40 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 provides methods of treating anemia in a patient in need thereof, comprising administering to the patient in need thereof an effective amount of salmeterol or a pharmaceutically acceptable salt thereof. Salmeterol or a pharmaceutically acceptable salt thereof may be administered conjointly with an erythropoiesis-stimulating agent, optionally wherein the anemia is refractory to the erythropoiesis-stimulating agent. Also provided are 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 salmeterol or a pharmaceutically acceptable salt thereof. The present disclosure further provides methods comprising administering salbutamol or a pharmaceutically acceptable salt thereof. Salmeterol, salbutamol, or a pharmaceutically acceptable salt thereof may be administered conjointly with other FDA-approved drugs such as luspatercept, lenalidomide, daprodustat, vadadustat, an erythropoiesis-stimulating agent (ESA), and / or a hypomethylating agent.

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 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.

The invention provides maslinic acid PROTACs as well as a preparation method and application thereof, and belongs to the technical field of drug development. According to the invention, maslinic acid is taken as a POI ligand, lenalidomide and fluoro-thalidomide are taken as E3 ligands, and linker selects a PEG chain or an aliphatic chain, so that the anti-cancer activity of the compound is superior to that of maslinic acid, and the compound has a good potential application prospect in the aspect of anti-tumor treatment.

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.

Methods of monitoring therapeutic efficacy in a subject with MDS are provided. Also provided is a method of identifying a subject with myelodysplastic syndrome (MDS) for treatment with a telomerase inhibitor, and methods of treating MDS. The subject methods can include administering to the subject an effective amount of a telomerase inhibitor and assessing the hTERT expression levels in a biological sample obtained from the subject. In some cases, a 50% or greater reduction in hTERT expression level identifies a subject who has an increased likelihood of benefiting from treatment with the telomerase inhibitor. The subject can be naive to treatment with a HMA, lenalidomide, or both. In some cases, the subject is classified as having low or intermediate-1 IPSS risk MDS and / or MDS relapsed / refractory to Erythropoiesis-Stimulating Agent (ESA). In some instances, the telomerase inhibitor is imetelstat sodium.

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.

A novel multi-fused-ring compound and a composition for preventing or treating multiple myeloma comprising the same as an active ingredient is described herein. The compound is a derivative synthesized from the natural compound ginsenoside as a starting material, and shows no cytotoxicity to normal hematopoietic stem cells, while exhibiting a significant killing effect on various multiple myeloma cell lines, indicating that it may be administered for a long period of time without side effects. In addition, the compound exhibits a significant synergistic effect when co-administered with the immunomodulator thalidomide or its analog lenalidomide, and thus may be useful as an efficient therapeutic agent or therapeutic aid agent composition for multiple myeloma, an incurable disease.

The present invention provides a method of dosing an anti-fragment crystallizable receptor-like 5 (FcRH5) / anti-cluster of differentiation 3 (CD3) bispecific antibody and lenalidomide for the treatment of cancers such as multiple myeloma.

The invention discloses a new application of lenalidomide (CC-5013) in the treatment of male oligospermia and azoospermia caused by hepatitis E virus (HEV) infection or the improvement of sperm quality, and particularly discloses a new application of lenalidomide (CC-5013) in the treatment of male oligospermia and azoospermia caused by hepatitis E virus (HEV) infection. The lenalidomide is proved to have an obvious treatment effect on sperm quality reduction caused by HEV infection through sperm staining, sperm motility detection, testis pathology analysis, quantitative detection of sperm development key genes and other methods by utilizing an HEV infected mouse model. The treatment scheme provided by the invention is safe and effective, good in treatment effect and low in medicine cost, is suitable for rapid treatment of male reproductive injuries such as male azoospermia, oligospermia and poor sperm quality caused by virus infection, and provides medicine support for diagnosis and treatment of male infertility patients caused by HEV infection.

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 present invention provides a novel compound having a chromanone or its ring-opening form, phenylpropenone, as backbone and compositions for the preventing or treating multiple myeloma, comprising the same. The compounds of the invention exhibit significant killing effects against various multiple myeloma cell lines and show in vivo anti-cancer effects that exceed those of lenalidomide, a commercially available immunomodulator widely used in the treatment of multiple myeloma and myelodysplastic syndromes. In addition, the compounds of the invention exhibit a significant synergistic effect when co-administered with the thalidomide or its analog lenalidomide, and thus are useful as an efficient therapeutic agent or therapeutic aid agent composition for multiple myeloma which is an incurable disease.

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.

Provided are compositions comprising a stable solution of an immune-mediated inflammatory disease (IMID) agent, such as an immunomodulatory imide drug (IMiD) including, but not limited to, lenalidomide (LLD). More particularly, embodiments relate to stable solutions of IMiDs for parenteral use. Methods of preparing stable solutions of IMiDs are also provided. In some embodiments, methods of treating inflammatory disorders and cancer(s) by parenteral use of stable IMiD solutions, and formulations thereof, are provided.

