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1. 发明申请

US20140364457A1 COMPOSITIONS FOR REDUCING AB 42 PRODUCTION AND THEIR USE IN TREATING ALZHEIMER'S DISEASE (AD) 有权
标题翻译：用于减少AB 42生产的组合物及其在治疗阿尔茨海默病（AD）中的应用
公开(公告)号：US20140364457A1
公开(公告)日：2014-12-11
申请号：US14469366
申请日：2014-08-26
申请人： KAREUS THERAPEUTICS SA
发明人： Venkateswarlu Akella , Uday Saxena , Anji Reddy Kallam
IPC分类号： C07D213/82 , C07D213/80 , C07D401/06 , C07D401/12
CPC分类号： C07D213/82 , C07D213/56 , C07D213/80 , C07D401/06 , C07D401/12
摘要： Novel small molecule compounds for reduction of Aβ 42 production and for treatment of Alzheimer's disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
摘要翻译：用于还原A和Bgr的新型小分子化合物描述了生产和治疗阿尔茨海默病和其他神经变性疾病，制备它们的方法和含有它们的药物组合物。

2. 发明授权

US09464053B2 Compositions for reducing Aβ 42 production and their use in treating alzheimer's disease (AD) 有权
标题翻译：用于减少Aβ42产生及其在治疗阿尔茨海默病（AD）中的应用的组合物
公开(公告)号：US09464053B2
公开(公告)日：2016-10-11
申请号：US14469366
申请日：2014-08-26
申请人： KAREUS THERAPEUTICS SA
发明人： Venkateswarlu Akella , Uday Saxena , Anji Reddy Kallam
IPC分类号： C07D213/80 , C07D401/06 , A61K31/44 , C07D213/82 , C07D213/56 , C07D401/12
CPC分类号： C07D213/82 , C07D213/56 , C07D213/80 , C07D401/06 , C07D401/12
摘要： Novel small molecule compounds for reduction of Aβ 42 production and for treatment of Alzheimer's disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
摘要翻译：描述了用于降低Aβ42产生和治疗阿尔茨海默氏病和其他神经变性疾病的新型小分子化合物，其制备方法和含有它们的药物组合物。

3. 发明申请

WO2013035053A3 NOVEL CONJUGATION-FACILITATED TRANSPORT OF DRUGS ACROSS BLOOD BRAIN BARRIER 审中-公开
公开(公告)号：WO2013035053A3
公开(公告)日：2013-03-14
申请号：PCT/IB2012/054593
申请日：2012-09-06
申请人： KAREUS THERAPEUTICS, SA , SAXENA, Uday , AKELLA, Venkateswarlu
发明人： SAXENA, Uday , AKELLA, Venkateswarlu
IPC分类号： A61K38/02 , A61P25/28 , A61P25/16 , A61P25/00
摘要： The present invention provides a conjugated therapeutic agent of formula I that can facilitate transport of therapeutic agent across the blood brain barrier thereby providing drug levels in brain to impart beneficial therapeutic effect.

4. 发明申请

WO2012090104A1 METHODS AND COMPOSITIONS FOR DESIGNING NOVEL CONJUGATE THERAPEUTICS 审中-公开
标题翻译：设计新型结合治疗方法和组合物
公开(公告)号：WO2012090104A1
公开(公告)日：2012-07-05
申请号：PCT/IB2011/055598
申请日：2011-12-12
申请人： KAREUS THERAPEUTICS, SA , AKELLA, Venkateswarlu , SAXENA, Uday , REDDY, Anji Reddy
发明人： AKELLA, Venkateswarlu , SAXENA, Uday , REDDY, Anji Reddy
IPC分类号： A61K51/00 , A61K39/00 , A61K39/385
CPC分类号： A61K47/48038 , A61K47/542 , A61K47/55
摘要： The present invention relates to novel drug conjugates, where in two drugs are linked together through an appropriate linker having at least two functional groups capable of forming covalent bond with drugs D1 and D2.The invention also relates to developing novel compositions, methods for their preparation and their use in treating various disease conditions.
摘要翻译：本发明涉及新的药物偶联物，其中两种药物通过具有至少两个能够与药物D1和D2形成共价键的官能团的适当接头连接在一起。本发明还涉及开发新的组合物，其制备方法并用于治疗各种疾病。

