50593-92-5Relevant articles and documents
PYRIDO[3,4-d]PYRIMIDINE DERIVATIVE AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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Paragraph 0165; 0166, (2018/04/19)
The purpose of the present invention is to provide a compound having an excellent CDK4/6 inhibiting activity. The present invention is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.
Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy
Huang, Ying,Zhang, Jeff,Yu, Zhengtian,Zhang, Hailong,Wang, Youzhen,Lingel, Andreas,Qi, Wei,Gu, Justin,Zhao, Kehao,Shultz, Michael D.,Wang, Long,Fu, Xingnian,Sun, Yongfeng,Zhang, Qiong,Jiang, Xiangqing,Zhang, Jiangwei,Zhang, Chunye,Li, Ling,Zeng, Jue,Feng, Lijian,Zhang, Chao,Liu, Yueqin,Zhang, Man,Zhang, Lijun,Zhao, Mengxi,Gao, Zhenting,Liu, Xianghui,Fang, Douglas,Guo, Haibing,Mi, Yuan,Gabriel, Tobias,Dillon, Michael P.,Atadja, Peter,Oyang, Counde
supporting information, p. 2215 - 2226 (2017/04/03)
Overexpression and somatic heterozygous mutations of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2), are associated with several tumor types. EZH2 inhibitor, EPZ-6438 (tazemetostat), demonstrated clinical efficacy in patients with acceptable safety profile as monotherapy. EED, another subunit of PRC2 complex, is essential for its histone methyltransferase activity through direct binding to trimethylated lysine 27 on histone 3 (H3K27Me3). Herein we disclose the discovery of a first-in-class potent, selective, and orally bioavailable EED inhibitor compound 43 (EED226). Guided by X-ray crystallography, compound 43 was discovered by fragmentation and regrowth of compound 7, a PRC2 HTS hit that directly binds EED. The ensuing scaffold hopping followed by multiparameter optimization led to the discovery of 43. Compound 43 induces robust and sustained tumor regression in EZH2MUT preclinical DLBCL model. For the first time we demonstrate that specific and direct inhibition of EED can be effective as an anticancer strategy.
IMIDAZOPYRIMIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER
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Paragraph 00283, (2018/04/12)
A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R3, R4, R6, and R7 are as defined herein.
SPIROCYCLIC CETP INHIBITORS
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Page/Page column 29; 30, (2014/07/08)
Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing at
7H-PYRIDO[3,4-D]PYRIMIDIN-8-ONES, THEIR MANUFACTURE AND USE AS PROTEIN KINASE INHIBITORS
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Page/Page column 30-31, (2008/06/13)
Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as we
General and facial synthesis of 2-amino-5-halogenpyrimidine-4-carboxylic acids and their derivatives
Blyumin, Evgeniy V.,Neunhoeffer, Hans,Volovenko, Yulian V.
, p. 2231 - 2241 (2008/02/07)
A facile synthetic approach to 2-amino-5-halogen-pyrimidine-4-carboxylic acids from 5-halogen-2-methylsulfonylpyrimidine-4-carboxylic acid by nucleophilic displacement of the methylsulfonyl group with primary and secondary aliphatic amines has been develo
AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE
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Page/Page column 50, (2010/11/08)
The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.
4-PHENYL-5-OXO-1,4,5,6,7,8-HEXAHYDROQUINOLINE DERIVATIVES THE TREATMENT OF INFERTILITY
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Page/Page column 45-46, (2010/11/24)
The present invention relates to 4-phenyl-5-oxo-l,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R1 is (l-6C)alkyl, (2-6C)alkenyl or (2-6C)aDcynyl; R2, R3 are independently halogen, (l-4C)allcyl, (2-4C)alkenyl, (2-4C)- alkynyl, (1 -4C)aBcoxy, (3-4C)alkenyloxy or (3-4C)alkynyloxy; R4 is phenyl or (2-5C)- heteroaryl, both substituted with R7 and optionally substituted on the (hetero)aromatic ring with one or more substituents selected from hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (l-4C)alkyl, (l-4C)alkoxy , (l-4C)alkylthio and (di)(l-4C)- alkylamino. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 4-phenyl-5-oxo-l, 4,5,6, 7,8-hexahydro- quinoline derivatives in therapy, more specifically for the treatment of infertility
