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1. 发明授权

US4918067A Heterocyclic substituted penicillin antibiotics 失效
标题翻译：杂环取代青霉素抗生素
公开(公告)号：US4918067A
公开(公告)日：1990-04-17
申请号：US76360
申请日：1987-07-22
申请人： Brian C. Gasson , Michael J. Pearson
发明人： Brian C. Gasson , Michael J. Pearson
IPC分类号： C07D499/00 , C07D499/70
CPC分类号： C07D499/00
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in-vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is a 5 or 6 membered sulphur and/or nitrogen containing heterocyclic group substituted by an optionally protected amino group, with the proviso that R.sup.1 is not 2-aminothiazol-4-yl, and R is hydrogen; optionally substituted C.sub.1-12 alkyl; optionally substituted C.sub.2-12 alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl.These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organizations.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐或体内可水解的酯：其中R 1是被任选地被取代的5或6元硫和/或含氮杂环基团保护的氨基，条件是R1不是2-氨基噻唑-4-基，R是氢; 任选取代的C 1-12烷基; 任选取代的C 12-12烯基或炔基; 碳环基芳基或杂环基。这些化合物具有抗菌性，因此可用于治疗由广泛组织引起的人和动物细菌感染。

2. 发明授权

US4515789A .beta.-Lactam antibiotics 失效
标题翻译： β-内酰胺抗生素
公开(公告)号：US4515789A
公开(公告)日：1985-05-07
申请号：US483062
申请日：1983-04-07
申请人： Karl G. Metzger , Wilfried Schrock , Dieter Habich , Paul Naab , Hans-Joachim Zeiler
发明人： Karl G. Metzger , Wilfried Schrock , Dieter Habich , Paul Naab , Hans-Joachim Zeiler
IPC分类号： C07D499/66 , A61K31/397 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D205/08 , C07D205/085 , C07D233/32 , C07D233/36 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D417/14 , C07D463/00 , C07D499/00 , C07D499/44 , C07D499/64 , C07D499/68 , C07D499/70 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/38 , C07D501/57 , C07D505/00 , C07F7/18 , C07D501/56
CPC分类号： C07D403/12 , C07D233/32 , C07D233/36 , C07D403/14 , C07D405/14 , C07D409/12 , C07D417/14 , C07D499/00 , C07D505/00 , C07F7/184
摘要： A 3-.beta.-(vic-dihydroxyphenylmethyleneamino-2-oxo-imidazolidine)- or 3-.beta.-(vic-dihydroxyphenyl-methyleneamino-2,3-dioxo-piperazine)-1-carbonylamino-acetamidoazetidin-2-one having an acidic grouping on .sub.1 N, e.g. of the formula ##STR1## The compounds are antibiotically active, especially against Pseudomonas bacteria and can be used in combating bacterial infection, as a preservative and as a growth promoting agent in animal feeds.
摘要翻译： 3β-（咔唑 - 二羟基苯基亚甲基氨基-2-氧代 - 咪唑烷） - 或3β-（咔 - 二羟基苯基 - 亚甲基氨基-2,3-二氧代 - 哌嗪）-1-羰基乙酰氨基吖丁啶-2-酮在1N上酸性分组，例如该化合物具有抗菌活性，特别是针对假单胞菌属细菌，可用于防治细菌感染，作为防腐剂和作为动物饲料中的生长促进剂。

3. 发明授权

US4386089A .beta.-Lactam antibiotics and their medicinal use 失效
标题翻译： β-内酰胺抗生素及其药用
公开(公告)号：US4386089A
公开(公告)日：1983-05-31
申请号：US276762
申请日：1981-06-24
申请人： Hans-Bodo Konig , Karl G. Metzger , Michael Preiss
发明人： Hans-Bodo Konig , Karl G. Metzger , Michael Preiss
IPC分类号： C07D499/70 , A61K31/43 , A61P31/04 , C07D233/38 , C07D277/20 , C07D277/48 , C07D499/00 , C07D499/46 , C07D499/64 , C07D501/20 , C07D501/34 , C07D501/36 , A61K31/545
CPC分类号： C07D277/20 , C07D233/38 , C07D277/48 , C07D499/00
摘要： .beta.-Lactam compounds of the formula ##STR1## in which B denotes an optionally substituted heterocyclic 5-membered or 6-membered ring or an optionally substituted phenyl ring,Z denotes a hydrogen atom or a C.sub.1 to C.sub.4 alkoxy group, ##STR2## Y, E.sub.1 and E.sub.2 independently of one another denote a divalent organic radical andR.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently of one another denote a hydrogen atom or an alkyl, alkenyl, alkinyl, alkadienyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, aryl or heterocyclyl radical, it also being possible for the above-mentioned radicals, with the exception of hydrogen, to be substituted, or an acyl radical,are antibacterial agents with a broad antibacterial spectrum and are useful as agents for promoting growth and for improving feed utilization in animals and as antioxidants.
摘要翻译：式（I）的β-内酰胺化合物，其中B表示任选取代的杂环5元或6元环或任选取代的苯环，Z表示氢原子或C1至C4烷氧基， Y，E1和E2彼此独立地表示二价有机基团，R 1，R 2，R 3和R 4彼此独立地表示氢原子或烷基，烯基，炔基，链烯基，环烷基，环烯基，环链二烯基，芳基或杂环基，除了氢被取代以外，上述基团也可以是酰基，是具有广谱抗菌谱的抗菌剂，并且可用作促进生长的试剂并提高动物和抗氧化剂的饲料利用率。

