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公开(公告)号：US4060606A
公开(公告)日：1977-11-29
申请号：US693976
申请日：1976-06-08
CPC分类号： C07J31/003 , C07J13/007 , C07J41/0055 , C07J43/003
摘要： The present invention relates to a new series of fusidic acid derivatives, to salts and easily hydrolysable esters thereof, to the preparation of these compounds, and to pharmaceutical compositions containing the compounds. The new compounds have the general formula ##STR1## in which the C.sub.24-25 bond is a single or a double bond, and in which Q.sub.1 and Q.sub.2 stand for ##STR2## or oxygen; A stands for oxygen, sulphur or a sulfinyl radical; R.sub.1 stands for a straight or branched alkyl radical having from 1 to 8 carbon atoms, an alkenyl or alkynyl radical having from 2 to 6 carbon atoms, a cycloalkyl radical having from 3 to 7 carbon atoms in the alicyclic ring, an aryl or aralkyl radical, a heterocyclic radical having 5 or 6 ring atoms, and containing oxygen, sulphur or nitrogen atoms, and pharmaceutically acceptable salts and easily hydrolysable esters thereof.The compound of the present invention show interesting antimicrobial and pharmacokinetic properties. Thereby the compounds of the invention can be used in the treatment of bacterial infections in humans and animals.
摘要翻译： 本发明涉及新一系列的夫西地酸衍生物，其盐类和易水解的酯，涉及这些化合物的制备，以及含有该化合物的药物组合物。 新化合物具有通式[IMAGE] I，其中C24-25键是单键或双键，其中Q1和Q2表示
或氧; A代表氧，硫或亚硫酰基; R1表示具有1至8个碳原子的直链或支链烷基，具有2至6个碳原子的烯基或炔基，脂环中具有3至7个碳原子的环烷基，芳基或芳烷基 ，具有5或6个环原子并且含有氧，硫或氮原子的杂环基，以及其药学上可接受的盐和易于水解的酯。 -
公开(公告)号：US4119717A
公开(公告)日：1978-10-10
申请号：US806376
申请日：1977-06-14
IPC分类号： A61K31/575 , A61K31/58 , A61P31/04 , C07J13/00 , C07J31/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J51/00 , A61K31/56
CPC分类号： C07J41/0027 , C07J13/007 , C07J31/003 , C07J31/006 , C07J33/002 , C07J41/0005 , C07J43/003 , C07J51/00
摘要： The present invention relates to a new series of fusidic acid derivatives, to salts and easily hydrolysable esters thereof, to the preparation of these compounds, and to pharmaceutical compositions containing the compounds, the new fusidic acid derivatives having the general formula: ##STR1## in which the dotted line between C-24 and C-25 indicates that the carbon atoms in question are connected by either a double bond or a single bond, and in which Q.sub.1 represents oxygen or one of the groupings ##STR2## Z being a hydroxy group, a halogen atom, an alkylsulfonyloxy or arylsulfonyloxy group, such as methanesulfonyloxy or p-toluenesulfonyloxy, an azido or a nitro group, Q.sub.2 is oxygen or the grouping ##STR3## and R.sub.1 stands for a straight or branched alkyl radical having from 1 to 6 carbon atoms, such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl or the known isomers of pentyl and hexyl, a phenyl or a heterocyclyl radical having 5 to 6 ring atoms and containing nitrogen, oxygen and/or sulfur atoms, these radicals being optionally substituted with halogen, nitro, lower alkyl or lower alkoxy radicals.The present compounds show both in vitro and in vivo interesting antimicrobial and pharmacokinetic properties.
