Abstract: Indazole derivatives represented by formula (I) or stereoisomers, tautomers, and pharmaceutically acceptable salts thereof are provided. A preparation method of indazole derivatives represented by formula (I) and a method of use of the indazole derivatives as therapeutic agents is also provided.

Abstract: The present disclosure relates to a piperazine derivative, a preparation method therefor, and use thereof in medicine. Specifically, the present invention relates to a piperazine derivative represented by general formula (I), a preparation method therefor, and a pharmaceutically acceptable salt or prodrug thereof, and use thereof as a therapeutic agent, in particular, as an inhibitor of coagulation factor XIa (FXIa), wherein the definition of each substituent in general formula (I) is the same as that in the description.

Abstract: The present invention relates to a tetracyclic derivative, a method for preparing same and the use thereof in medicine. In particular, the present invention relates to a tetracyclic derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, especially as a K-Ras GTPase inhibitor, with definitions of each substituent in general formula (I) being the same as of which are defined in the description.

Abstract: The present invention relates to a piperazine amide derivative as represented by formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition thereof, and use of same as a therapeutic agent, especially as a selective Rearranged During Transfection (RET) kinase inhibitor. Ring a, ring e, X1, X2, X3, X4, R1, R2, R3, R4, R4?, R5, R5?, R6, R6?, R7, R7?, R8, m and n have the same definitions as those in the specification.

Abstract: Indazole derivatives represented by formula (I) or stereoisomers, tautomers, and pharmaceutically acceptable salts thereof are provided. A preparation method of indazole derivatives represented by formula (I) and a method of use of the indazole derivatives as therapeutic agents is also provided.

Abstract: A solid dispersion, a method for preparing same, and a solid preparation comprising the solid dispersion. The solid dispersion contains (R)-4-amino-1-(1-(but-2-ynylacyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazine-7-one or a pharmaceutically acceptable salt thereof, and a carrier material. The carrier material is selected from hydroxypropyl methylcellulose acetate succinate and hydroxypropyl methylcellulose phthalate.

Abstract: The present invention provides a phenylpropanamide derivative as represented by formula (I), a manufacturing method of the derivative, application of the derivative as a ?-opioid receptor (KOR) agonist, and application of the derivative for manufacturing a pharmaceutical product for treating and/or preventing pain or a pain-related disease.

Abstract: The invention provides novel compounds that may serve as anticancer therapeutics. The compounds of the invention bind to polo-like kinases through the polo-box domain. In certain embodiments, the compounds of the invention are POM-protected peptide derivatives. The use of cationic bis-alkyl his residues in combination with a mono POM-protected phophoryl group results in a peptide possessing an overall neutral charge. The peptide derivatives of the invention have achieved both good efficacy and an enhanced bioavailability. The invention also provides methods of use, compositions, and kits thereof. Further, the invention provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.

Abstract: The invention provides novel compounds that may serve as anticancer therapeutics. The compounds of the invention bind to polo-like kinases through the polo-box domain. In certain embodiments, the compounds of the invention are POM-protected peptide derivatives. The use of cationic bis-alkyl his residues in combination with a mono POM-protected pho-phoryl group results in a peptide possessing an overall neutral charge. The peptide derivatives of the invention have achieved both good efficacy and an enhanced bioavailability. The invention also provides methods of use, compositions, and kits thereof. Further, the invention provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.

Abstract: Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds. The compounds of the invention have potential therapeutic activity in view of their binding and inhibitory activities towards Plk1. They are based on the amino acid sequence PLHSpT (phosphorylated Thr). The PEG moiety, when present, is covalently attached at the N-terminus.