Abstract: Disclosed are a new AXL-targeting monoclonal antibody and antibody-drug conjugate. Also disclosed is a method for preparing said antibody and antibody-drug conjugate. The AXL antibody of the present invention can bind with purified human AXL protein and multiple AXL on tumor cell surface with high effectiveness and high specificity. Said humanized antibody also has high affinity and low immunogenicity. Said AXL antibody-drug conjugate has markable performance against tumors having high AXL expression.

Abstract: Provided are an aromatic ring-lactam compound as shown in formula (I), and a preparation method therefor and the use thereof. The aromatic ring-lactam compound has a novel structure, has good inhibitory activity on ERK1/2 kinases, can inhibit the proliferation of tumor cells, and has anti-tumor activity.

Abstract: A benzothiazolyl biaryl compound represented by general formula I, or a pharmaceutically acceptable salt thereof, or an enantiomer, a diastereoisomer, a tautomer, a torsional isomer, a solvate, a polymorph, or a prodrug thereof, a preparation method therefor, and a use thereof as a KRASG12C inhibitor.

Abstract: The present disclosure relates to a fused ring pyrimidine amino compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically disclosed in the present disclosure are the compound shown in formula I, a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof. The fused ring pyrimidine amino compound of the present application has good inhibitory activity against DDRs, particularly DDR2, and has a good therapeutic effect on tumors and fibrotic diseases, especially pulmonary inflammation and pulmonary fibrosis. Also disclosed in the present disclosure are a preparation method for the compound shown in formula I, and a use thereof.

Abstract: A tissue factor (TF)-targeted antibody-drug conjugate (ADC) and a method for preparing the ADC. The ADC is capable of binding to TF antigen with high specificity, and has high affinity, low immunogenicity, high cytotoxicity, and significant anti-tumor activity.

Abstract: A tissue factor (TF)-targeted antibody-drug conjugate (ADC) and a method for preparing the ADC. The ADC is capable of binding to TF antigen with high specificity, and has high affinity, low immunogenicity, high cytotoxicity, and significant anti-tumor activity.

Abstract: The present disclosure relates to a fused ring pyrimidine amino compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically disclosed in the present disclosure are the compound shown in formula I, a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof. The fused ring pyrimidine amino compound of the present application has good inhibitory activity against DDRs, particularly DDR2, and has a good therapeutic effect on tumors and fibrotic diseases, especially pulmonary inflammation and pulmonary fibrosis. Also disclosed in the present disclosure are a preparation method for the compound shown in formula I, and a use thereof.

Abstract: The present invention relates to dihydroquinoxaline bromodomain recognition protein inhibitor, preparation method and use thereof. The inhibitor of the present invention is compound represented by general formula (I), or stereoisomer, pharmaceutically acceptable salt, prodrug, solvate, hydrate and crystal form thereof. The definition of each substituent is as described in the description and claims. The compound represented by general formula (I) of the present invention may inhibit bromodomain recognition protein and may be used for preparing medicament which regulates the apparent state of cells and treats series of diseases and symptoms which are mediated by the bromodomain recognition protein.

Abstract: Disclosed are a new AXL-targeting monoclonal antibody and antibody-drug conjugate. Also disclosed is a method for preparing said antibody and antibody-drug conjugate. The AXL antibody of the present invention can bind with purified humanAXL protein and multiple AXL on tumor cell surface with high effectiveness and high specificity. Said humanized antibody also has high affinity and low immunogenicity. Said AXL antibody-drug conjugate has markable performance against tumors having high AXL expression.

Abstract: Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.

Abstract: The present invention relates to dihydroquinoxaline bromodomain recognition protein inhibitor, preparation method and use thereof. The inhibitor of the present invention is compound represented by general formula (I), or stereoisomer, pharmaceutically acceptable salt, prodrug, solvate, hydrate and crystal form thereof. The definition of each substituent is as described in the description and claims. The compound represented by general formula (I) of the present invention may inhibit bromodomain recognition protein and may be used for preparing medicament which regulates the apparent state of cells and treats series of diseases and symptoms which are mediated by the bromodomain recognition protein.

Abstract: Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.

Abstract: A tissue factor (TF)-targeted antibody-drug conjugate (ADC) and a method for preparing the ADC. The ADC is capable of binding to TF antigen with high specificity, and has high affinity, low immunogenicity, high cytotoxicity, and significant anti-tumor activity.

Abstract: Provided is a process of synthesizing a substituted pyridine and pyrimidine compound. Particularly, provided is a method for preparing a compound of formula III via a compound of formula II?, wherein the definition of each of groups is as described as the description. Compound with other methods, the method in the present invention has features of high yield and a result product being easier to separate.

Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.

Abstract: This invention provides a class of five-member-heterocycle fused pyridine compounds as shown below in Formula (X), pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, a method of producing the same, pharmaceutical compositions containing the compound, and use of the compounds in preparing medicament for preventing and/or treating diseases and tumors associated with abnormal protein tyrosine kinase.

Abstract: Provided is a process of synthesizing a substituted pyridine and pyrimidine compound. Particularly, provided is a method for preparing a compound of formula III via a compound of formula II?, wherein the definition of each of groups is as described as the description. Compound with other methods, the method in the present invention has features of high yield and a result product being easier to separate.

Abstract: The present invention belongs to the field of pharmaceutical Chemistry. In particular, the present invention relates to a pyridopyrimidine or pyrimidopyrimidine compound as represented by general formula (I), or an isomer thereof or a pharmaceutically acceptable salt, ester, prodrug or solvate thereof, a preparation method, a pharmaceutical composition and uses thereof in preparing a mTOR inhibitor. As a mTOR inhibitor, the compound or the pharmaceutical composition thereof can be used for treating a disease or condition due to PI3K-AKT-mTOR signalling pathway malfunction.

Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I] which is useful as a renin inhibitor. wherein R1 is a cycloalkyl group or an alkyl, R22 is an optionally substituted aryl and the like, R is a lower alkyl group, R3, R4, R5 and R6 are the same or different, and are a hydrogen atom, an optionally substituted carbamoyl, an optionally substituted alkyl, or alkoxycarbonyl, or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are as represented by Formula (I) a quinazoline derivative and a pharmaceutical acceptable salt thereof, or, an enantiomer, a non-enantiomer, a tautomer, a racemate, a solvate, a metabolic precursor, or a prodrug of both. Also disclosed are a preparation method therefor, an intermediate, a pharmaceutical composition having the quinazoline derivative, and an application thereof. The quinazoline derivative of the present invention is provided with improved anti-tumor activity.