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107 条记录 (耗时 0.044 秒)

    RADIOPHARMACEUTICALS FOR IMAGING INFECTION AND INFLAMMATION AND FOR IMAGING AND TREATMENT OF CANCER
    61.
    发明公开
    RADIOPHARMACEUTICALS FOR IMAGING INFECTION AND INFLAMMATION AND FOR IMAGING AND TREATMENT OF CANCER 审中-公开
    放射性药物用于表示感染，点火和介绍和治疗癌症的

    公开(公告)号：EP1068222A1

    公开(公告)日：2001-01-17

    申请号：EP99912938.0

    申请日：1999-03-29

    申请人： Du Pont Pharmaceuticals Company

    发明人： EDWARDS, David, Scott ,  RAJOPADHYE, Milind

    IPC分类号： C07K7/06 ,  A61K51/08

    CPC分类号： C07K7/06 ,  A61K51/088

    摘要： The present invention provides novel radiopharmaceuticals useful for the diagnosis of infection and inflammation, reagents and kits useful for preparing the radiopharmaceuticals, methods of imaging sites of infection and/or inflammation in a patient, and methods of diagnosing diseases associated with infection or inflammation in patients in need of such diagnosis. The radiopharmaceuticals bind in vivo to the tuftsin receptor on the surface of white cells which accumulate at the site of infection and inflammation. The radiopharmaceuticals are also useful for imaging tumors and treating the cancer by delivering a cytotoxic dose of radiation to the tumors. The radiopharmaceuticals of the present invention are comprised of one to three pentapeptides, X?1X2X3X4X5¿, independently attached to a metal chelator or bonding moiety, C¿h?, to which is attached a Tc-99m, Re-186, or Re-188, optionally further comprising a linking group, Ln, between the peptides and the chelator or bonding moiety. The pentapeptide sequence binds to the tuftsin receptor and is attached at the N-terminus to Ln or Ch. The interaction of the pentapeptide recognition sequences of the radiopharmaceuticals with the tuftsin receptor on white blood cells results in localization of the radiopharmaceuticals in sites of infection and inflammation, and in tumors.

    PREPARATION OF ASYMMETRIC CYCLIC UREAS THROUGH A MONOACYLATED DIAMINE INTERMEDIATE
    66.
    发明公开
    PREPARATION OF ASYMMETRIC CYCLIC UREAS THROUGH A MONOACYLATED DIAMINE INTERMEDIATE 审中-公开
    不对称环脲在单酰基DIAMIN中间体生产

    公开(公告)号：EP1025092A2

    公开(公告)日：2000-08-09

    申请号：EP98952107.5

    申请日：1998-10-06

    申请人： Du Pont Pharmaceuticals Company

    发明人： STONE, Benjamin, R., P. ,  ANZALONE, Luigi ,  FORTUNAK, Joseph, M. ,  HARRIS, Gregory, D. ,  VALVIS, Ioannis, I. ,  WALTERMIRE, Robert, E.

    IPC分类号： C07D243/00

    CPC分类号： C07D491/04 ,  C07D243/04 ,  C07D317/14

    摘要： The present invention concerns an improved process for the preparation of asymmetric cyclic ureas as well as intermediates in the preparation of asymmetric cyclic ureas of formula (VI): wherein: R7 is selected from the following: C¿1?-C8 alkyl substituted with 0-3 R?11; C¿2-C8 alkenyl substituted with 0-3 R11; C2-C8 alkynyl substituted with 0-3 R11; and a C¿3?-C14 carbocyclic ring system substituted with 0-3 R?11; R10 is C1-C10¿ alkyl, benzyl, naphthylmethyl, 3,4-methylenedioxybenzyl, or C¿1?-C4 alkyl substituted with phenyl wherein said phenyl is substituted with 0-3 R?10a¿; G taken together along with the oxygen atoms to which G is attached forms a group selected from: -O-C(-CH¿2?CH2CH2CH2CH2-)-O-, -O-C(CH2CH3)2-O-, -O-C(CH3)(CH2CH3)-O-, -O-C(CH2CH2CH2CH3)2-O-, -O-C(CH3)(CH2CH(CH3)CH3)-O-, -O-CH(phenyl)-O-, OCH2O-, -OC(CH3)2O- and -OC(OCH3)(CH2CH2CH3)O-. In the process, a diamine of formula (I-a) is selectively monoacylated to give an asymmetric monoacylated diamine which can be converted into asymmetric intermediates. The asymmetric intermediates can be further alkylated, cyclized, and/or modified to give compounds which are useful as HIV protease inhibitors for the treatment of HIV infection. The invention allows for scalable preparation of a wide variety of asymmetrical cyclic ureas.