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公开(公告)号：US20130072711A1
公开(公告)日：2013-03-21
申请号：US13699585
申请日：2010-05-26
IPC分类号： C07C271/24 , C07C329/08 , C07C231/12 , C07C269/04 , C07C231/14 , C07C233/63 , C07C269/06
CPC分类号： C07C271/24 , C07C61/22 , C07C211/40 , C07C231/12 , C07C231/14 , C07C233/63 , C07C247/22 , C07C265/10 , C07C269/04 , C07C269/06 , C07C323/41 , C07C323/43 , C07C327/30 , C07C2601/14 , C07C2601/16 , C07D303/36 , Y02P20/55
摘要： A compound of formula wherein PROT is an amine protecting group and PROT′ is hydrogen; or PROT and PROT′ together with the nitrogen atom to which they are attached form a heterocyclic ring as an amine protecting group, and PROT″ is a thiol protecting group, processes for its production, intermediates in their production and production of intermediates in stereoisomerically pure form, and their use for the production of pharmaceutically active compounds.
摘要翻译： 下式化合物其中PROT是胺保护基团，PROT'是氢; 或PROT和PROT'与它们所连接的氮原子一起形成作为胺保护基团的杂环，并且PROT“是硫醇保护基，其生产方法，其制备中的中间体和立体异构纯的中间体的制备 形式及其用于制备药物活性化合物的用途。
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公开(公告)号：US08987498B2
公开(公告)日：2015-03-24
申请号：US13699585
申请日：2011-05-23
IPC分类号： C07C321/00 , C07C271/24 , C07C61/22 , C07C211/40 , C07C247/22 , C07C265/10 , C07C323/41 , C07C323/43 , C07C327/30 , C07D303/36 , C07C231/12 , C07C231/14 , C07C233/63 , C07C269/04 , C07C269/06
CPC分类号： C07C271/24 , C07C61/22 , C07C211/40 , C07C231/12 , C07C231/14 , C07C233/63 , C07C247/22 , C07C265/10 , C07C269/04 , C07C269/06 , C07C323/41 , C07C323/43 , C07C327/30 , C07C2601/14 , C07C2601/16 , C07D303/36 , Y02P20/55
摘要： A compound of formula wherein PROT is an amine protecting group and PROT′ is hydrogen; or PROT and PROT′ together with the nitrogen atom to which they are attached form a heterocyclic ring as an amine protecting group, and PROT″ is a thiol protecting group, processes for its production, intermediates in their production and production of intermediates in stereoisomerically pure form, and their use for the production of pharmaceutically active compounds.
摘要翻译： 下式化合物其中PROT是胺保护基团，PROT'是氢; 或PROT和PROT'与它们所连接的氮原子一起形成作为胺保护基团的杂环，并且PROT“是硫醇保护基，其生产方法，其制备中的中间体和立体异构纯的中间体的制备 形式及其用于制备药物活性化合物的用途。
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公开(公告)号：US20130079400A1
公开(公告)日：2013-03-28
申请号：US13699589
申请日：2011-05-23
申请人： Rosemarie Riedl , Werner Heilmayer , Lee Spence
发明人： Rosemarie Riedl , Werner Heilmayer , Lee Spence
IPC分类号： C07C319/20 , C07C57/145 , C07C59/08 , C07C323/52 , C07C53/10
CPC分类号： C07C319/20 , A61K31/215 , A61P17/00 , A61P31/00 , C07B2200/07 , C07B2200/13 , C07C53/10 , C07C57/145 , C07C59/08 , C07C319/14 , C07C323/41 , C07C323/43 , C07C323/52 , C07C2601/14 , C07C2603/82 , Y02P20/55
摘要： Process for the preparation of a compound of formula I in the form of a single stereoisomer in crystalline form, comprising deprotecting the amine group in a compound of formula IIa or in a mixture of a compound of formula IIa with a compound of formula IIb and isolating a compound of formula I from the reaction mixture; compounds and salts of compounds of formula I in crystalline form; pharmaceutical compositions comprising such salts; processes for the preparation of intermediates and intermediates in a process for the preparation of a compound of formula I.
