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    FLUORINE NMR SPECTROSCOPY FOR BIOCHEMICAL SCREENING
    1.
    发明公开
    FLUORINE NMR SPECTROSCOPY FOR BIOCHEMICAL SCREENING 有权
    FLUOR-NMR光谱进行生化检查

    公开(公告)号：EP1644512A2

    公开(公告)日：2006-04-12

    申请号：EP04740926.3

    申请日：2004-07-12

    申请人： Pharmacia Italia S.p.A.

    发明人： DALVIT, Claudio ,  ARDINI, Elena ,  FLOCCO, Maria, Magdalena ,  FOGLIATTO, Gianpaolo ,  MONGELLI, Nicola ,  VERONESI, Marina

    IPC分类号： C12Q1/00 ,  C12Q1/48 ,  C12Q1/37 ,  C12Q1/42

    CPC分类号： C12Q1/485

    摘要： High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498-505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.

    BENZOCYCLODECANE DERIVATIVES WITH ANTITUMOR ACTIVITY
    4.
    发明公开
    BENZOCYCLODECANE DERIVATIVES WITH ANTITUMOR ACTIVITY 审中-公开
    BENZOCYCLODECAN-DERIVATE MIT ANTITUMOR-EIGENS

    公开(公告)号：EP1458686A1

    公开(公告)日：2004-09-22

    申请号：EP02791850.7

    申请日：2002-12-18

    申请人： Pharmacia Italia S.p.A.

    发明人： DUCKI, Sylvie ,  MENICHINCHERI, Maria ,  MONGELLI, Nicola ,  VANOTTI, Ermes ,  ANGIOLINI, Mauro ,  CIOMEI, Marina

    IPC分类号： C07D233/54 ,  C07C69/013 ,  C07C69/616 ,  C07D277/30 ,  C07D263/32 ,  C07D213/55 ,  C07D405/12 ,  A61K31/44 ,  A61K31/42 ,  A61K31/425 ,  A61K31/415

    CPC分类号： C07D233/64 ,  C07C45/673 ,  C07C49/747 ,  C07C67/08 ,  C07C67/29 ,  C07C67/293 ,  C07C69/007 ,  C07C69/013 ,  C07C69/618 ,  C07C2602/12 ,  C07D213/56 ,  C07D263/32 ,  C07D277/30 ,  C07H15/203 ,  C07C69/16

    摘要： A compound which is a benzocyclodecane of the formula I wherein: ----- at positions 8-9 and 11-12 independently represents a single or double bond, -R1 is =O, or -OR7, R7 is H, C1-C7 alkanoyl, benzoyl, C1-C10 alkyl, C2-C10 alkenyl or COCH=CHR8, R8 is aryl or heterocyclyl;-R2 and -R3 are H, =O or -OR9, R9 is H, C1-C7 alkanoyl or benzoyl; when at position 11-12 there is a single bond, then -R4 represents=O, =CH2, =CHCOOR10, R10 is C1-C10 alkyl or aryl; =CH(OCH3), -OR9; -CH2OR11, R11 is H or a sugar residue, -COR12 , R12 is H, -OH or -OR10; or when at position 11-12 there is a double bond, then -R4 is -CH2OR11 or -COR12; - R5 and -R6 are H or, when at position 8-9 there is a single bond, taken together form a cyclopropane ring; R13 is H or 1-3 substituents selected from C1-C6 alkyl, C2-C6 alkenyl, phenyl, phenyl C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy, aryloxy, cyano, nitro, amino, C1-C10 alkylamino, arylamino, C1-C7 alkanoylamino, aroylamino, hydroxycarbonyl, aminocarbonyl, C1-C6 alkylcarbonyl, C1-C6 alkylaminosulfonyl and arylaminosulfonyl group; with the provisos that if R1 and R4 =O, then one of R2, R3, R5, R6 and R13 is not H atom; or a pharmaceutically acceptable salt thereof. These benzocyclodecane derivatives are endowed with antitumor activity; a process and new intermediates for their preparation, the pharmaceutical compositions containing them, and their use in the prevention, control and treatment of cancer are also provided.

    摘要翻译： 作为式I的苯并环十一烷的化合物，其中： - 位置8-9和11-12独立地表示单键或双键，-R1 = O或-OR7，R7为H，C1- C7烷酰基，苯甲酰基，C1-C10烷基，C2-C10烯基或COCH = CHR8，R8是芳基或杂环基; -R2和-R3是H，= O或-OR9，R9是H，C1-C7烷酰基或苯甲酰基; 当在11-12位存在单键时，则-R4表示= O，= CH2，= CHCOOR10，R10为C1-C10烷基或芳基; = CH（OCH 3），-OR 9; -CH 2 OR 11，R 11为H或糖残基，-COR 12，R 12为H，-OH或-OR 10; 或当在11-12位存在双键时，则-R 4是-CH 2 OR 11或-COR 12; -R 5和-R 6是H或当位置8-9存在单键时，一起形成环丙烷环; R13是H或1-3个选自C1-C6烷基，C2-C6烯基，苯基，苯基C1-C6烷基，卤素，羟基，C1-C6烷氧基，芳氧基，氰基，硝基，氨基，C1-C10烷基氨基， 芳基氨基，C 1 -C 7烷酰基氨基，芳酰氨基，羟基羰基，氨基羰基，C 1 -C 6烷基羰基，C 1 -C 6烷基氨基磺酰基和芳基氨基磺酰基; 条件是如果R1和R4 = O，则R2，R3，R5，R6和R13之一不是H原子; 或其药学上可接受的盐。 这些苯并环十一烷衍生物具有抗肿瘤活性; 还提供了其制备方法和新的中间体，含有它们的药物组合物及其在预防，控制和治疗癌症中的用途。