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1. 发明专利

JPS5931777A Beta-lactam antibiotic, manufacture and use 失效
标题翻译： BETA-LACTAM抗生素，制造和使用
公开(公告)号：JPS5931777A
公开(公告)日：1984-02-20
申请号：JP11838183
申请日：1983-07-01
申请人： Bayer Ag
发明人： MIHIYAERU BOBERUKU , KARURU GEORUKU METSUTSUGAA , HANSUUYOAHIMU TSUAIRAA
IPC分类号： A61K31/426 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D277/40 , C07D499/00 , C07D499/44 , C07D499/50 , C07D499/52 , C07D501/20 , C07D501/22 , C07D501/36 , C07D501/46 , C07D501/59 , C07F7/08
CPC分类号： C07D277/20 , C07D499/00 , C07F7/0812
摘要： Antibiotically active penicillins and cephalosporins of the formula in which Z is hydrogen or lower alkoxy, n is 1 or 2, Y, in the form of the free acid, is X is -S-, -n-, -SO- or -SO2-, T is an organic radical, hydrogen or halogen, A is hydroxyl, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, an optionally substituted polycyclic aromatic ring, an optionally substituted 5-membered or 6-membered heterocyclic ring with nitrogen, oxygen and/or sulphur as hetero atoms in the ring, or an optionally substituted polycyclic heterocyclic ring, or non-toxic pharmaceutically tolerated salts thereof.

2. 发明专利

JPS5259181A PREPARATION OF PENICILLINS AND CEPHALOSPORINS CONTAINING NITRO GROUPS 失效
公开(公告)号：JPS5259181A
公开(公告)日：1977-05-16
申请号：JP13398575
申请日：1975-11-10
申请人： ASAHI CHEMICAL IND
发明人： SHIBUYA KAZUYUKI , ISHII KUNIHIKO , ITOU HIRATAKA , KADOI KEIICHI , TAMURA ASAHIRO
IPC分类号： C07D499/48 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D499/12 , C07D499/50 , C07D499/58 , C07D501/06 , C07D501/20 , C07D501/22 , C07D501/28 , C07D501/34 , C07D501/36 , C07D501/40
摘要： PURPOSE:Penicillins and cephalosporins containing nitro group of formula I, whe wherein A is a radical of formula II or III (R is H, lower alkyl, tri-lower alkylsilyl, -CH2OCOR', salt-forming ions; R' is lower alkyl, aryl, aralkyl; X is H, OH, lower alkanoyloxy, aroyloxy); X1 is H, alkyl; Y is a covalent bond, alkylene; R1 is H, lower alkyl, lower alkenyl, OH; for example, 7-(2-nitroacetamido)-cephalosporanic acid.

3. 发明专利

JPS5116689A 失效
公开(公告)号：JPS5116689A
公开(公告)日：1976-02-10
申请号：JP7579975
申请日：1975-06-23
申请人： YEDA RES & DEV
发明人： ABURAHAMU PACHOANIKU , FUOTONA HABIBU
IPC分类号： C07C57/76 , C07D311/76 , C07D333/24 , C07D499/00 , C07D499/44 , C07D499/48 , C07D499/50 , C07D499/58 , C07D501/20

4. 发明专利

JPS58105993A NOVEL BETA-LACTAM DERIVATIVE WITH ISOMERIC STRUCTURE 失效
公开(公告)号：JPS58105993A
公开(公告)日：1983-06-24
申请号：JP20359781
申请日：1981-12-18
申请人： SAGAMI CHEM RES
发明人： TSUNEMOTO DAIEI , KOBORI TAKEO , KONDOU SEI
IPC分类号： C07D499/50 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/20
摘要： NEW MATERIAL:A compound of{R is H, amino-protecting group; Y is formula II, III[R is H, salt-forming cation, carboxyl-protecting group; R is H, CH2R (R is H, residue of nucleophilic compound]}. EXAMPLE:Benzhydril 7-[2-chloromethylene-2-( 2-formylaminothiazol -4- yl )acetamide]-(1-methyl-1H-tetrazol-5-yl)thiomethyl-3-cephem-4-carboxylate. USE:Antibacterial showing strong activity against Pseudomonas areuginosa. PREPARATION:2-Oxo-2-(2-aminothiazol-4-yl)acetic acid derivative is made to react with a Witig's reagent and then with a halogenating reagent and the product is isomerized to give a compound of formula VI. The reaction of a compound of formula V with the one of formula VI is conducted in a solvent in the presence of a dehydrating reagent.

