887574-32-5Relevant articles and documents
Preparation method of 3-(phenyl amino)ethyl propionate type compound
-
Paragraph 0019, (2018/09/29)
The invention belongs to the technical field of chemical synthesis and particularly relates to a preparation method of a 3-(phenyl amino)ethyl propionate type compound. The method is realized throughthe following steps: mixing an aromatic amine compound w
Heterocyclic Compounds and Methods of Use
-
Paragraph 0777; 0778, (2018/03/10)
This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.
Arylamino containing hydroxamic acids as potent urease inhibitors for the treatment of Helicobacter pylori infection
Liu, Qi,Shi, Wei-Kang,Ren, Shen-Zhen,Ni, Wei-Wei,Li, Wei-Yi,Chen, Hui-Min,Liu, Pei,Yuan, Jing,He, Xiao-Su,Liu, Jia-Jia,Cao, Peng,Yang, Pu-Zhen,Xiao, Zhu-Ping,Zhu, Hai-Liang
, p. 126 - 136 (2018/07/13)
A novel series of aniline-containing hydroxamic acids were designed, synthesized and evaluated as anti-virulence agents for the treatment of gastritis and gastric ulcer caused by Helicobacter pylori. In vitro enzyme-based screen together with in vivo assays and structure?activity relationship (SAR) studies led to the discovery of three potent urease inhibitors 3-(3,5-dichlorophenylamino)–N-hydroxypropanamide (3a), 3-(2-chlorophenylamino)–N-hydroxypropanamide (3d) and 3-(2,4-dichlorophenylamino)–N-hydroxypropanamide (3n). Compounds 3a, 3d and 3n showed excellent urease inhibition with IC50 values 0.043 ± 0.005, 0.055 ± 0.008 and 0.018 ± 0.002 μM, and significantly depressed gastritis developing at the dose of 32 mg/kg b. i.d with eradication rates of H. pylori reaching 92.3, 84.6 and 100%, respectively. Preliminary safety studies (acute toxicity in mice) disclosed that 3a, 3d and 3n was well-tolerated in KM mice with LD50s of 2982.8, 3349.4 and 3126.9 mg/kg, respectively. Collectively, the data obtained in this study indicate that 3a, 3d and 3n, in particular 3n, could considered as promising candidates for the potential treatment of H. pylori caused gastritis and gastric ulcer, and hence merit further studies.
A fluorine-containing agents compound and its preparation method and application (by machine translation)
-
Paragraph 0057; 0059; 0060, (2018/08/28)
The present invention provides a fluorine-containing agents compound and its preparation method and application, the fluorine-containing agents compounds have the formula I illustrated structure, its structure is simple, has good anticoagulant activity, c
A fluorine-containing agents compound and its preparation method and application (by machine translation)
-
Paragraph 0050; 0052; 0053, (2018/08/28)
The present invention provides a fluorine-containing agents compound and its preparation method and application, the fluorine-containing agents compounds have the formula I illustrated structure, its structure is simple, has good anticoagulant activity, c
Fluorine-containing benzimidazole compound and preparation method thereof and application thereof
-
Paragraph 0081; 0083; 0084, (2018/11/22)
The present invention provides a fluorine-containing benzimidazole compound and a preparation method thereof and an application thereof. The fluorine-containing benzimidazole compound has a structureas shown in a formula I, is simple in structure, has goo
Fluorine-containing benzimidazole compounds and preparation method and application thereof
-
Paragraph 0088; 0090; 0091, (2018/11/22)
The invention provides fluorine-containing benzimidazole compounds and a preparation method and application thereof. The fluorine-containing benzimidazole compounds have a structure represented in a formula I; the fluorine-containing benzimidazole compoun
Design, synthesis, and anti-thrombotic evaluation of some novel fluorinated thrombin inhibitor derivatives
Chen, Haifeng,Ren, Yujie
, p. 408 - 420 (2015/06/08)
Computer-aided simulation was used to design and synthesize nine novel fluorinated thrombin inhibitor derivatives. These compounds were confirmed by spectral analyses (1H NMR, 13C NMR, and FT-ICR-MS). Their inhibitory activities agai
BICYCLIC THIAZOLES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
-
Page/Page column 15, (2012/10/08)
The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.
BICYCLIC THIAZOLES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
-
Page/Page column 44-45, (2011/07/07)
The present invention relates to novel bicyclic thiazoles of formula (I) which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 ("mGluR5") and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.