63 results about "Isoflavone Derivatives" patented technology

Isoflavones are modified by esterification at one or more of the C4′, C5, C6, and C7 positions to promote bioavailability, and especially to enhance solubility over the corresponding unesterified isoflavones. Preferred modifications produce a carboxylic acid hemiester or a phosphate ester which is biologically hydrolysable. Preferred starting isoflavones are genistin and daidzin, and still more preferably comprises an aglycone form such as genistein or daidzein. Esterified isoflavones may be employed therapeutically or prophylactically for a variety of conditions, provided as a dietary supplement, or added to natural or processed food-stuffs. Further preferred uses include incorporation of contemplated compounds into topical formulations, and especially cosmetic topical formulations.

Disclosed are novel isoflavone derivatives having the structure of Formula Iwhich are useful as ALDH-2 inhibitors for treating mammals for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.

Methods for the hydrogenation of isoflavones are described which provide access to workable quantities of isoflavan-4-ols, isoflav-3-enes, and isoflavans. The isoflavone derivatives can be obtained in high purity and in near quantitative yields whilst employing pharmaceutically acceptable reagents and solvents.

Disclosed herein are compounds, pharmaceutical compositions, and methods for the treatment of viral infection, including RNA viral infection, as well as compounds, pharmaceutical compositions, and methods for modulating the RIG-I pathway in a subject and / or in cells. These compounds are isoflavone derivatives, typically substituted at the 3-position with an aryl group and at the 7-position with a heterofunctional group.

A fluoric isoflavone derivative and its preparing process are disclosed. Said derivative can be used to prepare the medicines for treating cancer, hypertension, hyperglycemia, dysphoria and bacterialand viral diseases. Its advantages are high curative effect and low poison.

Disclosed are novel isoflavone derivatives having the structure of Formula Iwhich are useful as ALDH-2 inhibitors for treating mammals for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.

An isoflavone derivative of tectorigenin compound as shown in formula (II), its preparation method and the antiviral medicine containing it as an effective constituent. The compound structure is shown as follows: Where:: R1 is H, NH2 or SO3M; R2 is OR′; R3 is H or —CH2NR″; where R′ is H, —CH2COONa or —CH2CH2NMe2; NR″ is or —NMe2; M is H, Na, K or N+H (CH2CH2OH)3.

The invention concerns novel flavone and isoflavone derivatives of formulae (Ia) and (Ib) wherein: X represents a group of formula —COOR, or —PO(OR)2; R represents a hydrogen atom or an alkaline or alkaline-earth metal, or a lower alkyl group; R1 represents a hydroxy group, a lower alkoxy group or an acyloxy group; R2 and R3, identical or different, represent a hydrogen or halogen atom, or a trifluoromethyl group, a trichloromethyl group, a hydroxy group, an alkoxy group or an acyloxy group comprising 1 to 5 carbon atoms, or R2 and R3 can combine to form an alkylene dioxy group. The invention is useful for rheumatic diseases.

The invention discloses multiple-target effects of an isoflavone derivative and its application in improvement of learning and memory. Specifically, the invention discloses that a compound J39136 has the effects of: upregulating the expression of SIRT1 protein with damage repair and neuroprotective effects; inhibiting the activity of acetylcholinesterase and butyrylcholinesterase, and dose-dependently inhibiting the acetylcholinesterase activity of cells under a safe dose; protecting nerve cells, inhibiting abnormal expression of beta-APP, and reducing Abeta1-42 secretion; and regulating neuroinflammation. Animal experimental results prove that J39136 has low toxicity, can penetrate the blood-brain barrier, and can significantly improve scopolamine caused mouse dementia and strengthen learning and memory functions. Preclinical study results prompt that J39136 is expected to become the drug for prevention and / or treatment of learning and memory disorder and Alzheimer's disease.

The invention discloses an isoflavone derivative, which specifically is a compound shown as formula (I), or its solvate, or its pharmaceutically acceptable salt. Specifically, R1-R3 are independently selected from alkyl of C1-C6 respectively, and M represents alkali metal or hydrogen. Experiments prove that the compound provided by the invention has anti-Coxsachie virus effect in test mice, and has effects superior to those of control drugs under high, medium and low doses. Therefore, the compound provided by the invention can be used for preparation of anti-Coxsachie virus drugs, and has simple and efficient preparation method, thus having broad market prospects. (formula (I)).

