专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4159984A Reductive cleavage of oxazolidine compounds 失效
标题翻译：还原性裂解恶唑烷化合物
公开(公告)号：US4159984A
公开(公告)日：1979-07-03
申请号：US790618
申请日：1977-04-25
申请人： Mitsuru Yoshioka , Teruji Tsuji , Yasuhiro Nishitani , Wataru Nagata
发明人： Mitsuru Yoshioka , Teruji Tsuji , Yasuhiro Nishitani , Wataru Nagata
IPC分类号： C07D205/08 , C07D205/085 , C07D205/095 , C07D499/00 , C07D499/44 , C07D499/48 , C07D499/72 , C07D503/00 , C07D505/00
CPC分类号： C07D205/085 , C07D499/00 , C07D505/00
摘要： Compounds represented by the following formula prepared from 6-aminopenicillanic acid are key intermediates in a stereo-specific synthesis of 1-oxadethiacephalosporins, highly active antibiotics: ##STR1## [wherein COA and COB each is carboxy or protected carboxy;Cox is carboxy, protected carboxy, or a group of the formula --COCQ.dbd.N.sub.2 or --COCHQ--Z (in which Q is hydrogen, lower alkyl or aryl; and Z is hydrogen or a nucleophilic group);Hal is halogen;R is lower alkyl or aralkyl; andY is hydrogen or acyl].
摘要翻译：由6-氨基青霉烷酸制备的下列化合物所代表的化合物是立体特异性合成1-羟基乙硫菌素，高活性抗生素的关键中间体：其中COA和COB各自为羧基或被保护的羧基; COX是羧基，受保护的羧基或式-COCQ = N2或-COCHQ-Z（其中Q是氢，低级烷基或芳基; Z是氢或亲核基团）的基团; 卤素是卤素; R是低级烷基或芳烷基; 和Y是氢或酰基]。

2. 发明授权

US4009159A Halogenated penam derivatives and the preparation thereof 失效
公开(公告)号：US4009159A
公开(公告)日：1977-02-22
申请号：US427232
申请日：1973-12-21
申请人： Takashi Kamiya , Yoshihisa Saito , Tsutomu Teraji , Osamu Nakaguti , Teruo Oku , Hitoshi Nakamura , Masashi Hashimoto
发明人： Takashi Kamiya , Yoshihisa Saito , Tsutomu Teraji , Osamu Nakaguti , Teruo Oku , Hitoshi Nakamura , Masashi Hashimoto
IPC分类号： C07D205/08 , C07D205/095 , C07D499/00 , C07D499/04 , C07D499/21 , C07D499/44 , C07D501/10 , C07D501/14 , C07D499/46 , C07D499/48 , C07D499/64
CPC分类号： C07D499/00 , C07D205/08 , C07D205/095
摘要： A penam derivative having the formula: ##STR1## wherein X represents a halogen atom, and wherein R.sub.1 represents an amino or acylamino, and R.sub.3 represents a radical selected from the group consisting of carboxy, ester, acid amide, acid anhydride, acid halide, and acid azide.

3. 发明授权

US3971776A Thio-.beta.-lactam penicillins 失效
标题翻译： Thio- {62-内酰胺青霉素
公开(公告)号：US3971776A
公开(公告)日：1976-07-27
申请号：US551221
申请日：1975-02-19
申请人： Christopher M. Cimarusti , Paul Wojtkowski , Joseph E. Dolfini
发明人： Christopher M. Cimarusti , Paul Wojtkowski , Joseph E. Dolfini
IPC分类号： C07D499/00 , C07D499/44 , C07D499/46 , C07D499/48
CPC分类号： C07D499/00
摘要： Thio-.beta.-lactam penicillins of the general formula ##EQU1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal; R.sub.1 is hydrogen, lower alkyl, cycloalkyl, phenyl, lower alkoxyphenyl, phenoxy, phenyl-lower alkyl or certain heterocyclic groups; R.sub.2 is hydrogen, amino, carboxy or ureido; and n is 0 or 1; are useful as antimicrobial agents.
摘要翻译：通式R2 | R1-CHn-CO-NH的硫代-β-内酰胺青霉素，其中R是氢，低级烷基，苯基 - 低级烷基，三卤代乙基，碱金属或碱土金属; R 1是氢，低级烷基，环烷基，苯基，低级烷氧基苯基，苯氧基，苯基 - 低级烷基或某些杂环基; R2是氢，氨基，羧基或脲基; 并且n为0或1; 作为抗微生物剂是有用的。

