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公开(公告)号:US07812032B2
公开(公告)日:2010-10-12
申请号:US11781804
申请日:2007-07-23
申请人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
发明人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
IPC分类号: C07D498/18 , A61K31/395
CPC分类号: A61K31/33
摘要: A rapamycin analog composition includes a crystalline form of a rapamycin analog. The crystal can be a hydrate, dehydrate, solvate, or desolvate. The rapamycin analog can have a structure of Formula 1, which is optionally a prodrug, salt, derivative, or combination thereof:
摘要翻译: 雷帕霉素类似物组合物包括雷帕霉素类似物的结晶形式。 该晶体可以是水合物,脱水剂,溶剂化物或去溶剂化物。 雷帕霉素类似物可以具有式1的结构,其可任选地是前药,盐,衍生物或其组合:
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公开(公告)号:US08034926B2
公开(公告)日:2011-10-11
申请号:US12886398
申请日:2010-09-20
申请人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
发明人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
IPC分类号: C07D498/18
CPC分类号: C07D498/18
摘要: A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic medium can be a solvent, and the process can include causing the rapamycin analog to dissolve into the solvent, and incubating the solvent until the rapamycin analog crystallizes. The following can also be performed: forming a slurry of crystalline rapamycin analog; stirring the rapamycin analog mixture until the rapamycin analog crystallizes; saturating the rapamycin analog solution; forming a supersaturated rapamycin analog solution; combining an antisolvent with the rapamycin analog and the solvent to form a biphasic mixture, and incubating the biphasic mixture to cause a liquid-liquid phase split.
摘要翻译: 制备结晶雷帕霉素类似物的方法包括:将雷帕霉素类似物与有机介质结合以形成混合物; 孵育混合物直到雷帕霉素类似物结晶; 并回收结晶雷帕霉素类似物。 有机介质可以是溶剂,并且该方法可以包括使雷帕霉素类似物溶解到溶剂中,并将溶剂温育直到雷帕霉素类似物结晶。 还可以进行以下操作:形成结晶雷帕霉素类似物的浆液; 搅拌雷帕霉素类似物混合物直到雷帕霉素类似物结晶; 饱和雷帕霉素类似物溶液; 形成过饱和雷帕霉素类似物溶液; 将抗溶剂与雷帕霉素类似物和溶剂组合以形成双相混合物,并将两相混合物温育以引起液 - 液相分裂。
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公开(公告)号:US07820812B2
公开(公告)日:2010-10-26
申请号:US11781807
申请日:2007-07-23
申请人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
发明人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
IPC分类号: C07D498/18
CPC分类号: C07D498/18
摘要: A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic medium can be a solvent, and the process can include causing the rapamycin analog to dissolve into the solvent, and incubating the solvent until the rapamycin analog crystallizes. The following can also be performed: forming a slurry of crystalline rapamycin analog; stirring the rapamycin analog mixture until the rapamycin analog crystallizes; saturating the rapamycin analog solution; forming a supersaturated rapamycin analog solution; combining an antisolvent with the rapamycin analog and the solvent to form a biphasic mixture, and incubating the biphasic mixture to cause a liquid-liquid phase split.
摘要翻译: 制备结晶雷帕霉素类似物的方法包括:将雷帕霉素类似物与有机介质结合以形成混合物; 孵育混合物直到雷帕霉素类似物结晶; 并回收结晶雷帕霉素类似物。 有机介质可以是溶剂,并且该方法可以包括使雷帕霉素类似物溶解到溶剂中,并将溶剂温育直到雷帕霉素类似物结晶。 还可以进行以下操作:形成结晶雷帕霉素类似物的浆液; 搅拌雷帕霉素类似物混合物直到雷帕霉素类似物结晶; 饱和雷帕霉素类似物溶液; 形成过饱和雷帕霉素类似物溶液; 将抗溶剂与雷帕霉素类似物和溶剂组合以形成双相混合物,并将两相混合物温育以引起液 - 液相分裂。
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4.
