1891 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 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 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.

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.

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.

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.

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).

Disclosed are an acryloyl compound and a use thereof. The present invention provides a compound as shown in Formula (I), a stereoisomer thereof, an isotopically labeled compound thereof, a solvate thereof, a prodrug thereof, an N-oxide thereof or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits good therapeutic effects against cancer.

The invention discloses an anti-tumor drug delivery system based on click chemistry and a hollow covalent organic framework material as well as a preparation method and application of the anti-tumor drug delivery system, and belongs to the technical field of novel biomedical materials. The anti-tumor drug delivery system based on the click chemistry and the hollow covalent organic framework material comprises a bowl-shaped hollow covalent organic framework material carrier, and a click chemistry prodrug 1 and a click chemistry prodrug 2 which are loaded in the bowl-shaped hollow covalent organic framework material carrier, the click chemistry prodrug 1 is a compound containing an aldehyde group, and the click chemistry prodrug 2 is a compound containing an amino group. By combining the high-specificity reaction of click chemistry with the excellent drug loading performance of HCOF, accurate drug release can be realized in a tumor-specific microenvironment, the toxicity of normal cells can be remarkably reduced, the treatment effect is improved, and a wide clinical application prospect is shown.

The invention discloses an ROS-responsive prostate cancer targeting prodrug as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The prodrug is formed by covalently linking a prostate cancer targeting peptide SYEELR, a ROS (reactive oxygen species) response type ketal thiol (TK) connexon and an active molecule Devimistat. The preparation method comprises the following two steps: firstly, coupling Devimistat with a TK linker to obtain an intermediate Dev-TK, and then coupling the intermediate Dev-TK with an SYEELR peptide fragment to obtain a target product. The prodrug can specifically break and release Devimistat in a tumor high active oxygen microenvironment, and active targeting delivery is realized by virtue of the SYEELR peptide. The invention provides a novel prostatic cancer treatment strategy with accurate targeting, controllable release, enhanced curative effect and toxicity reduction potential.

The present invention provides compounds of formula I for the treatment of diseases such as systemic lupus erythematosus, systemic sclerosis (SSc), interferonosis, nonalcoholic steatohepatitis (NASH), interstitial lung disease (ILD), and idiopathic pulmonary fibrosis (IPF). JPEG2026504613000125.jpg8493 (in the formula, R 1 , R 2 , R 3 , R 4 , A, D, E, G, J, K, and L are as defined in claim 1), and prodrugs, deuterated analogs, and pharmaceutically acceptable salts thereof.

The disclosure provides methods for the for treatment of psychosis, such as schizophrenia, or depression (such as bipolar depression) and / or anxiety, comprising administering to a patient in need thereof, (i) a 5-HT2A or 5-HT2A / D2 receptor ligand, for example a substituted heterocycle fused gamma-carboline as described herein, in free, pharmaceutically acceptable salt or prodrug form, and (ii) a nitric oxide donor, separately (sequentially or simultaneously), or in combination (e.g., in a fixed dose combination).

The invention relates to a pyrrolo [2, 3-d] pyrimidine-4-amine derivative and application thereof in medicine, in particular to a compound shown in a formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, pharmaceutically acceptable salt or eutectic of the compound, and application of the compound in preparation of medicines for treating sGC-related diseases.

The disclosure provides method of treating cancer in a patient with ATM-deficient or ATR-deficient tumors, comprising safely and efficaciously administering to the patient PLXO38, a long lasting-PEGylated prodrug of the topoisomerase I inhibitor. The disclosure further provides combination therapies of PLXO38 with inhibitors of the DNA damage response (DDR).

The invention relates to the field of medicinal chemistry, in particular to a long-acting ester derivative as well as a preparation method and application thereof. According to the invention, the structure of a parent compound is modified to prepare a prodrug with a long-acting property. The medicine is prepared into an injectable preparation through a preparation means, a medicine storage is formed in vivo, and the medicine is slowly, continuously and stably released from the storage and converted into a parent compound, so that a long-acting effect is achieved.

The present invention relates to the technical field of medicine. Specifically, the present invention relates to a KRAS inhibitor compound, a pharmaceutical composition thereof, and a use thereof. Specifically, the present invention relates to a compound as represented by formula (I), or a stereoisomer, tautomer, nitrogen oxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug of the compound as represented by formula (I). The compound and the pharmaceutical composition thereof provided in the present invention can be used for preparing medicaments for preventing or treating diseases related to KRAS amplification or mutations such as KRAS G12A, KRAS G12C, KRAS G12D, KRAS G12R, KRAS G12S, KRAS G12V, KRAS G13D, or KRAS Q61H, and can especially be used for preparing medicaments for preventing or treating cancer.

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.

