http://rdf.ncbi.nlm.nih.gov/pubchem/patent/UA-100640-C2

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c011cfdb5f40aeb932d4510bf12de543
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-662
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filingDate 2011-12-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c6606bad0befb0b658d2aaa266292b73
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publicationDate 2013-01-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber UA-100640-C2
titleOfInvention CALIQUE-CALIFORNIA CALIFORNIA
abstract The invention relates to bioorganic chemistry, namely the synthesis of calixarene-1-hydroxymethylene-1,1-bisphosphonic acids of General formula, where R = H, X = OH, Y = OCHCHCH (compound A), R = CH (OH) [PO (OH)], X = OH, Y = ONSNSN (compound B), and the study of their properties as inhibitors of protein tyrosine phosphatase 1B. In the in vitro system, compounds (A) and (B) demonstrate inhibitory capacity for human RTP1B with ICV micromolar range and selectivity over other protein tyrosine phosphatases (TC-RTR, PTP-LAR). Compounds (A) and (B) are recommended as inhibitors of protein tyrosine phosphatase 1B and can be used in biology, pharmacology and medicine. [The invention relates to bioorganic chemistry, namely the synthesis of calixaren-1-hydroxymethylene-1,1-bisphosphonic acids of the general formula where R = H, X = OH, Y = OCHCHCH (compound A), R = CH (OH) [PO (OH)], X = OH, Y = OCHSCH (compound B), and study their properties as protein tyrosine phosphatase 1B inhibitors Compounds (A) and (B) are prepared by the sequential reaction of calix [4] arecarbonyl chlorides with trimethylsilyl phosphite and methanol. In the in vitro system, compounds (A) and (B) demonstrate inhibitory capacity for human RTP1B with IC in the micromolar range and selectivity over other protein tyrosine phosphatases (TC-RTP, PTP-LAR). Compounds (A) and (B) are recommended as inhibitors of protein tyrosine phosphatase 1B and can find applications in biology, pharmacology and medicine.
priorityDate 2011-12-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 33.