An application of a Sesquiterpene lactone compound, and a stereoisomer, isotopic marker, solvate and polymorph thereof, or a pharmaceutically acceptable salt thereof in the preparation of drugs for alleviating radiotherapy-induced injuries. The Sesquiterpene lactone compound is applied to assist radiotherapy, can effectively alleviate the radiotherapy-induced injuries, achieves a protection effect on normal cell tissues of a human body, and has a broad medicinal value.
A hydrate of dimethylaminomicheliolide fumarate and a preparation method therefor and use thereof. The hydrate is a crystal form D, is high in crystallinity, smooth in particle surface, free of coalescence, high in bulk density and good in flowability, and has good stability and good reproducibility. The preparation method comprises: under a stirring action, adding dimethylamine micheliolide and fumaric acid into a mixed solvent system having a constant temperature of 30°C-70°C for reaction crystallization; and filtering after the reaction is finished, and drying filtered solid at normal pressure to obtain the crystal form D of the dimethylaminomicheliolide fumarate. The preparation method is simple, the product yield is high, and the preparation method is appliable to later preparation of patent medicines and is conducive to large-scale production.
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
5.
Uses of sesquiterpene lactone compounds and their derivatives in drugs preparation
The present invention relates to the uses of sesquiterpene lactone compounds and their derivatives in preparing drugs. It belongs to the field of drug technology, specifically relates to the uses of the compounds of Formula (I) in preparing the drugs, especially the uses in preparing the drugs to treat rheumatoid arthritis and treat cancers through inhibiting cancer stem cells.
A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
6.
USES OF SESQUITERPENE LACTONE COMPOUND AND DERIVATIVE THEREOF IN PREPARATION OF DRUGS
The present invention relates to uses of a sesquiterpene lactone compound and a derivative thereof in preparation of drugs, relates to the technical field of drugs, specially relates to uses of a formula (I) compound in preparation of drugs, and particularly relates to uses in preparation of drugs for treatment of rheumatoid arthritis and treatment of a cancer by means of inhibition of cancer stem cells.
A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention relates to the crystalline form of sphaelactone dimethylamine fumarate of formula (I) and the preparation method. The preparation method of the crystalline form operates simply, can easily be industrialized, and employs ethyl acetate as solvent, so it is highly safe.
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
The present invention relates to a compound as represented by formula (I), pharmaceutical composition thereof as well as preparation method and uses thereof, in particular to the uses of the compound as represented by formula (I) for treating rheumatoid arthritis and cancers.
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
The present invention relates to the preparation method of arglabin, comprising reacting micheliolide with epoxidation reagent to obtain 1,10-epoxy micheliolide and dehydration of 4-hydroxy and 3-hydrogen of 1,10-epoxy micheliolide to obtain arglabin. The character of the method is that arglabin is prepared from micheliolide through the crucial intermediate of 1,10-epoxy micheliolide.
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
Disclosed are a dehydrocostus lactone derivative as represented by formula (I) or salts thereof, a compound having a therapeutic dose as represented by formula (I) or salts thereof, pharmaceutical compositions of pharmaceutically acceptable carriers or other anti-cancer pharmaceutical compositions, a preparation method for the compound as represented by formula (I) or salts thereof, and uses thereof in preparing pharmaceuticals for treating cancers.
C07D 307/77 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
Disclosed is a preparation method of a sphaelactone which is prepared form parthenolide sphaelactone as raw material and a suitable acid as catalyst in suitable solvent at suitable reaction temperature and the yield is more than 60%. Also disclosed are uses of the sphaelactone and pharmaceutical composition comprising the sphaelactone and pharmaceutically acceptable carrier in preparation of drugs for treating cancer.
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
Disclosed are sphaelactone derivatives of formula (I) or salts, their pharmaceutical compositions, preparation methods and uses for preparing anti-cancer drugs.
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
patents
