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公开(公告)号：EP0597303A2
公开(公告)日：1994-05-18
申请号：EP93117216.7
申请日：1993-10-23
IPC分类号： C07D501/46 , C07D501/40 , A61K31/545
CPC分类号： C07D501/00
摘要： Cephalosporin derivatives of the general formula
in which R represents one of the groups
and
and the corresponding readily hydrolyzable, pharmaceutically acceptable esters and the pharmaceutically acceptable salts and hydrates of these compounds as well as a process for their manufacture and pharmaceutical preparations which contain these compounds, furthermore the use of the compounds in the control of illnesses and for the manufacture of the aforementioned preparations.摘要翻译： 其中R代表其中一个基团
的相应易溶于水的可药用酯类和这些化合物的药学上可接受的盐和水合物的头孢菌素衍生物及其制备方法和药物制剂 其含有这些化合物，此外，化合物在控制疾病和制备上述制剂中的应用。 -
公开(公告)号：EP0550775A1
公开(公告)日：1993-07-14
申请号：EP92100119.4
申请日：1992-01-07
IPC分类号： C07D501/46 , C07D501/42 , A61K31/545 , C07D501/44
CPC分类号： C07D501/00
摘要： Cephalosporin derivatives of the general formula
in which R³ is a group of the formula
R⁶⁰ and R⁶⁵ are hydrogen or lower alkyl, R¹⁵-R¹⁹ are each independently hydrogen, halogen or hydroxy, n is zero or 1, R⁴ and R⁵ are each hydrogen, halogen, lower alkyl, lower alkoxy or amino, R⁷ is hydrogen or lower alkyl and R⁸ is lower alkyl, halo- lower alkyl, C₃-C₇ cycloalkyl or mono-, di- or trihalophenyl, and Z is N or C-R⁹, where R⁹ is hydrogen, halogen, lower alkyl or lower alkoxy; and, when R⁴ is fluoro, R⁵ and R⁷ are hydrogen. R⁸ is cyclopropyl and Z is C-H, R³ can also be one of the groups
in which R⁶¹ and R⁶⁶ are hydrogen or methyl, R¹⁵-R¹⁹ are as above and R⁹⁰ is hydrogen, hydroxy, carboxy, amino or [[4-(lower alkyl)-2,3-dioxo-1-piperazinyl]carbonyl]amino;
pharmaceutically acceptable acid or base addition salts thereof, hydrates of compounds of formula I and hydrates of such salts.
The products have antibacterial activity.摘要翻译： 通式
的头孢菌素衍生物，其中R 3为式CHEM R 6和O 6的基团是氢或低级烷基，R 1， R 5 -R 9各自独立地为氢，卤素或羟基，n为0或1，R 4和R 5各自为氢，卤素，低级烷基，低级烷氧基或氨基， R 7是氢或低级烷基，R 8是低级烷基，卤代低级烷基，C 3 -C 7环烷基或单 - ，二 - 或三卤代苯基，Z是N或CR 9，其中R 9是 氢，卤素，低级烷基或低级烷氧基; 当R 4为氟时，R 5和R 7为氢。 R 8是环丙基，Z是CH，R 3也可以是其中R 6'和R 6'是氢或甲基的基团 ，R 1 R 5和R 9如上所述，R 9是氢，羟基，羧基，氨基或[[4-（低级烷基）-2,3-二氧代-1-哌嗪基 ]羰基]氨基; 其药学上可接受的酸或碱加成盐，式I化合物的水合物和这些盐的水合物。 该产品具有抗菌活性。 -
公开(公告)号：EP0409081A1
公开(公告)日：1991-01-23
申请号：EP90113352.0
申请日：1990-07-12
IPC分类号： C07D499/02 , C07D501/16 , C07D519/00 , C07D205/085 , C07D401/02 , C07D403/02 , A61K31/43 , A61K31/545 , A61K31/395 , A61K31/47
CPC分类号： C07D401/12 , C07D205/085 , C07D499/00 , C07D501/00
摘要： β-Lactam compounds of the formula
in which R₁ is a cyclic or secondary acyclic amino group which independently has antibacterial activity;
R₂ is hydrogen, lower alkoxy, lower alkylthio or formamido;
R₃ is hydrogen or an organic group bonded through carbon, oxygen, sulfur or nitrogen;
R₄ is an electronegative acidic group; or R₃ and R₄ together form a heterocycle; and
R₅ is hydrogen or lower alkyl, except when R₃ and R₄ form a heterocycle, in which case R₅ is hydrogen only;
and readily hydrolyzable esters and pharmaceutically acceptable salts of these compounds, and hydrates of any of the foregoing.
