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公开(公告)号：US4820701A
公开(公告)日：1989-04-11
申请号：US112103
申请日：1987-10-21
IPC分类号： C07D499/04 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/06 , C07D499/12 , C07D499/42 , C07D499/64 , C07D499/66 , C07D499/68 , C07D499/70 , C07D499/76
CPC分类号： C07D499/00
摘要： Antibacterial agents have the formula (I) or are pharmaceutically acceptable salts or in vivo hydrolysable esters thereof: ##STR1## wherein R.sup.3 is phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl or an optionally substituted 5- or 6-membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphur or nitrogen, R.sup.4 is hydrogen or formamido, R.sup.5 is hydrogen, C.sub.1-6 alkyl, substituted alkyl, aryl or aralkyl, R.sup.6 and R.sup.7 are the same or different and represent hydrogen, C.sub.1-6 alkyl, substituted alkyl, halogen, amino, phenyl, substituted phenyl, hydroxyl or C.sub.1-6 alkoxy or R.sup.6 and R.sup.7 form the residue of an optionally substituted 5- or 6-membered carbocyclic ring or a 5- or 6- membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphr or nitrogen, and X represents ##STR2## or tautomers thereof wherein R.sup.8 and R.sup.9 are the same or different and each represents hydroxy, or protected hydroxy.
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公开(公告)号：US4245089A
公开(公告)日：1981-01-13
申请号：US6435
申请日：1979-01-25
IPC分类号： C07D265/02 , C07D498/04 , C07D265/12
CPC分类号： C07D265/02
摘要： Compounds of the formula (III): ##STR1## wherein R.sub.1 is alkyl of up to 3 carbon atoms and R.sub.2 is alkyl of up to 3 carbon atoms optionally joined to R.sub.1 so that R.sub.1 and R.sub.2 and the carbon atom to which they are attached form a spiro-cyclopentyl or spiro-cyclohexyl ring, and wherein the configuration about the .beta.-lactam ring is trans, are useful in the preparation of antibacterial .beta.-lactam compounds.A process for the preparation of the compounds of the formula (III), is also desired.
摘要翻译： 式（III）的化合物：其中R 1是至多3个碳原子的烷基，R 2是至多3个碳原子的烷基，其任选地连接到R 1上，使得R 1和R 2及它们的碳原子 连接形成螺 - 环戊基或螺环己基环，并且其中关于β-内酰胺环的构型是反式的，可用于制备抗细菌β-内酰胺化合物。 还需要制备式（III）化合物的方法。
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3.发明授权3-(2'-Tetrahydropyr anylmethyl)-7-(2-thienylacetamido)-3-cephem-4-carboxylic acid and non-toxic salts thereof 失效3-（2- {40-四氢吡喃基甲基）-7-（2-噻吩乙酰氨基）-3-头孢烯-4-羧酸及其无毒盐
公开(公告)号：US3959267A
公开(公告)日：1976-05-25
申请号：US501961
申请日：1974-08-30
IPC分类号： C07D205/095 , C07D501/10 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/56 , C07F9/568
CPC分类号： C07D205/095 , C07F9/5683
摘要： This invention relates to novel substituted ceph-3-ems some of which are of value as intermediates in the synthesis of antimicrobially active cephalosporin analogues whilst others are useful as antimicrobial agents in their own right. The invention is described in Part D of this specification. Parts A, B, C and E relate to starting materials and processes necessary for the preparation of the novel cephems.
摘要翻译： 本发明涉及新型取代的ceph-3-ems，其中一些在抗微生物活性头孢菌素类似物的合成中具有价值作为中间体，而其它可以作为抗微生物剂本身是有用的。 本发明在本说明书的D部分中描述。 部分A，B，C和E涉及新型头皮的制备所需的起始材料和工艺。
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4.发明授权
公开(公告)号：US4401595A
公开(公告)日：1983-08-30
申请号：US312658
申请日：1981-10-19
IPC分类号： C07D205/08 , C07D205/12 , C07D477/08 , C07F9/535 , C07F9/54 , C07F9/568 , C07F9/6561 , C07D487/04
CPC分类号： C07F9/5683 , C07D205/08 , C07D205/12 , C07D477/08 , C07F9/5352 , C07F9/5442 , C07F9/65613
摘要： Compounds are provided of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group and A.sub.1 is a hydrogen atom or a methyl group. These compounds possess antibacterial activity. The preparation of these compounds is described.
摘要翻译： 化合物由式（II）提供：其中R 1是使CO 2 R 1是酯基并且A 1是氢原子或甲基的基团。 这些化合物具有抗菌活性。 描述了这些化合物的制备。
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公开(公告)号：US4350703A
公开(公告)日：1982-09-21
申请号：US222282
申请日：1981-01-05
IPC分类号： C07D205/08 , C07D205/12 , C07D477/08 , C07F9/535 , C07F9/54 , C07F9/568 , C07F9/6561 , C07D487/04 , A61K37/40
CPC分类号： C07F9/5352 , C07D205/08 , C07D205/12 , C07D477/08 , C07F9/5442 , C07F9/5683 , C07F9/65613
摘要： Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.
