21 results about "Lenalidomide" patented technology

The invention discloses application of an active compound in an anti-cataract drug, and particularly relates to the field of drugs. The active compound is lenalidomide, mycophenolic acid, glycyrrhetinic acid or bromfenac sodium hydrate. Through a solution based on a CRYAB structure and animal experiment screening, it is found that the active compound can serve as an effective component of an anti-cataract drug, the progress of cataract can be remarkably relieved or inhibited, and a new strategy and potential drug selection are provided for treatment of cataract.

The present invention relates to the treatment of subjects having CD20-positive cell proliferative disorders (e.g., B cell proliferative disorders, such as non-Hodgkin's lymphomas or chronic lymphocytic leukemia). More specifically, the invention pertains to the treatment of subjects having a B cell proliferative disorder by subcutaneous administration of mosunetuzumab as a monotherapy or in combination with lenalidomide.

The present disclosure relates to methods of treating myelodysplastic syndrome. The present disclosure provides methods of treating myelodysplastic syndrome (MDS) in a subject not treated with an agent selected from a hypomethylating agent (HMA) and lenalidomide, or both. The methods comprise administering to the subject an effective amount of a telomerase inhibitor, such as, for example, imestat or imestat sodium. In some cases, a subject being treated is classified as a low or moderate-1IPSS risk MDS subject and / or has an erythropoiesis stimulating agent (ESA) recurrent / refractory MDS.

Provided herein are methods of treating a subject having a CD20 - positive cell-proliferative disorder (e.g., a B-cell proliferative disorder, e.g., non-Hodgkin's lymphoma or chronic lymphocytic leukaemia).SOLUTION: The present invention provides the treatment of a subject having a B-cell proliferative disorder by subcutaneous administration of mosnetuzumab as monotherapy or in combination with lenalidomide.SELECTED DRAWING: Figure 10

The present invention relates to the treatment of subjects having CD20-positive cell proliferative disorders (e.g., B cell proliferative disorders, such as non-Hodgkin's lymphomas or chronic lymphocytic leukemia). More specifically, the invention pertains to the treatment of subjects having a B cell proliferative disorder by subcutaneous administration of mosunetuzumab as a monotherapy or in combination with lenalidomide.

The invention relates to a specifically degraded KIM1 liposome, preparation thereof and application of the specifically degraded KIM1 liposome in preparation of medicines for treating kidney diseases, and belongs to the technical field of biological medicines. According to the invention, a KIM1 targeting polypeptide and an E3 ubiquitin ligase ligand (such as lenalidomide) are respectively modified on the surface of a liposome. The lipidosome capable of specifically degrading the KIM1 can be rapidly enriched in a damaged kidney after renal injury occurs, and the KIM1 protein level in the damaged kidney is degraded by 75%. Meanwhile, the druggability problems of poor solubility, low bioavailability and the like caused by large molecular weight of the compound in the PROTAC drug development process are avoided, and the technical problems that drugs are difficult to prepare and kidney injury drugs are lacked in the prior art are solved.

The application discloses application of cryptoxanthin in preparation of a combination drug for treating lenalidomide-resistant multiple myeloma, and relates to the technical field of medicines.The application verifies the effect and potential mechanism of betaCRY in treating LEN-resistant MM through in-vivo and in-vitro experiments, specifically, betaCRY can inhibit the expression level of FSP1 protein in LEN-resistant tumors, thereby inducing the occurrence of ferroptosis, and then significantly reducing the activity of LEN-resistant tumor cells, and finally achieving the purpose of overcoming LEN tumor drug resistance.The discovery in the application proves that a plant extract serves as a new FSP1 inhibitor in the treatment of LEN-resistant MM cells, and provides a theoretical basis for further using betaCRY to treat LEN-resistant MM in clinic.Therefore, the application has a good application prospect in the field of treating drug-resistant MM.

The present invention relates to the treatment of subjects having CD20-positive cell proliferative disorders (e.g., B cell proliferative disorders, such as non-Hodgkin's lymphomas or chronic lymphocytic leukemia). More specifically, the invention pertains to the treatment of subjects having a B cell proliferative disorder by subcutaneous administration of mosunetuzumab as a monotherapy or in combination with lenalidomide.

