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    ERGOLINE DERIVATIVES AND THEIR USE AS CHEMOKINE RECEPTOR LIGANDS
    2.
    发明公开
    ERGOLINE DERIVATIVES AND THEIR USE AS CHEMOKINE RECEPTOR LIGANDS 审中-公开
    麦角灵衍生物和它们作为趋化因子受体配体的用途

    公开(公告)号：EP1893611A1

    公开(公告)日：2008-03-05

    申请号：EP06753946.0

    申请日：2006-05-29

    申请人： Novartis AG

    发明人： BAENTELI, Rolf ,  GLICKMAN, Fraser ,  KOVARIK, Jiri ,  LEWIS, Ian ,  STREIFF, Markus ,  THOMA, Gebhard ,  ZERWES, Hans-Günter

    IPC分类号： C07D457/06 ,  C07D457/08 ,  A61K31/48

    CPC分类号： C07D457/06 ,  C07D457/08

    摘要： Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or - phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2-CH2-OR1; CH2-CO-NR1R2; or CO-CH2R1R2; R4 is F; CI; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disorders or diseases mediated by interactions between chemokine receptors and their ligands.

    ANALOGS OF PTH
    4.
    发明授权
    ANALOGS OF PTH 失效
    类比PARATHORMONS的

    公开(公告)号：EP0672057B1

    公开(公告)日：2000-09-20

    申请号：EP93915814.3

    申请日：1993-07-06

    申请人： Novartis AG

    发明人： BAUER, Wilfried ,  BRECKENRIDGE, Robin ,  CARDINAUX, François ,  GOMBERT, Frank ,  GRAM, Hermann ,  RAMAGE, Paul ,  SCHNEIDER, Helmut ,  WAELCHLI, Rudolf ,  ALBERT, Rainer ,  LEWIS, Ian

    IPC分类号： C07K14/635 ,  C12N15/62 ,  C12P21/02 ,  C12N1/20 ,  A61K38/29

    CPC分类号： C07K14/005 ,  A61K38/00 ,  C07K14/635 ,  C07K2319/00 ,  C07K2319/50 ,  C07K2319/75 ,  C12N2795/10222

    摘要： PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1) at least one radical selected from an L- or D-α-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound; or 2) at least one α-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the α-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.