4. 发明授权

US4320133A Penicillins and their antibacterial use 失效
标题翻译：青霉素及其抗菌用途
公开(公告)号：US4320133A
公开(公告)日：1982-03-16
申请号：US119044
申请日：1980-02-06
申请人： Helmut Hamberger , Peter Stutz , Dieter Scholz , Hans Fliri
发明人： Helmut Hamberger , Peter Stutz , Dieter Scholz , Hans Fliri
IPC分类号： C07D499/12 , A61K31/545 , A61K31/546 , A61P31/04 , C07D275/02 , C07D275/03 , C07D311/22 , C07D333/34 , C07D335/06 , C07D495/04 , C07D499/00 , C07D499/04 , C07D499/64 , C07D499/66 , C07D499/68 , C07D501/20 , C07D501/30 , C07D513/04 , A61K31/41 , A61K31/43 , C07D499/70
CPC分类号： C07D275/03 , C07C323/00 , C07D311/22 , C07D333/34 , C07D335/06 , C07D495/04 , C07D499/00 , C07D513/04
摘要： The invention provides novel penicillins and cephalosporins of formula I, ##STR1## methods for their production and their anti-bacterial use.
摘要翻译：本发明提供了新颖的式I的青霉素和头孢菌素，其生产方法及其抗菌用途。

5. 发明授权

US4263302A Quinolinecarboxylic acid substituted penicillins and pharmaceutical compositions containing the same 失效
标题翻译：喹啉羧酸取代的青霉素和含有它们的药物组合物
公开(公告)号：US4263302A
公开(公告)日：1981-04-21
申请号：US96183
申请日：1979-11-20
申请人： Akira Matsubara , Hideaki Sakai , Takuo Nakano , Toshio Suganuma
发明人： Akira Matsubara , Hideaki Sakai , Takuo Nakano , Toshio Suganuma
IPC分类号： C07D215/56 , C07D499/00 , C07D499/64 , C07D499/68 , A61K31/47 , C07D499/70
CPC分类号： C07D215/56 , C07D499/00
摘要： A penicillanic acid of the general formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each represent a hydrogen atom or a lower alkyl group, provided that R.sup.1, R.sup.2 and R.sup.3 do not simultaneously represent a hydrogen atom, or a biologically acceptable salt thereof.
摘要翻译：其中R 1，R 2和R 3各自表示氢原子或低级烷基，其中R 1，R 2和R 3不同时表示氢原子或其生物学上可接受的盐，通式为“IMAGE”的青霉烷酸。

6. 发明授权

US4220587A Amino acid derivatives of 6-(2-amino-2-arylacetamido)penicillanic acids 失效
标题翻译： 6-（2-氨基-2-芳基乙酰氨基）青霉烷酸的氨基酸衍生物
公开(公告)号：US4220587A
公开(公告)日：1980-09-02
申请号：US915481
申请日：1978-06-14
申请人： Yoshiharu Morita , Kenzo Omata , Junichi Ohya , Kazuo Wagatsuma , Tadashi Shirasaka
发明人： Yoshiharu Morita , Kenzo Omata , Junichi Ohya , Kazuo Wagatsuma , Tadashi Shirasaka
IPC分类号： C07D499/00 , C07D499/68 , C07D499/70
CPC分类号： C07D499/00 , C10M2219/10 , C10M2219/102 , C10M2219/104 , C10M2219/106 , C10N2240/401
摘要： Amino acid derivatives of 6-(2-amino-2-arylacetamido)penicillanic acids are prepared and shown to be useful as antibacterial agents.

