23 results about "Ester prodrug" patented technology

The invention discloses a derivative of a rice bran extract as well as a preparation method and application of the derivative. A C-3 benzoate prodrug system is constructed, the transmembrane absorption efficiency is remarkably improved by optimizing the oil-water partition coefficient, fixed-point slow release of active ingredients is achieved through inflammatory tissue esterase, and high bioavailability and low irritation are both considered. Meanwhile, C-25 fluorine atoms are introduced to serve as biological electron isosteres, and target affinity is enhanced by means of the unique electronic effect and polar hydrophobicity of the C-25 fluorine atoms; spatial conformation is locked through side chain saturation, so that the compound shows anti-inflammatory and tissue repair activity which is obviously superior to that of natural cycloartanol under the same dosage.

The present disclosure relates to methods of treating PTEN-deficient metastatic hormone- sensitive prostate cancer (mHSPC) in patients in need thereof, the methods comprising administering to the patients a combination comprising capivasertib or a pharmaceutically acceptable salt thereof; and abiraterone or an ester prodrug thereof, or a pharmaceutically acceptable salt thereof.

This invention discloses a compound of formula I, or a pharmaceutically acceptable salt, stereoisomer, ester, prodrug, or solvate thereof. Experimental results show that the compound provided by this invention exhibits high inhibitory activity against PAK4 kinase and PAK I / II selectivity, good liver microsomal stability, and rat PK pharmacokinetic properties, especially with low hERG cardiotoxicity risk, representing a significant improvement over prior art compounds.

Disclosed are a compound shown in formula I and racemate, stereoisomer, tautomer, isotopically labeled, nitroxide, solvate, polymorph, metabolite, ester, prodrug or pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same, a preparation method thereof, and a use thereof as a GHSR agonist in the preparation of a drug for the diagnosis, prevention and / or treatment of growth hormone-dependent diseases, the structure of formula I is as follows:

The invention provides a compound as shown in a formula (I) and a racemate, a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a polymorphic substance, a metabolite, an ester, a prodrug or a pharmaceutically acceptable salt thereof, and the compound has a good p53-Y220C mutant activation effect and can be used for treating tumor diseases containing p53-Y220C mutant protein. And preparation of medicaments for such conditions or diseases.

Provided are a compound represented by formula (I), and a racemate, a stereoisomer, a tautomer, an isotope label, a nitrogen oxide, a solvate, a polymorphic substance, a metabolite, an ester, a prodrug or a pharmaceutically acceptable salt thereof. The compound has a good FGFR2 / 3 inhibition effect, can be used for treating or preventing FGFR2 / 3 mediated diseases and diseases, and can be used for preparing medicines for treating or preventing the diseases and diseases.

The invention relates to an amino-acid ester prodrug of peramivir, which has the following structural formula: in the formula, R is L-valine, D-valine and L-isoleucine taking 2, 3-butanediol as a connecting arm, and L-isoleucine, L-alanine, L-valine or D-valine taking 2-methyl-1, 3-propylene glycol as a connecting arm. Mouse in-vivo pharmacokinetic verification shows that the amino-acid ester prodrug of the peramivir has remarkably higher absolute bioavailability and is suitable for being prepared into an oral administration preparation.

The present application provides a compound shown in formula (I) and its racemate, stereoisomer, tautomer, isotopically labeled, nitroxide, solvate, polymorph, metabolite, ester, prodrug or pharmaceutically acceptable salt thereof. Such compounds have good FGFR2 / 3 inhibitory effect, and can be used for treating or preventing FGFR2 / 3 mediated disorders and diseases, and preparing drugs for treating or preventing such disorders and diseases.

The invention belongs to the technical field of biological medicine, and particularly relates to a lamivudine prodrug long-acting PLGA microsphere preparation and a preparation method thereof. The lamivudine prodrug long-acting PLGA microsphere comprises a lamivudine fatty acid ester prodrug and a PLGA carrier material, the structural general formula of the lamivudine fatty acid ester prodrug is [lamivudine mother nucleus]-O-CO-(CH2) n-CH3, n is an integer of 4-18, and the lamivudine fatty acid ester prodrug is formed by connecting lamivudine and fatty acid through an amido bond; the microspheres are prepared by adopting a single emulsion solvent evaporation method, and the prepared microspheres have the advantages of high drug loading capacity (5%-11%), high encapsulation efficiency (36%-98%) and low burst release effect (24 h lt) by optimizing a prodrug structure, PLGA material characteristics and process parameters; 10%) and the like, and stable drug release of more than 4 weeks can be realized.

