New pyridinyl-amino:methylidene bis:phosphonic acid derivs. - used to treat bone disease e.g. osteolytic bone diseases due to malignancy, Paget's disease and osteoporosis

New pyridinyl-amino:methylidene bis:phosphonic acid derivs. - used to treat bone disease e.g. osteolytic bone diseases due to malignancy, Paget's disease and osteoporosis

Pyridinyl-aminomethylidene bisphosphonic acid tetraesters of formula (I) are new: R1-R4 = 1-5C alkyl; X, Y = H, 1-5C alkyl, halo, OH, 1-5C alkoxy, benzyloxy, acyloxy, NO2, CF3 or NR5R6; R5, R6 = H, 1-5C alkyl or acyl. Also claimed is the use of (I) for the treatment of bone diseases, and a pharmaceu...

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Hauptverfasser: LIUKKO-SIPI,SIRPA, NIKANDER,HANNU, KLEIMOLA,TERTTU, SELLMAN,RAIJA, VAEAENAENEN,KALERVO, HEIKKILAE-HOIKKA,MARJAANA, HANNUNIEMI,RITVA, LAUREN,LEENA
Format: Patent
Sprache:eng ; fin ; swe
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ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Zusammenfassung:Pyridinyl-aminomethylidene bisphosphonic acid tetraesters of formula (I) are new: R1-R4 = 1-5C alkyl; X, Y = H, 1-5C alkyl, halo, OH, 1-5C alkoxy, benzyloxy, acyloxy, NO2, CF3 or NR5R6; R5, R6 = H, 1-5C alkyl or acyl. Also claimed is the use of (I) for the treatment of bone diseases, and a pharmaceutical compsn. contg. (I). In an example, 0.2 moles 2-aminopyridine were mixed with 0.8 mol triethylorthoformate and BF3.OEt2 and the mixt.heated at 150[deg]C for 4 hr. and the EtOH formed was distilled off. Triethylorthoformate was distilled off in vacuum. 0.4 mol diethylphosphite was then added to the reaction mixt. which was heated at 150[deg]C while distilling off the EtOH formed. The mixt. was cooled and the prod. purified to give 29g ((2-pyridinylamino) methylidene)bisphosphonic acid tetraethyl ester.