21573-10-4Relevant academic research and scientific papers
Cyclopropyl acetone and synthesis method thereof
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Paragraph 0030-0031; 0033-0038; 0040-0044; 0046-0050; 0052, (2018/12/13)
The invention discloses cyclopropyl acetone and a synthesis method thereof. The synthesis method comprises the following steps: adding sodium into anhydrous ethanol while stirring, cooling the mixture, generating reaction, and recycling ethanol to obtain a mixed solution; adding cyclopropyl acetone into the mixed solution, stirring the cyclopropyl acetone and the mixed solution, adding ethyl acetate which is 1/3 of the mass, generating reflux reaction, and recycling ethanol; then cooling the product, adding ethyl acetate which is 1/3 of the mass, generating reflux reaction, and recycling ethanol; cooling the product again, adding ethyl acetate which is 1/3 of the mass, generating reflux reaction, recycling ethanol and the ethyl acetate at negative pressure, and storing the product at reduced temperature, thus obtaining a cyclopropyl acetone sodium salt solution; adjusting the pH of the cyclopropyl acetone sodium salt solution to be 2 to 3, stirring the solution, standing still the solution, taking upper brown red liquid for fractionation, and obtaining the cyclopropyl acetone. The content of the obtained cyclopropyl acetone is about 90 percent, and the yield is more than 90 percent; the synthesis method is mild in reaction conditions, high in catalysis efficiency, low in energy consumption, low in cost, high in safety and suitable for large-scale production of an enterprise, and the product is easy to recycle.
Discovery and structure-activity relationships study of novel thieno[2,3-b]pyridine analogues as hepatitis C virus inhibitors
Wang, Ning-Yu,Zuo, Wei-Qiong,Xu, Ying,Gao, Chao,Zeng, Xiu-Xiu,Zhang, Li-Dan,You, Xin-Yu,Peng, Cui-Ting,Shen, Yang,Yang, Sheng-Yong,Wei, Yu-Quan,Yu, Luo-Ting
supporting information, p. 1581 - 1588 (2014/03/21)
Current treatment for hepatitis C is barely satisfactory, there is an urgent need to develop novel agents for combating hepatitis C virus infection. This study discovered a new class of thieno[2,3-b]pyridine derivatives as HCV inhibitors. First, a hit compound characterized by a thienopyridine core was identified in a cell-based screening of our privileged small molecule library. And then, structure activity relationship study of the hit compound led to the discovery of several potent compounds without obvious cytotoxicity in vitro (12c, EC50 = 3.3 μM, SI >30.3, 12b, EC50 = 3.5 μM, SI >28.6, 10l, EC50 = 3.9 μM, SI >25.6, 12o, EC 50 = 4.5 μM, SI >22.2, respectively). Although the mechanism of them had not been clearly elucidated, our preliminary optimization of this class of compounds had provided us a start point to develop new anti-HCV agents.
METHOD OF TREATMENT
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Paragraph 0745, (2014/09/29)
The present invention relates to a method of treating T cell mediated inflammatory immune diseases or T cell mediated hypersensitivity diseases, which comprises administering to a human in need thereof an effective amount of a compound which inhibits EZH2 and/or EZH1, or a pharmaceutically acceptable salt thereof.
NEW CRTH2 ANTAGONISTS
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Page/Page column 166-167, (2013/03/26)
The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
New CRTh2 antagonists.
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Paragraph 0179, (2013/03/26)
The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
NEW CRTh2 ANTAGONISTS
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Page/Page column 64-65, (2013/03/26)
The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
AZAINDAZOLES
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Page/Page column 56, (2013/03/28)
Herein are disclosed azaindazoles of formula (I), (I), where the various groups are defined herein, and which are useful for treating cancer.
ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
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Page/Page column 49, (2013/12/03)
This invention relates to novel substituted benzamide according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
Unusual base-catalyzed exchange in the synthesis of deuterated PF-2413873
Rozzey, Stuart J.,Fray, M. Jonathan
scheme or table, p. 435 - 442 (2010/07/05)
The preparation of deuterated PF-2413873 (4-[3-cyclopropyl-1- (methanesulfonylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy-2, 6-dimethylbenzonitrile, 1) is described for use as a bioanalytical standard in clinical trials. Two strategies were investigated. The sul
Compounds Useful In Therapy
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Page/Page column 17-18, (2008/06/13)
Compounds of Formula (I): and pharmaceutically acceptable salts, solvates (including hydrates) of said compounds and salts, or prodrugs of said compound, or pharmaceutically acceptable salts or solvates of said prodrugs, wherein the substituents are as herein defined, are useful in therapy, for example they may be useful for treating progesterone-mediated conditions such as endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