7. 发明授权

US4029806A Nitro-.beta.-lactam antibiotics and processes for their preparation and use 失效
标题翻译：硝基 - {62-内酰胺抗生素及其制备和使用的方法
公开(公告)号：US4029806A
公开(公告)日：1977-06-14
申请号：US707854
申请日：1976-07-22
申请人： Wolfgang Krohn , Karl Georg Metzger , Michael Preiss , Michael Walkowiak
发明人： Wolfgang Krohn , Karl Georg Metzger , Michael Preiss , Michael Walkowiak
IPC分类号： C07D499/10 , C07D499/00 , C07D499/04 , C07D499/44 , C07D499/46 , C07D499/48 , C07D499/54 , C07D499/64 , C07D499/66 , C07D499/68 , C07D499/70 , C07D499/74 , C07D501/20 , A61K31/43
CPC分类号： C07D499/00 , C10M2219/10 , C10M2219/102 , C10M2219/104 , C10M2219/106
摘要： Penicillin and cephalosporin derivatives characterized by the presence of a nitroalkyl, nitrocycloalkyl, nitrophenylalkyl or nitroanilinoalkyl group in the side chain are antibacterial agents. The compounds, of which 6-(2-nitro-3,3-dimethylbutyrylamido)-penicillanic acid, 7-nitroacetamido-3-methyl-ceph-3-em-4-carboxylic acid, and 6-[D-.alpha.-(2-nitro-2-methylpropionylamido)phenylacetamido] pencillanic acid are typical embodiments, are prepared by reacting 6-amino-penicillanic acid, 7-amino-cephalosporanic acid (or derivative thereof) or an .alpha.-substituted-.alpha.-amino-acetamido-penicillanic acid with an appropriate nitrated carboxylic acid or an equivalent nitrated acylating agent.
摘要翻译：特征在于在侧链中存在硝基烷基，硝基环烷基，硝基苯基烷基或硝基苯胺基烷基的青霉素和头孢菌素衍生物是抗菌剂。其中6-（2-硝基-3,3-二甲基丁酰氨基） - 青霉烷酸，7-硝基乙酰胺基-3-甲基 - 头孢-3-烯-4-羧酸和6- [D-α - （ 2-硝基-2-甲基丙酰胺基）苯乙酰氨基]辛酸是典型的实施方案，通过6-氨基 - 青霉烷酸，7-氨基 - 头孢烷酸（或其衍生物）或α-取代-α-氨基 - 乙酰氨基 - 青霉烷酸与适当的硝化羧酸或等同的硝化酰化剂。

8. 发明授权

US3992371A Penicillins substituted with heterocyclic and substituted phenyl groups 失效
标题翻译：用杂环和取代的苯基取代的青霉素
公开(公告)号：US3992371A
公开(公告)日：1976-11-16
申请号：US536181
申请日：1974-12-24
申请人： Hisao Tobiki , Hirotada Yamada , Iwao Nakatsuka , Kozo Shimago , Shigeru Okano , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Hiroshi Noguchi , Yasuko Eda
发明人： Hisao Tobiki , Hirotada Yamada , Iwao Nakatsuka , Kozo Shimago , Shigeru Okano , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Hiroshi Noguchi , Yasuko Eda
IPC分类号： C07D499/10 , C07D471/04 , C07D499/00 , C07D499/04 , C07D499/64 , C07D499/68 , C07D519/06 , C07D499/70
CPC分类号： C07D471/04 , C07D499/00
摘要： Novel penicillins of the formula ##SPC1##Wherein ##EQU1## represents a substituted or unsubstituted benzene or nitrogen atom-containing heteroaromatic ring which may be substituted, ##EQU2## represents a pyridine, pyrazine or pyridazine ring, X represents an oxygen or sulfur atom, Y represents a hydrogen atom or a loer alkoxycarbonyl or lower alkanoyl group, and R.sub.1, R.sub.2 and R.sub.3 are each a hydrogen or halogen atom or a nitro, lower alkylamino, di(lower)alkylamino, aine, lower alkoxycarbonylamino, lower alkanoylamino, amino(lower)alkyl, lower alkyl, lower alkoxy, hydroxyl, sulfamoyl, trifluoromethyl, lower alkylthio or lower alkylsulfonyl group, excluding the cases where all of R.sub.1, R.sub.2 and R.sub.3 are hydrogen atoms and where R.sub.1 is a hydroxyl group and R.sub.2 and R.sub.3 are each a hydrogen or halogen atom, and their nontoxic, pharmaceutically acceptable salts, which can be prepared by reacting a carboxylic acid of the formula: ##EQU3## wherein ##EQU4## X and Y are each as defined above or its reactive derivative with a compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2 and R.sub.3 are each as defined above or its reactive derivative, and are ueful as antimicrobial agents against gram-positive and gram-negative bacteria including Pseudomonas.
摘要翻译：式+ q，10的新型青霉素其中C | A C表示可被取代的取代或未取代的含有苯或含氮原子的杂芳环，C | C | CB表示吡啶，吡嗪或哒嗪环，X表示氧或硫原子，Y表示氢原子或低级烷氧基羰基或低级烷酰基，R 1，R 2和R 3各自为氢或卤素原子或硝基，低级烷基氨基，二（低级）烷基氨基，亚氨基，低级烷氧基羰基氨基，低级烷酰基氨基，氨基（低级）烷基，低级烷基，低级烷氧基，羟基，氨磺酰基，三氟甲基，低级烷硫基或低级烷基磺酰基，不包括R1，R2和R3全部为氢原子，其中R1为羟基， R2和R3各自为氢或卤素原子，以及它们的无毒的药学上可接受的盐，其可以通过使下式的羧酸：XY | C | C-COOH A | CB反应而制备，其中CC | | CA | | C，CB，X和Y为ea ch或其反应性衍生物与下式的化合物：+ q，21，其中R1，R2和R3各自如上所定义，或其反应性衍生物，并且作为抗革兰氏阳性和革兰氏阴性细菌的抗微生物剂包括假单胞菌。

