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21. 发明授权

US5580865A 2,2-disubstituted cephem sulphones 失效
标题翻译： 2,2-二取代的头孢烯砜
公开(公告)号：US5580865A
公开(公告)日：1996-12-03
申请号：US43023
申请日：1993-04-05
申请人： Marco Alpegiani , Pierluigi Bissolino , Ettore Perrone , Vincenzo Rizzo
发明人： Marco Alpegiani , Pierluigi Bissolino , Ettore Perrone , Vincenzo Rizzo
IPC分类号： A61K31/545 , A61K31/546 , A61P11/00 , A61P17/00 , A61P19/06 , A61P29/00 , C07D501/00 , C07D501/04 , C07D501/16 , C07D501/20 , C07D501/36 , C07D501/22 , C07D501/24
CPC分类号： C07D501/00
摘要： The present invention provides cephalosporin sulphones or formula (I), and pharmaceutically or veterinarily acceptable salts thereof; ##STR1## wherein n is zero, one or two; R.sub.1 is hydrogen, halogen or an optionally substituted C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio or C.sub.1 -C.sub.4 carboxamido group;R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.5 alkenyl or C.sub.3 -C.sub.6 cycloalkyl group;R.sub.3 is hydrogen or acetoxymethyl, methoxymethyl, methyl or an optionally substituted heterocyclylthiomethyl group;R.sub.4 is an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.6 alkenyl, aryl(C.sub.1 -C.sub.8)alkyl or heterocyclyl(C.sub.1 -C.sub.8)alkyl group; andR.sub.5 is an optionally substituted C.sub.6 -C.sub.10 aryl or a heterocyclyl group.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.
摘要翻译：本发明提供头孢菌素砜或式（I）化合物及其药学或兽医学上可接受的盐; （I）其中n为0，1或2; R 1是氢，卤素或任选取代的C 1 -C 4烷基，C 2 -C 4烯基，C 1 -C 4烷氧基，C 1 -C 4烷硫基或C 1 -C 4甲酰氨基; R 2是氢或任选取代的C 1 -C 8烷基，C 6 -C 10芳基，C 2 -C 5烯基或C 3 -C 6环烷基; R3是氢或乙酰氧基甲基，甲氧基甲基，甲基或任意取代的杂环硫基甲基; R4是任选取代的C 1 -C 8烷基，C 2 -C 6烯基，芳基（C 1 -C 8）烷基或杂环基（C 1 -C 8）烷基; 并且R 5是任选取代的C 6 -C 10芳基或杂环基。式I化合物及其药学上和兽医学上可接受的盐是弹性蛋白酶抑制剂。

22. 发明授权

US5254680A Process for the preparation of 7 alpha-alkoxycephem derivatives 失效
标题翻译：制备7α-烷氧基头孢烯衍生物的方法
公开(公告)号：US5254680A
公开(公告)日：1993-10-19
申请号：US691089
申请日：1991-04-25
申请人： Marco Alpegiani , Pierluigi Bissolino , Matteo D'Anello , Ettore Perrone
发明人： Marco Alpegiani , Pierluigi Bissolino , Matteo D'Anello , Ettore Perrone
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , A61P43/00 , C07D501/00 , C07D501/04
CPC分类号： C07D501/00
摘要： There is provided a process for preparing a compound of the formula (I): ##STR1## wherein R.sub.1 is an organic residue, R.sub.2 is a hydrogen or a chlorine atom, a methoxy, ethoxy or an acetoxy group, and n represents 0, 1 or 2.The process comprises reacting a compound of the formula (II): ##STR2## wherein R.sub.2 and n are as defined above, with an inorganic or organic nitrite, in an alcohol R.sub.1 OH, wherein R.sub.1 is as defined above, or in a mixture R.sub.1 OH-organic solvent in the presence of an inorganic or organic acid.The compounds of the formula (I) are known intermediates in the synthesis of human leucocyte elastase inhibitors (HLE).
摘要翻译：提供了制备式（I）化合物的方法：其中R1是有机残基，R2是氢或氯原子，甲氧基，乙氧基或乙酰氧基，n表示该方法包括使式（II）化合物：其中R2和n如上所定义的化合物与无机或有机亚硝酸盐在醇R 1 OH中反应，其中R 1为或在无机或有机酸存在下，在混合物中的R1OH-有机溶剂中。式（I）的化合物是合成人类白细胞弹性蛋白酶抑制剂（HLE）的已知中间体。

23. 发明授权

US5089489A 6-substituted penem esters as anti-inflammatory and anti-degenerative agents 失效
标题翻译：作为抗炎剂和抗变性剂的6-取代的雄蕊
公开(公告)号：US5089489A
公开(公告)日：1992-02-18
申请号：US504836
申请日：1990-04-05
申请人： Marco Alpegiani , Ettore Perrone , Piergiuseppe Orezzi , Paolo Carminati , Giuseppe Cassinelli
发明人： Marco Alpegiani , Ettore Perrone , Piergiuseppe Orezzi , Paolo Carminati , Giuseppe Cassinelli
IPC分类号： C07D499/897 , A61K31/43 , A61P29/00 , A61P43/00 , C07D499/06 , C07D499/88
CPC分类号： C07D499/88 , A61K31/43
摘要： 6-substituted penem esters of formula (I): ##STR1## wherein R.sub.1 is halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl, phenoxy, benzyl or sulphonyloxy group; R.sub.2 is a C.sub.1 -C.sub.4 alkyl, benzyl diphenylmethyl ##STR2## group where A is C.sub.1 -C.sub.4 alkyl, benzyl, p-nitrobenzyl or p-methoxybenzyl; and R.sub.3 is an organic radical, are elastase inhibitors and thereby useful antiinflammatory and antidegenerative agents.

