公开(公告)号：WO2009109476A1

公开(公告)日：2009-09-11

申请号：PCT/EP2009/052097

申请日：2009-02-23

Applicant: F. HOFFMANN-LA ROCHE AG ,  FISHER, Lawrence Emerson ,  HEGDE, Shridhar ,  KUO, Jane ,  LI, Fujun ,  STEFANIDIS, Dimitrios

Inventor： FISHER, Lawrence Emerson ,  HEGDE, Shridhar ,  KUO, Jane ,  LI, Fujun ,  STEFANIDIS, Dimitrios

IPC: A61K9/107 ,  A61K31/277 ,  A61K31/423 ,  A61K9/16

CPC classification number: A61K9/1075 ,  A61K9/1688 ,  A61K31/277 ,  A61K31/423

Abstract: The present invention provides a method for preparing supersaturated aqueous solutions of micelles of compounds in which the solubility in water is less than the critical micelle concentration. The solutions can be process to prepare solid micelles which have advantageous properties for drug delivery.

Abstract translation: 本发明提供一种制备其中在水中的溶解度小于临界胶束浓度的化合物胶束的过饱和水溶液的方法。 溶液可以是制备具有药物递送有利性质的固体胶束的方法。

公开(公告)号：WO2007068615A3

公开(公告)日：2007-09-07

申请号：PCT/EP2006069262

申请日：2006-12-04

Applicant: HOFFMANN LA ROCHE ,  AHMED HASHIM A ,  ALFREDSON THOMAS VERNON ,  BIRUDARAJ KONDAMRAJ ,  BRANDL MICHAEL THOMAS ,  PHUAPRADIT WANTANEE ,  SHAH NAVNIT HARGOVINDAS ,  STEFANIDIS DIMITRIOS

Inventor： AHMED HASHIM A ,  ALFREDSON THOMAS VERNON ,  BIRUDARAJ KONDAMRAJ ,  BRANDL MICHAEL THOMAS ,  PHUAPRADIT WANTANEE ,  SHAH NAVNIT HARGOVINDAS ,  STEFANIDIS DIMITRIOS

IPC: A61K9/16 ,  A61K9/50 ,  A61K31/70

CPC classification number: A61K9/2077 ,  A61K9/14 ,  A61K9/1641 ,  A61K9/2027 ,  A61K9/2095 ,  A61K9/2866 ,  A61K9/2893 ,  A61K31/655 ,  A61K31/70

Abstract: The present invention relates to a pharmaceutical composition comprising a solid suspension prepared by hot melt extrusion of isobutyric acid (2R,3S,4R,5R)-5-(4-amino- 2-oxo-2H-pyrimidin-1-yl)-2-azido-3,4-bis-iso-butyryloxy-tetrahydro-furan-2-ylmethyl ester; hydrochloride salt (I) and a polyethylene glycol (PEG)/polypropylene glycol (PPG) block copolymer.

Abstract translation: 本发明涉及药物组合物，其包含通过热熔挤出异丁酸（2R，3S，4R，5R）-5-（4-氨基-2-氧代-2H-嘧啶-1-基） - 2-叠氮基-3,4-双 - 异丁酰氧基 - 四氢 - 呋喃-2-基甲酯; 盐酸盐（I）和聚乙二醇（PEG）/聚丙二醇（PPG）嵌段共聚物。

公开(公告)号：WO2008119659A3

公开(公告)日：2009-03-05

申请号：PCT/EP2008053202

申请日：2008-03-18

Applicant: HOFFMANN LA ROCHE ,  BIRUDARAJ KONDAMRAJ ,  BRANDL MICHAEL THOMAS ,  HEGDE SHRIDAR ,  SANA FELIX ,  STEFANIDIS DIMITRIOS

Inventor： BIRUDARAJ KONDAMRAJ ,  BRANDL MICHAEL THOMAS ,  HEGDE SHRIDAR ,  SANA FELIX ,  STEFANIDIS DIMITRIOS

IPC: A61K9/20 ,  A61K9/16

CPC classification number: A61K9/2031 ,  A61K9/1641 ,  A61K9/2054

Abstract: The present invention relates to a method of forming granules of (2R,3S,4R,5R)-5-(4-amino-2-oxo-2 H -pyrimidin-1-yl)-2-azido-3,4-bis -iso-butyryloxy-tetrahydro-furan-2-ylmethyl isobutyrate; hydrochloride salt (I), comprising mixing I, with a granulating amount of a granulating liquid, and a polyethylene glycol (PEG)/polypropylene glycol (PPG) block copolymer as a binder and solubility enhancer to form wet granules which are then dried to remove the granulating liquid.

Abstract translation: 本发明涉及形成（2R，3S，4R，5R）-5-（4-氨基-2-氧代-2H-嘧啶-1-基）-2-叠氮基-3,4- 双异丁酰氧基 - 四氢呋喃-2-基甲基异丁酸酯; 盐酸盐（I），其包括将I与造粒量的造粒液和聚乙二醇（PEG）/聚丙二醇（PPG）嵌段共聚物作为粘合剂和溶解度增强剂混合以形成湿颗粒，然后将其干燥除去 制粒液。

公开(公告)号：WO2008119659A2

公开(公告)日：2008-10-09

申请号：PCT/EP2008/053202

申请日：2008-03-18

Applicant: F. HOFFMANN-LA ROCHE AG ,  BIRUDARAJ, Kondamraj ,  BRANDL, Michael Thomas ,  HEGDE, Shridar ,  SANA, Felix ,  STEFANIDIS, Dimitrios

