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. 发明公开

EP0272061A3 Crystalline cephalosporin antibiotic salts and solvates 失效
标题翻译：结晶CEPHALOSPORIN抗生素和溶剂
公开(公告)号：EP0272061A3
公开(公告)日：1990-03-28
申请号：EP87310907.8
申请日：1987-12-11
申请人： ELI LILLY AND COMPANY
发明人： Katner, Allen Samuel
IPC分类号： C07D501/46 , A61K31/545
CPC分类号： C07D501/46 , C07D519/00
摘要： The crystalline sulfate dihydrate, dimethylacetamide hydrate and dimethylformamide hydrate solvates of the antibiotic syn -7-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-(3-methyl-3H-imidazolo[4,5-c]pyridinium-5-ylmethyl)-3-cephem-4-carboxylate are provided.

2. 发明公开

EP0138552A2 Improvements on or relating to 3-bicyclicpyridinium-methyl cephalosporins 失效
标题翻译： Herstellung von 3-biclyclipyridinium-methyl Cephalosporinen。
公开(公告)号：EP0138552A2
公开(公告)日：1985-04-24
申请号：EP84306866.9
申请日：1984-10-09
申请人： ELI LILLY AND COMPANY
发明人： Katner, Allen Samuel
IPC分类号： C07D501/46
CPC分类号： C07D471/04 , C07D513/04
摘要： Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetyiamino group and of the formula
in which R is hydrogen, formyl, a-aminoadipoyl, protected a-aminoadipoyl, or an acyl group of the formula
in which R' is a 5- or 6-membered heterocyclic ring of the for mulae

R" is hydrogen, C 1 -C 4 alkyl, a carboxy-substituted alkyl or carboxy-substituted cycloalkyl group of the formula:

in which n is 0-3; a and b when taken separately are, independently, hydrogen or C 1 -C 3 alkyl, and when taken together with the carbon to which they are bonded form a C 3 -C 7 carbocyclic ring; R"' is hydrogen, C 1 -C 4 alkoxy, amino, or OR°, in which R° is indanyl, phthalidyl, or an acyloxymethyl group of the formula -CH 2 -O-C(O)-R 2 in wich R 2 is C 1 -C 4 alkyl or phenyl; or COOR° is a protected carboxy group; or R" is an N-substituted carbamoyl group of the formula
in which R"" is C 1 -C 4 alkyl, phenyl or C 1 -C 3 alkyl substituted by phenyl;

Y and m, independently, are integers equal to 0,1,2 or 3, provided that y plus m equals 3;
R 1 is hydrogen, C 1 -C 4 alkyl, phenyl, thienyl, amino or C 1 -C 4 alkanoylamino;
X is O, S or N-R 2 , where R 2 is hydrogen or C 1 -C 4 alkyl; or a pharmaceutically-acceptable salt or biologically-cleavable ester thereof.
摘要翻译：通过2-（5-或6-元杂环）-2-肟基乙酰基氨基和式CHEM的7-位取代的头孢菌素化合物，其中R是氢，甲酰基，α-氨基己二酰基，保护的α-氨基己二酰基，或式CHEM的酰基，其中R min是式CHEM> R sec的5-或6-元杂环是氢，C1-C4烷基，羧基取代的烷基或羧基取代的环烷基组式为：其中n为0-3的; a和b分别独立地为氢或C 1 -C 3烷基，并且当与它们所键合的碳一起形成C 3 -C 7碳环时; R“是氢，C 1 -C 4烷氧基，氨基或OR 0，其中R 0是2,3-二氢化茚基，邻苯二酰基或式-CH 2 -O（O）-R 2的酰氧基甲基，其中R 2是 C 1 -C 4烷基或苯基; 或COOR <0>是被保护的羧基; 或R sec为式 - @ -NHR sec sec的N-取代氨基甲酰基，其中R sec sec为C 1 -C 4烷基，苯基或被苯基取代的C 1 -C 3烷基; Y和m独立地是等于0,1,2或3的整数，条件是y加m等于3; R 1是氢，C 1 -C 4烷基，苯基，噻吩基，氨基或C 1 -C 4烷酰基氨基; X是O，S或N-R 2，其中R 2是氢或C 1 -C 4烷基; 或其药学上可接受的盐或生物可裂解的酯。

3. 发明公开

EP0233780A3 O-substituted oximino cephalosporins 失效
标题翻译： O-取代的肟基头孢菌素
公开(公告)号：EP0233780A3
公开(公告)日：1989-02-01
申请号：EP87301364.3
申请日：1987-02-17
申请人： ELI LILLY AND COMPANY
发明人： Katner, Allen Samuel
IPC分类号： C07D501/36 , A61K31/545
CPC分类号： C07D501/36
摘要： O-Substituted oximinocephalosporins represented by the formula
wherein R is a 5-membered or 6-membered heterocycle, preferably amino-substituted, e.g., 2-aminothiazol-4-yl, R 1 is an arylalkyl, aryloxyalkyl, or arylthioalkyl group, especially substituted benzyl; R 2 is a 1,2,4-triazin-3-yl thio group; and M is a salt or a biologically labile ester group; are potent antibacterial agents. Also provided are antibiotic formulations of said compounds and a method for treating infectious diseases in man or other animals comprising the administration of said compounds.
摘要翻译：由下式代表的O-取代的肟基头孢菌素：其中R是5元或6元杂环，优选氨基取代的，例如2-氨基噻唑-4-基，R1是芳基烷基，芳氧基烷基或芳硫基烷基，特别是取代的苄基 ; R2是1,2,4-三嗪-3-基硫基; M是盐或生物不稳定的酯基; 是有效的抗菌剂。还提供了所述化合物的抗生素制剂以及用于治疗人或其他动物中的感染性疾病的方法，其包括施用所述化合物。

