60208-05-1Relevant academic research and scientific papers
SUBSTITUTED DIHYDROPYRAZOLO PYRAZINE CARBOXAMIDE DERIVATIVES
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Page/Page column 241-242, (2020/01/10)
The invention relates to substituted dihydropyrazolo pyrazine carboxamide derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and diabetes, and also urogenital and ophthalmic disorders.
Synthesis of 2-aminothiazoles from styrene derivatives mediated by 1,3-dibromo-5,5-dimethylhydrantoin (DBH)
Ma, Chunhua,Miao, Yuqi,Zhao, Minghao,Wu, Ping,Zhou, Jianglu,Li, Zhi,Xie, Xilei,Zhang, Wei
, p. 3602 - 3607 (2018/05/26)
An efficient procedure for the synthesis of 2-aminothiazoles via DBH-mediated oxidative cyclization of styrenes and thioureas is reported. Various alkenes were successfully transformed to the corresponding 2-aminothiazoles in yields of 10–81% via a two-step one-pot manner using DBH as both the bromine source and oxidant. The method can be readily carried out in gram-scale and successfully applied to the synthesis of anti-inflammatory drug fanetizole using styrene as starting material.
1,3-Dibromo-5,5-dimethylhydantoin mediated oxidative amidation of terminal alkenes in water
Ma, Chunhua,Fan, Guojie,Wu, Ping,Li, Zhi,Zhou, Yang,Ding, Qingjie,Zhang, Wei
, p. 9889 - 9894 (2017/12/12)
A variety of terminal alkenes were converted to the corresponding amides in yields of 25 to 86% in water via treatment with 1,3-dibromo-5,5-dimethylhydantoin, followed by reaction with molecular iodine and aq. NH3 (or amine) in one pot. This metal- and organic solvent-free protocol is not only suitable for styrene derivatives, but also, for the first time, works well on terminal aliphatic alkenes.
NOVEL ANILINE DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USE THEREOF
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Paragraph 0509, (2017/01/31)
[Problem] The present invention provides a novel compound having an S1P1 receptor antagonistic activity. [Solution] The present invention provides a compound represented by the general formula (I): (in the formula, R1, R2
2-ACYLAMINOTHIAZOLES FOR THE TREATMENT OF CANCER
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Page/Page column 74, (2015/01/16)
The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) are useful in the preparation of a medicament, in particular for the treatment of cancer.
Indolin-2-one p38α inhibitors III: Bioisosteric amide replacement
Eastwood, Paul,González, Jacob,Gómez, Elena,Caturla, Francisco,Aguilar, Nuria,Mir, Marta,Aiguadé, Josep,Matassa, Victor,Balagué, Cristina,Orellana, Adelina,Domínguez, María
scheme or table, p. 6253 - 6257 (2011/11/29)
Crystallographic structural information was used in the design and synthesis of a number of bioisosteric derivatives to replace the amide moiety in a lead series of p38a inhibitors which showed general hydrolytic instability in human liver preparations. Triazole derivative 13 was found to have moderate bioavailability in the rat and demonstrated potent in-vivo activity in an acute model of inflammation.
New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
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Page/Page column 65, (2009/10/21)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