摘要翻译： 用于制备结晶形式的单一立体异构体形式的式I化合物的方法，包括使式IIa化合物中的胺基或式IIa化合物与式IIb化合物的混合物脱保护并分离 来自反应混合物的式I化合物; 结晶形式的式I化合物的化合物和盐; 包含这些盐的药物组合物; 在制备式I化合物的方法中制备中间体和中间体的方法。
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公开(公告)号：US09120727B2
公开(公告)日：2015-09-01
申请号：US13699589
申请日：2011-05-23
申请人： Rosemarie Riedl , Werner Heilmayer , Lee Spence
发明人： Rosemarie Riedl , Werner Heilmayer , Lee Spence
IPC分类号： C07C205/00 , C07C229/00 , C07C319/20 , A61K31/215 , C07C53/10 , C07C57/145 , C07C59/08 , C07C319/14 , C07C323/41 , C07C323/43 , C07C323/52 , A01N37/00 , A61K31/21
CPC分类号： C07C319/20 , A61K31/215 , A61P17/00 , A61P31/00 , C07B2200/07 , C07B2200/13 , C07C53/10 , C07C57/145 , C07C59/08 , C07C319/14 , C07C323/41 , C07C323/43 , C07C323/52 , C07C2601/14 , C07C2603/82 , Y02P20/55
摘要： Process for the preparation of a compound of formula I in the form of a single stereoisomer in crystalline form, comprising deprotecting the amine group in a compound of formula IIa or in a mixture of a compound of formula IIa with a compound of formula IIb and isolating a compound of formula I from the reaction mixture; compounds and salts of compounds of formula I in crystalline form; pharmaceutical compositions comprising such salts; processes for the preparation of intermediates and intermediates in a process for the preparation of a compound of formula I.
摘要翻译： 用于制备结晶形式的单一立体异构体形式的式I化合物的方法，包括使式IIa化合物中的胺基或式IIa化合物与式IIb化合物的混合物脱保护并分离 来自反应混合物的式I化合物; 结晶形式的式I化合物的化合物和盐; 包含这些盐的药物组合物; 在制备式I化合物的方法中制备中间体和中间体的方法。
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5.发明授权Pleuromutilin derivatives for use in the treatment of diseases mediated by microbes 有权Pleuromutilin衍生物用于治疗由微生物介导的疾病公开(公告)号：US09278920B2
公开(公告)日：2016-03-08
申请号：US13821446
申请日：2011-08-11
IPC分类号： C07C323/52 , A61K31/215 , A61P31/00 , A61K31/235 , A61K45/06
CPC分类号： C07C323/52 , A61K31/235 , A61K45/06 , C07C2601/04 , C07C2601/08 , C07C2601/18 , C07C2602/42 , C07C2602/44 , C07C2603/99
摘要： Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.
摘要翻译： 选自N-取代或N-烷基化或N-酰化的14-O- [（氨基（C 0-4）烷基 - 羟基 - 环烷基 - 或双环烷基硫烷基） - 乙酰基] - 木霉素的化合物是14-O- [ （氨基（C0-4）烷基 - 羟基 - 环丁基硫烷基） - 乙酰基] - 木兰林，14-O - [（氨基（C0-4）烷基 - 羟基 - 环戊基硫烷基） - 乙酰基] - 木霉素，14-O - [ （C0-4）烷基 - 羟基 - 环庚基硫烷基） - 乙酰基] - 木兰林，14-O - [（氨基（C0-4）烷基 - 羟基 - 环辛基硫烷基） - 乙酰基] - 木兰林，或14-O - [（氨基 C0-4）烷基 - 羟基 - 双环烷基硫烷基） - 乙酰基] - 木素，任选呈盐和/或溶剂化物形式，包含这些化合物的药物组合物及其作为药物的用途，例如 用于治疗微生物感染和治疗痤疮，任选地与其它药物活性剂组合。
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6.发明申请PLEUROMUTILIN DERIVATIVES FOR USE IN THE TREATMENT OF DISEASES MEDIATED BY MICROBES 有权用于治疗由MICROBES介导的疾病的胰岛素衍生物公开(公告)号：US20130274329A1
公开(公告)日：2013-10-17
申请号：US13821446
申请日：2011-08-11
IPC分类号： C07C323/52
CPC分类号： C07C323/52 , A61K31/235 , A61K45/06 , C07C2601/04 , C07C2601/08 , C07C2601/18 , C07C2602/42 , C07C2602/44 , C07C2603/99
摘要： Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.
摘要翻译： 选自N-取代或N-烷基化或N-酰化的14-O- [（氨基（C 0-4）烷基 - 羟基 - 环烷基 - 或双环烷基硫烷基） - 乙酰基] - 木霉素的化合物是14-O- [ （氨基（C0-4）烷基 - 羟基 - 环丁基硫烷基） - 乙酰基] - 木兰林，14-O - [（氨基（C0-4）烷基 - 羟基 - 环戊基硫烷基） - 乙酰基] - 木霉素，14-O - [ （C0-4）烷基 - 羟基 - 环庚基硫烷基） - 乙酰基] - 木兰林，14-O - [（氨基（C0-4）烷基 - 羟基 - 环辛基硫烷基） - 乙酰基] - 木兰林，或14-O - [（氨基 C0-4）烷基 - 羟基 - 双环烷基硫烷基） - 乙酰基] - 木素，任选呈盐和/或溶剂化物形式，包含这些化合物的药物组合物及其作为药物的用途，例如 用于治疗微生物感染和治疗痤疮，任选地与其它药物活性剂组合。
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