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1. 发明授权

US5416208A Process for penems 失效
标题翻译：青春期的过程
公开(公告)号：US5416208A
公开(公告)日：1995-05-16
申请号：US199963
申请日：1994-02-22
申请人： Ettore Perrone , Marco Alpegiani , Franco Zarini , Giuseppe Mazzini , Giovanni Franceschi
发明人： Ettore Perrone , Marco Alpegiani , Franco Zarini , Giuseppe Mazzini , Giovanni Franceschi
IPC分类号： C07D317/40 , C07D499/88 , A61K31/425 , C07D499/00
CPC分类号： C07D317/40 , C07D499/88 , Y02P20/55
摘要： Antibacterial penems of formula (I), where R represents a hydrogen atom or a hydroxy protecting group, are prepared by reacting a .beta.-lactam of formula (II) with an oxalyl halide in an inert solvent in the presence of an organic or inorganic base or an acid scavenger to produce a compound of formula (III), wherein X is a halogen atom, treating the resultant compound of formula (III) with a 1,3-dioxolen-2-one of formula (IV), wherein Y is a hydroxy group, in the presence of molecular sieves or an organic or inorganic base to produce a compound of formula (V), and cyclizing the compound of formula (V) in the presence of a trialkylphosphite to provide the penems of formula (I).
摘要翻译：通过在有机或无机碱的存在下，在惰性溶剂中使式（II）的β-内酰胺与草酰卤反应来制备式（I）的抗菌青霉烯，其中R表示氢原子或羟基保护基或酸清除剂，以制备其中X为卤素原子的式（III）化合物，用式（IV）的1,3-二氧戊环-2-酮处理所得的式（III）化合物，其中Y为在分子筛或有机或无机碱存在下制备式（V）化合物的羟基，并且在亚烷基三烷基膦存在下使式（Ⅴ）化合物环化以提供式（I）的pen）。

2. 发明授权

US4863914A Penem derivatives 失效
标题翻译： Penem衍生物
公开(公告)号：US4863914A
公开(公告)日：1989-09-05
申请号：US849387
申请日：1986-04-08
申请人： Ettore Perrone , Marco Alpegiani , Angelo Bedeschi , Franco Zarini , Giovanni Franceschi , Costantino D. Bruna
发明人： Ettore Perrone , Marco Alpegiani , Angelo Bedeschi , Franco Zarini , Giovanni Franceschi , Costantino D. Bruna
IPC分类号： C07D519/06 , A61K31/425 , A61K31/43 , A61K31/431 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61P31/04 , C07D499/00 , C07D499/04 , C07D499/06 , C07D499/861 , C07D499/88 , C07D499/897 , C07D519/00
CPC分类号： C07D499/88
摘要： Compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.4 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, A is a Z, Z--O--C--O-- or Z--C)-- residue, wherein Z is phenylene, naphthylene, heterocyclediyl, C.sub.1 -C.sub.7 alkylene, C.sub.2 -C.sub.4 alkenylene, alkynylene, ##STR2## C.sub.3 -C.sub.8 cycloalkylene, aralkylene radical optionally substituted, and O.sup.(+) represents a group +NR.sub.1 R.sub.2 R.sub.3, wherein R.sub.1, R.sub.2 and R.sub.3 are each either:(i) a optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2 and R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical, or(iii) R.sub.1, R.sub.2 and R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical, or(iv) R.sub.1, R.sub.2 and R.sub.3, taken together, represent an optionally substituted or fused pyridinium, pyrazinium, pyrazolium or pyridazinium radical, and the pharmaceutically or veterinarily acceptable salts thereof, are disclosed.A method of preparation is also provided. The compounds show high antibacterial activity.
摘要翻译：其中R是氢原子或任选被卤素原子或羟基取代的任选被保护的C 1 -C 4烷基的化合物，A是Z，ZOCO-或ZC）残基，其中Z是亚苯基，亚萘基，杂环基， C 1 -C 7亚烷基，C 2 -C 4亚烯基，亚炔基，C 3 -C 8亚环烷基，任选取代的亚芳基，O（+）表示基团+ NR 1 R 2 R 3，其中R 1，R 2和R 3各自为：（ⅰ）任选取代的烷基，芳烷基或芳基，或（ii）R 1如（i）中所定义，R 2和R 3一起表示任选取代或稠合的杂环基，或（iii）R 1，R 2和R 3一起代表任选取代的亚氮基 - 双环或三环基团，或（iv）R 1，R 2和R 3一起表示任选取代或稠合的吡啶鎓，吡嗪鎓，吡唑鎓或哒嗪鎓基，其药学或兽医学上可接受的盐是披露还提供了一种制备方法。该化合物显示出高抗菌活性。

