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1. 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。

2. 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。

3. 发明授权

US4839352A N-acyl derivatives of thienamycin 失效
标题翻译：噻吩霉素的N-酰基衍生物
公开(公告)号：US4839352A
公开(公告)日：1989-06-13
申请号：US90400
申请日：1987-08-27
申请人： Louis Barash , Burton G. Christensen , John Hannah , William J. Leanza , David H. Shih
发明人： Louis Barash , Burton G. Christensen , John Hannah , William J. Leanza , David H. Shih
IPC分类号： C07D205/08 , C07D477/20 , C07D498/04
CPC分类号： C07D477/20 , C07D205/08
摘要： Disclosed are N-acyl derivatives of the antibiotic thienamycin having the following structural formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen and acyl. Such derivatives and their pharmaceutically acceptable salts, 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式的抗生素硫霉素的N-酰基衍生物：其中R 1和R 2独立地选自氢和酰基。这些衍生物及其药学上可接受的盐可用作抗生素。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。

4. 发明授权

US4650794A 6-(1-hydroxyethyl)-2-carbamimidoyl-pen-2-em-3-carboxylic acids 失效
标题翻译： 6-（1-羟基乙基）-2-氨甲脒基 - 二氧戊环-3-羧酸
公开(公告)号：US4650794A
公开(公告)日：1987-03-17
申请号：US373088
申请日：1982-04-29
申请人： Burton G. Christensen , Frank P. DiNinno , William J. Leanza , Ronald W. Ratcliffe
发明人： Burton G. Christensen , Frank P. DiNinno , William J. Leanza , Ronald W. Ratcliffe
IPC分类号： C07D499/88 , C07D499/00 , A61K31/425
CPC分类号： C07D499/88
摘要： Disclosed are 6-(1-hydroxyethyl)-2-carbamimidoyl-pen-2-em-3-carboxylic acids (I) having the representative structure: ##STR1## wherein: A is a direct, single bond connecting the indicated S and C atoms, or A is a cyclic or acyclic connecting group selected, inter alia, from alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl; R.sup.1 and R.sup.2, which define the carbamimidoyl function, are, inter alia, independently selected from hydrogen, alkyl, aryl, alkoxy, amino; additionally, said carbamimidoyl is characterized by cyclic structures achieved by the joinder of the two nitrogen atoms via their substituents and by their joinder to connecting group A; additionally, "carbamimidiums" are disclosed by quaternization of one of the nitrogen atoms of said carbamimidoyl. Such compounds as well as their pharmaceutically acceptable salt, 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：公开了具有以下代表性结构的6-（1-羟基乙基）-2-氨基甲脒基 - 二-2-甲基-3-羧酸（I）：其中：A是连接所指示的S和 C原子或A是环状或无环连接基团，特别是选自烷基，环烷基，芳基，杂芳基，杂烷基; 定义氨基甲酰基官能团的R 1和R 2尤其独立地选自氢，烷基，芳基，烷氧基，氨基; 另外，所述的氨基甲脒基的特征在于通过两个氮原子通过它们的取代基并通过它们与连接基团A的连接而实现的环状结构; 此外，“氨基甲酰胺”通过所述氨甲脒基的氮原子之一的季铵化来公开。这些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。

5. 发明授权

US4194047A 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：US4194047A
公开(公告)日：1980-03-18
申请号：US852425
申请日：1977-11-17
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 , C07D477/20 , C07D498/04 , C07F7/10 , C07D487/04 , A61K31/40
CPC分类号： C07D477/20 , C07D205/08 , C07F7/10
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。

