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.

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 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 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 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.