9. 发明授权

US3972872A 6-[.alpha.-(.omega.-Guanidinoalkanoylamido)acylamido]penicillanic acids 失效
标题翻译： 6- {8 - （{10-氰基亚氨基酰氨基）酰基酰氨基{9青霉烷酸
公开(公告)号：US3972872A
公开(公告)日：1976-08-03
申请号：US575072
申请日：1975-05-06
申请人： Ernest S. Hamanaka
发明人： Ernest S. Hamanaka
IPC分类号： C07D499/64 , C07D499/68 , C07D499/70
CPC分类号： C07D499/64
摘要： 6-[.alpha.-(.omega.-GUANIDINOALKANOYLAMIDO)ACYLAMIDO]PENICILLANIC ACIDS, THE NON-TOXIC SALTS AND ESTERS THEREOF ARE USEFUL AS ANTIBACTERIAL AGENTS, THERAPEUTIC AGENTS IN ANIMALS, INCLUDING MAN, OF PARTICULAR VALUE AGAINST GRAM-NEGATIVE BACTERIA, AND AS ANIMAL FEED NUTRITIONAL SUPPLEMENTS.
摘要翻译： 6- [α-（ω-葡萄糖胺基甲酰胺）ACYLAMIDO] PENICILLANIC酸，其非毒性盐及其酯类有效地用作抗菌剂，动物中的治疗剂，包括人类对抗副反应性细菌的特定值，以及作为动物饲料营养补充剂。

10. 发明授权

US3963704A Penicillin esters 失效
标题翻译：青霉素酯
公开(公告)号：US3963704A
公开(公告)日：1976-06-15
申请号：US530763
申请日：1974-12-09
申请人： Harry Ferres
发明人： Harry Ferres
IPC分类号： C07D499/08 , A61K31/43 , A61K31/431 , A61P31/04 , C07C51/31 , C07D307/88 , C07D317/58 , C07D333/72 , C07D499/00 , C07D499/04 , C07D499/12 , C07D499/32 , C07D499/42 , C07D499/44 , C07D499/62 , C07D499/64 , C07D499/68 , C07D501/04 , C07D501/20 , C07D499/46 , C07D499/48 , C07D499/70
CPC分类号： C07D499/00 , C07C51/31 , C07D307/88 , C07D317/58 , C07D333/72 , Y02P20/55
摘要： This invention relates to a novel class of esters of penicillins and cephalosporins which, upon oral administration are absorbed into the bloodstream where they are split by enzymic action to release the antibacterially active parent penicillin or cephalosporin.
摘要翻译：本发明涉及一类新型的青霉素和头孢菌素酯，其口服给药被吸收到血流中，通过酶作用将其分解，以释放抗菌活性亲本青霉素或头孢菌素。

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