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首页> 外国专利> New pyrimidinone compounds are akt phosphorylation inhibitors useful for treating e.g. thyroid cancer, allergies, asthma, thrombosis, nervous system diseases, retinopathy, psoriasis, rheumatoid arthritis, diabetes and muscle degeneration

New pyrimidinone compounds are akt phosphorylation inhibitors useful for treating e.g. thyroid cancer, allergies, asthma, thrombosis, nervous system diseases, retinopathy, psoriasis, rheumatoid arthritis, diabetes and muscle degeneration

机译：新的嘧啶酮化合物是可用于治疗例如吡咯烷酮的akt磷酸化抑制剂。甲状腺癌，过敏，哮喘，血栓形成，神经系统疾病，视网膜病变，牛皮癣，类风湿性关节炎，糖尿病和肌肉变性

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Pyrimidinone compounds (I) and their racemic forms, enantiomers, diastereoisomers, and addition salts with mineral and organic acids or bases, are new. Pyrimidinone compounds of formula (I) and their racemic forms, enantiomers, diastereoisomers, and addition salts with mineral and organic acids or bases, are new. R : H or alkyl; R1 : H or methyl; R2 : H or F; R3 : H or halo; R4 : H, halo or hydroxyl, alkyl (optionally substituted by halo or OH), or alkoxy (optionally substituted by one or more halo); R5, R5a : H or alkyl group; R6 : H, alkyl (optionally substituted by halo or OH); and R7 : halo. Independent claims are included for: (1) the preparations of (I); and (2) intermediates comprising 2,3-dihydro-1H-indole compounds of formula (Q) (preferably 4-fluoro-2-methyl-2,3-dihydro-1H-indole, 4-fluoro-2-methyl-2,3-dihydro-1H-indole,5,6-difluoro-2-methyl-2,3-dihydro-1H-indole and 4-chloro-5-fluoro-2-methyl-2,3-dihydro-1H-indole), (4-morpholin-4-yl-6-oxo-1,6-dihydro-pyrimidin-2-yl)-acetic acid ethyl ester compound of formula (G) or (L), (4-morpholin-4-yl-6-oxo-1,6-dihydro-pyrimidin-2-yl)-acetic acid metal salt of formula (M) and [2-(4-morpholino-6-oxo-1H-pyrimidin-2-yl)acetyl]oxysodium of formula (H). Y0 : Na, Li or K. [Image] [Image] ACTIVITY : Cytostatic. MECHANISM OF ACTION : Akt phosphorylation inhibitor. The ability of (I) to inhibit akt phosphorylation was tested in human prostate carcinoma (PC3) cell line using multi- spot biomarker detection of meso scale technique. The result showed that 5-fluoro-2-[2-(4-chloro-5-fluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one exhibited an IC 5 0value of 2 nM.
机译：嘧啶酮化合物（I）及其外消旋形式，对映异构体，非对映异构体以及与矿物和有机酸或碱的加成盐是新的。式（I）的嘧啶酮化合物及其外消旋形式，对映异构体，非对映异构体以及与矿物和有机酸或碱的加成盐是新的。 R：H或烷基; R1：H或甲基; R2：H或F; R3：H或卤素; R4：H，卤素或羟基，烷基（任选被卤素或OH取代）或烷氧基（任选被一个或多个卤素取代）; R5，R5a：H或烷基; R6：H，烷基（任选被卤素或OH取代）;和R7：晕。独立索赔包括：（1）（I）的制剂; （2）包含式（Q）的2,3-二氢-1H-吲哚化合物（优选4-氟-2-甲基-2,3-二氢-1H-吲哚，4-氟-2-甲基-2的中间体） ，3-二氢-1H-吲哚，5,6-二氟-2-甲基-2,3-二氢-1H-吲哚和4-氯-5-氟-2-甲基-2,3-二氢-1H-吲哚），式（G）或（L）的（4-吗啉-4-基-6-氧代-1,6-二氢-嘧啶-2-基）-乙酸乙酯化合物，（4-吗啉-4-式（M）的yl-6-氧代-1,6-二氢-嘧啶-2-基）-乙酸金属盐和[2-（4-吗啉代-6-氧代-1H-嘧啶-2-基）乙酰基式（H）的]氧基钠。 Y0：Na，Li或K。[图像] [图像]活动：细胞静止。作用机理：Akt磷酸化抑制剂。使用中观尺度技术的多点生物标志物检测在人前列腺癌（PC3）细胞系中测试了（I）抑制akt磷酸化的能力。结果表明5-氟-2- [2-（4-氯-5-氟-2-甲基-2,3-二氢吲哚-1-基）-2-氧代乙基] -6-吗啉-4- yl-3H-嘧啶-4-酮的IC 5 0值为2 nM。

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