Steroids having 7-oxgen and 17-heteroaryl substitution
AssigneeHarbor Therapeutics, Inc.
InventorJames M. Frincke
Life of this patent
Estimating the term…
Abstract
The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3β-hydroxy-17β-aminoandrost-5-ene, 3β-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3α-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3β-hydroxy-16β-fluoro-17β-aminoandrost-5-ene, 1α,3β-dihydroxy-4α-fluoroandrost-5-ene-17-one, 1α,3β,17β-trihydroxy-4α-fluoroandrost-5-ene, 1β,3β-dihydroxy-6α-bromoandrost-5-ene, 1α-fluoro-3β,12α-dihydroxyandrost-5-ene-17-one, 1α-fluoro-3β,4α-dihydroxyandrost-5-ene and 4α-fluoro-3β,6α,17β-trihydroxyandrostane.
Claims14
A compound having the structure
- or a salt thereof, wherein the dotted line is an optional double bond;
- R1 is —OH, ═O, —SH, amide, ester or ether;
- R2 is —OH, ═O, halogen, alkyl, ester or ether;
- R3 is —H, —OH, halogen, alkyl, ester or ether;
- R4 is a heterocycle;
- R5 and R6 independently are —H, —CH3, —C2H5, —C3H7, alkyl, —OH, —F, —Cl, —Br or —I;
- R7 is —CH2—, —C(halogen)2—, CH(α-alkyl), —CH(β-alkyl), —CH(α-OH), —CH(β-OH) or —C(alkyl)2;
- R9 is —CH2—, —CH(α-OH), —CH(β-OH) or —C(alkyl)2— or R9 is ═CH— when the optional double bond is present,
- R10A, R10B, R10C and R10D independently are —H, alkyl, —CH3, halogen, —SRPR or —ORPR and each R10A, R10B, R10C and R10D is independently in the α-configuration or the β-configuration;
- and
- RPR independently are —H or a protecting group.
Dependencies are inferred from the claim text.