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chemical entities with anticancer activity
专利权人:
Fundación Centro Nacional de Investigaciones Oncológicas Carlos III
发明人:
PASTOR FERNANDEZ, Joaquín,FERNANDEZ-CAPETILLO RUIZ, Oscar,MARTINEZ GONZALEZ, Sonia,BLANCO APARICIO, Carmen,RICO FERREIRA, María del Rosario,TOLEDO LAZARO, Luis Ignacio,RODRIGUEZ ARISTEGUI, Sonsoles,MU
申请号:
ES14716910
公开号:
ES2670674T3
申请日:
2014.03.14
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A chemical entity selected from the compounds of Formula (I) ** Formula ** in which R 1 represents a bicyclic heteroaryl selected from the group consisting of indazolyl, indolyl, benzimidazolyl and pyrrolopyridinyl; R2 is selected from NR3SO2R3, alkyl and cycloalkyl; wherein R3 is independently selected at each occurrence from H, alkyl optionally substituted with 1, 2 or 3 halogen atoms, cycloalkyl optionally substituted with 1, 2 or 3 halogen atoms and heterocycloalkyl optionally substituted with 1, 2 or 3 atoms of halogen; and m is 1 or 2; alkyl is a linear saturated hydrocarbon having up to 10 carbon atoms (C1-C10) or a branched saturated hydrocarbon of between 3 and 10 carbon atoms (C3-C10); cycloalkyl is a monocyclic or bicyclic saturated C3-C10 hydrocarbon, which may optionally be condensed with an aryl group; or cycloalkyl is adamantyl; heterocycloalkyl is a saturated monocyclic or bicyclic ring attached to C or attached to 3-10 N members, containing 1, 2, 3 or 4 ring heteroatoms independently selected from N, S and O, in which an atom of N or S in the ring can be substituted with oxygen to form an N-oxide, sulfoxide or sulfone group; aryl is phenyl, biphenyl or naphthyl; and heteroaryl is a monocyclic, bicyclic or tricyclic aromatic ring of 5, 6, 9 or 10, 12, 13 or 14 members, which may contain 1, 2, 3 or 4 ring heteroatoms independently selected from N, S and O; wherein R2 represents alkyl or cycloalkyl, said alkyl or cycloalkyl is substituted with at least one substituent selected from (NR4) nSO2R4, wherein n is 0 or 1, OH and CN; and said alkyl or cycloalkyl is optionally further substituted with 1 or 2 substituents independently selected from halogen, CN, COOR4, CF3, C1-C6 alkyl optionally substituted with 1, 2 or 3 halogen atoms, cycloalkyl optionally substituted with 1, 2 or 3 halogen atoms and O-C1-C6 alkyl optionally substituted with 1, 2 or 3 halogen atoms, or two substituents can be taken in a single atom together with the atom to which they are fi
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