发明名称 SUBSTITUTED TRIAZOLOPYRIDINES HAVING ACTIVITY AS MPS-1 INHIBITORS
摘要 The present invention relates to substituted triazolopyridine compounds of general formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.;
申请公布号 US2016264568(A1) 申请公布日期 2016.09.15
申请号 US201414896429 申请日期 2014.06.03
申请人 BAYER PHARMA AKTIENGESELLSCHAFT 发明人 SCHULZE Volker K.;SCHALL Andreas;BRIEM Hans;WENGNER Antje Margret;SIEMEISTER Gerhard;STÖCKIGT Detlef;LIENAU Philip
分类号 C07D471/04;C07F5/04;C07F5/02;C07D333/54 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound of formula (I): in which: R1 represents a phenyl- or a pyridyl- group; which is substituted, one or more times, identically or differently, with a substituent selected from: R6—(C1-C6-alkoxy)-, R6—O—, —C(═O)R6, —C(═O)O—R6, —N(H)C(═O)R6, —N(H)C(═O)NR6R7, —NR6R7, —C(═O)N(H)R6, —C(═O)NR6R7, R6—S—, R6—S(═O)2—, —N(H)S(═O)2R6, and —S(═O)2N(H)R6; andwhich is optionally substituted, one or more times, identically or differently, with a substituent selected from: halo-, hydroxy-, nitro-, C1-C6-alkyl-, C1-C6-alkoxy-, hydroxy-C1-C6-alkyl-, —N(H)C(═O)R8, —N(H)C(═O)NR8R7, —C(═O)N(H)R8, and —N(H)S(═O)2R8; R2 represents: wherein * indicates the point of attachment of said group with the rest of the molecule; A represents a 4- to 6-membered heterocyclic ring; which is optionally substituted, one or more times, identically or differently, with halo-, —CN, —OH, nitro-, C1-C6-alkyl-, halo-C1-C6-alkyl-, C1-C6-alkoxy-, halo-C1-C6-alkoxy-, hydroxy-C1-C6-alkyl-, R8—(C1-C6-alkoxy)-, R8—O—, —NR8R7, R8—S—, R8—S(═O)—, R8—S(═O)2—, or (C3-C6-cycloalkyl)-(CH2)n—O—; B represents a 4- to 6-membered heterocyclic ring; which is optionally substituted, one or more times, identically or differently, with halo-, —CN, —OH, nitro-, C1-C6-alkyl-, halo-C1-C6-alkyl-, C1-C6-alkoxy-, halo-C1-C6-alkoxy-, hydroxy-C1-C6-alkyl-, R8—(C1-C6-alkoxy)-, R8—O—, —NR8R7, R8—S—, R8—S(═O)—, R8—S(═O)2—, or (C3-C6-cycloalkyl)-(CH2)n—O—; R3 represents a hydrogen atom; R4 represents a hydrogen atom; R5 represents a hydrogen atom or a C1-C3-alkyl- group; each R5a independently represents a group selected from: halo-, nitro-, C1-C6-alkyl-, halo-C1-C6-alkyl-, C1-C6-alkoxy-, hydroxy-C1-C6-alkyl-, R8—(C1-C6-alkoxy)-, R8—O—, —NR8R7, R8—S—, R8—S(═O)—, R8—S(═O)2—, and (C3-C6-cycloalkyl)-(CH2)n—O—; R6 represents a group selected from: C3-C6-cycloalkyl-, 3- to 10-membered heterocycloalkyl-,aryl-, heteroaryl-, —(CH2)q—(C3-C6-cycloalkyl), —(CH2)q-(3- to 10-membered heterocycloalkyl), —(CH2)q-aryl and —(CH2)q-heteroaryl;wherein said group being optionally substituted, one or more times, identically or differently, with a substituent selected from:halo-, hydroxy-, cyano-, nitro-, C1-C6-alkyl-, halo C1-C6 alkyl, hydroxy-C1-C6-alkyl-, —C6-alkoxy-C1-C6-alkyl-, —C6-alkoxy-C1-C6-alkyl-, R8—(CH2)n(CHOH)(CH2)m—, R8—(C1-C6-alkoxy)-, R8—(CH2)n(CHOH)(CH2)p—O—, R8—(C1-C6-alkoxy-C1-C6-alkyl)-O—, aryl-, R8—O—, —C(═O)R8, —C(═O)O—R8, —OC(═O)—R8, —N(H)C(═O)R8, —N(R7)C(═O)R8, —N(H)C(═O)NR8R7, —N(R7)C(═O)NR8R7, —N(H)R8, —NR8R7, —C(═O)N(H)R8, —C(═O)NR8R7, R8—S(═O)—, R8—S(═O)2—, —N(H)S(═O)R8, —N(R7)S(═O)R8, —S(═O)N(H)R8, —S(═O)NR8R7, —N(H)S(═O)2R8, —N(R7)S(═O)2R8, —S(═O)2N(H)R8, —S(═O)2NR8R7, —S(═O)(═NR8)R7, —S(═O)(═NR7)R8, and —N═S(═O)(R8)R7; R7 represents a C1-C3-alkyl- or a C3-C6-cycloalkyl- group; R8 represents a hydrogen atom or a C1-C6-alkyl- or C3-C6-cycloalkyl- group; wherein said C1-C6-alkyl- or C3-C6-cycloalkyl- group is optionally substituted, one or more times, identically or differently, with a substituent selected from: halo-, hydroxy-, —NHR7, —NR7R7, —N(C1-C3-alkyl)-C(═O)R7, —N(C1-C3-alkyl)-C(═O)OR7, R7—S(═O)2—, C1-C3-alkoxy-, and halo —C3-alkoxy-; or R7 and R8 together with the molecular fragment they are attached to represent a 4- to 6-membered heterocycloalkyl- group, which is optionally substituted, one or more times, identically or differently, with a halogen atom, a C1-C3-alkyl-, halo-C1-C3-alkyl- or C1-C3-alkoxy- group; n, m, and p, represent, independently from each other, an integer of 0, 1, 2 or 3; q represents an integer of 0, 1, 2 or 3; and t represents an integer of 0, 1 or 2;or a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.
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