124results about How to "High metabolic stability" patented technology

This invention is directed to an oral modified release formulation of the phytoestrogen 8-Prenylnaringenin in combination with a progestin, preferably with Drospirenone, and several uses thereof. In another aspect of the invention an oral modified formulation of 8-Prenylnaringenin with an immediately releasing progestin, like Drospirenone, is provided as well as several uses thereof.

The invention discloses a preparation method of a polyene-containing taxol nanoparticle mixed micelle preparation and a freeze-drying agent, which prepares docetaxel PLA-PEG nanoparticles or micelle or nanoparticle mixed micelle through a modified solvent evaporation method, takes PLA-PEG copolymer as a carrier, and wraps docetaxel in a PLA hydrophobic core. When in use, the docetaxel PLA-PEG containing long cycle freeze-dried preparation only needs to be added with water and is dissolved, and uniform nanoparticle suspension, micellar solution or mixed micellar nanoparticle suspension can be prepared. The preparation method does not need tween-80 and ethanol solubilization, only takes the biodegradable PLA-PEG as the carrier, and does not contain any surfactant; and compared with the docetaxel injection on sale, the preparation can reduce the toxicity and the adverse reactions of the medicine, and improve the clinical application safety of the medicine.

The invention discloses a method for preparing a block polymer micelle freeze-drying preparation carrying docetaxel, which uses a PEO-PPO-PEO block polymer as a micelle carrier to wrap the docetaxel inside the micelle and comprises the following steps: (1) dissolving the carrier and the docetaxel into an organic solvent to make the PEO-PPO-PEO block polymer and the docetaxel fully dissolved in the organic solvent, and then preparing aqueous solution of the docetaxel micelle by using the PEO-PPO-PEO block polymer as the carrier; and (2) adding a freeze-drying protective agent into the aqueous solution of the PEO-PPO-PEO block polymer carrying micelle, and filtering, sterilizing and freeze-drying the mixture to obtain freeze-drying preparation of the carrier micelle system. The block polymer micelle freeze-drying preparation carrying the docetaxel can increase the dissolubility, metabolic stability and in vivo circulation time of the docetaxel, reduce the toxicity and improve the bioavailability, and is more suitable for clinical application.

The invention relates to a total tanshinone composite preparation, in particular to a self-microemulsion medicine carrying composite preparation for improving the oral administration bioavailability of total tanshinone, which comprises the following components in part by mass: 0.5 to 5 parts of tanshinone, 25 to 75 parts of oil phase, 35 to 70 parts of surfactant and 0 to 25 parts of cosurfactant. In addition, the preparation can be prepared into a solid preparation or a liquid preparation by combining with other solid materials or water, and after entering a gastrointestinal tract, the solidpreparation or the liquid preparation can be emulsified automatically to form microemulsion of which the grain diameter is less than 100 nanometers when contacting water so as to increase the dissolution speed of the tanshinone, promote the absorption of the tanshinone and improve the oral administration bioavailability of the tanshinone; and the preparation conditions of the total tanshinone composite preparation is mild, a control method is simple and convenient, and special equipment is not required.

A method of contraception in mammalian females, which method comprises the oral administration of an estrogenic component and a progestogenic component to a female of childbearing capability in an amount effective to inhibit ovulation, wherein the estrogenic component is selected from the group consisting of substances represented by the following formula (1)

in which R₁, R₂, R₃, R₄ independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R₅, R₆, R₇ is a hydroxyl group; and no more than 3 of R₁, R₂, R₃, R₄ are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors. Another aspect of the invention concerns a pharmaceutical kit comprising oral dosage units that contain the aforementioned estrogenic component and/or a progestogenic component.