The products have antibacterial activity.摘要翻译： 式（CHEM）的β-内酰胺化合物，其中R1是独立地具有抗菌活性的环状或次级无环氨基; R2是氢，低级烷氧基，低级烷硫基或甲酰氨基; R3是氢或通过碳，氧，硫或氮键合的有机基团; R4是电负性酸性基团; 或R3和R4一起形成杂环; 并且R 5为氢或低级烷基，但当R 3和R 4形成杂环时，其中R 5为氢; 和这些化合物易于水解的酯和药学上可接受的盐，以及上述任何一种的水合物。 该产品具有抗菌活性。
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公开(公告)号：EP0335297A2
公开(公告)日：1989-10-04
申请号：EP89105359.7
申请日：1989-03-29
发明人： Albrecht, Harry Allen , Keith, Dennis Dalton , Konzelmann, Frederick Martin , Rossman, Pamela Loreen , Wei, Chung-Chen , Weigele, Manfred , Yang, Roxana
IPC分类号： C07D501/26 , C07D501/38 , A61K31/545
CPC分类号： C07D501/46 , C07D501/18 , C07D501/26 , C07D501/32 , C07D501/34 , C07D501/38 , C07D501/44 , C07D519/00
摘要： Beschrieben werden Acylderivate der allgemeinen Formel
in der R¹ einen substituierten N-Heterocyclus der Formeln
bedeutet, worin R¹⁰ eine der Gruppen
und Q eine substituierte Chinolinyl- oder Naphthyridinylgruppe darstellt, wobei der N-Heterocyclus gegebenenfalls durch eine oder mehrere niedere Alkylgruppen substituiert sein kann; und worin ferner R² Wasserstoff, niederes Alkoxy, niederes Alkylthio oder niederes Alkanoylamino, R³ eine Acylgruppe, m 0, 1 oder 2 und A ein pharmazeutisch verträgliches Anion darstellt,
sowie leicht hydrolysierbare Ester und pharmazeutisch verträgliche Salze dieser Verbindungen und Hydrate der Verbindungen der Formel I bzw. von deren Estern und Salzen sowie ein Verfahren zu deren Herstellung und pharmazeutische Präparate, welche diese Verbindung enthalten, ferner auch Zwischenprodukte zur Herstellung dieser Verbindungen, weiter die Verwendung der Verbindungen bei der Bekämpfung von Krankheiten und bei der Herstellung der erwähnten Präparate.
