- Coumadin female phenol split-ring analogue and its medical use
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The invention relates to the field of pharmaceutical chemistry, in particular to a coumestrol open-ring analogue with structures as shown in general formulae I and II and a medical application thereof, especially an application to the preparation of drugs as angiogenesis inhibition and vascular disruption agents.
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Paragraph 0033-0035
(2017/10/06)
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- Side chain impacts on pH- and thermo-responsiveness of tertiary amine functionalized polypeptides
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The systemic investigation of the structural impacts of side chains on the pH- and thermo-responsiveness of tertiary amine functionalized poly(l-glutamate)s (TA-PGs) was carried out. The TA-PGs polymers were effectively synthesized by Cu(I)-catalyzed azide-alkyne cycloaddition click reaction of azido tertiary amines with poly(γ-propargyl-l-glutamate) (PPLG). Turbimetric measurements were performed to characterize the pH- and temperature-induced phase transition of TA-PGs in aqueous solution, which suggested a structural dependence of the properties on the N-substituted groups and the "linkers" between 1,2,3-triazole ring and the tertiary amine groups in the side chains. In detail, the pH responsive properties of TA-PGs were basically determined by the hydrophobicity of the N-substituted groups in the side chains and the pH transition point (pHt) decreased as the increasing hydrophobicity of the N-substituted groups, while the temperature-responsiveness of TA-PGs were affected by either the N-substituted groups or the "linkers." TA-PGs with a moderate N-substituted amine group (e.g., DEA, PR, and PD) or a branched "linker" (e.g., iso-propylene and 2-methylpropylene group) were more likely to express the LCST-type phase transition tuned by pH variation. These structure-property relationships revealed in this study would help to develop the applications of TA-PGs in smart drug delivery systems. Copyright
- Xiao, Chunsheng,Cheng, Yilong,Zhang, Yu,Ding, Jianxun,He, Chaoliang,Zhuang, Xiuli,Chen, Xuesi
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p. 671 - 679
(2014/02/14)
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- INDENOISOQUINOLINONE DERIVATIVES, MANUFACTURING METHOD AND MEDICAL USE THEREOF
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Indenoisoquinolinone derivatives (I), the manufacturing method and the medical use thereof, which belong to pharmaceutical chemistry and organic chemistry field, are disclosed. These compounds can be used for treating several medical symptoms related to postmenopausal syndrome, uterine fibers deterioration and aortic smooth muscle cells proliferation, especially ER-(+) depend breast cancer. Meanwhile, these compounds can also be used for treating glioma and lung cancer, and have inhibiting effect on tumor metastasis effect on tumor metastasis.
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Paragraph 0068; 0069
(2013/04/13)
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- Benzimidazolone antiviral agents
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The present invention concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazolone derivatives for the treatment of respiratory syncytial virus infection.
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- 2,3-oxidosqualene-lanosterol cyclase inhibitors
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The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
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- Heterocyclic substituted 2-methyl-benzimidazole antiviral agents
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The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.
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- 1,2,3,4,5,6-hexahydroazepino(4,5-B)indole derivatives, their preparation, intermediate compounds, and their application in therapeutics
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The invention is related to new 1,2,3,4,5,6-hexahydro-5-hydroyalkylazepino[4,5-b]-indole derivatives, of formula: STR1 in which R1 denotes a hydrogen atom, an alkyl radical, an alkenyl radical, a benzyl radical, an alkylamino radical of the type STR2 where the groups R' are either hydrogen atoms or alkyl radicals or form, together with the nitrogen atom to which they are attached, a heterocyclic nucleus of the morpholinyl, piperidinyl, pyrrolidinyl or piperazinyl type, and m is 2 or 3, R2 denotes a hydrogen atom or a benzoyl or acyl radical, R3 denotes a hydrogen atom or an alkyl or benzyl radical, R4 denotes a hydrogen or halogen atom, an alkyl radical an alkoxy radical or a trifluoromethyl radical, and n is 1 or 2, and the salts of addition to pharmaceutically acceptable acids, and to process for their preparation, to intermediates obtained and to their therapeutical use in treating mental disorders.
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