Inventor： BIRUDARAJ, Kondamraj ,  BRANDL, Michael Thomas ,  HEGDE, Shridar ,  SANA, Felix ,  STEFANIDIS, Dimitrios

IPC: A61K9/20 ,  A61K9/16

CPC classification number: A61K9/2031 ,  A61K9/1641 ,  A61K9/2054

Abstract: The present invention relates to a method of forming granules of (2R,3S,4R,5R)-5-(4-amino-2-oxo-2 H -pyrimidin-1-yl)-2-azido-3,4- bis - iso -butyryloxy-tetrahydro-furan-2-ylmethyl isobutyrate; hydrochloride salt (I), comprising mixing I, with a granulating amount of a granulating liquid, and a polyethylene glycol (PEG)/polypropylene glycol (PPG) block copolymer as a binder and solubility enhancer to form wet granules which are then dried to remove the granulating liquid.

Abstract translation: 本发明涉及形成（2R，3S，4R，5R）-5-（4-氨基-2-氧代-2H-嘧啶-1-基）-2-叠氮基-3,4- 双异丁酰氧基 - 四氢呋喃-2-基甲基异丁酸酯; 盐酸盐（I），其包括将I与造粒量的造粒液和聚乙二醇（PEG）/聚丙二醇（PPG）嵌段共聚物作为粘合剂和溶解度增强剂混合以形成湿颗粒，然后将其干燥除去 制粒液。

公开(公告)号：WO2007068615A2

公开(公告)日：2007-06-21

申请号：PCT/EP2006/069262

申请日：2006-12-04

Applicant: F. HOFFMANN-LA ROCHE AG ,  AHMED, Hashim A. ,  ALFREDSON, Thomas Vernon ,  BIRUDARAJ, Kondamraj ,  BRANDL, Michael Thomas ,  PHUAPRADIT, Wantanee ,  SHAH, Navnit Hargovindas ,  STEFANIDIS, Dimitrios

Inventor： AHMED, Hashim A. ,  ALFREDSON, Thomas Vernon ,  BIRUDARAJ, Kondamraj ,  BRANDL, Michael Thomas ,  PHUAPRADIT, Wantanee ,  SHAH, Navnit Hargovindas ,  STEFANIDIS, Dimitrios

IPC: A61K9/20 ,  A61K9/50 ,  A61K31/70

CPC classification number: A61K9/2077 ,  A61K9/14 ,  A61K9/1641 ,  A61K9/2027 ,  A61K9/2095 ,  A61K9/2866 ,  A61K9/2893 ,  A61K31/655 ,  A61K31/70

Abstract: The present invention relates to a pharmaceutical composition comprising a solid suspension prepared by hot melt extrusion of isobutyric acid (2R,3S,4R,5R)-5-(4-amino- 2-oxo-2 H -pyrimidin-1-yl)-2-azido-3,4- bis -iso-butyryloxy-tetrahydro-furan-2-ylmethyl ester; hydrochloride salt (I) and a polyethylene glycol (PEG)/polypropylene glycol (PPG) block copolymer.

Abstract translation: 本发明涉及药物组合物，其包含通过热熔挤出异丁酸（2R，3S，4R，5R）-5-（4-氨基-2-氧代-2 H-嘧啶-1-基）-2-叠氮基-3,4-二异丁酰氧基 - 四氢 - 呋喃-2-基甲基酯; 盐酸盐（I）和聚乙二醇（PEG）/聚丙二醇（PPG）嵌段共聚物。

公开(公告)号：WO2006010545A1

公开(公告)日：2006-02-02

申请号：PCT/EP2005/007893

申请日：2005-07-20

Applicant: F. HOFFMANN-LA ROCHE AG ,  DUNN, James, Patrick ,  ELWORTHY, Todd, Richard ,  STEFANIDIS, Dimitrios ,  SWEENEY, Zachary, Kevin

Inventor： DUNN, James, Patrick ,  ELWORTHY, Todd, Richard ,  STEFANIDIS, Dimitrios ,  SWEENEY, Zachary, Kevin

IPC: C07D249/12

CPC classification number: C07D249/12

Abstract: The present invention relates to a compounds according to formula (I), methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula (I) and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula where R 1 , R 2 , R 3 , R 4 , R 5 , are as defined herein.

Abstract translation: 本发明涉及式（I）化合物，通过给予根据式（I）的化合物治疗由人免疫缺陷病毒介导的疾病的方法和用于治疗由含有根据本发明的化合物的化合物的人类免疫缺陷病毒介导的疾病的药物组合物 公式其中R

公开(公告)号：WO2005090317A1

公开(公告)日：2005-09-29

申请号：PCT/EP2005/002779

申请日：2005-03-16

Applicant: F.HOFFMANN-LA ROCHE AG ,  DUNN, James, Patrick ,  ELWORTHY, Todd, Richard ,  HOGG, Joan, Heather ,  STEFANIDIS, Dimitrios

Inventor： DUNN, James, Patrick ,  ELWORTHY, Todd, Richard ,  HOGG, Joan, Heather ,  STEFANIDIS, Dimitrios

IPC: C07D237/14

CPC classification number: C07D237/14 ,  Y10S514/85

Abstract: The present invention relates to a compounds according to formula (I), methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula (I) and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula (I) where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein.

Abstract translation: 本发明涉及式（I）化合物，通过给予根据式（I）的化合物治疗由人免疫缺陷病毒介导的疾病的方法和用于治疗由含有根据本发明的化合物的化合物的人类免疫缺陷病毒介导的疾病的药物组合物 式（I）其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义。