This invention discloses a combination drug of Akkermansia and an EET homologue and its uses, relating to the field of biomedical technology. Specifically, the combination drug of this invention comprises: A1) a first active ingredient, the first active ingredient comprising Akkermansia myxophilus; and A2) a second active ingredient, the second active ingredient comprising at least one of 14,15-epoxyeicosatetrienoic acid (14,15-EET) or an isomer of 14,15-epoxyeicosatetrienoic acid, a pharmaceutically acceptable salt, an ester, or a prodrug. The combination drug of this invention exhibits excellent anti-inflammatory and anti-tumor effects in LPS-induced inflammation models and LLC subcutaneous tumor models. The synergistic index SI > 1 calculated using the Bliss independent model indicates a good synergistic effect, and it can be used for the prevention, treatment, and prognostic improvement of non-small cell lung cancer.

This invention relates to a compound of formula (I), a pharmaceutically acceptable salt thereof or an ester prodrug thereof, and pharmaceutical compositions thereof for use in diseases or conditions associated with elevated lipoprotein (a) levels. The compounds of this invention exhibit strong lipoprotein (a) binding capacity and can effectively reduce the activity of lipoprotein (a) levels. Formula (I)

This invention relates to a series of 2'-deoxy-2',2'-difluorocytidine monophosphate amide derivatives (compounds of formula I) and methods for preparing their pharmaceutically acceptable salts, as well as their applications in the therapeutic field. Furthermore, this invention provides a series of novel, easily prepared, and highly active 2'-deoxy-2',2'-difluorocytidine-5'-monophosphate amide derivatives, namely ProTide, whose structure is mainly derived from the -5' hydroxyl group in the 2'-deoxy-2',2'-difluorocytidine structure to obtain the corresponding phosphate acyl amino acid ester prodrugs. These compounds exhibit good solubility and blood circulation stability, and can be used as single agents or in combination for the treatment of cancer diseases.

Provided in the present invention are a compound of general formula I or a pharmaceutically acceptable salt, a stereoisomer, an ester, a prodrug and a solvate thereof, a preparation method and use thereof, and in particular, the use of the compound of general formula I or the pharmaceutically acceptable salt, the stereoisomer, the ester, the prodrug and the solvate thereof as an HPK1 kinase inhibitor in the prevention and / or treatment of tumors and diseases caused by or associated with pathogen infection. The above-mentioned compound of general formula I contains at least one deuterium atom, and has high stability and good bioavailablility in an animal body.

The invention relates to a preparation method and anti-hepatic fibrosis application of a theanine derivative, the application further comprises treatment of chronic liver diseases such as alcoholic steatohepatitis and non-alcoholic steatohepatitis, and the structural formula of the theanine derivative is a compound shown as a formula I, the invention also relates to application of pharmaceutically acceptable salts or esters, prodrugs, stereoisomers, hydrates, solvates, crystal forms, metabolic forms of the pharmaceutically acceptable salts or esters, the prodrugs, the stereoisomers, the hydrates, the solvates and the crystal forms of the pharmaceutically acceptable salts or the pharmaceutically acceptable esters, the hydrates, the solvates and the crystal forms in preparation of medicines or reagents.

This application relates to the use of hydroxyphenylpropanoate compounds of formula (I), (II), (III), (IV), or (V), or pharmaceutically acceptable salts, solvates, and / or ester prodrugs thereof, compositions comprising the same, and their use in, for example, cancer immunotherapy, for increasing antitumor immunity. More particularly, this application relates to compounds useful in the treatment of diseases, disorders, or conditions that can be treated by increasing intracellular antitumor immunity, such as cancer.

