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1. 发明申请

WO2005062874A3 COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS 审中-公开
标题翻译：用于递送活性剂的化合物和组合物
公开(公告)号：WO2005062874A3
公开(公告)日：2005-12-15
申请号：PCT/US2004043035
申请日：2004-12-20
申请人： EMISPHERE TECH INC , FREEMAN JOHN J JR
发明人： FREEMAN JOHN J JR
IPC分类号： A61K31/195 , A61K38/11 , A61K38/13 , A61K38/18 , A61K38/20 , A61K38/21 , A61K38/22 , A61K38/23 , A61K38/24 , A61K38/26 , A61K38/27 , A61K38/28 , A61K38/29 , A61K38/30 , A61K38/31 , A61K38/35 , A61K38/55 , A61K45/06 , C07C235/60 , C07C237/40 , A61K31/715 , A61K38/00 , A61K47/12 , C07C229/06
CPC分类号： C07C237/40 , A61K31/195 , A61K38/26 , A61K38/28 , A61K45/06 , C07C235/60 , A61K2300/00
摘要： Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
摘要翻译：提供用于递送活性剂的化合物和组合物。也提供给药和制备方法。

2. 发明申请

WO2012109256A3 FORMATION OF N-PROTECTED BIS-3,6-(4-AMINOALKYL) -2,5,DIKETOPIPERAZINE 审中-公开
标题翻译：形成N-保护的BIS-3,6-（4-氨基二甲基）-2,5，二酮类
公开(公告)号：WO2012109256A3
公开(公告)日：2013-01-24
申请号：PCT/US2012024160
申请日：2012-02-07
申请人： MANNKIND CORP , FREEMAN JOHN J , STAMPER ADRIENNE , HEITMANN MELISSA
发明人： FREEMAN JOHN J , STAMPER ADRIENNE , HEITMANN MELISSA
IPC分类号： C07D241/08 , B01J31/02 , C07C229/00
CPC分类号： C07D241/08 , B01J31/0225 , B01J31/0258 , B01J31/0259 , B01J2231/40
摘要： The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1 -propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.
摘要翻译：所公开的实施方案详细描述了从氨基酸合成二酮哌嗪的改进方法。特别是用于由N-保护的氨基酸环化缩合和纯化N-保护的3,6-（氨基烷基）-2,5-二酮哌嗪的改进方法。公开的实施方案描述了合成3,6-双[N-保护的氨基烷基] -2,5-二酮哌嗪的方法，包括在催化剂存在下在有机溶剂中加热氨基酸的混合物。催化剂选自硫酸，磷酸，对甲苯磺酸，1-丙基膦酸环状酸酐，磷酸三丁酯，苯基膦酸和五氧化二磷等。溶剂选自二甲基乙酰胺，N-甲基-2-吡咯烷酮，二甘醇二甲醚，甘醇二甲醚，丙二醇，乙基二甘醇二甲醚，间甲酚，对甲酚，邻甲酚，二甲苯，乙二醇和苯酚等。

3. 发明申请

WO2012109256A2 FORMATION OF N-PROTECTED BIS-3,6-(4-AMINOALKYL) -2,5,DIKETOPIPERAZINE 审中-公开
标题翻译：形成N-保护的BIS-3,6-（4-氨基二甲基）-2,5，二酮类
公开(公告)号：WO2012109256A2
公开(公告)日：2012-08-16
申请号：PCT/US2012/024160
申请日：2012-02-07
申请人： MANNKIND, CORP , FREEMAN, John, J. , STAMPER, Adrienne , HEITMANN, Melissa
发明人： FREEMAN, John, J. , STAMPER, Adrienne , HEITMANN, Melissa
IPC分类号： C07D241/08 , C07C229/00 , B01J31/02
CPC分类号： C07D241/08 , B01J31/0225 , B01J31/0258 , B01J31/0259 , B01J2231/40
摘要： The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1 -propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.
摘要翻译：所公开的实施方案详细描述了从氨基酸合成二酮哌嗪的改进方法。特别是用于由N-保护的氨基酸环化缩合和纯化N-保护的3,6-（氨基烷基）-2,5-二酮哌嗪的改进方法。公开的实施方案描述了合成3,6-双[N-保护的氨基烷基] -2,5-二酮哌嗪的方法，包括在催化剂存在下在有机溶剂中加热氨基酸的混合物。催化剂选自硫酸，磷酸，对甲苯磺酸，1-丙基膦酸环状酸酐，磷酸三丁酯，苯基膦酸和五氧化二磷等。溶剂选自二甲基乙酰胺，N-甲基-2-吡咯烷酮，二甘醇二甲醚，甘醇二甲醚，丙二醇，乙基二甘醇二甲醚，间甲酚，对甲酚，邻甲酚，二甲苯，乙二醇和苯酚等。