3. 发明授权

US4713378A Penem derivatives 失效
标题翻译： Penem衍生物
公开(公告)号：US4713378A
公开(公告)日：1987-12-15
申请号：US747829
申请日：1985-06-24
申请人： Ettore Perrone , Marco Alpegiani , Franco Zarini , Costantino D. Bruna , Giovanni Franceschi
发明人： Ettore Perrone , Marco Alpegiani , Franco Zarini , Costantino D. Bruna , Giovanni Franceschi
IPC分类号： C07D513/04 , A61K31/425 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/04 , C07D499/06 , C07D499/88 , C07D499/897 , C07D519/00 , C07D519/06
CPC分类号： C07D499/88
摘要： There are provided compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.3 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, and Q.sup.(+) represents a group ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are each either: (i) optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2, R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical or(iii) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical or(iv) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted fused pyridinium radical or(v) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted pyrazimium, pyrazolium or pyridazinium radical, and the pharmaceutically or veterinarily acceptable salts thereof.A method of preparation is also provided.The compounds show high antibacterial activity.
摘要翻译：提供式IMA的化合物，其中R是氢原子或任选被卤素原子或任选被保护的羟基取代的C 1 -C 3烷基，Q（+）代表基团，其中R 1，R 2和R 3各自是（i）任选取代的烷基，芳烷基或芳基，或（ii）R 1如（i）中所定义，R 2，R 3一起表示任选取代或稠合的杂环基，或（iii）R 1，R 2， R 3一起代表任选取代的亚氮基 - 双环或三环基或（iv）R 1，R 2，R 3一起代表任选取代的稠合吡啶鎓基或（ⅴ）R 1，R 2，R 3一起代表任选取代的吡嗪鎓，吡唑鎓或哒嗪基，以及其药学或兽医学上可接受的盐。还提供了一种制备方法。该化合物显示出高抗菌活性。

4. 发明授权

US4952577A Methoxymethyl penem compounds 失效
标题翻译：甲氧基甲基化合物
公开(公告)号：US4952577A
公开(公告)日：1990-08-28
申请号：US202542
申请日：1988-06-06
申请人： Marco Alpegiani , Giovanni Franceschi , Ettore Perrone , Franco Zarini , Constantino Della Bruna
发明人： Marco Alpegiani , Giovanni Franceschi , Ettore Perrone , Franco Zarini , Constantino Della Bruna
IPC分类号： C07D499/897 , A61K31/43 , A61P31/04 , C07D499/06 , C07D499/88 , C07D499/883
CPC分类号： C07D499/88
摘要： A substantially (.gtoreq.95%) optically pure (5R,6S,1'R) penem of formula ##STR1## and the pharmaceutically acceptable salts and the ester prodrugs thereof, are endowed with antibacterial activity.

