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31. 发明授权

US3962224A Cephalosporin compounds 失效
公开(公告)号：US3962224A
公开(公告)日：1976-06-08
申请号：US336561
申请日：1973-03-05
申请人： Burton G. Christensen , Ronald W. Ratcliffe
发明人： Burton G. Christensen , Ronald W. Ratcliffe
IPC分类号： C07D501/08 , C07D501/16 , C07F9/568 , C07D501/14
CPC分类号： C07F9/5683
摘要： Novel 7-azido-3-cephem compounds are prepared via .alpha.-amino-phosphonoacetate esters. The cephem compounds are intermediates for the preparation of novel and known useful antibiotic cephalosporins.

32. 发明授权

US07157604B2 Selective estrogen receptor modulators 失效
标题翻译：选择性雌激素受体调节剂
公开(公告)号：US07157604B2
公开(公告)日：2007-01-02
申请号：US10486005
申请日：2002-08-09
申请人： Dongfang Meng , Dann LeRoy Parker, Jr. , Robert R. Wilkening , Ronald W. Ratcliffe
发明人： Dongfang Meng , Dann LeRoy Parker, Jr. , Robert R. Wilkening , Ronald W. Ratcliffe
IPC分类号： C07C211/45 , C07C233/15 , C07C233/25 , C07C233/33 , C07D307/46
CPC分类号： C07D295/088 , A61K31/135 , C07B2200/07 , C07C225/22 , C07C255/47 , C07C255/58 , C07C2603/18 , C07C2603/86 , C07D307/46
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，软骨退化，子宫内膜异位症，子宫肌瘤病，热特别是乳腺，子宫和前列腺的LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育症，血管平滑肌细胞增殖，肥胖症，失禁和癌症。

33. 发明授权

US6140318A Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US6140318A
公开(公告)日：2000-10-31
申请号：US168622
申请日：1998-10-08
申请人： Lovji D. Cama , Robert R. Wilkening , Ronald W. Ratcliffe , Kenneth J. Wildonger , Wanying Sun
发明人： Lovji D. Cama , Robert R. Wilkening , Ronald W. Ratcliffe , Kenneth J. Wildonger , Wanying Sun
IPC分类号： A61P31/06 , C07D487/04 , A61K31/395 , A01N43/60 , C07D413/00 , C07D487/00
CPC分类号： C07D487/04
摘要： Compounds of formula I are disclosed. ##STR1## as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group -A-Q-L-B.The carbapenems of the invention are effective against susceptible bacterial organisms, including methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS).
摘要翻译：公开了式I化合物。以及其药学上可接受的盐。萘磺叠胺被包括至少一个阳离子基团-A-Q-L-B的各种取代基取代。本发明的碳青霉烯类药物对抗敏感细菌生物有效，包括耐甲氧西林金黄色葡萄球菌（MRSA），耐甲氧西林葡萄球菌（MRSE）和耐甲氧西林凝固酶阴性葡萄球菌（MRCNS）。

34. 发明授权

US4833167A 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids 失效
标题翻译： 2-氮杂取代的1-碳代萘二烯-2-烯-3-羧酸
公开(公告)号：US4833167A
公开(公告)日：1989-05-23
申请号：US743139
申请日：1985-06-10
申请人： Burton G. Christensen , John C. Chabala , Ronald W. Ratcliffe
发明人： Burton G. Christensen , John C. Chabala , Ronald W. Ratcliffe
IPC分类号： C07D477/22 , C07F9/6561
CPC分类号： C07F9/65611 , C07D477/22 , Y02P20/55
摘要： Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, diaklylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R.sup.a is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety.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2-氮杂取代的1-碳代萘二甲酸-2-烯-3-羧酸I，其中通用2-氮杂基团包括叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑基，氮丙啶基及其药学上可接受的盐，酯，酸酐和酰胺衍生物，其可用作抗生素。还公开了通过2-叠氮中心中间体III从已知的适当取代的双环酮酯II制备I的方法：其中R 16是H或CH 3，优选β-甲基 ; R6和R7独立地是氢，直链，支链或环状的C 1 -C 5烷基，其可以被氟，羟基，保护的羟基，亚磺氧基，氨基，被保护的氨基取代，其中R 6和R 7一起也可以是C 2 -C 4亚烷基取代条件是R6和R7都不是未取代的烷基，R1和R2特别是氢，烷基，酰基，并且可以连接形成包含3至7个原子的环; Ra是氢，盐阳离子，可除去的保护基或药学上可接受的酯部分。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。