4. 发明公开

EP0048167A2 Bis-tetrazolemethyl thiols and their preparation 失效
标题翻译：双 - 四唑甲基 - 硫代和Herstellung。
公开(公告)号：EP0048167A2
公开(公告)日：1982-03-24
申请号：EP81304240.5
申请日：1981-09-16
申请人： ELI LILLY AND COMPANY
发明人： Katner, Allen Samuel , Bogard, Stephen James
IPC分类号： C07D257/04
CPC分类号： C07D257/04
摘要： 1H- and 2H-tetrazole-5-thiol compounds of the formula
and the C 1 -C 3 alkyl derivatives thereof are described. These compounds are useful in the preparation of broad spectrum cephalosporin antibiotics.
摘要翻译：描述了式...的CH-和2H-四唑-5-硫醇化合物及其C 1 -C 3烷基衍生物。这些化合物可用于制备广谱头孢菌素类抗生素。

5. 发明公开

EP0002605A1 Cephalosporin compounds and formulations containing them for use in the treatment of bacterial infections and the preparation of the cephalosporin compounds 失效
标题翻译：含有它们Cephalosporinderivative和药物组合物，其用于治疗细菌感染和Cephalosporinderivative的制备。
公开(公告)号：EP0002605A1
公开(公告)日：1979-06-27
申请号：EP78300801.4
申请日：1978-12-13
申请人： ELI LILLY AND COMPANY
发明人： Katner, Allen Samuel
IPC分类号： C07D501/36 , A61K31/545
CPC分类号： C07D501/36 , Y02P20/55
摘要： Cephalosporin antibiotics of formula
wherein R is hydrogen, an alkali metal cation, or a carboxylic acid protecting group; R 1 is hydrogen or methoxy; R 2 is hydrogen or an amino protecting group; R 3 is hydrogen or C 1 -C 4 alkyl; and R 4 is C 1 -C 4 alkyl.

6. 发明公开

EP0048167A3 Bis-tetrazolemethyl thiols and their preparation 失效
标题翻译：双 - 四唑甲基硫醇及其制备
公开(公告)号：EP0048167A3
公开(公告)日：1982-06-16
申请号：EP81304240
申请日：1981-09-16
申请人： ELI LILLY AND COMPANY
发明人： Katner, Allen Samuel , Bogard, Stephen James
IPC分类号： C07D257/04
CPC分类号： C07D257/04
摘要： 1H- and 2H-tetrazole-5-thiol compounds of the formula
and the C 1 -C 3 alkyl derivatives thereof are described. These compounds are useful in the preparation of broad spectrum cephalosporin antibiotics.

7. 发明公开

EP0048166A1 Bicyclic 1-oxa-beta-lactam compounds, their preparation and pharmaceutical formulations containing them 失效
标题翻译：双环1-氧杂β-内酰胺化合物，它们的制备和含有它们的药物组合物。
公开(公告)号：EP0048166A1
公开(公告)日：1982-03-24
申请号：EP81304239.7
申请日：1981-09-16
申请人： ELI LILLY AND COMPANY
发明人： Katner, Allen Samuel
IPC分类号： C07D498/04 , A61K31/535
CPC分类号： C07D257/04 , C07D505/00
摘要： Bicyclic 1-oxa-β-lactam diacid antibiotics are described. They are represented by the formula
wherein R is an a-carboxysubstituted arylmethyl group of the formula
wherein R' is hydrogen, hydroxy, protected hydroxy, acetoxy, C 1 -C 3 alkyl, or halogen;

R° is hydrogen or methoxy;
R 1 and R,' are hydrogen or a carboxy protecting group; and when R 1 and R 1 ' are hydrogen, the pharmaceutically acceptable salts thereof.

The compounds are prepared by reacting the corresponding 3-halomethyl diester with 1-cyanomethyl-1H-tetrazole-5-thiol followed by deesterification.

