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1. 发明申请

WO2009012039A3 CRYSTALLINE POLYMORPHS 审中-公开
标题翻译：晶体多晶体
公开(公告)号：WO2009012039A3
公开(公告)日：2009-03-19
申请号：PCT/US2008068558
申请日：2008-06-27
申请人： METABASIS THERAPEUTICS INC , KOPCHO JOSEPH J , HECKER SCOTT J , FRECH PATRICIA , DEASON MIKE , DANG QUN , GUSHURST KAREN , YANG DONGLAI
发明人： KOPCHO JOSEPH J , HECKER SCOTT J , FRECH PATRICIA , DEASON MIKE , DANG QUN , GUSHURST KAREN , YANG DONGLAI
IPC分类号： C07C213/00 , C07C213/10 , C07C217/00 , C07C217/60
CPC分类号： C07F9/65586
摘要： The present invention provides for crystalline forms of 2-amino-5-(2,2- dimethylpropionyl)-4-{[5-(N,N'-(2-ethoxycarbonylprop-2-yl)phosphonamido] furan-2-yl}thiazole and compositions thereof including pharmaceutical compositions. The present invention further provides for methods of using and processes for making the same.
摘要翻译：本发明提供2-氨基-5-（2,2-二甲基丙酰基）-4 - {[5-（N，N' - （2-乙氧羰基丙-2-基）膦酰氨基]呋喃-2-基 }噻唑及其组合物，包括药物组合物，本发明进一步提供使用方法和制备方法。

2. 发明申请

WO2006023515A2 NOVEL THIAZOLE INHIBITORS OF FRUCTOSE 1,6-BISPHOSPHATASE 审中-公开
标题翻译：新型果糖1,6-二磷酸果糖酯的噻唑类抑制剂
公开(公告)号：WO2006023515A2
公开(公告)日：2006-03-02
申请号：PCT/US2005029176
申请日：2005-08-18
申请人： METABASIS THERAPEUTICS INC , DANG QUN , KOPCHO JOSEPH J , HECKER SCOTT J , UGARKAR BHEEMARAO G
发明人： DANG QUN , KOPCHO JOSEPH J , HECKER SCOTT J , UGARKAR BHEEMARAO G
CPC分类号： C07F9/65586 , C12N9/99
摘要： Compounds of Formula I, their prodrugs and salts, their preparation and their uses are described.
摘要翻译：描述了式I的化合物，它们的前药和盐，它们的制备和它们的用途。

3. 发明申请

WO2004037161A3 CYCLIC PRODRUGS OF PMEA ONE OF ITS ANALOGUES 审中-公开
标题翻译： PMEA的循环产品一种类似的方法
公开(公告)号：WO2004037161A3
公开(公告)日：2005-03-31
申请号：PCT/US0314821
申请日：2003-05-12
申请人： METABASIS THERAPEUTICS INC , REDDY K RAJA , ERION MARK D , MATELICH MICHAEL C , KOPCHO JOSEPH J
发明人： REDDY K RAJA , ERION MARK D , MATELICH MICHAEL C , KOPCHO JOSEPH J
IPC分类号： A61P1/16 , A61P31/20 , A61P35/00 , C07F9/6561 , C07F9/6574 , A61K31/375 , C07F9/6512
CPC分类号： C07F9/65742 , C07F9/65616
摘要： Prodrugs of Formula I, their uses, their intermediates, and their method of manufacture are described: (I) wherein: M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, (R)-9-(2-phosphonylmethoxy propyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, 9-(2-phosphonylmethoxy ethyloxy)adenine, 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine, (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine, 9-(3-hydroxy-2-phosphonylmethoxypropyl)guanine, and (S)-9-(3-fluoro-2-phosphonyl methoxypropyl)adenine;V is selected from a group consisting of phenyl, 2-pyridyl , 3-pyridyl, 4-pyridyl, 2-furanyl, 3-furanyl, 2-thienyl, and 3-thienyl, all optionally substituted with 1-3 substituents selected from a group consisting of F, Cl, Br, C1-C3 alkyl, CF3 and OR6;R6 is selected from the group consisting of C1-C3 alkyl, and CF3;and pharmaceutically acceptable salts thereof.
摘要翻译：描述了式I的前药，其用途及其中间体及其制备方法：（I）其中：M和V彼此是顺式的，MPO3H2是选自9-（2-膦酰基甲氧基乙基）腺嘌呤，（R）-9-（2-膦酰基甲氧基丙基）腺嘌呤，9-（2-膦酰基甲氧基乙基）鸟嘌呤，9-（2-膦酰基甲氧基乙氧基）腺嘌呤，9-（2-膦酰基甲氧基乙基）-2,6-二氨基嘌呤，（S）-1-（3-羟基-2-膦酰基甲氧基丙基）胞嘧啶，（S）-9-（3-羟基-2-膦酰基甲氧基丙基）腺嘌呤，9-（3-羟基-2-膦酰基甲氧基丙基）鸟嘌呤和（S ）-9-（3-氟-2-膦酰基甲氧基丙基）腺嘌呤; V选自苯基，2-吡啶基，3-吡啶基，4-吡啶基，2-呋喃基，3-呋喃基，2-噻吩基，和任选被1-3个选自F，Cl，Br，C 1 -C 3烷基，CF 3和OR 6的取代基取代的3-噻吩基; R 6选自C 1 -C 3烷基和CF 3; 及其药学上可接受的盐。

