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    2-(imidazol-1-yl)-2-benzylethyldiene-aminoxyalkanoic acid derivatives
    1.
    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。

    N-imidazolyl derivatives of substituted alkoxyimino tetrahydronaphthalenes and chromans having antithromboxane A.sub.2 activity
    2.
    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.

    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。

    ">
    5.
    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。

    Dihydropyridine derivatives useful in antitumor therapy
    6.
    发明授权
    Dihydropyridine derivatives useful in antitumor therapy 失效
    用于抗肿瘤治疗的二氢吡啶衍生物

    公开(公告)号：US5362729A

    公开(公告)日：1994-11-08

    申请号：US937681

    申请日：1992-09-01

    申请人： Paolo Cozzi ,  Maria Menichincheri ,  Laura Capolongo ,  Nicola Mongelli

    发明人： Paolo Cozzi ,  Maria Menichincheri ,  Laura Capolongo ,  Nicola Mongelli

    IPC分类号： A61K31/435 ,  A61K9/20 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/4427 ,  A61P35/00 ,  C07D213/80 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D521/00 ,  A61K31/535

    CPC分类号： C07D213/80 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： Compounds which are useful in anti-tumors therapy having the formula (I) ##STR1## wherein Het imidazole, A represents a direct linkage at the phenyl 4-position: R is hydrogen; one of R.sub.3 and R.sub.4 is C.sub.1 -C.sub.3 alkyl unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy, and the other, independently, is:a) C.sub.1 -C.sub.3 alkyl unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy; orb) --(CH.sub.2).sub.m --O--(CH.sub.2).sub.n --NR.sub.a R.sub.b wherein each of m and n, which may be the same or different is an integer of 1 to 3, each of R.sub.a and R.sub.b, which may be the same or different, is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by a morpholino;each of R.sub.1 and R.sub.2 is independently a group --OR' wherein R' is C.sub.1 -C.sub.6 alkyl; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 可用于具有式（I）的抗肿瘤治疗的化合物（I）其中Het咪唑，A表示在4-位苯基上的直接键：R是氢; R3和R4中的一个是未取代或被C1-C3烷氧基取代的ω-C3烷基，另一个独立地是：a）未取代或被C1-C3烷氧基取代的ω-C3烷基; 或b） - （CH 2）m O-（CH 2）n -NR a R b，其中m和n可以相同或不同，为1〜3的整数，Ra和Rb各自可以相同或不同 是氢或C 1 -C 3烷基; R5是氢或未被取代或被吗啉代取代的C1-C6烷基; R 1和R 2各自独立地是基团-OR'，其中R'是C 1 -C 6烷基; 或其药学上可接受的盐。

    Imidazolyl and pyridyl derivatives of phenyl substituted 1,4-dihydropyridines and process for their preparation
    7.
    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。

    Combined therapy against tumors comprising substituted acryloyl distamycin derivatives and platinum derivatives
    10.
    发明授权
    Combined therapy against tumors comprising substituted acryloyl distamycin derivatives and platinum derivatives 失效
    针对包含取代的丙烯酰基霉素衍生物和铂衍生物的肿瘤的组合疗法

    公开(公告)号：US08642580B2

    公开(公告)日：2014-02-04

    申请号：US10311995

    申请日：2001-06-20

    申请人： M. Cristina Geroni ,  Paolo Cozzi ,  Italo Beria

    发明人： M. Cristina Geroni ,  Paolo Cozzi ,  Italo Beria

    IPC分类号： A01N43/00 ,  A61K31/33 ,  A61K38/00 ,  A61P35/00 ,  A61P35/02

    CPC分类号： A61K45/06

    摘要： Compounds which are α-halogenoacryloyl distamycin derivatives of formula (I) wherein R1 is a bromine or chlorine atom; R2 is a distamycin or distamycin-like framework as set forth in the specification; or a pharmaceutically acceptable salt thereof; are cytotoxic agents particularly effective in the treatment of tumors over expressing GSH/GSTs system and which are poorly responsive or even resistant to conventional antitumor therapies.

    摘要翻译： 化合物，其是式（I）的α-卤代丙烯酰基霉霉素衍生物，其中R 1是溴或氯原子; R2是本说明书中阐述的一种类霉素或类霉素样骨架; 或其药学上可接受的盐; 是细胞毒性剂在治疗肿瘤时特别有效地表达GSH / GSTs系统，并且对常规抗肿瘤疗法的反应性甚弱。