公开(公告)号:US20110009618A1
公开(公告)日:2011-01-13
申请号:US12886398
申请日:2010-09-20
申请人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
发明人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
IPC分类号: C07D498/16
CPC分类号: C07D498/18
摘要: A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic medium can be a solvent, and the process can include causing the rapamycin analog to dissolve into the solvent, and incubating the solvent until the rapamycin analog crystallizes. The following can also be performed: forming a slurry of crystalline rapamycin analog; stirring the rapamycin analog mixture until the rapamycin analog crystallizes; saturating the rapamycin analog solution; forming a supersaturated rapamycin analog solution; combining an antisolvent with the rapamycin analog and the solvent to form a biphasic mixture, and incubating the biphasic mixture to cause a liquid-liquid phase split.
摘要翻译: 制备结晶雷帕霉素类似物的方法包括:将雷帕霉素类似物与有机介质结合以形成混合物; 孵育混合物直到雷帕霉素类似物结晶; 并回收结晶雷帕霉素类似物。 有机介质可以是溶剂,并且该方法可以包括使雷帕霉素类似物溶解到溶剂中,并将溶剂温育直到雷帕霉素类似物结晶。 还可以进行以下操作:形成结晶雷帕霉素类似物的浆液; 搅拌雷帕霉素类似物混合物直到雷帕霉素类似物结晶; 饱和雷帕霉素类似物溶液; 形成过饱和雷帕霉素类似物溶液; 将抗溶剂与雷帕霉素类似物和溶剂组合以形成双相混合物,并将两相混合物温育以引起液 - 液相分裂。
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5.
公开(公告)号:US20120028908A1
公开(公告)日:2012-02-02
申请号:US13251207
申请日:2011-10-01
申请人: Shekhar VISWANATH , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
发明人: Shekhar VISWANATH , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
IPC分类号: A61K38/16 , A61K31/437 , A61K31/7048 , A61P35/00 , A61K31/565 , A61K31/56 , C07D498/12 , A61K31/5365 , A61K31/573
CPC分类号: C07D498/18
摘要: A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic medium can be a solvent, and the process can include causing the rapamycin analog to dissolve into the solvent, and incubating the solvent until the rapamycin analog crystallizes. The following can also be performed: forming a slurry of crystalline rapamycin analog; stirring the rapamycin analog mixture until the rapamycin analog crystallizes; saturating the rapamycin analog solution; forming a supersaturated rapamycin analog solution; combining an antisolvent with the rapamycin analog and the solvent to form a biphasic mixture, and incubating the biphasic mixture to cause a liquid-liquid phase split.
摘要翻译: 制备结晶雷帕霉素类似物的方法包括:将雷帕霉素类似物与有机介质结合以形成混合物; 孵育混合物直到雷帕霉素类似物结晶; 并回收结晶雷帕霉素类似物。 有机介质可以是溶剂,并且该方法可以包括使雷帕霉素类似物溶解到溶剂中,并将溶剂温育直到雷帕霉素类似物结晶。 还可以进行以下操作:形成结晶雷帕霉素类似物的浆液; 搅拌雷帕霉素类似物混合物直到雷帕霉素类似物结晶; 饱和雷帕霉素类似物溶液; 形成过饱和雷帕霉素类似物溶液; 将抗溶剂与雷帕霉素类似物和溶剂组合以形成双相混合物,并将两相混合物温育以引起液 - 液相分裂。
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公开(公告)号:US08030326B2
公开(公告)日:2011-10-04
申请号:US12886410
申请日:2010-09-20
申请人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
发明人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
IPC分类号: A61K31/395 , A61P37/06
CPC分类号: A61K31/33
摘要: Provided is a rapamycin analog composition including a crystalline form of a rapamycin analog. The crystal can be a hydrate. dehydrate, solvate, or desolvate. The rampamycin analog can have a structure of Formula 1, which is optionally a prodrug, salt, derivative, or combination thereof:
摘要翻译: 提供了包含雷帕霉素类似物的结晶形式的雷帕霉素类似物组合物。 晶体可以是水合物。 脱水,溶剂化物或去溶剂化物。 吡草霉素类似物可以具有式1的结构,其可任选地是前药,盐,衍生物或其组合:
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公开(公告)号:US20110009325A1
公开(公告)日:2011-01-13
申请号:US12886410
申请日:2010-09-20
申请人: SHEKHAR VISWANATH , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
发明人: SHEKHAR VISWANATH , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
IPC分类号: A61K31/436 , A61K31/437 , A61K31/7048 , A61K31/704 , A61K31/662 , A61K38/12 , A61K38/06 , A61K38/16 , A61K31/573 , A61K31/565 , A61P35/00 , A61P29/00 , A61P37/02 , A61P9/00
CPC分类号: A61K31/33
摘要: Provided is a rapamycin analog composition including a crystalline form of a rapamycin analog. The crystal can be a hydrate. dehydrate, solvate, or desolvate. The rampamycin analog can have a structure of Formula 1, which is optionally a prodrug, salt, derivative, or combination thereof:
摘要翻译: 提供了包含雷帕霉素类似物的结晶形式的雷帕霉素类似物组合物。 晶体可以是水合物。 脱水,溶剂化物或去溶剂化物。 吡草霉素类似物可以具有式1的结构,其可任选地是前药,盐,衍生物或其组合:
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8.