5. 发明授权

US4886793A Penem derivatives 失效
标题翻译： Penem衍生物
公开(公告)号：US4886793A
公开(公告)日：1989-12-12
申请号：US022247
申请日：1987-03-05
申请人： Ettore Perrone , Marco Alpegiani , Angelo Bedeschi , Franco Zarini , Costantino Della Bruna , Giovanni Franceschi
发明人： Ettore Perrone , Marco Alpegiani , Angelo Bedeschi , Franco Zarini , Costantino Della Bruna , Giovanni Franceschi
IPC分类号： C07D237/00 , A61K31/43 , A61K31/431 , A61K31/435 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/53 , A61P31/04 , C07D499/04 , C07D499/06 , C07D499/861 , C07D499/88 , C07D499/897 , C07D519/00 , C07D519/06
CPC分类号： C07D499/88
摘要： There are provided compounds of formula I: ##STR1## wherein R.sup.1 is hydrogen or a C.sub.1 -C.sub.4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy or halogen atom;R.sup.2 is a free or esterified carboxy group or carboxylate anion;R.sup.3 and R.sup.4 are each independently hydrogen or organic group,X is --O--, ##STR2## --S--, Q is either(a") free or protected hydroxy, or(b") a C.sub.1 -C.sub.1 acyloxy, or(c") carbamoyloxy OCONH.sub.2, or(d") an optionally substituted heterocyclylthio group, or(e") an optionally substituted imido group, or(f") an optionally substituted quaternary ammonium group or(g") a halogen atom,A and the pharmaceutically or veterinarily acceptable salts thereof. There are provided also methods for preparing compounds of formula I. The compounds of formula I are useful as antibacterial agents.
摘要翻译：提供式I化合物：其中R 1是氢或未被取代或被一个或多个选自游离的或保护的羟基或卤原子的取代基取代的C 1 -C 4烷基; R2是游离或酯化的羧基或羧酸根阴离子; R 3和R 4各自独立地为氢或有机基团，X为-O-，Q为（a“）或保护的羟基，或（b”）a C1 -C 1酰氧基或（C“）氨基甲酰氧基OCONH 2，或（d”）任选取代的杂环硫基，或（e“）任选取代的亚氨基，或（f”）任选取代的季铵基团或（g“）卤素原子，A及其药学上或兽医学上可接受的盐。还提供了制备式I化合物的方法。式I化合物可用作抗菌剂。

