公开(公告)号：EP3568135B1

公开(公告)日：2021-04-07

申请号：EP18702014.4

申请日：2018-01-11

发明人： FULLER, Nathan, Oliver ,  LOWE, John, A., III

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/519 ,  A61P25/28

公开(公告)号：EP3233920B1

公开(公告)日：2020-08-26

申请号：EP15871152.3

申请日：2015-12-18

申请人： Alkermes, Inc.

发明人： ALVARAZ, Juan ,  MOUSTAKAS, Demetri, T. ,  BRODKIN, Heather, R. ,  MCSWEENEY, Leslie, A.

IPC分类号： C07K16/30 ,  C07K14/54 ,  C07K14/55 ,  C07K14/565 ,  C07K14/705 ,  C07K14/715 ,  C12N9/64 ,  A61K38/00

公开(公告)号：EP2858672B1

公开(公告)日：2018-04-04

申请号：EP13800676.2

申请日：2013-06-06

申请人： Alkermes, Inc.

发明人： ALVAREZ, Juan ,  MCSWEENEY, Leslie, A.

IPC分类号： C12N15/62 ,  C07K14/47

CPC分类号： C07K14/55 ,  A61K38/00 ,  A61K2039/505 ,  C07K14/4713 ,  C07K14/4727 ,  C07K14/50 ,  C07K14/54 ,  C07K14/5412 ,  C07K14/5443 ,  C07K14/545 ,  C07K14/57563 ,  C07K14/70503 ,  C07K14/71 ,  C07K14/7155 ,  C07K2319/00 ,  C07K2319/02 ,  C07K2319/30 ,  C07K2319/31 ,  C07K2319/74 ,  C07K2319/91

摘要： The present invention provides fusion polypeptides comprising polypeptide ligands that are modified by circular permutation and fused to at least one polypeptide fusion partner wherein such fusion polypeptides have new, improved or enhanced biological functions or activities. Such improvements include, but are not limited to, increased binding affinity, increased activity, increased agonist activity (super agonist), antagonist activity, increased accessibility, increased flexibility of the active site, increased stability, broader and/or changed substrate specificity, and combinations thereof.

公开(公告)号：EP2874639B1

公开(公告)日：2018-03-28

申请号：EP13799943.9

申请日：2013-06-06

申请人： Alkermes, Inc.

发明人： ALVAREZ, Juan ,  CHAMOUN, Jean ,  LOSEY, Heather, C.

IPC分类号： C12N15/62 ,  C07K14/47 ,  C07K14/575 ,  C07K14/715

CPC分类号： C07K14/55 ,  A61K38/00 ,  A61K2039/505 ,  C07K14/4713 ,  C07K14/4727 ,  C07K14/50 ,  C07K14/54 ,  C07K14/5412 ,  C07K14/5443 ,  C07K14/545 ,  C07K14/57563 ,  C07K14/70503 ,  C07K14/71 ,  C07K14/7155 ,  C07K2319/00 ,  C07K2319/02 ,  C07K2319/30 ,  C07K2319/31 ,  C07K2319/74 ,  C07K2319/91

摘要： The present invention provides fusion polypeptides comprising polypeptide ligands that are modified by circular permutation and fused to at least one polypeptide fusion partner wherein such fusion polypeptides have new, improved or enhanced biological functions or activities. Such improvements include, but are not limited to, increased binding affinity, increased activity, increased agonist activity (super agonist), antagonist activity, increased accessibility, increased flexibility of the active site, increased stability, broader and/or changed substrate specificity, and combinations thereof.

公开(公告)号：EP2725908B1

公开(公告)日：2017-05-31

申请号：EP12805087.9

申请日：2012-06-29

申请人： Alkermes, Inc.

发明人： BLUMBERG, Laura, Cook ,  ARNELLE, Derrick

IPC分类号： C07D471/08 ,  C07D489/02

CPC分类号： A61K31/513 ,  A61K31/485 ,  C07D471/08 ,  C07D489/02

公开(公告)号：EP2675276A1

公开(公告)日：2013-12-25

申请号：EP12747008.6

申请日：2012-02-14

申请人： Alkermes, Inc.

发明人： SILVERMAN, Bernard ,  TODTENKOPF, Mark ,  DEAVER, Daniel ,  DIPETRILLO, Lauren

IPC分类号： A01N43/42 ,  A61K31/44

CPC分类号： A61K31/485

摘要： The present invention relates to a novel functional peripherally-acting μ opioid receptor antagonist of Formula I: The novel compounds of the present invention have reduced oral bioavailability without compromising opiate-induced analgesia in the CNS. The compounds of the present invention are further efficacious at low doses and are useful in treating gastrointestinal conditions associated with opioid analgesic therapy.

