3607 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.

Provided herein are compounds, or salts, esters, tautomers, prodrugs, zwitterionic forms, or stereoisomers thereof, as well as pharmaceutical compositions comprising the same. Also provided herein are methods of using the same in modulating (e.g., inhibiting) KRAS (e.g., KRAS having a Q61H, G12D, G12V, G12C, G12S, G12A, G12R, or G13D mutation or wild-type KRAS, including wild-type amplified KRAS) and treating diseases or disorders such as cancers in subjects in need thereof.

The invention relates to compounds of formula (I), a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, a prodrug thereof, a deuterated molecule thereof or a PROTAC molecule thereof that selectively inhibit the activity of K-Ras G12D protein, compositions comprising the same, the methods of using the same and related intermediates.

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.

The disclosure provides transmucosal bilayer film for delivering N,N-dimethyltryptamine (DMT) comprising an active layer comprising DMT or a pharmaceutically acceptable salt or prodrug thereof in a polymeric carrier matrix and a backing layer.

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

Provided in the present invention are a tetrahydropyridopyrazole derivative and use thereof in medicine. Specifically provided is a compound as shown in general formula (I) or a racemate, stereoisomer, tautomer, deuterated substance, solvate, prodrug, metabolite, pharmaceutically acceptable salt or eutectic crystal thereof, an intermediate thereof, a preparation method therefor, and use thereof in the preparation of a related drug for treating diabetes or obesity.

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 nitroreductase response fluorescence and magnetic resonance bimodal probe NO2-Cy-Gxtb-Gd-Biotin designed on the basis of a gemcitabine prodrug as well as a synthesis method and application of the nitroreductase response fluorescence and magnetic resonance bimodal probe NO2-Cy-Gxtb-Gd-Biotin. The probe has relatively low fluorescence signals and magnetic resonance signals, and has relatively low biotoxicity. After the nitroreductase responds, on one hand, the gemcitabine anti-cancer drug is released, and tumor cell apoptosis is promoted; on the other hand, a molecular skeleton can generate a series of electron transfer to form an intermediate structure of methylquinone, and the intermediate structure of methylquinone is very high in reaction activity and is easily attacked by an external residue nucleophilic group of protein, so that the probe is anchored on nitroreductase, and a fluorescence signal and a magnetic resonance signal are remarkably enhanced; therefore, tumor enrichment is increased, an imaging time window is expanded, and early monitoring of tumors is facilitated. The medicine and the imaging probe are integrated, so that the treatment of monitoring tumors is facilitated.

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 #

The invention relates to an active oxygen responsive triptolide prodrug immunoregulation hydrogel preparation as well as a preparation method and application thereof. Triptolide is coupled with an active oxygen responsive group to synthesize a triptolide derivative; then, the triptolide derivative is coupled with polypeptide, and a polypeptide-reactive oxygen responsive group-triptolide conjugate is obtained; then dissolving the polypeptide-active oxygen responsive group-triptolide conjugate in a solvent, standing, and carrying out self-assembly to obtain a triptolide prodrug nanofiber solution; finally, an immunomodulator is added into the triptolide prodrug nanofiber solution for incubation, and the active oxygen responsive triptolide prodrug immunoregulation hydrogel preparation is obtained. The hydrogel preparation disclosed by the invention can responsively release the medicine triptolide and the immunomodulator at the focus part of rheumatoid arthritis, so that the medicine accumulation of non-target organs is reduced, the safety and effectiveness of treatment are improved, and the progress of diseases is effectively controlled.

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 present invention relates to a method of treating a glucose-6-phosphate dehydrogenase dysregulated disorder in a subject in need thereof, the method comprising administering to the subject an effective amount of oleanolic acid, a conjugated salt thereof, or a prodrug thereof. The glucose 6-phosphate dehydrogenase dysregulated disorder can be myofibrillar myopathy, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Alzheimer's disease caused by BCL2 associated immortal gene mutation.

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.

A class of aromatic hydrocarbon receptor modulator compounds represented by the following formula I, or respective optical isomers, deuterated compounds, prodrugs or pharmaceutically acceptable salts thereof, and a preparation method therefor and the use thereof. The compounds can be used as aromatic hydrocarbon receptor modulators to regulate the activity of aromatic hydrocarbon receptors in vivo, which is of great significance for the treatment of related diseases such as immune diseases, inflammatory diseases, infections, skin diseases, osteoporosis, cancers and neurodegenerative diseases.

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.

Disclosed herein are methods, pharmaceutical combinations, or kits for the prevention or treatment of extrapyramidal syndromes, for example, dyskinesia, dystonia, akathisia, or drug-induced Parkinsonism, with the administration of a therapeutic effective amount of Trapidil, a derivative, a metabolite, a prodrug, an analog, or a pharmaceutically acceptable salt thereof.

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 belongs to the field of biological functional materials, and discloses rare earth up-conversion nanoparticles as well as a preparation method and application thereof. The rare earth up-conversion nanoparticles comprise an inner core and a shell layer, and the shell layer is formed by growing on the surface of the inner core through a one-pot method; the inner core is formed by taking beta-NaYF4 as a matrix and doping 0.4%-0.6% of Tm and 25% of Yb with rare earth nanoparticles; the chemical composition of the shell layer is NaYF4; the particle size of the core-shell double-layer structure of the rare earth up-conversion nanoparticle is 246.7 + / -43.2 nm; the polymer HPMCP is used for wrapping up-conversion nanoparticles and a prodrug for drug delivery and enteric release; 800nm up-conversion light generated by irradiation of low-power 980nm laser is used for nano material tracking, and ultraviolet up-conversion luminescence is generated under irradiation of high-power 980nm near-infrared laser to decompose prodrugs for drug release.

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 #

Disclosed are compounds of Formula (I) or a salt or prodrug thereof, wherein: X1 and X2 are independently C or N, provided that zero or one of X1 and X2 is N; Ring A represented by the structure is: or; and Q, R1, R2, R3, R4, R6, and p are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.

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.