The invention relates to an isoflavone derivative and a preparation method and application thereof, which belong to the field of chemical medicaments. The technical problem solved by the invention is to provide the isoflavone derivative and the preparation and the application thereof. The isoflavone derivative has a structural formula as shown by (I), wherein R1 and R2 in the structural formula are C1-C5 alkyls. The isoflavone derivative has a significant effect of resisting Coxsackie viruses, can be used for preparing medicaments for resisting the Coxsackie viruses, and has an intensive application prospect.

The invention discloses a calycosin derivative and a synthesis method thereof. The derivative is prepared by the steps of: dissolving a compound 1 and a compound 2 in an organic solvent, making the compound 1 and the compound 2 react under a basic condition to obtain an intermediate product 3, and dissolving the intermediate product 3 and a compound 4 in an organic solvent to obtain the targeted crude product. Applicants find that the proliferation of human umbilical vein endothelial cells can be promoted by the derivative of low concentration, so that an effect of good vascular protection isachieved, and therefore the derivative can be applied to the preparation of ERalpha and GPR30 agonists; meanwhile, an inhibitory effect on MCF-7 cells can be generated by the derivative of low concentration (10 uM); the structures of the compound 1, the compound 2, the intermediate product 3 and the compound 4 which are involved in the derivative and the synthesis method of the derivative are shown as follows respectively.

The invention discloses an isoflavone derivative modified by acetylaminoacid benzyl ester of a general formula Ia-q, in which R1, R2 and R3 are all CH2CO-AA-OBzl or both R1 and R2 are all CH2CO-AA-OBzl, while R3 is H, wherein the AA in the CH2CO-AA-OBzl is selected from glycin, lactamine, phenyl alanine, tryptophan, isoleucine, leucine, valine, aspartic acid and glutamic acid. The invention also discloses a preparation method of the isoflavone derivative modified by the acetylaminoacid benzyl ester of the general formula Ia-q. The invention adopts an S180 mouse model to evaluate the antitumor effects of the isoflavone derivative modified by the acetylaminoacid benzyl ester of the general formula Ia-q, thus indicating that the isoflavone derivative has excellent antitumor activity and can be used as an antitumor agent.

Disclosed are novel isoflavone derivatives having the structure of Formula I which are useful as ALDH-2 inhibitors for treating mammals for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.

The invention discloses application of a calycosin derivative in preparation of a drug for treating an ER feminine breast cancer. An applicant finds through an experiment that the calycosin derivativecan lower the expression levels of MALAT1 and GPR30, inactivate ERK1 / 2 and Akt phosphorylation levels and inhibit cell proliferation of the ER negative breast cancer. An MTT experiment shows that theproliferation effect of inhibiting SKBR3 and MDA-MB-468 of the compound shown in a formula (I) is most obvious when the amount is 15 microns, while the same concentration of calycosin (15 microns) has no obvious effect on cell proliferation of SKBR3 and MDA-MB-468. The structure of the calycosin derivative is represented in the following formula (I) (shown in the description).

Disclosed are novel isoflavone derivatives having the structure of Formula (I) which are useful as ALDH-2 inhibitors for treating mammals for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.

The invention relates to a Vegetable estrogen analogy composition capable of replacing estrogen and its application, wherein the composition includes various isoflavones, isoflavone derivatives and phenol substance extracted from a plurality of plants, Chinese medicinal herbs and leguminous plants which has the function of estrogenic hormones.

The invention belongs to the field of medical technology and discloses a genistein derivative with a structure shown by formula I in the specification or a pharmaceutically acceptable salt thereof. The invention also discloses an application of the genistein derivative or the pharmaceutically acceptable salt thereof in preparing a tumor treating medicine, an application in preparing an inflammation-related tumor treating medicine and an application in preparing a medicine inhibiting tumor cell invasion and migration. The genistein derivative disclosed by the invention generates a growth inhibiting and killing effect on tumor cells to realize an anti-tumor effect and has broad-spectrum anti-tumor activity while the effect is relatively good; the genistein derivative promises a perfect treatment effect on the AOM / DSS induced inflammation related tumor; and with relatively good ability of inhibiting tumor cell invasion and migration, the genistein derivative can be used for preparing a medicine inhibiting tumor migration and can be made into tumor migration inhibiting medicines of various dosage forms, thereby providing a better choice for tumor patients.

Disclosed are novel isoflavone derivatives having the structure of Formula Iwhich are useful as ALDH-2 inhibitors for treating mammals for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.

