公开(公告)号：WO2011112558A2

公开(公告)日：2011-09-15

申请号：PCT/US2011/027511

申请日：2011-03-08

Applicant: ABBOTT LABORATORIES ,  ENANTA PHARMACEUTICALS INC. ,  LIEPOLD, Bernd ,  ROSENBLATT, Karin ,  HÖLIG, Peter ,  GOKHALE, Rajeev ,  PRASAD, Leena ,  MILLER, Jonathan ,  SCHMITT, Eric, A. ,  MORRIS, John, B.

Inventor： LIEPOLD, Bernd ,  ROSENBLATT, Karin ,  HÖLIG, Peter ,  GOKHALE, Rajeev ,  PRASAD, Leena ,  MILLER, Jonathan ,  SCHMITT, Eric, A. ,  MORRIS, John, B.

CPC classification number: A61K9/10 ,  A61K9/146 ,  A61K9/1635 ,  A61K9/1694 ,  A61K9/2027 ,  A61K31/497 ,  A61K2300/00

Abstract: The present invention features solid compositions comprising amorphous Compound I. A solid dispersion of the present invention also contains a pharmaceutically acceptable hydrophilic polymer and a pharmaceutically acceptable surfactant. Compound I may be formulated in an amorphous solid dispersion which comprises a pharmaceutically acceptable hydrophilic polymer and preferably a pharmaceutically acceptable surfactant.

Abstract translation: 本发明的特征在于包含无定形化合物I的固体组合物。本发明的固体分散体还含有药学上可接受的亲水性聚合物和可药用的表面活性剂。 化合物I可以配制成包含药学上可接受的亲水性聚合物和优选药学上可接受的表面活性剂的无定形固体分散体。

公开(公告)号：WO2011156578A1

公开(公告)日：2011-12-15

申请号：PCT/US2011/039769

申请日：2011-06-09

Applicant: ABBOTT LABORATORIES ,  LIEPOLD, Bernd ,  JUNG, Tina ,  HOLIG, Peter ,  SCHROEDER, Rudolf ,  SEVER, Nancy E. ,  LAFOUNTAINE, Justin ,  SINCLAIR, Brent D. ,  GAO, Yi ,  WU, Jianwei ,  ERICKSON, Bryan K. ,  KULLMANN, Simon ,  WESTEDT, Ulrich ,  PAULI, Mirko ,  HEITERMANN, Tanja ,  KOENIG, Renato ,  THIEL, Madlen

Inventor： LIEPOLD, Bernd ,  JUNG, Tina ,  HOLIG, Peter ,  SCHROEDER, Rudolf ,  SEVER, Nancy E. ,  LAFOUNTAINE, Justin ,  SINCLAIR, Brent D. ,  GAO, Yi ,  WU, Jianwei ,  ERICKSON, Bryan K. ,  KULLMANN, Simon ,  WESTEDT, Ulrich ,  PAULI, Mirko ,  HEITERMANN, Tanja ,  KOENIG, Renato ,  THIEL, Madlen

IPC: A61K9/14 ,  A61K9/16 ,  A61K9/20 ,  A61K31/00

CPC classification number: A61K31/4025 ,  A61K9/146 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/1694 ,  A61K9/2027 ,  A61K9/2054 ,  A61K31/00

Abstract: The present invention features solid compositions comprising Compound I A , I B , I C or I D , or a pharmaceutically acceptable salt thereof, in an amorphous form. In one embodiment, Compound I A , I B , I C or I D , or a pharmaceutically acceptable salt thereof, is formulated in an amorphous solid dispersion which comprises a pharmaceutically acceptable hydrophilic polymer and preferably a pharmaceutically acceptable surfactant.

Abstract translation: 本发明的特征在于包含无定形形式的包含化合物1A，IB，IC或ID的固体组合物或其药学上可接受的盐。 在一个实施方案中，将化合物1A，IB，IC或ID或其药学上可接受的盐配制在包含药学上可接受的亲水性聚合物，优选药学上可接受的表面活性剂的无定形固体分散体中。

公开(公告)号：WO2008067164A2

公开(公告)日：2008-06-05

申请号：PCT/US2007/084617

申请日：2007-11-14

Applicant: ABBOTT LABORATORIES ,  BERNDL, Gunther ,  ROSENBERG, Joerg ,  FASTNACHT, Katja ,  LIEPOLD, Bernd ,  BREITENBACH, Joerg ,  JUNG, Tina ,  ROTH, Wolfgang ,  MORRIS, John ,  KLEIN, Cheri, E. ,  CAI, Yan ,  ALANI, Laman ,  GHOSH, Soumojeet

Inventor： BERNDL, Gunther ,  ROSENBERG, Joerg ,  FASTNACHT, Katja ,  LIEPOLD, Bernd ,  BREITENBACH, Joerg ,  JUNG, Tina ,  ROTH, Wolfgang ,  MORRIS, John ,  KLEIN, Cheri, E. ,  CAI, Yan ,  ALANI, Laman ,  GHOSH, Soumojeet

IPC: A61K9/20 ,  A61K31/427

CPC classification number: A61K31/427 ,  A61K9/146 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2077 ,  A61K9/2095

Abstract: The present invention features solid pharmaceutical dosage formulations comprising ritonavir. As a non-limiting example, a dosage form of the present invention comprises a solid dispersion or solid solution of ritonavir in a matrix, where the matrix comprises at least one water-soluble polymer, such as copovidone, and at least one surfactant, such as polyoxyl 40 hydrogenated castor oil or macrogolglycerol hydroxystearate. Preferably, the solid dispersion or solution does not include, or includes only an insignificant amount of, PEG.

