87 results about "Muzolimine" patented technology

This invention generally relates to novel compositions and methods for the treatment of certain cancers. Additionally, this invention relates to novel compositions and methods to screen drugs for the treatment of certain cancers. Specifically, the invention contemplates that temozolomide and methoxyamine, in combination or in sequence, shall be used as a treatment for certain tumors that are resistant to treatment by temozolomide alone.

The invention discloses a binary solution type formulation for intravenous and intracerebral injection, shown as right. The main active component thereof is temozolomide with the binary system and having temozolomide sterile powder and solvent for dissolving medicaments. The operating temozolomide solution agent can be obtained through the combination of the solvent. The invention is characterized in that, 1, the binary formulation is stable at the room temperature for over 2 years; 2, the prepared medicaments liquid is stable at the room temperature at least for 48h to meet the operating requirement of injection administration; 3, the solvent is nontoxic and non-irritant, and the prepared medicaments can be used for the intracerebral injection during the operation and stereotaxic intraturmor injection of local chemotherapy.

This invention relates to unit dosage forms of temozolomide. These unit dosage forms are particularly well-suited for decreasing the pill burden and increasing patient compliance. The invention also relates to methods of treating proliferative disorders in a patient with these unit dosage forms. The invention additionally relates to kits comprising these unit dosage forms.

The invention relates to a pharmaceutical preparation, in particular to a compound pharmaceutical preparation with ginsenoside Rh2 and temozolomide as medicine active ingredients.

Disclosed herein is a method for the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject in need thereof a PARP inhibitor, particularly, (R)-2-fluoro-10a-methyl-7, 8, 9, 10, 10a, 11-hexahydro-5, 6, 7a, 11-tetraazacyclohepta [def] cyclopenta [a] fluoren-4 (5H)-one, a sesqui-hydrate thereof, or a pharmaceutically acceptable salt thereof, in combination with temozolomide and/or radiation therapy. Also, disclosed a pharmaceutical combination comprising a PARP inhibitor, particularly, (R)-2-fluoro-10a-methyl-7, 8, 9, 10, 10a, 11-hexahydro-5, 6, 7a, 11-tetraazacyclohepta [def] cyclopenta [a] fluoren-4 (5H)-one, a sesqui-hydrate thereof, or a pharmaceutically acceptable salt thereof, in combination with temozolomide and the use thereof.

The invention relates to sustained release temozolomide capsules and a preparation method thereof, and belongs to the technical field of medicine. Each sustained release temozolomide capsule comprises2-20 sustained release micro-tablets and a capsule shell, wherein each micro-tablet contains 2-20 mg of temozolomide. The sustained release micro-tablets comprise raw and auxiliary materials in percentage by weight as follows: 5%-50% of temozolomide, 5%-40% of a diluent, 10%-70% of a sustained release agent, 0.5%-2% of an antioxidant, 0-5% of an adhesive and 0.5%-2% of a lubricant. The inventionfurther discloses the preparation method of the sustained release temozolomide capsules. The materials are pelletized or mixed and pressed into the micro-tablets directly, and the micro-tablets are loaded to hollow capsules quantitatively. The sustained release temozolomide capsules have the advantages of being good in dissolution, convenient to use, stable in plasma concentration and long in acting time, compliance of patients is improved, the preparation process is simple and lower in cost, and industrial production is easy.

The invention discloses application of manidipine combined temozolomide and a pharmaceutical composition thereof in preparation of a drug for treating brain glioma. The manidipine combined temozolomide can obviously enhance the treatment effect of temozolomide on brain glioma and helps reduce the dosage of temozolomide, thus providing a new treatment scheme for treatment of brain glioma.

The present invention discloses general formula I of Temozolomide-8-carboxylate compounds, the process for preparation, pharmaceutical compositions comprising the compounds and the use of the compounds and pharmaceutical compositions for the manufacture of an antitumor medicament. The said pharmaceutical composition comprises one or more general formula I Temozolomide-8-carboxylate compounds as active ingredient, together with conventional pharmaceutical carriers. The composition also comprises one or more pharmaceutically acceptable acidic material, optionally second or tertiary alcohol or ester or ether derivatives thereof. The said pharmaceutical composition can be made into various common formulations, particularly oral formulations as well as topically transdermal patches. The present invention also discloses the application of the compounds and the compositions to treat tumor.

