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    NOVEL PRODRUGS FOR PHOSPHORUS-CONTAINING COMPOUNDS
    1.
    发明申请
    NOVEL PRODRUGS FOR PHOSPHORUS-CONTAINING COMPOUNDS 审中-公开
    含磷化合物的新产品

    公开(公告)号：WO9945016A9

    公开(公告)日：2000-03-02

    申请号：PCT/US9904908

    申请日：1999-03-05

    Applicant: METABASIS THERAPEUTICS INC

    Inventor： ERION MARK D ,  REDDY K RAJA ,  ROBINSON EDWARD D

    IPC: C07H19/213 ,  A61K31/665 ,  A61K31/675 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  A61K49/00 ,  A61P1/16 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P43/00 ,  C07F9/6571 ,  C07F9/6574 ,  C07H19/10 ,  C07H19/11 ,  C07H19/20 ,  C07H19/207 ,  C07H19/00

    CPC classification number: C07H19/10 ,  C07F9/657154 ,  C07F9/657181 ,  C07F9/65742 ,  C07F9/65744 ,  C07H19/20 ,  C07H19/207

    Abstract: Prodrugs of formula (I), their uses, their intermediates, and their method of manufacture are described, wherein V is selected from the group consisting of -H, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, 1-alkynyl, and -R ; or together V and Z are connected via 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, substituted with hydroxy, acyloxy, alkoxycarbonyloxy, or aryloxycarbonyloxy attached to a carbon atom that is three atoms from an oxygen attached to the phosphorus; or together V and Z are connected via 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, that is fused to an aryl group at the beta and gamma position to the oxygen attached to the phosphorus; or together V and W are connected via 3 carbon atoms to form an optionally substituted cyclic group containing 6 carbon atoms and substituted with one substituent selected from the group consisting of hydroxy, acyloxy, alkoxycarbonyloxy, alkylthiocarbonyloxy, and aryloxycarbonyloxy, attached to a carbon atom that is three atoms from an oxygen attached to the phosphorus; W and W' are independently selected from the group consisting of -H, alkyl, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, 1-alkynyl, and -R ; Z is selected from the group consisting of -CHR OH, -CHR OC(O)R , -CHR OC(S)R , -CHR OC(S)OR , -CHR OC(O)SR , -CHR OCO2R , -OR , -SR , -CHR N3, -CH2aryl, -CH(aryl)OH, -CH(CH=CR 2)OH, -CH(CCR )OH, -R , -NR 2, -OCOR , -OCO2R , -SCOR , -SCO2R , -NHCOR , -NHCO2R , -CH2NHaryl, -(CH2)p-OR , and -(CH2)p-SR ; R is an R or -H; R is selected from the group consisting of alkyl, aryl, aralkyl, and alicyclic; and R is selected from the group consisting of alkyl, aralkyl, and alicyclic; p is an integer from 2 to 3; with the provisos that a) V, Z, W, and W' are not all -H; and b) when z is -R , then at least one of V and W is not -H, or -R ; and M is selected from the group that attached to PO3 , P2O6 , or P3O9 is biologically active in vivo, and that is attached to the phosphorus in formula (I) via a carbon, oxygen, or nitrogen atom; and pharmaceutically acceptable prodrugs and salts thereof.

    Abstract translation: 描述了式（I）的前药，其用途，其中间体及其制备方法，其中V选自-H，芳烷基，脂环族，芳基，取代的芳基，杂芳基，取代的杂芳基，1-烯基 ，1-炔基和-R 9; 或一起V和Z通过3-5个原子连接形成环状基团，任选地含有1个被连接到磷上的氧原子连接到三个原子上的羟基，酰氧基，烷氧基羰基氧基或芳氧基羰基氧基的杂原子; 或一起V和Z通过3-5个原子连接以形成任选地含有1个杂原子的环状基团，其在β和γ位置处的芳基与连接到磷的氧融合; 或者一起V和W通过3个碳原子连接形成任选取代的含有6个碳原子的环状基团，并被一个选自羟基，酰氧基，烷氧基羰基氧基，烷硫基羰基氧基和芳氧基羰基氧基的一个取代基取代， 是从附着于磷的氧的三个原子; W和W'独立地选自-H，烷基，芳烷基，脂环族，芳基，取代的芳基，杂芳基，取代的杂芳基，1-烯基，1-炔基和-R 9。 Z选自-CHR 2 OH，-CHR 2 OC（O）R 3，-CHR 2 OC（S）R 3，-CHR 2 OC（ S）OR 3，-CHR 2 OC（O）SR 3，-CHR 2 OCO 2 R 3，-OR 2，-SR 2，-CHR 2 N 3， -CH 2芳基，-CH（芳基）OH，-CH（CH = CR 2）OH，-CH（CCR 2）OH，-R 2，-NR 2，-OCOR 3 ，-OCO 2 R 3，-SCOR 3，-SCO 2 R 3，-NHCOR 2，-NHCO 2 R 3，-CH 2 NH芳基， - （CH 2）p -OR 2和 - （CH 2 ）对 - SR <2>; R 2是R 3或-H; R 3选自烷基，芳基，芳烷基和脂环族; 并且R 9选自烷基，芳烷基和脂环族; p是2至3的整数; 条件是a）V，Z，W和W'不全为-H; 和b）当z是-R 2时，V和W中的至少一个不是-H或-R 9; 并且M选自附着于PO 3 2-，P 2 O 6 3-或P3O 9 4-的基团在体内具有生物活性，并且通过碳与式（I）中的磷连接， 氧或氮原子; 及其药学上可接受的前药及其盐。

    NOVEL PHOSPHORUS-CONTAINING PRODRUGS
    5.
    发明申请
    NOVEL PHOSPHORUS-CONTAINING PRODRUGS 审中-公开
    新型含磷原料

    公开(公告)号：WO0052015A2

    公开(公告)日：2000-09-08

    申请号：PCT/US0005672

    申请日：2000-03-03

    Applicant: METABASIS THERAPEUTICS INC

    Inventor： ERION MARK D ,  REDDY K RAJA ,  BOYER SERGE H

    IPC: C07F9/6584 ,  C07F9/02

    CPC classification number: C07F9/65846 ,  C07F9/65848

    Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula (I) of parent drugs MH their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.

    Abstract translation: 描述了母体药物的式（I）药物的新型环状氨基磷酸酯前药，其用于向肝中递送药物，其用于提高口服生物利用度及其制备方法。

    CYCLIC PRODRUGS OF PMEA ONE OF ITS ANALOGUES
    10.
    发明申请
    CYCLIC PRODRUGS OF PMEA ONE OF ITS ANALOGUES 审中-公开
    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

    Applicant: METABASIS THERAPEUTICS INC ,  REDDY K RAJA ,  ERION MARK D ,  MATELICH MICHAEL C ,  KOPCHO JOSEPH J

    Inventor： REDDY K RAJA ,  ERION MARK D ,  MATELICH MICHAEL C ,  KOPCHO JOSEPH J

    IPC: A61P1/16 ,  A61P31/20 ,  A61P35/00 ,  C07F9/6561 ,  C07F9/6574 ,  A61K31/375 ,  C07F9/6512

    CPC classification number: C07F9/65742 ,  C07F9/65616

    Abstract: 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.

    Abstract translation: 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。

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