Glucocortiocoid-selective agents
AssigneeAbbott Laboratories
InventorsMichael J. Coghlan, Jay R. Luly, Jeffrey M. Schkeryantz, Alan X. Wang
Life of this patent
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Abstract
Compounds having Formula I ##STR1## are useful for modulating the glucocorticoid receptor in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of treating immune, autoimmune, inflammatory, adrenal imbalance, cognitive and behavioral diseases in a mammal.
Claims9
A method of selectively modulating the glucocorticoid receptor-mediated gene expression in a mammal comprising administering an effective amount of a compound of Formula I ##STR8## or a pharmaceutically acceptable salt or prodrug thereof, where R.sup.1 is hydrogen;
- L.sup.1 is a covalent bond;
- R.sup.2 and R.sup.3 are independently selected from
- (1) hydrogen, and
- (2) alkyl of one to six carbons;
- R.sup.4 and R.sup.5 are independently selected from
- (1) hydrogen, and
- (2) NR.sup.12 R.sup.13, where R.sup.12 and R.sup.13 are independently selected from
- (a) hydrogen,
- (b) an amino-protecting group,
- (c) alkyl of one to six carbons, and
- (d) alkyl of one to six carbons substituted with 1, 2, or 3 substituents independently selected from
- (i) --OR.sup.10, where R.sup.10 is selected from
- (aa) hydrogen,
- (bb) alkyl of one to six carbons,
- (cc) a hydroxy-protecting group, and
- (dd) --C(O)R.sup.11 where R.sup.11 is selected from alkyl of one to six carbons, phenyl, and phenyl substituted with 1, 2, or 3 substituents independently selected from --NO.sub.2, alkyl of one to six carbons, and halogen;
- and
- (ii) phenyl, or
- R.sup.12 and R.sup.13 together with the nitrogen to which they are attached for a 4 to 8 membered ring selected from the group consisting of heterocycle;
- and
- R.sup.6, R.sup.7, and R.sup.8 are independently selected from
- (1) hydrogen,
- (2) halogen, and
- (3) --NO.sub.2.
A compound of Formula II ##STR9## or a pharmaceutically-acceptable salt or prodrug thereof, where R.sup.1 is hydrogen;
- L.sup.1 is a covalent bond;
- R.sup.2 and R.sup.3 are independently selected from
- (1) hydrogen, and
- (2) alkyl of one to six carbons;
- R.sup.4 and R.sup.5 are independently selected from
- (1) hydrogen, and
- (2) NR.sup.12 R .sup.3, where R.sup.12 and R.sup.13 are independently selected from
- (a) hydrogen,
- (b) an amino-protecting group,
- (c) alkyl of one to six carbons, and
- (d) alkyl of one to six carbons substituted with 1, 2, or 3 substituents independently selected from
- (i) --OR.sup.10, where R.sup.10 is selected from
- (aa) hydrogen,
- (bb) alkyl of one to six carbons,
- (cc) a hydroxy-protecting group, and
- (dd) --C(O)R.sup.11 where R.sup.11 is selected from alkyl of one to six carbons, phenyl, and phenyl substituted with 1, 2, or 3 substituents independently selected from --NO.sub.2, alkyl of one to six carbons, and halogen;
- and
- (ii) phenyl, or
- R.sup.12 and R.sup.13 together with the nitrogen to which they are attached for a 4 to 8 membered ring selected from the group consisting of heterocycle;
- and
- R.sup.6, R.sup.7, and R.sup.8 are independently selected from
- (1) hydrogen,
- (2) halogen, and
- (3) --NO.sub.2.
A method of treating inflammation and immune, autoimmune, and inflammatory diseases in a mammal comprising administering an effective amount of a compound of Formula I.
A method of treating adrenal imbalance in a mammal comprising administering an effective amount of a compound of Formula I.
A method of treating cognitive and behavioral processes comprising administering an effective amount of a compound of Formula I.
Dependencies are inferred from the claim text.