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    Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
    3.
    发明申请
    Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases 审中-公开
    核苷类，其制备和用作RNA病毒聚合酶的抑制剂

    公开(公告)号：US20050080053A1

    公开(公告)日：2005-04-14

    申请号：US10928177

    申请日：2004-08-30

    申请人： Yarlagadda Babu ,  Pooran Chand ,  Yahya El-Kattan ,  Pravin Kotian ,  Minwan Wu

    发明人： Yarlagadda Babu ,  Pooran Chand ,  Yahya El-Kattan ,  Pravin Kotian ,  Minwan Wu

    IPC分类号： A61K31/675 ,  C07F9/6561

    CPC分类号： C07F9/65616

    摘要： 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.

    摘要翻译： 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

    AZA nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
    4.
    发明申请
    AZA nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases 有权

    公开(公告)号：US20070099942A1

    公开(公告)日：2007-05-03

    申请号：US11157867

    申请日：2005-06-22

    申请人： Yarlagadda Babu ,  Pooran Chand ,  Ajit Ghosh ,  Pravin Kotian ,  V. Kumar

    发明人： Yarlagadda Babu ,  Pooran Chand ,  Ajit Ghosh ,  Pravin Kotian ,  V. Kumar

    IPC分类号： A61K31/519 ,  C07D487/02 ,  C07F7/02

    CPC分类号： C07D487/04 ,  C07D491/048 ,  C07F9/6561

    摘要： Compounds represented by the formula: , and pharmaceutically acceptable salts thereof and prodrugs thereof; wherein R1 is H, CH3, C2H5, C3H7 R2 is H, CH3, C2H5, C3H7, CH═CH2, CH2—OH, CH2F, CF3 R′2 is H, OH, NH2, NH-alkyl, F, N3, OCH3, O—C(O)CH(NH2)alkyl R3 is H, CH3, C2H5, C3H7 R′3 is H, OH, NH2, NH-alkyl, F, N3, OCH3, O—C(O)CH(NH2)alkyl R4 is H, CH3, C2H5, C3H7 At least one of R2, R3, or R4 has to be other than H, when X═NH in B R6 is H, CH3, C2H5, R7 is selected from H, alkyl, alkenyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl, aminoacids, CH2CH2SC(O)alkyl; and B is represented by the following structure: X is independently NR6, O, S, R8 and R9 independently is H, NH2, OH, SH, F, Cl, Br, I, aryl, heterocycle, alkyl, alkene, alkyne, S-alkyl, S-aryl, S(O)-alkyl, SO2-alkyl, SO2NH2, SO2NH-alkyl, SO2NH-aryl, NH-alkyl, NH-aryl, N(alkyl)2, N(aryl)2, O-alkyl, O-aryl, O-heterocycle, NH-(CH2)n-aryl, NH—C(O)-alkyl, NH—C(O)-aryl are useful for inhibiting viral RNA polymerases and treating patients suffering from diseases caused by various RNA viruses.

    Process for the preparation of substituted pyrrolidine derivatives and intermediates
    5.
    发明申请
    Process for the preparation of substituted pyrrolidine derivatives and intermediates 有权
    取代的吡咯烷衍生物和中间体的制备方法

    公开(公告)号：US20060128789A1

    公开(公告)日：2006-06-15

    申请号：US11210691

    申请日：2005-08-25

    申请人： Pooran Chand ,  Yahya El-Kattan ,  Pravin Kotian

    发明人： Pooran Chand ,  Yahya El-Kattan ,  Pravin Kotian

    IPC分类号： A61K31/4015 ,  C07D207/12

    CPC分类号： C07D277/60 ,  C07D207/12 ,  C07D207/16 ,  C07D417/06

    摘要： Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from benzylamine instead of phenethylamine (Scheme 3) which provides a crystalline intermediate. The synthesis of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is achieved from (S)-diethylmalate as described in Scheme 4. A process for preparing camphor sultam is also provided.

    摘要翻译： 提供两个合成; （3R，4R）-4-（羟基甲基）吡咯烷-3-醇等制备（3S，4R）-4-（羟基甲基）吡咯烷-3-醇的化合物。 （3R，4R）-4-（羟甲基）吡咯烷-3-醇使用由苄胺代替苯乙胺制备的非手性叶立德制备（方案3），其提供了结晶中间体。 （3S，4R）-4-（羟甲基）吡咯烷-3-醇的合成如方案4所述从（S） - 二乙基苹果酸得到。还提供了制备樟脑磺酸钠的方法。