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).

The invention provides application of lenalidomide or pharmaceutically acceptable salts, esters and hydrates thereof in preparation of medicines for treating skin fibrosis diseases, which shows that lenalidomide has an effect of slowing down and treating skin fibrosis and has a good application prospect in development of medicines for treating skin fibrosis diseases. The invention provides a new drug research and development direction for treating, relieving and improving skin fibrosis diseases, and has the potential of becoming a new drug for treating skin fibrosis diseases.

The invention discloses an application of a compound Ixcarpacone A in preparation of an anti-tumor drug, relates to the technical field of medicines, and in particular relates to an application of a natural small molecule compound Ixcarpacone A in preparation of an anti-multiple myeloma drug. The compound Ixcarpacone A has a remarkable inhibition effect on multiple myeloma cells (including drug-resistant strains), and is relatively low in toxicity to normal cells. The combined application of the compound Ixcarpafactone A and the multiple myeloma footstone medicine lenalidomide can obviously enhance the action effect of the compound Ixcarpafactone A and the multiple myeloma footstone medicine lenalidomide.

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.

The invention relates to a lenalidomide medicine solid dispersion and a preparation method thereof, the solid dispersion comprises 40% of lenalidomide and 60% of a water-soluble carrier, and the water-soluble carrier is povidone; the invention also provides a lenalidomide capsule and a preparation method thereof. The lenalidomide pharmaceutical composition provided by the invention is large in drug loading capacity, and a prepared solid preparation is high in bioavailability, good in solubility and stable and controllable in quality; the preparation method is simple in process, good in reproducibility, high in operability and suitable for large-scale production.

The invention discloses sampling equipment for lenalidomide quality detection, and relates to the technical field of powder sampling, the sampling equipment comprises an isolation cavity, an outward opening window is arranged in the isolation cavity, a self-adaptive killing mechanism is arranged in the isolation cavity, the outward opening window is arranged on the front surface of the isolation cavity, and the self-adaptive killing mechanism is arranged in the isolation cavity. The self-adaptive killing mechanism comprises a cylindrical cover, a group of external connection seats are fixedly mounted on the outer surface wall of the cylindrical cover, an ultraviolet lamp panel is fixedly connected to the interior of each external connection seat, an annular frame is fixedly mounted at the bottom of the cylindrical cover, the mechanism adopts an operation mode of chemical labeling and physical sterilization, an independent detention space is constructed, and the self-adaptive killing mechanism is arranged in the annular frame. According to the device, the cavity is sealed, isolation from outside air is completed, microorganisms and bacteria contained in the cavity are fully and cleanly treated in a treatment mode of combining fluorescence labeling and ultraviolet killing, the time of a sterile state in the cavity is further prolonged by adopting a physical blocking mode, and it is guaranteed that medicine is prevented from being polluted by the outside air when transferred.

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.

Disclosed in the present invention are an (S)-lenalidomide-5-derivative, a synthesis method therefor, and a use thereof. The use comprises the following steps: removing a tert-butoxycarbonyl protecting group from a compound 1 under an acidic condition to obtain a compound 2; adding a benzyloxycarbonyl protecting group to the compound 2 in the presence of an organic amine to obtain a compound 3; subjecting the compound 3 to a reductive amination reaction with L-glutamine tert-butyl ester to obtain a compound 4; subjecting the compound 4 to a ring-closure reaction under an acidic condition to obtain a compound 5; subjecting the compound 5 to a hydrogenation and benzyloxycarbonyl removal reaction with hydrogen under an acidic condition under the action of a hydrogenation catalyst to obtain a compound 6; and subjecting the compound 6 to a reductive amination reaction with a compound 7 to obtain a compound 8. The compounds 5, 6, and 8 are (S)-lenalidomide 5-derivatives. The synthesis method of the present invention has simple post-treatment, less racemization and high yield, does not generate toxic pollutants, and is environmentally friendly and safe.

The present invention establishes a rapid and sensitive analytical method for simultaneously determining 11 lenalidomide metabolites in human urine; the metabolites are identified by mass spectrometry; thereby providing the possibility of analyzing the metabolism of lenalidomide in the body and the pathological and physiological conditions of the body; the differences in metabolites between multiple myeloma patients in remission (EG), with no change in symptoms (SG), and with worsening symptoms (IG) are compared. From the perspective of metabolite analysis, the use of urinary metabolites to identify lenalidomide resistance is studied, and at the same time, the possibility of early and rapid screening of lenalidomide-resistant patients is provided, thereby avoiding worsening of patients' symptoms and unnecessary treatment.