arsenia Rossi ,  Patricia Salvati ,  Corrado Ferti

    发明人： Paolo Cozzi ,  Antonio Giordani ,  Arsenia Rossi ,  Patricia Salvati ,  Corrado Ferti

    IPC分类号： A61K31/415 ,  A61K31/353 ,  A61K31/366 ,  A61K31/4178 ,  A61K31/695 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  A61P43/00 ,  C07D233/54 ,  C07D233/61 ,  C07D405/06 ,  C07D409/14 ,  C07D521/00 ,  C07F7/08

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The invention provides new imidazole containing alkoxyimino derivatives of tetrahydronaphthalene and chroman of general formula (I) ##STR1## wherein Z is --CH.sub.2 --or--O--;m is an integer of 1 to 4;n is zero of 1;T is a straight or branched saturated C.sub.1 -C.sub.6 hydrocarbon chain or C.sub.2 -C.sub.5 alkenylene chain;A is a bond or a divalent group consisting of --Si(R'R")--; --O--CH.sub.2 --,--CF.sub.2 --,C(R'R")--,vinylene or isopropenylene, wherein each of R' and R" being the same or different is hydrogen or C.sub.1 -C.sub.4 alkyl;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, being the same, are hydrogen or methyl, or one of R.sub.1 and R.sub.2 is hydrogen and the other isa) a C.sub.1 -C.sub.8 alkyl group;b) a C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkyl-C.sub.1 C.sub.4 alkyl group, wherein the cycloalkyl group or moiety is unsubstituted or substituted by 1 to 4 C.sub.1 -C.sub.4 alkyl groups; orc) an aryl or aryl-C.sub.1 -C.sub.4 alkyl group, wherein the aryl group or the aryl moiety is unsubstituted or substituted by 1 to 4 substituents independently chosen from halogen, hydroxy, C.sub.1 -C.sub.4 alkyl, trihalo-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio and C.sub.1 -C.sub.4 alkylsulfonyl;R.sub.3 is hydrogen or a substituent chosen from halogen, hydroxy, C.sub.1 -C.sub.4 alkyl, trihalo-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio and C.sub.1 -C.sub.4 alkylsulfonyl;R.sub.4 is an --OR.sub.5 or --N(R.sub.5 R.sub.6) group, wherein each of R.sub.5 and R.sub.6 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl;and the pharmaceutically acceptable salts thereof, which are useful in the treatment of a disease state in which an enhancement of TxA.sub.2 synthesis exerts a pathogenic effect.

    2-(imidazol-1-yl)-2-benzylethyldiene-aminoxyalkanoic acid derivatives
    2.
    发明授权
    2-(imidazol-1-yl)-2-benzylethyldiene-aminoxyalkanoic acid derivatives 失效
    2-（咪唑-1-基）-2-苯基乙基二烯 - 氨基亚氨基酸衍生物

    公开(公告)号：US5283254A

    公开(公告)日：1994-02-01

    申请号：US917245

    申请日：1992-07-22

    申请人： Paolo Cozzi ,  Maria Menichincheri ,  Arsenia Rossi ,  Corrado Ferti ,  Patricia Salvati

    发明人： Paolo Cozzi ,  Maria Menichincheri ,  Arsenia Rossi ,  Corrado Ferti ,  Patricia Salvati

    IPC分类号： A61K31/415 ,  A61P3/06 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D233/61 ,  C07D233/64 ,  C07D521/00 ,  C07D233/60

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The present invention relates to 2-(imidazol-1-yl)-2 -benzylethylidene-aminoxyalkanoic acid derivatives of formula (I) ##STR1## wherein A is a divalent group of formula ##STR2## in which R is hydrogen, halogen, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylsulfonyl or cyano;R.sub.1 is a) phenyl unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy, CF.sub.3 or C.sub.1 -C.sub.4 alkylsulfonyl; b) cyclohexyl; or c) a straight or branched C.sub.1 -C.sub.6 alkyl group;T is a branched or straight C.sub.3 -C.sub.5 alkylene chain;R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl, and the pharmaceutically acceptable salts thereof, which are useful as selective inhibitors of thromboxane A.sub.2 (TxA.sub.2) synthesis.