4. 发明授权

US3093633A Novel penicillin compounds 失效
公开(公告)号：US3093633A
公开(公告)日：1963-06-11
申请号：US3945660
申请日：1960-06-29
申请人： PFIZER & CO C
发明人： HOBBS DONALD C
IPC分类号： C07D499/00 , C07D499/48
CPC分类号： C07D499/00

5. 发明申请

US20110269731A1 NANOPARTICLES OF BETA-LACTAM DERIVATIVES 审中-公开
标题翻译： BETA-LACTAM衍生物的纳米颗粒
公开(公告)号：US20110269731A1
公开(公告)日：2011-11-03
申请号：US13126756
申请日：2009-10-28
申请人： Patrick Couvreur , Didier Demaele , Fatima Zouhiri
发明人： Patrick Couvreur , Didier Demaele , Fatima Zouhiri
IPC分类号： A61K31/43 , C07D499/48 , A61P31/04 , B82Y5/00 , B82Y99/00 , B82Y40/00
CPC分类号： A61K47/54
摘要： The present invention relates to a complex made up of at least one beta-lactam molecule covalently bonded to at least one hydrocarbon radical including at least 18 carbon atoms and containing at least one unit of 2-methyl-buta-2-ene, to nanoparticles of said complexes, and to a method for preparing same, said complex and/or said nanoparticles optionally being in the form of a lyophilisate. The present invention also relates to a pharmaceutical composition including at least said complex and/or said nanoparticles. The invention finally relates to said complex and/or to said nanoparticles for the treatment and/or prevention of bacterial infections, in particular caused by strains that are sensitive to beta-lactams.
摘要翻译：本发明涉及一种由至少一种共价结合至少一个包含至少18个碳原子并含有至少一个2-甲基丁-2-烯单元的烃基的β-内酰胺分子与纳米颗粒组成的复合物的所述复合物，以及其制备方法，所述复合物和/或所述纳米颗粒任选地为冻干物形式。本发明还涉及包含至少所述复合物和/或所述纳米颗粒的药物组合物。本发明最终涉及用于治疗和/或预防细菌感染的所述复合物和/或所述纳米颗粒，特别是由对β-内酰胺类敏感的菌株引起的。

6. 发明申请

US20040110740A1 Beta-lactamase inhibitor prodrug 失效
标题翻译： β-内酰胺酶抑制剂前药
公开(公告)号：US20040110740A1
公开(公告)日：2004-06-10
申请号：US10648408
申请日：2003-08-25
申请人： Pfizer Inc
发明人： Anthony Marfat , Dale G. McLeod
IPC分类号： A61K031/43 , C07D499/48
CPC分类号： C07D499/00
摘要： Prodrugs of 6-null-hydroxymethylpenicillanic acid sulfone having the structure 1 wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention or a solvate thereof, an optional beta-lactam antibiotic and a pharmaceutically acceptable excipient. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a beta-lactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.
摘要翻译：公开了具有其中R为H或甲基的结构及其溶剂合物的6-β-羟甲基青霉烷酸砜的前药。还公开了包含本发明的前药或其溶剂合物，任选的β-内酰胺抗生素和药学上可接受的赋形剂的药物组合物。进一步公开的是通过施用有效量的β-内酰胺抗生素和增加有效量的本发明的前药或其溶剂化物来增加哺乳动物中β-内酰胺抗生素的治疗有效性的方法。另外公开了通过向有需要的哺乳动物施用治疗有效量的本发明药物组合物来治疗哺乳动物细菌感染的方法。

7. 发明授权

US4722924A Peptide substituted penicillins 失效
标题翻译：肽取代青霉素
公开(公告)号：US4722924A
公开(公告)日：1988-02-02
申请号：US766429
申请日：1985-08-22
申请人： Jack E. Baldwin
发明人： Jack E. Baldwin
IPC分类号： A61K31/43 , A61K38/00 , A61P31/04 , C07C59/315 , C07C271/22 , C07D499/00 , C07D499/48 , C07D499/62 , C07K5/02 , C07K5/06 , C12N9/00 , C12P37/00 , C12R1/465 , C12R1/75 , C12R1/82
CPC分类号： C12N9/93 , C07C271/22 , C07C59/315 , C07D499/00 , C07K5/0215 , C12P37/00 , A61K38/00
摘要： A compound of formula I or a physiologically acceptable salt thereof ##STR1## wherein X represents sulphur or methylene, R.sub.1 represents hydrogen, amino or an acylated or carbamylated amino group, R.sub.2 represents hydrogen or an alkyl group and R.sub.3 represents an alkoxy group.
摘要翻译：式I化合物或其生理上可接受的盐其中X表示硫或亚甲基，R 1表示氢，氨基或酰化或氨基甲酰化的氨基，R 2表示氢或烷基，R 3表示烷氧基。

