发明名称 Substituted benzothienopyrimidines
摘要 The present invention relates to substituted benzothienopyrimidine compounds of general formula I: in which R1a, R1b, R2a, R2b, and R2c are 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.;
申请公布号 US9296757(B2) 申请公布日期 2016.03.29
申请号 US201314402665 申请日期 2013.05.17
申请人 BAYER PHARMA AKTIENGESELLSCHAFT 发明人 Klar Ulrich;Kettschau Georg;Kosemund Dirk;Pühler Florian;Eis Knut;Lienau Philip;Bömer Ulf;Sülzle Detlev;Wortmann Lars
分类号 C07D495/04;A61K31/38;A61K31/519;A61K45/06;C07D519/00 主分类号 C07D495/04
代理机构 代理人
主权项 1. A compound of general formula I: in which: R1a represents a hydrogen atom or a group selected from: —O—C1-C6-alkyl, —(CH2)r—R8, —(CH2)r—NR3R4, —(CH2)r—N(R4)C(═O)R3, —(CH2)r—N(R4)S(═O)2R3, —(CH2)r—C(═O)OR3, —(CH2)r—C(═O)NR3R4, —(CH2)r—N(R4)C(═O)OR3, —(CH2)r—N(R4)C(═O)N(H)R3, R1b represents a hydrogen atom or a group selected from: C1-C6-alkyl-, —(CH2)r—O—(C1-C6-alkyl); or R1a and R1b together form an oxygen atom or a —O—(C2-C6-alkylene)-O— group; R2a represents a hydrogen atom or a halogen atom or a group selected from: C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, halo-C1-C3-alkoxy-, hydroxy-, cyano-, —N(H)R5, —NR5R4; R2b represents a hydrogen atom or a halogen atom or a group selected from: C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, halo-C1-C3-alkoxy-, hydroxy-, cyano-, —N(H)R5, —NR5R4, —N(H)C(═O)R5, —N(R4)C(═O)R5, —N(H)C(═O)NR5R4, —N(R4)C(═O)NR5R4, —C(═O)N(H)R5, —C(═O)NR5R4; R2c represents a hydrogen atom or a halogen atom or a group selected from: C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, halo-C1-C3-alkoxy-, hydroxy-, cyano-, —N(H)R5, —NR5R4; R3 represents a hydrogen atom or a group selected from: C1-C6-alkyl-, C2-C6-alkynyl-, C3-C6-cycloalkyl-, —(CH2)q—(C3-C6-cycloalkyl), —(CH2)q—O—(C3-C6-cycloalkyl), 3- to 10-membered heterocycloalkyl,—(CH2)q-(3- to 10-membered heterocycloalkyl),—(CH2)q—O-(3- to 10-membered heterocycloalkyl),4- to 10-membered heterocycloalkenyl,—(CH2)q-(4- to 10-membered heterocycloalkenyl),—(CH2)q—O-(4- to 10-membered heterocycloalkenyl),aryl, —(CH2)q-aryl, —(CH2)q—O-aryl, heteroaryl, —(CH2)q-heteroaryl, —(CH2)q—O-heteroaryl, —(3- to 10-membered heterocycloalkyl)-(CH2)q-(3- to 10-membered heterocycloalkyl), -(3- to 10-membered heterocycloalkyl)-(CH2)q-aryl,-(3- to 10-membered heterocycloalkyl)-(CH2)q-heteroaryl,said group being optionally substituted, identically or differently, with 1, 2, 3, 4 or 5 R8 groups; orwhen 2 R8 groups are present ortho to each other on an aryl- or heteroaryl-ring, said 2 R8 groups together form a bridge:*O(CH2)pO*, * NH(C(═O))NH*, wherein * represent the point of attachment to said aryl- or heteroaryl-ring; R4 represents a hydrogen atom or a group selected from: C1-C6-alkyl-, —(CH2)q-aryl, C1-C6-alkoxy-C1-C6-alkyl-; or NR3R4 together represent a 3- to 10-membered heterocycloalkyl group, a benzo fused 3- to 10-membered heterocycloalkyl group or a 4- to 10-membered heterocycloalkenyl group; said 3- to 10-membered heterocycloalkyl or 4- to 10-membered heterocycloalkenyl group being optionally substituted, one or more times, identically or differently, with halo-, hydroxyl-, cyano-, nitro-, C1-C6-alkyl-, 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-, C2-C6-alkenyl-, C2-C6-alkynyl-, C3-C6-cycloalkyl-, —(CH2)q-aryl, —(CH2)q-heteroaryl, —N(R4)C(═O)R5, —NR5R4 or —(CH2)r—C(═O)NR6R7; R5 represents a hydrogen atom, a C1-C6-alkyl- or a C3-C6-cycloalkyl-group; R6 represents a hydrogen atom, a C1-C6-alkyl- or a C3-C6-cycloalkyl-group; R7 represents a hydrogen atom, a C1-C6-alkyl- or a C3-C6-cycloalkyl-group; or NR6R7 together represent a 3- to 10-membered heterocycloalkyl group; R8 represents halo-, azido-, 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, —OC(═O)—R5, —N(H)C(═O)R5, —N(R4)C(═O)R5, —N(H)C(═O)NR5R4, —N(R4)C(═O)NR5R4, —N(R4)C(═O)OR5, —N(H)R5, —NR5R4, —C(═O)N(H)R5, —C(═O)NR5R4, R4—S—, R4—S(═O)—, R4—S(═O)2—, —N(H)S(═O)R4, —N(R4)S(═O)R4, —S(═O)N(H)R5, —S(═O)NR5R4, —N(H)S(═O)2R4, —N(R4)S(═O)2R4, —S(═O)2N(H)R5, —S(═O)2NR5R4, —S(═O)(═NR5)R4, —S(═O)(═NR4)R5 or —N═S(═O)(R5)R4; p represents an integer of 1 or 2; q represents an integer of 1, 2 or 3; r represents an integer of 0, 1 or 2; or a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof.
地址 Berlin DE
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