    摘要翻译： 本发明涉及式（I）的2-（咪唑-1-基）-2-苯并亚乙基 - 氨基亚油酸衍生物（*化学结构*）（I）其中A是式（*化学结构*）的二价基团， 其中R是氢，卤素，CF 3，C 1 -C 4烷氧基，C 1 -C 4烷基磺酰基或氰基; R 1是a）未被取代或被卤素，C 1 -C 4烷氧基，CF 3或C 1 -C 4烷基磺酰基取代的苯基; b）环己基; 或c）直链或支链的C 1 -C 6烷基; T是支链或直链C 3 -C 5亚烷基链; R2是氢或C1-C4烷基及其药学上可接受的盐，其可用作血栓烷A2（TxA2）合成的选择性抑制剂。

    Substituted 1-(alkoxy-iminoalkyl) imidazole derivatives and their use in treating disease related to an enhancement of thromboxane-A.sub.2 syntheis
    3.
    发明授权
    Substituted 1-(alkoxy-iminoalkyl) imidazole derivatives and their use in treating disease related to an enhancement of thromboxane-A.sub.2 syntheis 失效
    取代的1-（烷氧基 - 亚氨基烷基）咪唑衍生物及其在治疗与凝血恶烷-A2合成增强有关的疾病中的用途

    公开(公告)号：US5280033A

    公开(公告)日：1994-01-18

    申请号：US768568

    申请日：1991-10-25

    申请人： Paolo Cozzi ,  Marla Menichincheri ,  Arsenia Rossi ,  Corrado Ferti ,  Patricia Salvati

    发明人： Paolo Cozzi ,  Marla Menichincheri ,  Arsenia Rossi ,  Corrado Ferti ,  Patricia Salvati

    IPC分类号： A61K31/415 ,  A61P3/06 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D233/61 ,  C07D521/00 ,  C07F7/08 ,  A61K31/44 ,  C07D409/06

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07F7/0812

    摘要： 1-(Alkoxy-iminoalkyl)imidazole derivatives of formula ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl; A is C.sub.1 -C.sub.4 alkylene optionally substituted by phenyl optionally substituted by halogen or trifluoromethyl; R is (a) hydrogen or a C.sub.1 -C.sub.10 hydrocarbon radical; (b) an aryl or aryl-C.sub.1 -C.sub.4 alkyl group wherein the said aryl is optionally substituted either by halogen, trihalo-methyl, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio or C.sub.1 -C.sub.4 alkylsulfonyl or by C.sub.5 -C.sub.8 alkyl, C.sub.4 -C.sub.8 alkenyl, C.sub.5 -C.sub.8 alkoxy, C.sub.5 -C.sub.8 alkylthio or phenyl optionally substituted by halogen, trihalomethyl or C.sub.1 -C.sub.4 alkyl; or (c) a C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl group, wherein the said cycloalkyl is optionally substituted by C.sub.1 -C.sub.4 alkyl; T is a C.sub.1 -C.sub.6 hydrocarbon chain or phenylene; X is a bond, --O--CH.sub.2 --, --C(R' R")--, Si(R' R")--, vinylene or isopropenylene, each R' and R" being hydrogen, fluorine or C.sub.1 -C.sub.4 alkyl; and R.sub.2 is --OR.sub.3 or --N(R.sub.3 R.sub.4), each R.sub.3 and R.sub.4 being hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl; and the pharmaceutically acceptable salts thereof; are useful in the treatment of a disease state related to enhancement of thromboxane A.sub.2 (TxA.sub.2) synthesis.

    摘要翻译： 式（I）的1-（烷氧基亚氨基烷基）咪唑衍生物，其中R是氢或C 1 -C 4烷基; A是任选被任选被卤素或三氟甲基取代的苯基取代的C 1 -C 4亚烷基; R是（a）氢或C 1 -C 10烃基; （b）芳基或芳基-C 1 -C 4烷基，其中所述芳基任选被卤素，三卤代甲基，C 1 -C 4烷基，C 2 -C 3烯基，C 2 -C 6炔基，C 1 -C 4烷氧基， C 1 -C 4烷基磺酰基或C 5 -C 8烷基，C 4 -C 8烯基，C 5 -C 8烷氧基，C 5 -C 8烷硫基或任选被卤素，三卤代甲基或C 1 -C 4烷基取代的苯基; 或（c）C 5 -C 8环烷基或C 5 -C 8环烷基-C 1 -C 4烷基，其中所述环烷基任选被C 1 -C 4烷基取代; T是C1-C6烃链或亚苯基; X是键，-O-CH 2 - ， - C（R'R“） - ，Si（R'R”） - 亚乙烯基或异亚丙基，每个R'和R“是氢，氟或C1- C4烷基; 并且R 2是-OR 3或-N（R 3 R 4），每个R 3和R 4是氢，C 1 -C 6烷基，苯基或苄基; 及其药学上可接受的盐; 可用于治疗与凝血恶烷A2（TxA2）合成增强相关的疾病状态。

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    4.
    发明授权
    "N-imidazolyl derivatives of bicyclic compounds and pharmaceutical compositions containing the same" 失效
    “双环化合物的N-咪唑基衍生物和含有相同的”

