Patent ID: 9180099
Filing Date: 2015-11-10
Classification: A61K,A61P,Y10T

Abstract:
1. A tablet composition comprising a compound having solubility of 0 to 10 μg/mL in water at 37° C. and less than 0.5% surfactant, wherein the compound is in the form of crystalline particles and wherein 99% of the particles have a diameter of 27 μm or lower, and wherein 50% of the particles have a diameter of about 1 μm to about 4 μm, wherein the compound is a compound of formula III, IVa, IVb, Va, or Vb: or a pharmaceutically acceptable salt thereof, wherein: R1, R2 and R3 are independently selected from the group consisting of hydrogen, F, Cl, Br, I, —NR5R6, —(C R4 is selected from the group consisting of hydrogen, —(C R5 and R6 are independently selected from the group consisting of hydrogen and —(C R7 is selected from the group consisting of —O—P(═O)(OH) Q is selected from the group consisting of aryl, heteroaryl, —O-aryl, —S-aryl, —O-heteroaryl, and —S-heteroaryl; X is selected from the group consisting of —(CH R8 is selected from the group consisting of hydrogen, —(C Y is selected from the group consisting of —(CH m is 1 or 2, wherein the aryl, heteroaryl, —O-aryl, —S-aryl, —O-heteroaryl, and —S-heteroaryl groups may be substituted with one or more substituents independently selected from the group consisting of F, Cl, Br, I, —NR5R6, —(C 1 -C 6 ) alkyl, —(C 1 -C 6 ) substituted alkyl, —(C 3 -C 9 ) cycloalkyl, —(C 3 -C 9 ) substituted cycloalkyl, —O—(C 1 -C 6 ) alkyl, —O—(C 1 -C 6 ) substituted alkyl, —O—(C 3 -C 9 ) cycloalkyl, —O—(C 3 -C 9 ) substituted cycloalkyl, -aryl, -aryl-(C 1 -C 6 ) alkyl, -aryl-(C 1 -C 6 ) alkyl, —O-aryl, —O—(C 1 -C 4 ) alkyl aryl, heteroaryl, heterocyclyl, —O—(C 1 -C 4 ) alkyl heterocycle, and —(S(═O) 2 )—(C 1 -C 6 ) alkyl.