8. 发明授权

US4462934A Bis-esters of dicarboxylic acids with amoxicillin and certain hydroxymethylpenicillanate 1,1-dioxides 失效
标题翻译：二羧酸与阿莫西林和某些羟甲基青霉素1,1-二氧化物的双酯
公开(公告)号：US4462934A
公开(公告)日：1984-07-31
申请号：US481108
申请日：1983-03-31
申请人： Vytautas J. Jasys
发明人： Vytautas J. Jasys
IPC分类号： C07D519/06 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/32 , C07D499/68 , C07D499/86 , C07D499/861 , C07D499/87 , C07D499/897 , C07D519/00 , C07D499/48
CPC分类号： C07D499/00
摘要： Antibacterial bis-esters of 1,4-cyclohexanedicarboxylic acids and alkane dicarboxylic acids wherein the ester moieties are derived from different alcohols; one alcohol being hydroxymethylpenicillanate 1,1-dioxide, or the 6-beta-hydroxymethyl or the 6-alpha-aminomethyl derivative thereof; and the other being 6-[D-(2-amino-2-(p-hydroxyphenyl)acetamido)]penicillanic acid (amoxicillin); and pharmaceutically acceptable salts thereof; a method for the use of said esters and their salts, and methods for their preparation.
摘要翻译： 1,4-环己烷二羧酸和烷二羧酸的抗菌双酯，其中酯部分衍生自不同的醇; 一种醇是羟甲基青霉素1,1-二氧化物，或6-β-羟甲基或其6-α-氨基甲基衍生物; 另一个是6- [D-（2-氨基-2-（对羟基苯基）乙酰氨基）]青霉烷酸（阿莫西林）; 及其药学上可接受的盐; 所述酯及其盐的使用方法及其制备方法。

9. 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。

10. 发明授权

US4008220A Penicillins 失效
标题翻译：青霉素
公开(公告)号：US4008220A
公开(公告)日：1977-02-15
申请号：US495914
申请日：1974-08-08
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： C07D499/00 , C07D499/68 , C07D499/48
CPC分类号： C07D499/00 , Y02P20/55
摘要： A penicillin of the formula: ##STR1## wherein ##STR2## is a six-membered heteroaromatic ring containing 1 or 2 nitrogen atoms as the hetero atom, Y is hydrogen, lower alkanoyl or lower alkoxycarbonyl, R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkanoyl, benzoyl, lower alkylmercapto, hydroxyl, mercapto, hydroxy(lower)alkyl, halogen or cyano or R.sub.1 and R.sub.2 may link together to form a lower alkylene chain which may be substituted with an oxo group, and Z is phenyl, hydroxyphenyl, lower alkyl, cyclohexadienyl, thienyl or isothiazolyl, which is prepared by reacting a compound of the formula: ##STR3## wherein Z is as defined above or its derivative with a carboxylic acid of the formula: ##STR4## wherein ##STR5## and R.sub.2 are each as defined above or its reactive derivative, if necessary, followed by hydrolysis or acylation of the resulting product and/or elimination of any protective group and which is useful as an antimicrobial agent against various gram-positive and gram-negative bacteria including Pseudomonas.
摘要翻译：一种下式的青霉素：其中是含有1或2个氮原子作为杂原子的六元杂芳环，Y是氢，低级烷酰基或低级烷氧基羰基，R 1和R 2各自是氢，低级烷基，低级烷酰基，苯甲酰基，低级烷基巯基，羟基，巯基，羟基（低级）烷基，卤素或氰基，或者R 1和R 2可以连接在一起形成可被氧代基取代的低级亚烷基链，Z是苯基，低级烷基，环己二烯基，噻吩基或异噻唑基，其通过使下式化合物：其中Z如上所定义或其衍生物与下式的羧酸反应制备：其中和R2 各自如上所定义，或其反应性衍生物，如果需要，随后水解或酰化所得产物和/或消除任何保护基团，并且其可用作针对各种革兰氏阳性和革兰氏阴性菌的抗微生物剂，包括 uding假单胞菌

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式