Abstract translation: 本发明的特征在于包含利托那韦的固体药物剂型。 作为非限制性实例，本发明的剂型包含利托那韦在基质中的固体分散体或固体溶液，其中基质包含至少一种水溶性聚合物如共聚维酮，和至少一种表面活性剂，例如 作为聚氧乙烯40氢化蓖麻油或聚乙二醇羟基硬脂酸酯。 优选地，固体分散体或溶液不包括或仅包含不显着量的PEG。

公开(公告)号：WO2006091529A2

公开(公告)日：2006-08-31

申请号：PCT/US2006/005944

申请日：2006-02-21

Applicant: ABBOTT LABORATORIES ,  ROSENBERG, Jöerg ,  REINHOLD, Ulrich ,  LIEPOLD, Bernd ,  BERNDL, Gunther ,  BREITENBACH, Jörg ,  ALANI, Laman ,  GHOSH, Soumojeet

Inventor： ROSENBERG, Jöerg ,  REINHOLD, Ulrich ,  LIEPOLD, Bernd ,  BERNDL, Gunther ,  BREITENBACH, Jörg ,  ALANI, Laman ,  GHOSH, Soumojeet

IPC: A61K31/513 ,  A61K31/426 ,  A61K9/20 ,  A61K9/28

CPC classification number: A61K9/1694 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/204 ,  A61K9/2077 ,  A61K9/2095 ,  A61K9/2866 ,  A61K31/00 ,  A61K31/426 ,  A61K31/427 ,  A61K31/513 ,  A61K47/32 ,  A61K2300/00

Abstract: The present invention provides a pharmaceutical dosage formulation, and more particularly, to a pharmaceutical dosage formulation comprising an HIV protease inhibitor.

Abstract translation: 本发明提供药物剂型制剂，更具体地说，涉及包含HIV蛋白酶抑制剂的药物剂型。

公开(公告)号：WO2011042420A1

公开(公告)日：2011-04-14

申请号：PCT/EP2010/064804

申请日：2010-10-05

Applicant: ABBOTT GMBH & CO. KG ,  ABBOTT LABORATORIES ,  BREITENBACH, Jörg ,  LIEPOLD, Bernd ,  LEFEBVRE, Didier ,  BOSSMANN, Steffen ,  STEITZ, Benedikt ,  HÖLIG, Peter

Inventor： BREITENBACH, Jörg ,  LIEPOLD, Bernd ,  LEFEBVRE, Didier ,  BOSSMANN, Steffen ,  STEITZ, Benedikt ,  HÖLIG, Peter

IPC: A61K9/20 ,  A61K31/216

CPC classification number: A61K31/216 ,  A61K9/0024 ,  A61K9/146

Abstract: A delivery system for sustained release of a calcium-channel blocking agent is adapted for introduction in the cerebrospinal fluid of a subject. The delivery system comprises a solid dispersion product of a calcium-channel blocking agent in a mixture of a (i) first poly(lactide-co-glycolide) having a molecular weight distribution centered around a first number average molecular weight Mn1 and a (ii) second poly(lactide-co- glycolide) having a molecular weight distribution centered around a second number average molecular weight Mn2, wherein Mn1 is in the range of from 2000 to 3000 g/mol and the ratio of Mn1/Mn2 is from 1.8 to 3.5. The delivery system is deposited in the vicinity of or adjacent to a blood vessel showing vasospasm or suspected of developing vasospasm.

Abstract translation: 用于钙通道阻断剂持续释放的递送系统适于引入受试者的脑脊液中。 递送系统包括钙通道阻断剂在（i）第一聚（丙交酯 - 共 - 乙交酯）的混合物中的固体分散产物，其分子量分布围绕第一数均分子量Mn1和（ii ）第二聚（丙交酯 - 共 - 乙交酯），其分子量分布以第二数均分子量Mn2为中心，其中Mn1为2000-3000g / mol，Mn1 / Mn2的比为1.8〜 3.5。 输送系统沉积在显示血管痉挛或怀疑发生血管痉挛的血管附近或邻近。

公开(公告)号：WO2005039551A2

公开(公告)日：2005-05-06

申请号：PCT/US2004/027401

申请日：2004-08-23

Applicant: ABBOTT LABORATORIES ,  ROSENBERG, Jöerg ,  REINHOLD, Ulrich ,  LIEPOLD, Bernd ,  DERNDL, Gunther ,  BREITENBACH, Jörg ,  ALANI, Laman ,  GHOSH, Soumojeet

Inventor： ROSENBERG, Jöerg ,  REINHOLD, Ulrich ,  LIEPOLD, Bernd ,  DERNDL, Gunther ,  BREITENBACH, Jörg ,  ALANI, Laman ,  GHOSH, Soumojeet

IPC: A61K31/00

CPC classification number: A61K31/425 ,  A61K9/146 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2866

Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50 °C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.