5. 发明申请

WO2013035053A2 NOVEL CONJUGATION-FACILITATED TRANSPORT OF DRUGS ACROSS BLOOD BRAIN BARRIER 审中-公开
标题翻译：新型凝血运输药物血脑屏障
公开(公告)号：WO2013035053A2
公开(公告)日：2013-03-14
申请号：PCT/IB2012054593
申请日：2012-09-06
申请人： KAREUS THERAPEUTICS SA , SAXENA UDAY , AKELLA VENKATESWARLU
发明人： SAXENA UDAY , AKELLA VENKATESWARLU
IPC分类号： A61K31/44
CPC分类号： C07D491/06 , A61K47/55 , C07D213/80
摘要： The present invention provides a conjugated therapeutic agent of formula I that can facilitate transport of therapeutic agent across the blood brain barrier thereby providing drug levels in brain to impart beneficial therapeutic effect.
摘要翻译：本发明提供式I的缀合治疗剂，其可促进治疗剂跨越血脑屏障的转运，从而提供脑中的药物水平以赋予有益的治疗效果。

6. 发明申请

WO2012040177A1 METHODS AND COMPOSITIONS FOR TREATMENT OF DIABETES AND DYSLIPIDEMIA 审中-公开
标题翻译：用于治疗糖尿病和DYSLIPIDEMIA的方法和组合物
公开(公告)号：WO2012040177A1
公开(公告)日：2012-03-29
申请号：PCT/US2011/052318
申请日：2011-09-20
申请人： KAREUS THERAPEUTICS, SA , KHANNA, Ish , PILLARISETTI, Sivaram
发明人： KHANNA, Ish , PILLARISETTI, Sivaram
IPC分类号： A61K31/225
CPC分类号： C07C311/51 , C07C31/27 , C07C43/115 , C07C53/132 , C07C61/12 , C07C61/15 , C07C69/608 , C07C69/74 , C07C233/58 , C07C233/60 , C07C255/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D257/04
摘要： Novel compounds of Formula I are provided: its stereoisomers and/or pharmaceutically acceptable salts for the treatment of diabetes and diabetes-associated dyslipidemia, wherein R1 is selected from a group consisting of hydroxy, alkoxy, amine, alkyl, haloalkyl, NHSO 2 R, or NHCOR wherein R is selected from alkyl or cycloalkyl, NHR' wherein R' is alkyl or cycloalkyl optionally substituted by hydroxy or alkoxy; and n 1 and n 2 are independently selected from 0, 1, and 2. At least one of R 3 and R 4 and/or R 5 and R 6 form a cyclic ring of 3-8 carbon atoms optionally containing alkyl groups, hetero atoms, or functional groups such as O, N, SO 2 . Additionally, when R 3 and R 4 or R 5 and R 6 do not form a cyclic ring, then they may be independently selected from hydrogen, alkyl, branched alkyl, and cycloalkyl. L 1 is a linear aliphatic chain optionally containing from 4 to 16 carbon atoms. The chain may optionally be substituted one or more times by alkyl, branched alkyl, cycloalkyl, or aryl. R 2 is independently selected from hydrogen, alkoxy, hydroxy, alkyl, haloalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, cyano, or COR 7 , wherein R 7 is selected from hydroxy, alkyl, alkoxy, or amine, NHR', NHSO2R, or NHCOR. Y 1 is oxygen or hydrogen. Y 2 is optional, wherein when Y2 is present, Y 1 and Y 2 are hydrogen. When Y 2 is not present, Y 1 is a carbonyl group.
摘要翻译：提供式I的新型化合物：其用于治疗糖尿病和糖尿病相关血脂异常的其立体异构体和/或药学上可接受的盐，其中R 1选自羟基，烷氧基，胺，烷基，卤代烷基，NHSO 2 R或NHCOR 其中R选自烷基或环烷基，NHR'，其中R'是任选被羟基或烷氧基取代的烷基或环烷基; 并且n1和n2独立地选自0,1和2. R3和R4和/或R5和R6中的至少一个形成3-8个碳原子的环状环，任选地含有烷基，杂原子或官能团，例如作为O，N，SO 2。此外，当R3和R4或R5和R6不形成环时，它们可以独立地选自氢，烷基，支链烷基和环烷基。 L1是任选含有4至16个碳原子的直链脂族链。该链可以任选地被烷基，支链烷基，环烷基或芳基取代一次或多次。 R 2独立地选自氢，烷氧基，羟基，烷基，卤代烷基，环烷基，杂环烷基，杂芳基，氰基或COR 7，其中R 7选自羟基，烷基，烷氧基或胺，NHR'，NHSO 2 R或NHCOR。 Y1是氧或氢。 Y2是任选的，其中当存在Y2时，Y1和Y2是氢。当不存在Y2时，Y1是羰基。

