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

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 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 a PDE2 inhibitor phenylpyrazolopyrimidine compound and a preparation method thereof, belonging to the field of medicinal chemistry. The general formula of the phenylpyrazolopyrimidine compound is that the compound has better PDE2 inhibitory activity, exhibits more excellent pharmacodynamic properties and has less side effects. This type of compound can be used to prepare medicines for treating senile dementia, depression, anxiety, cardiovascular and cerebrovascular diseases and the like.

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 isobenzofuran derivatives with a structure represented by a formula I shown in the description for an SGLT-2 inhibitor, a pharmaceutical composition and preparation of the derivatives, and an application of the derivatives, wherein in the description, R1 and R2 are independently selected from hydrogen or deuterium and at least contain one deuterium. The isobenzofuran derivatives having the structure represented by the formula I provided by the invention have good SGLT-2 inhibitory activity, excellent pharmacodynamic properties, and lower toxicity.

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 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.