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    Compounds a containing a solid support
    1.
    发明授权
    Compounds a containing a solid support 失效
    含有固体支持物的化合物

    公开(公告)号：US5912342A

    公开(公告)日：1999-06-15

    申请号：US909823

    申请日：1997-08-12

    申请人： Petri Heinonen ,  Harri Lonnberg ,  Victor Cockcroft

    发明人： Petri Heinonen ,  Harri Lonnberg ,  Victor Cockcroft

    IPC分类号： C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C08F8/34 ,  C07D217/00

    CPC分类号： C07D401/12 ,  C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D405/04 ,  C07D405/12 ,  C08F8/34 ,  B01J2219/00497 ,  C08F2810/30

    摘要： The invention relates to a compound of the formula (I) wherein whereinY is the fraction of a solid or soluble support, where Y may include a residue of a functional group having been attached to said support, said functional group having been hydroxy, amino, thio, epoxy or halogen,R.sup.1 is aryl, heteroaryl, alkyl chain or ring or ring system, which may include a heteroatom, or R.sup.1 is nothing, and R.sup.2 is vinyl;CH.sub.2 CH.sub.2 X, where X is halogen; orR.sup.3 C.dbd.CHR or R.sup.3 CH--CH.sub.2 R.sup.4 X, where R.sup.3 and R.sup.4 are the same or different and are alkyl, acyl, carbonyl, cyano or nitro groups and X is halogen.The invention also relates to a method for preparation of compound (I) and to its use as a substrate in the synthesis of tertiary amines. The invention still concerns a group of alpha-2-receptor active tetrahydroisoquinoline derivatives.

    摘要翻译： 本发明涉及式（I）化合物，其中Y为固体或可溶性载体的级分，其中Y可包括已连接至所述载体的官能团的残基，所述官能团为羟基，氨基 ，硫基，环氧基或卤素，R 1是芳基，杂芳基，烷基链或环或环系，其可以包括杂原子，或者R 1不是，并且R 2是乙烯基; CH2CH2X，其中X是卤素; 或R3C = CHR或R3CH-CH2R4X，其中R3和R4相同或不同，为烷基，酰基，羰基，氰基或硝基，X为卤素。 本发明还涉及一种制备化合物（I）的方法及其在合成叔胺中作为底物的用途。 本发明还涉及一组α-2受体活性四氢异喹啉衍生物。

    Method for the preparation of tertiary amines, a compound useful therefor and alpha-2-receptor active tetrahydroisoquinoline derivatives
    2.
    发明授权
    Method for the preparation of tertiary amines, a compound useful therefor and alpha-2-receptor active tetrahydroisoquinoline derivatives 失效
    制备叔胺的方法，可用的化合物和α-2受体活性四氢异喹啉衍生物

    公开(公告)号：US6096752A

    公开(公告)日：2000-08-01

    申请号：US167740

    申请日：1998-10-07

    申请人： Petri Heinonen ,  Harri Lonnberg ,  Victor Cockcroft

    发明人： Petri Heinonen ,  Harri Lonnberg ,  Victor Cockcroft

    IPC分类号： C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C08F8/34 ,  C07D217/00

    CPC分类号： C07D401/12 ,  C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D405/04 ,  C07D405/12 ,  C08F8/34 ,  B01J2219/00497 ,  C08F2810/30

    摘要： The invention relates to the preparation of teriatry amines of the formula (V) where R is alkyl and R.sup.6 and R.sup.7 are alkyl groups which are optionally substituted or where R.sup.6 and R.sup.7 form a ring or ring system, via a substrate which is a compound of the formula (I) ##STR1## wherein Y is the fraction of a solid or soluble support, where Y may include a residue of a functional group having been attached to said support, said functional group having been hydroxy, amino, thio, epoxy or halogen,R.sup.1 is aryl, heteroaryl, alkyl chain or a ring or ring system, which may include a heteroatom, or R.sup.1 is nothing, and R.sup.2 is vinyl; CH.sub.2 CH.sub.2 X, where X is halogen; or R.sup.3 C.dbd.CHR.sup.4 or R.sup.3 CH--CH.sub.2 R.sup.4 X, where R.sup.3 and R.sup.4 are the same or different and are alkyl, acyl, carbonyl, cyano or nitro groups and X is halogen. The invention particularly relates to the preparation of alpha-2-receptor active tetrahydroisoquinoline derivatives.

