首页> 外国专利> New 1-(substituted methylene)-1H-indene derivatives, are Ras protein modulators useful for treating tumor or inflammatory diseases

New 1-(substituted methylene)-1H-indene derivatives, are Ras protein modulators useful for treating tumor or inflammatory diseases

机译:新的1-(取代亚甲基)-1H-茚衍生物是Ras蛋白调节剂,可用于治疗肿瘤或炎性疾病

摘要

1-(Cyclopentadienyl-, furanyl-, thienyl- or pyrrolyl-methylene)-3-(substituted methyl)-1H-indene derivatives (I) are new. 1-(Cyclopentadienyl-, furanyl-, thienyl- or pyrrolyl-methylene)-3-(substituted methyl)-1H-indene derivatives of formula (I) and their salts and isomers are new. A1-A2-A3 = -X-C(R9)=C(R10)- or -C(R9)=C(R10)-X-; R1 - R11 = H, D (deuterium), halo, up to 8C, linear, branched or cyclic, saturated or unsaturated, optionally substituted hydrocarbyl (e.g. alkyl, cycloalkyl, aryl, alkaryl or alkaryl; optionally bonded to the basic structure via O (as e.g. in OMe) or S (as e.g. in SMe)), mono- or dihydrocarbylamino (e.g. NHMe, NMe2 or NHEt), NO2, CN, COOH, OSO3H, OH, CH2OH, NH2, amidino, guanidino or aminoacetate (at least one substituent preferably being halo, NH2, CN, COOH, 1-6C alkoxy or OH); or two adjacent groups may be linked to form a saturated or unsaturated carbocyclic or heterocyclic ring system; Q = NO2, CN, COOH, OSO3H, OH, CH2OH, OMe, amidino, guanidino, aminoacetate or COOR12; R12 = linear, branched or cyclic, saturated or unsaturated, optionally substituted hydrocarbyl or 1-8C alkoxy (where the substituents are preferably one or more of halo, NH2, CN, COOH, 1-6C alkoxy or OH); X = O, S, CR13R14 or NR15; and R13 - R15 = linear, branched or cyclic, saturated or unsaturated, optionally substituted hydrocarbyl, alkylthio or 1-8C alkoxy (where the substituents are preferably one or more of halo, NH2, CN, COOH, 1-6C alkoxy or OH). An Independent claim is included for the use of the cell lines MDCK (canine epithelial kidney cells) and/or C57MG (murine epithelial mammary gland cells) as test system for detecting the biological activity of test agents.
机译:1-(环戊二烯基-,呋喃基-,噻吩基-或吡咯基-亚甲基)-3-(取代的甲基)-1H-茚衍生物(I)是新的。式(I)的1-(环戊二烯基-,呋喃基-,噻吩基-或吡咯基-亚甲基)-3-(取代的甲基)-1H-茚衍生物及其盐和异构体是新的。 A1-A2-A3 = -X-C(R9)= C(R10)-或-C(R9)= C(R10)-X-; R1-R11 = H,D(氘),卤素(最高8C),直链,支链或环状,饱和或不饱和,可选取代的烃基(例如烷基,环烷基,芳基,烷芳基或烷芳基;可选地通过O与基本结构键合) (例如在OMe中)或S(例如在SMe中)),单或二烃基氨基(例如NHMe,NMe2或NHEt),NO2,CN,COOH,OSO3H,OH,CH2OH,NH2,a基,胍基或氨基乙酸(在至少一个取代基,优选为卤素,NH 2,CN,COOH,1-6C烷氧基或OH);或两个相邻的基团可连接形成饱和或不饱和的碳环或杂环系统; Q = NO2,CN,COOH,OSO3H,OH,CH2OH,OMe,a基,胍基,氨基乙酸或COOR12; R12 =直链,支链或环状,饱和或不饱和的,任选取代的烃基或1-8C烷氧基(其中取代基优选为卤素,NH2,CN,COOH,1-6C烷氧基或OH中的一种或多种); X = O,S,CR13R14或NR15;和R13-R15 =直链,支链或环状,饱和或不饱和的,任选取代的烃基,烷硫基或1-8C烷氧基(其中取代基优选为卤素,NH2,CN,COOH,1-6C烷氧基或OH中的一种或多种) 。包括独立权利要求,其涉及细胞系MDCK(犬上皮肾细胞)和/或C57MG(鼠上皮乳腺细胞)作为检测系统以检测测试剂的生物学活性。

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