- Synthesis method of ponatinib intermediate 3-acetenylimidazo [1, 2-b] pyridazine
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The invention discloses a synthesis method of ponatinib intermediate 3-acetenylimidazo [1, 2-b] pyridazine. The synthesis method comprises the following steps: synthesizing a compound I from 3-pyridazinone and 2-chloroethylamine acid salt under an alkalin
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Paragraph 0034; 0036
(2020/04/22)
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- HETEROARYL SUBSTITUTED AMINOPYRIDINE COMPOUNDS
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Disclosed are compounds of Formula (I) Formula(I) or salts thereof, wherein HET is a heteroaryl selected from oxazolyl, pyrazolyl, imidazo[l,2-b]pyridazin-3-yl, and pyrazolo[l,5-a]pyrimidin-3-yl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a carbon ring atom in the heteroaryl and wherein said heteroaryl is substituted with zero to 2 Rb; and R1, R3, and Rb are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.
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- Benzamide derivative, preparation and application
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The invention relates to a benzamide derivative expressed in the formula N-(3-(4-(3-imidazo[1,2-b]pyridazinyl)-1-pyraxolyl)-4-methyl phenyl), preparation and application and belongs to the field of medicinal chemistry. R1 represents -OCH3 or -F or -CF3 or
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Paragraph 0079 ; 0080 ; 0081; 0082; 0083; 0084
(2016/10/08)
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- Design, synthesis, and biological activity of 4-(imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-phenylbenzamide derivatives as BCR–ABL kinase inhibitors
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A series of 4-((pyrazolo[1,5-a]pyrimidin-6-yl)-1H-pyrazol-1-yl)phenyl-3-benzamide derivatives and 4-((imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-)phenyl-3-benzamide derivatives were designed, synthesized as new BCR–ABL tyrosine kinase inhibitors by using combinational strategies of scaffold hopping and conformational constraint. These new compounds were screened for BCR–ABL1 kinase inhibitory activity, and most of them appeared good inhibitory activity against BCR–ABL1 kinase. One of the most potent compounds 16a strongly suppressed BCR–ABL1 kinase with IC50value of 8.5 nM. The tested compounds 16a and 16i showed strong inhibitory activities against K562 with IC50value of less than 2 nM. Molecular docking studies indicated that these compounds fitted well with the active site of BCR–ABL1 protein. The results showed these inhibitors may serve as lead compounds for further developing new drugs targeted BCR–ABL kinase.
- Hu, Liming,Cao, Tingting,Lv, Yongjuan,Ding, Yiming,Yang, Leifu,Zhang, Qiang,Guo, Mingzhou
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supporting information
p. 5830 - 5835
(2016/11/25)
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- A 2-amino-thiazole compounds (by machine translation)
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The present invention relates to the technical field of pharmaceutical chemistry, particularly relates to a 2-amino thiazole compound or its pharmaceutically acceptable salts, its preparation method, and pharmaceutical compositions containing such compounds and its application in the preparation of antineoplastic. (by machine translation)
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Paragraph 0326-0328
(2016/10/08)
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- A novel benzoyl amide compounds
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The invention relates to the field of medicinal chemistry, in particular to a novel benzamides compound or a salt acceptable in parmacy of the novel benzamides compound, a preparation method of the novel benzamides compound, a pharmaceutical composition containing the novel benzamides compound and an application of the pharmaceutical composition in preparation of antineoplastic drugs.
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Paragraph 0288-0290
(2016/11/21)
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- Method for synthesizing 3-bromoimidazo[1,2-b]pyrazine
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The invention relates to a method for synthesizing 3-bromoimidazo[1,2-b]pyrazine. 3-aminopyridazine, a chloroacetaldehyde aqueous solution and N-bromosuccinimide are used as raw materials. The ratio of the amount of substances of the 3-aminopyridazine to
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Paragraph 0024
(2016/12/01)
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- Nitrogen bicyclic compounds as inhibitors for Scyl1 and Grk5
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The present invention relates to compounds assumed to be capable of modulating the activity of the proteins ScyI1 and Grk5, thereby regulating the expression and/or release of insulin as well as to pharmaceutical compositions containing such compounds and the use thereof especially for the treatment of a metabolic disease such as diabetes, obesity and impaired adipogenesis.
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Paragraph 0122; 0123
(2015/01/18)
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- PROCESSES FOR MAKING PONATINIB AND INTERMEDIATES THEREOF
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Novel synthetic approaches to make 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide, intermediates and pharmaceutically acceptable salts thereof are provided.
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Paragraph 0074; 0086
(2014/12/09)
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- IMIDAZO[1,2-a]PYRIDINES AND IMIDAZO[1,2-b]PYRIDAZINES AS MARK INHIBITORS
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The invention encompasses imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.
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Page/Page column 38-39
(2010/08/08)
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