公开(公告)号：US20170217987A1

公开(公告)日：2017-08-03

申请号：US15329673

申请日：2015-07-29

申请人： LEK PHARMACEUTICALS D.D. ,  SANDOZ AG

发明人： Andreas Hotter ,  Andrea Thaler ,  Andrija Lebar ,  Biljana Jankovic ,  Klemen Naversnik ,  Uros Klancar ,  Zrinka Abramovic

IPC分类号： C07D498/14

CPC分类号： C07D498/14

摘要： The invention relates to novel hydrates of dolutegravir sodium and to processes for their preparation. Furthermore, the invention relates to a novel crystalline form of dolutegravir sodium, which is a useful intermediate for the preparation of one of the novel hydrates. In addition, the invention relates to the use of the novel hydrates for the production of pharmaceutical compositions. Finally, the invention relates to pharmaceutical compositions comprising an effective amount of the novel hydrates, to oral dosage forms comprising said pharmaceutical compositions, to a process for preparing said oral dosage forms, and to the use of said pharmaceutical compositions or dosage forms in the treatment of retroviral infections such as HIV-1 infections.

公开(公告)号：US20200163882A1

公开(公告)日：2020-05-28

申请号：US16751521

申请日：2020-01-24

申请人： Lek Pharmaceuticals d.d.

发明人： Rok Grahek ,  Andrija Lebar ,  Petra Draksler ,  Bostjan Petek ,  Jerneja Opara ,  Klemen Naversnik ,  Petra Bozic

IPC分类号： A61K9/14 ,  A61K31/4166 ,  A61K9/48 ,  A61K31/4439 ,  A61K9/20 ,  A61K31/4152 ,  A61K9/16

摘要： The present invention belongs to the field of pharmaceutical industry and relates to a solid pharmaceutical composition comprising androgen receptor antagonists, e.g. Enzalutamide or ARN-509, as well as to processes for preparing the same. The solid pharmaceutical compositions are useful in the treatment of prostate cancer.

公开(公告)号：US10189860B2

公开(公告)日：2019-01-29

申请号：US15329673

申请日：2015-07-29

申请人： LEK PHARMACEUTICALS D.D. ,  SANDOZ AG

发明人： Andreas Hotter ,  Andrea Thaler ,  Andrija Lebar ,  Biljana Jankovic ,  Klemen Naversnik ,  Uros Klancar ,  Zrinka Abramovic

IPC分类号： C07D498/14

摘要： The invention relates to novel hydrates of dolutegravir sodium and to processes for their preparation. Furthermore, the invention relates to a novel crystalline form of dolutegravir sodium, which is a useful intermediate for the preparation of one of the novel hydrates. In addition, the invention relates to the use of the novel hydrates for the production of pharmaceutical compositions. Finally, the invention relates to pharmaceutical compositions comprising an effective amount of the novel hydrates, to oral dosage forms comprising said pharmaceutical compositions, to a process for preparing said oral dosage forms, and to the use of said pharmaceutical compositions or dosage forms in the treatment of retroviral infections such as HIV-1 infections.

公开(公告)号：US20160346207A1

公开(公告)日：2016-12-01

申请号：US15114890

申请日：2015-02-04

申请人： LEK PHARMACEUTICALS D.D.

发明人： Rok Grahek ,  Andrija Lebar ,  Petra Draksler ,  Bostjan Petek ,  Jerneja Opara ,  Klemen Naversnik ,  Petra Bozic

IPC分类号： A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/4166 ,  A61K31/4439

CPC分类号： A61K9/143 ,  A61K9/1611 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/4825 ,  A61K9/485 ,  A61K31/4152 ,  A61K31/4166 ,  A61K31/4439

摘要： The present invention belongs to the field of pharmaceutical industry and relates to a solid pharmaceutical composition comprising androgen receptor antagonists, e.g. Enzalutamide or ARN-509, as well as to processes for preparing the same. The solid pharmaceutical compositions are useful in the treatment of prostate cancer.

摘要翻译： 本发明属于制药工业领域，涉及包含雄激素受体拮抗剂的固体药物组合物，例如， 恩扎拉替胺或ARN-509，以及其制备方法。 固体药物组合物可用于治疗前列腺癌。