| 摘要 |
PURPOSE: Provided are variants of parathyroid hormone(PTH), a process for their production, pharmaceutical preparations comprising them and their use as a pharmaceutical. CONSTITUTION: A PTH compound has PTH-like activity and comprises at least one modification, wherein the modification is either (1) at least one radical selected from an L- or D-alpha-amino acid,C2-6 alkoxycarbonyl and optionally substituted C1-8 alkyl, C2 -8 alkenyl, C2-8 alkynyl, aralkyl, aralkenyl or C3-6 cycloalkyl-C1-4 alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C26 alkoxycarbonyl and optionally substituted C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aralkyl, aralkenyl or C3-6 cycloalkyl-C1-4 alkyl and attached to one or more side chain amino groups of the PTH compound, or (2) at least one a-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 a-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence together are replaced by a pseudo-peptide, or a combination of such modifications. It has pharmacological activity, for example, 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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