- Bisphosphonic acid derivatives, as bone resorption inhibitors
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A bisphosphonic acid derivative of the formula (I) or a pharmaceutically acceptable salt thereof: STR1 wherein A is STR2 each of R3 and R4, which may be the same or different, is (i) a hydrogen atom, (ii) a C1-6 alkyl grou
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- Synthesis and evaluation of (piperidinomethylene)bis(phosphonic acid) derivatives as anti-osteoporosis agents
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Some (piperidinomethylene)bis(phosphonic acid) derivatives were prepared and their activity to inhibit a rise in serum calcium induced by parathyroid hormone in thyroparathyroidectomised rats was evaluated. Several (4- alkylidene-, 4,4-dialkyl-, or 4-alkyl-4- halopiperidinomethylene)bis(phosphonic acid) derivatives showed considerable inhibitory activity. But compounds having aromatic and polar substituents such as azido, hydroxy, amino and amido on the piperidine ring were generally inactive. In this study, two 4-alkylidene compounds (8a and 8b) and a 4,4- cyclic dialkyl compound (61) showed potent activity when administered either intravenously or perorally.
- Mimura,Hayashida,Nomiyama,Ikegami,Iida,Tamura,Hiyama,Ohishi
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p. 1971 - 1986
(2007/10/02)
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