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公开(公告)号:US5994307A
公开(公告)日:1999-11-30
申请号:US203388
申请日:1998-12-02
申请人: Laszlo Vertesy , Martin Knauf , Joachim Wink , Dieter Isert , Wilhelm Stahl , Gunther Riess , Jozsef Aszodi , Dominique Le Beller
发明人: Laszlo Vertesy , Martin Knauf , Joachim Wink , Dieter Isert , Wilhelm Stahl , Gunther Riess , Jozsef Aszodi , Dominique Le Beller
IPC分类号: C12P1/06 , A61K38/00 , A61P31/00 , C07K7/08 , C12N1/20 , C12P21/02 , C12R1/465 , C12R1/645 , A61K38/02 , C07K5/00 , C07K7/00
摘要: This invention relates to the antibiotic feglymycin, as well as processes for its preparation and use. Feglymycin is represented by the structural formula (SEQ. ID. NO. 1) ##STR1##
摘要翻译: 本发明涉及抗生素feglymycin,以及其制备和应用的方法。 铁氰霉素由结构式(SEQ ID NO:1)表示,
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公开(公告)号:US08178554B2
公开(公告)日:2012-05-15
申请号:US13068399
申请日:2011-05-10
IPC分类号: A61K31/44 , C07D498/02
CPC分类号: C07D487/08
摘要: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.
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公开(公告)号:US07612087B2
公开(公告)日:2009-11-03
申请号:US10898754
申请日:2004-07-26
IPC分类号: A61K31/44 , A61K31/545
CPC分类号: A61K31/439 , A61K31/55 , A61K2300/00
摘要: This invention discloses and claims methods for inhibiting bacterial β-lactamases and treating bacterial infections by inhibiting bacterial β-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a β-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a β-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed.
摘要翻译: 本发明公开并要求通过抑制人或动物中的细菌β-内酰胺酶抑制细菌β-内酰胺酶和治疗细菌感染的方法,包括向所述人或所述动物施用治疗有效量的化合物或其药学上可接受的盐 式(I)单独或与β-内酰胺抗生素组合,其中所述组合可以分开施用,一起或随时间隔开。 还公开和要求保护包含式(I)化合物或式(I)化合物与治疗有效量的β-内酰胺抗生素和药学上可接受的载体的组合物的药物组合物。
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公开(公告)号:US20090215747A1
公开(公告)日:2009-08-27
申请号:US12434270
申请日:2009-05-01
IPC分类号: A61K31/55
CPC分类号: A61K31/439 , A61K31/55 , A61K2300/00
摘要: This invention discloses and claims methods for inhibiting bacterial β-lactamases and treating bacterial infections by inhibiting bacterial β-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a β-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a β-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed.
摘要翻译: 本发明公开并要求通过抑制人或动物中的细菌β-内酰胺酶抑制细菌β-内酰胺酶和治疗细菌感染的方法,包括向所述人或所述动物施用治疗有效量的化合物或其药学上可接受的盐 式(I)单独或与β-内酰胺抗生素组合,其中所述组合可以分开施用,一起或随时间隔开。 还公开和要求保护包含式(I)化合物或式(I)化合物与治疗有效量的β-内酰胺抗生素和药学上可接受的载体的组合物的药物组合物。
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公开(公告)号:US5710147A
公开(公告)日:1998-01-20
申请号:US499168
申请日:1995-07-07
申请人: Jozsef Aszodi , Patrick Fauveau
发明人: Jozsef Aszodi , Patrick Fauveau
IPC分类号: C07D501/56 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/24 , C07F9/40 , C07F9/553 , C07F9/6539 , C07F9/6561
CPC分类号: C07F9/6539 , C07D501/00 , C07F9/4056 , C07F9/5537 , C07F9/65613
摘要: The syn isomer of (R) or (S) or (R,S) mixture, in the form of internal salts or salts with acids or bases of a compound of the formula ##STR1## wherein the substituents are defined as in the specification having a very good antibiotic activity.
摘要翻译: (R)或(S)或(R,S)混合物的顺式异构体以内部盐形式或与酸或碱的盐形式,其中取代基如在说明书中所定义 具有非常好的抗生素活性。
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公开(公告)号:US4425358A
公开(公告)日:1984-01-10
申请号:US370503
申请日:1982-04-21
申请人: Csaba Szantay , Lajos Novak , Jozsef Aszodi , Vilmos Simonidesz , Geza Galambos , Gabor Kovacs , Sandor Virag , Istvan Stadler , Peter Kormoczy
发明人: Csaba Szantay , Lajos Novak , Jozsef Aszodi , Vilmos Simonidesz , Geza Galambos , Gabor Kovacs , Sandor Virag , Istvan Stadler , Peter Kormoczy
IPC分类号: C07D307/935 , A61K31/557 , A61P7/02 , A61P9/12 , C07C405/00 , C07D307/937 , C07D407/12
CPC分类号: C07D307/937 , C07C405/0033 , C07D407/12 , Y10S514/822
摘要: The invention relates to new optically active or racemic 13-thia-prostacycline derivatives of the Formula I ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation or a straight or branched chain alkyl group having 1-5 carbon atoms;R.sup.2 is straight or branched chain alkyl having 4-9 carbon atoms or monosubstituted phenoxymethyl;--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- of Z-- or E-- configuration or --C.tbd.C--;one of the symbols X and Y is hydrogen, methyl or ethyl and the other is hydroxy, tetrahydropyranyoxy, 1-ethoxy-ethoxy or trialkylsilyloxy; orX and Y together form a --O--CH.sub.2 --CH.sub.2 --O-- group;Z is a sulfur atom or a --SO-- group.The compounds of the Formula I can be prepared by reacting a 13-thia-prostaglandine of the Formula III ##STR2## if desired after oxidation into the corresponding 13-oxide derivative--with a halogenating agent; and treating the 5-halogeno-13-thia-prostacycline of the Formula II ##STR3## thus obtained wherein E is halogen with an organic or inorganic base; and thereafter if desired removing the protecting groups X and/or Y and if desired converting a compound of the Formula I obtained into a salt or setting free the same from a salt. The new compounds of the Formula I possess anti-coagulant and hypotensive properties and can be used in therapy.
摘要翻译: 本发明涉及式I的新的光学活性或外消旋的13-前列环素衍生物,其中R1是氢,可药用阳离子或具有1-5个碳原子的直链或支链烷基; R2是具有4-9个碳原子的直链或支链烷基或单取代的苯氧基甲基; -A-B-是Z-或E-构型的-CH 2 -CH 2 - , - CH = CH-或-C 3 D C-; 符号X和Y之一是氢,甲基或乙基,另一个是羟基,四氢吡喃基氧基,1-乙氧基 - 乙氧基或三烷基甲硅烷氧基; 或X和Y一起形成-O-CH 2 -CH 2 -O-基团; Z是硫原子或-SO-基。 式I的化合物可以通过使式III的13-前 - 前列腺素(III)反应来制备。
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