2864 results about "Prodrug" patented technology

Provided are compounds of Formula I:nucleosides, nucleoside phosphates and prodrugs thereof, wherein R6 is CN, ethenyl, 2-haloethen-1-yl, or (C2-C8)-alkyn-1-yl. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.

A spiro compound, and a preparation method therefor and a use thereof. Specifically, the present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, tautomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite, or prodrug thereof, a pharmaceutical composition comprising the compound, a preparation method therefor, and a use thereof in preparation of a drug for preventing or treating KRAS-mediated related diseases.

To provide a compound which is a novel proline derivative, and to provide a pharmaceutical composition comprising the compound for the treatment of, for example, systemic sclerosis (SSc) and non-alcoholic steatohepatitis (NASH).SOLUTION: A pharmaceutical composition comprises, as a cGAS inhibitor, a compound which is a novel proline derivative encompassed by formula (I), or a prodrug, a pharmaceutically acceptable salt, or a stereoisomer of the compound.SELECTED DRAWING: None

Pharmaceutical compositions for the transmucosal delivery of N-N-dimethyltryptamine (DMT) acceptable salt or prodrug thereof in combination with a monoamine oxidase inhibitor to achieve desired bioavailability suitable for the treatment of neurological disorders.

The present invention provides a heterocyclic compound for inducing degradation of mutant KRAS protein, a pharmaceutically acceptable salt, a stereoisomer, a solvate or a prodrug thereof, as shown in formula (I), and the definition of each group in the formula is detailed in the specification. In addition, the invention also discloses a pharmaceutical composition containing the compound, and application of the pharmaceutical composition in preparation of a kit for treating cancers, immune diseases or prognosis evaluation of cancer patients. # imgabs0 #

Disclosed in the present invention are a KRAS G12D degradation agent as well as a preparation method therefor and the use thereof. The present invention provides compounds as shown below, and / or stereoisomers, enantiomers, diastereoisomers, atropisomers, deuterated compounds, hydrates, solvates, prodrugs and / or pharmaceutically acceptable salts thereof. The compounds provided by the present invention can effectively degrade and / or inhibit KRAS G12D protein in cells, and can be used for preparing drugs for treating and / or preventing related diseases or disorders caused by KRAS G12D mediation. G-L-E I

The invention relates to the technical field of biological medicine, and discloses a pharmaceutical composition of paclitaxel dimer prodrug nanoparticles and a traditional Chinese medicine compound and application of the pharmaceutical composition, and the pharmaceutical composition is composed of Qiyuansanlong prescription freeze-dried powder and paclitaxel dimer prodrug nanoparticles; wherein the paclitaxel dimer prodrug nanoparticles comprise one of NQO1 response type PTX dimer prodrug nanoparticles (PTX-Q-PTX NPs) or GSH (glutathione) response type PTX dimer prodrug nanoparticles (PTX-SeSe-PTXNPs), and the paclitaxel dimer prodrug nanoparticles comprise one of NQO1 response type PTX dimer prodrug nanoparticles (PTX-Q-PTX NPs) and GSH response type PTX dimer prodrug nanoparticles (PTX-SeSe-PTXNPs). According to the pharmaceutical composition disclosed by the invention, a traditional Chinese and western medicine synergistic treatment system is innovatively constructed, and the advantage of multi-dimensional synergistic interaction is shown. Firstly, an NQO1 / GSH double-response type intelligent release system is adopted, and a biomarker highly expressed by tumor tissue can be specifically responded to realize precise drug release, so that the PTX concentration in tumors is improved compared with that of a traditional dosage form, and meanwhile, the drug circulation time is prolonged. Secondly, the active ingredients in the Qiyuansanlong prescription freeze-dried powder can significantly down-regulate the PD-L1 expression level, synergistically enhance CD4 + T and CD8 + T cell infiltration, and form chemical-immune dual killing effects.

The invention discloses a nitrogen-containing fused ring compound as well as a preparation method and application thereof, and particularly relates to a nitrogen-containing fused ring compound as shown in a general formula I, or pharmaceutically acceptable salt thereof, or enantiomers, diastereoisomers, tautomers, torsion isomers, solvates, polymorphic substances or prodrugs thereof, and a preparation method and application thereof in pharmacy, and particularly relates to a nitrogen-containing fused ring compound as shown in a general formula I, or pharmaceutically acceptable salts thereof, or enantiomers, diastereoisomers, tautomers, torsion isomers, solvates, polymorphic substances or prodrugs thereof. Wherein the definition of each group is described in the specification. # imgabs0 #

Provided herein are novel compounds, for example, compounds having a Formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof. Also provided herein are methods of preparing the compounds and methods of using the compounds, for example, in inhibiting WRN, and / or in treating various diseases such as cancer.