    公开(公告)号：US4882347A

    公开(公告)日：1989-11-21

    申请号：US201909

    申请日：1988-06-02

    申请人： Paolo Cozzi ,  Corrado Ferti ,  Patricia Salvati ,  Germano Carganico ,  Antonio Pillan

    发明人： Paolo Cozzi ,  Corrado Ferti ,  Patricia Salvati ,  Germano Carganico ,  Antonio Pillan

    IPC分类号： C07D233/60 ,  A61K31/415 ,  A61P13/02 ,  A61P15/00 ,  C07D233/61 ,  C07D405/04

    CPC分类号： A61K31/415 ,  Y10S514/866

    摘要： A pharmaceutical compositon having activity against nephropathies comprising, as an active agent, a therapeutically effective amount of a compound of formula (I) ##STR1## wherein (a) ##STR2## wherein Y completes a single bond or is oxygen or a --CH.sub.2 -- group and the symbol ##STR3## represents a single bond or (b) ##STR4## ##STR5## and the symbol ##STR6## represents a double bond; one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is --CH.sub.2 OH, C.sub.2 -C.sub.4 acyl, ##STR7## in which each of R.sub.1, R.sub.8 and R.sub.9 is independently hydrogen or C.sub.1 -C.sub.4 alkyl and the others are independently chosen from hydrogen, hydroxy, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and --COOR, wherein R.sub.7 is as defined above, and one of R.sub.5 and R.sub.6 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier and/or diluent.

    摘要翻译： 具有抗肾病活性的药物组合物，其包含作为活性剂的治疗有效量的式（I）化合物（I），其中（a）其中Y完成单键或氧或氧 -CH 2 - 基，符号表示单键或（b） ，符号表示双键; R 1，R 2，R 3和R 4中的一个是-CH 2 OH，C 2 -C 4酰基，其中R 1，R 8和R 9各自独立地为氢或C 1 -C 4烷基，其余各自独立地选自氢， 羟基，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基和-COOR，其中R 7如上所定义，R 5和R 6之一是氢，另一个是氢，C 1 -C 6烷基或苯基; 或其药学上可接受的盐; 和药学上可接受的载体和/或稀释剂。

    Imidazolyl and pyridyl derivatives of phenyl substituted 1,4-dihydropyridines and process for their preparation
    6.
    发明授权
    Imidazolyl and pyridyl derivatives of phenyl substituted 1,4-dihydropyridines and process for their preparation 失效
    苯基取代的1,4-二氢吡啶的咪唑基和吡啶基衍生物及其制备方法

    公开(公告)号：US5514693A

    公开(公告)日：1996-05-07

    申请号：US92566

    申请日：1993-07-16

    申请人： Paolo Cozzi ,  Germano Carganico ,  Mariia Menichincheri ,  Patricia Salvati

    发明人： Paolo Cozzi ,  Germano Carganico ,  Mariia Menichincheri ,  Patricia Salvati

    IPC分类号： C07D401/10 ,  C07D521/00 ,  A61K31/44

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/10

    摘要： Imidazolyl and pyridyl derivatives of phenyl substituted 1,4-dihydropyridines of formula (I) ##STR1## wherein Het is ##STR2## A represents a direct linkage, --CH.sub.2 --, CH.sub.2 --CH.sub.2 -- or, when Het is ##STR3## A may also represent --CH.dbd.CH--; R is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy; each of R.sub.3 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group; one of R.sub.1 and R.sub.2 is a group --OR' wherein R' is a C.sub.1 -C.sub.6 alkyl either unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy or cyano, and the other is, independently,a) a group --OR";b) a group ##STR4## or c) a group --OR.sup.IV wherein R.sup.IV is hydrogen or a substituent selected from:(i) --(CH.sub.2).sub.m --CH.dbd.CH--Ph, ##STR5## are useful as Thromboxane A.sub.2 (TxA.sub.2) Synthase inhibitors and as calcium antagonists.

    摘要翻译： 式（I）的苯基取代的1,4-二氢吡啶的咪唑基和吡啶基衍生物其中Het为直链，-CH 2 - ，CH 2 -CH 2 - 或当Het为 A也可以表示-CH = CH-; R是氢，卤素，C 1 -C 3烷基或C 1 -C 3烷氧基; R 3和R 4各自为C 1 -C 3烷基; R1和R2之一是基团-OR'，其中R'是未被取代或被C1-C3烷氧基或氰基取代的ω-的C1-C6烷基，另一个独立地是a）基团-OR“; 或者c）基团-ORIV，其中RIV是氢或选自下列的取代基：（i） - （CH 2）m -CH = CH-Ph，（ii）图像（iii） ）和（iv）可用作Thromboxane A2（TxA2）合酶抑制剂和钙拮抗剂。