5. 发明授权

US4539149A .beta.-Lactam antibacterial agents 失效
标题翻译： β-内酰胺抗菌剂
公开(公告)号：US4539149A
公开(公告)日：1985-09-03
申请号：US401266
申请日：1982-07-23
申请人： Peter H. Milner
发明人： Peter H. Milner
IPC分类号： C07D501/14 , C07D241/08 , C07D311/12 , C07D463/00 , C07D499/00 , C07D499/21 , C07D499/44 , C07D501/57 , C07D505/00 , C07D499/50 , C07D499/54 , C07D501/24
CPC分类号： C07D241/08 , C07D311/12 , C07D463/22 , C07D499/00 , C07D505/00
摘要： .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.
摘要翻译： β-内酰胺抗生素在与β-内酰胺环的羰基相邻的碳原子上具有α-甲酰氨基取代基，特别是具有部分结构的双环化合物：进一步公开了制备化合物的中间体和方法。

6. 发明授权

US4048320A Penicillins 失效
标题翻译：青霉素
公开(公告)号：US4048320A
公开(公告)日：1977-09-13
申请号：US647131
申请日：1976-01-07
申请人： John Peter Clayton , Peter Hubert Bentley
发明人： John Peter Clayton , Peter Hubert Bentley
IPC分类号： A61K31/43 , A61P31/04 , C07D499/00 , C07D499/04 , C07D499/12 , C07D499/21 , C07D499/46 , C07D499/72 , C07D499/50
CPC分类号： C07D499/00
摘要： A class of 6-methoxy-.alpha.-carboxy penicillins have antibacterial activity against a wide range of Gram-negative organisms.
摘要翻译：一类6-甲氧基-α-羧基青霉素对广泛的革兰氏阴性生物具有抗菌活性。

7. 发明授权

US4044000A Substituted .beta.-lactam antibiotics 失效
标题翻译：取代{62-内酰胺抗生素
公开(公告)号：US4044000A
公开(公告)日：1977-08-23
申请号：US716606
申请日：1976-08-23
申请人： Gary A. Koppel
发明人： Gary A. Koppel
IPC分类号： C07D499/44 , C07D499/46 , C07D499/50 , C07D499/58
CPC分类号： C07D501/57 , C07D499/44
摘要： 6-Alkoxylated-6-acylamidopenicillanic acids and 7-alkoxylated-7-acylamidocephalosporin acids and esters thereof, are provided by reacting a 6-acylamidopenicillanic acid ester or a 7-acylamidocephalosporin ester under anhydrous conditions at -90.degree. C. to -15.degree. C. with an alkali metal salt of a lower alkyl alcohol in the presence of an excess of the corresponding alcohol to produce, in situ, the anionic form of the antibiotic which on halogenation with a positive halogen compound, e.g. t-butyl hypochlorite, yields the compound of the invention. Compounds of the invention, e.g. 6-methoxy-6-phenoxy-acetamidopenicillanic acid and 7-methoxy-7-[2-(2-thienyl)acetamido]cephalosporanic acid are useful antibiotics.
摘要翻译： 6-烷氧基化-6-酰氨基青霉烷酸和7-烷氧基化-7-酰基酰氨基头孢菌素酸及其酯通过6-酰基氨基青霉烷酸酯或7-酰基酰氨基头孢菌素酯在-90℃至-15℃的无水条件下反应来提供用低级烷基醇的碱金属盐在过量相应的醇的存在下，原位生成阴离子形式的抗生素，其用正卤素化合物卤化，例如叔丁基次氯酸盐，得到本发明的化合物。本发明的化合物，例如 6-甲氧基-6-苯氧基 - 乙酰氨基青霉烷酸和7-甲氧基-7- [2-（2-噻吩基）乙酰氨基]头孢烷酸是有用的抗生素。