6. 发明授权

US4837215A Penem derivatives 失效
标题翻译： Penem衍生物
公开(公告)号：US4837215A
公开(公告)日：1989-06-06
申请号：US849388
申请日：1986-04-08
申请人： Ettore Perrone , Marco Alpegiani , Angelo Bedeschi , Franco Zarini , Giovanni Franceschi , Costantino D. Bruna
发明人： Ettore Perrone , Marco Alpegiani , Angelo Bedeschi , Franco Zarini , Giovanni Franceschi , Costantino D. Bruna
IPC分类号： C07D519/06 , A61K31/425 , A61K31/43 , A61K31/435 , A61K31/44 , A61K31/535 , A61P31/04 , C07D499/00 , C07D499/88 , C07D499/897
CPC分类号： C07D499/00
摘要： Compounds of the following formula I ##STR1## wherein X represents a sulphur or an oxygen atom,R is hydrogen or a C.sub.1 -C.sub.4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy group and halogen atom;A is a Z, Z--O--CO-- or --Z--CO-- residue, whereinZ represents(a) an optionally substituted phenylene or naphthylene group,(b) an optionally substituted heterocyclediyl radical wherein the hetero ring is mono or bicyclic, saturated or unsaturated containing at least one heteroatom selected from the group of oxygen, sulphur and nitrogen;(c) an optionally substituted linear or branched C.sub.1 -C.sub.7 alkylene radical;(d) a C.sub.2 -C.sub.4 alkenylene or alkynylene group or a group of formula ##STR2## (e) an optionally substituted C.sub.3 -C.sub.8 cycloalkylene ring; (f) an aralkylene radical of the formula ##STR3## wherein n is 1, 2 or 3; andQ.sup.(+) represents a +NR.sub.1 R.sub.2 R.sub.3 group, wherein(i) R.sub.1, R.sub.2, R.sub.3, are each independently an optionally substituted alkyl, aralkyl or aryl radical; or p1 (ii) R.sub.1 is as defined above under (i) and R.sub.2, R.sub.3 taken together with the nitrogen atom represent an optionally substituted heterocyclic or fused heterocyclic radical; or(iii) R.sub.1, R.sub.2, R.sub.3, taken together with the nitrogen atom, represent an optionally substituted azoniabicyclo or azoniatricyclo radical; or(iv) R.sub.1, R.sub.2, R.sub.3, taken together with nitrogen atom, represent an optionally substituted pyridinium, pirazinium, pyrazolium, or pyridazinium radical, such radicals being optionally fused with one phenyl ring or with a 5-7 membered, saturated or unsaturated cycloaliphatic or heterocyclic ring,or a pharmaceutically or veterinarily acceptable salt thereof having high antibacterial activity.
摘要翻译：下式I的化合物其中X表示硫或氧原子，R是氢或未被取代或被一个或多个选自游离或保护的羟基的取代基取代的C 1 -C 4烷基，卤素原子; A是Z，ZO-CO-或-Z-CO-残基，其中Z表示（a）任选取代的亚苯基或亚萘基，（b）任选取代的杂环二基，其中杂环是单或双环，饱和或不饱和的含有至少一个选自氧，硫和氮的杂原子; （c）任选取代的直链或支链C 1 -C 7亚烷基; （d）C 2 -C 4亚链烯基或亚炔基或式（A）的基团：（e）任选取代的C 3 -C 8亚环烷基环; （f）下式的芳亚烷基：其中n为1,2或3; 并且Q（+）表示+ NR 1 R 2 R 3基团，其中（i）R 1，R 2，R 3各自独立地为任选取代的烷基，芳烷基或芳基; 或p1（ii）R1如上文（i）和（R2）中所定义，R3与氮原子一起表示任选取代的杂环或稠合杂环基; 或（iii）与氮原子一起的R 1，R 2，R 3代表任选取代的二氮杂双环或氮杂三环基; 或（iv）R 1，R 2，R 3与氮原子一起代表任选取代的吡啶鎓，吡嗪鎓，吡唑鎓或哒嗪鎓基团，该基团任选地与一个苯环或与5-7元饱和或不饱和的脂环族或杂环，或其具有高抗菌活性的药学上或兽医学上可接受的盐。