24. 发明授权

US4729990A Substituted penem derivatives 失效
标题翻译：被取代的penem衍生物
公开(公告)号：US4729990A
公开(公告)日：1988-03-08
申请号：US807688
申请日：1985-12-11
申请人： Marco Alpegiani , Angelo Bedeschi , Maurizio Foglio , Giovanni Francheschi , Ettore Perrone
发明人： Marco Alpegiani , Angelo Bedeschi , Maurizio Foglio , Giovanni Francheschi , Ettore Perrone
IPC分类号： C07D499/897 , A61K31/43 , A61K31/431 , A61P31/04 , C07D499/04 , C07D499/06 , C07D499/88 , C07D499/883 , C07D519/00 , C07F7/18 , C07D499/00 , A61K31/425
CPC分类号： C07F7/186 , C07D499/88 , C07F7/1804 , Y02P20/55
摘要： Antibacterial compounds of formula (I) ##STR1## wherein, R.sub.1 ' is alkyl or hydroxyalkyl;R.sub.2 is hydrogen or a carboxy protecting group; andY' is a group-S-heterocyclic or pyridyl, which group may be substituted, and pharmaceutically or veterinarily acceptable salts thereof and pharmaceutical compositions containing the same.
摘要翻译：式（I）的抗菌化合物其中R1'是烷基或羟烷基; R2是氢或羧基保护基; Y'是可以被取代的基团S-杂环或吡啶基，以及其药学上或兽医学上可接受的盐和含有它们的药物组合物。

25. 发明授权

US5356888A 1,1-dioxo-cephem-4-carbothiolic acid derivatives 失效
标题翻译： 1,1-二氧代 - 头孢烯-4-硫代硫酸衍生物
公开(公告)号：US5356888A
公开(公告)日：1994-10-18
申请号：US780549
申请日：1991-10-22
申请人： Marco Alpegiani , Pierluigi Bissolino , Ettore Perrone , Francesco Di Matteo , Piergiuseppe Orezzi , Giuseppe Cassinelli
发明人： Marco Alpegiani , Pierluigi Bissolino , Ettore Perrone , Francesco Di Matteo , Piergiuseppe Orezzi , Giuseppe Cassinelli
IPC分类号： C07D519/06 , A61K31/545 , A61K31/546 , A61K38/55 , A61P11/00 , A61P17/00 , A61P19/06 , A61P29/00 , A61P43/00 , C07D501/00 , C07D501/20 , C07K1/113 , C07K5/06 , C07K5/08 , C07K14/81
CPC分类号： C07D501/00
摘要： There are provided compounds I ##STR1## wherein A is a hydrogen atom or an organic group,R.sub.1 is hydrogen or halogen atom or an organic group,R.sub.2 is hydrogen or halogen atom, C.sub.1 -C.sub.4 alkyl or acyloxy group,R.sub.3 is hydrogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy, benzyl group or a methylene andR.sub.4 is chloro, fluoro, hydrogen atom or an organic group.The compounds I are elastase inhibitors. A process for their preparation is also provided, as are pharmaceutical compositions containing them.
摘要翻译：提供了化合物I，其中A是氢原子或有机基团，R 1是氢或卤素原子或有机基团，R 2是氢或卤素原子，C 1 -C 4烷基或酰氧基，R 3是氢原子，C 1 -C 4烷基或烷氧基，苄基或亚甲基，R 4是氯，氟，氢原子或有机基团。化合物I是弹性蛋白酶抑制剂。还提供了其制备方法，以及含有它们的药物组合物。

26. 发明授权

US5200403A Inhibition of .beta.lactamase with 6 .beta.-(substituted methyl)-penicillanic acid derivatives 失效
标题翻译：用6β-（取代的甲基） - 青霉烷酸衍生物抑制β-内酰胺酶
公开(公告)号：US5200403A
公开(公告)日：1993-04-06
申请号：US734559
申请日：1991-07-23
申请人： Marco Alpegiani , Stephen Hanessian , Giuseppe Meinardi , Ettore Perrone
发明人： Marco Alpegiani , Stephen Hanessian , Giuseppe Meinardi , Ettore Perrone
IPC分类号： C07D499/00
CPC分类号： C07D499/00
摘要： Compounds of the formula I ##STR1## wherein R' is a free or esterified carboxy group or a carboxylate anion and R.sup.2 is an organic group have beta-lactamase inhibition activity. A process for the preparation of the same and pharmaceutical compositions containing these compounds are provided.
摘要翻译：其中R'为游离或酯化的羧基或羧酸根阴离子且R 2为有机基团的式I的化合物具有β-内酰胺酶抑制活性。提供了制备其的方法和含有这些化合物的药物组合物。

