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1. 发明授权

US08729260B2 Process for the preparation of carbapenem using cabapenem intermediates and recovery of cabapenem 有权
标题翻译：使用卡巴培南中间体制备碳青霉烯类化合物和卡巴培南回收的方法
公开(公告)号：US08729260B2
公开(公告)日：2014-05-20
申请号：US13100635
申请日：2011-05-04
申请人： Wei-Hong Tseng , Wen-Hsin Chang , Chia-Mao Chang , Chia-Wei Yeh , Yuan-Liang Kuo
发明人： Wei-Hong Tseng , Wen-Hsin Chang , Chia-Mao Chang , Chia-Wei Yeh , Yuan-Liang Kuo
IPC分类号： C07D487/04 , C07D477/20
CPC分类号： C07D477/20 , C07D477/06 , C07F9/65611
摘要： The present invention relates to an efficient process of synthesizing some known Ertapenem compounds and to provide new intermediate compounds of Meropenem and Doripenem. The process and the intermediate can substantially increase the effective yield and reduce the impurity generation. The present invention further provides a novel and effective process for recovering and purifying ertapenem compounds by utilizing a low cost, materials with chemical stability as a carrier for isolating ertapenem compounds from extracts.
摘要翻译：本发明涉及合成一些已知的二硫青霉烯化合物的有效方法，并提供新的中间体化合物美罗培南和多西平。该方法和中间体可显着提高有效产率并减少杂质产生。本发明还提供了一种利用低成本的具有化学稳定性的材料作为从提取物中分离厄来替奈姆化合物的载体来回收和纯化ertapenem化合物的新颖而有效的方法。

2. 发明授权

US07538212B2 Intermediate for carbapenem compound for oral administration and process for producing the same 失效
标题翻译：用于口服给药的碳青霉烯类化合物的中间体及其制备方法
公开(公告)号：US07538212B2
公开(公告)日：2009-05-26
申请号：US10533868
申请日：2003-11-13
申请人： Keita Nishino , Teruyoshi Koga
发明人： Keita Nishino , Teruyoshi Koga
IPC分类号： C07F9/572 , C07D205/08
CPC分类号： C07F9/65611 , C07D205/08 , C07D477/18 , Y02P20/55
摘要： The present invention provides a novel intermediate represented by formula (1), (3), or (4) for efficiently producing a 1β-methylcarbapenem compound for oral administration, and a process for producing the intermediate. That is, the present invention provides a process for producing a novel β-lactam compound represented by formula (4), the process including allowing a β-lactam compound represented by formula (5) as a starting material to react with a compound represented by formula (6) in the presence of a base to obtain a novel β-lactam compound represented by formula (1), protecting the hydroxyl group, subsequently performing cyclization in the presence of a strong base, allowing the cyclized compound to react with diphenylphosphoryl chloride to obtain a novel β-lactam compound represented by formula (3), and eliminating the protecting group therefrom. The formulae referred to are diagrammed as follows: (In the formulae, R1 represents a trimethylsilyl group or a triethylsilyl group; R2 represents an aryl group or a heteroaryl group; R2 represents an aryl group or a heteroaryl group; R3 represents an alkyl group having 1 to 10 carbon atoms or a cycloalkyl group having 3 to 10 carbon atoms; and X represents a halogen atom.)
摘要翻译：本发明提供了一种用于高效制备口服给药的1β-甲基碳青霉烯化合物的式（1），（3）或（4）所示的新型中间体及其制备方法。也就是说，本发明提供一种制备由式（4）表示的新型β-内酰胺化合物的方法，该方法包括使由式（5）表示的β-内酰胺化合物作为起始原料与由式（6）的化合物，得到由式（1）表示的新型β-内酰胺化合物，保护羟基，随后在强碱存在下进行环化，使环化的化合物与二苯基磷酰氯得到式（3）所示的新型β-内酰胺化合物，除去保护基。所用的化合物如下：（式中，R1表示三甲基甲硅烷基或三乙基甲硅烷基; R2表示芳基或杂芳基; R2表示芳基或杂芳基; R3表示具有 1至10个碳原子或具有3至10个碳原子的环烷基; X表示卤素原子。

