27-12-2012 дата публикации
Номер: US20120329826A1
Принадлежит:
Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by RON and/or MET. 2. The compound or salt of claim 1 , wherein:X is O;Y is CH;{'sup': '2', 'Ris H or Cl;'}{'sup': '3', 'Ris H; and'}{'sup': 4', '1, 'sub': '3', 'Ris —CH(CH)-A.'}4. The compound or salt of claim 3 , wherein: Ais phenyl substituted by one or more independent halogen or methoxy optionally substituted by 1-3 fluorine atoms.5. The compound or salt of claim 3 , wherein Ais 2 claim 3 ,6-dichloro-3-fluorophenyl.6. The compound or salt of claim 5 , wherein Ris H claim 5 , Caliphatic optionally substituted by cyclic which is optionally substituted claim 5 , —S(O)R claim 5 , or —C(O)OR.7. The compound or salt of claim 5 , wherein Ris H or Caliphatic optionally substituted by cyclic which is optionally substituted.8. The compound or salt of claim 5 , wherein Ris H or Caliphatic optionally substituted by heterocyclic which is optionally substituted.11. The compound or salt of claim 1 , wherein:X is absent;Y is CH;{'sup': '1', 'sub': 1-4', '5-6, 'Ris H or Calkyl optionally substituted by cyclic or aryl which is optionally substituted;'}{'sup': '2', 'Ris H or Cl;'}{'sup': '3', 'Ris H; and'}{'sup': '4', 'sub': '0-3', 'Ris benzofuran-2-yl which can be substituted by 1-3 independent halogen, hydroxy, or —OCaliphatic optionally substituted by 1-3 halogen atoms.'}12. The compound or salt of claim 11 , wherein Ris H.14. The compound or salt of claim 1 , which exhibits inhibition of RON in a biochemical assay with an ICof about 10 mM or less.15. The compound or salt of claim 1 , which exhibits inhibition of MET in a biochemical assay with an ICof about 10 mM or less.16. The compound or salt of any one of the examples herein.17. A pharmaceutical composition comprising the compound or salt of claim 1 , formulated with or without one or more pharmaceutical ...
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