发明名称 Substituted benzothienyl-pyrrolotriazines and uses thereof
摘要 This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
申请公布号 US9475815(B2) 申请公布日期 2016.10.25
申请号 US201314380755 申请日期 2013.02.20
申请人 BAYER INTELLETUAL PROPERTY GMBH 发明人 Lobell Mario;Hübsch Walter;Schirok Hartmut;Héroult Mélanie;Brohm Dirk;Collin Marie-Pierre;Grünewald Sylvia;Lustig Klemens;Bömer Ulf;Voehringer Verena;Lindner Niels
分类号 C07D487/04;C07D409/04;C07D409/14;A61K31/53;A61K31/4985;A61K31/4427;A61P35/00;A61K31/5377;A61K31/5513;C07D519/00 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, and G represents the group —CH2—OR3, —CH2—NR4R5 or —C(═O)—NR6R7, wherein R3 is (C1-C6)-alkyl substituted with a residue selected from the group consisting of amino, mono-(C1-C4)-alkylamino, di-(C1-C4)-alkylamino, aminocarbonyl, mono-(C1-C4)-alkylaminocarbonyl, di-(C1-C4)-alkylaminocarbonyl and 4- to 6-membered heterocycloalkyl, or is 4- to 6-membered heterocycloalkyl,wherein said 4- to 6-membered heterocycloalkyl groups are optionally substituted with one or two residues independently selected from the group consisting of (C1-C4)-alkyl, oxo, hydroxy, amino and aminocarbonyl,R4 is hydrogen or (C1-C4)-alkyl,R5 is (C1-C6)-alkyl substituted with one or two residues independently selected from the group consisting of hydroxy, (C1-C4)-alkoxy, amino, mono-(C1-C4)-alkylamino, di-(C1-C4)-alkylamino, hydroxycarbonyl, aminocarbonyl, mono-(C1-C4)-alkylamino-carbonyl, di-(C1-C4)-alkylaminocarbonyl, (C1-C4)-alkylcarbonylamino, aminocarbonylamino and 4- to 6-membered heterocycloalkyl, wherein said 4- to 6-membered heterocycloalkyl is optionally substituted with one or two residues independently selected from the group consisting of (C1-C4)-alkyl, oxo, hydroxy, amino and amino-carbonyl, oris (C1-C4)-alkylcarbonyl optionally substituted with a residue selected from the group consisting of hydroxy, (C1-C4)-alkoxy, amino, mono-(C1-C4)-alkylamino and di-(C1-C4)-alkylamino, oris (C3-C6)-cycloalkyl optionally substituted with one or two residues independently selected from the group consisting of (C1-C4)-alkyl, hydroxy, (C1-C4)-alkoxy, amino, mono-(C1-C4)-alkylamino and di-(C1-C4)-alkylamino, oris 4- to 6-membered heterocycloalkyl optionally substituted with one or two residues independently selected from the group consisting of (C1-C4)-alkyl, oxo, hydroxy, amino and aminocarbonyl,orR4 and R5 are joined and, taken together with the nitrogen atom to which they are attached, form a mono- or bicyclic, saturated, 4- to 10-membered heterocycloalkyl ring which may contain a second ring heteroatom selected from N and O, and which may be substituted with up to three residues independently selected from the group consisting of (C1-C4)-alkyl, oxo, hydroxy, (C1-C4)-alkoxy, amino, mono-(C1-C4)-alkylamino, di-(C1-C4)-alkylamino, azetidino, pyrrolidino, piperidino, (C1-C4)-alkyl-carbonyl, (C3-C6)-cycloalkylcarbonyl, hydroxycarbonyl, am inocarbonyl, mono-(C1-C4)-alkylaminocarbonyl, di-(C1-C4)-alkylaminocarbonyl, thienyl and phenyl, wherein the alkyl groups of said (C1-C4)-alkyl, (C1-C4)-alkoxy, mono-(C1-C4)-alkylamino, di-(C1-C4)-alkylamino and (C1-C4)-alkyl-carbonyl residues, for their part, are optionally substituted with a residue selected from the group consisting of hydroxy, amino and am inocarbonyl,andwherein said thienyl and phenyl groups are optionally substituted with one or two residues independently selected from the group consisting of fluoro, chloro, cyano, methyl and trifluoromethyl,orR4 and R5 are joined and, taken together with the nitrogen atom to which they are attached, form an imidazol-1-yl or 1,2,4-triazol-1-yl ring each of which may be substituted with one or two residues independently selected from the group consisting of (C1-C4)-alkyl and cyano,R6 is hydrogen,R7 is 4- to 6-membered heterocycloalkyl optionally substituted with one or two residues independently selected from the group consisting of (C1-C4)-alkyl, oxo, hydroxy, amino and aminocarbonyl,orR6 and R7 are joined and, taken together with the nitrogen atom to which they are attached, form a monocyclic, saturated, 4- to 7-membered heterocycloalkyl ring which may contain a second ring heteroatom selected from N and O, and which may be substituted with one or two residues independently selected from the group consisting of (C1-C4)-alkyl, oxo, hydroxy, amino, mono-(C1-C4)-alkylamino, di-(C1-C4)-alkyl-amino and aminocarbonyl, or a pharmaceutically acceptable salt thereof.
地址 Monheim am Rhein DE