专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明授权

US4208330A O-Derivatives of thienamycin 失效
标题翻译：噻吩霉素的O-衍生物
公开(公告)号：US4208330A
公开(公告)日：1980-06-17
申请号：US861234
申请日：1977-12-16
申请人： Burton G. Christensen , William J. Leanza
发明人： Burton G. Christensen , William J. Leanza
IPC分类号： C07D477/20 , C07D487/04
CPC分类号： C07D477/20
摘要： Disclosed are O- derivatives (esters and ethers of the secondary alcohol group) of the antibiotic thienamycin which has the following structure: ##STR1## Such derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives, and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.
摘要翻译：公开了具有以下结构的抗生素硫霉素的O-衍生物（仲醇基的酯和醚）：

12. 发明授权

US4713451A Crystalline dimethyliminothienamycin 失效
标题翻译：结晶二甲基亚硫霉素
公开(公告)号：US4713451A
公开(公告)日：1987-12-15
申请号：US597944
申请日：1984-04-09
申请人： William J. Leanza , Kenneth J. Wildonger
发明人： William J. Leanza , Kenneth J. Wildonger
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04 , C07D477/20 , C07D487/04
CPC分类号： C07D477/20
摘要： Crystalline dimethyliminothienamycin having the formula ##STR1## and its preparation are disclosed.
摘要翻译：公开了具有式“IMAGE”及其制备的结晶二甲基亚氨基噻吩霉素。

13. 发明授权

US4397861A N- And carboxyl derivatives of thienamycin 失效
标题翻译：噻吩霉素的N-和羧基衍生物
公开(公告)号：US4397861A
公开(公告)日：1983-08-09
申请号：US321497
申请日：1981-11-16
申请人： Burton G. Christensen , John Hannah , William J. Leanza , David H. Shih
发明人： Burton G. Christensen , John Hannah , William J. Leanza , David H. Shih
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/495 , A61K31/505 , A61K31/675 , A61P31/04 , C07D205/08 , C07D477/20 , C07D487/04 , C07D498/04
CPC分类号： C07D477/20 , C07D205/08
摘要： Disclosed are N-acyl and carboxyl derivatives of the antibiotic thienamycin, which has the following structure: ##STR1## Such derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.
摘要翻译：公开了抗生素噻吩霉素的N-酰基和羧基衍生物，其具有以下结构：所述衍生物可用作抗生素。还公开了制备这种衍生物的方法，包含这些衍生物的药物组合物和治疗方法，包括当指示抗生素效果时施用这样的衍生物和组合物。

14. 发明授权

US4232030A Substituted N-methylene derivatives of thienamycin sulfoxide and sulfone 失效
标题翻译：噻吩霉素亚砜和砜的取代N-亚甲基衍生物
公开(公告)号：US4232030A
公开(公告)日：1980-11-04
申请号：US833619
申请日：1977-09-15
申请人： Burton G. Christensen , William J. Leanza , Kenneth J. Wildonger
发明人： Burton G. Christensen , William J. Leanza , Kenneth J. Wildonger
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04 , C07D477/20 , C07F7/10 , C07F7/18 , C07F9/6561 , C07D487/04 , A61K31/44
CPC分类号： C07D477/20 , C07F7/10 , C07F7/186
摘要： Disclosed are substituted N-methylene derivatives of thienamycin sulfoxide (I, n=1) and sulfone (I, n=2) which may be represented by the following structural formula: ##STR1## wherein X and Y are selected from the group consisting of hydrogen, R, OR, SR, and NR.sup.1 R.sup.2 wherein, inter alia, R is substituted or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R.sup.1 and R.sup.2 are hydrogen or R. Such compounds and their pharmaceutically acceptable salt, ether, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要翻译：公开了噻吩霉素亚砜（I，n = 1）和砜（I，n = 2）的取代的N-亚甲基衍生物，其可以由以下结构式表示：其中X和Y选自氢，R，OR，SR和NR1R2，其中特别是R是取代或未取代的：烷基，烯基，炔基，环烷基，环烷基烷基，芳基，芳烷基，杂芳基，杂芳烷基，杂环基和杂环基烷基; R1和R2是氢或R.这些化合物及其药学上可接受的盐，醚，酯和酰胺衍生物可用作抗生素。还公开了制备这些化合物的方法; 包含这些化合物的药物组合物; 和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。

