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US 2011/0212935 A1Published application
Compositions and treatment methods-4
AssigneeHarbor BioSciences, 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.
Claims26
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, optionally substituted alkyl, ester or ether;
- R3 is —H, —OH, halogen, optionally substituted alkyl, ester or ether;
- R4 is optionally substituted heterocycle;
- R5 and R6 independently are —H, —CH3, —C2H5, —C3H7, optionally substituted alkyl, —OH, —F, —Cl, —Br or —I;
- R7 is —CH2—, —C(halogen)2-, —CH(α-optionally substituted alkyl), —CH(β-optionally substituted alkyl), —CH(α-OH), —CH(β-OH) or —C(optionally substituted alkyl)2-;
- R9 is —CH2—, —CH(α-OH), —CH(β-OH) or —C(optionally substituted alkyl)2-;
- and
- R10A, R10B, R10C and R10D independently are —H, optionally substituted alkyl, —CH3, halogen, —SRPR or —ORPR and each R10A, R10B, R10C and R10D is independently in the α-configuration or the β-configuration and wherein RPR independently are —H or a protecting group.
7 more elements
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, optionally substituted alkyl, ester or ether;
- R3 is —H, —OH, halogen, optionally substituted alkyl, ester or ether;
- R4 is optionally substituted heterocycle;
- R5 and R6 independently are —H, —CH3, —C2H5, —C3H7, optionally substituted alkyl, —OH, —F, —Cl, —Br or —I;
- R7 is —CH2—, —C(halogen)2-, —CH(α-optionally substituted alkyl), —CH(β-optionally substituted alkyl), —CH(α-OH), —CH(β-OH) or —C(optionally substituted alkyl)2-;
- R9 is —CH2—, —CH(α-OH), —CH(β-OH) or —C(optionally substituted alkyl)2-;
- and
- R10A, R10B, R10C and R10D independently are —H, optionally substituted alkyl, —CH3, halogen, —SRPR or —ORPR and each R10A, R10B, R10C and R10D is independently in the α-configuration or the β-configuration and wherein RPR independently are —H or a protecting group.
7 more elements
A compound having the structure
- or a salt thereof, wherein the dotted lines are optional double bonds;
- R1 is —OH, ═O, —SH, amide, ester or ether;
- R2 is —OH, ═O, halogen, optionally substituted alkyl, ester or ether;
- R3 is —H, —OH, halogen, optionally substituted alkyl, ester or ether;
- R4 is —OH, ester, ether, —NH2, —NH—C(O)CH3, —NH—CH3, —N(CH3)2, —NHOH or optionally substituted heterocycle;
- R5 and R6 independently are —H, —CH3, —C2H5, —C3H7, optionally substituted alkyl, —OH, —F, —Cl, —Br or —I;
- R7 is —C(halogen)2-, —CH(α-optionally substituted alkyl), —CH(β-optionally substituted alkyl), —CH(α-OH), —CH(β-OH) or —C(optionally substituted alkyl)2-;
- and
- R9 is —CH(α-OH), —CH(β-OH) or —C(optionally substituted alkyl)2-.
6 more elements
A compound having the structure
- or a salt thereof, wherein the dotted lines are optional double bonds;
- R1 is —OH, ═O, —SH, amide, ester or ether;
- R2 is —OH, ═O, halogen, optionally substituted alkyl, ester or ether;
- R3 is —H, —OH, halogen, optionally substituted alkyl, ester or ether;
- one R4 is —OH, ester, ether, —NH2, —NH—C(O)CH3, —NH—CH3, —N(CH3)2, —NHOH or optionally substituted heterocycle;
- the other R4 is —H, optionally substituted alkyl, halogen, —SH or —OH;
- R5 and R6 independently are —H, —CH3, —C2H5, —C3H7, optionally substituted alkyl, —OH, —F, —Cl, —Br or —I;
- R7 is —CH2—, —C(halogen)2-, —CH(α-optionally substituted alkyl), —CH(β-optionally substituted alkyl), —CH(α-OH), —CH(β-OH) or —C(optionally substituted alkyl)2-;
- R9 is —CH2—, —CH(α-OH), —CH(β-OH) or —C(optionally substituted alkyl)2-;
- and
- R10A, R10B, R10C and R10D independently are —H, optionally substituted alkyl, —CH3, halogen, —SRPR or —ORPR and each R10A, R10B, R10C and R10D is independently in the α-configuration or the β-configuration, wherein RPR independently are —H or a protecting group and wherein one or two of R10A, R10B, R10C and R10D are not —H.
8 more elements
A compound having the structure
- or a salt thereof, wherein the dotted lines are optional double bonds;
- R1 is —OH, ═O, —SH, amide, ester or ether;
- R2 is —H, —OH, ═O, halogen, optionally substituted alkyl, ester or ether;
- R3 is —H, —OH, halogen, optionally substituted alkyl, ester or ether;
- one R4 is —OH, ester, ether, —NH2, —NH—C(O)CH3, —NH—CH3, —N(CH3)2, —NHOH or optionally substituted heterocycle;
- the other R4 is —H, optionally substituted alkyl, halogen, —SH or —OH;
- R5 and R6 independently are —H, —CH3, —C2H5, —C3H7, optionally substituted alkyl, —OH, —F, —Cl, —Br or —I;
- R7 is —CH2—, —C(halogen)2-, —CH(α-optionally substituted alkyl), —CH(β-optionally substituted alkyl), —CH(α-OH), —CH(β-OH) or —C(optionally substituted alkyl)2-;
- R9 is —CH2—, —CH(α-OH), —CH(β-OH) or —C(optionally substituted alkyl)2-;
- and
- R10A, R10B, R10C and R10D independently are —H, optionally substituted alkyl, —CH3, halogen, —SRPR, —ORPR, α-OH, β-OH or ═O and each R10A, R10B, R10C and R10D is independently in the α-configuration or the β-configuration,
- wherein RPR independently are —H or a protecting group and wherein R10A and R10C, R10B and R10C or R10C and R10D are not —H.
9 more elements
Dependencies are inferred from the claim text.