    摘要翻译： 本发明涉及制备式（Ⅴ）的三元胺，其中R是烷基，R 6和R 7是任选被取代的烷基，或其中R 6和R 7形成环或环体系， 式（I）其中Y是固体或可溶性载体的级分，其中Y可以包括已连接到所述载体上的官能团的残基，所述官能团已经是羟基，氨基，硫代，环氧基或卤素，R1 是芳基，杂芳基，烷基链或环或环系，其可以包括杂原子，或R 1不是，并且R 2是乙烯基; CH2CH2X，其中X是卤素; 或R3C = CHR4或R3CH-CH2R4X，其中R3和R4相同或不同，为烷基，酰基，羰基，氰基或硝基，X为卤素。 本发明特别涉及α-2-受体活性四氢异喹啉衍生物的制备。

    2-5A ANALOGS AND THEIR METHODS OF USE
    3.
    发明申请
    2-5A ANALOGS AND THEIR METHODS OF USE 审中-公开
    2-5A模拟及其使用方法

    公开(公告)号：US20090181921A1

    公开(公告)日：2009-07-16

    申请号：US12340507

    申请日：2008-12-19

    申请人： Lawrence Blatt ,  Leonid Beigelman ,  Harri Lonnberg

    发明人： Lawrence Blatt ,  Leonid Beigelman ,  Harri Lonnberg

    IPC分类号： A61K31/7064 ,  C07H19/20 ,  A61P31/12

    CPC分类号： C07H21/02

    摘要： Disclosed herein are compounds that activate RNaseL, methods of synthesizing compounds that activate RNaseL and the use of compounds that activate RNaseL for treating and/or ameliorating a disease or a condition, such as a viral infection, cancer and/or parasitic disease.

    摘要翻译： 本文公开的是激活RNaseL的化合物，合成活化RNaseL的化合物的方法和使用激活RNaseL的化合物来治疗和/或改善疾病或病症如病毒感染，癌症和/或寄生虫病。

    PROTECTED NUCLEOTIDE ANALOGS
    7.
    发明申请
    PROTECTED NUCLEOTIDE ANALOGS 审中-公开
    保护核苷类似物

    公开(公告)号：US20090176732A1

    公开(公告)日：2009-07-09

    申请号：US12340408

    申请日：2008-12-19

    申请人： Leonid Beigelman ,  Lawrence Blatt ,  Harri Lonnberg

    发明人： Leonid Beigelman ,  Lawrence Blatt ,  Harri Lonnberg

    IPC分类号： A61K31/7056 ,  C07H19/10 ,  C07H19/056 ,  A61K31/7072 ,  C07C69/02

    CPC分类号： C07H19/056 ,  Y02P20/55

    摘要： Disclosed herein are nucleotide analogs with one or more protecting groups, methods of synthesizing nucleotide analogs with one or more protecting groups and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with one or more protecting groups.

    摘要翻译： 本文公开了具有一个或多个保护基团的核苷酸类似物，与一个或多个保护基团合成核苷酸类似物的方法以及用一种或多种与核苷酸类似物一起治疗疾病和/或病症如病毒感染，癌症和/或寄生虫病的方法 或更多的保护基团。

    Chemical phosphorylation of oligonucleotides and reactants used therefor
    9.
    发明授权
    Chemical phosphorylation of oligonucleotides and reactants used therefor 失效
    用于此的寡核苷酸和反应物的化学磷酸化

    公开(公告)号：US5959090A

    公开(公告)日：1999-09-28

    申请号：US886456

    申请日：1997-07-01

    申请人： Andrei Guzaev ,  Alex Azhayev ,  Harri Lonnberg

    发明人： Andrei Guzaev ,  Alex Azhayev ,  Harri Lonnberg

    IPC分类号： C07F9/24 ,  C07H21/00 ,  C12Q1/68 ,  C07H19/00 ,  C07H21/02

    CPC分类号： C07H21/00 ,  C07F9/2408

    摘要： Phosphoramidite building blocks according to the following formula 1 are used for phosphorylating oligonucleotides, preferably at the 5'- or 3'-terminus. The building blocks include phosphoramidite compounds according to formula 1: ##STR1## wherein DMTr is a 4,4'-dimethoxytrityl group; R.sub.1 is an electron withdrawing group; R.sub.2 is an electron withdrawing group which may be the same or different from the R.sub.1 group; R.sub.3 is an alkyl group; and R.sub.4 is an alkyl group which may be the same or different from the R.sub.3 group. Preferred electron withdrawing groups include --CO.sub.2 Et groups, --CO.sub.2 Me groups, --CN groups, --CON(Me).sub.2 groups, and --CONHMe groups, wherein Et represents an ethyl group and Me represents a methyl group. One preferred alkyl group is an isopropyl group.

    摘要翻译： 根据下式1的亚磷酰胺结构单元用于磷酸化寡核苷酸，优选在5'-或3'-末端。 构建单元包括式1的亚磷酰胺化合物：其中DMTr是4,4'-二甲氧基三苯甲基; R1是吸电子基团; R2是可以与R1基团相同或不同的吸电子基团; R3是烷基; 并且R 4是可以与R 3基团相同或不同的烷基。 优选的吸电子基团包括-CO 2 Et基团，-CO 2 Me基团，-CN基团，-CON（Me）2基团和-CONHMe基团，其中Et表示乙基，Me表示甲基。 一个优选的烷基是异丙基。