35. 发明授权

US4725594A Carbapenems having an internally or externally alkylated mono- or bicyclic 2-quaternary heteroarylalxyl heteromethyl substituent 失效
标题翻译：具有内部或外部烷基化单环或双环2-季杂芳基甲基取代基的碳青霉烯
公开(公告)号：US4725594A
公开(公告)日：1988-02-16
申请号：US681344
申请日：1984-12-13
申请人： Burton G. Christensen , James V. Heck , Ronald W. Ratcliffe , Thomas N. Salzmann
发明人： Burton G. Christensen , James V. Heck , Ronald W. Ratcliffe , Thomas N. Salzmann
IPC分类号： C07D487/04 , A61K31/40 , A61P31/04 , C07D477/14
CPC分类号： C07D477/14
摘要： Carbapenems having the formula: ##STR1## wherein: R.sup.1 is H;R.sup.4 and R.sup.5 are independently H, CH.sub.3 --, CH.sub.3 CH.sub.2 --, (CH.sub.3).sub.2 CH--, HOCH.sub.2 --, CH.sub.3 CH(OH)--, (CH.sub.3).sub.2 C(OH)--, FCH.sub.2, F.sub.2 CH--, F.sub.3 C--, CH.sub.3 CH(F)--, CH.sub.3 CF.sub.2 --, (CH.sub.3).sub.2 C(F)--; X is --S--, --SO--, --SO.sub.2 --, --O-- or --NH; L is a bridging group comprising substituted or unsubstituted C.sub.1 --C.sub.4 straight, C.sub.2 -C.sub.6 branched or C.sub.3 -C.sub.7 cycloalkyl groups wherein the substituents are selected from C.sub.1 -C.sub.6 alkyl, O--C.sub.1 -C.sub.6 alkyl, S--C.sub.1 -C.sub.6 alkyl, CF.sub.3, N(C.sub.1 -C.sub.6 alkyl).sub.2 ; Y is a carboxy-containing substituent; Het is internally alkylated heteroarylium, ##STR2## or externally alkylated heteroarylium, ##STR3## their preparation and antibiotic use are disclosed.
摘要翻译：具有下式的碳青霉烯类：其中：R1是H; （CH 3）2 CH-，HOCH 2 - ，CH 3 CH（OH） - ，（CH 3）2 C（OH） - ，FCH 2，F 2 CH-，F 3 C - ，CH 3 CH（F） - ，CH 3 CF 2 - ，（CH 3）2 C（F） - ; X是-S - ， - SO - ， - SO 2 - ， - O-或-NH; L是包含取代或未取代的C 1 -C 4直链，C 2 -C 6支链或C 3 -C 7环烷基的桥连基团，其中取代基选自C 1 -C 6烷基，O-C 1 -C 6烷基，S-C 1 -C 6烷基，CF 3 ，N（C 1 -C 6烷基）2; Y是含羧基的取代基; Het是内部烷基化杂芳族化合物，图像或外部烷基化杂芳基，其公开了它们的制备和抗生素用途。

36. 发明授权

US4707547A Process for preparing carbapenem compounds 失效
标题翻译：碳青霉烯化合物的制备方法
公开(公告)号：US4707547A
公开(公告)日：1987-11-17
申请号：US859281
申请日：1986-05-02
申请人： Burton G. Christensen , Ronald W. Ratcliffe
发明人： Burton G. Christensen , Ronald W. Ratcliffe
IPC分类号： C07D205/08 , C07D477/22 , C07F7/10 , C07F9/6561 , C07D487/04 , A61K31/40
CPC分类号： C07D205/08 , C07D477/22 , C07F7/10 , C07F9/65611
摘要： Disclosed are 6- and 6,6-disubstituted-3-substituted amino-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I): ##STR1## wherein R.sup.1 and R.sup.2 are, inter alia, independently selected from the group consisting of hydrogen, substituted and unsubstituted: alkyl, aryl, and aralkyl; and R' and R" are independently selected from the group consisting of: H, substituted and unsubstituted alkyl and aralkyl, or together form a substituted or unsubstituted cyclic group.Such compounds and 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 compounds and compositions when an antibiotic effect is indicated.
摘要翻译：公开了6-和6,6-二取代-3-取代的氨基-1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸（I）：其中R1和R2是尤其是独立地选自氢，取代和未取代的：烷基，芳基和芳烷基; 并且R'和R“独立地选自：H，取代和未取代的烷基和芳烷基，或一起形成取代或未取代的环状基团。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，其中包括当指出抗生素效应时施用化合物和组合物。