摘要翻译： 本发明涉及新的一系列夫西地酸衍生物，其盐和易于水解的酯，以及这些化合物的制备，以及含有这些化合物的药物组合物，具有以下通式的新的夫西地酸衍生物： 其中C-24和C-25之间的虚线表示所讨论的碳原子通过双键或单键连接，并且其中Q1表示氧或基团中的一个作为羟基 基团，卤素原子，烷基磺酰氧基或芳基磺酰氧基，例如甲磺酰氧基或对甲苯磺酰氧基，叠氮基或硝基，Q 2是氧或分组，并且具有1至6个直链或支链烷基的R1st 碳原子，例如甲基，乙基，丙基，异丙基，丁基，异丁基，叔丁基或已知的戊基和己基异构体，苯基或具有5至6个环原子并含有氮的杂环基，氧化 n和/或硫原子，这些基团任选被卤素，硝基，低级烷基或低级烷氧基取代。
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公开(公告)号：US4100276A
公开(公告)日：1978-07-11
申请号：US744978
申请日：1976-11-24
IPC分类号： C07J9/00 , A61K31/575 , A61P31/04 , C07J13/00 , C07J17/00 , C07J31/00 , C07J41/00 , C07J51/00 , A61K31/56
CPC分类号： C07J51/00 , C07J13/00 , C07J31/003 , C07J41/0088
摘要： The invention relates to a new series of fusidic acid derivatives, to salts and easily hydrolyzable esters thereof, to the preparation of these compounds and to pharmaceutical compositions containing the compounds, the new compounds having the general formula: ##STR1## in which Q.sub.1 and Q.sub.2 stand for the group ##STR2## or oxygen, A represents oxygen or sulphur, and R.sub.1 stands for a straight or branched alkyl radical having from 1 to 12 carbon atoms, R.sub.1 can further be an alkenyl or alkynyl radical having from 3 to 6 carbon atoms, a cycloalkyl radical having from 3 to 7 carbon atoms in the alicyclic ring, an aralkyl or aryl radical, R.sub.1 can also be a heterocyclic radical having 5 or 6 ring atoms and containing oxygen, sulphur and/or nitrogen atoms, R.sub.1 optionally being further substituted, and in which formula I the dotted line between C-24 and C-25 indicates that the carbon atoms in question are connected by either a double bond or a single bond, and the asterix at C-20 indicates that the compounds exist in two diastereomeric forms, and thus the invention comprises the pure diastereomers as well as mixtures of these.The compounds of the present invention possess antibacterial properties and show further interesting antimicrobial and pharmacokinetic properties.
摘要翻译： 本发明涉及新的一系列夫西地酸衍生物，其盐和容易水解的酯，用于制备这些化合物和含有该化合物的药物组合物，具有以下通式的新化合物：其中Q1和 Q2代表组
或氧，A表示氧或硫，R1表示具有1至12个碳原子的直链或支链烷基，R1可以进一步为具有3-6个碳原子的烯基或炔基 原子，脂环中具有3至7个碳原子的环烷基，芳烷基或芳基，R 1也可以是具有5或6个环原子并含有氧，硫和/或氮原子的杂环基，R 1可任选地为 并且其中式I中C-24和C-25之间的虚线表示所讨论的碳原子通过双键或单键连接，C-20处的星号表示com 磅以两种非对映体形式存在，因此本发明包括纯非对映异构体以及它们的混合物。 -
公开(公告)号：US06593319B1
公开(公告)日：2003-07-15
申请号：US09787539
申请日：2001-08-14
申请人： Tore Duvold , Welf von Daehne
发明人： Tore Duvold , Welf von Daehne
IPC分类号： A61K3170
摘要： Novel 17,20-dihydrofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.
摘要翻译： 新颖的17,20-二氢富马酸衍生物用于治疗感染的药物组合物中，特别是用于治疗皮肤或眼睛感染的局部组合物中。
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5.发明授权Antibacterial beta-lactams, pharmaceuticals thereof and methods of using them 失效抗菌β-内酰胺类，其药物和使用它们的方法
公开(公告)号：US4840944A
公开(公告)日：1989-06-20
申请号：US118063
申请日：1980-01-24
IPC分类号： A61K31/43 , C07D20060101 , C07D498/04 , C07D499/00 , C07D499/21 , C07D499/32 , C07D499/42 , C07D499/64 , C07D499/66 , C07D499/68 , C07D499/70 , C07D499/72 , C07D499/74 , C07D503/00 , C07D519/00
CPC分类号： C07D503/00 , C07D499/00
摘要： The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R.sub.1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R.sub.2 represents a primary amino or a carboxy group; R.sub.3 is a hydrogen atom, or a lower alkyl, aryl or aralkyl radical, and A stands for a radical of a .beta.-lactamase inhibitor containing a .beta.-lactam ring as well as a carboxy group, A being connected via the carboxy group.The present invention provides new compounds useful in the treatment of bacterial infections. The new compounds are in particular strongly active against .beta.-lactamase producing bacteria.
