SYNTHETIC DERIVATIVES OF RAPAMYCIN AS MULTIMERIZING AGENTS FOR CHIMERIC PROTEINS WITH IMMUNOPHILIN-DERIVED DOMAINS
    5.
    发明公开
    SYNTHETIC DERIVATIVES OF RAPAMYCIN AS MULTIMERIZING AGENTS FOR CHIMERIC PROTEINS WITH IMMUNOPHILIN-DERIVED DOMAINS 失效
    合成雷帕霉素衍生物ALS多聚FOR PROTEIN物质WITH亲免素的次域CHIMERE

    公开(公告)号:EP0888303A1

    公开(公告)日:1999-01-07

    申请号:EP97907937.0

    申请日:1997-02-28

    摘要: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula (I): M-L-Q, a resolved stereoisomer thereof or mixture of one or more such stereoisomers, and pharmaceutically acceptable salts thereof, wherein M is an immunophilin-binding group comprising a moiety of formula (II); G is independently selected from the group consisting of (a), (b), and (c); Q comprises a moiety of formula (II), a naturally occurring macrocyclic FKBP ligand or derivative thereof, or is a synthetic FKBP ligand of formula (III); n = 1 or 2; X = O, NH or CH2; B?1 and B2¿ are independently H or aliphatic, heteroaliphatic, aryl or heteroaryl; Y = O, S, NH, -NH(C=O)-, -NH(C=O)-O-, -NH(SO¿2?)- or NR?3¿, or represents a covalent bond from R2 to carbon 9; R?1, R2, and R3¿ are the same or different and are independently aliphatic, heteroaliphatic, aryl or heteroaryl; and, L is a linker moiety covalently linking monomers M to Q or covalently linking M1 to M2 through covalent bonds to either R1, R2, not necessarily the same in each of M?1 and M2¿.

    COMBINATION THERAPY
    6.
    发明公开
    COMBINATION THERAPY 审中-公开
    联合治疗

    公开(公告)号:EP2054061A2

    公开(公告)日:2009-05-06

    申请号:EP07810979.0

    申请日:2007-08-01

    IPC分类号: A61K31/44

    摘要: Disclosed are methods for treating various cancers. Methods encompass the administration of a first drug such as AP23573, temsirolimus or everolimus in combination with a second drug selected from Remicade, Humira, Enbrel, Raptiva, Abatacept, Actermra, Cimzia or anakinra. The methods are aimed at providing a desirable therapeutic window while maintaining prior, if not higher, dose levels of the first drug.

    摘要翻译: 公开了用于治疗各种癌症的方法。 方法包括给予第一种药物如AP23573,替西罗莫司或依维莫司与选自Remicade,Humira,Enbrel,Raptiva,Abatacept,Actermra,Cimzia或Anakinra的第二种药物的组合。 该方法旨在提供理想的治疗窗口,同时维持第一种药物的先前(如果不是更高的话)剂量水平。

    RAPAMCYCIN-BASED REGULATION OF BIOLOGICAL EVENTS
    7.
    发明授权
    RAPAMCYCIN-BASED REGULATION OF BIOLOGICAL EVENTS 失效
    生物过程雷帕霉素基于调控

    公开(公告)号:EP0833894B1

    公开(公告)日:2008-08-13

    申请号:EP96921491.5

    申请日:1996-06-07

    摘要: This invention concerns new configurations for biological switches and provides new methods and materials useful for regulating biological events in animal cells. The invention involves recombinant DNA constructs comprising DNA sequences derived from sequences encoding the proteins FRAP, Tor1, Tor2 and other proteins capable of binding to FKBP:rapamycin, other recombinant DNA constructs comprising DNA sequences encoding part or all of an FKBP protein, the proteins encoded by those constructs, cells (especially animal cells) transformed with one or more of the constructs, small molecules (multivalent multimerizing agents) which bind to and are capable of inducing multimerization of the chimeric proteins, and methods for preparing and using the foregoing.