5270 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.

Compounds shown as formula (I) or stereoisomers thereof, or pharmaceutically acceptable salts, solvates or prodrugs thereof, a pharmaceutical composition comprising same, and the use of same in the preparation of drugs for preventing and / or treating diseases or disorders related to RAS protein activity, such as cancer.

Disclosed is a nitrogen-containing heterocyclic compound, pharmaceutical composition thereof and application thereof. The present disclosure provides a nitrogen-containing heterocyclic compound of formula I, a pharmaceutically acceptable salt thereof, a prodrug thereof, a stereoisomer thereof, a tautomer thereof or an isotopically labeled compound thereof. The nitrogen-containing heterocyclic compounds as represented in Formula I in the present disclosure have good inhibitory effects on cells of various mutations such as KRAS G12C, KRAS G12D, KRAS G12V, KRAS Q61H and other mutations, as well as on KRAS-amplified wild-type cells, and are expected to treat and / or prevent a wide range of diseases associated with Ras.

The invention provides a KRAS G12D protein degradation agent and application thereof in medicine, and particularly provides a compound with a structure as shown in a formula (I) and application of a stereoisomer or a prodrug molecule containing the compound or pharmaceutically acceptable salt of the compound as medicine. The compound can degrade KRAS G12D protein in a targeted manner through a ubiquitin-proteasome way, so that the compound can be used for treating indications mediated by abnormal expression of the KRAS G12D protein. Wherein each group in the formula (I) is defined in the specification. # imgabs0 #

Compounds represented by general formula (I), or stereoisomers, tautomers, deuterated substances, solvates, prodrugs, metabolites, and pharmaceutically acceptable salts or eutectic crystals thereof, an intermediate thereof, and the use thereof in diseases related to KRAS inhibition or degradation such as cancers.

The invention relates to a compound shown in a general formula (I) or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a co-crystal of the compound, an intermediate of the compound, and application of the compound in inhibiting or degrading Kras related diseases such as cancers. B-L-K (I)

Provides heterocyclic compounds and use thereof, specially relates to a compound represented by Formula (I), a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a solvate thereof, a crystal form thereof, a metabolite thereof or a prodrug thereof, further relates to a PROTAC comprising a compound of Formula (I), a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a solvate thereof, a crystal form thereof, a metabolite thereof or a prodrug thereof. The heterocyclic compounds can be used for preventing or treating a SOS l-associated disease.

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 present invention relates to an oxo-tricyclic derivative and the pharmaceutical use thereof, in particular to a compound as shown in general formula (I), or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a cocrystal thereof, an intermediate thereof, a preparation method therefor, and the use thereof in the preparation of a drug for treating diseases associated with WRN activity or expression level.

The invention provides a tetrahydropyridinopyrazole derivative and application thereof in medicine, and particularly relates to a compound shown in a general formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or eutectic of the compound, and an intermediate and a preparation method of the tetrahydropyridinopyrazole derivative. The invention also relates to application in preparation of related medicines for treating diabetes mellitus. # imgabs0 #

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.

Provided herein are compounds of Formula I, or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, X, Y, Z, W, and m are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula I or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipients, and methods of using the same, e.g., in the treatment of mental health diseases and / or disorders.

Pharmaceutical compositions including N-N-dimethyltryptamine (DMT) acceptable salt or prodrug thereof in combination with an antihypertensive agent to reduce sympathomimetic effects associated with the administration of DMT.

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.

A novel prodrug compound having GLP1R agonist activity. Specifically disclosed is a compound having a structure represented by formula (I) as a GLP1R agonist, or a pharmaceutically acceptable salt, solvate, hydrate, isotopic substituent or isomer thereof.