4. 发明专利

BRPI0514372A 未知
公开(公告)号：BRPI0514372A
公开(公告)日：2008-06-10
申请号：BRPI0514372
申请日：2005-08-18
申请人： METABASIS THERAPEUTICS INC
发明人： DANG QUN , KOPCHO JOSEPH J , HECKER SCOTT J , UGARKAR BHEEMARAO G
IPC分类号： A61K31/662 , A61P3/10 , C07F9/6558
摘要： Compounds of Formula I, their prodrugs and salts, their preparation and their uses are described.

5. 发明专利

CA2485597C PROCESS FOR PREPARATION OF CYCLIC PRODRUGS OF PMEA AND PMPA 未知
公开(公告)号：CA2485597C
公开(公告)日：2013-07-02
申请号：CA2485597
申请日：2003-05-12
申请人： METABASIS THERAPEUTICS INC
发明人： KOPCHO JOSEPH J , REDDY K RAJA , MATELICH MICHAEL C , UGARKAR BHEEMARAO G
IPC分类号： A61K31/66 , C07F9/6571 , A61K31/675 , A61P31/12 , A61P31/18 , A61P35/00 , C07F9/6574
摘要： The method of preparing compounds of Formula I is described: Formula Iwherein:M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, and (R)-9-(2-phosphonylmethoxypropyl)adenine; wherein V is phenyl, optionally substituted with 1-2 substituents selected from a group consisting of fluoro, chloro, and bromo; comprising:coupling a chiral 1-phenylpropane-1,3-diol, wherein the phenyl may be optionally substituted, with MPOCl2 or an N-6 substituted analogue thereof.Additionally, methods and salt forms are described that enable isolation and purification of the desired isomer.

6. 发明专利

CA2577373A1 NOVEL THIAZOLE INHIBITORS OF FRUCTOSE 1,6-BISPHOSPHATASE 未知
公开(公告)号：CA2577373A1
公开(公告)日：2006-03-02
申请号：CA2577373
申请日：2005-08-18
申请人： METABASIS THERAPEUTICS INC
发明人： KOPCHO JOSEPH J , DANG QUN , HECKER SCOTT J , UGARKAR BHEEMARAO G
IPC分类号： A61K31/662 , A61P3/10 , C07F9/6558
摘要： Compounds of Formula I, their prodrugs and salts, their preparation and their uses are described.

