34results about How to "Good pharmacodynamic properties" patented technology

The invention belongs to the field of pharmacy, and discloses protein nanometer granules wrapped with taxane medicaments and a preparation method for the nanometer granules. In a formula, the granules comprise the following substances in percentage by weight: 0.1 to 10 percent of taxane medicaments, 0.1 to 40 percent of water-soluble carrier material and 50 to 90 percent of protein substances. The method comprises the following steps of: preparing water-soluble carrier solid dispersion containing the taxane medicaments from the taxane medicaments and the water-soluble carrier material; adding the obtained solid dispersion into an aqueous medium containing the protein substances, mixing uniformly, and performing high-shear treatment on the mixture to obtain suspension of the protein nanometer granules wrapped with slightly-soluble medicaments; and further preparing required formulations. The protein nanometer granules have the advantages of large medicine-carrying quantity, uniform grain diameters, high stability and safety and the like; and by the method, toxic organic solvent residues are avoided, the safety of clinical administration is improved, and a process is simple, low in cost and high in operability.

The invention belongs to the field of pharmacy and discloses a protein nanometer particle for wrapping slightly soluble medicines and a preparation method thereof. The formula of the particle comprises, by weight, 0.1% to 10% of slightly soluble medicines, 0.1% to 40% of soluble carrier material and 50% to 90% of protein material. The preparation method comprises the steps of first making the slightly soluble medicines and the soluble carrier material into a soluble carrier solid dispersoid containing the slightly soluble medicines; then adding the obtained solid dispersoid into an aqueous medium containing the protein material, mixing evenly, performing high shearing condition processing to mixture, and obtaining suspension of the protein nanometer particle containing the slightly soluble medicines; and further preparing a required dosage form. The protein nanometer particle has the advantages of being high in medicine loading quantity, even in grain diameter, good in stability, high in safety and the like. The preparation method avoids residue of toxic organic solvents, improves safety of clinical medicine usage, and is easy in process, low in cost and strong in operability.

Provided are novel antibody drug conjugates (ADCs), and methods of using such ADCs to treat proliferative disorders.

A compound of general formula I their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, methods of treating diseases with said compounds, and the use of said compounds in the manufacture of medicaments.

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 provides a benzyloxy aromatic ring structure compound represented by a general formula (I), a stereoisomer, an enantiomer or a pharmaceutically acceptable salt thereof, a preparation method thereof, a pharmaceutical composition containing the same, and uses thereof. The compound shown in the general formula (I) can be used for preparing a small-molecule inhibitor of PD1 / PDL1 interaction, and can be used for preventing and / or treating diseases related to PD1 / PDL1 interaction, especially cancers, such as non-small cell lung cancer, small cell lung cancer, melanoma, head and neck cancer, kidney cancer, bladder cancer, local advanced or metastatic urothelial cancer, breast cancer, cervical cancer, metastatic Merkel cell cancer, prostate cancer, liver cancer, intestinal cancer, stomach cancer, multiple myeloma, mantle cell lymphoma, diffuse large B cell lymphoma, liver cancer, hodgkin lymphoma, chronic lymphocytic leukemia, squamous cell carcinoma and the like.

This invention relates to deuterated ω-diphenylurea and derivatives and pharmaceutical acceptable salts thereof. And the pharmaceutical compositions comprising the pharmaceutically acceptable carrier and the deuterium-substituted ω-diphenylurea and derivatives and pharmaceutical acceptable salts thereof are also provided. The deuterium-substituted diphenylurea can be used in treatment or prevention of cancer and other related diseases.

The invention relates to certain 2-(2,4,5-substituted anilino)pyrimidine compounds as shown in a formula I which is described in the specification and an application thereof. The compounds or salts thereof exhibit higher inhibition to EGFR in an activated or drug-resistant mutant form than inhibition to wild-type EGFR. The toxicity associated with wild-type EGFR inhibition is reduced, so the compounds or the salts thereof are expected to have excellent pharmacodynamic properties, higher metabolic stability and better blood-brain barrier permeability, are more applicable to being used as a therapeutic agent, and are specifically applicable to being used for treatment of cancer. Therefore, the compounds or the salts thereof can be used for preparing medicines for treating EGFR-mediated diseases in certain mutant forms, especially medicines for non-small cell lung cancer.

The invention provides a substituted heterocyclic compound as well as a preparation method and application thereof, particularly a substituted heterocyclic compound as well as a derivative, a medicinal composition, a preparation method and application thereof to preparation of a medicine for treating neurogenic diseases. Furthermore, the invention provides a compound or a derivative thereof of a structure of formula A shown in the specification. The derivative is a pharmaceutically acceptable salt, a solvent compound, a nitric oxide, a prodrug, an isomer or a mixture of the substances.

The invention relates to a substituted quinazoline compound, a pharmaceutical composition containing the compound, and applications of the compound, wherein the substituted quinazoline compound with ageneral formula (I) and the pharmaceutically acceptable salt thereof have excellent brain barrier permeability, enhanced metabolic stability and long metabolic half-life period, show high inhibitoryactivity on activated or drug-resistant mutant form EGFR compared with wild type EGFR, and can effectively reduce side effects.