Provided is a compound and so on having aldehyde dehydrogenase 2 (ALDH2) activation effect. A compound, a pharmaceutically acceptable salt of the compound, or a prodrug of the compound or the salt, the compound being represented by the following formula (1):whereinA is a heterocycle,R1 and R2 are each independently hydrogen, an alkyl, an alkenyl, or an alkynyl,R3 is an alkyl, an alkenyl, or an alkynyl, andX1 and X2 are each independently a halogen.

Provided herein are novel triazine compound derivatives, compositions containing the compounds, and preparation methods and uses thereof. The triazine compound derivatives are compounds represented by Formula (I) or (II), or tautomers, stereoisomers, prodrugs, crystal forms, isotopically labeled forms, pharmaceutically acceptable salts, hydrates or solvates thereof. The compounds and compositions of the present disclosure can be used to treat diseases or disorders mediated by USP1, in particular, cancer. Formula (I) Formula (II)

Disclosed are an optically pure oxaspiro-substituted pyrrolopyrazole derivative, a preparation method therefor and the pharmaceutical use thereof. The compounds are compounds as shown in formula (I) and formula (II) or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a prodrug thereof. Also disclosed are a preparation method therefor and the use thereof.

The invention belongs to the field of biological medicine, and particularly relates to application of deaminotyrosine in preparation of a medicine for treating vascular calcification symptoms. The invention finds that deaminotyrosine can significantly reduce the vascular calcification degree of an in-vitro cell model and an in-vivo animal model by inhibiting osteogenic differentiation and calcium salt deposition of vascular smooth muscle cells; therefore, the invention provides a new application of the deaminated tyrosine or pharmaceutically acceptable salt, ester, solvate or prodrug thereof in preparation of drugs for treating vascular calcification symptoms. The invention also provides a pharmaceutical composition, which takes deaminated tyrosine as an active component, and provides a brand new drug choice for clinical prevention and treatment of vascular calcification.

The invention provides a compound as shown in a formula (I), a stereoisomer thereof, an optical isomer thereof, a pharmaceutically acceptable salt thereof, a crystal form thereof, an isotope derivative thereof, a prodrug thereof and a metabolite thereof. The solvate or hydrate of the compound can be used for preparing a pharmaceutical composition for treating and / or preventing diseases related to mycobacterium tuberculosis and / or nontuberculous mycobacterium. The compound provided by the invention has an excellent bactericidal effect and strong specificity, has no cross resistance with the existing antituberculosis drugs, and provides a breakthrough direction for treatment of drug-resistant tuberculosis.

The invention provides a diketone biphenyl compound serving as a VAV1 degradation agent and application of the diketone biphenyl compound. Specifically provided are a compound represented by formula (I), a tautomer, a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof. The compound provided by the invention is good in drug effect and can be used for preparing drugs for treating or preventing VAV1 related diseases.

The invention relates to the field of medicines, and discloses a compound with a GLP-1 receptor agonistic effect and application. The structure of the compound or the pharmaceutically acceptable salt, stereoisomer, isotope isomer, solvate or prodrug thereof is as shown in formula (I).

The invention belongs to the field of biological medicine and ultrasonic medicine, and provides a barium titanate (BTO) piezoelectric material-based ultrasonic responsive targeting nano system (BTO at BAL), which is used for matrix microenvironment remodeling and immunopotentiation of compact tumors such as pancreatic cancer and the like. According to the nanoparticles, oleic acid modified BTO is taken as a core, ROS responsive prodrug molecules containing a small molecule PD-L1 inhibitor BMS1166 and a nitric oxide donor (Arg) 9 are loaded on the surface, and specific targeting on pancreatic cancer cells is realized by combining a targeting peptide LFC131. Under ultrasonic excitation, BTO generates reactive oxygen species (ROS), on one hand, (Arg) 9 is oxidized to release NO, tumor matrix is degraded, tumor hardness is reduced, drug delivery efficiency is improved, and meanwhile, ROS and NO synergistically enhance tumor immunogenicity; on the other hand, the ROS breaks a thioketal bond to release BMS1166, PD-L1 expression is down-regulated, and immunosuppression is reversed. According to the present invention, the significant tumor inhibition and immune activation effects are represented in the animal model, and the clinical transformation potential is provided.

The present application provides the use of betaine in preventing the occurrence of autism spectrum disorder (ASD). Specifically, the present application provides the use of betaine or a pharmaceutically acceptable salt, stereoisomer, tautomer, nitroxide, solvate, metabolite or prodrug thereof in the preparation of a medicament for preventing the occurrence of ASD, optimizing fetal neural development or reducing the risk of fetal neural development disorder. By using betaine or a pharmaceutically acceptable salt, stereoisomer, tautomer, nitroxide, solvate, metabolite or prodrug thereof as an active ingredient, the occurrence of ASD can be effectively prevented, fetal neural development can be optimized, or the risk of fetal neural development disorder can be reduced.