7. 发明专利

CA2485702C NOVEL PHOSPHONIC ACID BASED PRODRUGS OF PMEA AND ITS ANALOGUES 未知
公开(公告)号：CA2485702C
公开(公告)日：2011-07-19
申请号：CA2485702
申请日：2003-05-12
申请人： METABASIS THERAPEUTICS INC
发明人： REDDY K RAJA , ERION MARK D , MATELICH MICHAEL C , KOPCHO JOSEPH J
IPC分类号： C07F9/6574 , A61K31/52 , A61K31/665 , A61K31/675 , A61K31/70 , A61P1/16 , A61P31/20 , A61P35/00 , C07F9/6561
摘要： Prodrugs of Formula I, their uses, their intermediates, and their method of manufacture are described: Formula 1wherein:M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, (R)-9-(2-phosphonylmethoxy propyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, 9-(2-phosphonylmethoxy ethyloxy)adenine, 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine, (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine, 9-(3-hydroxy-2-phosphonylmethoxypropyl)guanine, and (S)-9-(3-fluoro-2-phosphonyl methoxypropyl)adenine;V is selected from a group consisting of phenyl, 2-pyridyl , 3-pyridyl, 4-pyridyl, 2-furanyl, 3-furanyl, 2-thienyl, and 3-thienyl, all optionally substituted with 1-3 substituents selected from a group consisting of F, Cl, Br, C1-C3 alkyl, CF3 and OR6;R6 is selected from the group consisting of C1-C3 alkyl, and CF3;and pharmaceutically acceptable salts thereof.

8. 发明专利

AU2003299492A1 NOVEL PHOSPHONIC ACID BASED PRODRUGS OF PMEA AND ITS ANALOGUES 未知
公开(公告)号：AU2003299492A1
公开(公告)日：2004-05-13
申请号：AU2003299492
申请日：2003-05-12
申请人： METABASIS THERAPEUTICS INC
发明人： REDDY K RAJA , ERION MARK D , MATELICH MICHAEL C , KOPCHO JOSEPH J
IPC分类号： A61P1/16 , A61P31/20 , A61P35/00 , C07F9/6561 , C07F9/6574

9. 发明专利

NZ536327A PMEA and PMPA cyclic producing synthesis 未知
公开(公告)号：NZ536327A
公开(公告)日：2007-08-31
申请号：NZ53632703
申请日：2003-05-12
申请人： METABASIS THERAPEUTICS INC
发明人： KOPCHO JOSEPH J , REDDY K RAJA , MATELICH MICHAEL C , UGARKAR BHEEMARAO G
IPC分类号： A61P31/12 , A61K31/66 , A61P31/18 , A61P35/00 , C07F9/6571 , C07F9/6574
摘要： Disclosed is a method of preparing compounds of formula I wherein M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, and (R)-9-(2-phosphonylmethoxypropyl)adenine; wherein V is phenyl, optionally substituted with 1-2 substituents selected from a group consisting of fluoro, chloro, and bromo; comprising: coupling a chiral 1-phenylpropane-1,3-diol, wherein the phenyl may be optionally substituted, with fluoro, chloro and bromo with MPOCl2 or an N-6 substituted analogue thereof. Additionally, methods and salt forms are described that enable isolation and purification of the desired isomer.

10. 发明专利

AU2003235501A1 PROCESS FOR PREPARATION OF CYCLIC PRODRUGS OF PMEA AND PMPA 未知
公开(公告)号：AU2003235501A1
公开(公告)日：2003-11-11
申请号：AU2003235501
申请日：2003-05-12
申请人： METABASIS THERAPEUTICS INC
发明人： KOPCHO JOSEPH J , REDDY K RAJA , MATELICH MICHAEL C , UGARKAR BHEEMARAO G
IPC分类号： A61K31/66 , A61P31/12 , A61P31/18 , A61P35/00 , C07F9/6571 , C07F9/6574
摘要： The method of preparing compounds of Formula I is described: wherein: M and V are cis to one another and MPO 3 H 2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, and (R)-9-(2-phosphonylmethoxypropyl)adenine; wherein V is phenyl, optionally substituted with 1-2 substituents selected from a group consisting of fluoro, chloro, and bromo; comprising: coupling a chiral 1-phenylpropane-1,3-diol, wherein the phenyl may be optionally substituted, with MPOCl 2 or an N-6 substituted analogue thereof. Additionally, methods and salt forms are described that enable isolation and purification of the desired isomer.

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