The invention discloses a polysubstituted quinazoline compound and application thereof, and belongs to the field of chemical medicines. The substituted quinazoline compound shown in 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 activated or drug-resistant mutant form EGFR than wild type EGFR, and can effectively reduce side effects.

The invention discloses purine compounds as Trk kinase inhibitors, and belongs to the field of chemical medicines. The purine compounds disclosed by the invention are shown in a general formula (I), have good inhibitory activity on Trk-family protein tyrosine kinase, can be used for treating cancers, pains, inflammation, neurodegenerative diseases, Trypanosome cruzi infection or osteolysis diseases of mammals, and has a wide application prospect.

The invention discloses a phthalimide compound used as a PDE2 / 4 dual inhibitor and a preparation method thereof. The general formula of the phthalimide compound is shown in the specification, and thephthalimide compound has good PDE2 / 4 dual inhibitory activity, can show more excellent pharmacodynamic properties and has small side effects compared with the traditional single PDEs inhibitor. The compound can be used for preparing medicines for treating senile dementia, depression, arthritis, asthma, chronic obstructive pulmonary diseases and the like.

The present invention relates to thiazolidinedione derivatives and pharmaceutical compositions comprising the same. Specifically, the compounds disclosed by the invention have a structure shown as a formula (I), and the definitions of all groups and substituents are as described in the specification; the invention also discloses application of the compounds as a peroxisome proliferator-activated receptor (PPAR) agonist, and particularly relates to application of the compounds in prevention and / or treatment of non-alcoholic steatohepatitis and related diseases.

The present invention relates to certain 2-(2,4,5-substituted anilino)pyrimidine compounds represented by the following formula I and applications thereof. These compounds or salts thereof show higher inhibition of EGFR in activated or drug-resistant mutant forms than in wild-type EGFR. Due to the reduced toxicity associated with wild-type EGFR inhibition, the compound or its salt is expected to have excellent pharmacodynamic properties, higher metabolic stability, better permeability of the blood-brain barrier, and is more suitable for use as a therapeutic agent, Especially suitable for the treatment of cancer. Therefore, these compounds or their salts can be used to prepare drugs for treating certain mutation forms of EGFR-mediated diseases, especially non-small cell lung cancer.

The present invention relates to a substituted pyrimidine compound, its pharmaceutical composition and the use of the compound. It has excellent inhibitory activity on mutant EGFR and mutant HER2, and the substituted pyrimidine compounds with general formula (I) and pharmaceutically acceptable salts thereof have excellent pharmacodynamic properties, metabolic stability and / or better Blood-brain barrier permeability.

The invention relates to a fused ring compound and a preparation method, a pharmaceutical composition and application thereof. The fused ring compound has the structural characteristics of a formula (I). The fused ring compound is a somatostatin receptor subtype 4 (SSTR4) agonist compound which is novel in structure, better in drug effect, high in bioavailability and better in solubility.

The present invention provides a compound with benzyloxy aromatic ring structure represented by general formula (I), its stereoisomer, enantiomer or pharmaceutically acceptable salt thereof, its preparation method, and its pharmaceutical combination objects and their uses. The compound represented by the general formula (I) can be used to prepare small molecule inhibitors of PD1 / PD-L1 interaction, which can be used to prevent and / or treat diseases related to PD1 / PD-L1 interaction, especially cancer , such as, inter alia, non-small cell lung cancer, small cell lung cancer, melanoma, head and neck cancer, kidney cancer, bladder cancer, locally advanced or metastatic urothelial cancer, breast cancer, cervical cancer, metastatic Merkel cell carcinoma, prostate cancer Carcinoma, liver cancer, colon cancer, gastric cancer, multiple myeloma, mantle cell lymphoma, diffuse large B-cell lymphoma liver cancer, Hodgkin's lymphoma, chronic lymphocytic leukemia, squamous cell carcinoma and other cancers.

The invention discloses an arylpyrazole compound. The arylpyrazole compound has a structure shown in the description. The arylpyrazole compound has good selective PDE4 inhibition activity and weak PDE4D inhibition effect, and can show more excellent pharmacodynamic properties and small side effects compared with a traditional PDE4 inhibitor. The compound can be used for preparing medicines for treating arthritis, asthma, chronic obstructive pulmonary diseases, senile dementia, depression and the like.

The invention belongs to the field of pharmacy, and discloses a preparation method of protein nanoparticles coating an insoluble drug, which comprises the following steps: preparing an insoluble drug and a water-soluble carrier material into a water-soluble carrier solid dispersion containing the insoluble drug; adding the solid dispersion into a water-based medium containing protein substances, evenly mixing, and processing the mixture under high shear conditions to obtain the protein nanoparticle suspension coating the insoluble drug; and preparing the required preparation formulation. The method does not need to introduce any other organic solvent except ethanol, and even does not need to introduce any organic solvent, thereby preventing organic solvent residues in the preparation, and greatly enhancing the safety of clinical application. The method has the advantages of simple technique, low cost and strong operability.