The invention relates to a quinazoline compound as well as a preparation method and application thereof. Specifically, the invention relates to a compound as shown in a formula (I) or pharmaceutically acceptable salt, stereoisomer, tautomer, polymorphic substance, solvate, N-oxide, isotope labeled compound, metabolite or prodrug thereof, and a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt, the stereoisomer, the tautomer, the polymorphic substance, the solvate, the N-oxide, the isotope labeled compound, the metabolite or the prodrug thereof. The invention also relates to a preparation method of the compound and application of the compound in preparation of drugs for preventing or treating KRAS G12D-mediated related diseases. # imgabs0 #

The present embodiments are directed to methods of using glycine transporter inhibitors, such as GlyT1 inhibitors, or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions thereof, for preventing or treating erythropoietic protoporphyria (EPP), X-linked protoporphyria (XLPP), and / or congenital erythropoietic porphyria (CEP), and related syndromes thereof.

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof:which inhibit Human Respiratory Syncytial Virus (HRSV) or Human Metapneumovirus (HMPV) inhibitors. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HRSV or HMPV infection. The invention also relates to methods of treating an HRSV or HMPV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

The invention provides a benzofuranone compound as well as a pharmaceutical composition and application thereof, and relates to the technical field of medicines. The benzofuranone compound is a compound as shown in a formula I, a stereoisomer thereof, a tautomer thereof, a crystalline hydrate thereof, a solvate thereof, a prodrug thereof or a pharmaceutically acceptable salt thereof. The benzofuranone compound and the pharmaceutical composition and the pharmaceutical preparation prepared from the benzofuranone compound can prevent or treat organ injury diseases, and have good treatment effects in kidney injury, liver injury, lung injury, brain injury and heart injury.

The invention relates to a PLpro protease small-molecule inhibitor for treating or preventing coronavirus infection and application of the PLpro protease small-molecule inhibitor. Specifically, the invention relates to a compound shown as a formula (I) or an isotope labeled compound thereof, or an optical isomer, a geometric isomer, a tautomer or an isomer mixture thereof, or a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a metabolite thereof, and the use thereof in the preparation of a medicament for treating or preventing coronavirus infection or diseases or symptoms caused by coronavirus.

To provide a compound which is a novel proline derivative, and to provide a pharmaceutical composition comprising the compound for the treatment of diseases, for example, systemic lupus erythematosus.SOLUTION: A pharmaceutical composition comprises, as a cGAS inhibitor, a compound which is a novel proline derivative of formula (I) (where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and G are as defined in claim 1), or a prodrug, a pharmaceutically acceptable salt, or a stereoisomer of the compound.SELECTED DRAWING: None

The present application relates to a sustained release delivery composition of a vesicular monoamine transporter type 2 (VMAT2) inhibitor, a deuterated derivative thereof, a pharmaceutically acceptable salt thereof, an active metabolite thereof, or a prodrug thereof for treatment of hyperkinetic movement disorders including, but not limited to, tardive dyskinesia (TD), Huntington's disease (HD) chorea, tremors, dystonia, chorea, tics, myoclonus, stereotypies, restless legs syndrome, and various other disorders with abnormal involuntary movements. The present application also relates to a sustained release delivery composition of an antipsychotic agent, a pharmaceutically acceptable salt thereof, an active metabolite thereof, or a prodrug thereof for treatment of schizophrenia, bipolar disorder, and other psychiatric diseases or disorders. The method of making or using the composition is also disclosed.

The invention relates to a norhalal-enoxacin conjugate as well as a preparation method and application thereof. The norhalal-enoxacin conjugate comprises a norhalal-enoxacin coupling compound, or a stereoisomer, a prodrug, a crystal form, a pharmaceutically acceptable salt, a pharmaceutically acceptable ester or a pharmaceutically acceptable solvate selected from the compound. Compared with enoxacin, kanamycin, streptomycin, lincomycin and azithromycin, the norharmann-enoxacin conjugate disclosed by the invention has a smaller MIC (Minimum Inhibitory Concentration) value, which shows that the norharmann-enoxacin conjugate has a better anti-staphylococcus aureus effect.

The invention discloses a nitrogen-containing heterocyclic ring compound as well as a preparation method and application thereof, and particularly relates to a nitrogen-containing heterocyclic ring compound as shown in a general formula (I), or pharmaceutically acceptable salts thereof, or enantiomers, diastereoisomers, tautomers, torsion isomers, solvates, polymorphic substances or prodrugs thereof, and a preparation method and pharmaceutical application thereof. Wherein the definition of each group is described in the specification. # imgabs0 #

The invention provides an ultrasonic activated blood coagulation targeting tumor selective prodrug as well as a preparation method and application thereof. The blood coagulation targeting tumor selective prodrug has a structure as shown in a formula I. The blood coagulation targeting tumor selective prodrug can trigger a blood coagulation cascade reaction by utilizing tumor vascular injury generated by ultrasonic induction so as to realize targeted anchoring of the drug and inhibit off-target diffusion of an active drug; meanwhile, the prodrug is activated by ultrasound, so that the limitation of tumor heterogeneity on the activation of the prodrug can be overcome. According to the technical scheme, selective enrichment of active drugs in tumors can be effectively improved, and toxicity caused by drug off-target is reduced while tumor growth is remarkably inhibited.