摘要翻译： 化合物描述为式（II）：其中R 1是使CO 2 R 1是酯基的基团; A1是氢原子; A2为基团CR2R3R4，其中R2为氢原子或羟基; R3是氢原子或低级烷基; R4为氢原子或低级烷基，苄基，苯基或与R3结合形成C5-7羧酸环的一部分，或为式CH（OH）R5或CHX的基团，其中R5 是氢原子或低级烷基，X是氧原子或其中R6是氢原子或低级烷基，苯基，CN，CO2R8的CR6R7基团，其中R8是低级烷基，苯基或苄基，R7是氢 原子或低级烷基，或者连接到R6以形成C5-7碳环的一部分。 已经发现这些化合物具有抗菌性质。 描述了这些化合物的制备。
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公开(公告)号：US4521337A
公开(公告)日：1985-06-04
申请号：US475247
申请日：1983-03-14
申请人： Robert Southgate , Pamela Brown
发明人： Robert Southgate , Pamela Brown
IPC分类号： C07D507/04 , A61K31/535 , A61P31/04 , C07C29/62 , C07C31/36 , C07D265/06 , C07D265/14 , C07D265/16 , C07D498/04 , C07D507/06 , C07D507/08
CPC分类号： C07D265/14 , C07C247/00 , C07C29/62 , C07C31/36 , C07D265/06
摘要： A process for the preparation of a compound of the formulae (Ia) and/or (Ib): ##STR1## wherein R.sup.1 and R.sup.2 are independently substituted or unsubstituted hydrocarbon groups or are joined together so as to form a carbocyclic or heterocyclic ring, and R.sup.3 is a substituted or unsubstituted hydrocarbon group; which process comprises the ring-closing cyclization of a compound of the formula (II): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in relation to formulae (Ia) and (Ib).
摘要翻译： 制备式（Ia）和/或（Ib）化合物的方法：其中R 1和R 2独立地是取代或未取代的烃基或连接在一起以形成碳环或杂环，以及 R3是取代或未取代的烃基; 该方法包括式（II）化合物的闭环环化：其中R 1，R 2和R 3如关于式（Ia）和（Ib）所定义）。
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7.发明授权.beta.-Lactam antibiotics, a process for their preparation and their use in pharmaceutical compositions 失效β-内酰胺抗生素，其制备方法及其在药物组合物中的应用
公开(公告)号：US4263314A
公开(公告)日：1981-04-21
申请号：US4891
申请日：1979-01-19
IPC分类号： C07D477/04 , C07D477/20 , A61K31/40 , C07D487/04
CPC分类号： C07D477/20 , C07D477/04
摘要： The present invention provides the antibacterial agents of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is a carboxylic acid group or a salt thereof or is a group of the formula CO.sub.2 R.sub.1.sup.1 wherein R.sub.1.sup.1 is a group such that CO.sub.2 R.sub.1.sup.1 is an ester group, R.sub.2 is a hydrogen atom or a lower alkyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a phenyl group or a phenyl group substituted by one or two groups selected from fluorine, chlorine, OR.sub.5, NH.CO.R.sub.5, NH.CO.sub.2 R.sub.5 or CO.sub.2 R.sub.5 where R.sub.5 is a lower alkyl or benzyl group.A process for their preparation and their use in pharmaceutical compositions is also described.
摘要翻译： 本发明提供式（II）的抗菌剂：其中R 1是CO 2 R 1是羧酸基或其盐的基团，或者是式CO 2 R 11的基团，其中R 11是这样的基团，使得CO 2 R 11 是酯基，R2是氢原子或低级烷基; R3是氢原子或低级烷基; R 4是苯基或被一个或两个选自氟，氯，OR 5，NH.CO.R 5，NH.CO 2 R 5或CO 2 R 5的基团取代的苯基，其中R 5是低级烷基或苄基。 还描述了其制备方法及其在药物组合物中的应用。
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公开(公告)号：US4446146A
公开(公告)日：1984-05-01
申请号：US59463
申请日：1979-07-20
IPC分类号： C07D205/08 , C07D265/06 , C07D265/14 , C07D477/04 , C07D477/20 , C07F7/00 , C07F7/10 , C07F9/568 , A61K31/40 , C07D487/04
CPC分类号： C07D477/20 , C07D205/08 , C07D265/06 , C07D265/14 , C07D477/04 , C07F7/00 , C07F7/10 , C07F9/5683 , Y02P20/55
摘要： The compounds of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is a carboxylic acid group or a salt or ester thereof; R.sub.2 is a group of the sub-formula (a) or (b):--CR.sub.4 .dbd.C(R.sub.5) NH.CO.sub.n R.sub.6 (a)--CR.sub.7 .dbd.C(R.sub.8)R.sub.9 (b)wherein R.sub.4 is a hydrogen atom or a lower alkyl group; R.sub.5 is a hydrogen atom or a lower alkyl group; R.sub.6 is a lower alkyl, phenyl, fluorophenyl, chlorophenyl, bromophenyl or benzyl group; and n is 1 or 2; R.sub.7 is a hydrogen or a lower alkyl group; R.sub.8 is a hydrogen atom or a lower alkyl group; R.sub.9 is a hydrogen atom or a lower alkyl or phenyl group; R.sub.3 is a group of the sub-formula (c):CR.sub.10 R.sub.11 R.sub.12 (c)wherein R.sub.10 is a hydrogen atom or a hydroxyl or O.CO.R.sub.13 or O.CO.OR.sub.13 group where R.sub.13 is a lower alkyl, phenyl, benzyl, fluorobenzyl, chlorobenzyl, bromobenzyl, lower alkoxybenzyl or nitrobenzyl group; R.sub.11 is a hydrogen atom or a lower alkyl group; R.sub.12 is a hydrogen atom or a lower alkyl group; said compounds being in the form of R,S-mixture at C-5: are antibacterial agents. Their use and a process for their preparation is described.