摘要翻译： 本发明涉及迄今未知的通式Ⅰ化合物：其中R1代表苯基，4-羟基苯基，1,4-环己二烯基或3-噻吩基; R2表示伯氨基或羧基; R3是氢原子或低级烷基，芳基或芳烷基，A代表含有β-内酰胺基的羧基的羧基，A通过羧基连接。 本发明提供了可用于治疗细菌感染的新化合物。 新化合物特别对β-内酰胺酶生产细菌具有强烈的活性。
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公开(公告)号：US4407751A
公开(公告)日：1983-10-04
申请号：US291081
申请日：1981-08-07
IPC分类号： C07D499/00 , C07D499/32 , C07D503/00 , C07D519/00 , C07D499/04
CPC分类号： C07D503/00 , C07D499/00
摘要： The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R.sub.1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R.sub.2 represents a primary amino or a carboxy group; R.sub.3 is a hydrogen atom, or a lower alkyl, aryl or aralkyl radical, and A stands for a radical of a .beta.-lactamase inhibitor containing a .beta.-lactam ring as well as a carboxy group, A being connected via the carboxy group.The present invention provides new compounds useful in the treatment of bacterial infections. The new compounds are in particular strongly active against .beta.-lactamase producing bacteria.
摘要翻译： 本发明涉及迄今未知的通式Ⅰ化合物：其中R1代表苯基，4-羟基苯基，1,4-环己二烯基或3-噻吩基; R2表示伯氨基或羧基; R3是氢原子或低级烷基，芳基或芳烷基，A代表含有β-内酰胺基的羧基的羧基，A通过羧基连接。 本发明提供了可用于治疗细菌感染的新化合物。 新化合物特别对β-内酰胺酶生产细菌具有强烈的活性。
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公开(公告)号：US06399797B1
公开(公告)日：2002-06-04
申请号：US09543418
申请日：2000-04-05
申请人： Welf von Daehne , Gunnar Grue-Sørensen , Martin John Calverley , Claus Aage Svensgaard Bretting
发明人： Welf von Daehne , Gunnar Grue-Sørensen , Martin John Calverley , Claus Aage Svensgaard Bretting
IPC分类号： C07C40100
CPC分类号： C07C401/00
摘要： The present invention relates to compounds of formula (I), in which formula X is hydrogen or hydroxy or protected hydroxy; R1 an R2 stand for hydrogen, methyl or ethyl, or, when taken together with the carbon atom bearing the group X, R1 and R2 can form a C3-C5 carbocyclic ring; Q is a C3-C6 hydrocarbylene, hydrocarbylene indicating the diradical obtained after removal of 2 hydrogen atoms for a straight or banched, saturated or unsaturated hydrocarbon, in which one of any CH2 groups may optionally be replaced by an oxygen atom or a carbonyl group, such that the carbon atom (C-22) directly bonded to C-20 is an sp2 or sp3 hybridized carbon atom, i.e. bonded to 2 or 3 other atoms; and in which another of the CH2 groups may be replaced by phenylene, and where Q may optionally be substituted with one or more hydroxy or C1-C4-alkoxy groups. These compounds have been discovered to possess exceptionally high immunosuppressive activites together with high tumour cell proliferation inhibiting activities.
摘要翻译： 本发明涉及式（I）化合物，其中式X为氢或羟基或被保护的羟基; R1，R2代表氢，甲基或乙基，或者当与带有基团X的碳原子一起时，R 1和R 2可以形成C 3 -C 5碳环; Q是C3-C6亚烃基，表示在去除2个氢原子之后获得的直链或带有饱和或不饱和烃的二价基团，其中任何一个CH 2基团可以任选被氧原子或羰基取代， 使得直接键合到C-20的碳原子（C-22）是sp2或sp3杂化的碳原子，即键合到2或3个其它原子; 并且其中另一个CH 2基团可以被亚苯取代，并且其中Q可以任选地被一个或多个羟基或C 1 -C 4 - 烷氧基取代。 已经发现这些化合物具有特别高的免疫抑制活性以及高肿瘤细胞增殖抑制活性。
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公开(公告)号：US4446144A
公开(公告)日：1984-05-01
申请号：US207614
申请日：1980-11-17
申请人： Welf von Daehne
发明人： Welf von Daehne
IPC分类号： A61K31/425 , A61K31/43 , A61P31/04 , A61P43/00 , C07D499/00 , C07D499/26 , C07D499/32 , C07D499/68 , C07D499/86 , C07D499/87 , C07D499/893 , C07D499/897 , C12N9/99 , C07D499/08
CPC分类号： C07D499/00
摘要： This invention relates to penicillanic acid derivatives of the formula I ##STR1## in which X stands for chlorine, bromine or iodine, to pharmaceutically acceptable, non-toxic salts of the compounds of formula I, to pharmaceutically acceptable, easily hydrolyzable esters thereof, including salts of such esters, to pharmaceutical compositions containing the compounds of the invention and dosage units thereof, to methods for the preparation of the compounds of the invention, and to methods of using the said new compounds in the human and veterinary therapy.The 6.beta.-halopenicillanic acids of formula I are potent inhibitors of .beta.-lactamases from a variety of gram-positive and gram-negative bacteria, making the 6.beta.-halopenicillanic acids as well as their salts and easily hydrolyzable esters valuable in human and veterinary medicine.