3. 发明授权

US5623081A Method for producing tetrahydrofuranyl compounds 失效
标题翻译：四氢呋喃基化合物的制备方法
公开(公告)号：US5623081A
公开(公告)日：1997-04-22
申请号：US448052
申请日：1995-05-23
申请人： Yang-I Lin , Panayota Bitha , Subas Sakya , Timothy W. Strohmeyer , Karen Bush , Carl B. Ziegler , Gregg B. Feigelson
发明人： Yang-I Lin , Panayota Bitha , Subas Sakya , Timothy W. Strohmeyer , Karen Bush , Carl B. Ziegler , Gregg B. Feigelson
IPC分类号： A61K31/40 , A61K31/397 , A61K31/4015 , A61K31/403 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/495 , A61K31/535 , A61P31/00 , A61P31/04 , C07D307/18 , C07D333/34 , C07D333/48 , C07D477/00 , C07D477/04 , C07D477/06 , C07D477/12 , C07D477/14 , C07D477/20 , C07F9/6561 , C07H11/00 , C07H19/01 , C07D307/02
CPC分类号： C07D307/18 , C07D333/34 , C07D477/14 , C07F9/65611 , C07H11/00 , C07H19/01 , Y02P20/582
摘要： Tetrahydrofuanyl compounds of the following formulae: ##STR1## are disclosed.
摘要翻译：公开了下式的四氢芳烃基化合物：。

4. 发明授权

US5580976A Preparation of .beta.-lactam compounds, and intermediates therefor 失效
标题翻译： β-内酰胺化合物及其中间体的制备
公开(公告)号：US5580976A
公开(公告)日：1996-12-03
申请号：US425225
申请日：1995-04-18
申请人： Masaharu Kume , Tadatoshi Kubota
发明人： Masaharu Kume , Tadatoshi Kubota
IPC分类号： C07D205/08 , C07D477/04 , C07D501/04 , C07F9/6561 , C07D205/09 , C07D205/085 , C07D205/095
CPC分类号： C07F9/65611 , C07D205/08 , C07D477/04 , Y02P20/55
摘要： A process for preparing a .beta.-lactam compound of the formula (I): ##STR1## which comprises cyclization of an azetidinone derivative of the formula: ##STR2## is provided in which R.sup.1 is hydrogen, alkyl which is optionally substituted, or amino which is optionally substituted; R.sup.2 is a carboxy-protecting group; and X is alkylene which is optionally intervened by --O-- or --S--, and/or which is optionally substituted; and R.sup.3 is aryl which is optionally substituted.
摘要翻译：提供了式（I）的β-内酰胺化合物的制备方法：其中包括下式所示的氮杂环丁酮衍生物（II）的环化：其中R 1是氢，烷基是任选取代的，或任选取代的氨基; R2是羧基保护基; 并且X是任选被-O-或-S-所介导的亚烷基，和/或任选被取代的; 并且R 3是任选被取代的芳基。

