255 results about "Betulinic acid" patented technology

Salts of 3-O-(3′,3′-dimethylsuccinyl)Betulinic acid (DSB) are disclosed. Particularly, the preparation, pharmaceutical evaluation, and in vivo bioavailability evaluation of N-methyl-D-glucamine and alkali metal salt forms of DSB are disclosed. Pharmaceutical compositions including these salt forms are used in methods of treating HIV and related diseases. Methods of making the salts of DSB and the pharmaceutical compositions are also provided.

Personal care composition comprising at least one hair growth regulating compound selected from the group consisting of glyceryl dilaurate, apigenin, tetrahydrocurcumin, oleanolic acid, azelaic acid, sulforaphane, canavanine, pyridoxal 5-phosphate, phytic acid, tannic acid, grape seed extract, NG-nitro-L-arginine-methyl ester, benzamidine, sodium butyrate, betulinic acid, polyornithine, polyarginine, fisetin, jasmonates, methyl-jasmonate, cis-jasmone, caffeic acid phenethyl ester, delphinidin, ethyl abietate, esculetin, sorbic acid methyl ester, canaline, N-formyl-methionine, N-formyl-alanine, taurine, palmitoyl carnitine, undecanol, undecylenic acid, rutin, fusidic acid, phenyl pyruvic acid, L-isoleucine, phenyl glycine, silibinin, silymarin, L-ascorbic acid-6-palmitate, N-undecylenoyl-L-phenylalanine, and salts, derivatives and mixtures of any of the foregoing; and a dermatologically-acceptable carrier.

The present invention is, generally, directed to the use of betulinic acid and derivatives thereof for the treatment of neuroectodermal tumors. The present invention is based on the discovery that betulinic acid and its derivatives are potent anti-neuroectodermal agents. As disclosed herein, betulinic acid and its derivatives are useful for the treatment of neuroectodermal tumors, including, due to its distinct mechanism of action, neuroectodermal tumors that are resistant to conventional chemotherapeutical agents. In addition to the new use of known compounds, the invention discloses novel compounds and pharmaceutical compositions for the treatment of neuroectodermal tumors.

The invention relates to novel betulinic acid derivatives having antiangiogenic activity, processes for producing such derivatives and their use for treating tumor associated angiogenesis.

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 betulinic acid and other structurally related natural products derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.

A kind of modified 23-hydroxy betulic acid derivatives, their preparing process, the medicinal composition containing them and their application in preventing and treating tumor are disclosed.

The present invention provides triterpenoids produced from natural compounds such as oleanolic acid, ursolic acid, betulinic acid, and hederagenin.

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS. In particular, the following compounds are provided herein, including pharmaceutically acceptable salts thereof:

a compound of formula I

a compound of formula II

and a compound of formula III

A method for the treatment of obesity, diabetes, high cholesterol and related diseases including hyperglycemia, lipid disorders, hyperglyceridemia, dyslipidemia and atherosclerosis in mammals using anthocyanins, anthocyanidins, ursolic acid and/or betulinic acid is described. Compositions adapted for these treatments are also described.

The present invention is a method for preparing triterpenoids such as 2-cyano-3,12-dioxoolean-1,9-dien-28-methyl ester and derivatives thereof from oleanic acid, ursolic acid, betulinic acid, sumaresinolic acid or hederagenin.

The invention discloses a 23-hydroxy betulinic acid derivative as well as a preparation method and application thereof. The derivative has a structure as shown in a formula (I). The 23-hydroxy betulinic acid derivative can be used for resisting tumors and used as a tumor medicament resistance reversal agent. The 23-hydroxy betulinic acid derivative can be used for effectively inhibiting the proliferation of tumor cells and also can be used for obviously increasing the antipersonnel force of DOX (doxorubicin) on a P-glycoprotein overexpression cell strain HepG2/ADM under the condition of non-toxicity dosage.

Provided herein provided herein are novel analogs and derivatives of betulinic acid. Also provided is a method for inhibiting an activity of one or more specificity protein (Sp) transcription factors cells associated with a neoplastic disease using betulinic acid, betulinic acid analog(s) and/or derivative(s) effective to decrease expression of a microRNA with concomitant increase in Sp suppressor gene expression. The betulinic acid analogs and derivatives also are effective in methods provided herein for inhibiting proliferation of cells associated with a neoplastic disease for treating a cancer or for reducing toxicity of a cancer therapy in a subject via administration of an analog or derivative of betulinic acid and, optionally, another anticancer drug.

The present invention provides a process of preparing betulin-28-aldehyde from betulin. The process includes contacting betulin with a compound of formula (I), e.g., TEMPO (2,2,6,6-tetramethylpiperidine 1-oxyl) for a period of time effective to provide betulin-28-aldehyde. The present invention also provides a process of preparing betulinic acid. The process includes contacting betulin with a composition that includes: sodium hypochlorite (NaOCl); sodium chlorite (NaClO₂), potassium chlorite (KClO₂), or a combination thereof; and a compound of formula (I), e.g., TEMPO (2,2,6,6-tetramethylpiperidine 1-oxyl); for a period of time effective to provide betulinic acid.

The present invention relates to compounds with a structure shown as a formula I or pharmaceutically acceptable salts thereof. R1, R2, R3, R4, R5 and R6 are defined as in the specification. The invention also provides a preparation method of the compounds with a structure shown as the formula I or pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the compounds and pharmaceutically acceptable salts thereof, and application of betulinic acid analogues or solvates thereof as active ingredients to preparation of antineoplastic medicaments for treating lung cancer, prostate cancer, colon cancer, leukemia, breast cancer, liver cancer, gastric cancer, pancreatic cancer, human malignant glioma and brain tumor.

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, alkyl and alkenyl C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV:

a compound of Formula I

a compound of Formula II

a compound of Formula III

and a compound of Formula IV

These compounds are useful for the treatment of HIV and AIDS.

The present invention provides compounds of the general structure:

which are substituted at the 3 and 28 positions, along with pharmaceutical formulations containing the same and methods of treating viral infections employing the same.

The invention relates to modified 23-hydroxybetulinic acid derivative (1), which belongs to the natural medicine and pharmaceutical chemistry field. The definition of R1, R2, and R3 is shown in the instruction. The invention also discloses a preparation method of the 23-hydroxybetulinic acid derivative, the medicine composition containing the 23-hydroxybetulinic acid derivative, and the use thereof in tumor resistance.