Die Produkte sind antibiotisch wirksam.摘要翻译： 通式“IMAGE”的酰基衍生物，其中R 1表示式“IMAGE”的取代的N-杂环，其中R 1表示基团之一，且表示取代的喹啉基 或萘啶基，其中N-杂环可任选被一个或多个低级烷基取代; 并且其中R 2另外表示氢，低级烷氧基，低级烷硫基或低级烷酰基氨基，R 3表示酰基，m表示0,1或2，A表示药学上可耐受的阴离子，易于水解的酯和药学上可接受的 这些化合物的可耐受盐和式I化合物或其酯和盐的水合物及其制备方法和含有该化合物的药物制剂，以及制备这些化合物的中间体，另外使用 描述了用于控制疾病和制备所述制剂的化合物。 该产品具有抗生素活性。
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5.发明授权Cephalosporinderivate, Verfahren zu ihrer Herstellung sowie entsprechende pharmazeutische Präparate 失效头孢菌素衍生物，它们的制备方法和相应的药物制剂。
公开(公告)号：EP0251330B1
公开(公告)日：1993-12-01
申请号：EP87109613.7
申请日：1987-07-03
发明人： Albrecht, Harry Allen , Chan, Ka-Kong , Keith, Dennis Dalton , Then, Rudolf Ludwig , Weigele, Manfred
IPC分类号： C07D501/34 , A61K31/545
CPC分类号： B82Y5/00 , A61K47/552 , A61K47/555 , A61K47/6899
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公开(公告)号：EP0492277A3
公开(公告)日：1992-10-14
申请号：EP91121222.3
申请日：1991-12-11
IPC分类号： C07D501/38 , A61K31/545
CPC分类号： C07D501/00
摘要： 57 Cephalosporin derivatives of the general formula
in which R 3 is a group of the formula
R 6 ° and R 65 are hydrogen or lower alkyl, R 15 -R 19 are each independently hydrogen, halogen or hydroxy, n is zero or 1, R 4 and R 5 are each hydrogen, halogen, lower alkyl, lower alkoxy or amino, R 7 is hydrogen or lower alkyl and R 8 is lower alkyl, halo-lower alkyl, C 3 -C 7 cycloalkyl or mono-, di- or trihalophenyl, and Z is N or C-R 9 , where R 9 is hydrogen, halogen, lower alkyl or lower alkoxy; and, when R 4 is fluoro, R 5 and R 7 are hydrogen, R 8 is cyclopropyl and Z is C-H, R 3 can also be one of the groups
in which R 61 and R 66 are hydrogen or methyl, R 15 -R 19 are as above and R 90 is hydrogen, hydroxy, carboxy, amino or [[4-(lower alkyl)-2,3-dioxo-1-piperazinyl]carbonyl]amino;
pharmaceutically acceptable acid or base addition salts thereof, hydrates of compounds of formula I and hydrates of such salts. The products have antibacterial activity.摘要翻译： 其中R3为式R6和R65为氢或低级烷基的基团的通式的头孢菌素衍生物，R15-R19各自独立地为氢，卤素或羟基，n为0或1，R4和R5各自为氢 卤素，低级烷基，低级烷氧基或氨基，R 7是氢或低级烷基，R 8是低级烷基，卤代低级烷基，C 3 -C 7环烷基或单，二或三卤代苯基，Z是N或C-R 9， 其中R9是氢，卤素，低级烷基或低级烷氧基; 当R4是氟时，R5和R7是氢，R8是环丙基，Z是CH，R3也可以是其中R61和R66是氢或甲基，R15-R19如上所述并且R90是氢的基团之一， 羟基，羧基，氨基或[[4-（低级烷基）-2,3-二氧代-1-哌嗪基]羰基]氨基; 其药学上可接受的酸或碱加成盐，式I化合物的水合物和该盐的水合物。 该产品具有抗菌活性。
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公开(公告)号：EP0367124A1
公开(公告)日：1990-05-09
申请号：EP89119941.6
申请日：1989-10-27
IPC分类号： C07D499/84 , A61K31/43
CPC分类号： C07D499/00 , Y02P20/55
摘要： The compounds of the general formula
in which R is hydrogen, a readily hydrolyzable ester group or a protecting group, R¹ is hydrogen and R² is hydrogen or an acyl group, or R¹ and R² taken together are the group
in which n is 5, 6 or 7,
X is fluoro, thiocyanato, azido or the group R 3a CO₂-