7. 发明授权

US5480880A Penem derivatives 失效
标题翻译： Penem衍生物
公开(公告)号：US5480880A
公开(公告)日：1996-01-02
申请号：US972444
申请日：1993-04-09
申请人： Giuseppina Visentin , Franco Zarini , Daniela Jabes , Ettore Perrone , Costantino della Bruna , Marco Alpegiani
发明人： Giuseppina Visentin , Franco Zarini , Daniela Jabes , Ettore Perrone , Costantino della Bruna , Marco Alpegiani
IPC分类号： A61K31/43 , A61K31/431 , A61K31/44 , A61K31/675 , A61P31/04 , C07D499/88 , C07D499/883 , C07D499/893 , C07D499/897 , C07D499/00
CPC分类号： C07D499/88
摘要： The invention provides compounds of the general formula I ##STR1## wherein R.sub.1 is a hydrogen atom, a negative charge or an ester residue; R is:a) --(CH.sub.2).sub.n --A--CO.sub.2 H, --(CH.sub.2)n--A--SO.sub.3 H or --(CH.sub.2).sub.n --A--PO.sub.3 H.sub.2, wherein n is either zero, one or two and A is a group --CH.dbd.CH-- (either E or Z), --OCH.sub.2 --, --SCH.sub.2 -- or --CHOH--;b) --(CH.sub.2).sub.n --PO.sub.3 H.sub.2, --(CH.sub.2).sub.n SO.sub.2 NHCN, --(CH.sub.2).sub.n NHSO.sub.3 H, --(CH.sub.2).sub.n CONHSO.sub.2 CH.sub.3 or --(CH.sub.2).sub.n CONHSO.sub.2 CF.sub.3, wherein n is as defined above;c) --(CH.sub.2 S).sub.m --W--(CH.sub.2).sub.n Z, wherein W is an arylene group or a heterocyclediyl group, m is 0 or 1, n is as above defined, and Z represents CO.sub.2 H, PO.sub.3 H.sub.2, SO.sub.2 NHCN, NHSO.sub.3 H, CONHSO.sub.2 CH.sub.3 or CONHSO.sub.2 CF.sub.3 ;d) ##STR2## wherein Y is O or NH and X is NH, N--OH or N--O--(CH.sub.2).sub.n+1 COOH wherein n is as defined above; ore) --(CH.sub.2 S).sub.m --W', wherein W' is a heterocyclyl group convertible into an anion at physiological pH and m is as defined above.Compounds I, their salts and ester prodrugs have antibacterial activity.
摘要翻译： PCT No.PCT / EP92 / 01396 Sec。 371日期：1993年4月9日 102（e）日期1993年4月9日PCT提交1992年6月22日PCT公布。出版物WO93 / 00345 日本1993年1月7日。本发明提供通式Ⅰ（I）的化合物，其中R1是氢原子，负电荷或酯残基; R是：a） - （CH 2）n A-CO 2 H， - （CH 2）n A-SO 3 H或 - （CH 2）n A-PO 3 H 2，其中n是零，一个或两个，A是基团-CH = CH- E或Z），-OCH 2 - ， - CH 2 - 或-CHOH-; b） - （CH 2）n -PO 3 H 2， - （CH 2）n SO 2 NHCN， - （CH 2）n NHSO 3 H， - （CH 2）n CONHSO 2 CH 3或 - （CH 2）n CONHSO 2 CF 3，其中n如上所定义; c） - （CH 2 S）m W-（CH 2）n Z，其中W是亚芳基或杂环基，m是0或1，n如上所定义，Z代表CO 2 H，PO 3 H 2，SO 2 NHCN，NHSO 3 H，CONHSO 2 CH 3或CONHSO 2 CF 3 ; d）其中Y是O或NH，X是NH，N-OH或N-O-（CH 2）n + 1COOH，其中n如上定义; 或e） - （CH 2 S）m -W'，其中W'是在生理pH下可转化成阴离子的杂环基，m如上所定义。化合物I，其盐和酯前药具有抗菌活性。

8. 发明授权

US5077286A Beta-lactam derivatives of the 4-acylcephem sulphone and 3-acylpenam sulphone-type 失效
标题翻译： 4-亚氨基磺酸钠和3-乙酰氧基苯酚类型的BETA-LACTAM衍生物
公开(公告)号：US5077286A
公开(公告)日：1991-12-31
申请号：US335824
申请日：1989-04-10
申请人： Pierluigi Bissolino , Marco Alpegiani , Ettore Perrone , Piergiuseppe Orezzi , Giuseppe Cassinelli , Giovanni Franceschi
发明人： Pierluigi Bissolino , Marco Alpegiani , Ettore Perrone , Piergiuseppe Orezzi , Giuseppe Cassinelli , Giovanni Franceschi
IPC分类号： C07D499/87 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D499/00 , C07D499/08 , C07D499/28 , C07D499/44 , C07D499/86 , C07D499/861 , C07D499/865 , C07D499/897 , C07D501/00 , C07D501/02 , C07D501/04 , C07D501/20
CPC分类号： C07D499/00
摘要： Compounds of formulae Ia and Ib ##STR1## wherein A is hydrogen atom or an organic residue, R.sup.1 is halogen atom, or an organic group, R.sup.2 is hydrogen or halogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy group, R.sup.3 is hydrogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy group, benzyl or a methylene group and R.sub.4 is an organic residue are disclosed. Compounds (Ia) and (Ib) are endowed with elastase inhibitory activity. A two-step process for their preparation starting from the corresponding 4-carboxy cephem or 3-carboxy penam is also provided.

