IP Library Patent Application 18425572
Patent Application
App. No. 18/425,572

Aminosteroids for the Treatment of a PTP1B Associated Disease

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Quick Facts
Patent No.
US None
App. No.
18/425,572
Abstract

This application is directed to the use of aminosteroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.

Claims (30)

1 . A compound or pharmaceutically acceptable salt thereof selected from the group consisting of:

2 . A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable diluent or carrier.

3 . A method of treating a disorder in a mammal mediated by inhibition of protein tyrosine phosphatase PTP18 comprising administering to a mammal in need thereof a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.

4 . A compound of formula

or a pharmaceutically acceptable salt thereof,

wherein:

R 1 =—NH(CH 2 ) 1-4 —NH —R 6 , H,

R 6 =—(CH 2 ) 1-4 —NH —R 7 or —(CH 2 ) 0-3 —C 1 —C 5 alkyl or —(CH 2 ) 0-3 —C 3 -C 7 cycloalkyl or —(CH 2 ) 0-3 —C 3 -C 6 heterocycloalkyl or —(CH 2 ) 0-3 -aromatic or —(CH 2 ) 0-3 -heteroaromatic or H;

R 7 =—(CH 2 ) 1-4 —NH 2 or —(CH 2 ) 1-4 —NH —(C 1 -C 5 alkyl) or —(CH 2 ) 1-4 —NH —(C 3 -C 6 heterocycloalkyl) or —(CH 2 ) 1-4 —NH-aromatic or —(CH 2 ) 1-4 —NH-heteroaromatic or H;

R 2 =—OH or H;

R 3 =—OH or NH—R 8 methylsulfone or methyl sulfide or H;

R 8 =acetyl, —SO z —CH 3 or —C(O)OCH 3 ;

R 4 =—OH or H; and

5 . A compound of formula

or a pharmaceutically acceptable salt thereof,

wherein:

X 2 =—OH or H;

X 3 =H, —OH, —S(O) 2 —CH 3 , —NHC(O)—CH 3 , —NHC(O)—OCH 3 , —NHC(O)—SCH 3 , —NH—SO 2 CH 3 or —SCH 3 ;

X 4 =—OH or H; and

X 5 =H or —CH 3 .

6 . A compound of formula

or a pharmaceutically acceptable salt thereof,

wherein:

X 2 =—OH or H;

X 7 =—OH or H;

X 4 =—OH or H; and

X 8 =—OH or H.

7 . A method of treating a disorder in a mammal mediated by inhibition of protein tyrosine phosphatase PTP18 comprising administering to a mammal in need thereof a therapeutically effective amount of a compound of claim 4 , or a pharmaceutically acceptable salt thereof.

8 . The method of claim 7 , wherein the disorder is selected from the group consisting of diabetes, obesity, high serum cholesterol, sleep apnea and nonalcoholic steatohepatitis.

9 . A pharmaceutical composition comprising a compound of claim 4 , and a pharmaceutically acceptable diluent or carrier.