7. 发明公开

EP2618824A4 METHODS AND COMPOSITIONS FOR TREATMENT OF DIABETES AND DYSLIPIDEMIA 审中-公开
标题翻译： VERFAHREN UND ZUSAMMENSETZUNGEN ZUR BEHANDLUNG VON DIABETES UNDDYSLIPIDÄMIE
公开(公告)号：EP2618824A4
公开(公告)日：2015-05-06
申请号：EP11827340
申请日：2011-09-20
申请人： KAREUS THERAPEUTICS SA
发明人： KHANNA ISH , PILLARISETTI SIVARAM
IPC分类号： A61K31/225 , C07C31/27 , C07C43/115 , C07C53/132 , C07C69/608 , C07C233/58 , C07C233/60 , C07C311/51 , C07D257/04
CPC分类号： C07C311/51 , C07C31/27 , C07C43/115 , C07C53/132 , C07C61/12 , C07C61/15 , C07C69/608 , C07C69/74 , C07C233/58 , C07C233/60 , C07C255/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D257/04

8. 发明公开

EP2618824A1 METHODS AND COMPOSITIONS FOR TREATMENT OF DIABETES AND DYSLIPIDEMIA 审中-公开
标题翻译：方法和组合物的糖尿病和血脂异常
公开(公告)号：EP2618824A1
公开(公告)日：2013-07-31
申请号：EP11827340.8
申请日：2011-09-20
申请人： Kareus Therapeutics SA
发明人： KHANNA, Ish , PILLARISETTI, Sivaram
IPC分类号： A61K31/225
CPC分类号： C07C311/51 , C07C31/27 , C07C43/115 , C07C53/132 , C07C61/12 , C07C61/15 , C07C69/608 , C07C69/74 , C07C233/58 , C07C233/60 , C07C255/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D257/04
摘要： Novel compounds of Formula I are provided: its stereoisomers and/or pharmaceutically acceptable salts for the treatment of diabetes and diabetes-associated dyslipidemia, wherein R1 is selected from a group consisting of hydroxy, alkoxy, amine, alkyl, haloalkyl, NHSO
2 R, or NHCOR wherein R is selected from alkyl or cycloalkyl, NHR' wherein R' is alkyl or cycloalkyl optionally substituted by hydroxy or alkoxy; and n
1 and n
2 are independently selected from 0, 1, and 2. At least one of R
3 and R
4 and/or R
5 and R
6 form a cyclic ring of 3-8 carbon atoms optionally containing alkyl groups, hetero atoms, or functional groups such as O, N, SO
2 . Additionally, when R
3 and R
4 or R
5 and R
6 do not form a cyclic ring, then they may be independently selected from hydrogen, alkyl, branched alkyl, and cycloalkyl. L
1 is a linear aliphatic chain optionally containing from 4 to 16 carbon atoms. The chain may optionally be substituted one or more times by alkyl, branched alkyl, cycloalkyl, or aryl. R
2 is independently selected from hydrogen, alkoxy, hydroxy, alkyl, haloalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, cyano, or COR
7 , wherein R
7 is selected from hydroxy, alkyl, alkoxy, or amine, NHR', NHSO2R, or NHCOR. Y
1 is oxygen or hydrogen. Y
2 is optional, wherein when Y2 is present, Y
1 and Y
2 are hydrogen. When Y
2 is not present, Y
1 is a carbonyl group.