The present invention provides an anti-tumor or anti-angiogenesis medicament, the combination or kit containing the medicament, and the method for producing the same. The anti-tumor or anti-angiogenesis medicament contains a conjugate comprising a modifying agent and the angiostatin or its fragments, wherein the conjugate exhibits prolonged in vivo half-life as compared to an unmodified angiostatin or its fragments. The modifying agent is selected from the group consisting of macromolecular polymers, protein molecules or fragments thereof, peptides, small molecules, or chemical substances of any other forms.

The present invention relates to heterocyclic derivatives, and more particularly, to novel heterocyclic derivatives useful for the preparation of medicaments for treating diseases related to uric acid.

[Problem]

To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or the like.

[Means of solving the problem]

A compound of Formula (III):

The present invention discloses a stabilized cell-penetrating peptide with a hydrophobic side chain and a preparation method and use of the stabilized cell-penetrating peptide. The stabilized cell-penetrating peptide comprises a cell-penetrating peptidyl peptide and the hydrophobic side chain, and the cell-penetrating peptidyl peptide is a cell-penetrating peptide rich in arginine; and the hydrophobic side chain contains hydrophobic small molecules, the stabilized cell-penetrating peptide is a cyclic peptide with a cyclized side chain and obtained by introducing two natural cysteines into a sequence of the cell-penetrating peptidyl peptide and crosslinking the cell-penetrating peptidyl peptide with the hydrophobic small molecules by an alkylation/arylation reaction of the cysteines. The preparation method of the stabilized cell-penetrating peptide is simple and effective, besides, metabolic stability and cell-penetrating capacity of the cell-penetrating peptide are remarkably improvedby adjusting conformation of the amino acids and hydrophilicity and hydrophobicity of the side chain, deep penetration of in-vitro cell spheres and living tumor tissues by the cell-penetrating peptideis realized, and the cell-penetrating peptide has a good application prospect in the field of medicine delivery.

[Problem]

To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases.

[Means of solving the problem]

A compound of Formula (I):

(where n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR⁷—; and R¹ to R⁷ are specific groups),

a salt of the compound, or a solvate of the salt or the compound.

The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as CDM-Hs, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by introducing cytotoxic moieties to gp120-expressing cells, thereby causing cell death and preventing cell infection and spread of HIV. It is shown that CDM-Hs bind to gp120 and gp-120 expressing cells competitively with CD4, and these compounds cause cell death of HIV-infected cells, thereby decreasing viral infectivity. Compounds and methods are described herein.

The invention discloses a biphenyl compound as well as a preparation method and medical application thereof, the structure of the biphenyl compound is shown as a formula (I) or a formula (II), and thebiphenyl compound or pharmaceutically acceptable salt, tautomer, meso-isomer, raceme, stereoisomer, metabolite, metabolite precursor, prodrug or solvate thereof is a PD-L1 inhibitor. The compound hasa remarkable inhibiting effect on the interaction of PD-1 and PD-L1 protein, so that the compound can be applied to the preparation of PD-L1 inhibitors and immunomodulator drugs for preventing or treating tumors, autoimmune diseases, organ transplant rejection, infectious diseases and inflammatory diseases.

The invention discloses a polysubstituted quinazoline compound and an application thereof, and belongs to the field of chemical medicines. The substituted quinazoline compound represented by the general formula (I) and the pharmaceutically acceptable salt thereof have excellent brain barrier permeability, enhanced metabolic stability and longer metabolic half-life period, show higher inhibitory activity on an activated or drug-resistant mutant form EGFR than a wild type EGFR, and can effectively reduce side effects.

The invention relates to an alpha-amido acyl-ring imide peptoid metalloprotease inhibitor and an application thereof. The invention provides a powerful peptoid metalloprotease inhibitor which embodies outstanding selectivity between endopeptidases and exopeptidases so as to effectively treat diseases expressed by abnormal metalloprotease activity. Specifically, the invention relates to a peptoid compound with a structure of a general formula (I) and salt thereof acceptable on pharmacy. The invention also relates to a medical composition of the peptoid compound with the structure of the formula (I) and the pharmacy application thereof.