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1. 发明授权

US10822374B2 Cancer therapies and diagnostics 有权
公开(公告)号：US10822374B2
公开(公告)日：2020-11-03
申请号：US13884709
申请日：2011-11-14
申请人： Loren D. Walensky , Federico Bernal , Geoffrey Wahl , Mark Wade
发明人： Loren D. Walensky , Federico Bernal , Geoffrey Wahl , Mark Wade
IPC分类号： C07K4/12 , A61K38/17
摘要： Compositions and methods for increasing p53-dependent transcriptional activity in a cell.

2. 发明授权

US09822165B2 Hydrocarbon stapled stabilized alpha-helices of the HIV-1 GP41 membrane proximal external region 有权
公开(公告)号：US09822165B2
公开(公告)日：2017-11-21
申请号：US13378929
申请日：2010-06-18
申请人： Loren D. Walensky , Gregory Bird
发明人： Loren D. Walensky , Gregory Bird
IPC分类号： C07K16/10 , A61K39/21 , A61K39/12
CPC分类号： C07K16/1045 , A61K39/12 , A61K39/21 , C07K16/1063 , C07K2317/34 , C07K2317/76 , C12N2740/16034 , C12N2740/16122 , C12N2740/16134
摘要： The invention provides structurally constrained viral peptides for use as therapeutic and vaccination agents, and for the production of antibodies for use in a number of applications including as therapeutic agents. The invention further provides methods and kits for use of the structurally constrained peptides and antibodies of the instant invention. The invention is based, at least in part, on the result provided herein demonstrating that viral hydrocarbon stapled helical peptides display excellent proteolytic, acid, and thermal stability, restore the native helical structure of the peptide, are highly effective in interfering with the viral fusogenic process, and possess superior pharmacokinetic properties compared to the corresponding unmodified peptides.

3. 发明授权

US09290545B2 Compositions and methods for the treatment of viral infections 有权
标题翻译：用于治疗病毒感染的组合物和方法
公开(公告)号：US09290545B2
公开(公告)日：2016-03-22
申请号：US12864375
申请日：2010-07-23
申请人： Loren D. Walensky , Gregory H. Bird
发明人： Loren D. Walensky , Gregory H. Bird
IPC分类号： C07K14/005 , A61K38/16
CPC分类号： C07K14/005 , A61K38/162 , A61K39/145 , A61K39/155 , A61K39/21 , C07K16/1063 , C07K2317/76 , C12N2740/15022 , C12N2740/15034 , C12N2740/15071 , C12N2740/16122 , C12N2740/16134 , C12N2740/16171 , C12N2740/16222 , C12N2740/16234 , C12N2740/16271 , C12N2760/14022 , C12N2760/14034 , C12N2760/14071 , C12N2760/16022 , C12N2760/16034 , C12N2760/16071 , C12N2760/18022 , C12N2760/18034 , C12N2760/18071 , C12N2760/18522 , C12N2760/18534 , C12N2760/18571 , C12N2760/18622 , C12N2760/18634 , C12N2760/18671
摘要： The invention provides compositions, kits and methods utilizing polypeptides having a viral alpha-helix heptad repeat domain in a stabilized α-helical structure (herein also referred to as SAH). The compositions are useful for treating and/or preventing viral infections. The invention is based, at least in part, on the result provided herein demonstrating that viral hydrocarbon stapled alpha helical peptides display excellent proteolytic, acid, and thermal stability, restore the native alpha-helical structure of the peptide, are highly effective in interfering with the viral fusogenic process, and possess superior pharmacokinetic properties compared to the corresponding unmodified peptides.
摘要翻译：本发明提供了利用在稳定的α-螺旋结构（本文中也称为SAH）中具有病毒α-螺旋七肽重复结构域的多肽的组合物，试剂盒和方法。该组合物可用于治疗和/或预防病毒感染。本发明至少部分地基于本文提供的结果，证明病毒性碳氢化合物钉扎的α螺旋肽显示优异的蛋白水解，酸和热稳定性，恢复肽的天然α-螺旋结构，在干扰病毒融合过程，并且与相应的未修饰的肽相比具有优异的药代动力学性质。

