Pharmaceutical formulations

A pharmaceutical composition comprising a substantially amorphous high energy dispersion, said high energy dispersion comprising:

• a pharmaceutically active ingredient comprising a compound having the Formula:
• where,
• (d) R1 and R2 are, independently of one another, each a C1-15 alkyl group, branched or straight chain, with or without one or more substituents, a C2-15 alkenyl group, branched or straight chain, with or without one or more substituents, a C2-15 alkynyl group, branched or straight chain, with or without one or more substituents, a C3-15 cycloalkyl group, with or without one or more substituents, an arylalkyl group, with or without one or more substituents, an aryl group, with or without one or more substituents, a heteroaryl group, with or without one or more substituents, —OR5, —COOR5, —C(O)R5 or —C(O)N(R5)2, where, R5 is a hydrogen atom or a hydrocarbon radical, with or without one or more substituents, or one of R1 and R2 is a hydrogen atom and the other one of R1 and R2 is defined the same as above;
• (e) R3 is an aryl group, with or without one or more substituents, a heteroaryl group, with or without one or more substituents, or a heterocyclic group having 1 to 3 heteroatoms fused to a 5- or 6-membered aryl ring, with or without one or more substituents, with the proviso that R3 is not an aryl group substituted at its para position with a —Y-aryl group, where, Y is a carbon-carbon single bond, —CO—, —O—, —S—, —N(R21)—, —CON(R22)—, —N(R22)CO—, —OCH2—, —CH2O—, —SCH2—, —CH2S—, —NHC(R23)(R24)—, —NR23SO2—, —SO2NR23—, (R23)(R24)NH—, —CH═CH—, —CF═CF—, —CH═CF—, —CF═CH—, —CH2CH2—, —CF2CF2—,
• where,
• R21 is a hydrogen atom or a —CO(C1-4 alkyl), C1-6 alkyl, allyl, C3-6 cycloalkyl, phenyl or benzyl group;
• R22 is a hydrogen atom or a C1-6 alkyl group;
• R23 is a hydrogen atom or a C1-5 alkyl, aryl or —CH2-aryl group;
• R24 is a hydrogen atom or a C1-4 alkyl group;
• R25 is a hydrogen atom or a C1-8 alkyl, C1-8 perfluoroalkyl, C3-6 cycloalkyl, phenyl or benzyl group;
• R26 is a hydrogen atom or a C1-6 alkyl, C3-6 cycloalkyl, phenyl or benzyl group;
• R27 is —NR23R24, —OR24, —NHCONH2, —NHCSNH2,
• R28 and R29 are, independently of one another, each a C1-4 alkyl group or, taken together with each other, a —(CH2)q group, where q is 2 or 3;
• and
• (f) R4 is a C3-15 cycloalkyl group, with or without one or more substituents, a C3-15 cycloalkenyl group, with or without one or more substituents, or a heterocycloalkyl group of 3 to 15 members, with or without one or more substituents;
• wherein, the one or more substituents for all the groups are chemically-compatible compatabile and are, independently of one another, each an:
• alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, arylalkyl, alkylaryl, aryl, heteroaryl, heterocycloalkyl, hydroxyalkyl, arylalkyl, aminoalkyl, haloalkyl, thioalkyl, alkylthioalkyl, carboxyalkyl, imidazolylalkyl, indolylalkyl, mono-, di- and trihaloalkyl, mono-, di- and trihaloalkoxy, amino, alkylamino, dialkylamino, alkoxy, hydroxy, halo, nitro, oximino, —COOR50, —COR50, —SO0-2R50, —SO2NR50R51, NR52SO2R50, ═C(R50R51), ═N—OR50, ═N—CN, ═C(halo)2, ═S, ═O, —CON(R50R51), —OCOR50, —OCON(R50R51), —N(R52)CO(R50), —N(R52)COOR50 or —N(R52)CON(R50R51) group, where:
• R50, R51 and R52 are, independently of one another, each a hydrogen atom or a branched or straight-chain, optionally substituted, C1-6 alkyl, C3-6 cycloalkyl, C4-6 heterocycloalkyl, heteroaryl or aryl group, or R50 and R51 are joined together to form a carbocyclic or heterocyclic ring system, or R50, R51 and R52 are, independently of one another, each:
• where,
• R40 and R41 are, independently of one another, each a hydrogen atom or a branched or straight-chain, optionally substituted, alkyl, cycloalkyl, heterocycloalkyl, halo, aryl, imidazolylalkyl, indolylalkyl, heteroaryl, arylalkyl, arylalkoxy, heteroarylalkyl, heteroarylalkoxy, aminoalkyl, haloalkyl, mono-, di- or trihaloalkyl, mono-, di- or trihaloalkoxy, nitro, cyano, alkoxy, hydroxy, amino, phosphino, phosphate, alkylamino, dialkylamino, formyl, alkylthio, trialkylsilyl, alkylsulfonyl, arylsulfonyl, alkylsulfinyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxyalkyl, morpholino, thioalkyl, alkylthioalkyl, carboxyalkyl, oximino, —COOR50, —COR50, —SO0-2R50, —SO2NR50R51, —NR52SO2R50, —CON(R50R51), —OCON(R50R51), —N(R52)CO(R50), —N(R52)COOR50, —N(R52)CON(R50R51) or —OCONR50 group, where, R50, R51 and R52 are defined the same as above;
• R42 is a hydrogen atom or a branched or straight-chain, optionally substituted, alkyl, alkenyl, arylalkyl or acyl group;
• and
• R43 is a hydrogen atom or a branched or straight-chain, optionally substituted, alkyl or aryl group;
• wherein, the optional substituents are defined the same as above for the one or more substituents;
• in admixture with a polymer matrix comprising a polymeric carrier and a wetting agent, wherein the ratio of the pharmaceutically active ingredient to the polymer matrix is about 1:1 to about 1:10.