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1. 发明授权

US5280033A Substituted 1-(alkoxy-iminoalkyl) imidazole derivatives and their use in treating disease related to an enhancement of thromboxane-A.sub.2 syntheis 失效
标题翻译：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。

2. 发明授权

US5246956A N-imidazolyl derivatives of substituted alkoxyimino tetrahydronaphthalenes and chromans having antithromboxane A.sub.2 activity 失效
标题翻译：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.

3. 发明授权

US5283254A 2-(imidazol-1-yl)-2-benzylethyldiene-aminoxyalkanoic acid derivatives 失效
标题翻译： 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。

4. 发明授权

US5847127A Process for the preparation of 2,2'-bipyrrolyl-pyrromethene (prodigiosins) derivatives 失效
标题翻译：制备2,2'-联吡咯基亚甲基吡咯（prodigiosins）衍生物的方法
公开(公告)号：US5847127A
公开(公告)日：1998-12-08
申请号：US930575
申请日：1997-10-15
申请人： Roberto D'Alessio , Arsenia Rossi , Marcellino Tibolla , Lucio Ceriani
发明人： Roberto D'Alessio , Arsenia Rossi , Marcellino Tibolla , Lucio Ceriani
IPC分类号： A61K31/40 , A61P31/04 , A61P37/06 , C07D207/44 , C07D413/04
CPC分类号： C07D207/44
摘要： The present invention is related to a process for the preparation of 5-�2H-pyrrol-2-ylidene)methyl!-2,2'-bi-1H-pyrrole compounds and an intermediate compound.
摘要翻译： PCT No.PCT / EP97 / 00368 Sec。 371日期：1997年10月15日 102（e）1997年10月15日PCT PCT 1997年1月22日PCT公布。第WO97 / 30029号公报日期1997年8月21日本发明涉及制备5- [2H-吡咯-2-亚基）甲基] -2,2'-二-1H-吡咯化合物和中间体化合物的方法。

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