8. 发明公开

EP0048165A1 Bis-tetrazolemethyl substituted beta-lactam antibiotics, their preparation and pharmaceutical formulations containing them 失效
标题翻译：双 - 取代的tetrazolmethylβ-内酰胺抗生素，其制备方法和含有它们的药物制剂。
公开(公告)号：EP0048165A1
公开(公告)日：1982-03-24
申请号：EP81304238.9
申请日：1981-09-16
申请人： ELI LILLY AND COMPANY
发明人： Katner, Allen Samuel
IPC分类号： C07D498/04 , A61K31/535
CPC分类号： C07D257/04 , C07D505/00
摘要： Broad spectrum β-lactam antibiotics are described. They are represented by the formula
wherein R is hydrogen or an acyl group of the formula
wherein R° is an aryl or aralkyl group of the formula
wherein R' is phenyl or phenyl substituted by halogen, hydroxy amino, acetamido, C,-C 4 alkyl, C 1 -C 4 alkoxy, cyano, carboxy, carboxamido, carboxymethyl, C,-C 4 alkoxycarbony-Imethyl, hydroxymethyl, or aminomethyl; or R' is a di- or tri-substituted phenyl group of the formula
wherein each of a, a', and a" are independently hydrogen, halogen, hydroxy, C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and
or R° is an aryloxymethyl or arylthiomethyl group of the formula
wherein R' has the same meanings as defined above. and z is O or S; or R° is a heterocyclic methyl group of the formula
wherein R 2 is thienyl, furyl, 1H-tetrazol-1-yl, 1H-tetrazol-5-yl,
wherein each b is hydrogen, amino, protected-amino, C 1 -C 3 alkyl or phenyl; or R° is a group of the formula
wherein R 3 is R' as defined above and in addition 1,4-cyclohexadienyl, thienyl or furyl, and Q is hydroxy, carboxy, sulfo, or amino; or R° is an oximino substituted group represented by the formula
wherein R 4 is R' as defined above and in addition thienyl, furyl, or
wherein b has the same meanings as defined above and R 5 is hydrogen, or C 1 -C 4 alkyl; or R° is a group of the formula
wherein R 3 is as defined above and R 6 is phenyl substituted by 1-3 hydroxy groups or pyridyl substituted with from 1-3 hydroxy groups; or R 6 is a group of the formula
wherein R' is C 1 -C 4 alkylamino, phenyl, chlorophenyl, furyl, styrryl, chlorostyrryl, or nitrostyrryl; or R 6 is a group of the formula
wherein n' is 1 or 2 and m is 2 or 3 with the limitation that when n' is 2, m is 2; and R 8 is hydrogen, C 1 -C 3 alkyl, C 2 -C 4 alkanoyl, or C 1 -C 3 alkylsulfonyl; R, is hydrogen or a carboxy protecting group; R 2 is hydrogen or methoxy; R 3 is a bis-tetrazolemethyl group of the formula
wherein R 4 is hydrogen or C 1 -C 3 alkyl; and when R, is hydrogen, the pharmaceutically acceptable salts thereof.
The compounds are obtained by reacting a 7-acylamino-3-halomethyl-1-oxa-β-lactam ester with the desired 1- or 2-tetrazolemethyl substituted 1H or 2H tetrazole-5-thiol, or alternatively by reacting a 7-amino-3-halomethyl-1-oxa-b-lactam ester with the bis-tetrazole thiol and then N-acylating with the desired carboxylic acid.

9. 发明公开

EP0272061A2 Crystalline cephalosporin antibiotic salts and solvates 失效
标题翻译： Kristalline，抗生素Cephalosporinsalze不溶性。
公开(公告)号：EP0272061A2
公开(公告)日：1988-06-22
申请号：EP87310907.8
申请日：1987-12-11
申请人： ELI LILLY AND COMPANY
发明人： Katner, Allen Samuel
IPC分类号： C07D501/46 , A61K31/545
CPC分类号： C07D501/46 , C07D519/00
摘要： The crystalline sulfate dihydrate, dimethylacetamide hydrate and dimethylformamide hydrate solvates of the antibiotic syn -7-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-(3-methyl-3H-imidazolo[4,5-c]pyridinium-5-ylmethyl)-3-cephem-4-carboxylate are provided.
摘要翻译：抗生素顺式-7- [2-（2-氨基噻唑-4-基）-2-甲氧基亚氨基乙酰氨基] -3-（3-甲基-3H-咪唑并[4,3-a]嘧啶）的结晶硫酸盐二水合物，二甲基乙酰胺水合物和二甲基甲酰胺水合物溶剂合物， 5-c]吡啶鎓-5-基甲基）-3-头孢烯-4-羧酸酯。

10. 发明公开

EP0233780A2 O-substituted oximino cephalosporins 失效
标题翻译： O-取代的肟基头孢菌素。
公开(公告)号：EP0233780A2
公开(公告)日：1987-08-26
申请号：EP87301364.3
申请日：1987-02-17
申请人： ELI LILLY AND COMPANY
发明人： Katner, Allen Samuel
IPC分类号： C07D501/36 , A61K31/545
CPC分类号： C07D501/36
摘要： O-Substituted oximinocephalosporins represented by the formula
wherein R is a 5-membered or 6-membered heterocycle, preferably amino-substituted, e.g., 2-aminothiazol-4-yl, R 1 is an arylalkyl, aryloxyalkyl, or arylthioalkyl group, especially substituted benzyl; R 2 is a 1,2,4-triazin-3-yl thio group; and M is a salt or a biologically labile ester group; are potent antibacterial agents. Also provided are antibiotic formulations of said compounds and a method for treating infectious diseases in man or other animals comprising the administration of said compounds.

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