9. 发明授权

US4585874A Process for preparing penem derivatives 失效
标题翻译：制备penin衍生物的方法
公开(公告)号：US4585874A
公开(公告)日：1986-04-29
申请号：US558629
申请日：1983-12-06
申请人： Marco Alpegiani , Angelo Bedeschi , Maurizio Foglio , Giovanni Franceschi , Ettore Perrone
发明人： Marco Alpegiani , Angelo Bedeschi , Maurizio Foglio , Giovanni Franceschi , Ettore Perrone
IPC分类号： C07D205/09 , C07D417/12 , C07D499/06 , C07D499/86 , C07D499/861 , C07D499/87 , C07D499/88 , C07D499/897 , C07D513/04 , C07F7/18 , C07D499/00
CPC分类号： C07D417/12 , C07D205/09 , C07D499/88 , C07D513/04 , C07F7/1804 , C07F7/186 , Y02P20/55
摘要： A new process is described for the preparation of (5R)-penem derivatives of the general formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or an organic group; R.sub.2 represents a hydrogen atom or a carboxy protecting group and Y represents a hydrogen or halogen atom or an organic group. A 2-thiacephem derivative of the general formula II: ##STR2## wherein R.sub.1, R.sub.2 and Y have the meanings/given above is oxidized by means of organic peracids to the corresponding sulphone of the general formula III: ##STR3## which is subsequently submitted to a desulphurative ring contraction by extrusion of SO.sub.2 to give exclusively the desired (5R)-penem derivatives of the general formula I.
摘要翻译：描述了用于制备通式I的（5R） - 衍生物的新方法：其中R 1表示氢原子或有机基团; R2表示氢原子或羧基保护基，Y表示氢或卤素原子或有机基团。通式II的2-噻虫氨酸衍生物：其中R1，R2和Y具有上述含义，通过有机过酸被氧化成通式III的相应的砜：随后通过挤出SO 2使脱硫环收缩，从而纯化得到通式I所需的（5R） - 顺式衍生物。

10. 发明授权

US5348952A .beta.-lactam derivatives of the cephem sulphone type 失效
标题翻译：头孢类型的β-内酰胺衍生物
公开(公告)号：US5348952A
公开(公告)日：1994-09-20
申请号：US853745
申请日：1992-06-12
申请人： Pierluigi Bissolino , Marco Alpegiani , Ettore Perrone , Piergiuseppe Orezzi , Giuseppe Cassinelli , Giovanni Franceschi
发明人： Pierluigi Bissolino , Marco Alpegiani , Ettore Perrone , Piergiuseppe Orezzi , Giuseppe Cassinelli , Giovanni Franceschi
IPC分类号： A61K31/545 , A61K31/546 , A61P11/00 , A61P17/00 , A61P19/06 , A61P29/00 , A61P31/04 , A61P37/08 , C07D501/00 , C07D501/04 , C07D501/16 , C07D501/18 , C07D501/22 , C07D501/24 , C07D501/26 , C07D501/28 , C07D501/30 , C07D501/34 , C07D501/36 , C07D501/38 , C07D501/40 , C07D501/42 , C07D501/46 , C07D501/48 , C07D501/50 , C07D501/52 , C07D501/56 , C07D519/06 , C07D501/20
CPC分类号： C07D501/00
摘要： Cephalosporins of the formula (I): ##STR1## wherein m is one or two; n is zero, one or two; A and B are organic residues; and R.sub.1 and R.sub.2 are halogen or hydrogen atoms or organic groups are endowed with elastase inhibitory activity. Two processes for their preparation starting from the corresponding 4-acyl cephem are also provided.
摘要翻译： PCT No.PCT / EP90 / 02189 371日期：1992年6月12日 102（e）日期1992年6月12日PCT 1990年12月14日PCT PCT。出版物WO91 / 09036 日期：1991年6月27日。式（I）的头孢菌素：其中m为1或2; n为零，一或二; A和B是有机残基; 并且R 1和R 2是卤素或氢原子或有机基团赋予弹性蛋白酶抑制活性。还提供了从相应的4-酰基头孢烯开始的两种其制备方法。

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