1190380-38-1Relevant articles and documents
Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer
Wang, Ao,Wang, Yawan,Meng, Xin,Yang, Yushe
, (2021)
Prostate cancer (PC) is the most common malignancy in men worldwide. Here, two series of novel thiohydantoin derivatives of enzalutamide as potent androgen receptor (AR) antagonists were designed and synthesized. Among them, compound 31c was identified as an AR antagonist which is 2.3–fold more potent than enzalutamide. Molecular docking studies were performed to explain the improved potency of 31c at AR. In cell proliferation assays, 31c exhibited similar anti-proliferative activities with enzalutamide against hormone sensitive LNCaP cells and AR-overexpressing LNCaP/AR cells. These data indicate that 31c can be a good lead compound for further structure optimization for the treatment of prostate cancer.
PYRIDAZINE-3-FORMAMIDE COMPOUND, AND PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
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Paragraph 0666; 0668; 0677-0680, (2022/02/24)
Disclosed in the present invention are a pyridazine-3-formamide compound suitable for inhibiting or regulating the Janus kinase (JAK), in particular tyrosine kinase 2 (TYK2), and a preparation method therefor and the medical use thereof. In particular, disclosed in the present invention are a compound as represented by general formula (I) and a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof, a method for treating and/or preventing Janus kinase-mediated related diseases, in particular autoimmune diseases, inflammatory diseases and cancers, by means of using the compound or the pharmaceutically acceptable salt thereof, and a method for preparing the compound or the pharmaceutically acceptable salt thereof. Each substituent of general formula (I) has the same definition as that in the description.
Diarylurea PI3Kalpha/mTOR double-target inhibitor and pharmaceutical composition, and application of inhibitor and pharmaceutical composition
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Paragraph 0168-0172; 0183-0186, (2021/07/01)
The invention discloses a diarylurea PI3Kalpha/mTOR double-target inhibitor as well as a pharmaceutical composition, and application of the diarylurea PI3K alpha/mTOR double-target inhibitor and the pharmaceutical composition. The diarylurea PI3Kalpha/mTOR double-target inhibitor comprises a substituted triazine compound with a general formula (I) described in the specification, and a stereoisomer, a hydrate or a pharmaceutically acceptable salt thereof. The diarylurea PI3Kalpha/mTOR double-target inhibitor provided by the invention and the pharmaceutical composition containing the diarylurea PI3K alpha/mTOR double-target inhibitor can be used for inhibiting PI3Kalpha/mTOR double kinase and proliferative diseases caused by the PI3Kalpha/mTOR double kinase, and an inhibitor with better effectiveness and selectivity can be provided for treatment of the PI3Kalpha/mTOR double-kinase-induced proliferative diseases.
Pyridazine-3-carboxamide compound and preparation method and application thereof in medicine
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Paragraph 0670-0672; 0681-0684, (2020/03/02)
The invention relates to a pyridazine-3-carboxamide compound suitable for inhibiting or regulating Janus kinase (JAK), especially tyrosine kinase 2 (TYK2), a preparation method of the pyridazine-3-carboxamide compound and an application of the pyridazine-3-carboxamide compound in medicine. Specifically, the invention relates to a compound represented by a general formula (I) and pharmaceutically acceptable salts thereof, a pharmaceutical composition containing the compound or the pharmaceutically acceptable salts thereof, and a method for treating and/or preventing Janus kinase-mediated related diseases, especially autoimmune diseases, inflammatory diseases and cancer by applying the compound or the pharmaceutically acceptable salts thereof, and a preparation method of the compound or thepharmaceutically acceptable salts thereof. Each substituent of the general formula (I) has the same definition as in the specification.
HETEROARYL COMPOUNDS AND USES THEREOF
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, (2016/06/28)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are effective as inhibitors of one or more protein kinases. Such compounds have general formula I or a pharmaceutically acceptable salt thereof, wherein Ring A, Ring B, W, Ry, R3 and R4 are as defined herein.
SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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, (2011/02/24)
Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
PYRIMIDINE DERIVATIVES CAPABLE OF INHIBITING ONE OR MORE KINASES
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, (2009/10/30)
A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, formula (I): wherein: R1 is C3-8-cycloalkyl; X is O, NR7 or C3-6-heterocycloalkyl; R2 is aryl, heteroaryl, fused or unfused aryl-C3-6-heterocycloalkyl or fused or unfused heteroaryl-C3-6-heterocycIoalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C1-6-alkyl, C3-7-cycloalkyl and a group A, wherein said C1-6-alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R10 and a group A, said heteroaryl group is optionally substituted by one or more R10 groups; and wherein said C3-6-heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R3 is C1-6-alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, -NR4R5, -OR6, -NR7(CO)R6, -NR7(CO)NR4R5, -NR7SO2R6, -NR7COOR7, -CONR4R5, C3-6-heterocycloalkyl and formula (a, b, c): wherein R4-7 and A are as defined in the claims. Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of one or more kinases.