Provided in the present invention are compounds as VAV1 degradation agents and the use thereof. Specifically provided are compounds represented by formula (II), and tautomers, stereoisomers, pharmaceutically acceptable salts or prodrugs thereof. The compounds provided by the present invention have good efficacy, and can be used for preparing drugs for treating or preventing VAV1-related diseases.

This invention relates to the field of pharmaceutical technology, specifically to a substituted pyridotriazole compound, its preparation method, and its uses. This specification discloses a substituted pyridotriazole compound that inhibits RIPK1 and / or MLK, as well as its pharmaceutically acceptable salts, stereoisomers, solvent compounds, or prodrugs. The compound is shown in formula (I), where the definitions of each group are detailed in the specification. Furthermore, this invention also discloses pharmaceutical compositions comprising this compound and their use in the preparation of medicaments for treating RIPK1-related diseases or conditions.

Disclosed are an ecteinascidin compound and a use thereof. The present invention provides a compound as shown in formula (I), or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, polymorph, solvate, isotope-labeled compound, metabolite, or prodrug thereof. The compound provided by the present invention exhibits one or more effects selected from the following group: (1) having inhibitory activity on in vitro proliferation of tumor cells; (2) having in vivo antitumor effect; (3) having in vivo tumor-targeting ability; and (4) having good in vivo safety.

The invention discloses a cationic lipid compound, a lipid carrier containing the same and application, and belongs to the technical field of gene therapy. The cationic lipid compound disclosed by the invention has a structure as shown in a formula I, or an isomer, a pharmaceutically acceptable salt and a prodrug thereof. The lipid nanoparticles have the advantages of stable nanostructure, uniform size distribution, good biological biocompatibility, high in-vivo and in-vitro mRNA delivery efficiency, selective organ targeting and the like. The cationic lipid reaction operation is simple, the raw materials are cheap and easy to obtain, and the cationic lipid has high safety, is beneficial to industrial production and quality control, and has a good application prospect.

The invention discloses a compound as shown in a formula (I), and / or pharmaceutically acceptable salts thereof, and / or a raceme mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof, and belongs to the technical field of medicines. The invention also discloses a pharmaceutical composition containing the compound as shown in the formula (I), and the compound as shown in the formula (I) and / or a pharmaceutically acceptable salt thereof, and / or a racemic mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof, and / or the pharmaceutical composition, a pharmaceutically acceptable salt thereof, and / or a racemic mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof. The invention further discloses application of the cGAS agonist in preparation of the cGAS agonist and a medicament for treating diseases responding to activation of the cGAS-STING signal channel.

The invention relates to the field of biological medicine, in particular to a prodrug structure with ROS signal response performance and a preparation method and application thereof. The prodrug molecule with ROS signal response performance developed by the invention can quickly release living active molecules in a disease signal ROS-enriched environment, and plays a role in targeted therapy. The method has good universality, prodrug modification can be carried out on multiple molecules, four kinds of drug molecules approved to appear on the market are included, and it is verified that the solubility and biocompatibility of drugs can be improved, cytotoxicity can be reduced, and the effect of targeted therapy can be improved. Based on the structural characteristics of the molecules, the molecules can also be complexed with PVA hydrogel, and responsive controllable release of the medicine is further achieved.

Provided are a compound as shown in general formula (I), or a stereoisomer, deuterate, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, an intermediate thereof, a preparation method therefor, and the use thereof in the preparation of a drug for treating a disease associated with the activity or expression quantity of complement factor B.

To provide compounds as new proline derivatives, and to provide a pharmaceutical composition comprising the compounds for the treatment of diseases such as systemic lupus erythematosus, systemic sclerosis, non-alcoholic steatohepatitis, interstitial lung disease and idiopathic pulmonary fibrosis.SOLUTION: There are provided new proline derivatives of formula (I) as cGAS inhibitors, or pharmaceutical compositions comprising a prodrug, a pharmaceutically acceptable salt, or a stereoisomer of the compound.SELECTED DRAWING: None

The invention relates to a benzopyrimidine derivative and application thereof in medicine, in particular to a compound shown in a general formula (I) or a stereoisomer, a racemate, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, pharmaceutically acceptable salt or eutectic of the compound, an intermediate of the compound and application of the compound to inhibition or degradation of KRAS related diseases such as cancers. And B-L-K (I).

Formula (I): JPEG2025536322000043.jpg74140 (in the formula, L, R 1 , R 2 , R 3 and W is as defined in the specification. and their enantiomers, diastereomers, racemates, tautomers, prodrugs, hydrates, solvates and pharmaceutically acceptable salts are useful in the treatment of diseases and conditions affected by the inhibition of Mer kinase, such as cancer.

The disclosure provides method of treating cancer in a patient in need thereof, comprising safely and efficaciously administering to the patient PLX038, a long lasting-PEGylated prodrug of the topoisomerase I inhibitor. The disclosure further provides combination therapies of PLX038 with inhibitors of the DNA damage response (DDR).