6. 发明授权

US4675317A 2-unsaturated alkylthio-pen-2-em-3-carboxylic acids 失效
标题翻译： 2-不饱和烷硫基 - 笔-2-烯-3-羧酸
公开(公告)号：US4675317A
公开(公告)日：1987-06-23
申请号：US460728
申请日：1983-01-25
申请人： Frank P. DiNinno , William J. Leanza , Ronald W. Ratcliffe , David A. Muthard
发明人： Frank P. DiNinno , William J. Leanza , Ronald W. Ratcliffe , David A. Muthard
IPC分类号： C07D205/09 , C07D205/095 , C07D499/88 , C07F7/18 , C07D499/00 , A61K31/425
CPC分类号： C07D499/88 , C07D205/09 , C07D205/095 , C07F7/186
摘要： Disclosed are 6- and 6,6-disubstituted-2-substituted thio-pen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from: hydrogen; substituted and unsubstituted: alkyl, cycloalkyl, halo, alkoxyl, alkenyl, aralkyl, aryl, heterocyclyl, heteroaryl, and heterocyclylalkyl; W is an electron withdrawing group, and, for example, is selected from: --COR.sup.5, --CN, SO.sub.2 C.sub.6 H.sub.5 ; R.sup.5 is hydrogen; substituted and unsubstituted: alkyl, aryl, aralkyl, heteroaryl, heterocyclyl, or heterocyclylalkyl; or R.sup.5 may be --OR.sup.6, --NR.sup.7 R.sup.8, and --SR.sup.9 ; wherein R.sup.6 is H; substituted and unsubstituted: alkyl, alkenyl, or a group which defines --CO.sub.2 R.sup.6 as a pharmaceutically acceptable ester wherein R.sup.6 is, for example, phthalidyl, or 5-methyl-2-oxo-1,3-dioxolen-4-ylmethyl; R.sup.7 and R.sup.8 are independently selected from: hydrogen; substituted and unsubstituted: alkyl, aralkyl, aryl, heterocyclyl, and heterocyclylalkyl; R.sup.9 is substituted and unsubstituted: alkyl, aralkyl, aryl, heterocyclyl, and heterocyclyclalkyl; R.sup.3 may also be W; n is 0 or 1; when the unsaturated moiety attached to the exocyclic sulfur atom is acetylenic, then R.sup.3 and R.sup.4 are nonexistent and W is as previously defined. Such compounds I are new and they and their pharmaceutically acceptable salt and ester derivatives are useful as antibiotics.
摘要翻译：公开了具有以下结构的6-和6,6-二取代-2-取代的硫代 - 笔 - 2-em-3-羧酸：其中：R1，R2，R3和R4独立地选自：氢; 烷基，环烷基，卤素，烷氧基，烯基，芳烷基，芳基，杂环基，杂芳基和杂环基烷基; W是吸电子基团，例如，选自：-COR 5，-CN，SO 2 C 6 H 5; R5是氢; 取代和未取代的：烷基，芳基，芳烷基，杂芳基，杂环基或杂环基烷基; 或者R 5可以是-OR 6，-NR 7 R 8和-SR 9; 其中R6是H; 取代和未取代的：烷基，烯基或定义-CO 2 R 6作为药学上可接受的酯的基团，其中R 6是例如酞基或5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基甲基; R7和R8独立地选自：氢; 取代和未取代的：烷基，芳烷基，芳基，杂环基和杂环基烷基; R9是取代和未取代的：烷基，芳烷基，芳基，杂环基和杂环烷基; R3也可以是W; n为0或1; 当连接到环外硫原子上的不饱和部分是炔属时，则R3和R4不存在，W如前所定义。这些化合物I是新的，它们及其药学上可接受的盐和酯衍生物可用作抗生素。

7. 发明授权

US4311704A 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：US4311704A
公开(公告)日：1982-01-19
申请号：US159573
申请日：1980-06-16
申请人： Burton G. Christensen , William J. Leanza , David H. Shih , Kenneth J. Wildonger
发明人： Burton G. Christensen , William J. Leanza , David H. Shih , Kenneth J. Wildonger
IPC分类号： C07D477/20 , C07D487/04 , A61K31/40 , A61K31/425 , A61K31/44
CPC分类号： C07D477/20
摘要： Disclosed are substituted N-methylene derivatives of thienamycin having the formula: ##STR1## wherein: (1.) X.dbd.--NR.sup.1 R.sup.2, and Y.dbd.--R'--N.dbd.CRNR.sup.1 R.sup.2, and(2.) X.dbd.R, and Y.dbd.--NR.sup.1 R'N.dbd.CRNR.sup.1 R.sup.2 ; andwherein: R is, inter alia, hydrogen, NH.sub.2, --NHR.sup.1, --NR.sup.1 R.sup.2, R.sup.1 and R.sup.2 ; R.sup.1 and R.sup.2 are independently selected from: hydrogen, substituted, or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R' is --(CH.sub.2).sub.n.sup.-, n is 1-6, or --(CH.sub.2).sub.m --Q--(CH.sub.2).sub.p.sup.-, m, n.dbd.1-3 and Q is O, S or R' is a carbocyclic or heterocyclic ring. 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：公开了具有下式的噻吩霉素的取代的N-亚甲基衍生物：其中：（1）X = -NR 1 R 2，Y = -R'-N = CRNR 1 R 2，和（2）X = R，Y = -NR1R'N = CRNR1R2; 并且其中：R特别是氢，NH 2，-NHR 1，-NR 1 R 2，R 1和R 2; R 1和R 2独立地选自：氢，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; R'为 - （CH 2）n - ，n为1-6或 - （CH 2）m Q-（CH 2）p - ，m，n = 1-3，Q为O，S或R'为碳环或杂环环。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。

8. 发明授权

US4309438A N-Alkyl-N-iminomethyl derivatives of thienamycin 失效
标题翻译：噻吩霉素的N-烷基-N-亚氨基甲基衍生物
公开(公告)号：US4309438A
公开(公告)日：1982-01-05
申请号：US135574
申请日：1980-03-31
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 , C07D477/20 , C07D487/04 , A61K31/40 , A61K31/425 , A61K31/44
CPC分类号： C07D477/20 , C07C251/72
摘要： Disclosed are N-alkyl-N-iminomethyl derivatives of thienamycin which may be represented by the following structural formula: ##STR1## wherein R.sup.5 is, inter alia, alkyl, alkenyl, aryl, or aralkyl, R.sup.6 is selected from R, OR, SR and NR.sup.1 R.sup.2 wherein R is, inter alia, hydrogen and substituted or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; and R.sup.1 and R.sup.2 are hydrogen or R. Such compounds, including their O-- and carboxyl derivatives are useful as antibiotics. Also dislosed 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N-烷基-N-亚氨基甲基衍生物，其可以由以下结构式表示：其中R 5特别是烷基，烯基，芳基或芳烷基，R 6选自R，OR，SR 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;其中R是尤其是氢和取代或未取代的：并且R 1和R 2是氢或R.这些化合物，包括其O-和羧基衍生物可用作抗生素。还包括这样的化合物的制备方法：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。

9. 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）：

10. 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。

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