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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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2.
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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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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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: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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6.
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:US06897318B2
公开(公告)日:2005-05-24
申请号:US10254445
申请日:2002-09-25
申请人: Kimberly K. Allen , Dennis K. Anderson , John E. Baldus , Jerry D. Clark , Albert D. Edeny , Patrick H. Lau , Daniel R. Dukesherer , Lisa McDermott , Michael K. Mao , Gopi Yalamanchili , Jodi L. Moe , Partha Mudipalli , Win Naing , Shaun R. Selness , Christine Seymour , Shekhar Viswanath , John K. Walker
发明人: Kimberly K. Allen , Dennis K. Anderson , John E. Baldus , Jerry D. Clark , Albert D. Edeny , Patrick H. Lau , Daniel R. Dukesherer , Lisa McDermott , Michael K. Mao , Gopi Yalamanchili , Jodi L. Moe , Partha Mudipalli , Win Naing , Shaun R. Selness , Christine Seymour , Shekhar Viswanath , John K. Walker
IPC分类号: C07D403/14 , A61K31/506 , A61P1/04 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/14 , A61P25/28 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/04 , A61P31/16 , A61P31/18 , A61P31/22 , A61P33/06 , A61P35/00 , A61P37/06 , C07D401/14 , C07D401/04
CPC分类号: C07D401/14
摘要: This invention is directed generally to a process for making substituted pyrazoles, tautomers of the substituted pyrazoles, and salts of the substituted pyrazoles and tautomers. The substituted pyrazoles correspond in structure to Formula (I): wherein R3A, R3B, R3C, Y1, Y2, Y3, Y4, and Y5 are as defined in the specification.
摘要翻译: 本发明一般涉及制备取代的吡唑,取代的吡唑的互变异构体和取代的吡唑和互变异构体的盐的方法。 取代的吡唑在结构上对应于式(I):其中R 3A,R 3B,R 3C,Y 1, Y 2,Y 2,Y 3,Y 4和Y 5如说明书中所定义。
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公开(公告)号:US07057049B2
公开(公告)日:2006-06-06
申请号:US10406150
申请日:2003-04-01
申请人: Kimberley C. Allen , Dennis K. Anderson , John E. Baldus , Todd Boehlow , Jerry D. Clark , Dan R. Dukesherer , Albert D. Edney , Tom Fevig , Sastry Kunda , Jon P. Lawson , Patrick H. Lau , Lisa L. McDermott , Michael K. Mao , Jodi L. Moe , Partha Mudipalli , Win Naing , Shaun R. Selness , Christine B. Seymour , Tobin C. Schilke , Shekhar Viswanath , John K. Walker , Gopichand Yalamanchili
发明人: Kimberley C. Allen , Dennis K. Anderson , John E. Baldus , Todd Boehlow , Jerry D. Clark , Dan R. Dukesherer , Albert D. Edney , Tom Fevig , Sastry Kunda , Jon P. Lawson , Patrick H. Lau , Lisa L. McDermott , Michael K. Mao , Jodi L. Moe , Partha Mudipalli , Win Naing , Shaun R. Selness , Christine B. Seymour , Tobin C. Schilke , Shekhar Viswanath , John K. Walker , Gopichand Yalamanchili
IPC分类号: C07D231/12 , C07D211/06 , C07D211/16
CPC分类号: C07D401/06 , C07D401/14
摘要: This invention is directed generally to a process for making substituted pyrazoles, tautomers of the substituted pyrazoles, and salts of the substituted pyrazoles and tautomers. The substituted pyrazoles correspond in structure to Formula (I): wherein R3A, R3B, R3C, Y1, Y2, Y3, Y4, and Y5 are as defined in the specification.
摘要翻译: 本发明一般涉及制备取代的吡唑,取代的吡唑的互变异构体和取代的吡唑和互变异构体的盐的方法。 取代的吡唑在结构上对应于式(I):其中R 3A,R 3B,R 3C,Y 1, Y 2,Y 2,Y 3,Y 4和Y 5如说明书中所定义。
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