Abstract: Provided in the present invention are a substituted fused bicyclic compound as a kinase inhibitor and the use thereof. The substituted fused bicyclic compound has a structure as represented by formula I below, wherein a ring A, R0, B1-B3, D1-D3, R7 and R8 are defined herein. The compound of formula I is an NUAK1/2 inhibitor. Therefore, the compound of the present invention can be used for treating and preventing NUAK1/2-mediated diseases, disorders and conditions, such as cancer, and used in the preparation of drugs for treating and preventing NUAK1/2-mediated diseases, disorders and conditions.

Abstract: Provided is a use of Wee1 kinase inhibitors in the treatment of cancer. In particular, provided is a use of Wee1 kinase inhibitors in the preparation of drugs for the treatment of cancers with Histone H3K27M mutation.

Abstract: The disclosure provides novel substituted imidazo [1, 5-b] pyridazine compounds as represented in Formula I: wherein A, R0, R1, R2 and R3 are defined herein. The compounds of Formula I are kinase inhibitors, especially ATR kinase inhibitors. Therefore, the compounds of the disclosure may be used to treat ATR-mediated diseases, disorders and conditions, such as cancer.

Abstract: Disclosed are dihydroimidazopyrimidopyrimidinone compounds, specifically represented by Formula I: or pharmaceutically acceptable salts or prodrugs thereof, wherein the substituents are defined herein. Compounds of Formula I are Wee1 kinase inhibitors. Therefore, compounds of the invention may be used to treat diseases caused by abnormal Wee1 activity.

Abstract: The present disclosure relates to method of combination therapies of PARP inhibitors. Specifically, the present disclosure relates to combination therapies of a PARP inhibitor represented by the following Formula (I) and a low dose of a DNA damaging anti-cancer drug. Adopting the combination therapy of the present disclosure can reduce the daily dose of DNA damaging anti-cancer drugs, reduce toxicity and improve anti-cancer effects.

Abstract: The disclosure provides novel substituted fused heteroaromatic compounds as represented in Formula I, wherein A1-A6 and R1-R4 are defined herein. The compounds of Formula I are kinase inhibitors, especially ATR kinase inhibitors. Therefore, the compounds of the disclosure may be used to treat ATR-mediated diseases, disorders and conditions, such as cancer.

Abstract: The disclosure relates to substituted fused heteroaromatic tricyclic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A1-A3, B1-B3, D1-D4 and R1-R2 are defined herein. Compounds having Formula I are ATM kinase inhibitors. Therefore, compounds of the disclosure may be used to treat clinical conditions caused by DDR functional defects, such as cancer.

Abstract: The disclosure provides substituted imidazo[1,5-a]quinoxaline and related compounds as kinase inhibitors, and their uses. Specifically, the disclosure provides compounds of Formula I, or pharmaceutically acceptable salts thereof or prodrugs thereof, wherein, A1-A3, Cy and R1-R2 are defined herein. The compounds of Formula I are kinase inhibitors. Therefore, the compounds of the disclosure can be used to treat clinical conditions caused by DDR function defects, such as cancers.

Abstract: The disclosure provides novel compounds as represented in Formula I, wherein A0-A2, R0-R6, L, Z and Q are defined herein. The compounds of Formula I are CHK1 inhibitors. Therefore, the compounds of the disclosure can be used to treat diseases, disorders and conditions associated with continuous activation of CHK1 or with high internal DNA damage or injury during DNA replication, such as cancers.

Abstract: The disclosure provides novel substituted fused heteroaromatic compounds as represented in Formula I, wherein A1-A6 and R1-R4 are defined herein. The compounds of Formula I are kinase inhibitors, especially ATR kinase inhibitors. Therefore, the compounds of the disclosure may be used to treat ATR-mediated diseases, disorders and conditions, such as cancer.

Abstract: A compound of formula I, or a stereoisomer, tautomer, N-oxide, hydrate, isotope-substituted derivative, or solvate thereof, or a pharmacologically acceptable salt thereof, or a mixture thereof, of a prodrug thereof. The compound of formula I is a kinase inhibitor which can be used for treating clinical disorder caused by DDR deficiencies, such as cancers.

Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones represented by the Formula (I): wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.

Abstract: Disclosed are imidazo[1,2-b]pyrimido[4,5-d]pyridazin-5(6H)-one compounds, specifically represented by the Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A and R1-R5 are defined herein. Compounds having Formula I are Wee1 kinase inhibitors. Therefore, compounds of the disclosure may be used to treat diseases caused by abnormal Wee1 activity.

Abstract: Disclosed are 8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one compounds, specifically represented by the Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A and R1-R7 are defined herein. Compounds having Formula I are Wee1 kinase inhibitors. Therefore, compounds of the disclosure may be used to treat diseases caused by abnormal Wee1 activity.

Abstract: The disclosure relates to substituted fused heteroaromatic tricyclic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A1-A3, B1-B3, D1-D4 and R1-R2 are defined herein. Compounds having Formula I are ATM kinase inhibitors. Therefore, compounds of the disclosure may be used to treat clinical conditions caused by DDR functional defects, such as cancer.

Abstract: The disclosure relates to substituted fused heteroaromatic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A1-A4, B1-B3, D1-D4 and R1-R3 are defined herein. Compounds having Formula I are kinalse inhibitors. Therefore, compounds of the disclosure may be used to treat clinical conditions caused by DDR functional defects, such as cancer.

Abstract: Disclosed are 8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one compounds, specifically represented by the Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A and R1-R7 are defined herein. Compounds having Formula I are Wee1 kinase inhibitors. Therefore, compounds of the disclosure may be used to treat diseases caused by abnormal Wee1 activity.

Abstract: Disclosed are 8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one compounds, specifically represented by the Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A and R1-R7 are defined herein. Compounds having Formula I are Wee1 kinase inhibitors. Therefore, compounds of the disclosure may be used to treat diseases caused by abnormal Wee1 activity.

Abstract: Disclosed are novel N-(3-heteroarylaryl)-4-arylarylcarboxamides and analogs thereof, represented by the Formula I: wherein C cyclic group, D1-D4, Q1, Q2, R5 are defined herein. Compounds having Formula (I) are hedgehog pathway inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of hedgehog activity, such as cancer.

Abstract: Disclosed are imidazo[1,2-b]pyrimido[4,5-d]pyridazin-5(6H)-one compounds, specifically represented by the Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A and R1-R5 are defined herein. Compounds having Formula I are Wee1 kinase inhibitors. Therefore, compounds of the disclosure may be used to treat diseases caused by abnormal Wee1 activity.