5. 发明授权

US5177064A Targeted drug delivery via phosphonate derivatives 失效
标题翻译：目标药物通过磷酸盐衍生物递送
公开(公告)号：US5177064A
公开(公告)日：1993-01-05
申请号：US553548
申请日：1990-07-13
申请人： Nicholas S. Bodor
发明人： Nicholas S. Bodor
IPC分类号： A61K31/56 , A61K31/66 , A61K31/675 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K45/00 , A61K47/48 , A61P29/00 , A61P31/12 , A61P43/00 , C07F9/40 , C07F9/553 , C07F9/572 , C07F9/576 , C07F9/58 , C07F9/59 , C07F9/645 , C07F9/6506 , C07F9/6509 , C07F9/6512 , C07F9/6547 , C07F9/6558 , C07F9/6561 , C07H15/252 , C07H19/04 , C07H19/048 , C07H19/052 , C07H19/056 , C07H19/10 , C07H19/12 , C07H19/20 , C07H19/207 , C07H19/23 , C07H19/24 , C07J51/00
CPC分类号： C07H15/252 , A61K47/48023 , C07F9/4075 , C07F9/4087 , C07F9/5532 , C07F9/5535 , C07F9/5722 , C07F9/5728 , C07F9/5765 , C07F9/582 , C07F9/591 , C07F9/645 , C07F9/65061 , C07F9/650958 , C07F9/65121 , C07F9/65125 , C07F9/6547 , C07F9/65583 , C07F9/65586 , C07F9/6561 , C07F9/65611 , C07F9/65613 , C07F9/65616 , C07H19/04 , C07H19/048 , C07H19/052 , C07H19/056 , C07H19/10 , C07H19/12 , C07H19/20 , C07H19/207 , C07H19/23 , C07H19/24 , C07J51/00 , Y10S514/885
摘要： The invention provides compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein [D] is the residue of a drug having a reactive functional group, said functional group being attached, directly or through a bridging group, via an oxygen-phosphorus bond to the phosphorus atom of the ##STR2## moiety; R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.12 aralkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.4 -C.sub.9 heteroaryl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloheteroalkyl or C.sub.7 -C.sub.12 aralkyl; and R.sub.3 is selected from the group consisting of C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl having one or two double bonds; (C.sub.3 -C.sub.7 cycloalkyl)--C.sub.r H.sub.2r --wherein r is zero, one, two or three, the cycloalkyl portion being unsubstituted or bearing 1 or 2 C.sub.1 -C.sub.4 alkyl substituents on the ring portion; (C.sub.6 -C.sub.10 aryloxy)C.sub.1 -C.sub.8 alkyl; 2--, 3-- or 4-- pyridyl; and phenyl-C.sub.r H.sub.2r -- wherein r is zero, one, two or three and phenyl is unsubstituted, or is substituted by 1 to 3 alkyl each having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halo, trifluoromethyl, dialkylamino having 2 to 8 carbon atoms or alkanoylamino having 2 to 6 carbon atoms. The compounds are adapted for targeted drug delivery, especially to the brain.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中[D]是具有反应性官能团的药物的残基，所述官能团直接或通过桥连基团连接，通过与部分的磷原子的氧 - 磷键; R1是C1-C8烷基，C6-C10芳基或C7-C12芳烷基; R2是氢，C1-C8烷基，C6-C10芳基，C4-C9杂芳基，C3-C7环烷基，C3-C7环杂烷基或C7-C12芳烷基; 并且R 3选自C 1 -C 8烷基; 具有一个或两个双键的C 2 -C 8烯基; （C 3 -C 7环烷基）-Cr H 2r - 其中r为0,1,2或3，所述环烷基部分为未取代的或在环部分上带有1或2个C 1 -C 4烷基取代基; （C 6 -C 10芳氧基）C 1 -C 8烷基; 2-，3-或4-吡啶基; 和苯基-CrH 2r-，其中r为0,1,2或3，苯基未取代，或被1至3个具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基，卤素，三氟甲基， 2至8个碳原子或具有2至6个碳原子的烷酰基氨基。这些化合物适用于靶向药物递送，特别适用于大脑。

6. 发明授权

US4746736A Carbapenem antibiotics 失效
标题翻译：卡巴布本抗生素
公开(公告)号：US4746736A
公开(公告)日：1988-05-24
申请号：US923065
申请日：1986-10-24
申请人： Choung U. Kim
发明人： Choung U. Kim
IPC分类号： C07D213/32 , C07D233/54 , C07D249/04 , C07D249/08 , C07D257/04 , C07D277/26 , C07D285/06 , C07D477/20 , C07F7/18 , C07F9/6561 , C07D487/04 , A61K31/40
CPC分类号： C07D233/64 , C07D213/32 , C07D249/04 , C07D249/08 , C07D257/04 , C07D277/26 , C07D285/06 , C07D477/20 , C07F7/1856 , C07F9/65611
摘要： Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents a C.sub.1 -C.sub.6 straight or branched chain alkylene group; R.sup.5 represents an optionally substituted aliphatic cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical and ##STR2## represents a nitrogen-containing aromatic heterocycle attached to the alkylene group A at a ring carbon atom and quaternized by substituent R.sup.5. Such derivatives are useful as potent antibacterial agents.
摘要翻译：公开了新的碳青霉烯衍生物，其特征在于其中A表示C1-C6直链或支链亚烷基的式“IMAGE”的2-取代基; R5表示任选取代的脂族环脂族，脂环族 - 脂族 - 脂族，芳基，芳脂族，杂芳基，杂脂肪族，杂环基或杂环基 - 脂族基团，并且“IMAGE”表示在环碳原子上连接到亚烷基A上的含氮芳族杂环，通过取代基R5。这些衍生物可用作有效的抗菌剂。