摘要翻译： 式（II）的化合物：其中R1是使CO 2 R 1是羧酸基团或其盐或酯的基团; R2是亚式（a）或（b）的基团：-CR4 = C（R5）NH.COnR6（a）-CR7 = C（R8）R9（b）其中R4是氢原子或低级 烷基; R5是氢原子或低级烷基; R6是低级烷基，苯基，氟苯基，氯苯基，溴苯基或苄基; n为1或2; R7是氢或低级烷基; R8是氢原子或低级烷基; R9是氢原子或低级烷基或苯基; R3是下式（c）的基团：CR10R11R12（c）其中R10是氢原子或羟基或O.CO.R13或O.CO.OR13基团，其中R13是低级烷基，苯基，苄基， 氟苄基，氯苄基，溴苄基，低级烷氧基苄基或硝基苄基; R 11是氢原子或低级烷基; R12是氢原子或低级烷基; 所述化合物是C-5的R，S-混合物的形式：是抗菌剂。 描述了它们的用途及其制备方法。
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公开(公告)号：US4431587A
公开(公告)日：1984-02-14
申请号：US330656
申请日：1981-12-14
IPC分类号： C07D205/08 , C07D205/12 , C07D477/08 , C07F9/535 , C07F9/54 , C07F9/568 , C07F9/6561 , C07D487/04 , A61K31/40 , C07D403/12
CPC分类号： C07F9/5352 , C07D205/08 , C07D205/12 , C07D477/08 , C07F9/5442 , C07F9/5683 , C07F9/65613
摘要： Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.
摘要翻译： 化合物描述为式（II）：其中R 1是使CO 2 R 1是酯基的基团; A1是氢原子; A2为基团CR2R3R4，其中R2为氢原子或羟基; R3是氢原子或低级烷基; R4为氢原子或低级烷基，苄基，苯基或与R3结合形成C5-7羧酸环的一部分，或为式CH（OH）R5或CHX的基团，其中R5 是氢原子或低级烷基，X是氧原子或其中R6是氢原子或低级烷基，苯基，CN，CO2R8的CR6R7基团，其中R8是低级烷基，苯基或苄基，R7是氢 原子或低级烷基，或者连接到R6以形成C5-7碳环的一部分。 已经发现这些化合物具有抗菌性质。 描述了这些化合物的制备。
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公开(公告)号：US4428961A
公开(公告)日：1984-01-31
申请号：US227765
申请日：1981-01-23
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04 , C07C271/22 , C07D477/20 , C07F9/568
CPC分类号： C07D477/20 , C07C271/22 , C07F9/5683
摘要： The present invention provides a compound of formula (I): ##STR1## wherein R.sup.1 is a group such that COOR.sup.1 is a carboxyic acid group or a salt or ester thereof;R.sup.3 is hydrogen or an organic radical;n is zero or 1;R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.3 alkyl;X is C.sub.1 -C.sub.6 alkylene optionally substituted by hydroxy or a carboxylic acid group or a salt or ester thereof;Y is an amino, or substituted amino, wherein the substituent is carboxylic acyl, C.sub.1 -C.sub.6 alkyl or a group .dbd.C(R.sup.14)NR.sup.15 R.sup.16 wherein R.sup.15 and or C.sub.1 -C.sub.6 alkyl and R.sup.14 is hydrogen or C.sub.1 -C.sub.6 alkyl, or a group --NR.sup.A R.sup.B wherein R.sup.A and R.sup.B are independently hydrogen or C.sub.1 -C.sub.6 alkyl.
摘要翻译： 本发明提供式（I）化合物：其中R 1为COOR 1为羧酸基或其盐或酯的基团; R3是氢或有机基团; n为零或1; R4和R5独立地是氢或C1-C3烷基; X是任选被羟基或羧酸基团取代的C 1 -C 6亚烷基或其盐或酯; Y是氨基或取代的氨基，其中取代基是羧酰基，C 1 -C 6烷基或基团= C（R 14）NR 15 R 16，其中R 15和/或C 1 -C 6烷基和R 14是氢或C 1 -C 6烷基，或 基团-NRA RB，其中RA和RB独立地是氢或C 1 -C 6烷基。
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