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US 2021/0230150 A1Published application
Compounds for use in preventing or treating cancer
AssigneesFUNDAClÓ HOSPITAL UNIVERSITARI VALL D'HEBRON- INSTITUT DE RECERCA, Institut Univ. De CièNcia I Tecnologia, S. A.
InventorsJosep ROMA CASTANYER, Marta PASCUAL GILABERT, José SÁNCHEZ DE TOLEDO CODINA, Soledad GALLEGO MELCÓN, Patricia ZARZOSA MARTÍNEZ, Javier ALONSO FERNÁNDEZ, Sergio PÉREZ OZCÁRIZ, Cristina LÓPEZ GÓMEZ, Josep CASTELLS BOLIART
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Abstract
The present invention relates to compounds of formula (I) for use in preventing and/or treating cancer.
Claims15
A compound having formula (I)
- and the salts and stereoisomers thereof, wherein
- R1 is hydrogen;
- OH;
- NH2;
- SH;
- F;
- Cl;
- Br;
- I;
- methyl;
- an optionally substituted alkyl chain;
- an optionally substituted alkenyl chain;
- an optionally substituted alkynyl chain;
- trihaloalkyl;
- OR6;
- NR6R7;
- CN;
- COR6;
- CONR6R7;
- CO2R6;
- C(S)OR6;
- OCONR6R7;
- OCOR6;
- OCO2R6;
- OC(S)OR6;
- NHCONR6R7;
- NHCOR6;
- NR6CO2R7;
- NHCO2R6;
- NHC(S)OR6;
- NO2;
- N3;
- SR6;
- SO3H;
- SO2R6;
- SO2NR6R7 aryl;
- Het;
- an optionally substituted aryl linked by an optionally substituted alkyl, alkenyl, alkynyl chain, aryl or Het;
- or an optionally substituted heterocycle linked by an optionally substituted alkyl, alkenyl or alkynyl chain;
- wherein x is one, two, three, four or five, independently of y, z;
- wherein the phenyl ring bearing substituent R1 is in para position regarding the position “a” of the phenyl ring bearing substituent R2;
- R2 is hydrogen;
- OH;
- NH2;
- SH;
- F;
- Cl;
- Br;
- I;
- methyl;
- an optionally substituted alkyl chain;
- an optionally substituted alkenyl chain;
- an optionally substituted alkynyl chain;
- trihaloalkyl;
- OR6;
- NR6R7;
- CN;
- COR6;
- CONR6R7;
- CO2R6;
- C(S)OR6;
- OCONR6R7;
- OCOR6;
- OCO2R6;
- OC(S)OR6;
- NO2;
- N3;
- NHCONR6R7;
- NHCOR6;
- NR6CO2R7;
- NHCO2R6;
- NHC(S)OR6;
- NO2;
- SO3H;
- SO2R6;
- SO2NR6R7;
- aryl;
- Het;
- an optionally substituted aryl linked by an optionally substituted alkyl, alkenyl, alkynyl chain, aryl or Het;
- or an optionally substituted heterocycle linked by an optionally substituted alkyl, alkenyl or alkynyl chain;
- wherein y is one, two, three, four or five, independently of x, z;
- R3 is hydrogen;
- R4 is hydrogen;
- OH;
- NH2;
- methyl;
- an optionally substituted alkyl chain;
- an optionally substituted alkenyl chain;
- an optionally substituted alkynyl chain;
- an optionally substituted cycloalkyl linked to S through an optionally substituted alkyl chain;
- an optionally substituted cycloalkyl linked to S through an optionally substituted alkenyl chain;
- an optionally substituted cycloalkyl linked to S through an optionally substituted alkynyl chain;
- an optionally substituted cycloalkenyl;
- an optionally substituted cycloalkenyl linked to S through an optionally substituted alkyl chain;
- an optionally substituted cycloalkenyl linked to S through an optionally substituted alkenyl chain;
- an optionally substituted cycloalkenyl linked to S through an optionally substituted alkynyl chain;
- an optionally substituted cycloalkynyl chain;
- an optionally substituted cycloalkynyl linked to S through an optionally substituted alkyl chain;
- an optionally substituted cycloalkynyl linked to S through an optionally substituted alkenyl chain;
- an optionally substituted cycloalkynyl linked to S through an optionally substituted alkynyl chain;
- trihaloalkyl;
- OR6;
- NR6R7;
- CN;
- COR6;
- CONR6R7;
- CO2R6;
- C(S)OR6;
- OCONR6R7;
- OCOR6;
- OCO2R6;
- OC(S)OR6;
- NO2;
- N3;
- NHCONR6R7;
- NHCOR6;
- NR6CO2R7;
- NHCO2R6;
- NHC(S)OR6;
- NO2;
- SO3H;
- SO2R6;
- SO2NR6R7;
- aryl;
- Het;
- an optionally substituted aryl linked by an optionally substituted alkyl, alkenyl, alkynyl chain, aryl or Het;
- or an optionally substituted heterocycle linked by an optionally substituted alkyl, alkenyl or alkynyl chain;
- R5 is hydrogen;
- OH;
- NH2;
- methyl;
- an optionally substituted alkyl chain;
- an optionally substituted alkenyl chain;
- an optionally substituted alkynyl chain;