15. 发明授权

US5606030A Coconjugates of OMPC, HIV related peptides and anionic moieties 失效
标题翻译： OMPC的结合物，HIV相关肽和阴离子部分
公开(公告)号：US5606030A
公开(公告)日：1997-02-25
申请号：US305862
申请日：1994-09-14
申请人： Emilio A. Emini , William J. Leanza , Stephen Marburg , Richard L. Tolman
发明人： Emilio A. Emini , William J. Leanza , Stephen Marburg , Richard L. Tolman
IPC分类号： A61K35/74 , A61K35/76 , A61K38/00 , A61K39/00 , A61K39/21 , A61P31/12 , A61P31/18 , C07K1/113 , C07K14/00 , C07K14/155 , C07K14/16 , C07K14/195 , C07K14/22 , C07K14/41 , C07K16/10 , C07K16/12 , C07K19/00 , C07K17/02 , A61K39/385
CPC分类号： C07K14/005 , C07K14/22 , C07K16/1063 , C07K16/1217 , A61K38/00 , A61K39/00 , C12N2740/16122
摘要： A novel coconjugate comprising an immunogenic protein or protein complex having a first set of covalent linkages to low molecular weight moieties, --a.sup.--, which have an anionic or polyanionic character at physiological pH, and a second set of covalent linkages to peptides comprising Human Immunodeficiency Virus (HIV) Principal Neutralizing Determinants (PNDs), or peptides immunologically equivalent therewith, is useful for inducing anti-peptide immune responses in mammals, for inducing HIV-neutralizing antibodies in mammals, for formulating vaccines to prevent HIV infection or disease, including the Acquired Immune Deficiency Syndrome (AIDS), or for treating humans afflicted with HIV infection or disease.
摘要翻译：包含具有与低分子量部分具有第一组共价键的免疫原性蛋白质或蛋白质复合物的新颖的缀合物， - 在生理pH下具有阴离子或聚阴离子特征，以及与包含人免疫缺陷的肽的第二组共价键病毒（HIV）主要中和决定因子（PND）或与其免疫学相似的肽可用于在哺乳动物中诱导抗肽免疫应答，用于在哺乳动物中诱导HIV-中和抗体，用于配制疫苗以预防HIV感染或疾病，包括获得性免疫缺陷综合征（AIDS）或用于治疗患有HIV感染或疾病的人。

16. 发明授权

US4335043A Substituted N-methylene derivatives of thienamycin 失效
标题翻译：噻吩霉素的取代的N-亚甲基衍生物
公开(公告)号：US4335043A
公开(公告)日：1982-06-15
申请号：US84013
申请日：1979-10-11
申请人： Burton G. Christensen , William J. Leanza , Kenneth J. Wildonger
发明人： Burton G. Christensen , William J. Leanza , Kenneth J. Wildonger
IPC分类号： C07D205/08 , C07F7/10 , C07D487/04 , A61K31/40
CPC分类号： C07F7/10 , C07D205/08
摘要： Disclosed are substituted N-methylene derivatives of thienamycin which may be represented by the following structural formula: ##STR1## wherein X and Y are selected from the group consisting of hydrogen, R, OR, SR, and NR.sup.1 R.sup.2 wherein, inter alia, R is substituted or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R.sup.1 and R.sup.2 are hydrogen or R. Such compounds and their pharmaceutically acceptable salt, ether, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要翻译：公开了噻吩霉素的取代的N-亚甲基衍生物，其可以由以下结构式表示：其中X和Y选自氢，R，OR，SR和NR 1 R 2，其中除了其中R是取代或未取代的：烷基，烯基，炔基，环烷基，环烷基烷基，芳基，芳烷基，杂芳基，杂芳烷基，杂环基和杂环基烷基; R1和R2是氢或R.这些化合物及其药学上可接受的盐，醚，酯和酰胺衍生物可用作抗生素。还公开了制备这些化合物的方法; 包含这些化合物的药物组合物; 和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。

17. 发明授权

US4150145A N-alkylated derivatives of thienamycin sulfoxide and sulfone 失效
标题翻译：噻吩霉素亚砜和砜的N-烷基化衍生物
公开(公告)号：US4150145A
公开(公告)日：1979-04-17
申请号：US833618
申请日：1977-09-15
申请人： Burton G. Christensen , Raymond A. Firestone , William J. Leanza
发明人： Burton G. Christensen , Raymond A. Firestone , William J. Leanza
IPC分类号： C07D477/20 , C07D487/04
CPC分类号： C07D477/20
摘要： Disclosed are N-alkylated derivatives of thienamycin sulfoxide (I, n=1) and sulfone (I, n=2): ##STR1## wherein n=1 or 2; and R.sup.5, R.sup.6, and R.sup.7 are, inter alia, hydrogen or alkyl. Such compounds the their pharmaceutically acceptable O- and carboxyl- derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.
摘要翻译：公开了噻吩那霉素亚砜（I，n = 1）和砜（I，n = 2）的N-烷基化衍生物：其中n = 1或2; 和R 5，R 6和R 7尤其是氢或烷基。这些化合物其药学上可接受的O-和羧基衍生物可用作抗生素。还公开了制备这种衍生物的方法，包含这些衍生物的药物组合物和治疗方法，包括当指示抗生素效果时施用这样的衍生物和组合物。

