| 主权项 |
1. An aqueous suspension pharmaceutical composition suitable for parenteral administration in a mammalian patient comprising a very slightly soluble, practically insoluble or insoluble active ingredient that is a compound of formula Iwherein:
R1 is H, alkyl, —COalkyl, —COaryl, —COheteroaryl, —CO2alkyl, —(CH2)aOH, —(CH2)bCOOR10, —(CH2)cCONH2, —SO2alkyl, or —SO2aryl; R2 is H or alkyl; R3 is H, alkyl, —(CH2)daryl, —(CH2)eheteroaryl, —(CH2)fcycloalkyl, —(CH2)gheterocycloalkyl, —CH(cycloalkyl)2, or —CH(heterocycloalkyl)2; R4 and R6 are independently H or alkyl; R5 is H, alkyl, alkoxy, or OH; or R4 and R5, together with the atoms to which they are attached, to form a 5- or 6-membered azacycloalkyl structure; R7 and R8 are independently H, alkyl, alkoxy, CN, or halo; R9 is aryl or heteroaryl; R10 is H or alkyl; a, b, c, d, e, f and g are independently 1, 2 or 3; *1 and *2 denote chiral centres; alkyl is a linear saturated hydrocarbon having up to 10 carbon atoms (C1-C10) or a branched saturated hydrocarbon of between 3 and 10 carbon atoms (C3-C10); wherein the alkyl may optionally be substituted with 1 or 2 substituents that are independently (C3-C10)cycloalkyl, (C1-C6)alkoxy, OH, CN, CF3, COOR11, fluoro, or NR11R12; cycloalkyl is a mono- or bi-cyclic saturated hydrocarbon of between 3 and 10 carbon atoms; wherein the cycloalkyl may optionally be fused to an aryl group; heterocycloalkyl is a C-linked or N-linked 3 to 10 membered saturated, mono- or bi-cyclic ring, wherein said heterocycloalkyl ring contains, where possible, 1, 2 or 3 heteroatoms that are independently N, NR1, or O; alkoxy is a linear O-linked hydrocarbon of between 1 and 6 carbon atoms (C1-C6) or a branched O-linked hydrocarbon of between 3 and 6 carbon atoms (C3-C6); wherein the alkoxy may optionally be substituted with 1 or 2 substituents that are independently (C3-C10)cycloalkyl, OH, CN, CF3, COOR11, fluoro, or NR11R12; aryl is phenyl, biphenyl or naphthyl; wherein the aryl may be optionally substituted with up to 5 substituents that are independently alkyl, alkoxy, OH, halo, CN, COOR11, CF3, or NR11R12; heteroaryl is a 5, 6, 9 or 10 membered mono- or bi-cyclic aromatic ring, containing, where possible, 1, 2 or 3 ring members that are independently N, NR11, S and O; heteroaryl may be optionally substituted with 1, 2 or 3 substituents independently selected from alkyl, alkoxy, OH, halo, CN, COOR11, CF3, or NR11R12; R and R12 are independently H or alkyl;or a tautomer, isomer, stereoisomer (including an enantiomer, diastereoisomer or a racemic or scalemic mixture thereof), pharmaceutically acceptable salt, and/or solvate thereof. |
