发明授权
- 专利标题: ANALOGS OF PTH
- 专利标题(中): 类比PARATHORMONS的
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申请号: EP93915814.3申请日: 1993-07-06
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公开(公告)号: EP0672057B1公开(公告)日: 2000-09-20
- 发明人: BAUER, Wilfried , BRECKENRIDGE, Robin , CARDINAUX, François , GOMBERT, Frank , GRAM, Hermann , RAMAGE, Paul , SCHNEIDER, Helmut , WAELCHLI, Rudolf , ALBERT, Rainer , LEWIS, Ian
- 申请人: Novartis AG
- 申请人地址: Schwarzwaldallee 215 4058 Basel CH
- 专利权人: Novartis AG
- 当前专利权人: Novartis AG
- 当前专利权人地址: Schwarzwaldallee 215 4058 Basel CH
- 优先权: GB9215009 19920715; GB9226415 19921218; GB9226861 19921223; GB9226859 19921223; GB9301691 19930128; GB9301692 19930128; GB9307673 19930414; GB9308033 19930419
- 国际公布: WO9402510 19940203
- 主分类号: C07K14/635
- IPC分类号: C07K14/635 ; C12N15/62 ; C12P21/02 ; C12N1/20 ; A61K38/29
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.
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