175137-46-9Relevant articles and documents
2-pyridine substituted urea structural small molecule compounds as well as synthesis and application thereof
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Paragraph 0197; 0588; 0589-0590, (2020/03/03)
The invention relates to 2-pyridine substituted urea structural small molecule compounds as well as synthesis and application thereof. Specifically, the invention discloses the compounds represented by a formula (I) shown in the specification, enantiomers, diastereomers, racemates or a mixture of the compounds, or a pharmaceutically acceptable salt, hydrate and solvate of the compounds, a preparation method of the above materials, and applications of the above materials in preparation of an ASK1 small molecule inhibitor, or medicines for preventing and/or treating diseases related to ASK1, especially liver diseases, lung diseases, cardiovascular diseases, kidney diseases and metabolic diseases.
Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy
Rana, Sandeep,Sonawane, Yogesh A.,Taylor, Margaret A.,Kizhake, Smitha,Zahid, Muhammad,Natarajan, Amarnath
supporting information, p. 3736 - 3740 (2018/10/24)
We synthesized a library of aminopyrazole analogs to systematically explore the hydrophobic pocket adjacent to the hinge region and the solvent exposed region of cyclin dependent kinases. Structure-activity relationship studies identified an optimal substitution for the hydrophobic pocket and analog 24 as a potent and selective CDK2/5 inhibitor.
Novel pyrimidine derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating DRAK relating diseases containing the same as an active ingredient
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Paragraph 0116; 0162; 0225-0227, (2017/08/02)
The present invention relates to a novel pyrimidine derivative, a production method thereof, and a pharmaceutical composition for preventing or treating death-associated protein related apoptosis inducing protein kinase (DRAK)-associated diseases containing the same as an active ingredient. According to the present invention, the novel pyrimidine derivative, an optical isomer thereof, or a pharmaceutically acceptable salt thereof exhibits effective inhibitory activities on DRAK, and thus can be useful for treating diseases caused by DRAK such as cancer and tumor.COPYRIGHT KIPO 2017
BENZENE SULFONAMIDES AS CCR9 INHIBITORS
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Page/Page column 74, (2015/07/15)
The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD).
8-FLUOROPHTHALAZIN-1(2H)-ONE COMPOUNDS
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Paragraph 0376, (2013/05/21)
8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula II for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE
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Page/Page column 192, (2011/11/30)
Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases
Wang, Tao,Lamb, Michelle L.,Scott, David A.,Wang, Haixia,Block, Michael H.,Lyne, Paul D.,Lee, John W.,Davies, Audrey M.,Zhang, Hai-Jun,Zhu, Yanyi,Gu, Fei,Han, Yongxin,Wang, Bin,Mohr, Peter J.,Kaus, Robert J.,Josey, John A.,Hoffmann, Ethan,Thress, Ken,MacIntyre, Terry,Wang, Haiyun,Omer, Charles A.,Yu, Dingwei
scheme or table, p. 4672 - 4684 (2009/07/25)
The design, synthesis and biological evaluation of a series of 4-aminopyrazolylpyrimidines as potent Trk kinase inhibitors is reported. High-throughput screening identified a promising hit in the 4- aminopyrazolylpyrimidine chemotype. Initial optimization of the series led to more potent Trk inhibitors. Further optimization using two strategies resulted in significant improvement of physical properties and led to the discovery of 10z (AZ-23), a potent, orally bioavailable Trk A/B inhibitor. The compound offers the potential to test the hypothesis that modulation of Trk activity will be of benefit in the treatment of cancer and other indications in vivo.
QUINAZOLINE DERIVATIVES
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Page/Page column 120, (2008/06/13)
The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
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, (2008/06/13)
3-ureido-pyrazole derivatives represented by formula (I): where R, R1and R2are as described herein, or pharmnaceutically acceptable salts thereof; are useful, for example, for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.