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1. 发明公开

EP0148283A1 Novel penicillanic acid derivatives 失效
标题翻译： Penicillansäure衍。
公开(公告)号：EP0148283A1
公开(公告)日：1985-07-17
申请号：EP83112841.8
申请日：1983-12-20
申请人： F. HOFFMANN-LA ROCHE & CO. Aktiengesellschaft
发明人： Wei, Chung-Chen , Weigele, Manfred
IPC分类号： C07D499/02 , C07D401/06 , C07D403/06 , A61K31/43 , A61K31/545
CPC分类号： C07D231/12 , C07D211/18 , C07D211/34 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D403/06 , C07D499/00 , Y02P20/55
摘要： @ 6-Amidinopenicillanic acid derivatives wherein one of the nitrogen atoms of the amidino group is part of a heterocyclic ring having on a side chain an unsubstituted heterocyclic ring containing 2 to 3 nitrogen atoms, with formula:
wherein n is 0 or 1;
is a saturated 5 to 7 membered heterocyclic ring containing the nitrogen atom as the only heteroatom, said ring being unsubstituted or substituted in one or more positions with lower alkyl;
is a 5 to 7 membered heterocyclic ring having at most one additional nitrogen atom, from 0 to 2 additional double bonds, and, aside from R, either being unsubstituted or substituted in one or more positions with lower alkyl; R is lower alkyl, nitro, hydrogen,-COOH,-(CH 2 ) y -NHR 4 ;-(CH 2 ) y -OR 3 and
R 3 is hydrogen or lower alkyl, y is an integer from 0 to 4; R, is hydrogen, lower alkyl or an amino-protecting group, (Continuation next page) R 5 and R 6 are hydrogen or lower alkyl and R 7 is lower alkylene, hydrolyzable esters thereof, salts thereof and hydrates thereof, and with formula:
wherein n is an integer from 0 to 1; R, is hydrogen or lower alkyl;
is a saturated 5 to 7 membered heterocyclic ring containing the nitrogen atom as the only heteroatom, said ring being unsubstituted or substituted in one or more positions with lower alkyl;
is a 5 to 7 membered heterocyclic ring containing no additional double bonds or can be additionally aromatic when it is 5 membered, said ring being either unsubstituted or substituted in one or more positions with lower alkyl; and R 7 is lower alkylene, hydrolyzable esters thereof, salts thereof and hydrates thereof.
These compounds are useful as antibiotics.
摘要翻译： 6-脒基青霉烷酸衍生物，其中脒基中的一个氮原子是在侧链上含有2至3个氮原子的未取代杂环的杂环的一部分，其中n为0或1; 是饱和的5至7元杂环，其含有氮原子作为唯一的杂原子，所述环是未取代的或在一个或多个位置被低级烷基取代; 是具有至多一个另外的氮原子，0至2个另外的双键的5至7元杂环，并且除R1之外未被取代或在一个或多个位置被低级烷基取代; R是低级烷基，硝基，氢，-COOH， - （CH2）y-NHR4; - （CH 2）y -OR 3和 R 3是氢或低级烷基，y是0至4的整数; R4为氢，低级烷基或氨基保护基，R5和R6为氢或低级烷基，R7为低级亚烷基，其可水解酯，其盐及其水合物，式为：其中n为 0到1; R1是氢或低级烷基; 是饱和的5至7元杂环，其含有氮原子作为唯一的杂原子，所述环是未取代的或在一个或多个位置被低级烷基取代; 是不含另外双键的5至7元杂环，或当其为5元时可另外为芳族，所述环为未取代的或在一个或多个位置被低级烷基取代; 并且R 7为低级亚烷基，其可水解酯，其盐及其水合物。这些化合物可用作抗生素。

2. 发明公开

EP0409081A1 Beta-Lactam Derivatives 失效
标题翻译： β-Lactamderivate。
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
申请人： F. HOFFMANN-LA ROCHE AG
发明人： Keith, Dennis Dalton , Roberts, John Lawson , Wei, Chung-Chen
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。

3. 发明公开

EP0055099A1 Penicillin derivatives 有权转让
标题翻译：青霉素衍生物
公开(公告)号：EP0055099A1
公开(公告)日：1982-06-30
申请号：EP81305957.3
申请日：1981-12-18
申请人： ICI PHARMA , IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Jung, Frédéric Henri , Davies, Gareth Morse
IPC分类号： C07D499/02 , A61K31/43
CPC分类号： C07D499/00
摘要： A penicillin derivative of the formula I:
in which R 1 is any one of the C-3 substituents from antibacterially-active penicillins known in the art; ⊕

