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US 2016/0106700 A1Published application
Pharmaceutical Formulation for Histone Deacetylase Inhibitors
AssigneeTetraLogic Shape UK Ltd
InventorsTodd W. Chappell, Keith A. Johnson
Life of this patent
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Abstract
A pharmaceutical composition, comprising a therapeutically effective amount of an active pharmaceutical ingredient (API) compound represented by the following structural formula at least one acidifying agent; and a vehicle base comprising at least one pharmaceutically acceptable non-aqueous solvent. Values and preferred values of the variables in structural formula (I) are defined herein.
Claims38
A pharmaceutical composition, comprising:
- a therapeutically effective amount of an active pharmaceutical ingredient (API) compound represented by the following structural formula
- at least one acidifying agent;
- and
- a vehicle base comprising at least one pharmaceutically acceptable non-aqueous solvent,
- wherein
- n is an integer from 0 to 15,
- R1 and R2 are each independently hydrogen, halogen, an aliphatic group, a heteroaliphatic group, an aryl, a heteroaryl;
- —ORA;
- —C(O)RA;
- —C(O)N(RA)2;
- —CO2RA;
- —CN;
- —SCN;
- —SRA;
- —SORA;
- —SO2RA;
- —NO2;
- —N(RA)2;
- —NHRA;
- —NRAC(O)RA;
- or —C(RA)3;
- and wherein RA for each occurrence is, independently, a hydrogen, an aliphatic group, a heteroaliphatic group, an acyl moiety, an aryl moiety, a heteroaryl moiety, alkoxy;
- aryloxy;
- alkylthio, arylthio, amino, alkylamino, dialkylamino, heteroaryloxy, or heteroarylthio moiety.
21 more elements
A pharmaceutical composition, comprising:
- at least 0.01% by weight of an active pharmaceutical ingredient (API) compound represented by the following structural formula
- at least one acidifying agent;
- and
- at least one pharmaceutically acceptable non-aqueous solvent, wherein:
- n is 6, R2 is hydrogen and R1 is —C(O)ORA, RA is a C1-C12 alkyl;
- the at least one pharmaceutically acceptable non-aqueous solvent is a mixture of ethanol and propylene glycol;
- the at least one acidifying agent is selected from one or more of citric acid and phosphoric acid and the measured pH of the pharmaceutical composition is from about 3 to about 5,
- the pharmaceutical composition further optionally including one or more of the following:
- at least one humectant selected from glycerin and hexylene glycol;
- at least one emollient selected from diisopropyl adipate and oleyl alcohol;
- at least one permeation enhancer selected from ethanol, propylene glycol, or oleyl alcohol a hydroxypropylcellulose gelling agent;
- and
- a butylated hydroxytoluene as an antioxidant.
10 more elements
Dependencies are inferred from the claim text.