27. 发明授权

US4954493A 6-substituted penem esters as anti-inflammatory and anti-degenerative agents 失效
标题翻译： 6-取代的半胱氨酸酯作为抗炎和抗退行剂
公开(公告)号：US4954493A
公开(公告)日：1990-09-04
申请号：US206375
申请日：1988-06-14
申请人： Marco Alpegiani , Ettore Perrone , Piergiuseppe Orezzi , Paolo Carminati , Giuseppe Cassinelli
发明人： Marco Alpegiani , Ettore Perrone , Piergiuseppe Orezzi , Paolo Carminati , Giuseppe Cassinelli
IPC分类号： C07D499/897 , A61K31/43 , A61P29/00 , A61P43/00 , C07D499/06 , C07D499/88
CPC分类号： C07D499/88 , A61K31/43
摘要： 6-substituted penem esters of formula (I): ##STR1## wherein R.sub.1 is halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl, phenoxy, benzyl, or sulphonyloxy group; R.sub.2 is a C.sub.1 -C.sub.4 alkyl, benzyl diphenylmethyl ##STR2## group where A is C.sub.1 -C.sub.4 is C.sub.1 -C.sub.4 alkyl, benzyl, p-nitrobenzyl or p-methoxybenzyl; and R.sub.3 is an organic radical, are elastase inhibitors and thereby useful antiinflammatory and antidegenerative agents.
摘要翻译：式（I）的6-取代的戊二酸酯：其中R 1是卤素或C 1 -C 4烷基，C 1 -C 4烷氧基，苯基，苯氧基，苄基或磺酰氧基; R2是C1-C4烷基，苄基二苯基甲基，其中A是C1-C4是C1-C4烷基，苄基，对硝基苄基或对甲氧基苄基; 和R3是有机基团，是弹性蛋白酶抑制剂，从而有用的抗炎和抗再生剂。

28. 发明授权

US4771134A Ring-opening process for preparing azetidinone intermediates 失效
标题翻译：制备氮杂环丁酮中间体的开环方法
公开(公告)号：US4771134A
公开(公告)日：1988-09-13
申请号：US818235
申请日：1986-01-13
申请人： Marco Alpegiani , Angelo Bedeschi , Ettore Perrone
发明人： Marco Alpegiani , Angelo Bedeschi , Ettore Perrone
IPC分类号： C07D205/08 , C07D205/09 , C07D205/095 , C07D499/00 , C07D499/86 , C07D499/861 , C07D499/87 , C07D499/88 , C07D499/897 , C07F7/18 , C07B45/06
CPC分类号： C07D205/09 , C07F7/186
摘要： Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 is each H, halo or an organic group, R.sub.3 is H or organic group, n=1 or 2, M is a heavy mono- or divalent metal, or M.sub.2 A wherein M.sub.2 is a heavy divalent metal and A is an organic or inorganic group, are prepared by treating a starting penicillin in a solvent with a salt of M.sub.1 or M.sub.2 A in the presence of a base at a temperature of from -70.degree. to 100.degree. C.
摘要翻译：式I的化合物其中R 1和R 2各自为H，卤素或有机基团，R 3为H或有机基团，n = 1或2，M为重质单价或二价金属或M2A，其中 M2是重的二价金属，A是有机或无机基团，通过在碱存在下在-70至100℃的温度下，用M1或M2A的盐处理起始青霉素在溶剂中制备。

29. 发明申请

US20100311784A1 STEREOSELECTIVE PROCESS AND CRYSTALLINE FORMS OF A CAMPTOTHECIN 有权
公开(公告)号：US20100311784A1
公开(公告)日：2010-12-09
申请号：US12857776
申请日：2010-08-17
申请人： Paolo Carminati , Maria Ornella Tinti , Mauro Marzi , Fabrizio Giorgi , Walter Cabri , Marco Alpegiani , Domenico Vergani , Paolo Ghetti
发明人： Paolo Carminati , Maria Ornella Tinti , Mauro Marzi , Fabrizio Giorgi , Walter Cabri , Marco Alpegiani , Domenico Vergani , Paolo Ghetti
IPC分类号： A61K31/4375 , C07D491/22 , A61P35/00
CPC分类号： C07D491/22
摘要： A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process.

30. 发明授权

US09447109B2 Crystalline salts of asenapine 有权
标题翻译：阿替那磷的结晶盐
公开(公告)号：US09447109B2
公开(公告)日：2016-09-20
申请号：US14113091
申请日：2012-04-30
申请人： Samuele Frigoli , Davide Longoni , Tamara Danelli , Marco Alpegiani
发明人： Samuele Frigoli , Davide Longoni , Tamara Danelli , Marco Alpegiani
IPC分类号： C07D491/044
CPC分类号： C07D491/044
摘要： Disclosed is asenapine phosphate of formula (I) and its enantiomer (I) which can be used to prepare asenapine maleate. Further disclosed is a monoclinic crystalline form of asenapine maleate.

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