公开(公告)号：EP2497476A1

公开(公告)日：2012-09-12

申请号：EP12165213.5

申请日：2004-07-29

申请人： Alkermes, Inc.

发明人： Greco, Kristyn ,  Wright, James

IPC分类号： A61K31/445 ,  A61K31/495 ,  C07D211/52 ,  C07D403/02 ,  A61P25/18 ,  A61K31/496

CPC分类号： C07D211/52 ,  A61K31/445

摘要： The invention relates to the discovery that pamoate salt of aripiprazole results in a good to superior long acting and/or extended release profile. Thus, in one aspect of the invention, the invention includes pamoate salt of aripiprazole. Preferably, the pamoate salt is characterized by a ratio of aripiprazole to pamoate of 1:1 or 2:1. The invention further relates to methods of treating an individual in need thereof comprising administering a pharmaceutical composition comprising a pamoate salt of aripiprazole.

摘要翻译： 本发明涉及发现阿立哌唑的双羟萘酸盐导致良好至优异的长效和/或延长释放曲线。 因此，在本发明的一个方面，本发明包括阿立哌唑的双羟萘酸盐。 优选地，双羟萘酸盐的特征在于阿立哌唑与双羟萘酸盐的比例为1：1或2：1。 本发明进一步涉及治疗有需要的个体的方法，其包括施用包含阿立哌唑的双羟萘酸盐的药物组合物。

公开(公告)号：EP1734971B1

公开(公告)日：2011-11-02

申请号：EP04750134.1

申请日：2004-04-15

申请人： Alkermes, Inc. ,  Amylin Pharmaceuticals, Inc.

发明人： WRIGHT, Steven, G. ,  CHRISTENSON, Troy ,  YEOH, Thean, Y. ,  RICKEY, Michael, E. ,  HOTZ, Joyce, M. ,  KUMAR, Rajesh ,  COSTANTINO, Henry, R. ,  SMITH, Christine ,  LOKENSGARD, David ,  ONG, John

IPC分类号： A61K31/573 ,  C07K1/00 ,  C07K7/00 ,  C07K14/00

CPC分类号： A61K47/34 ,  A61K9/0002 ,  A61K9/1647 ,  A61K9/1694 ,  A61K9/5089 ,  A61K31/573 ,  A61K38/2278 ,  A61K38/26

摘要： This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide and a sugar.

公开(公告)号：EP2340810A1

公开(公告)日：2011-07-06

申请号：EP10193459.4

申请日：2004-07-29

申请人： Alkermes, Inc.

发明人： Brown, Josiah

IPC分类号： A61K9/08 ,  A61K9/10

CPC分类号： A61K9/0019 ,  A61K9/10 ,  A61K31/496 ,  A61K47/02 ,  A61K47/26 ,  A61K47/38

摘要： The present invention relates, in part, to the discovery that a pharmaceutical composition comprising aripiprazole and a carrier administered in a bolus injection resulted in an extended release profile similar to that obtained by the injection of a polylactide-co-glycolide microsphere formulation containing the active agent. This surprising result provides pharmacologically beneficial extended release formulations without the complexities and expense associated with the manufacture of microspheres.

摘要翻译： 本发明部分地涉及包含阿立哌唑和以推注剂给药的载体的药物组合物的发现，导致延长的释放曲线类似于通过注射含有活性物质的聚丙交酯 - 共 - 乙交酯微球制剂而获得的 剂。 这个惊人的结果提供了药理学上有用的延长释放制剂，而没有与微球制造有关的复杂性和费用。

公开(公告)号：EP1531794A4

公开(公告)日：2011-03-16

申请号：EP03742233

申请日：2003-06-26

申请人： ALKERMES INC

发明人： BATYCKY RICHARD P ,  CAPONETTI GIOVANNI ,  CHILDS MARIKO ,  EHRICH ELLIOT ,  FU KAREN ,  HRKACH JEFFREY S ,  LI WEN-I ,  LIPP MICHAEL M ,  PAN MEI-LING ,  SUMMA JASON

IPC分类号： A61K9/00 ,  A61K9/12 ,  A61K9/14 ,  A61K9/16 ,  A61K31/137 ,  A61K31/19 ,  A61K31/195 ,  A61L9/04 ,  A61M20060101

CPC分类号： A61K31/137 ,  A61K9/0073 ,  A61K9/0075 ,  A61K9/1617 ,  A61K31/135 ,  A61M15/0091 ,  A61M2202/06