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DERIVADOS DE INDOL N-SUSTITUIDOS COMO MODULADORES DE LOS RECEPTORES DE PGE2
专利权人:
IDORSIA PHARMACEUTICALS LTD.
发明人:
FRETZ, Heinz,LYOTHIER, Isabelle,POTHIER, Julien,RICHARD-BILDSTEIN, Sylvia,SIFFERLEN, Thierry,WYDER PETERS, Lorenza,POZZI, Davide,CORMINBOEUF, Olivier
申请号:
PE0009942018
公开号:
PE13042018A1
申请日:
2016.11.17
申请国别(地区):
PE
年份:
2018
代理人:
摘要:
Refers to a compound of formula (i), wherein n represents 1 (R1), two or three Optional Substituent on the indole ring.Where the substituents are independently selected from alkyl (1 to 3 carbon ATOMS, alkoxyl (1 to 3 carbon Atoms)Among others, R2 is alkyl (1 to 4 carbon ATOMS, or halogeno, cyano R3 is Hydrogen or Methyl trifluoro Methyl and R4A r4b are independently Hydrogen, Methyl,Or R4A r4b and together with the carbon Atom to which they are United, represent a Group cicloprop - 1.1 - Di - ilo r5a and r5b are independently Hydrogen, Methyl,Or r5a and r5b along with the carbon Atom to which they are United, represent a Group cicloprop - 1.1 - Di - ilo AR1 is phenyl or heteroaryl of 5 to 6 members, alkyl of 1 to 6 carbon Atoms)Alkoxyl (1 to 4 carbon Atoms), among others these are n-substituted indole Derivatives.It also relates to their preparation, pharmaceutically acceptable salts of the samePharmaceutical compositions and their use as modulators of the prostaglandin (PGE2) 2 Receptors, EP2 and EP4 \/ or.Can be used as Single agents or in combination with one or more therapeutic agents, and \/ or chemotherapy in the Prevention or treatment of cancer, including melanoma, Lung Cancer,Renal carcinomas, gastrointestinal cancer, among others.Referido a un compuesto de la formula (I), en donde (R1)n representa 1 , dos o tres sustituyentes opcionales sobre el anillo de indol, en donde los sustituyentes se seleccionan independientemente a partir de alquilo (de 1 a 3 atomos de carbono, alcoxilo (de uno a 3 atomos de carbono), entre otros R2 es alquilo (de 1 a 4 atomos de carbono), halogeno, o ciano R3 es hidrogeno, metilo o trifluoro-metilo R4a y R4b son independientemente hidrogeno, metilo, o R4a y R4b junto con el atomo de carbono con el que estan unidos, representan un grupo cicloprop-1,1-di-ilo R5a y R5b son independientemente hidrogeno, metilo, o R5a y R5b junto con el atomo de carbono con el que estan unidos, representan un grupo cicloprop-1,1-di-ilo Ar1 es fenilo
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