    Alpha-aminoamide derivatives useful in the treatment of cognitive disorders
    9.
    发明授权
    Alpha-aminoamide derivatives useful in the treatment of cognitive disorders 有权
    可用于治疗认知障碍的α-氨基酰胺衍生物

    公开(公告)号：US08741957B2

    公开(公告)日：2014-06-03

    申请号：US12304455

    申请日：2007-06-13

    申请人： Patricia Salvati ,  Stefano Rossetti ,  Luca Benatti

    发明人： Patricia Salvati ,  Stefano Rossetti ,  Luca Benatti

    IPC分类号： A61K31/165 ,  A61K31/404 ,  A61K31/085 ,  A61K31/135 ,  A61K31/341 ,  A61K31/402

    CPC分类号： A61K31/404 ,  A61K31/085 ,  A61K31/135 ,  A61K31/165 ,  A61K31/341 ,  A61K31/402

    摘要： The present invention is in the field of pharmacotherapy of cognitive deficits in learning and memory by administering an α-aminoamide, particularly safinamide. Examples of disturbances in cognition that can be treated with compounds of the invention are the ones associated with disorders such as autism, dyslexia, attention deficit hyperactivity disorder, schizophrenia, obsessive compulsive disorders, psychosis, bipolar disorders, depression, Tourette's syndrome, Mild Cognitive Impairment (MCI) and disorders of learning in children, adolescents and adults, Age Associated Memory Impairment, Age Associated Cognitive Decline, Alzheimer's Disease, Parkinson's Disease, Down's Syndrome, traumatic brain injury Huntington's Disease, Progressive Supranuclear Palsy (PSP), HIV, stroke, vascular diseases, Pick's or Creutzfeldt-Jacob diseases, multiple sclerosis (MS), other white matter disorders and drug-induced cognitive worsening.

    摘要翻译： 本发明通过给予α-氨基酰胺，特别是safinamide，在学习和记忆中的认知缺陷的药物治疗领域。 可以用本发明化合物治疗的认知障碍的例子是与自闭症，阅读困难，注意缺陷多动障碍，精神分裂症，强迫症，精神病，双相情感障碍，抑郁症，Tourette综合征，轻度认知障碍 （MCI）和儿童，青少年和成年人学习障碍，年龄相关记忆障碍，年龄相关认知衰退，阿尔茨海默病，帕金森病，唐氏综合征，创伤性脑损伤亨廷顿病，进行性核核麻痹（PSP），艾滋病毒，中风， 血管疾病，Pick's或Creutzfeldt-Jacob疾病，多发性硬化症（MS），其他白质病症和药物诱导的认知恶化。

    Alpha-aminoamide derivatives useful in the treatment of psychiatric disorders
    10.
    发明授权
    Alpha-aminoamide derivatives useful in the treatment of psychiatric disorders 有权
    用于治疗精神疾病的α-氨基酰胺衍生物

    公开(公告)号：US08445539B2

    公开(公告)日：2013-05-21

    申请号：US12816143

    申请日：2010-06-15

    申请人： Emanuela Izzo ,  Laura Faravelli ,  Elena Barbanti ,  Patricia Salvati

    发明人： Emanuela Izzo ,  Laura Faravelli ,  Elena Barbanti ,  Patricia Salvati

    IPC分类号： A61K31/165

    CPC分类号： A61K31/165

    摘要： The disclosure relates to pharmacotherapy of a psychiatric disorder which is schizophrenia and/or anxiety, wherein schizophrenia includes schizophrenia related disorders such as brief psychotic disorders, delusional disorders, schizoaffective disorders, and schizophreniform disorders, and anxiety includes panic disorders, obsessive-compulsive disorders (OCD), post-traumatic stress disorders (PTSD), social phobia or social anxiety disorders, specific phobia, and generalized anxiety disorders (GAD). The compounds of the disclosure are useful for the treatment of the above psychiatric disorders alone or in combination with other therapeutical agents effective in the treatment of schizophrenia and/or anxiety disorders.

    摘要翻译： 本公开涉及精神障碍和/或焦虑症的精神障碍的药物治疗，其中精神分裂症包括精神分裂症相关的疾病，例如短暂性精神病，妄想障碍，分裂情感障碍和精神分裂症样症状，焦虑包括恐慌症，强迫症（强迫症） OCD），创伤后应激障碍（PTSD），社交恐惧症或社会焦虑症，特定恐惧症和广泛性焦虑症（GAD）。 本公开的化合物可用于单独或与治​​疗精神分裂症和/或焦虑症有效的其它治疗剂组合治疗上述精神障碍。