Substituted pyrazolopyrimidinylamino-indazoles

摘要

The present invention relates to substituted pyrazolopyrimidinylamino-indazole compounds of formula I, below, as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients;
wherein R1a, R1b, R1c, and R2 are defined herein.

主权项

1. A compound of formula I: in which: R1a, R1b, R1c, R1d are the same or different and are independently selected from R1 R1 represents a hydrogen atom or a halogen atom or a hydroxy-, cyano-, C1-C6-alkyl-, halo-C1-C6-alkyl-, C2-C6-alkenyl-, C2-C6-alkynyl-, C1-C6-alkoxy-, halo-C1-C6-alkoxy-, C3-C6-cycloalkyl-, C3-C6-cycloalkyloxy-,
3- to 10-membered heterocycloalkyl-,(3- to 10-membered heterocycloalkyl)-O—, —NR5aR5b, —SCF3 or —SF5 group;wherein said C1-C6-alkyl-, C2-C6-alkenyl-, C2-C6-alkynyl-, C1-C6-alkoxy-, C3-C6-cycloalkyl-, C3-C6-cycloalkyloxy-, (3- to 10-membered heterocycloalkyl)-, and (3- to 10-membered heterocycloalkyl)-O— group is optionally substituted, identically or differently, with 1, 2, 3, 4 or 5 R4 groups; R2 represents a hydrogen atom or a halogen atom or a group selected from: C1-C6-alkyl-, C3-C6-cycloalkyl-, C2-C6-alkenyl-, C2-C6-alkynyl-,
3- to 10-membered heterocycloalkyl-,4- to 10-membered heterocycloalkenyl-, aryl-, heteroaryl-,halo-C1-C3-alkyl-, cyano-, —(CH2)q—X—(CH2)p—R3;wherein said C1-C6-alkyl-, C3-C6-cycloalkyl-, C2-C6-alkenyl-, C2-C6-alkynyl-, 3- to 10-membered heterocycloalkyl-,4- to 10-membered heterocycloalkenyl-, aryl-, and heteroaryl- group is optionally substituted, identically or differently, with 1, 2, 3, 4 or 5 R4 groups; X represents a bond or a bivalent group selected from: —O—, —S—, —S(═O)—, —S(═O)2—, —S(═O)—(NR3a)—, —(NR3a)—S(═O)—, —S(═O)2—(NR3a)—, —(NR3a)—S(═O)2—, —C(═O)—, —(NR3a)—, —C(═O)—O—, —O—C(═O)—, —C(═S)—O—, —O—C(═S)—, —C(═O)—(NR3a)—, —(NR3a)—C(═O)—, —(NR3a)—C(═O)—(NR3b)—, —O—C(═O)—(NR3a)—, —(NR3a)—C(═O)—O—; R3a, R3b are the same or different and are independently selected from R3; R3 represents a hydrogen atom or a group selected from C1-C6-alkyl-, C3-C6-cycloalkyl-, 3- to 10-membered heterocycloalkyl-, aryl-, heteroaryl-, halo-C1-C3-alkyl-;
wherein said C1-C6-alkyl-, C3-C6-cycloalkyl-, 3- to 10-membered heterocycloalkyl-, aryl-, and heteroaryl- group is optionally substituted, identically or differently, with 1, 2, 3, 4 or 5 R4 groups; or R3 together with R3a or R3b represent a 3- to 10-membered heterocycloalkyl- or a 4- to 10-membered heterocycloalkenyl- group, which is optionally substituted, one or more times, identically or differently, with halo-, hydroxyl-, cyano-; R4 represents halo-, hydroxy-, oxo-(O═), cyano-, nitro-, C1-C6-alkyl-, C2-C6-alkenyl-, C2-C6-alkynyl-, halo-C1-C6-alkyl-, C1-C6-alkoxy-, halo-C1-C6-alkoxy-, hydroxy-C1-C6-alkyl-, C1-C6-alkoxy-C1-C6-alkyl-, halo-C1-C6-alkoxy-C1-C6-alkyl-, R5—O—, —C(═O)—R5, —C(═O)—O—R5, —O—C(═O)—R5,
—N(R5a)—C(═O)—R5b, —N(R5a)—C(═O)—NR5bR5c, —NR5aR5b, —C(═O)—NR5aR5b, R5—S—, R5—S(═O)—, R5—S(═O)2—, —N(R5a)—S(═O)—R5b, —S(═O)—NR5aR5b, —N(R5a)—S(═O)2—R5b, —S(═O)2—NR5aR5b, —S(═O)(═NR5a)R5b, —S(═O)(═NR5a)R5b or —N═S(═O)(R5a)R5b; R5a, R5b, R5c are the same or different and are independently selected from R5; R5 represents a hydrogen atom, a C1-C6-alkyl- or a C3-C6-cycloalkyl- group; or R5a and R5b, or R5a and R5c, or R5b and R5c together may form a C2-C6-alkylene group, in which one methylene is optionally replaced by —O—, —C(═O)—, —NH—, or —N(C1-C4-alkyl)-; p represents an integer of 0, 1, 2 or 3; q represents an integer of 0, 1, 2 or 3; or a tautomer, an N-oxide, a solvate, or a pharmaceutically acceptable salt thereof, or a mixture of same.