Abstract translation: 公开了提供改善的口服生物利用度的固体药物剂型，用于HIV蛋白酶的抑制剂。 特别地，剂型包含至少一种HIV蛋白酶抑制剂和至少一种药学上可接受的水溶性聚合物和至少一种药学上可接受的表面活性剂的固体分散体，所述药学上可接受的水溶性聚合物的Tg至少为约50 C。 优选地，药学上可接受的表面活性剂具有约4至约10的HLB值。

公开(公告)号：EP2544689A2

公开(公告)日：2013-01-16

申请号：EP11753907.2

申请日：2011-03-08

Applicant: Abbott Laboratories

Inventor： LIEPOLD, Bernd ,  ROSENBLATT, Karin ,  HÖLIG, Peter ,  GOKHALE, Rajeev ,  PRASAD, Leena ,  MILLER, Jonathan ,  SCHMITT, Eric, A. ,  MORRIS, John, B.

IPC: A61K31/4965 ,  A61K31/498 ,  A61K31/395 ,  A61K9/20 ,  A61K47/30 ,  A61P31/14

CPC classification number: A61K9/10 ,  A61K9/146 ,  A61K9/1635 ,  A61K9/1694 ,  A61K9/2027 ,  A61K31/497 ,  A61K2300/00

Abstract: The present invention features solid compositions comprising amorphous Compound I. A solid dispersion of the present invention also contains a pharmaceutically acceptable hydrophilic polymer and a pharmaceutically acceptable surfactant. Compound I may be formulated in an amorphous solid dispersion which comprises a pharmaceutically acceptable hydrophilic polymer and preferably a pharmaceutically acceptable surfactant.

Abstract translation: 本发明的特征在于包含无定形化合物I的固体组合物。 化合物I可以配制成无定形固体分散体，其包含药学上可接受的亲水聚合物并优选药学上可接受的表面活性剂

公开(公告)号：EP2112925A2

公开(公告)日：2009-11-04

申请号：EP07871461.5

申请日：2007-11-14

Applicant: Abbott Laboratories

Inventor： BERNDL, Gunther ,  ROSENBERG, Joerg ,  FASTNACHT, Katja ,  LIEPOLD, Bernd ,  BREITENBACH, Joerg ,  JUNG, Tina ,  ROTH, Wolfgang ,  MORRIS, John ,  KLEIN, Cheri E. ,  CAI, Yan ,  ALANI, Laman ,  GHOSH, Soumojeet

IPC: A61K9/28 ,  A01N43/54 ,  A01N43/78

CPC classification number: A61K31/427 ,  A61K9/146 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2077 ,  A61K9/2095

Abstract: The present invention features solid pharmaceutical dosage formulations comprising ritonavir. As a non-limiting example, a dosage form of the present invention comprises a solid dispersion or solid solution of ritonavir in a matrix, where the matrix comprises at least one water-soluble polymer, such as copovidone, and at least one surfactant, such as polyoxyl 40 hydrogenated castor oil or macrogolglycerol hydroxystearate. Preferably, the solid dispersion or solution does not include, or includes only an insignificant amount of, PEG.

公开(公告)号：EP1663183B1

公开(公告)日：2011-07-13

申请号：EP04816820.7

申请日：2004-08-23

Applicant: ABBOTT LABORATORIES

Inventor： ROSENBERG, Jöerg ,  REINHOLD, Ulrich ,  LIEPOLD, Bernd ,  DERNDL, Gunther ,  BREITENBACH, Jörg ,  ALANI, Laman ,  GHOSH, Soumojeet

IPC: A61K9/14 ,  A61K31/425 ,  A61K9/20

CPC classification number: A61K31/425 ,  A61K9/146 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2866

Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50 °C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.

公开(公告)号：EP1663183B9

公开(公告)日：2012-06-13

申请号：EP04816820.7

申请日：2004-08-23

Applicant: ABBOTT LABORATORIES

Inventor： ROSENBERG, Jöerg ,  REINHOLD, Ulrich ,  LIEPOLD, Bernd ,  DERNDL, Gunther ,  BREITENBACH, Jörg ,  ALANI, Laman ,  GHOSH, Soumojeet

IPC: A61K9/14 ,  A61K31/425 ,  A61K9/20

CPC classification number: A61K31/425 ,  A61K9/146 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2866

Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50 °C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.