X is a nitrogen atom or a radical of the formula N-R 3 ; R 2 and R 3 , which may be the same or different, are hydrogen atoms or 1-6C alkyl, 1-6C alkanoyl, hydroxy, 1-6C alkoxy, amino, 1-6C alkanoylamino, 1-6C alkylamino, 1-6C aminoalkyl, 1-6C hydroxyalkyl, 2-6C carboxyalkyl, 2-6C alkenyl, 3-6C alkoxyalkyl, 3-8C alkoxycarbonylalkyl, furylmethyl, phenyl or 7-11 C phenylalkyl radicals, in the latter two of which the phenyl ring is optionally substituted by a halogen atom or by a methyl, methoxy, nitro, hydroxy, amino, carboxy or methoxycarbonyl radical;
A in which R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are as described in the specification; and the pharmaceutically-acceptable acid- or base-addition salts thereof. Pharmaceutical compositions and manufacturing processes are also described.
摘要翻译：式I的青霉素衍生物：其中R1是来自本领域已知的抗细菌活性青霉素的C-3取代基中的任何一个; ⊕X是氮原子或式N-R3的基团; R2和R3可以相同或不同，为氢原子或1-6C烷基，1-6C烷酰基，羟基，1-6C烷氧基，氨基，1-6C烷酰基氨基，1-6C烷基氨基，1-6C氨基烷基， 1-6C羟基烷基，2-6C羧基烷基，2-6C链烯基，3-6C烷氧基烷基，3-8C烷氧基羰基烷基，呋喃基甲基，苯基或7-11C苯基烷基，后两个苯基环任选被卤素原子或被甲基，甲氧基，硝基，羟基，氨基，羧基或甲氧基羰基取代; A是式II或III的基团：其中R 4，R 5，R 6，R 7，R 8和R 9如说明书中所述; 及其药学上可接受的酸或碱加成盐。还描述了药物组合物和制造过程。

4. 发明授权

EP0043546B1 7-Oxo-cephalosporins and 6-oxo-penicillins, their analogues and process for their preparation 有权
标题翻译： 7-OXO-CEPHALOSPORINS和6-OXO-PENICILLINS，它们的制备方法及其制备方法
公开(公告)号：EP0043546B1
公开(公告)日：1986-01-29
申请号：EP81105077.2
申请日：1981-07-01
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： Hashimoto, Masashi , Aratani, Matsuhiko , Hagiwara, Daijiro , Sawada, Kozo , Onami, Tetsuo
IPC分类号： C07D501/00 , C07D501/18 , C07D501/04 , C07D501/20 , C07D499/00 , C07D499/02
CPC分类号： C07D505/00 , C07D499/00 , C07D503/00 , Y02P20/55

5. 发明公开

EP0000392A3 Cephalosporins and penicillins, processes for their preparation and pharmaceutical compositions containing them 失效
标题翻译： CEPHALOSPORINS和PENICILLINS，其制备和包含它们的药物组合物的方法
公开(公告)号：EP0000392A3
公开(公告)日：1979-08-22
申请号：EP78100352
申请日：1978-07-11
申请人： BAYER AG
发明人： Preiss, Michael, Dr , König, Hans-Bodo, Dr. , Metzger, Karl Georg, Dr. , Feyen, Peter, Dr.
IPC分类号： C07D501/20 , C07D499/70 , C07D499/00 , C07D499/02 , A23K01/17
CPC分类号： C07D231/12 , C07D277/48 , C07D277/587 , C07D307/54 , C07D499/00

6. 发明授权

EP0055099B1 Penicillin derivatives 有权转让
标题翻译：青霉素衍生物
公开(公告)号：EP0055099B1
公开(公告)日：1984-10-24
申请号：EP81305957.3
申请日：1981-12-18
申请人： ICI PHARMA , IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Jung, Frédéric Henri , Davies, Gareth Morse
IPC分类号： C07D499/02 , A61K31/43
CPC分类号： C07D499/00