9. 发明专利

ZA201301936B METHODS AND COMPOSITIONS FOR TREATMENT OF DIABETES AND DYSLIPIDEMIA 未知
公开(公告)号：ZA201301936B
公开(公告)日：2014-05-28
申请号：ZA201301936
申请日：2013-03-14
申请人： KAREUS THERAPEUTICS SA
发明人： KHANNA ISH , PILLARISETTI SIVARAM
IPC分类号： A61K20060101
摘要： Novel compounds of Formula I are provided: its stereoisomers and/or pharmaceutically acceptable salts for the treatment of diabetes and diabetes-associated dyslipidemia, wherein R1 is selected from a group consisting of hydroxy, alkoxy, amine, alkyl, haloalkyl, NHSO2R, or NHCOR wherein R is selected from alkyl or cycloalkyl, NHR′ wherein R′ is alkyl or cycloalkyl optionally substituted by hydroxy or alkoxy; and n1 and n2 are independently selected from 0, 1, and 2. At least one of R3 and R4 and/or R5 and R6 form a cyclic ring of 3-8 carbon atoms optionally containing alkyl groups, hetero atoms, or functional groups such as O, N, SO2. Additionally, when R3 and R4 or R5 and R6 do not form a cyclic ring, then they may be independently selected from hydrogen, alkyl, branched alkyl, and cycloalkyl. L1 is a linear aliphatic chain optionally containing from 4 to 16 carbon atoms. The chain may optionally be substituted one or more times by alkyl, branched alkyl, cycloalkyl, or aryl. R2 is independently selected from hydrogen, alkoxy, hydroxy, alkyl, haloalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, cyano, or COR7, wherein R7 is selected from hydroxy, alkyl, alkoxy, or amine, NHR′, NHSO2R, or NHCOR. Y1 is oxygen or hydrogen. Y2 is optional, wherein when Y2 is present, Y1 and Y2 are hydrogen. When Y2 is not present, Y1 is a carbonyl group.

10. 发明公开

EP2528898A2 NOVEL COMPOSITIONS FOR REDUCING Aß 42 PRODUCTION AND THEIR USE IN TREATING ALZHEIMER'S DISEASE (AD) 审中-公开
标题翻译： NEW状组合减少Aß42生产及其用途阿尔茨海默氏病的治疗
公开(公告)号：EP2528898A2
公开(公告)日：2012-12-05
申请号：EP11708084.6
申请日：2011-01-22
申请人： Kareus Therapeutics SA
发明人： AKELLA, Venkateswarulu , SAXENA, Uday , KALLAM, Anji Reddy
IPC分类号： C07D213/80 , C07D213/82 , C07D401/06 , C07D401/12 , A61K31/4406 , A61P25/28
CPC分类号： C07D213/82 , C07D213/56 , C07D213/80 , C07D401/06 , C07D401/12
摘要： Novel small molecule compounds for reduction of Aß 42 production and for treatment of Alzheimer's Disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
摘要翻译：新型小分子减少A化合物？ 42生产用于治疗阿尔茨海默病和其它神经变性病症中，描述了制备它们的方法和含有它们的药物组合物。

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