TRICYCLIC COMPOUNDS AND THEIR ANALOGS AS INHIBITORS OF CYTOKINE SIGNALING
    2.
    发明申请
    TRICYCLIC COMPOUNDS AND THEIR ANALOGS AS INHIBITORS OF CYTOKINE SIGNALING 审中-公开
    三聚体化合物及其作为细胞因子信号抑制剂的模拟物

    公开(公告)号:WO02068421A3

    公开(公告)日:2003-07-31

    申请号:PCT/US0143048

    申请日:2001-11-09

    CPC classification number: C07D487/14 A61K31/522 A61K31/675 C07D513/14

    Abstract: Novel tricyclic compounds having the formula (II) or (I), wherein: R1 is optionally substituted and selected from a member of the group consisting of hydrogen, methyl, C1-20alkyl, C1-20alkenyl, C1-20alkynyl, C1-20hydroxyalkyl, C1-20cyanoalkyl, C1-20alkoxyl, and C1-20alkoxyalkyl R2 and R3 join to form an optionally substituted heterocycle, each R2 and R3 being independantly selected from a member of the group consisting of hydrogen, halo, thio, oxo, C1-20alkyl, C1-20hydroxyalkyl, C1-20thioalkyl, C1-20alkylthio, C1-20alkylamino, C1-20alkylaminoalkyl, C1-20aminoalkyl, C1-20aminoalkyloxyalkenyl, C1-20aminoalkyloxyalkynyl, C1-20diaminoalkyl, C1-20triaminoalkyl, C1-20tetraaminoalkyl, C1-20aminotrialkoxyamino, C1-20alkylamido, C1-20alkylamidoalkyl, C1-20amidoalkyl, C1-20acetamidoalkyl, C1-20alkenyl, C1-20alkynyl, C1-20alkoxyl, C1-20alkoxyalkyl, and C1-20dialkoxyalkyl, are found to be used for the treatment or prevention of symptoms of manifestations associated with diseases or disorders affected by cytosine and intracellular signaling.

    Abstract translation: 具有式(II)或(I)的新型三环化合物,其中:R 1任选被取代并选自氢,甲基,C 1-20烷基,C 1-20烯基,C 1-20炔基,C 1-20羟烷基, C 1-20烷酰基,C 1-20烷氧基烷基和C 1-20烷氧基烷基R 2和R 3连接形成任选取代的杂环,每个R 2和R 3独立地选自氢,卤素,硫代,氧代,C 1-20烷基, C 1-20烷氧基烷基,C 1-20二氨基烷基,C 1-20二氨基烷基,C 1-20二氨基烷基,C 2-20氨基三烷氧基氨基,C 1 -C 20烷基氨基烷基, 20个烷基酰氨基,C 1-20烷基酰氨基烷基,C 1-20氨基烷基,C 1-20乙酰胺基烷基,C 1-20烯基,C 1-20炔基,C 1-20烷氧基,C 1-20烷氧基烷基和C 1-20二烷氧基烷基被用于治疗或预防相关表现的症状 与疾病或病症affec 由胞嘧啶和细胞内信号传导。

    8.
    发明专利
    未知

    公开(公告)号:BR0014652A

    公开(公告)日:2003-06-10

    申请号:BR0014652

    申请日:2000-10-12

    Abstract: The present invention relates to conjugates comprising a polyglutamic acid polymer covalently bonded to a camptothecin molecule selected from the group consisting of 20(S)(+)-camptothecin, 9-aminocamptothecin, 9-nitrocamptothecin, 7-ethyl-10-hydroxycamptothecin, 9-dimethyl-aminomethyl-10-hydroxycamptothecin and 7-methylpiperizinomethyl-10,11-ethylenedioxy-camptothecin. The present invention also relates to such compounds as medicaments, in particular for the treatment of cancer.

    Second messenger cell signaling onhibitors

    公开(公告)号:ZA942317B

    公开(公告)日:1995-02-10

    申请号:ZA942317

    申请日:1994-03-31

    Abstract: Therapeutic compounds have the formula:(X)j-(core moiety),j being an integer from one to three, the core moiety comprising a core moiety, the core moiety being a heterocycle having one ring or two-fused rings, each ring having five or six ring atoms, A being a carbon atom of the core moiety and attached to a terminal carbon atom of (CH2)m, and X has a structure and X being a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH2)n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R1 and R2 may be a hydrogen, a straight or branched chain alkyl or alkenyl of up to twelve carbon atoms in length, or -(CH2)wR5, w being an integer from two to fourteen and R5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R5 being hydroxy, chloro, fluoro, bromo, or C1-6 alkoxyl. Or jointly, R1 and R2 form a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, N being a hetero atom. R3 is a hydrogen or C1-3. Or, therapeutic compounds may also have the formula: ed chain alkyl or alkenyl of up to eight carbon atoms in length, -(CH2)wR5, w being an integer from two to fourteen and R5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R5 being hydroxy, chloro, fluoro, bromo, or C1-6 alkoxyl, or a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, r and s are independently integers from one to four, the sum (r+s) not being greater than five. t is an integer from one to fourteen and one or more carbon atoms of (CH2)s or (CH2)t may be substituted by a keto or hydroxyl group.

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