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 Quercetin derivatives and their medical usages

Details
Inventors: Zhao, Yimin; Yang, Ming; Li, Yunfeng; Luan, Xinhui; Luo, Zhipu;
Assignee: Academy of Military Medical Sciences Institute of Pharmacology and Toxicology (Beijing, CN) N/A (
Primary Examiner: Peselev; Elli
Assistant Examiner:
Attorney, Agent or Firm: Ladas and Parry LLP

This invention relates to quercetin derivative, its preparation, and a pharmaceutical combination, as well as their medical uses for the prevention or treatment of diseases related to 5HT.sub.1A receptor or neuron cell damages, including Alzeheimer's disease, drug or alcohol dependence, sleep disorders or panic state; and for delaying senility, improving learning and memory, preventing and treatment of neuron cell damages caused by various kinds of cerebral damages.

DETAILED DESCRIPTION The invention claimed is: 1.
A purified compound of formula I ##STR00002## wherein R.
sub.
1, R.
sub.
2, R.
sub.
3, R.
sub.
4 are all or partly hydrogen atoms, or alkyl containing 1 to 5 carbon atoms; or pharmaceutically acceptable salts thereof.
2.
Compound of formula I according to claim 1, wherein R.
sub.
1, R.
sub.
2, R.
sub.
3, R.
sub.
4 are all hydrogen atoms.
3.
Compound of formula I according to claim 2, characterized in that the compound is derived from cottonseeds.
4.
Compound of formula I according to claim 1, which is quercetin-3-O-.
beta.
-D-apiofuranosyl-(1.
fwdarw.
2-[.
alpha.
-D-rhamnopyranos- yl-(1.
fwdarw.
6)]-.
beta.
-D- glucopyranoside.
5.
A pharmaceutical composition comprising compound of formula I, ##STR00003## wherein R.
sub.
1, R.
sub.
2, R.
sub.
3, R.
sub.
4 are all or partly hydrogen atoms, or alkyl containing 1 to 5 carbon atoms; and a pharmaceutical carrier.
6.
Pharmaceutical composition according to claim 5, for the treatment of diseases or symptoms related to 5HT.
sub.
1A receptor,.
7.
Pharmaceutical composition according to claim 5, for protection of neuron cells.
8.
Pharmaceutical composition according to claim 5, wherein the pharmaceutical carriers are adjuvants for use in solid medicaments including disintegrants, diluting agents, binders, lubricants, and those for use in liquid medicaments including solvents, pH adjusting agents, osmotic regulators, antioxidants, metal complexing agents, preservatives, flavoring agents, and mixtures thereof.
9.
Pharmaceutical composition according to claim 5, wherein R.
sub.
1, R.
sub.
2, R.
sub.
3, R.
sub.
4 of formula I are all hydrogen atoms.
10.
Method of treating a disease related to 5HT.
sub.
1A acceptor or for protection of neuron cells which comprises administering to a patient in need thereof a therapeutically effective amount of a compound of formula I, ##STR00004## wherein R.
sub.
1R.
sub.
2, R.
sub.
3 and R.
sub.
4 are all or partly hydrogen atoms or alkyl containing 1 to 5 carbon atoms.
11.
Method according to claim 10, wherein R



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