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Indol N-substituted derivative as modulator of PGE2 receptor
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:
PE2018000994
公开号:
PE20181304A1
申请日:
2016.11.17
申请国别(地区):
PE
年份:
2018
代理人:
摘要:
A compound (I) of a formula,Where (R1) n stands for 1,Two or three substitutes in the ring of Indian glycol, which are selected independently from asphalt (1-3 carbon atoms, oxygen (1-3 carbon atoms),R2 is, among other things, a tar (1-4 carbon atoms),Hydrogen halide, or cyanogen; R3 is hydrogen, methyl or trifluoromethyl; R4A and r4b are independent hydrogen, methyl, or R4A and r4b, plus the carbon atom connected with them, representing a cyclopropane-1,1-di-ilo group; r5a and r5b are independent hydrogen, methyl, or r5a and r5b, plus the carbon atom connected with them, They represent a cyclopropane-1,1-di-yl-ilo; AR1 is phenyl or isopropene (1-6 carbon atoms) of 5-6 members,Oxygen (from 1 to 4 carbon atoms)Among other things, these are products of indol n-replacement. It also refers to its formulation, acceptable pharmaceutical salts, pharmacological components and its use as prostate receptor modulator 2 (PGE2): EP2 and / or EP4. They can be used as individual agents or in combination with one or more therapeutic agents and / or chemotherapy to prevent or treat cancer, such as melanoma, lung cancer, kidney cancer, stomach cancer, etc.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 o heteroarilo de 5 a 6 miembros, alquilo (de 1 a 6 atomos de carbono), alcoxilo (de 1 a 4 atomos de
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