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 present invention provides a solid pharmaceutical formulation of PARP inhibitors and its use thereof, and more specifically a solid dispersion powder including 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl)piperazine-1-carbonyl)benzyl)quinazoline-2,4(1H,3H)-dione and polymers, wherein the content of polymers is from about 50 wt % to about 80 wt %, and wherein less than 10 wt % of 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl)piperazine-1-carbonyl)benzyl)quinazoline-2,4(1H,3H)-dione is in crystalline form. The present invention also provides a method for preparing the solid dispersion powder, a pharmaceutical composition including the solid dispersion powder and the use of the pharmaceutical composition for treating diseases caused by PARP activity abnormalities.

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 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.

Abstract: This disclosure provides a process for preparing 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones, specially provides a method for preparing the compound of Formula I, and the method comprises the step of reacting the compound of Formula II with the compound of Formula A in the presence of a condensation agent, an organic base and an organic solvent by condensation.

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 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: This disclosure provides a process for preparing 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones, specially provides a method for preparing the compound of Formula I, and the method comprises the step of reacting the compound of Formula II with the compound of Formula A in the presence of a condensation agent, an organic base and an organic solvent by condensation.

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 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, 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 novel 1-(arylmethyl)-5,6,7,8-tetrahydroquinazoline-2,4-diones and analogs thereof, represented by the Formula 1: wherein Ar, A, R1, R3-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, such as cancer.

Abstract: The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP.

Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, 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 3-aryl-6-aryl-[1,2,4]triazolo[4,3-?]pyridines thereof, represented by the Formula (I) wherein Ar1, Ar2, R1—R3 are defined herein. Compounds having Formula (I) are inhibitors of cell proliferation. Therefore, compounds of the invention may be used to treat clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.