CN-121987624-A - Application of compound BA-7 in preparing medicine for treating and preventing cerebral infarction

Abstract

The invention belongs to the technical field of medicines, and discloses application of a compound BA-7 in preparing a medicine for treating and preventing cerebral infarction. In particular to pharmacological actions of p-hydroxybenzyl substituted tryptophan compounds for treating cerebral infarction. Experimental results prove that the compound BA-7 has obvious effects of reducing cerebral infarction volume of rats after acute cerebral ischemia and improving neurological deficit, and is expected to be a therapeutic drug for diseases related to inflammation.

Inventors

• PENG YING
• LEI XIAOQIANG
• TANG JINGSHU
• LAN JIAQI
• SHI JIANGONG
• GUO QINGLAN
• GONG SHUANG
• HU HAIYANG
• LI XIA
• KANG YUYING
• XU CHENGBO
• QU KAI

Assignees

• 中国医学科学院药物研究所

Dates

Publication Date

20260508

Application Date

20241105

Claims (5)

1. 1. The application of a compound shown as a formula (I) and pharmaceutically acceptable salts thereof in preparing medicines for preventing or treating cerebral ridge plugs: wherein the configuration of the compound (I) is selected from R or S.
2. 2. The use according to claim 1, characterized in that said cerebral infarction is caused by permanent and ischemic cerebral ischemia.
3. 3. Use according to claim 1, characterized in that the effective dose of the compound is 7.5-30 mg/kg/day.
4. 4. Use of a pharmaceutical composition for the preparation of a medicament for the prevention or treatment of a cerebral ridge plug, the pharmaceutical composition comprising a compound as claimed in claim 1 and pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier or excipient.
5. 5. The use according to claim 4, wherein said pharmaceutical composition comprises an injection, a tablet, a pill, a capsule, a suspension, a cream or an ointment, and the administration route is selected from intravenous or intramuscular injection, oral administration, transdermal administration, mucosal administration, rectal administration, vaginal administration.

Description

Application of compound BA-7 in preparing medicine for treating and preventing cerebral infarction Technical Field The invention relates to application of p-hydroxybenzyl substituted tryptophan derivative BA-7 and medicinal salts thereof in preparation of medicines for preventing and treating cerebral infarction, including permanent cerebral infarction and local cerebral infarction. Belongs to the technical field of medicine. Background Cerebral apoplexy is a serious disease seriously harming human health, and has the characteristics of high recurrence rate, high disability rate and the like. Meanwhile, for treating acute ischemic cerebral apoplexy, no good therapeutic drug is available at home and abroad. The only approval of the thrombolytic drug t-PA in the United states by FDA still has the adverse reactions of short treatment time window, high intracranial hemorrhage and the like, and the curative effect is still controversial. Development of effective cerebral ischemia treatment and protection drugs is a major medical problem to be solved urgently. Gastrodia elata (Gastrodia elata Blume) also known as Ganoderma lucidum karst, ganoderma sinense, rhizoma Bolbostematis, herba Hedyotidis Diffusae, SHENCAO, SHUDUZI, MUYANG, MINGTIANMA, TINGFENGCAO, and BAILONGPI, red arrow, etc., is a perennial symbiotic plant of the genus gastrodia (Gastrodia r.br.) of the family orchidaceae (Orchidaceae), and the dried tuber thereof is used as a medicine. Rhizoma Gastrodiae is a rare Chinese medicine, which is listed as the top grade in Shen nong Ben Cao Jing, and is pungent, warm and nontoxic. The compound BA-7 is a derivative of p-hydroxybenzyl substituted amino acid obtained by separating traditional rare traditional Chinese medicine gastrodia elata, pharmacological experiments prove that the derivative can obviously reduce cerebral infarction volume, improve neurobehavioral functions and prompt that the compound has obvious anti-cerebral ischemia activity. Disclosure of Invention The invention discloses a compound shown in a general formula I, and pharmacological experiments show that the compound and a preparation thereof have obvious improvement effects on cerebral infarction volume and nerve behavior function of a rat acute cerebral ischemia model caused by middle cerebral artery occlusion. Therefore, the compounds of the present invention are useful for the prevention and/or treatment of cerebral stroke. A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof In a further aspect the invention relates to pharmaceutical compositions comprising the compounds of the invention as active ingredient. Any dosage form suitable for human or animal use may be made by combining the compounds of the invention with one or more pharmaceutically acceptable solid or liquid excipients and/or adjuvants. Pharmaceutical compositions of the compounds of the present invention may be prepared according to methods well known in the art. For this purpose, the compounds of the invention may, if desired, be combined with one or more solid or liquid pharmaceutical excipients and/or auxiliaries, in suitable administration forms or dosage forms which can be used as human or veterinary medicine. Typically, the pharmaceutical compositions of the present invention contain 0.1 to 95% by weight of the compound of the present invention. The compound of the present invention or a pharmaceutical composition containing it may be administered in unit dosage form by the enteral or parenteral route, such as oral, intramuscular, subcutaneous, nasal, oral mucosal, dermal, peritoneal or rectal, etc., preferably oral. The route of administration of the compounds of the invention or pharmaceutical compositions containing them may be by injection. Injections include intravenous, intramuscular, subcutaneous, intradermal, and the like. The administration dosage form may be liquid dosage form or solid dosage form. For example, the liquid dosage form may be true solution, colloid, microparticle, emulsion, or suspension. Other dosage forms such as tablet, capsule, dripping pill, aerosol, pill, powder, solution, suspension, emulsion, granule, suppository, lyophilized powder for injection, etc. The extract or the compound of the invention can be prepared into common preparations, sustained release preparations, controlled release preparations, targeted preparations and various microparticle administration systems. For the purpose of shaping the unit dosage form into a tablet, various carriers known in the art can be widely used. Examples of carriers are diluents and absorbents such as starch, dextrin, calcium sulfate, lactose, mannitol, sucrose, sodium chloride, glucose, urea, calcium carbonate, kaolin, microcrystalline cellulose, aluminum silicate and the like, wetting agents and binders such as water, glycerin, polyethylene glycol, ethanol, propanol, starch slurry, dextrin, syrup, honey, dextrose solution, acacia slurry, gelat