The application discloses an (S)-lenalidomide-5-position derivative, a synthetic method and application thereof, and the application comprises the following steps: removing a tert-butyloxycarbonyl protective group of a compound 1 under acidic conditions to obtain a compound 2; in the presence of an organic amine, the compound 2 is provided with a benzyloxy carbonyl protective group to obtain a compound 3; the compound 3 is subjected to an amination reduction reaction with L-glutamine tert-butyl ester to obtain a compound 4; the compound 4 is subjected to ring closing under acidic conditions to obtain a compound 5; the compound 5 is subjected to a hydrogenation debenzyl-oxy carbonyl reaction with hydrogen under the action of an acid condition and a hydrogenation catalyst to obtain a compound 6; the compound 6 and 7 are subjected to an amination reduction reaction to obtain a compound 8; and the compounds 5, 6 and 8 are (S)-lenalidomide 5-position derivatives. The synthetic method is simple in post-treatment, less in racemization, high in yield, free of toxic pollutants, and safe and environmentally friendly.

The invention discloses a continuous flow preparation method of lenalidomide and derivatives thereof, and belongs to the technical field of medical chemistry. According to the preparation method, acetonitrile is adopted as a solvent, a substrate solution A and a brominating agent solution B are prepared respectively, the substrate solution A and the brominating agent solution B are mixed online to obtain a first mixed solution, the first mixed solution is introduced into a continuous flow photochemical reactor for a photo-bromination reaction, and the continuous flow photochemical reactor is provided with an LED light source with an integrated circulating cooling function; the method comprises the following steps: mixing 3-aminopiperidine-2, 6-dione hydrochloride with alkali to obtain a bluish violet pre-activated solution, mixing the pre-activated solution with light bromination reaction effluent on line, and carrying out condensation and cyclization reaction in a flowing state; and continuously carrying out hydrogenation reduction reaction in a flowing state, and collecting effluent to obtain the target compound lenalidomide or the derivative thereof. According to the continuous flow preparation method disclosed by the invention, the total retention time of the three-step reaction is shortened to 42 minutes from more than 40 hours of the traditional process, and the production capacity in unit time is remarkably improved.

This disclosure provides methods of treating a myelodysplastic syndrome (MDS) in a subject who has not previously been treated with an agent selected from a hypomethylating agent (HMA) and lenalidomide, or both. The method includes administering to the subject an effective amount of a telomerase inhibitor, such as, for example, imetelstat or imetelstat sodium. In some cases, the subject being treated is classified as IPSS low or intermediate-1 risk MDS and / or has relapsed / refractory MDS to erythropoiesis stimulating agent (ESA).

Methods are provided for the continuous administration to a subject requiring treatment of a formulation comprising an immunomodulatory imide compound. In some modalities, the method is used for the treatment of multiple myeloma, transfusion-dependent anemia due to low- or intermediate-risk myelodysplastic syndromes, mantle cell lymphoma, hematologic cancers, or solid tumor cancers.

The invention discloses application of cryptoxanthin in preparation of a combined medicine for treating lenalidomide-resistant multiple myeloma, and relates to the technical field of medicines. The effect and potential mechanism of the beta CRY in treating LEN drug-resistant MM are verified through in-vivo and in-vitro experiments, specifically, the beta CRY can induce ferroptosis by inhibiting the expression level of FSP1 protein in LEN drug-resistant tumors, then the activity of LEN drug-resistant tumor cells is remarkably reduced, and finally the purpose of overcoming LEN tumor drug resistance is achieved. The discovery in the invention proves the treatment effect of the plant extract as a novel FSP1 inhibitor in LEN drug-resistant MM cells, and provides a theoretical basis for further clinical treatment of LEN drug-resistant MM by using beta CRY. Therefore, the invention has a good application prospect in the field of treatment of drug-resistant MM.

Provided herein are methods and uses for treating multiple myeloma (such as Newly Diagnosed Multiple Myeloma) in a patient in need thereof. The methods comprise administering to the patient an anti-CD38 antibody, bortezomib, lenalidomide, and dexamethasone.

