1351813-02-9Relevant articles and documents
COMPOUND SERVING AS IRAK INHIBITOR
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, (2021/10/07)
The present disclosure relates a compound as an IRAK inhibitor. Specifically, the present disclosure provides a compound of formula I, or a cis-trans isomer, an optical isomer, a racemate, a pharmaceutically acceptable salt, a prodrug, a deuterated derivative thereof, a hydrate or a solvate thereof. The compounds disclosed herein have potent inhibitory effects on IRAK and thus have therapeutic effect on IRAK-related diseases.
N-HETEROARYL INDAZOLE DERIVATIVES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
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, (2020/05/28)
The present invention is directed to substituted certain N-heteroaryl indazole derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.
PYRIDONE DERIVATIVES AND THEIR USE AS KINASE INHIBITORS
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Page/Page column 196; 197, (2017/05/10)
Disclosed in the present application is a compound of formula (I) as defined herein as well as a pharmaceutical composition comprising said compound. Further disclosed in the present application is the use of such pharmaceutical compositions for treating diseases, namely inter alia for use in the treatment of cancer, metabolic, inflammatory, autoimmune and viral diseases. The compounds disclosed herein are inhibitors of MNK1 and/or MNK2 kinases.
Indazole Compounds as IRAK4 Inhibitors
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, (2016/11/28)
The present invention provides indazole compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors, wherein Z1, Z2, R1, R2, R3, ‘m’ and ‘n’ have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical compositions comprising at least one of the compounds of the compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.
INDAZOLE COMPOUNDS AS IRAK4 INHIBITORS
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, (2015/07/23)
The present invention provides indazole compound of formula (I), which are therapeutically useful as kinase inhibitor, particularly IRAK4 inhibitors. wherein Z1, Z2, R1, R2, R3, 'm' and 'n' have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomers thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
THIENOPYRIMIDINES AS MKNK1 AND MKNK2 INHIBITORS
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Page/Page column 237, (2015/06/08)
The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compos
Indazole-based potent and cell-active Mps1 kinase inhibitors: Rational design from pan-kinase inhibitor anthrapyrazolone (SP600125)
Kusakabe, Ken-Ichi,Ide, Nobuyuki,Daigo, Yataro,Tachibana, Yuki,Itoh, Takeshi,Yamamoto, Takahiko,Hashizume, Hiroshi,Hato, Yoshio,Higashino, Kenichi,Okano, Yousuke,Sato, Yuji,Inoue, Makiko,Iguchi, Motofumi,Kanazawa, Takayuki,Ishioka, Yukichi,Dohi, Keiji,Kido, Yasuto,Sakamoto, Shingo,Yasuo, Kazuya,Maeda, Masahiro,Higaki, Masayo,Ueda, Kazuo,Yoshizawa, Hidenori,Baba, Yoshiyasu,Shiota, Takeshi,Murai, Hitoshi,Nakamura, Yusuke
, p. 4343 - 4356 (2013/07/19)
Monopolar spindle 1 (Mps1) is essential for centrosome duplication, the spindle assembly check point, and the maintenance of chromosomal instability. Mps1 is highly expressed in cancer cells, and its expression levels correlate with the histological grades of cancers. Thus, selective Mps1 inhibitors offer an attractive opportunity for the development of novel cancer therapies. To design novel Mps1 inhibitors, we utilized the pan-kinase inhibitor anthrapyrazolone (4, SP600125) and its crystal structure bound to JNK1. Our design efforts led to the identification of indazole-based lead 6 with an Mps1 IC50 value of 498 nM. Optimization of the 3- and 6-positions on the indazole core of 6 resulted in 23c with improved Mps1 activity (IC50 = 3.06 nM). Finally, application of structure-based design using the X-ray structure of 23d bound to Mps1 culminated in the discovery of 32a and 32b with improved potency for cellular Mps1 and A549 lung cancer cells. Moreover, 32a and 32b exhibited reasonable selectivities over 120 and 166 kinases, respectively.
