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    Method for inactivation of pathogens in platelets using 4' and 5' primary amino-substituted psoralens
    3.
    发明授权
    Method for inactivation of pathogens in platelets using 4' and 5' primary amino-substituted psoralens 失效
    使用4'和5'伯氨基取代的补骨脂素使血小板中的病原体失活的方法

    公开(公告)号：US6004742A

    公开(公告)日：1999-12-21

    申请号：US962903

    申请日：1997-11-03

    申请人： Susan Wollowitz ,  Stephen T. Isaacs ,  Henry Rapoport ,  Hans Peter Spielmann

    发明人： Susan Wollowitz ,  Stephen T. Isaacs ,  Henry Rapoport ,  Hans Peter Spielmann

    IPC分类号： A61K31/37 ,  A61K41/00 ,  A61L2/00 ,  A01N1/02 ,  C12N7/06

    CPC分类号： A61K41/0066 ,  A01N1/0215 ,  A01N1/0294 ,  A61K31/37 ,  A61L2/0011 ,  A61L2/0088

    摘要： Psoralen compounds are synthesized which have substitutions on the 4, 4', 5', and 8 positions of the psoralen, which permit enhanced binding to nucleic add of pathogens. Higher psoralen binding levels and lower mutagenicity are described, resulting in safer, more efficient, and reliable inactivation of pathogens in blood products. The invention contemplates inactivation methods using the new psoralens which do not compromise the function of blood products for transfusion. In particular compounds with primary aminoalkyl substitutions on the 4' or 5' positions of psoralen are used to inactivate pathogens in blood products such as platelets.

    摘要翻译： 合成补骨脂素化合物，其在补骨脂素的4,4'，5'和8位上具有取代，其允许增强与病原体的核酸添加结合。 描述了更高的补骨脂素结合水平和较低的致突变性，导致血液制品中病原体的更安全，更有效和可靠的失活。 本发明考虑使用新的补骨脂素的灭活方法，其不损害用于输血的血液制品的功能。 特别是在补骨脂素的4'或5'位上具有伯氨基烷基取代的化合物用于灭活血液制品如血小板中的病原体。

    Cyclic carbamate analogues of (+)-pilocarpine
    9.
    发明授权
    Cyclic carbamate analogues of (+)-pilocarpine 失效
    （+） - 毛果芸香碱的环状氨基甲酸酯类似物

    公开(公告)号：US5025027A

    公开(公告)日：1991-06-18

    申请号：US446486

    申请日：1989-12-05

    申请人： Henry Rapoport ,  Per Sauerberg

    发明人： Henry Rapoport ,  Per Sauerberg

    IPC分类号： C07D413/06

    CPC分类号： C07D413/06

    摘要： Pilocarpine analogues are provided having the structure ##STR1## where one of R.sub.1 or R.sub.2 is an alkyl, such as methyl, ethyl, propyl, butyl, and so forth, and the corresponding secondary alkyl groups, an aralkyl, such as benzyl, phenylethyl, phenylpropyl, and the corresponding secondary aralkyl residues, or a cycloalkyl having less than about 12 carbon atoms. R.sub.3 has at least two carbon atoms but less than about 9. These pilocarpine analogues have improved duration of biological activity with respect to pilocarpine. A particularly preferred compound is a muscarinic agonist equipotent with pilocarpine, where R.sub.2 is methyl, and R.sub.3 is ethyl.

    摘要翻译： 提供具有结构“IMAGE”的毛果芸香碱类似物，其中R 1或R 2中的一个为烷基，例如甲基，乙基，丙基，丁基等，以及相应的仲烷基，芳烷基如苄基，苯乙基， 苯基丙基和相应的仲芳烷基或具有小于约12个碳原子的环烷基。 R3具有至少两个碳原子但小于约9.这些毛果芸香碱类似物相对于毛果芸香碱具有改善的生物活性持续时间。 特别优选的化合物是与毛果芸香碱等效的毒蕈碱激动剂，其中R2是甲基，R3是乙基。

    Preparation of optically active ketones
    10.
    发明授权
    Preparation of optically active ketones 失效
    光学活性酮的制备

    公开(公告)号：US4618710A

    公开(公告)日：1986-10-21

    申请号：US417771

    申请日：1982-09-13

    申请人： Henry Rapoport ,  Thomas F. Buckley, III

    发明人： Henry Rapoport ,  Thomas F. Buckley, III

    IPC分类号： C07C271/06 ,  C07C307/02 ,  C07C311/00 ,  C07C125/065 ,  C07C125/067 ,  C07C143/74 ,  C07C143/78

    CPC分类号： C07C307/02 ,  C07C271/06 ,  C07C311/00

    摘要： An optically active alpha-amino acid derivative having the formula: ##STR1## wherein: X is OH, Cl, Br, I, or OCOR.sub.3 ;Y is a radical selected to stabilize the alpha carbon atom of the alpha-amino acid derivative sufficiently to prevent significant change in symmetry thereof during replacement of X with an alkyl, aryl, alkenyl, alkynyl, alkaryl, aralkyl, alkenaryl or alkynaryl radical, or such radical having one or more chemical constituents thereon; andR.sub.1 and R.sub.2 are different from one another and are each hydrogen or an alkyl, aryl, alkenyl, alkynyl, alkaryl, aralkyl, alkenaryl, or alkynaryl radical, or such radical having one or more non-protic chemical constituents thereon is conventionally synthesized from the corresponding alpha-amino acid. The ##STR2## portion of the above derivative is converted to a ketone functionality without racemization.

    摘要翻译： 具有下式的光学活性α-氨基酸衍生物：其中：X是OH，Cl，Br，I或OCOR3; Y是选择的基团，以充分稳定α-氨基酸衍生物的α碳原子，以防止在用烷基，芳基，烯基，炔基，烷芳基，芳烷基，烯芳基或炔烃基取代X时其对称性的显着变化，或 这种基团在其上具有一种或多种化学成分; 并且R 1和R 2彼此不同，并且各自为氢或烷基，芳基，烯基，炔基，烷芳基，芳烷基，烯芳基或炔烃基，或者其上具有一个或多个非质子化学成分的基团通常由 相应的α-氨基酸。 上述衍生物的部分转化为酮官能团而不外消旋化。