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: An oral capsule formulation of a PARP inhibitor and a preparation method. The oral capsule formulation comprises a solid dispersion powder of an active ingredient 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl)piperazine-1-carbonyl)benzyl)quinazoline-2,4(1H,3H)-dione, a filler, a disintegrant, a glidant, and a lubricant, wherein less than 10 wt. % of the active ingredient in the solid dispersion powder is in a crystalline form. The defects of the fluidity, hygroscopicity and cohesiveness of the solid dispersion powder which result in the difficulty of production scale up of capsule formulation are addressed, and thus commercial scale production can be achieved, and the prepared capsule exhibits proper dissolution rate, excellent storage stability, meanwhile with a reasonable production cost.

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: Provide crystal forms of 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl) piperazine-1-carbonyl) benzyl) quinazoline-2, 4 (1H,3H)-dione and preparation method thereof.

Abstract: A requirement conformity parsing method and system, an electronic device and a storage medium. The method includes: obtaining a requirements document that needs to be parsed, and viewing a requirement in the requirements document; performing requirement conformity parsing on several upper-level requirements and corresponding lower-level requirements thereof in the requirements document; introducing a requirements knowledge map to semantically expand a proper noun in the requirements; checking a requirement traceability relationship; checking a requirement traceability label existing in the requirements document; and automatically supplementing the requirements document. The method carries out assistant checking on the requirement conformity between different levels, and facilitates requirement analysts to conveniently and quickly review the requirements between different levels.

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 instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.

Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.

Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

Abstract: The present disclosure provides the Pyridopyrimidinone compounds having the structure represented by the general Formula (II) and applications thereof. Studies have shown that the compounds provided by the present disclosure can effectively inhibit the KRAS G12C mutation. KRAS mutation accounts for a large proportion of tumors, and currently there is no approved drug for its treatment. The compounds provided by the present disclosure have the potential to become a therapeutic medicine for malignant tumors (especially non-small cell lung cancer (NSCLC) and colorectal cancer) haboring KRAS G12C mutation, and have great application value.

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: 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: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.