7. 发明公开

EP0043546A2 7-Oxo-cephalosporins and 6-oxo-penicillins, their analogues and process for their preparation 有权
标题翻译： 7-Oxo-cephalosporine und 6-Oxo-penicilline，ihre Analoge und Verfahren zu ihrer Herstellung。
公开(公告)号：EP0043546A2
公开(公告)日：1982-01-13
申请号：EP81105077.2
申请日：1981-07-01
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： Hashimoto, Masashi , Aratani, Matsuhiko , Hagiwara, Daijiro , Sawada, Kozo , Onami, Tetsuo
IPC分类号： C07D501/00 , C07D501/18 , C07D501/04 , C07D501/20 , C07D499/00 , C07D499/02
CPC分类号： C07D505/00 , C07D499/00 , C07D503/00 , Y02P20/55
摘要： New compound of the formula:
wherein A' is a group of the formula:
in which R 3 is hydrogen or alkyl,

R 4 is hydrogen, halogen, alkyl, alkoxy, acyloxymethyl, or substituted or unsubstituted heterocyclic-thiomethyl,
R 5 is carboxy or protected carboxy, and
X is -S- or -0-,

provided that when A' is a group of the formula: R 5 then R 4 is hydrogen, halogen, alkoxy or carbamoyloxy- methyl protected by an amino-protecting group, and R 3 and R 5 are each as defined above, or a salt thereof or a hydrate thereof and processes for their preparation.
摘要翻译：新的化合物：... 其中A min是下式的基团：其中R 3是氢或烷基，R 4是氢，卤素，烷基，烷氧基，酰氧基甲基或取代或未取代的杂环硫代甲基，R 5为羧基或受保护的羧基，X为-S-或-O-，条件是当A min为下列基团时：...

8. 发明授权

EP0382268B1 New amino carboxylic acid derivatives 失效
标题翻译：氨基羧酸的衍生物。
公开(公告)号：EP0382268B1
公开(公告)日：1994-08-24
申请号：EP90200031.4
申请日：1990-01-04
申请人： GIST-BROCADES N.V.
发明人： Verweij, Jan , Hirs, Henri Gerard Julius , Witkamp, Hendrik Adrianus
IPC分类号： C07D501/18 , C07D499/02 , C07C251/02
CPC分类号： C07D499/00

9. 发明公开

EP0382268A1 New amino carboxylic acid derivatives 失效
标题翻译：衍生on氨基羧基。
公开(公告)号：EP0382268A1
公开(公告)日：1990-08-16
申请号：EP90200031.4
申请日：1990-01-04
申请人： GIST-BROCADES N.V.
发明人： Verweij, Jan , Hirs, Henri Gerard Julius , Witkamp, Hendrik Adrianus
IPC分类号： C07D501/18 , C07D499/02 , C07C251/02
CPC分类号： C07D499/00
摘要： New amino carboxylic acid derivatives are described which comprise, as N-terminal group, a (cyclo)alkylideneammonio group. Processes for their preparation and their use as synthetic intermediates are also disclosed.
摘要翻译：描述了新的氨基羧酸衍生物，其包含作为N-末端基团的（环）亚烷基氨基基团。还公开了其制备方法及其作为合成中间体的用途。

10. 发明公开

EP0043546A3 7-Oxo-cephalosporins and 6-oxo-penicillins, their analogues and process for their preparation 有权
标题翻译： 7-OXO-CEPHALOSPORINS和6-OXO-PENICILLINS，它们的制备方法及其制备方法
公开(公告)号：EP0043546A3
公开(公告)日：1982-08-11
申请号：EP81105077
申请日：1981-07-01
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： Hashimoto, Masashi , Aratani, Matsuhiko , Hagiwara, Daijiro , Sawada, Kozo , Onami, Tetsuo
IPC分类号： C07D501/00 , C07D501/18 , C07D501/04 , C07D501/20 , C07D499/00 , C07D499/02
CPC分类号： C07D505/00 , C07D499/00 , C07D503/00 , Y02P20/55
摘要： New compound of the formula:
wherein A' is a group of the formula:
in which R 3 is hydrogen or alkyl,
R 4 is hydrogen, halogen, alkyl, alkoxy, acyloxymethyl, or substituted or unsubstituted heterocyclic-thiomethyl, R 5 is carboxy or protected carboxy, and X is -S- or -0-,
provided that when A' is a group of the formula: R 5 then R 4 is hydrogen, halogen, alkoxy or carbamoyloxy- methyl protected by an amino-protecting group, and R 3 and R 5 are each as defined above, or a salt thereof or a hydrate thereof and processes for their preparation.

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