8. 发明授权

US3984397A 2,3-Lower alkylenepenam-3-carboxylic acid derivatives and processes for the preparation thereof 失效
标题翻译： 2,3-低亚烷基山梨醇-3-羧酸衍生物及其制备方法
公开(公告)号：US3984397A
公开(公告)日：1976-10-05
申请号：US586585
申请日：1975-06-13
申请人： Takashi Kamiya , Tsutomu Teraji , Masashi Hashimoto
发明人： Takashi Kamiya , Tsutomu Teraji , Masashi Hashimoto
IPC分类号： C07D499/04 , C07D499/44 , C07D499/46 , C07D499/50 , C07D499/58
CPC分类号： C07D499/04 , C07D499/44
摘要： A process for the preparation of ##SPC1##Which comprises reacting ##SPC2##With a base, wherein Y is a residue of an acid, wherein R.sup.1 is amino, (halophenylimino-1-lower alkanoylthiomethyl)amino or acylamino and wherein R.sup.2 is carboxy or a protected carboxy, R.sup.3 is lower alkyl, R.sup.4 is lower alkylene and X is --S-- or ##EQU1##
摘要翻译：一种制备其中包含与碱反应的方法，其中Y是酸的残基，其中R 1是氨基，（卤代苯基亚氨基-1-低级烷酰基硫代甲基）氨基或酰基氨基，其中R 2是羧基或保护的羧基，R 3是低级烷基，R4是低级亚烷基，X是-S-或O | -S-。

9. 发明授权

EP0064040B1 Therapeutically active disulphide compounds and their use 失效
标题翻译：治疗活性磷酸盐化合物及其用途
公开(公告)号：EP0064040B1
公开(公告)日：1985-08-28
申请号：EP82850071.0
申请日：1982-04-05
申请人： PHARMACIA AKTIEBOLAG
发明人： Carlsson, Jan Per Erik , Axen, Rolf Erik Axel Verner
IPC分类号： C07H15/24 , C07D499/50 , A61K31/43 , A61K31/70
CPC分类号： C07D213/71 , C07D213/89 , C07D277/78 , C07D499/00 , C07H15/252

10. 发明公开

EP0064040A1 Therapeutically active disulphide compounds and their use 失效
标题翻译： Therapeutisch aktive Disulfidverbindungen und ihre Verwendung。
公开(公告)号：EP0064040A1
公开(公告)日：1982-11-03
申请号：EP82850071.0
申请日：1982-04-05
申请人： PHARMACIA AKTIEBOLAG
发明人： Carlsson, Jan Per Erik , Axen, Rolf Erik Axel Verner
IPC分类号： C07H15/24 , C07D499/50 , A61K31/43 , A61K31/70
CPC分类号： C07D213/71 , C07D213/89 , C07D277/78 , C07D499/00 , C07H15/252
摘要： Therapeutically active organic compound exhibiting at least one group comprising a structure -S'-S"-R, wherein the group -S"-R is defined by R being an organic group comprised in a physiologically acceptable compound H-S"-R obtainable by the splitting of the disulfide bridge -S'-S"- in said structure, in which compound H-S"-R the sulfur atom S" is bound to a carbon atom in a heterocyclic aromatic ring in R having a configuration being such that the compound H-S"-R, while maintaining physiological acceptability, is stabilized, by tautomerism or resonance involving the sulfur atom S" bound to R, so as to be mainly excluded from reaction involving thiol disulfide exchange; S' being bound to an aliphatic carbon atom; and said compound, in addition to the group or groups comprising the structure -S'-S"-R, consisting of a residue of a therapeutically active organic base compound of non-poly-peptide structure bound to S'.
The invention also relates to a method of modifying a therapeutically active organic compound of non-polypeptide structure by introducing a structure -S'-S"-R according to above; a method of treating diseases by administration of a compound according to the invention and also to a pharmaceutical composition containing at least one compound according to the invention.
摘要翻译：表现出至少一个包含结构-Smin -Ssec -R的基团的治疗活性有机化合物，其中基团-Ssec -R由R是由生理学上可接受的化合物HS sec -R中包含的有机基团所述结构中的二硫键-Smin -Ssec的分解，其中化合物HSsec-R硫原子S sec与R中的杂环芳环中的碳原子结合，其结构使得化合物HS 秒-R，同时保持生理可接受性，通过互变异构或包含与R结合的硫原子的共振的共振来稳定，以便主要排除在涉及硫醇二硫化物交换的反应之外; S min与脂肪族碳原子结合; 和所述化合物，除了包含结构-Smin -Ssec-R的基团或基团，由与S min结合的非多肽结构的治疗活性有机碱性化合物的残基组成。本发明还涉及通过引入上述结构-Smin -Ssec -R来修饰非多肽结构的治疗活性有机化合物的方法; 通过施用根据本发明的化合物治疗疾病的方法，还涉及含有至少一种本发明化合物的药物组合物。

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