- Discovery of Novel 3-Amino-4-alkoxyphenylketones as PDE4 Inhibitors with Improved Oral Bioavailability and Safety against Spatial Memory Impairments
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To realize PDE4 inhibitors with good developmental potentiality for the treatment of dementia, structure-based optimizations of lead compound FCPR03 resulted in novel aminophenylketones 9c and 9H with low nanomolar potency, which displayed comparable acti
- Feng, Kai-Wen,He, Jia-Peng,Liu, Lu,Wang, Hai-Tao,Xia, Chuang,Xu, Jiang-Ping,Zheng, Lei,Zhou, Zhong-Zhen
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p. 390 - 405
(2022/02/07)
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- Aminophenone compounds as well as preparation method and application thereof
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The invention belongs to the technical field of medicinal chemistry, and particularly relates to aminophenone compounds as well as a preparation method and application thereof. The aminophenone compounds provided by the invention have a good inhibition effect on PDE4, also have good bioavailability, can be applied to preparation of drugs for treating PDE4-related diseases, and increase the optionsof drugs for treating PDE4-related diseases; and the effect of a part of the aminophenone compounds is equivalent to the effect of positive drugs, and the aminophenone compounds have good developmentpotential.
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Paragraph 0047-0050; 0208-0212
(2021/02/06)
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- Tandem α-Alkylation/Asymmetric Transfer Hydrogenation of Acetophenones with Primary Alcohols
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Tandem α-alkylation/asymmetric transfer hydrogenation of acetophenones with primary alcohols, mediated by a single ruthenium catalyst, is described. Under optimized reaction conditions and with use of [Ru(p-cymene)Cl2]2 in combination with an amino acid hydroxyamide ligand, the chiral secondary alcohol products were isolated in moderate yields and in moderate to good enantiomeric excess (up to 89 % ee). One catalyst - one pot - two reactions. Acetophenones are initially alkylated with primary alcohols by the borrowing hydrogen methodology. The alkylation products are directly converted to enantiomerically enriched secondary alcohols.
- Kovalenko, Oleksandr O.,Lundberg, Helena,Hübner, Dennis,Adolfsson, Hans
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supporting information
p. 6639 - 6642
(2016/02/19)
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- Aromatic amides as potentiators of bioefficacy of anti-infective drugs
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The present invention relates to an aromatic substituted pentadienoic acid amides and there use in combination of specific amounts of aromatic amides i.e. 4-alkyl-5-(substituted phenyl)-2(E),4(E)-pentadienoic acid amides, its geometrical isomers or their dihydro or tetrahydro derivatives and an anti-infective drug useful in potentiating the bioefficacy of antiinfective drug. The combination of the present invention is useful in the treatment of certain infections and disease at lower concentration of anti-infectives necessary to inhibit the growth of microbial strains and may also find applications in reducing the resistance in microorganisms.
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Page/Page column 10
(2008/06/13)
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- AROMATIC SUBSTITUTED PENTADIENOIC ACID AMIDE FOR COMBINATION WITH ANTI-INFECTIVE DRUGS
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The present invention relates to an aromatic substituted pentadienoic acid amides and there use in combination of specific amounts of aromatic amides i.e. 4-alkyl-5-(substituted phenyl)-2(E),4(E)-pentadienoic acid amides, its geometrical isomers or their dihydro or tetrahydro derivatives and an anti-infective drug useful in potentiating the bioefficacy of antiinfective drug. The combination of the present invention is useful in the treatment of certain infections and disease at lower concentration of anti-infectives necessary to inhibit the growth of microbial strains and may also find applications in reducing the resistance in microorganisms.
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Page/Page column 23
(2008/06/13)
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