The invention provides a compound with Janus kinase inhibitory activity, a composition containing the compound and application of the compound. The compound is a 4-(3H-imidazo [1, 2-a] pyrrolo [2, 3-e] pyrazine-8-yl)-pyrrolidine-1-amide compound as shown in a formula I or a derivative thereof, and the derivative is a pharmaceutically acceptable salt, ester, prodrug, single crystal or polymorphic substance, solvate or hydrate thereof. The 4-(3H-imidazo [1, 2-a] pyrrolo [2, 3-e] pyrazine-8-yl)-pyrrolidine-1-amide compound or the derivative thereof provided by the invention has excellent Janus kinase inhibition activity and excellent pharmacodynamic performance, and can be used as a Janus kinase inhibitor to provide a new effective choice for treating related diseases.

The present invention is plaster matrix of tolterodine tartrate and / or tolterodine fumarate and the preparation process of plaster for treating bladder hypermobility syndrome. The plaster matrix includes medicine component, adhesive and organic solvent. The tolterodine tartrate and / or tolterodine fumarate plaster is prepared through the following steps: 1. mixing tolterodine tartrate and / or tolterodine fumarate, adhesive and organic solvent, and smearing the mixture onto the lining layer; and 2. covering protection film onto the matrix after the matrix become dry. The tolterodine tartrate and / or tolterodine fumarate plaster is used in treating bladder hypermobility syndrome, and has high effective rate and short curing period.

The invention belongs to the field of pharmacy, and discloses protein nanometer granules wrapped with taxane medicaments and a preparation method for the nanometer granules. In a formula, the granules comprise the following substances in percentage by weight: 0.1 to 10 percent of taxane medicaments, 0.1 to 40 percent of water-soluble carrier material and 50 to 90 percent of protein substances. The method comprises the following steps of: preparing water-soluble carrier solid dispersion containing the taxane medicaments from the taxane medicaments and the water-soluble carrier material; adding the obtained solid dispersion into an aqueous medium containing the protein substances, mixing uniformly, and performing high-shear treatment on the mixture to obtain suspension of the protein nanometer granules wrapped with slightly-soluble medicaments; and further preparing required formulations. The protein nanometer granules have the advantages of large medicine-carrying quantity, uniform grain diameters, high stability and safety and the like; and by the method, toxic organic solvent residues are avoided, the safety of clinical administration is improved, and a process is simple, low in cost and high in operability.

The invention belongs to the field of pharmacy and discloses a protein nanometer particle for wrapping slightly soluble medicines and a preparation method thereof. The formula of the particle comprises, by weight, 0.1% to 10% of slightly soluble medicines, 0.1% to 40% of soluble carrier material and 50% to 90% of protein material. The preparation method comprises the steps of first making the slightly soluble medicines and the soluble carrier material into a soluble carrier solid dispersoid containing the slightly soluble medicines; then adding the obtained solid dispersoid into an aqueous medium containing the protein material, mixing evenly, performing high shearing condition processing to mixture, and obtaining suspension of the protein nanometer particle containing the slightly soluble medicines; and further preparing a required dosage form. The protein nanometer particle has the advantages of being high in medicine loading quantity, even in grain diameter, good in stability, high in safety and the like. The preparation method avoids residue of toxic organic solvents, improves safety of clinical medicine usage, and is easy in process, low in cost and strong in operability.

The invention provides a substituted heterocyclic compound as well as a preparation method and application thereof, particularly a substituted heterocyclic compound as well as a derivative, a medicinal composition, a preparation method and application thereof to preparation of a medicine for treating neurogenic diseases. Furthermore, the invention provides a compound or a derivative thereof of a structure of formula A shown in the specification. The derivative is a pharmaceutically acceptable salt, a solvent compound, a nitric oxide, a prodrug, an isomer or a mixture of the substances.

The invention discloses benzoxadiazatetradecene derivatives and applications thereof, belonging to the field of medicine. A class of benzoxadiazatetradecene derivatives with a structure represented by the general formula (I) provided by the present invention has excellent anaplastic lymphoma enzyme (ALK) inhibitory activity and excellent pharmacodynamic properties, It can significantly prolong the half-life of drug metabolism; it can be safely and effectively used in the treatment of anaplastic lymphoma kinase positive (ALK+) metastatic (advanced) non-small cell lung cancer (NSCLC), etc. Vascular and neurological diseases provide new means.

The present invention provides a 1-[(pyridin-3-yl-sulfonyl)-1H-pyrrol-3-yl]methylamine derivative with the structure shown in the following formula (I), its pharmaceutical composition and application. The 1-[(pyridin-3-yl-sulfonyl)-1H-pyrrole-3-yl]methylamine derivatives provided by the present invention have good gastric acid secretion inhibitory activity and excellent pharmacodynamic properties, and lower toxicity.