R 3a is C₂- to C₁₆-alkyl, aryl, a heterocycle, -(CH₂) m -aryl, -(CH₂) m -heterocycle, a heterocycle-lower alkenyl or aryl-lower alkenyl, R³ is C₁- to C₁₆-alkyl, aryl, a heterocycle, -(CH₂) m -aryl, a -(CH₂) m -heterocycle, a heterocycle-lower alkenyl or aryl-lower alkenyl, R⁴ and R 4′ independently are hydrogen, lower alkyl, lower alkenyl or lower alkynyl, R a is hydrogen, halogen, amino, amino-lower alkyl, carboxy, carbamoyl, carboxy-lower alkyl, carbamoyl-lower alkyl or lower carbalkoxy-lower alkyl, m is from 1 to 4 and p is 3, 4 or 5, provided that X is other than fluoro when R is a protecting group, a hydrate, a readily hydrolyzable ester or salt thereof, or a hydrate of the ester or the salt, when R is hydrogen are useful as anti-bacterial agents for the prevention and treatment of bacterial infections in mammals, including humans.摘要翻译： 其中R是氢，容易水解的酯基或保护基，R 1是氢和R 2是氢或酰基，或R 1和R 2一起形成通式的化合物是其中n是5,6的基团 或7，X是氟，氰硫基，叠氮基或基团R3aCO 2 -R 3a是C 2 -C 16烷基，芳基，杂环， - （CH 2）m - 芳基， - （CH 2）m-杂环，杂环 - 低级链烯基 或芳基低级链烯基，R 3是C 1 -C 16烷基，芳基，杂环， - （CH 2）m - 芳基， - （CH 2）m - 杂环，杂环低级链烯基或芳基低级链烯基，R 4和 低级烷基，低级烯基或低级炔基，Ra是氢，卤素，氨基，氨基 - 低级烷基，羧基，氨基甲酰基，羧基 - 低级烷基，氨基甲酰基 - 低级烷基或低级烷氧基 - 低级烷基，m是 1至4且p为3,4或5，条件是当R为保护基，水合物，易水解的酯或盐或e的水合物时，X不是氟 当R是氢时，该化合物或盐可用作预防和治疗哺乳动物包括人的细菌感染的抗菌剂。
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公开(公告)号：EP0335297B1
公开(公告)日：1996-03-13
申请号：EP89105359.7
申请日：1989-03-29
发明人： Albrecht, Harry Allen , Keith, Dennis Dalton , Konzelmann, Frederick Martin , Rossman, Pamela Loreen , Wei, Chung-Chen , Weigele, Manfred , Yang, Roxana
IPC分类号： C07D501/26 , C07D501/38 , A61K31/545
CPC分类号： C07D501/46 , C07D501/18 , C07D501/26 , C07D501/32 , C07D501/34 , C07D501/38 , C07D501/44 , C07D519/00
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公开(公告)号：EP0492277A2
公开(公告)日：1992-07-01
申请号：EP91121222.3
申请日：1991-12-11
IPC分类号： C07D501/38 , A61K31/545
CPC分类号： C07D501/00
摘要： 57 Cephalosporin derivatives of the general formula
in which R 3 is a group of the formula
R 6 ° and R 65 are hydrogen or lower alkyl, R 15 -R 19 are each independently hydrogen, halogen or hydroxy, n is zero or 1, R 4 and R 5 are each hydrogen, halogen, lower alkyl, lower alkoxy or amino, R 7 is hydrogen or lower alkyl and R 8 is lower alkyl, halo-lower alkyl, C 3 -C 7 cycloalkyl or mono-, di- or trihalophenyl, and Z is N or C-R 9 , where R 9 is hydrogen, halogen, lower alkyl or lower alkoxy; and, when R 4 is fluoro, R 5 and R 7 are hydrogen, R 8 is cyclopropyl and Z is C-H, R 3 can also be one of the groups
in which R 61 and R 66 are hydrogen or methyl, R 15 -R 19 are as above and R 90 is hydrogen, hydroxy, carboxy, amino or [[4-(lower alkyl)-2,3-dioxo-1-piperazinyl]carbonyl]amino;
pharmaceutically acceptable acid or base addition salts thereof, hydrates of compounds of formula I and hydrates of such salts.
