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17 条记录 (耗时 0.032 秒)

    Cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs
    2.
    发明授权
    Cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs 有权
    1,3-丙烷-1-芳基二醇的环磷酸二酯及其在制备前药中的用途

    公开(公告)号：US07498320B2

    公开(公告)日：2009-03-03

    申请号：US11528283

    申请日：2006-09-28

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

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

    IPC分类号： A61K31/665 ,  C07F9/02

    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。

    Process for preparation of cyclic prodrugs of PMEA and PMPA
    4.
    发明授权
    Process for preparation of cyclic prodrugs of PMEA and PMPA 有权
    制备PMEA和PMPA的环状前药的方法

    公开(公告)号：US07193081B2

    公开(公告)日：2007-03-20

    申请号：US10436799

    申请日：2003-05-12

    申请人： Joseph J. Kopcho ,  K. Raja Reddy ,  Michael C. Matelich ,  Bheemarao G. Ugarkar

    发明人： Joseph J. Kopcho ,  K. Raja Reddy ,  Michael C. Matelich ,  Bheemarao G. Ugarkar

    IPC分类号： C07F9/6574

    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。

    Orally active adenosine kinase inhibitors
    10.
    发明授权
    Orally active adenosine kinase inhibitors 失效
    口服活性腺苷激酶抑制剂

    公开(公告)号：US5763597A

    公开(公告)日：1998-06-09

    申请号：US660506

    申请日：1996-06-07

    申请人： Bheemarao G. Ugarkar ,  Mark D. Erion ,  Jorge E. Gomez Galeno ,  Angelo J. Castellino ,  Clinton E. Browne

    发明人： Bheemarao G. Ugarkar ,  Mark D. Erion ,  Jorge E. Gomez Galeno ,  Angelo J. Castellino ,  Clinton E. Browne

    IPC分类号： C07H19/14 ,  C07H19/16

    CPC分类号： C07H19/14

    摘要： This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to orally active, substituted 5-aryl pyrrolo�2,3-d! pyrimidine and 3-aryl pyrazolo�3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention also relates to the preparation and use of these and other adenosine kinase inhibitors in the treatment of cardiovascular and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.

    摘要翻译： 本发明涉及腺苷激酶抑制剂和核苷类似物，特别是具有作为腺苷激酶活性的口服活性的取代的5-芳基吡咯并[2,3-d]嘧啶和3-芳基吡唑并[3,4-d]嘧啶核苷类似物 抑制剂。 本发明还涉及这些和其它腺苷激酶抑制剂在治疗心血管和脑血管疾病，炎症等疾病中的制备和应用，可以通过增加腺苷的局部浓度来调节。