- an optionally substituted cycloalkyl linked to S through an optionally substituted alkyl chain;
- an optionally substituted cycloalkyl linked to N through an optionally substituted alkenyl chain;
- an optionally substituted cycloalkyl linked to N through an optionally substituted alkynyl chain;
- an optionally substituted cycloalkenyl;
- an optionally substituted cycloalkenyl linked to N through an optionally substituted alkyl chain;
- an optionally substituted cycloalkenyl linked to N through an optionally substituted alkenyl chain;
- an optionally substituted cycloalkenyl linked to N through an optionally substituted alkynyl chain;
- an optionally substituted cycloalkynyl chain;
- an optionally substituted cycloalkynyl linked to N through an optionally substituted alkyl chain;
- an optionally substituted cycloalkynyl linked to N through an optionally substituted alkenyl chain;
- an optionally substituted cycloalkynyl linked to N through an optionally substituted alkynyl chain;
- trihaloalkyl;
- OR6;
- NR6R7;
- CN;
- COR6;
- CONR6R7;
- CO2R6;
- C(S)OR6;
- OCONR6R7;
- OCOR6;
- OCO2R6;
- OC(S)OR6;
- NO2;
- N3;
- NHCONR6R7;
- NHCOR6;
- NR6CO2R7;
- NHCO2R6;
- NHC(S)OR6;
- NO2;
- SO3H;
- SO2R6;
- SO2NR6R7;
- aryl;
- Het;
- an optionally substituted aryl linked by an optionally substituted alkyl, alkenyl, alkynyl chain, aryl or Het;
- or an optionally substituted heterocycle linked by an optionally substituted alkyl, alkenyl or alkynyl chain;
- R6 and R7 are selected, independently of each other, from hydrogen;
- methyl;
- an optionally substituted alkyl chain;
- an optionally substituted alkenyl chain;
- an optionally substituted alkynyl chain;
- an optionally substituted heterocycle;
- and an optionally substituted aryl, preferably phenyl or naphthyl;
- each aryl as a group or part of a group is phenyl, naphthalenyl, anthracenyl, phenantrenyl, biphenyl, optionally fused to Het;
- each optionally substituted with one, two, three or four substituents selected from OH;
- F;
- Cl;
- Br;
- I;
- methyl;
- an optionally substituted alkyl chain;
- an optionally substituted alkenyl chain;
- an optionally substituted alkynyl chain;
- an optionally substituted cycloalkyl;
- an optionally substituted cycloalkenyl;
- an optionally substituted cycloalkynyl;
- OR6;
- NR6R7;
- CN;
- COR6;
- CONR6R7;
- CO2R6;
- C(S)OR6;
- OCONR6R7;
- OCOR6;
- OCO2R6;
- OC(S)OR6;
- N3;
- NHCONR6R7;
- NHCOR6;
- NR6CO2R7;
- NHCO2R6;
- NHC(S)OR6;
- NO2;
- SR6;
- SO3H;
- SO2R6;
- SO2NR6R7;
- aryl;
- Het;
- an optionally substituted aryl linked by an optionally substituted alkyl, alkenyl, alkynyl chain, aryl or Het;
- and an optionally substituted heterocycle linked by an optionally substituted alkyl, alkenyl or alkynyl chain;
- each Het as a group or part of a group is a monocyclic ring with 5, 6 or 7 ring atoms optionally fused to an aryl or a bicyclic ring structure comprising a 5, 6 or 7 membered ring linked to a 4, 5, or 6 membered ring;
- each of the rings being saturated, partially unsaturated, or completely unsaturated;
- at least one of the rings containing 1 to 5 heteroatoms each independently selected from nitrogen, oxygen and sulphur;
- and any one of the rings being optionally substituted with one, two, three or four substituents each independently selected from the group consisting of OH;
- F;
- Cl;
- Br;
- I;
- methyl;
- an optionally substituted alkyl chain;
- an optionally substituted alkenyl chain;
- an optionally substituted alkynyl chain;
- an optionally substituted cycloalkyl;
- an optionally substituted cycloalkenyl;
- an optionally substituted cycloalkynyl;
- OR6;
- NR6R7;
- CN;
- COR6;
- CONR6R7;
- CO2R6;
- C(S)OR6;
- OCONR6R7;
- OCOR6;
- OCO2R6;
- OC(S)OR6;
- N3;
- NO2;
- NHCONR6R7;
- NHCOR6;
- NR6CO2R7;
- NHCO2R6;
- NHC(S)OR6;
- NO2;
- SR6;
- SO3H;
- SO2R6;
- SO2NR6R7;
- aryl;
- Het;
- an optionally substituted aryl linked by an optionally substituted alkyl, alkenyl, alkynyl chain, aryl or Het;
- and an optionally substituted heterocycle linked by an optionally substituted alkyl, alkenyl or alkynyl chain;
- for use in the prevention or treatment of cancer.
258 more elements
Dependencies are inferred from the claim text.