The products have antibacterial activity.摘要翻译： 通式
的头孢菌素衍生物，其中R 3为式CHEM R 6和O 6的基团是氢或低级烷基，R 1， R 5 -R 9各自独立地为氢，卤素或羟基，n为0或1，R 4和R 5各自为氢，卤素，低级烷基，低级烷氧基或氨基， R 7是氢或低级烷基，R 8是低级烷基，卤代低级烷基，C 3 -C 7环烷基或单 - ，二 - 或三卤代苯基，Z是N或CR 9，其中R 9是 氢，卤素，低级烷基或低级烷氧基; 当R 4是氟时，R 5和R 7是氢，R 8是环丙基，Z是CH，R 3也可以是其中R CH R 6和R 6均为氢或甲基，R 1，R 5，R 9和R 9如上所述，R 9为氢，羟基， 羧基，氨基或[[4-（低级烷基）-2,3-二氧代-1-哌嗪基]羰基]氨基; 其药学上可接受的酸或碱加成盐，式I化合物的水合物和这些盐的水合物。 该产品具有抗菌活性。 -
公开(公告)号：EP0451764A1
公开(公告)日：1991-10-16
申请号：EP91105550.7
申请日：1991-04-08
IPC分类号： C07D519/00 , C07D477/00 , A61K31/435
CPC分类号： C07D477/14 , C07D477/26 , Y02P20/55
摘要： Carbapenem compounds of the general formula
wherein R is hydrogen or a carboxylic acid protecting group; R 1 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy and hydroxyalkyl; R 2 and R 3 are each independently hydrogen, lower alkyl, lower alkoxy or lower alkylthio; and Y is
(i) an ester group;
(ii) a thioester group;
(iii) a piperazinyl or pyrrolidinyl derived carbamate group;
(iv) a piperazinyl derived amine group;
(v) a piperazinyl derived quaternary ammonium group; or
(vi) a group comprising a covalent bond;
the ester group and the thioester group being bonded to a substituted quinolonyl or naphthyridonyl group; the piperazinyl or pyrrolidinyl derived carbamate group, the piperazinyl derived amine group and the piperazinyl derived quaternary ammonium group containing a piperazinyl nucleus or a pyrrolidinyl nucleus having a nitrogen atom bonded directly to a substituted quinolonyl or naphthyridonyl group, the piperazinyl and the pyrrolidinyl nuclei being unsubstituted or substituted with one or more lower alkyl groups; and the covalent bond of the corresponding group being connected to a substituted isothiazolo or isoxazolo quinolonyl or naphthyridonyl group via a nitrogen atom in an isothiazolo or isoxazolo nucleus;
as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of any of the foregoing compounds.
The products have antibacterial activity.摘要翻译： 通式
的碳青霉烯化合物，其中R为氢或羧酸保护基; R 1选自氢，低级烷基，低级烷氧基和羟烷基; R 2和R 3各自独立地为氢，低级烷基，低级烷氧基或低级烷硫基; Y为（i）酯基; （ii）硫酯基; （iii）哌嗪基或吡咯烷基衍生的氨基甲酸酯基; （iv）哌嗪衍生的胺基; （v）哌嗪衍生的季铵基团; 或（vi）包含共价键的基团; 酯基和硫酯基与取代的喹啉基或萘啶酮基键合; 哌嗪基或吡咯烷基衍生的氨基甲酸酯基，哌嗪衍生的胺基和含有哌嗪基核的哌嗪衍生的季铵基或具有氮原子的吡咯烷基核直接键合到取代的喹啉酮基或萘啶酮基上，哌嗪基和吡咯烷基核是未取代的 或被一个或多个低级烷基取代; 并且相应基团的共价键通过异噻唑或异恶唑环中的氮原子与取代的异噻唑或异恶唑喹啉酮或萘啶酮基连接; 以及任何前述化合物的相应的易水解的酯，药学上可接受的盐和水合物。 该产品具有抗菌活性。
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