7. 发明授权

US4308259A Penicillin derivatives 失效
标题翻译：青霉素衍生物
公开(公告)号：US4308259A
公开(公告)日：1981-12-29
申请号：US121175
申请日：1980-02-13
申请人： Peter H. Bentley
发明人： Peter H. Bentley
IPC分类号： C07D499/00 , C07D499/21 , C07D499/46 , C07D499/56 , C07F9/6524 , C07F9/6541 , C07F9/6561 , A61K31/67 , A61K31/43 , C07F9/65
CPC分类号： C07F9/65611 , C07C309/00 , C07D499/00
摘要： A penicillin of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R is C.sub.1-6 alkyl; an optionally substituted 5-membered heterocyclic ring containing one or two heteroatoms selected from oxygen, sulphur and nitrogen; phenyl; mono-substituted phenyl where the substituent is halogen, hydroxy, C.sub.1-6 alkoxy, nitro, amino, C.sub.1-6 alkyl, or C.sub.1-6 haloalkyl, C.sub.1-6 alkylcarbonyloxy, or C.sub.1-6 alkyl sulphonylamino; or di-substituted phenyl where the substituents are selected from hydroxy, halogen, methoxy, acetoxy and amino; and X represents a group of formula: ##STR2## wherein R.sup.1 represents C.sub.1 to C.sub.6 alkyl, or C.sub.1 to C.sub.6 alkoxy.Their preparation and use is described.
摘要翻译：式（I）的青霉素或其药学上可接受的盐或体内可水解的酯：其中R是C 1-6烷基; 含有一个或两个选自氧，硫和氮的杂原子的任选取代的5元杂环; 苯基; 硝基，氨基，C 1-6烷基或C 1-6卤代烷基，C 1-6烷基羰基氧基或C 1-6烷基磺酰基氨基;单取代的苯基，其中取代基是卤素，羟基，C 1-6烷氧基，硝基，氨基，或二取代的苯基，其中取代基选自羟基，卤素，甲氧基，乙酰氧基和氨基; 并且X表示下式的基团：其中R 1表示C 1至C 6烷基或C 1至C 6烷氧基。描述了它们的制备和使用。

8. 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。

9. 发明授权

US4061628A Intermediates for producing semi-synthetic penicillins and cephalosporins and methods of production 失效
标题翻译：用于生产半合成青霉素和头孢菌素的中间体和生产方法
公开(公告)号：US4061628A
公开(公告)日：1977-12-06
申请号：US378727
申请日：1973-07-12
申请人： John H. Sellstedt
发明人： John H. Sellstedt
IPC分类号： C07D499/04 , C07D499/08 , C07D499/10 , C07D499/12 , C07D499/21 , C07D501/06 , C07F9/6561 , C07D501/04
CPC分类号： C07F9/65613 , C07F9/65611 , Y02P20/55
摘要： Novel 6-APA, 7-ACA, and 7-ADCA derivatives are described which comprise phosphorylated derivatives of 6-APA, 7-ACA, or 7-ADCA and the corresponding acylated derivatives thereof. The novel compounds are prepared by the reaction of 6-APA, 7-ACA, 7-ADCA or a salt thereof with a phosphorus halide in the presence of an acid acceptor and subsequently acylating the thus formed phosphorylated compound, to form a phosphorylated acylated derivative which upon hydrolysis with water splits off the protective group(s) to provide the corresponding semi-synthetic penicillin or cephalosporin having useful antibacterial activity.

10. 发明授权

US3997532A Intermediates for producing semi-synthetic cephalosporins 失效
标题翻译：用于生产半合成头孢菌素的中间体
公开(公告)号：US3997532A
公开(公告)日：1976-12-14
申请号：US538497
申请日：1975-01-03
申请人： John H. Sellstedt
发明人： John H. Sellstedt
IPC分类号： C07D501/20 , C07F9/6561
CPC分类号： C07F9/65611 , Y02P20/55
摘要： Novel 6-APA, 7-ACA, and 7-ADCA derivatives are described which comprise phosphorylated derivatives of 6-APA, 7-ACA, or 7-ADCA and the corresponding acylated derivatives thereof. The novel compounds are prepared by the reaction of 6-APA, 7-ACA, 7-ADCA or a salt thereof with a phosphorus halide in the presence of an acid acceptor and subsequently acylating the thus formed phosphorylated compound, to form a phosphorylated acylated derivative which upon hydrolysis with water splits off the protective group(s) to provide the corresponding semi-synthetic penicillin or cephalosporin having useful antibacterial activity.
摘要翻译：描述了新的6-APA，7-ACA和7-ADCA衍生物，其包含6-APA，7-ACA或7-ADCA的磷酸化衍生物及其相应的酰化衍生物。该新化合物通过在酸受体存在下通过6-APA，7-ACA，7-ADCA或其盐与卤化磷的反应制备，随后酰化由此形成的磷酸化化合物，形成磷酸化酰化衍生物其在用水分解保护基团时提供相应的具有有效抗菌活性的半合成青霉素或头孢菌素。

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