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    AMINO- AND MERCURIO-SUBSTITUTED 4',5'-DIHYDROPSORALENS AND THERAPEUTICAL USES THEREOF
    3.
    发明申请
    AMINO- AND MERCURIO-SUBSTITUTED 4',5'-DIHYDROPSORALENS AND THERAPEUTICAL USES THEREOF 审中-公开
    AMINO-和MERCURIO-取代的4'，5'-二氢松香油及其治疗用途

    公开(公告)号：WO0031081A3

    公开(公告)日：2000-11-23

    申请号：PCT/US9927739

    申请日：1999-11-24

    Applicant: BUCKMAN LABOR INC ,  HEINDEL NED D ,  LASKIN JEFFREY D ,  HECK DIANE E ,  RAPP ROBERT D ,  MCNEEL THOMAS E ,  JABIN IVAN ,  WHITTEMORE MARILYN S

    Inventor： HEINDEL NED D ,  LASKIN JEFFREY D ,  HECK DIANE E ,  RAPP ROBERT D ,  MCNEEL THOMAS E ,  JABIN IVAN ,  WHITTEMORE MARILYN S

    IPC: A61P17/06 ,  A61P35/00 ,  C07D311/44 ,  C07D311/56 ,  C07D493/04 ,  C07F3/14 ,  A61K31/34

    CPC classification number: C07D493/04 ,  C07D311/44 ,  C07D311/56 ,  C07F3/14

    Abstract: 5'- substituted, 4', 5'- dihydropsoralen compounds (5) bearing tertiary amines (and salts thereof), quaternary ammonium moieties or organomercurial moieties are described. Also described are 2- substituted mercurimethyl -2-3- dihydro -benzofurans of formula (7). Also reported are versatile direct syntheses through a hitherto unknown compounds such as 3-R-4, 8-dimethyl -4',5'-dihydro -5'-bromomethylpsoralen or a 3-R-4, 8-dimethyl-4, 5'-dihydro- 5'-iodomethylpsoralen to prepare a structurally diverse array of partially reduced psoralens and benzofurans. The presence of a permanent ammonium charge in these psoralens precludes membrane passage and the mono-unsaturation precludes the cross linking of nuclear DNA, thereby minimizing the mutagenic/carcinogenic side effects long associated with psoralen-derived therapies. The presence of a mercury functionality provides a reactive cell-binding group on these psoralens with unique cytotoxicity without light activation and an enhancement of cytotoxicity activity upon light activation. The invention also relates to these partially reduced and quaternized psoralens, amino-substituted psoralens, and mercurio psoralens display impressive pharmacology against PAM 212 keratinocytes, a model cell line employed as a test system to indicate epidermal cytotoxicity and cancer. The compounds of the invention also have antimicrobicidal activity useful in pharmacologic agents for mammals (e.g. the treatment of tuberculosis) as well as in controlling the growth of microorganisms on substrates and in aqueous systems.

    Abstract translation: 描述了带有叔胺（及其盐），季铵部分或有机金属部分的5'-取代的，4'，5'-二氢补骨脂化合物（5）。 还描述了式（7）的2-取代的汞甲基-2-3-二氢 - 苯并呋喃。 还报道了通过迄今未知的化合物如3-R-4,8-​​二甲基-4'，5'-二氢-5'-溴甲基补骨脂素或3-R-4,8-​​二甲基-4,5 ' - 二氢-5'-碘甲基补骨脂素以制备结构多样化的部分减少的补骨脂素和苯并呋喃。 这些补骨脂素中永久性铵电荷的存在排除了膜通道，单不饱和度排除了核DNA的交联，从而使与补骨脂素衍生疗法长期相关的致突变/致癌性副作用最小化。 汞功能的存在提供了这些补骨脂素上的反应性细胞结合基团，其具有独特的细胞毒性而没有光激活并且在光活化时增强细胞毒性活性。 本发明还涉及这些部分还原的和季铵化的补骨脂素，氨基取代的补骨脂素和补骨脂素显示出对PAM212角质形成细胞的令人印象深刻的药理学，PAM212角质形成细胞是用作表明表皮细胞毒性和癌症的测试系统的模型细胞系。 本发明化合物还具有抗哺乳动物药理活性剂（例如治疗结核病）以及控制微生物在底物和水系统中生长的抗微生物活性。

    AMINO- AND MERCURIO-SUBSTITUTED 4',5'-DIHYDROPSORALENS AND THERAPEUTICAL USES THEREOF
    4.
    发明申请
    AMINO- AND MERCURIO-SUBSTITUTED 4',5'-DIHYDROPSORALENS AND THERAPEUTICAL USES THEREOF 审中-公开
    AMINO-和MERCURIO取代4'，5'-二羟基丙酸酯及其治疗用途

