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    • 27. 发明申请
      US20050033051A1 Nucleosides preparation thereof and use as inhibitors of rna viral polymerases 审中-公开
    • Nucleosides preparation thereof and use as inhibitors of rna viral polymerases
    • 核苷的制备及用作rna病毒聚合酶的抑制剂
    • US20050033051A1
    • 2005-02-10
    • US10496116
    • 2002-11-14
    • Yarlagadda Babu , Pooran Chand , Yahya El-Kattan , Minwan Wu
    • Yarlagadda Babu , Pooran Chand , Yahya El-Kattan , Minwan Wu
    • A61K31/13 , A61K31/575 , A61K31/66 , A61K31/662 , A61K31/663 , A61K31/704 , A61K31/7056 , A61K36/28 , A61K38/20 , A61K38/21 , A61P31/14 , A61P31/16 , A61P31/20 , A61P43/00 , C07F9/10 , C07F9/6512 , C07F9/6561 , C07F9/02
    • C07F9/65616 , A61K31/13 , A61K31/66 , A61K36/28 , A61K38/20 , A61K38/208 , A61K38/21 , A61K38/212 , C07F9/10 , C07F9/6512 , Y02A50/393 , Y02A50/465 , A61K2300/00
    • Compounds represented by the formula (I) R is H, OH, alkyl, O-alkyl, CH2—O-alkyl, (CH2)nOH, (CH2)nNH2, (CH2)nCONH2, (CH2)nOOOH; R1 is H, OH, alkyl, O-alkyl, CH2—O-alkyl, C6H11, CH2OH; R2 is H, alkyl, OH, CH2OH, CH2—O-alkyl, CH(OH)-alkyl, CH(OH)CH2OH, CH2-halogen; R3 and R4 independently is H, OH, alkyl; Z is OR5, OR6, or aminoacids and esters thereof R5 and R6 independently is H, alkyl, aryl, pivaloyloxymethyl, C(R7)2OC(O) X (R8)a formula (II), R7 independently is —H, C1-C12 alkyl, C5-C12 aryl, C2-C12 alkenyl, C2-C12 alkynyl, C7-C12 alkenylaryl, C7-C12 alkynylaryl, or C6-C12 alkaryl, any of which is unsubstituted or is substituted with 1 or 2 halo, cyano, azido, nitro, or —OR9; R9 is C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl or C5-C12 aryl; provided that at least one R8 is not H; and a is 1 when X is CH2, or direct bond, or 1 or 2 when X is N with the proviso that when a is 2 and X is N, (a) two N-linked R groups can be taken together to form a carbocyclic or oxygen containing heterocycle, (b) one N-linked R8 additionally can be —OR9 or (c) both N-linked R8 groups can be —H; R10 is H or C1-C8 alkyl; R11 is selected from H, alkyl, alkenyl, alkynyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl n is 1-5 m is 0 to 5 X is S, N(R8) or direct bond Y is O, S, N (R8), and CHR1 B is selected from the group consisting of adenine, guanine, cytosine, uracil, thymine, modified purines and pyrimidines such as inosin-9-yl, 2-amino-purin-9-yl, 2amino-6-chloro-purin-9-yl, 2-6-diamino-purin-9-yl, 3-carboxamido-1, 2, 4-triazol-1-yl, 3-deaza-adenin-9-yl, 3-deaza-guanin-9-yl, 3-deaza-inosin-9-yl, 3-deaza-2-amino-purin-9-yl, 3-deaza-2-amino-6-chloro-purin-9-yl, 3-deaza-2, 6-diamino-purin-9-yl, 7-deaza-adenin-9-yl, 7-deaza-guanin-9-yl, 7-deaza-inosin-9-yl, 7-deaza-2-amino-purin-9-yl, 7-deaza-2-amino-6-chloro-purin-9-yl, 7-deaza-2-6-diamino-purin-9-yl, 7-deaza-8-aza-adenin-9-yl, 7-deaza-8-aza-guanin-9-yl, 7-deaza-8-aza-inosnin-9-yl, 7-deaza-8-aza-2-amino-purin-9-yl, 7-deaza-8-aza-2-amino-6-chloro-purin-9-yl, 7-deaza-8-aza-2-6-diamino-purin-9-yl, -8-aza-adenin-9-yl,-8-aza-guanin-9-yl, -8-aza-inosnin-9-yl, -8-aza-2-amino-purin-9-yl, -8-aza-2-amino-6-chloro-purin-9-yl, -8-aza-2-6-diamino-purin-9-yl, 5-aza-thymin-1-yl, 5-aza-cytosin-1-yl, 5-aza-uracil-1-yl, 6-aza-thymin-1-yl, 6-aza-cytosin-1-yl, 6-aza-uracil-1-yl, 2-thiouracil-1-yl, 4-thiouracil-1-yl, 2 thiocytosine-1-yl, uracil-5-yl, 2-thiouracil-5-yl, 4-thiouracil-5-yl, substituted pyridine derivatives such as 6-azauracil, and azacyzosine. In general, attachment may be at different positions in the ring at nitrogen or carbon. These B ring systems may be substituted with halo, alkyl, substituted alkyl (F, Cl, Br, I, OH), NH2, N3, aryl, substituted aryl (F, Cl, Br, I, OH, NH2), aralkyl; and pharmaceutically acceptable salts thereof and prodrugs thereof are provided.