公开(公告)号:US20080091008A1
公开(公告)日:2008-04-17
申请号:US11781807
申请日:2007-07-23
申请人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
发明人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
IPC分类号: C07D267/22
CPC分类号: C07D498/18
摘要: A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic medium can be a solvent, and the process can include causing the rapamycin analog to dissolve into the solvent, and incubating the solvent until the rapamycin analog crystallizes. The following can also be performed: forming a slurry of crystalline rapamycin analog; stirring the rapamycin analog mixture until the rapamycin analog crystallizes; saturating the rapamycin analog solution; forming a supersaturated rapamycin analog solution; combining an antisolvent with the rapamycin analog and the solvent to form a biphasic mixture, and incubating the biphasic mixture to cause a liquid-liquid phase split.
摘要翻译: 制备结晶雷帕霉素类似物的方法包括:将雷帕霉素类似物与有机介质结合以形成混合物; 孵育混合物直到雷帕霉素类似物结晶; 并回收结晶雷帕霉素类似物。 有机介质可以是溶剂,并且该方法可以包括使雷帕霉素类似物溶解到溶剂中,并将溶剂温育直到雷帕霉素类似物结晶。 还可以进行以下操作:形成结晶雷帕霉素类似物的浆液; 搅拌雷帕霉素类似物混合物直到雷帕霉素类似物结晶; 饱和雷帕霉素类似物溶液; 形成过饱和雷帕霉素类似物溶液; 将抗溶剂与雷帕霉素类似物和溶剂组合以形成双相混合物,并将两相混合物温育以引起液 - 液相分裂。
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公开(公告)号:US20080085880A1
公开(公告)日:2008-04-10
申请号:US11781804
申请日:2007-07-23
申请人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
发明人: Shekhar Viswanath , Larry Bartelt , Robert Leanna , Michael Rasmussen , Madhup Dhaon , Rodger Henry , Thomas Borchardt , Shuang Chen , Geoff Zhang
CPC分类号: A61K31/33
摘要: A rapamycin analog composition includes a crystalline form of a rapamycin analog. The crystal can be a hydrate, dehydrate, solvate, or desolvate. The rapamycin analog can have a structure of Formula 1, which is optionally a prodrug, salt, derivative, or combination thereof:
摘要翻译: 雷帕霉素类似物组合物包括雷帕霉素类似物的结晶形式。 该晶体可以是水合物,脱水剂,溶剂化物或去溶剂化物。 雷帕霉素类似物可以具有式1的结构,其可任选地是前药,盐,衍生物或其组合:
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公开(公告)号:US09464078B2
公开(公告)日:2016-10-11
申请号:US13238239
申请日:2011-09-21
IPC分类号: A61K31/44 , C07D471/08 , C07D451/14 , A61K31/439 , A61K45/06
CPC分类号: C07D451/14 , A61K31/439 , A61K45/06 , C07D471/08
摘要: The invention relates to a crystalline monohydrate of (4s)-4-(5-phenyl-1,3,4-thiadiazol-2-yloxy)-1-azatricyclo[3.3.1.13,7]decane dihydrogen citrate, compositions comprising such compound, and a process for preparing such compound.
摘要翻译: 本发明涉及(4s)-4-(5-苯基-1,3,4-噻二唑-2-基氧基)-1-氮杂三环[3.3.1.13,7]癸烷二氢二氢柠檬酸盐的结晶一水合物,包含这种化合物 ,以及这种化合物的制备方法。
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