摘要翻译： 本发明涉及式I的青霉烷酸衍生物，其中X代表氯，溴或碘，以及式I化合物的药学上可接受的无毒盐，其药学上可接受的，易水解的酯， 包括这些酯的盐，含有本发明化合物的药物组合物及其剂量单位，以及制备本发明化合物的方法，以及在人和兽医疗法中使用所述新化合物的方法。 式I的6个β-卤代青霉烷酸是来自多种革兰氏阳性和革兰氏阴性细菌的β-内酰胺酶的有效抑制剂，使6β-卤代青霉烷酸及其盐和容易水解的酯在人和兽医中有价值 医学。
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9.发明授权6-Amidinopenicillanic acid derivatives including the radical of a .beta.-lactamase inhibitor 失效包括β-内酰胺酶抑制剂基团的6-脒基青霉烷酸衍生物
公开(公告)号：US4325960A
公开(公告)日：1982-04-20
申请号：US116651
申请日：1980-01-29
IPC分类号： C07D499/80 , A61K31/431 , A61P31/04 , C07D499/00 , C07D499/21 , C07D499/32 , C07D499/42 , C07D503/00 , C07D519/00
CPC分类号： C07D503/00 , C07D499/00
摘要： The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R.sub.1 stands for a five- to ten-membered azacycloalkyl or azabicycloalkyl residue attached via the nitrogen atom and optionally being substituted by one or two, the same or different, lower alkyl groups; R.sub.2 represents a hydrogen atom or a lower alkyl, aryl, or aralkyl radical; and A represents a radical of a .beta.-lactamase inhibitor containing a .beta.-lactam ring as well as a carboxy group, A being connected via the carboxy group.The present compounds are useful in the treatment of bacterial infections. The new compounds are in particular strongly active against .beta.-lactamase producing bacteria.
摘要翻译： 本发明涉及迄今为止未知的通式I化合物：其中R1代表通过氮原子连接并任选被一个或两个相同的5至10元氮杂环烷基或氮杂双环烷基取代的相同 或不同的低级烷基; R2表示氢原子或低级烷基，芳基或芳烷基; 而A代表含有β-内酰胺环以及羧基的β-内酰胺酶抑制剂的基团，A通过羧基连接。
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公开(公告)号：US4315004A
公开(公告)日：1982-02-09
申请号：US44163
申请日：1979-05-31
申请人： Welf von Daehne , Poul R. Rasmussen
发明人： Welf von Daehne , Poul R. Rasmussen
IPC分类号： C07J9/00 , A61K31/575 , A61P31/04 , C07J13/00 , C07J17/00 , C07J31/00 , C07J41/00 , C07J51/00 , A01N45/00 , A61K31/56
CPC分类号： C07J51/00 , C07J13/00 , C07J31/003 , C07J41/0088
摘要： A method for treating arthritis which comprises administering to a subject in need of such treatment an effective amount of a fusidic acid derivative selected from compounds of the formula I: ##STR1## in which R.sub.1 stands for a straight or branched alkyl radical having from 1 to 12 carbon atoms, and pharmaceutically acceptable, non-toxic salts and easily hydrolyzable esters thereof, and salts of such esters. The pure diastereomers as well as mixtures thereof may be used in carrying out the invention.
摘要翻译： 一种治疗关节炎的方法，其包括向需要这种治疗的受试者施用有效量的选自式I化合物的夫西地酸衍生物：其中R 1表示具有1个直链或支链烷基的直链或支链烷基 至12个碳原子，以及其药学上可接受的无毒盐和易于水解的酯，以及这些酯的盐。 纯的非对映体及其混合物可用于实施本发明。
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