37. 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。

38. 发明授权

US4610820A Process for the preparation of thienamycin and intermediates 失效
标题翻译：噻吩霉素和中间体的制备方法
公开(公告)号：US4610820A
公开(公告)日：1986-09-09
申请号：US786366
申请日：1985-10-11
申请人： Burton G. Christensen , Ronald W. Ratcliffe , Thomas N. Salzmann
发明人： Burton G. Christensen , Ronald W. Ratcliffe , Thomas N. Salzmann
IPC分类号： C07D205/08 , C07D477/04 , C07D477/10 , C07F7/10
CPC分类号： C07D477/04 , C07D205/08 , C07D477/10 , C07F7/10 , Y02P20/55
摘要： In a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: ##STR1## R=H, blocking group or salt cation there is disclosed a process for preparing III via ##STR2## wherein R is a protecting group.
摘要翻译：在通过中间体III从L-天冬氨酸全合成噻吩那霉素的方法中，公开了通过其中R是保护基的式III化合物的制备方法。

39. 发明授权

US4388310A 6-Amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids 失效
标题翻译：取代的2-有机硫代-2-烯-3-羧酸的6-酰氨基-2-氧化物
公开(公告)号：US4388310A
公开(公告)日：1983-06-14
申请号：US353450
申请日：1982-03-01
申请人： Burton G. Christensen , Frank P. DiNinno , David A. Muthard , Ronald W. Ratcliffe
发明人： Burton G. Christensen , Frank P. DiNinno , David A. Muthard , Ronald W. Ratcliffe
IPC分类号： C07D499/21 , C07D499/88 , A61K31/67 , A61K31/43 , C07D277/02 , C07D499/44
CPC分类号： C07D499/88 , Y02P20/55
摘要： Disclosed are 6-amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids (I) which are useful as antibiotics and as intermediates in the synthesis of substituted pen-2-em-3-carboxylic acids: ##STR1## wherein: R.sup.1 is H or acyl; R.sup.2 is hydrogen or methoxyl; R.sup.3 is alkyl having from 1-6 carbon atoms; phenylalkyl having 7-12 carbon atoms; and cycloalkyl having 3-6 carbon atoms; and R.sup.4 is hydrogen, a removable protecting group or a pharmaceutically acceptable salt or ester moiety.
摘要翻译：公开了用作抗生素和作为取代的笔式2-em-3合成中的中间体的取代的2-有机硫代 - 二-2-甲-3-羧酸（I）的6-酰胺基-2-氧化物 - 羧酸：其中：R1是H或酰基; R2是氢或甲氧基; R3是具有1-6个碳原子的烷基; 具有7-12个碳原子的苯基烷基; 和具有3-6个碳原子的环烷基; 和R4是氢，可除去的保护基或药学上可接受的盐或酯部分。

40. 发明授权

US4383946A Process for the preparation of 1-carbapenems and intermediates via silyl-substituted dithioacetals 失效
标题翻译：通过甲硅烷基取代的二硫缩醛制备1-碳青霉烯和中间体的方法
公开(公告)号：US4383946A
公开(公告)日：1983-05-17
申请号：US303459
申请日：1981-09-18
申请人： Burton G. Christensen , Ronald W. Ratcliffe , Thomas N. Salzmann
发明人： Burton G. Christensen , Ronald W. Ratcliffe , Thomas N. Salzmann
IPC分类号： C07D205/08 , C07D477/04 , C07D477/10 , C07F7/08 , C07F7/10 , C07D487/04
CPC分类号： C07D477/04 , C07D205/08 , C07D477/10 , C07F7/0812 , C07F7/10 , Y02P20/55
摘要： Disclosed is a process for the total synthesis of 1-carbapenem antibiotics (I) from L-aspartic acid via central intermediates II and III: ##STR1## wherein R is hydrogen, a pharmaceutically acceptable ester moiety or salt cation, or a readily removable blocking group; R.sup.6, R.sup.7 and R.sup.8 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl; R.sup.1' and R.sup.e are hydrogen, or a readily removable protecting group; R.sup.a, R.sup.b and R.sup.c are selected from alkyl, aryl or aralkyl.
摘要翻译：公开了通过中心中间体II和III从L-天冬氨酸全合成1-碳青霉烯类抗生素（I）的方法：其中R是氢，药学上可接受的酯部分或盐阳离子，或易于除去的封闭基团; R6，R7和R8特别是独立地选自氢，烷基，烯基，芳基和芳烷基; R 1和Re为氢或易脱除的保护基; R a，R b和R c选自烷基，芳基或芳烷基。

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