18. 发明授权

US5274122A Acidic derivatives of homocysteine thiolactone 失效
标题翻译：同型半胱氨酸硫内酯的酸性衍生物
公开(公告)号：US5274122A
公开(公告)日：1993-12-28
申请号：US963324
申请日：1992-10-15
申请人： Richard L. Tolman , Stephen Marburg , William J. Leanza
发明人： Richard L. Tolman , Stephen Marburg , William J. Leanza
IPC分类号： C07D333/36 , C07F9/6553
CPC分类号： C07D333/36 , C07F9/655345
摘要： Homocysteine thiolactone derivatives in which the nitrogen is acylated with groups containing acidic functionalities have been synthesized. These include the succinyl, the carboxymethylglutaryl, the 3-phosphonopropionyl and the 3-sulfopropionyl derivatives. These thiolactones can be used to introduce a thiol functionality into proteins such as the outer membrane protein complex of Neisseria meninioitidis (OMPC) allowing conjugation with electrophilic ligands. This chemistry is similar to known N-acetyl-homocysteine thiolactone chemistry, but the pK.sub.a values are such that at pH 7, concomitant negative charge is introduced into the conjugate. Such negative charge neutralizes excess positive charge introduced when arginine- and lysine-rich peptides are bonded as ligands. In the case of OMPC, introduction of positive charge commonly effects irreversible precipitation of the conjugate. Conjugates prepared with the anionic thiolactones have improved solubility.
摘要翻译：已经合成了其中氮与含有酸性官能团的基团进行酰化的同型半胱氨酸硫内酯衍生物。这些包括琥珀酰基，羧甲基葡萄糖基，3-膦酰基丙酰基和3-磺基丙酰基衍生物。可以使用这些硫内酯将硫醇官能团引入蛋白质，例如允许与亲电子配体缀合的奈瑟氏球菌（OMPC）的外膜蛋白复合物。该化学类似于已知的N-乙酰基 - 同型半胱氨酸硫内酯化学，但pKa值使得在pH7时，伴随的负电荷被引入缀合物中。当富含精氨酸和富含赖氨酸的肽作为配体键合时，这种负电荷中和了引入的过量正电荷。在OMPC的情况下，引入正电荷通常会影响缀合物的不可逆沉淀。用阴离子硫醇内酯制备的缀合物具有改善的溶解性。

19. 发明授权

US4235920A N-Alkylated derivatives of thienamycin 失效
标题翻译：噻吩霉素的N-烷基化衍生物
公开(公告)号：US4235920A
公开(公告)日：1980-11-25
申请号：US861235
申请日：1977-12-16
申请人： Burton G. Christensen , Raymond A. Firestone , William J. Leanza
发明人： Burton G. Christensen , Raymond A. Firestone , William J. Leanza
IPC分类号： C07D205/08 , C07D477/20 , C07D498/04 , C07D407/04 , A61K31/40
CPC分类号： C07D477/20 , C07D205/08
摘要： Disclosed are N-alkylated derivatives of the antibiotic thienamycin, which has the following structure: ##STR1## Such compounds and their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives, and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.
摘要翻译：公开了抗生素硫霉素的N-烷基化衍生物，其具有以下结构：此类化合物及其药学上可接受的盐，酯和酰胺衍生物可用作抗生素。还公开了制备这种衍生物的方法，包含这种衍生物的药物组合物，以及治疗方法，包括当指示抗生素效果时施用这样的衍生物和组合物。

20. 发明授权

US4235917A N-Alkyl-N-acyl derivatives of thienamycin 失效
标题翻译：噻吩霉素的N-烷基-N-酰基衍生物
公开(公告)号：US4235917A
公开(公告)日：1980-11-25
申请号：US793974
申请日：1977-05-05
申请人： Burton G. Christensen , William J. Leanza
发明人： Burton G. Christensen , William J. Leanza
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04 , C07D477/20 , C07F9/6561 , C07D487/04
CPC分类号： C07D477/20 , C07F9/65611
摘要： Disclosed are N-alkyl- N-acyl derivatives of the antibiotic thienamycin having the following structural formula: ##STR1## wherein R.sup.1 is, inter alia, alkyl, alkenyl, aryl or aralkyl; and R.sup.2 is acyl. Such compounds, including their O- and carboxyl derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要翻译：公开了具有以下结构式的抗生素硫霉素的N-烷基-N-酰基衍生物：其中R 1特别是烷基，烯基，芳基或芳烷基; R2是酰基。这些化合物，包括其O-和羧基衍生物可用作抗生素。还公开了制备这些化合物的方法，包含这些化合物的药物组合物，以及治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。

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