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

The present invention provides compounds of formula (I) that are prodrugs of catecholamine for use in treatment of neurodegenerative diseases and disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating neurodegenerative or neuropsychiatric diseases and disorders using the compounds of the invention, in particular Parkinson's disease.Accordingly, the present invention relates to compounds of formula (Id)whereinR1 is H and R2 is selected from one of the substituents (i) and (ii) below; orR1 is selected from one of the substituents (i) and (ii) below and R2 is H; orR1 and R2 are both represented by substituent (i) below; orR1 and R2 are both represented by substituent (ii) below; orR1 is substituent (i) and R2 is substituent (ii); orR1 is substituent (ii) and R2 is substituent (i);wherein * indicates the attachment point; andwherein the carbon atom at the attachment point on substituent (i) is in the S-configuration; or a pharmaceutically acceptable salt thereof.

The invention belongs to the field of medical chemistry, relates to a compound serving as a WRN inhibitor and application of the compound, and particularly provides a compound shown in a formula (I) or pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug of the compound, processes for their preparation, pharmaceutical compositions containing these compounds and the use of these compounds or compositions for the treatment of diseases associated with WRN. # imgabs0 #

The invention discloses a compound represented by a formula (1), or a tautomer, a mesomer, a raceme, an enantiomer, a diastereoisomer, or a mixture form thereof, or a pharmaceutically acceptable salt, a prodrug or a solvate thereof, the structure of the formula (1) is represented as follows: # imgabs0. Strong hydrophilic sulfonic acid inner salt and / or phosphoric acid inner salt side chains are introduced at the position of (AAA and the like)-PAB (self-destruction group), so that the druggability (including hydrophilicity and stability) of the antibody drug conjugate corresponding to the compound is greatly enhanced, the in-vivo drug removal effect is reduced, and the tumor treatment effect is improved.

A WRN helicase-inhibiting bis-heterocyclic derivative, a pharmaceutical composition containing same, and use thereof. Specifically, a compound represented by formula (I), a stereoisomer thereof, an optical isomer thereof, a pharmaceutically acceptable salt thereof, a crystal form thereof, an isotopic derivative thereof, a prodrug thereof, a metabolite thereof, a solvate thereof, or a hydrate thereof, a composition containing the compound, and use thereof as a WRN helicase inhibitor, which can be used to prepare a drug for treating WRN helicase-mediated diseases.

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 #

The invention relates to a compound shown in a general formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or co-crystal of the compound, an intermediate of the compound, and application of the compound in inhibiting or degrading KRAS related diseases such as cancers. # 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 provides a diheterocyclic derivative for inhibiting WRN helicase, a pharmaceutical composition containing the diheterocyclic derivative and application of the diheterocyclic derivative. Specifically, 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, a metabolite thereof, a solvate thereof or a hydrate thereof. The invention also provides a composition containing the compound and application of the composition as a WRN helicase inhibitor, and the composition can be used for preparing medicines for treating WRN helicase mediated diseases. # imgabs0 #

A compound represented by formula (1), or a tautomer, mesomer, racemate, enantiomer, and diastereomer thereof, or mixture form thereof, or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein the structure of formula (1) is as shown below: formula (1). According to the compound, a strong hydrophilic sulfonate inner salt and / or phosphate inner salt side chain are introduced at the position of polypeptide (VC, VA, AAA, etc.)-PAB (self-immolative group) of a linker, greatly enhancing the druggability (comprising hydrophilicity and stability) of an antibody drug conjugate corresponding to the compound, reducing the in-vivo drug clearance effect, and improving the tumor treatment effect.

The invention discloses a PROTACs compound for targeted degradation of PRMT5 and application of the PROTACs compound. The PROTACs compound comprises a compound as shown in the following formula, and related analogues or pharmaceutically acceptable salts, metabolites or prodrugs of the compound: in the # imgabs0 # formula, X represents a ligand bound to PRMT5 protein, Z represents a ligand of E3 ubiquitin ligase, and Y represents a linking group for linking X and Z; according to the invention, CRBN is used as E3 ligase, and a series of PRMT5-targeted PROTAC degradation compounds are designed and synthesized. The compound can effectively induce PRMT5 degradation, significantly inhibit proliferation, growth, migration, infiltration, clone formation and metastasis of tumor cells, promote apoptosis of cancer cells, promote autophagy of the tumor cells, prevent or overcome drug resistance of BTK inhibitors and / or prolong the lifetime of tumor patients, and has wide application prospects.

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.