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    Novel cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs
    1.
    发明申请
    Novel cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs 有权
    1,3-丙烷-1-芳基二醇的新型环状磷酸二酯及其在制备前药中的用途

    公开(公告)号：US20070021388A1

    公开(公告)日：2007-01-25

    申请号：US11528283

    申请日：2006-09-28

    申请人： K. Reddy ,  William Craigo ,  Zhili Sun ,  Serge Boyer ,  Bheemarao Ugarkar

    发明人： K. Reddy ,  William Craigo ,  Zhili Sun ,  Serge Boyer ,  Bheemarao Ugarkar

    IPC分类号： A61K31/675 ,  C07F9/6512 ,  C07F9/6509

    CPC分类号： C07F9/65742 ,  C07H19/04

    摘要： Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: wherein: V and L are trans relative to one another; V is selected from group consisting of carbocyclic aryl, substituted carbocyclic aryl, heteroaryl, and substituted heteroaryl; and L is a leaving group selected from the group consisting of halogen, alkyl sulfonate, aryloxy optionally substituted with 1-2 substituents, N-containing heteroaryl, and N-hydroxy-nitrogen containing heteroaryl; and salts thereof.

    摘要翻译： 式I化合物，其制备方法和合成中间体及其在前体药物合成中的应用：其中：V和L相对于彼此是反式的; V选自碳环芳基，取代的碳环芳基，杂芳基和取代的杂芳基; 并且L是选自卤素，烷基磺酸酯，任选被1-2个取代基取代的芳氧基，含N杂芳基和N-羟基 - 含氮杂芳基的离去基团; 及其盐。

    Novel-prodrugs for phosphorus-containing compounds
    2.
    发明申请
    Novel-prodrugs for phosphorus-containing compounds 有权

    公开(公告)号：US20050288240A1

    公开(公告)日：2005-12-29

    申请号：US11145194

    申请日：2005-06-03

    申请人： Mark Erion ,  K. Reddy ,  Edward Robinson ,  Bheemarao Ugarkar

    发明人： Mark Erion ,  K. Reddy ,  Edward Robinson ,  Bheemarao Ugarkar

    IPC分类号： A61K31/7056 ,  A61K31/7072 ,  A61K31/7076 ,  C07F9/6571 ,  C07F9/6574 ,  C07H19/10 ,  C07H19/20 ,  C07H19/207

    CPC分类号： C07H19/10 ,  A61K31/7056 ,  A61K31/7072 ,  A61K31/7076 ,  C07F9/657154 ,  C07F9/657181 ,  C07F9/65742 ,  C07F9/65744 ,  C07H19/20 ,  C07H19/207 ,  Y02A50/411

    摘要： Prodrugs of formula I, their uses, their intermediates, and their method of manufacture are described: wherein: V, W, and W′ are independently selected from the group consisting of —H, alkyl, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, and 1-alkynyl; or together V and Z are connected via an additional 3-5 atoms to form a cyclic group containing 5-7 atoms, optionally 1 heteroatom, substituted with hydroxy, acyloxy, alkoxycarbonyloxy, or aryloxycarbonyloxy attached to a carbon atom that is three atoms from both O groups attached to the phosphorus; or together V and Z are connected via an additional 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 O attached to the phosphorus; together V and W are connected via an additional 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 one of said carbon atoms that is three atoms from an O attached to the phosphorus; together Z and W are connected via an additional 3-5 atoms to form a cyclic group, optionally containing one heteroatom, and V must be aryl, substituted aryl, heteroaryl, or substituted heteroaryl; together W and W′ are connected via an additional 2-5 atoms to form a cyclic group, optionally containing 0-2 heteroatoms, and V must be aryl, substituted aryl, heteroaryl, or substituted heteroaryl; Z is selected from the group consisting of —CHR2OH, —CHR2OC(O)R3, —CHR2OC(S)R3, —CHR2OC(S)OR3, —CHR2OC(O)SR3, —CHR2OCO2R3, —OR2, —SR2, —CHR2N3, —CH2aryl, —CH(aryl)OH, —CH(CH═CR22)OH, —CH(C≡CR2)OH, —R2, —NR22, —OCOR3, —OCO2R3, —SCOR3, —SCO2R3, —NHCOR2, —NHCO2R3, —CH2NHaryl, —(CH2)p—OR12, and —(CH2)p—SR12; p is an integer 2 or 3; with the provisos that: a) V, Z, W, W′ are not all —H; and b) when Z is —R2, then at least one of V, W, and W′ is not —H, alkyl, aralkyl, or alicyclic; R2 is selected from the group consisting of R3 and —H; R3 is selected from the group consisting of alkyl, aryl, alicyclic, and aralkyl; R12 is selected from the group consisting of —H, and lower acyl; M is selected from the group that attached to PO32−, P2O63−, or P3O94− is a biologically active agent, and is attached to the phosphorus in formula I via a carbon, oxygen, sulfur or nitrogen atom; and pharmaceutically acceptable prodrugs and salts thereof.

    Process for Preparation of Cyclic Prodrugs of PMEA and PMPA
    3.
    发明申请
    Process for Preparation of Cyclic Prodrugs of PMEA and PMPA 审中-公开
    制备PMEA和PMPA循环前药的方法

    公开(公告)号：US20070203339A1

    公开(公告)日：2007-08-30

    申请号：US11670806

    申请日：2007-02-02

    申请人： Joseph KOPCHO ,  K. Reddy ,  Michael Matelich ,  Bheemarao Ugarkar

    发明人： Joseph KOPCHO ,  K. Reddy ,  Michael Matelich ,  Bheemarao Ugarkar

    IPC分类号： C07F9/655 ,  C07D263/04

    CPC分类号： C07F9/657181

    摘要： The method of preparing compounds of Formula I is described: 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 MPOCl2 or an N-6 substituted analogue thereof. Additionally, methods and salt forms are described that enable isolation and purification of the desired isomer.

    摘要翻译： 描述了制备式I化合物的方法：其中：M和V彼此是顺式的，MPO 3 H 2是选自以下的膦酸： 9-（2-膦酰基甲氧基乙基）腺嘌呤和（R）-9-（2-膦酰基甲氧基丙基）腺嘌呤; 其中V是苯基，任选被1-2个选自氟，氯和溴的取代基取代; 包括：将其中苯基可以任选取代的手性1-苯基丙烷-1,3-二醇与MPOCl 2 N或其N-6取代的类似物偶联。 另外，描述了能够分离和纯化所需异构体的方法和盐形式。