The invention discloses an injectable anticancer drug temozolomide freeze-dried powder injection preparation and its preparation method. The powder injection preparation is stable, controllable in quality, simple in preparation process and strong in operability, and a prepared product has the characteristics of good solubility, convenient clinical use, a long period of storage and the like.

The invention discloses an application of IncRNA LNC_004208 and detection reagent thereof in preparing a glioma prognosis reagent. Through research on and utilization of IncRNA sequencing, the invention finds that IncRNA LNC_004208 has ultrahigh expression in a temozolomide-resisted glioma cell line; through telephone follow-up for 104 glioma patients, detailed inquiry for their first onset time,level, treatment condition, relapse situation, other diseases, other drugs, relapse time, death time, and the like, and registration for survival time and state, a result shows that average survival time and progression free survival of high expression patients are obviously shorter than those of low expression or no expression patients and are related to reactivity of temozolomide; thus, LNC_004208 is a molecular marker related to glioma prognosis; IncRNA LNC_004208 is high in expression; prognosis of patients is poor.

The invention discloses a compound or a pharmaceutically acceptable salt thereof. The compound includes a moiety derived from temozolomide and a moiety derived from elemene, and the moiety derived from temozolomide and the moiety derived from elemene are directly covalently linked or covalently linked via a linker. The invention also discloses a composition comprising the above compound, and a method of treating cancers.

The invention relates to eutectic crystal of temozolomide and baicalein as well as a preparation method for the eutectic crystal. Specifically, an X-ray powder diffraction pattern of the eutectic crystal has characteristic peaks with 2 theta value being 7.7 +/-0.2 degree, 8.6+/-0.2 degree, and 12.7+/-0.2 degree. The eutectic crystal provided by the invention has obvious advantages in stability, solubility, pharmacokinetic properties and the like of two pharmaceutical ingredients in comparison with existing temozolomide and baicalein bulk drugs, has an important value in developing drug combination of two drugs.

The invention discloses a temozolomide and hesperetin cocrystal and a preparation method thereof. The molar ratio of temozolomide to hesperetin in the cocrystal is 1:1, and an X-ray powder diffractionpattern of the cocrystal has characteristic peaks when the 2theta values are 11.9+/-0.2 degrees, 25.3+/-0.2 degrees, 26.8+/-0.2 degrees and 27.1+/-0.2 degrees. The cocrystal preparation method provided by the invention is simple in process, the crystallization process is easy to control, the reproducibility is good, and the method is suitable for industrial production. The cocrystal can effectively improve the stability and tabletting property of temozolomide, improve the solubility of hesperetin and slow down the dissolution of temozolomide, and provides a research basis for treatment of cancer by combining temozolomide and hesperetin.

The invention discloses a novel application of a human CD133 protein 1-108 peptide fragment (FECD133), namely an application of FECD133 in preparation of a medicine for inhibiting CD133 positive tumors and an application of FECD133 in preparation of a medicine for treating treatment gliomas; the human FECD133 peptide fragment is applied to temozolomide chemotherapy for treating glioma as an intensive chemotherapy drug, wherein the amino acid sequence of the human FECD133 is shown as SEQ ID NO: 1. The high-expression GLT8D1 can glycosylate and stabilize a marker CD133 of the glioma stem cell and activate a Wnt/beta-catenin signal path, so that the activity of the glioma stem cell is promoted, while the FECD133 can obviously block the interaction of the GLT8D1 and the CD133, thereby inhibiting the onset and progression of tumors; and more importantly, the FECD133 is combined with the glioma clinical chemotherapeutic drug temozolomide, so that the killing effect on tumor cells can be enhanced.

The invention relates to an interference plasmid for knocking down expression of COPS5 protein in a glioblastoma cell line, application of the interference plasmid as a drug for solving the drug resistance problem of temozolomide in treatment, and application of a combined drug formed by the interference plasmid for knocking down expression of the COPS5 protein and temozolomide as a glioblastoma chemotherapeutics. The interference plasmids knock down expression of COPS5 protein and regulate the ferroptosis process of glioblastoma cells, specifically, the expression of ferroptosis promoting protein is increased, and the expression of ferroptosis inhibiting protein is reduced.