4. 发明申请

WO2005062874A2 COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS 审中-公开
公开(公告)号：WO2005062874A2
公开(公告)日：2005-07-14
申请号：PCT/US2004/043035
申请日：2004-12-20
申请人： EMISPHERE TECHNOLOGIES, INC. , FREEMAN, John, J., Jr.
发明人： FREEMAN, John, J., Jr.
IPC分类号： A61K31/195 , A61K38/11 , A61K38/13 , A61K38/18 , A61K38/20 , A61K38/21 , A61K38/22 , A61K38/23 , A61K38/24 , A61K38/26 , A61K38/27 , A61K38/28 , A61K38/29 , A61K38/30 , A61K38/31 , A61K38/35 , A61K38/55 , A61K45/06 , C07C235/60 , C07C237/40
CPC分类号： C07C237/40 , A61K31/195 , A61K38/26 , A61K38/28 , A61K45/06 , C07C235/60 , A61K2300/00
摘要： Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

5. 发明申请

WO0132596A8 PHENOXY CARBOXYLIC ACID COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS 审中-公开
标题翻译：苯甲酸羧酸化合物和用于递送活性剂的组合物
公开(公告)号：WO0132596A8
公开(公告)日：2001-08-09
申请号：PCT/US0030662
申请日：2000-11-06
申请人： EMISPHERE TECH INC , LEONE BAY ANDREA , KRAFT KELLY , MOYE SHERMAN DESTARDI , GSCHNEIDNER DAVID , BOYD MARIA A P , LIU PUCHUN , TANG PINWAH , LIAO JUN , SMART JOHN E , FREEMAN JOHN J JR
发明人： LEONE-BAY ANDREA , KRAFT KELLY , MOYE-SHERMAN DESTARDI , GSCHNEIDNER DAVID , BOYD MARIA A P , LIU PUCHUN , TANG PINWAH , LIAO JUN , SMART JOHN E , FREEMAN JOHN J JR
IPC分类号： A61K9/08 , A61K9/14 , A61K9/20 , A61K9/48 , A61K31/352 , A61K31/727 , A61K38/00 , A61K38/21 , A61K38/23 , A61K38/27 , A61K38/28 , A61K45/00 , A61K47/12 , A61K47/18 , A61P3/10 , A61P5/10 , A61P5/14 , A61P5/48 , A61P7/02 , A61P19/08 , A61P19/10 , A61P31/04 , A61P37/08 , A61P43/00 , C07C59/66 , C07C59/68 , C07C59/90 , C07C59/92 , C07C65/21 , C07C65/24 , C07C65/40 , C07C205/37 , C07C217/84 , C07C229/18 , C07C229/56 , C07C233/25 , C07C235/46 , C07C235/48 , C07C237/30 , C07C62/32
CPC分类号： C07C65/24 , C07C59/68 , C07C59/90 , C07C59/92 , C07C65/40 , C07C229/18 , C07C229/56 , C07C237/30
摘要： Phenoxy carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
摘要翻译：提供了苯氧基羧酸化合物和用于递送活性剂的组合物。也提供给药和制备方法。

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