4. 发明授权

US08796418B2 Stabilized alpha helical peptides and uses thereof 有权
标题翻译：稳定的α螺旋肽及其用途
公开(公告)号：US08796418B2
公开(公告)日：2014-08-05
申请号：US12233555
申请日：2008-09-18
申请人： Loren D. Walensky , Gregory L. Verdine , Susan Korsmeyer
发明人： Loren D. Walensky , Stanley J. Korsmeyer , Gregory L. Verdine
IPC分类号： C07K1/00
CPC分类号： C07K7/08 , A61K38/00 , C07K1/113 , C07K1/1136 , C07K7/64 , C07K14/001 , C07K14/435 , C07K14/4747
摘要： Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.
摘要翻译：本文描述了新颖的多肽及其制备和使用方法。多肽包括交联（“烃装订”）部分以提供限制多肽二级结构的两个氨基酸部分之间的系链。本文所述的多肽可用于治疗以过度或不充分的细胞死亡为特征的疾病。

5. 发明申请

US20130035304A1 SMALL MOLECULES FOR THE MODULATION OF MCL-1 AND METHODS OF MODULATING CELL DEATH, CELL DIVISION, CELL DIFFERENTIATION AND METHODS OF TREATING DISORDERS 审中-公开
公开(公告)号：US20130035304A1
公开(公告)日：2013-02-07
申请号：US13576116
申请日：2011-01-31
申请人： Loren D. Walensky , Michelle L. Stewart , Nicole Cohen
发明人： Loren D. Walensky , Michelle L. Stewart , Nicole Cohen
IPC分类号： A61K31/7034 , C07D311/30 , A61K31/352 , A61P35/00 , C07C255/42 , A61K31/26 , C07D407/04 , A61K31/351 , C07J43/00 , A61K31/58 , C07D493/04 , A61K31/366 , C07C321/30 , A61K31/10 , C07C39/16 , A61K31/055 , C07H15/203 , C07D405/14 , A61K31/498 , A61K31/53 , C07D409/12 , A61K31/5415 , C07D279/06 , A61K31/54 , C07D409/14 , A61K31/55 , C12N5/071
CPC分类号： C07D513/04 , C07C251/20 , C07C251/84 , C07C311/20 , C07C335/16 , C07C337/08 , C07C2602/10 , C07D239/60 , C07D249/12 , C07D277/34 , C07D279/06 , C07D307/54 , C07D327/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14
摘要： This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.

6. 发明授权

US08198405B2 Stabilized alpha helical peptides and uses thereof 有权
标题翻译：稳定的α螺旋肽及其用途
公开(公告)号：US08198405B2
公开(公告)日：2012-06-12
申请号：US12182673
申请日：2008-07-30
申请人： Loren D. Walensky , Stanley J. Korsmeyer , Susan Korsmeyer, legal representative , Gregory Verdine
发明人： Loren D. Walensky , Stanley J. Korsmeyer , Gregory Verdine
IPC分类号： C07K14/00
CPC分类号： C07K7/08 , A61K38/00 , C07K1/113 , C07K1/1136 , C07K7/64 , C07K14/001 , C07K14/435 , C07K14/4747
摘要： Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.
摘要翻译：本文描述了新颖的多肽及其制备和使用方法。多肽包括交联（“烃装订”）部分以提供限制多肽二级结构的两个氨基酸部分之间的系链。本文所述的多肽可用于治疗以过度或不充分的细胞死亡为特征的疾病。

7. 发明授权

US09296805B2 Stabilized insulinotropic peptides and methods of use 有权
标题翻译：稳定的促胰岛素肽及其使用方法
公开(公告)号：US09296805B2
公开(公告)日：2016-03-29
申请号：US13809259
申请日：2011-07-08
申请人： Loren D. Walensky , Gregory Bird
发明人： Loren D. Walensky , Gregory Bird
IPC分类号： C07K14/575 , C07K14/62 , A61K38/22 , A61K38/26 , A61P3/10 , C07K14/605 , A61K38/00
CPC分类号： C07K14/605 , A61K38/00 , C07K14/575 , C07K14/57563
摘要： The present invention provides stably cross-linked insulionotropic polypeptides having superior and unexpected benefits in the treatment of conditions involving abnormal glucose homeostasis, e.g., type 2 diabetes and conditions relating to type 2 diabetes. Such benefits include, but are not limited to, extended polypeptide half-life, enhanced alpha-helicity, improved thermal stability and protease resistance, increased functional activity and pharmacologic properties, improved bioavailability when administered by any route, and improved bioavailability and gastrointestinal absorption when delivered orally, as compared to the corresponding unmodified polypeptides. The invention also provides compositions for administering the polypeptides of the invention, as well as methods for preparing and evaluating the polypeptides of the invention.
摘要翻译：本发明提供了在治疗涉及异常葡萄糖体内平衡的病症（例如2型糖尿病和与2型糖尿病有关的病症）方面具有优异和意想不到的益处的稳定的交联的富含丝氨酸的多肽。这些益处包括但不限于扩展的多肽半衰期，增强的α-螺旋性，改善的热稳定性和蛋白酶抗性，增加的功能活性和药理学性质，通过任何途径施用时提高的生物利用度，以及改善的生物利用度和胃肠道吸收与相应的未修饰多肽相比，口服递送。本发明还提供了用于施用本发明多肽的组合物，以及制备和评价本发明多肽的方法。