The invention discloses an isoflavone derivative, specifically a compound represented by formula (I), or a solvate thereof, or a pharmaceutically acceptable salt thereof: wherein, R 1 ~R 3 are independently selected from C 1 ~C 6 The alkyl group, M represents an alkali metal or hydrogen. Experiments have proved that the compound provided by the invention has anti-Coxsackie virus effects in test mice, and its effects at high, medium and low doses are all superior to those of the control drug. Therefore, the compound of the present invention can be used to prepare anti-Coxsackie virus drugs, and its preparation method is simple and efficient, and has broad market prospects.

The invention relates to a 7,4'-disubstituted isoflavone derivative and a preparation method and application thereof. The structural formula is shown in the specification, wherein R is 2-hydroxyl-3-di-n-propylaminly propyl, 2-hydroxyl-3-piperidyl propyl, 3-dimethylamino propyl or 3-diethylin propyl. The preparation method of the compound is simple and high in yield. The compound prepared according to the invention has good antitumor activity in vitro.

This invention belonging to chemical field is about preparation of high water-solubility soybean isoflavone and its derivative. By using cyclo-glucosyl transferase as enzyme and the highly dense starch as glycosyl donor, we convert natural soybean isoflavone to polysaccharide-isoflavone mostly complexed with cyclo-glucosyl. This invention is advantageous in high water-solubility compared with the natural ones. At the indoor temperature, its dissolvability is 95.2mM, 222 times higher than the natural soybean isoflavones. In the procedure, the aglycone structure hasn't been changed to remain natural activity in maximum. After filter and sterilization, the products could be injection, oral liquid and powder injection with cryodesiccation. It could be used in tumor (especially mammary cancer and prostate cancer), hectic fever, osteoporosis, hyperlipoidemia and so on. It overcomes the previous soybean isoflavone which could only be oral and which is low in biological effectiveness and therapeutic efficacy.

The invention discloses a calycosin derivative as well as a synthesis method and application thereof. The synthesis method of the calycosin derivative mainly comprises the following steps of: dissolving a compound 1 and a compound 2 in an organic solvent, adding an acid-binding agent, and reacting under a heating condition to obtain a target crude product. Experimental results of the applicant show that the calycosin derivative can inhibit proliferation of ER positive breast cancer cells and ER negative breast cancer cells at the same time; along with the increase of the concentration of the derivative, the proliferation rate of breast cancer cells is gradually reduced, the inhibition effect is the most obvious at high concentration, and no influence is caused to normal breast cells MCF-10A.

The invention discloses a composition of multiple isoflavone derivatives, and further discloses a preparing method of the composition and medical application of the composition in treating diabetes. The composition of the isoflavone derivatives is prepared by carrying out structural modification on 4,7-diacetyl isoferulic acid genistein, 7-2-bromo-ethoxy genistei and a genistein vanadyl complex. Results of administration hypoglycemic activity screening and cell activity experiments show that the composition has a very good hypoglycemic effect which is better that that of single compounds, and can be used for preparing medicine for treating type II diabetes.

The invention belongs to the field of medicines, and relates to a separating method of isoflavone derivatives and application thereof. The invention discloses application of isoflavone in preparationof medicines for treating oxidative stress-induced diseases. A chemical formula of the isoflavone is shown in the attached figure. The isoflavone can be used for regulating up the protein levels of Nrf2 (nuclear factor-erythroid 2-related factor 2) and Nrf2-regulated II phase detoxification enzyme NQO1 and anti-oxidizing enzyme GCS; an activation mechanism is achieved by increasing the protein stability of Nrf2 to inhibit the protein degrading of Nrf2; an arsenic-induced lung bronchial epithelium Beas-2B cell injury model is used for evaluating the cell protecting function of the isoflavone; proofed by results, the isoflavone can increase the GSH level of cell endogenous antioxidant, and the injury and withering of arsenic-induced Beas-2B cell are inhibited.

The invention relates to the field of medicinal chemistry, aims to provide a substituted furan isoflavone derivative and a preparation method thereof. The substituted furan isoflavone derivative has a structure represented by the formula (I), wherein R1 and R2 are separately independently selected from the group consisting of a hydrogen atom, methyl, methoxyl or halogen. The product is a natural furan isoflavone analogue having a novel skeleton, and has potential pharmaceutical activity; the preparation of the compound can provide a support for research of the pharmaceutical activity of furan isoflavones; the preparation method has the advantages of simple steps and low loss rate and has great significance for industrialized production.

A soluble antioxidant flavone derivative, its production and use are disclosed. The process is sulfonating for daidzin or genistein and salting. It can remove hydroxyl-free radical or superoxide anion free radical.