发明名称 NOVEL COMPOUNDS
摘要 The present invention relates to substituted N-(phenyl-heteroaryl)-3-acetylamino-benzamides and N-[3-(acetylamino)phenyl]-phenyl-heteroaryl-carboxamides of general formula (I) 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 such as cancer, wherein i.a.: LA represents an optionally substituted methylene or ethylene group; LB represents —N(H)—C(═0)- or —C(═0)—N(H)—; R1 represents an optionally substituted 5- to 8-membered heterocycloalkyl, 4- to 10-membered heterocycloalkenyl, aryl, heteroaryl or —N(R7)(Ci-C6-alkyl) group; R2 represents an optionally substituted 5- or 6-membered heteroaryl group; R3 represents an optionally substituted phenyl group.;
申请公布号 US2016263122(A1) 申请公布日期 2016.09.15
申请号 US201414778568 申请日期 2014.03.17
申请人 BAYER PHARMA AKTIENGESELLSCHAFT 发明人 THEDE Kai;SCOTT William;BENDER Eckhard;GOLZ Stefan;HÄGEBARTH Andrea;LIENAU Philip;PUEHLER Florian;BASTING Daniel;SCHNEIDER Dirk;MOWES Manfred;RICHTER Anja;ZORN Ludwig;LIU Ningshu;MONNING Ursula;SIEGEL Franziska
分类号 A61K31/5377;C07C205/45;C07D213/75;C07C233/54;C07D295/15;C07C233/15;C07D213/82;C07D333/38;C07D285/135;C07D295/155;C07C205/59;C07C317/44;C07C229/64;C07D213/76;C07D213/73;C07C255/56;A61K31/5386;A61K31/4439;A61K31/496;A61K31/433;A61K31/4418;A61K31/4995;A61K31/551;A61K31/553;A61K45/06;C07D277/56 主分类号 A61K31/5377
代理机构 代理人
主权项 1. A compound of formula (I): in which: LA represents a methylene or ethylene group, said methylene or ethylene group being optionally substituted, one or more times, identically or differently, with a substituent selected from: hydroxy-, cyano-, C1-C3-alkoxy-, hydroxy-C1-C3-alkyl-,halo-C1-C3-alkoxy-, C3-C7-cycloalkyl-, 3- to 10-membered heterocycloalkyl-;or, when two substituents are present at the same carbon atom, the two substituents, together with the carbon atom they are attached to, may form a C3-C6-cycloalkyl- or 3- to 6-membered heterocycloalkyl- ring; wherein said ring is optionally substituted one or more times, identically or differently, with a substituent selected from:halo-, hydroxy-, cyano-, C1-C3-alkyl-, C1-C3-alkoxy-; LB represents —N(H)—C(═O)— or —C(═O)—N(H)—; R1 represents a group selected from: 5- to 8-membered heterocycloalkyl-, 4- to 10-membered heterocycloalkenyl-, aryl-, heteroaryl-, and —N(R7)—(C1-C6-alkyl); wherein said 5- to 8-membered heterocycloalkyl-, 4- to 10-membered heterocycloalkenyl-, aryl-, heteroaryl-, and —N(R7)—(C1-C6-alkyl) group is optionally substituted, one or more times, identically or differently, with a substituent selected from: halo-, hydroxy-, cyano-, C1-C3-alkoxy-, hydroxy-C1-C3-alkyl-, halo-C1-C3-alkoxy-, C3-C7-cycloalkyl-; R2 represents a group selected from: wherein “*” indicates the point of attachment to R3, and “**” indicates the point of attachment to LB; wherein said group is optionally substituted, one or more times, identically or differently, with a C1-C3-alkyl- group; R3 represents a phenyl-group, said phenyl-group being optionally substituted, one or more times, identically or differently, with a substituent selected from:halo-, hydroxy-, —N(R9)(R10), —N(H)C(═O)R9, cyano-, nitro-, C1-C3-alkyl-, C1-C3-alkoxy-,halo-C1-C3-alkyl-, hydroxy-C1-C3-alkyl-, amino-C1-C3-alkyl-, halo-C1-C3-alkoxy-; R4 represents a hydrogen atom or a C1-C3-alkyl- group; R5 represents a hydrogen atom or a halogen atom or a group selected from: cyano-, C1-C3-alkyl-, C1-C3-alkoxy-; R6 represents a group selected from: C1-C6-alkyl-, C2-C6-alkenyl-, C2-C6-alkynyl-,C1-C6-alkoxy-, C3-C6-cycloalkoxy-, halo-, hydroxy-, cyano-, aryl-,heteroaryl-, —N(R9)(R10), —C(═O)—O—C1-C4-alkyl, —C(═O)—N(R9)(R10, R9—S—, R9—S(═O)—, R9—S(═O)2—;said C1-C6-alkyl-, C2-C6-alkenyl-, C2-C6-alkynyl-, aryl-, heteroaryl-, and C1-C6-alkoxy- group being optionally substituted, one or more times, identically or differently, with a substituent selected from: halo-, cyano-, nitro-, hydroxy-, C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkoxy-, hydroxy-C1-C3-alkoxy-, C1-C3-alkoxy-C2-C3-alkoxy-,C3-C7-cycloalkyl-, C4-C7-cycloalkenyl-,3- to 10-membered heterocycloalkyl-, 4- to 10-membered heterocycloalkenyl-,aryl-, heteroaryl-, —C(═O)R9, —C(═O)O—(C1-C4-alkyl), —OC(═O)—R9, —N(H)C(═O)R9, —N(R10)C(═O)R9,—N(H)C(═O)NR10R9, —N(R11)C(═O)NR10R9, —N(H)R9, —NR10R9,—C(═O)N(H)R9, —C(═O)NR10R9, R9—S—, R9—S(═O)—, R9—S(═O)2—,—N(H)S(═O)R9, —N(R10S(═O)R9, —S(═O)N(H)R9, —S(═O)NR10R9,—N(H)S(═O)2R9, —N(R9)S(═O)2R10, —S(═O)2N(H)R9, —S(═O)2NR10R9,—S(═O)(═NR10R9, —N═S(═O)(R10R9; R7 represents a hydrogen atom or a C1-C3-alkyl- or C1-C3-alkoxy-C1-C3-alkyl- group; R9, R10, R11 represent, independently from each other, a hydrogen atom or a C1-C3-alkyl- or C1-C3-alkoxy-C1-C3-alkyl- group; or R9R10 together with the atom or the group of atoms they are attached to, form a 3- to 10-membered heterocycloalkyl- or 4- to 10-membered heterocycloalkenyl- group; m represents 0, 1, or 2; or a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.
地址 Berlin DE