    • 由式（I）R表示的化合物是H，OH，烷基，O-烷基，CH 2 -O-烷基，（CH 2）n OH，（CH 2）n NH 2，（CH 2）n CONH 2，（CH 2） R 1是H，OH，烷基，O-烷基，CH 2 -O-烷基，C 6 H 11，CH 2 OH; R 2是H，烷基，OH，CH 2 OH，CH 2 -O-烷基，CH（OH） - 烷基，CH（OH）CH 2 OH， R 3和R 4独立地是H，OH，烷基; Z为OR 5，OR 6或其氨基酸及其酯R 5和R 6独立地为H，烷基，芳基，新戊酰氧基甲基，C（R 7）2 OC（O）X（R 式（II）中，R 7独立地是-H，C 1 -C 12烷基，C 5 -C 12芳基，C 2 -C 12烯基，C 2 -C 12炔基，C 7 -C 12链烯基芳基，C 7 -C 12炔基芳基或 C 6 -C 12烷芳基，其中任何一个是未取代的或被1或2个卤素，氰基，叠氮基，硝基或-OR 9取代。 R 9是C 1 -C 12烷基，C 2 -C 12烯基，C 2 -C 12炔基或C 5 -C 12芳基; 条件是至少一个R 8不是H; 当X为CH 2或直接键合时，a为1，X为N时为1或2，条件是当a为2且X为N时，（a）两个N-连接的R基团可以一起形成 碳环或含氧杂环，（b）一个N-连接的R 8另外可以是-OR 9或（c）两个N-连接的R 8基团可以是-H; R 10是H或C 1 -C 8烷基; R 11选自H，烷基，烯基，炔基，芳基，酰氧基烷基和新戊酰氧基烷基
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 30. 发明申请
      US20050080053A1 Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases 审中-公开
    • Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
    • 核苷类，其制备和用作RNA病毒聚合酶的抑制剂
    • US20050080053A1
    • 2005-04-14
    • US10928177
    • 2004-08-30
    • Yarlagadda Babu , Pooran Chand , Yahya El-Kattan , Pravin Kotian , Minwan Wu
    • Yarlagadda Babu , Pooran Chand , Yahya El-Kattan , Pravin Kotian , Minwan Wu
    • A61K31/675 , C07F9/6561
    • C07F9/65616
    • Compounds represented by the formula: Wherein A is —(CH2)n—R, —CH═CH2, —CH2—CH═CH2, —O—(CH2)n—R, —CH(OH)CH3, —CH(OH)—CH2OH, —CH2—CH(OH)CH3, —CH2—CH(OH)—CH2OH, —CH(OH)—CH(OH)—CH3; R is H, OH, F, N3, NH2, CO2H, SH, alkyl, S-alkyl, O-acyl, CONH2, CONH-alkyl; Z and Z′ independently is OR′, OR2, O—(CH2)n—O-alkyl or aminoacids and esters thereof; R1 and R2 independently is H, alkyl, aryl, pivaloyloxymethyl, phthalyl or substituted phthalyl, C(R3)2OC(O) X (R4)a, R3 is —H, C1-C12 alkyl, C5-C12 aryl, C2-C12 alkenyl, C2-C12 alkynyl, C7-C12 alkenylaryl, C7-C12 alkynylaryl, or C6-C12 alkaryl, any of which is unsubstituted or is substituted with 1 or 2 halo, cyano, azido, nitro, or —OR5; R4 is —H, C1-C12 alkyl, C5-C12 aryl, C2-C12 alkenyl, C2-C12 alkynyl, C7-C12 alkenylaryl, C7-C12 alkynylaryl, or C6-C12 alkaryl, any of which is unsubstituted or is substituted with 1 or 2 halo, cyano, azido, nitro, —N(R6)2 or —OR5; R5 is C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl or C5-C12 aryl; provided that at least one R4 is not H; and a is 1 when X is CH2, or direct bond, or 1 or 2 when X is N with the proviso that when a is 2 and X is N, (a) two N-linked R groups can be taken together to form a carbocyclic or oxygen containing heterocycle, (b) one N-linked R4 additionally can be —OR5 or (c) both N-linked R4 groups can be —H; R6 is H or C1-C8 alkyl; R7 is selected from H, alkyl, alkenyl, alkynyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl; n is 1-3; Y is O, S or NH; W is O or S; B is selected from the group consisting of adenine, guanine, and modified purines are provided.
    • 由下式表示的化合物：其中A是 - （CH2）nR，-CH = CH2，-CH2-CH = CH2，-O-（CH2）nR，-CH（OH）CH3，-CH（OH）-CH2OH， -CH 2 -CH（OH）CH 3，-CH 2 -CH（OH）-CH 2 OH，-CH（OH）-CH（OH）-CH 3; R是H，OH，F，N 3，NH 2，CO 2 H，SH，烷基，S-烷基，O-酰基，CONH 2，CONH-烷基; Z和Z'独立地是OR'，OR 2，O-（CH 2）n -O-烷基或其氨基酸及其酯; R 1和R 2独立地是H，烷基，芳基，新戊酰氧基甲基，邻苯二甲酰基或取代的邻苯二甲酰基，C（R 3）2 OC（O）X（R 4）a，R 3是 - H，C 1 -C 12烷基，C 5 -C 12芳基，C 2 -C 12烯基，C 2 -C 12炔基，C 7 -C 12链烯基芳基，C 7 -C 12炔基芳基或C 6 -C 12烷芳基，其中任何一个是未取代的或被1或2 卤素，氰基，叠氮基，硝基或-OR 5; R 4是-H，C 1 -C 12烷基，C 5 -C 12芳基，C 2 -C 12烯基，C 2 -C 12炔基，C 7 -C 12链烯基芳基，C 7 -C 12炔基芳基或C 6 -C 12烷芳基，其中任何一个是未取代的或 被1或2个卤素，氰基，叠氮基，硝基，-N（R 6）2或-OR 5取代; R 5是C 1 -C 12烷基，C 5
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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