The application discloses a preparation method of a chiral phthalic ester prodrug and relates to the technical field of organic chemical synthesis. In the application, isothiourea is used as a Lewis base catalyst, and acyl chloride is used as an acylating agent, so that an acylation dynamic kinetic resolution process of racemic 3-hydroxyisobenzofuran-1(3H)-one (hereinafter referred to as phthalide) is realized, thereby forming a chiral phthalic ester with good to excellent yield and enantioselectivity and natural products and drugs containing the structure.

The present application relates to a PROTAC targeting a Bcl-xL protein and a use thereof. Specifically, the present invention provides a compound of formula I or a pharmaceutically acceptable salt, ester, prodrug, solvate, stereoisomer or deuterated compound thereof: A-L-E (I), wherein A is a small molecule ligand moiety targeting a Bcl-xL protein; E is a small molecule ligand moiety targeting an E3 ubiquitin ligase complex; and L is a linker. The compound or composition of the present invention can be used for selectively killing one or more senescent cells or treating senescence-related diseases or disorders in a subject.

The invention relates to the technical field of biological medicines, in particular to a psoralen derivative and application thereof in preparation of a medicine for treating rheumatoid arthritis. According to the derivative, through an ester prodrug strategy, psoralen C8 / C5 hydroxyl and a non-steroidal anti-inflammatory drug are coupled to obtain a double-pharmacophore molecule. According to the invention, the problems of poor lipid solubility and high hepatotoxicity of psoralen are solved through an ester prodrug design strategy, a high-efficiency and low-toxicity novel drug candidate is provided for RA treatment, and the prepared psoralen derivative can effectively treat rheumatoid arthritis and complications thereof, and can significantly improve arthropathy caused by RA.

The present invention provides a compound represented by a general formula I and a pharmaceutically acceptable salt, stereisomer, ester, prodrug, metabolite, solvate, or deuterated compound thereof. The compound is a JAK inhibitor and can prevent and / or treat an inflammatory disease or cancer in humans and / or animals.

The application provides a compound of a general formula I or a pharmaceutically acceptable salt, a stereoisomer, an ester, a prodrug, a solvate thereof, and a preparation method and application thereof, in particular, application of the compound of the general formula I or a pharmaceutically acceptable salt, a stereoisomer, an ester, a prodrug, a solvate thereof as an HPK1 kinase inhibitor in prevention and / or treatment of tumors, diseases caused by pathogen infection or related to pathogen infection. The compound of the general formula I contains at least one deuterium atom, has high stability in an animal body and good bioavailability.

The invention provides a pyrimido indolone small-molecule PI3Kalpha inhibitor and application thereof, and belongs to the technical field of antitumor drugs. The structure of the pyrimido indolone micromolecule PI3K alpha inhibitor is shown as a formula I, wherein R1 is selected from the following groups: C1-6 alkyl, phenyl, heteroaryl, condensed cycloalkyl, heterocondensed ring group, 3-6-membered saturated cycloalkyl and 3-6-membered saturated heterocyclic group; r2 is selected from the following groups: C1-6 alkyl groups, phenyl groups, heteroaryl groups, condensed cycloalkyl groups, heterocondensed ring groups, 3-6-membered saturated cycloalkyl groups and 3-6-membered saturated heterocyclic groups. The invention further discloses application of the pyrimido indolone small-molecule PI3K alpha inhibitor or the pharmaceutically acceptable salt thereof or ester, prodrug, solvate or deuterated compound of the compound in preparation of antitumor drugs. The compound disclosed by the invention is targeted to a PI3K alpha kinase ATP site, has excellent anti-tumor activity, and has anti-proliferative activity on tumor cells such as MCF-7, H1299, A549 and HCT-116.

The present invention provides a compound of general formula I, and a pharmaceutically acceptable salt, a stereoisomer, an ester, a prodrug, a solvate and a deuterated compound thereof, wherein the compound is an IRAK4 kinase inhibitor, and can be used for preventing and / or treating diseases related to IRAK4, such as autoimmune diseases, inflammatory diseases, cancers, heteroimmune diseases, thromboembolism, atherosclerosis, myocardial infarction and metabolic syndrome.

The present invention provides a compound represented by a general formula I and a pharmaceutically acceptable salt, stereisomer, ester, prodrug, metabolite, solvate, or deuterated compound thereof. The compound is a JAK inhibitor and can prevent and / or treat an inflammatory disease or cancer in humans and / or animals.