9 results about "Vinca alkaloid" patented technology

The present invention concerns antibody-conjugate having general structure (2):wherein AB is an antibody capable of targeting Trop-2-expressing tumours and D is selected from the group consisting of taxanes, anthracyclines, camptothecins, epothilones, mytomycins, combretastatins, vinca alkaloids, maytansinoids, enediynes such as calicheamicins, duocarmycins, tubulysins, amatoxins, bleomycins, dolastatins and auristatins, pyrrolobenzodiazepine dimers, indolinobenzodiazepine dimers, radioisotopes, therapeutic proteins and peptides (or fragments thereof), kinase inhibitors, MEK inhibitors, KSP inhibitors, and analogues or prodrugs thereof. These antibody-conjugates exhibit an improved therapeutic index. The invention further concerns a process for preparing the antibody-conjugate according to the invention, a method for targeting Trop-2-expressing cells, medical uses of the antibody-conjugates according to the invention.

IT-139, sodium trans-[tetrachlorobis(1H-indazole)ruthenate(III)], is an intravenously administered small molecule compound. In preclinical anti-tumor and mechanism of action studies, IT-139 showed activity against a broad range of tumor types, including those which are resistant to standard anti-cancer agents (e.g., platinums, vinca alkaloids, taxanes, anthracyclines). This activity is believed to arise from IT-139's novel mechanism of action that targets the GRP78 pathway. It was found that up-regulation of GRP78 is a key cancer cell survival pathway. Downregulation of GRP78 using IT-139 removes this resistance pathway allowing for chemotherapy and immuno-oncology agents to be more effective in treating cancer.

Described herein are methods of treating cancer m a subject by administering a therapeutically effective amount of an AP2 associated kinase 1 (AAK1 ) inhibitor and a therapeutically effective amount of a taxane or a vinca alkaloid. -Also disclosed herein are methods of enhancing the responsiveness of a cancer cell to a taxane or a vinca alkaloid, and methods of increasing the efficacy of a taxane or a vinca alkaloid in a subject with cancer by administering a therapeutically effective amount of an AAK1 inhibitor and a therapeutically effective amount of a taxane or a vinca alkaloid. Hie methods can be useful in subjects with cancer that are resistant to the taxane or a vinca alkaloid prior to the administration of the AAK1 inhibitor.

The application belongs to the technical field of organic synthesis, and particularly relates to an asymmetric total synthesis method of catharanthine. Commercially available oxazolidinone 1 is used as a starting material, and is condensed with bromoacrylic acid to obtain compound 2. Then, asymmetric DA reaction of compound 2 and compound 3 occurs under the catalysis of scandium triflate to obtain compound 4. Compound 4 is hydrolyzed into a carboxylic acid under the condition of lithium hydroxide and hydrogen peroxide, and is treated by trimethylsilane diazomethane to obtain compound 6. Compound 6 is selectively reacted with sodium methoxide, and after the protective group is removed by treatment of iodo-trimethylsilane, compound 6 is condensed with an acid to obtain compound 9. Compound 9 is subjected to radical annulation under the catalysis of a photocatalyst Ir(ppy)3 to obtain compound 10. Finally, selective reduction of the amide obtains natural product (+) - catharanthine. The asymmetric total synthesis route of the application has a total step of 8 or 9, and a total yield of 17.8% - 23.5%, which is shorter than that of the prior art, and the total yield is significantly improved.

This invention pertains in general to therapy using pre-treated T cells and / or vesicles secreted by these T cells. In particular there is provided for the use of such pre-treated T cells and / or vesicles secreted by these T cells as a medicament. The pre-treated T cells and / or vesicles secreted by these T cells are useful in the treatment of various conditions including cancer. In particular the pre-treated T cells and / or vesicles secreted by these T cells are useful in therapy that is aimed at preventing adverse effects such as neuropathy that is normally induced by the use of antimitotic agents such as taxanes and vinca alkaloids. The invention also pertains to a method of producing the pre-treated T cells and / or vesicles secreted by these T cells of the invention.

The invention belongs to the technical field of medicine, and particularly relates to application of strictosamide in preparation of a medicine for treating periodontitis, strictosamide is extracted and separated from a nauclea officinalis medicinal material, a periodontitis animal model is constructed, strictosamide is adopted to conduct intervention treatment on the model, and the periodontitis treatment effect is improved. Periodontium is taken to be subjected to TRAP staining, Micro-CT detection and HE staining detection respectively, and it is proved that the strictosamide can specifically regulate and control activation of osteoclasts, pathological alveolar bone resorption caused by periodontitis is effectively inhibited, alveolar bone loss is reduced, meanwhile, damage to the periodontium can be remarkably relieved, bone repair is promoted, and the treatment effect is good. And the disease progress of periodontitis is fundamentally blocked. The experimental result has clinical significance, and a new scheme is provided for clinical treatment of periodontitis.

Described herein are methods of treating cancer m a subject by administering a therapeutically effective amount of an AP2 associated kinase 1 (AAK1 ) inhibitor and a therapeutically effective amount of a taxane or a vinca alkaloid. -Also disclosed herein are methods of enhancing the responsiveness of a cancer cell to a taxane or a vinca alkaloid, and methods of increasing the efficacy of a taxane or a vinca alkaloid in a subject with cancer by administering a therapeutically effective amount of an AAK1 inhibitor and a therapeutically effective amount of a taxane or a vinca alkaloid. Hie methods can be useful in subjects with cancer that are resistant to the taxane or a vinca alkaloid prior to the administration of the AAK1 inhibitor.

The present application relates to a long-changma class derivative and its preparation method and application, belong to long-changma class derivative preparation technical field. The long-changma class derivative disclosed by the present application has the following advantages: (i) the modification of the tail chain increases the fat solubility of the long-changma class compound, and does not affect the brain blood flow regulation of the long-changma class itself, helps to carry the drug to penetrate the blood-brain barrier, and plays a brain protection role, improves the brain microcirculation disorder; (ii) the tertiary amine group in the parent nucleus structure of the long-changma class derivative has the property of ionization under acidic conditions, can achieve efficient carrying and lysosome escape of nucleic acid drugs through charge adsorption, and improve intracellular transport; (iii) the long-changma class derivative inherits the inherent various pharmacological activities of long-changma, and has high safety. Therefore, the long-changma class derivative disclosed by the present application has good application prospect in brain-targeted delivery of drugs for treating brain diseases.

This invention relates to the field of pharmaceutical application technology, specifically a method for preparing and applying a vincristine derivative-antibody conjugate. It involves a composition of a small molecule compound represented by general formula (I), a linker (L), and an antibody (Ab), wherein the small molecule compound is a vincristine derivative, which is conjugated to a targeting antibody via the linker to form an ADC drug with significant antitumor activity. Experiments show that this type of ADC exhibits excellent therapeutic effects in a mouse model of acute myeloid leukemia (AML), with efficacy significantly superior to first-line clinical treatment regimens (such as cytarabine combined with veneclade) and traditional vincristine monotherapy. The ADC provided by this invention has the characteristics of high targeting and low toxicity, providing a new candidate drug for the treatment of malignant tumors such as AML, and possesses significant clinical development value.