    公开(公告)号：WO00031081A2

    公开(公告)日：2000-06-02

    申请号：PCT/US1999/027739

    申请日：1999-11-24

    IPC: A61P17/06 ,  A61P35/00 ,  C07D311/44 ,  C07D311/56 ,  C07D493/04 ,  C07F3/14 ,  A61K31/34

    CPC classification number: C07D493/04 ,  C07D311/44 ,  C07D311/56 ,  C07F3/14

    Abstract: 5'- substituted, 4', 5'- dihydropsoralen compounds (5) bearing tertiary amines (and salts thereof), quaternary ammonium moieties or organomercurial moieties are described. Also described are 2- substituted mercurimethyl -2-3- dihydro -benzofurans of formula (7). Also reported are versatile direct syntheses through a hitherto unknown compounds such as 3-R-4, 8-dimethyl -4',5'-dihydro -5'-bromomethylpsoralen or a 3-R-4, 8-dimethyl-4, 5'-dihydro- 5'-iodomethylpsoralen to prepare a structurally diverse array of partially reduced psoralens and benzofurans. The presence of a permanent ammonium charge in these psoralens precludes membrane passage and the mono-unsaturation precludes the cross linking of nuclear DNA, thereby minimizing the mutagenic/carcinogenic side effects long associated with psoralen-derived therapies. The presence of a mercury functionality provides a reactive cell-binding group on these psoralens with unique cytotoxicity without light activation and an enhancement of cytotoxicity activity upon light activation. The invention also relates to these partially reduced and quaternized psoralens, amino-substituted psoralens, and mercurio psoralens display impressive pharmacology against PAM 212 keratinocytes, a model cell line employed as a test system to indicate epidermal cytotoxicity and cancer. The compounds of the invention also have antimicrobicidal activity useful in pharmacologic agents for mammals (e.g. the treatment of tuberculosis) as well as in controlling the growth of microorganisms on substrates and in aqueous systems.

    Abstract translation: 描述了含有叔胺（及其盐），季铵部分或有机体部分的5'-取代的4'，5'-二氢补骨脂素化合物（5）。 还描述了式（7）的2-取代的醇二甲基-2- 3-二氢 - 苯并呋喃。 还报道了通过迄今未知的化合物如3-R-4,8-​​二甲基-4'，5'-二氢-5'-溴甲基口服或3-R-4,8-​​二甲基-4,5 ' - 二氢-5'-碘甲基肌醇来制备结构不同的部分还原的补骨脂素和苯并呋喃的阵列。 在这些补骨脂素中存在永久铵电荷排除了膜通过，并且单不饱和度排除了核DNA的交联，从而最小化与补骨脂素衍生疗法长期相关的致突变/致癌副作用。 汞功能的存在在这些补骨脂素上提供了具有独特细胞毒性的反应性细胞结合基团，而没有光活化，并且在光活化时增强细胞毒性活性。 本发明还涉及这些部分还原和季铵化的补骨脂素，氨基取代的补骨脂素和补骨脂素，其显示出对PAM 212角质细胞的令人印象深刻的药理学，该模型细胞系用作测试系统以指示表皮细胞毒性和癌症。 本发明的化合物还具有用于哺乳动物的药理学（例如治疗结核病）以及控制底物和水系统中的微生物生长的抗除菌活性。

    CHROMONE COMPOUNDS AND USE THEREOF
    6.
    发明申请
    CHROMONE COMPOUNDS AND USE THEREOF 审中-公开
    色酮化合物及其用途

    公开(公告)号：WO99019318A1

    公开(公告)日：1999-04-22

    申请号：PCT/JP1998/004524

    申请日：1998-10-07

    IPC: A01N43/653 ,  A01N47/34 ,  C07D309/22 ,  C07D309/24 ,  C07D309/30 ,  C07D311/24 ,  C07D311/44 ,  C07D311/56 ,  C07D335/06 ,  C07D405/04 ,  C07D311/22 ,  C07D311/54 ,  C07D409/04

    CPC classification number: C07D335/06 ,  A01N43/653 ,  C07D309/22 ,  C07D309/24 ,  C07D309/30 ,  C07D405/04

    Abstract: Novel substituted chromone compounds which are intermediates for chromone compounds useful as bactericides and herbicides. Specifically, substituted chromone compounds represented by general formula (1) wherein R represents hydrogen, C1-6 alkyl, etc.; R represents hydrogen or C1-6 alkyl; R represents halogeno, etc.; R represents hydrogen, halogeno, etc.; R represents hydrogen, C1-6 alkyl, etc.; X represents oxygen or sulfur; and A represents nitro, etc.

    Abstract translation: 新颖的取代色酮化合物，其是用作色酮化合物的中间体，可用作杀菌剂和除草剂。 具体来说，由通式（1）表示的取代的色酮化合物，其中R 1表示氢，C 1-6烷基等; R 2表示氢或C 1-6烷基; R 3表示卤素等。 R 4表示氢，卤素等; R 5表示氢，C 1-6烷基等; X表示氧或硫; A代表硝基等

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