The application discloses a preparation method of lenalidomide, which comprises the following steps: S1, methyl 2-bromomethyl-3-nitrobenzoate, 3-aminopiperidine-2,6-dione hydrochloride and a base are dissolved in a polar solvent, and reaction is carried out at 50-60 DEG C for 5-8 h; after the reaction is completed, the obtained mixed product is refined and purified to obtain 3-(7-nitro-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione; S2, 3-(7-nitro-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione, ammonium formate and a palladium-carbon catalyst are added into a mixed solvent, and reaction is carried out at 35-45 DEG C for 4-7 h; after the reaction is completed, the obtained crude product is further treated; S3, the crude product is stirred and dissolved in a polar solvent, and then filtered; ammonium formate and sodium mercaptoacetate are added into the filtrate, and reaction is carried out under stirring for 2-5 h; after the reaction is completed, the obtained mixed solution is refined and purified to obtain lenalidomide.

The invention relates to a combination containing CD20 / CD47 blocking bifunctional fusion protein and application of the combination. The invention provides a scheme for treating cancers (especially non-Hodgkin's lymphoma) by combining the CD20 / CD47 double-blocking bifunctional fusion protein and lenalidomide or the salt thereof, realizes a better anti-tumor effect than a single drug (CD20 / CD47 double-blocking bifunctional fusion protein or lenalidomide), and has a remarkable synergistic effect.

This invention relates to the field of microneedle patch technology, specifically to a lenalidomide-loaded nanohydrogel microneedle patch and its preparation method. A dual-network hydrogel matrix is ​​constructed using methacrylamide gelatin and methacrylamide hyaluronic acid, and PLGA-PEG nanoparticles loaded with lenalidomide are encapsulated as microneedle patches. The resulting microneedle patch exhibits high mechanical strength and can effectively penetrate the skin; its hydrogel matrix can rapidly dissolve and release the drug, significantly improving local drug concentration and cumulative release rate.

The application belongs to the technical field of biological medicine, and relates to an SLC15A1 targeted protein degradation agent, a construction method thereof and application of the agent in preparation of a drug for treating brain metastasis of lung adenocarcinoma. The application constructs an SLC15A1 targeted PROTAC protein degradation agent IL-PROTAC. The degradation agent couples ibuprofen with a ligand of an E3 ubiquitin ligase, lenalidomide, through a linker, so as to form a bifunctional molecule capable of targeting SLC15A1 and inducing protein degradation of SLC15A1. The IL-PROTAC drug constructed by the application has been proved to be capable of significantly inhibiting tumor growth of a LUAD brain metastasis model and prolonging the survival cycle of an animal model.

The present disclosure provides a composition comprising temozolomide or lenalidomide, a medium chain triglyceride (e.g., miglyol), silica, and a surfactant wherein the composition optionally comprises an antioxidant and / or a flavouring agent, and wherein the temozolomide composition is a non-aqueous, preservative-free suspension. Also provided are methods for treating cancer in a subject (e.g., a child or a subject with and / or with dysphagia).

The present invention provides methods of treating anemia in a patient in need thereof, comprising administering to the patient in need thereof an effective amount of formoterol or a pharmaceutically acceptable salt thereof (e.g., formoterol fumarate or arformoterol tartrate). The formoterol or a pharmaceutically acceptable salt thereof (e.g., formoterol fumarate or arformoterol tartrate) may be administered conjointly with an erythropoiesis-stimulating agent, optionally wherein the anemia is refractory to the erythropoiesis-stimulating agent. The present invention further provides methods of promoting differentiation of an erythroid progenitor cell toward a mature red blood cell in a patient in need thereof, comprising administering an effective amount of formoterol or a pharmaceutically acceptable salt thereof (e.g., formoterol fumarate or arformoterol tartrate). The formoterol or a pharmaceutically acceptable salt thereof (e.g., formoterol fumarate or arformoterol tartrate) may be administered conjointly with other FDA approved drugs such as luspatercept, lenalidomide, erythropoiesis-stimulating agents (ESAs), including but not limited to epoetin alfa or darbepoetin alfa, and / or a hypomethylating agent, such as azacitidine and / or decitabine.