8. 发明授权

US08921323B2 Methods and compositions for modulating BCL-2 family polypeptides 有权
标题翻译：用于调节BCL-2家族多肽的方法和组合物
公开(公告)号：US08921323B2
公开(公告)日：2014-12-30
申请号：US12680098
申请日：2008-09-26
申请人： Loren D. Walensky , Nico Tjandra , Evripidis Gavathiotis , Motoshi Suzuki , Gregory Bird
发明人： Loren D. Walensky , Nico Tjandra , Evripidis Gavathiotis , Motoshi Suzuki , Gregory Bird
IPC分类号： A61K38/00 , C07K14/00 , G01N33/50 , C07K14/47
CPC分类号： G01N33/5079 , C07K14/4747 , G01N33/5011 , G01N33/5035 , G01N2510/00
摘要： The present invention is based, at least in part, on the identification of a novel active site on BCL-2 family polypeptide such as BAX, which when bound by a compound, modifies the activity of the BCL-2 family polypeptide.
摘要翻译：本发明至少部分地基于BCL-2家族多肽如BAX上的新活性位点的鉴定，当被化合物结合时，其修饰BCL-2家族多肽的活性。

9. 发明申请

US20120082636A1 STABILIZED ALPHA HELICAL PEPTIDES AND USES THEREOF 有权
标题翻译：稳定的ALPHA HELICAL PEPTIDES及其用途
公开(公告)号：US20120082636A1
公开(公告)日：2012-04-05
申请号：US13252751
申请日：2011-10-04
申请人： Loren D. Walensky , Stanley J. Korsmeyer , Susan Korsmeyer , Gregory Verdine
发明人： Loren D. Walensky , Stanley J. Korsmeyer , Susan Korsmeyer , Gregory Verdine
IPC分类号： A61K31/787 , A61P35/02 , A61P11/06 , A61P29/00 , A61P19/02 , A61P1/00 , A61P25/00 , A61P3/10 , A61P9/10 , A61P9/00 , A61P9/04 , A61P9/12 , A61P13/12 , A61P3/06 , A61P35/00
CPC分类号： C07K7/08 , A61K38/00 , C07K1/113 , C07K1/1136 , C07K7/64 , C07K14/001 , C07K14/435 , C07K14/4747
摘要： Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.
摘要翻译：本文描述了新颖的多肽及其制备和使用方法。多肽包括交联（“烃装订”）部分以提供限制多肽二级结构的两个氨基酸部分之间的系链。本文所述的多肽可用于治疗以过度或不充分的细胞死亡为特征的疾病。

10. 发明申请

US20100286057A1 METHODS AND COMPOSITIONS FOR MODULATING BCL-2 FAMILY POLYPEPTIDES 有权
标题翻译：调节BCL-2家族多肽的方法和组合物
公开(公告)号：US20100286057A1
公开(公告)日：2010-11-11
申请号：US12680098
申请日：2008-09-26
申请人： Loren D. Walensky , Nico Tjandra , Evripidis Gavathiotis , Motoshi Suzuki , Gregory H. Bird
发明人： Loren D. Walensky , Nico Tjandra , Evripidis Gavathiotis , Motoshi Suzuki , Gregory H. Bird
IPC分类号： A61P43/00 , G01N33/53 , A61K38/16 , C07K14/435
CPC分类号： G01N33/5079 , C07K14/4747 , G01N33/5011 , G01N33/5035 , G01N2510/00
摘要： The present invention is based, at least in part, on the identification of a novel active site on BCL-2 family polypeptide such as BAX, which when bound by a compound, modifies the activity of the BCL-2 family polypeptide.
摘要翻译：本发明至少部分地基于BCL-2家族多肽如BAX上的新活性位点的鉴定，当被化合物结合时，其修饰BCL-2家族多肽的活性。

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