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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| creator | LIUKKO-SIPI,SIRPA NIKANDER,HANNU KLEIMOLA,TERTTU SELLMAN,RAIJA VAEAENAENEN,KALERVO HEIKKILAE-HOIKKA,MARJAANA HANNUNIEMI,RITVA LAUREN,LEENA |
| description | 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. |
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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.</description><language>eng ; fin ; swe</language><subject>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</subject><creationdate>2006</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20060531&DB=EPODOC&CC=FI&NR=117053B$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20060531&DB=EPODOC&CC=FI&NR=117053B$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>LIUKKO-SIPI,SIRPA</creatorcontrib><creatorcontrib>NIKANDER,HANNU</creatorcontrib><creatorcontrib>KLEIMOLA,TERTTU</creatorcontrib><creatorcontrib>SELLMAN,RAIJA</creatorcontrib><creatorcontrib>VAEAENAENEN,KALERVO</creatorcontrib><creatorcontrib>HEIKKILAE-HOIKKA,MARJAANA</creatorcontrib><creatorcontrib>HANNUNIEMI,RITVA</creatorcontrib><creatorcontrib>LAUREN,LEENA</creatorcontrib><title>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</title><description>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.</description><subject>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM</subject><subject>CHEMISTRY</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2006</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqFjrEKwkAQRNNYiPoNbmdjgiIiWCqKNmJhH9bcGhcut0f2otwv-ZVGFLGzGKaYecN0k8eB7uBjzYZdtClW7GRZUbhGy4YcwZl16a-irRwXgAUbMFTzTTNIoVEyEARCTRjgLC1gWAmVgLIyA9FAYmNoyd9QwTT04iq0XDp0RRzDEUsKI_0OoDNv3kstytpPOhe0SoOP95LhdnNa71LykpN6LNq_Id_up9PFZD5brWb_G09EoFel</recordid><startdate>20060531</startdate><enddate>20060531</enddate><creator>LIUKKO-SIPI,SIRPA</creator><creator>NIKANDER,HANNU</creator><creator>KLEIMOLA,TERTTU</creator><creator>SELLMAN,RAIJA</creator><creator>VAEAENAENEN,KALERVO</creator><creator>HEIKKILAE-HOIKKA,MARJAANA</creator><creator>HANNUNIEMI,RITVA</creator><creator>LAUREN,LEENA</creator><scope>EVB</scope></search><sort><creationdate>20060531</creationdate><title>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</title><author>LIUKKO-SIPI,SIRPA ; NIKANDER,HANNU ; KLEIMOLA,TERTTU ; SELLMAN,RAIJA ; VAEAENAENEN,KALERVO ; HEIKKILAE-HOIKKA,MARJAANA ; HANNUNIEMI,RITVA ; LAUREN,LEENA</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_FI117053BB3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; fin ; swe</language><creationdate>2006</creationdate><topic>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM</topic><topic>CHEMISTRY</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>LIUKKO-SIPI,SIRPA</creatorcontrib><creatorcontrib>NIKANDER,HANNU</creatorcontrib><creatorcontrib>KLEIMOLA,TERTTU</creatorcontrib><creatorcontrib>SELLMAN,RAIJA</creatorcontrib><creatorcontrib>VAEAENAENEN,KALERVO</creatorcontrib><creatorcontrib>HEIKKILAE-HOIKKA,MARJAANA</creatorcontrib><creatorcontrib>HANNUNIEMI,RITVA</creatorcontrib><creatorcontrib>LAUREN,LEENA</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>LIUKKO-SIPI,SIRPA</au><au>NIKANDER,HANNU</au><au>KLEIMOLA,TERTTU</au><au>SELLMAN,RAIJA</au><au>VAEAENAENEN,KALERVO</au><au>HEIKKILAE-HOIKKA,MARJAANA</au><au>HANNUNIEMI,RITVA</au><au>LAUREN,LEENA</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>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</title><date>2006-05-31</date><risdate>2006</risdate><abstract>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.</abstract><oa>free_for_read</oa></addata></record> |
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| subjects | 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 |
| title | 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 |
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