102294-90-6Relevant articles and documents
Indazole derivative, preparation method and application thereof
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Paragraph 0104; 0107-0108; 0111-0112, (2021/04/26)
The invention relates to an indazole derivative, a preparation method and application thereof, and belongs to the field of chemical medicines. The invention provides a compound shown as a formula I or a pharmaceutically acceptable salt thereof. The invention also provides a preparation method and application of the compound. Biological experiments show that the compounds show an obvious inhibition effect on FGFR1, and part of the compounds can effectively inhibit breast cancer cells, colorectal cancer cells, lung cancer cells and other cancer cells under the condition of single use, so that the compounds have a broad-spectrum anti-cancer effect; besides, the compound also has an obvious inhibiting effect on proliferation of fibroblasts and human hepatic stellate cells, the effect of resisting bleomycin-induced pulmonary fibrosis in an animal body is equivalent to that of a current clinical drug nintedanib for treating pulmonary fibrosis, and the anti-fibrosis curative effect is remarkable. The invention provides a new choice for development and application of anti-cancer and anti-fibrosis drugs.
NEW COMPOUNDS
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Paragraph 0176; 0177, (2014/09/29)
The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions w
The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing
Jones, Clifford D.,Andrews, David M.,Barker, Andrew J.,Blades, Kevin,Daunt, Paula,East, Simon,Geh, Catherine,Graham, Mark A.,Johnson, Keith M.,Loddick, Sarah A.,McFarland, Heather M.,McGregor, Alexandra,Moss, Louise,Rudge, David A.,Simpson, Peter B.,Swain, Michael L.,Tam, Kin Y.,Tucker, Julie A.,Walker, Mike
body text, p. 6369 - 6373 (2009/10/01)
The development of a novel series of imidazole pyrimidine amides as cyclin-dependent kinase (CDK) inhibitors is described. Optimisation of inhibitory potency against multiple CDK's (1, 2 and 9) resulted in imidazole pyrimidine amides with potent in vitro anti-proliferative effects against a range of cancer cell lines. Excellent physiochemical properties and large margins against inhibition of CYP isoforms and the hERG ion channel were achieved by modification of lipophilicity and amine basicity. A candidate with disease model activity in human cancer cell line xenografts and with suitable physiochemical and pharmacokinetic profiles for intravenous (iv) dosing was selected for further development as AZD5597.