Carbonate and carbamate modified forms of glucocorticoids in combination with B2 adrenergic agonists
AssigneeSepracor Inc.
InventorsMark G. Currie, Steve Jones, Paul Grover, Chris H. Senanayake, Q. Kevin Fang
Life of this patent
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Abstract
Compositions containing β2 adrenergic agonists in combination with carbonates and carbamates of the formula and in combination with related steroid carbonates and carbamates are disclosed. The compositions are useful for treating bronchospasm, for inducing bronchodilation and for treating rhinitis, asthma, and chronic obstructive pulmonary disease (COPD) and inflammatory diseases, particularly by inhalation.
Claims25
A composition comprising a β2 adrenergic agonist in combination with a compound of Formula I:
- wherein
- R1 and R2, independently for each occurrence, represent lower alkyl or lower acyl, or taken together R1 and R2 form a substituted or unsubstituted ketal;
- R3 is —OR4 or —NR5R6;
- R4 is chosen from C7 to C24 hydrocarbon, —(C7 to C24 hydrocarbon)-COOH and —(C7 to C24 hydrocarbon)-NR9R10;
- R5 is hydrogen or C7 to C24 hydrocarbon;
- R6 is chosen from C7 to C24 hydrocarbon and —(C7 to C24 hydrocarbon)-COOH;
- R9 is hydrogen or C1 to C17 hydrocarbon;
- R10 is hydrogen or C1 to C17 hydrocarbon;
- R11 is OR2;
- and
- X and Y are independently hydrogen or halogen.
A composition comprising a β2 adrenergic agonist in combination with a compound of formula:
- wherein
- R4 chosen from C7 to C24 hydrocarbon, —(C7 to C24 hydrocarbon)-COOH and —(C7 to C24 hydrocarbon)-NR9R10;
- R9 hydrogen or C1 to C17 hydrocarbon;
- and
- R10 is hydrogen or C1 to C17 hydrocarbon.
A composition comprising a β2 adrenergic agonist in combination with a compound of formula:
- wherein
- R5 is hydrogen or C7 to C24 hydrocarbon;
- R6 is chosen from C7 to C24 hydrocarbon and —(C7 to C24 hydrocarbon)-COOH.
A method for treating bronchospasm comprising administering a β2 adrenergic agonist and a compound of Formula I:
- wherein
- R1 and R2, independently for each occurrence, represent lower alkyl or lower acyl, or taken together R1 and R2 form a substituted or unsubstituted ketal;
- R3 is —OR4 or NR5R6;
- R4 is chosen from C7 to C24 hydrocarbon, —(C7 to C24 hydrocarbon)-COOH and —(C7 to C24 hydrocarbon) -NR9R10;
- R5 is hydrogen or C7 to C24 hydrocarbon;
- R6 is chosen from C7 to C24 hydrocarbon and —(C7 to C24 hydrocarbon)-COOH;
- R9 hydrogen or C1 to C17 hydrocarbon;
- R10 is hydrogen or C1 to C17 hydrocarbon;
- R11 is —OR2;
- and
- X and Y are independently hydrogen or halogen.
A method for inducing bronchodilation comprising administering a β2 adrenergic agonist and a compound of Formula I:
- wherein
- R1 and R2, independently for each occurrence, represent lower alkyl or lower acyl, or taken together R1 and R2 form a substituted or unsubstituted ketal;
- R3 is —OR or —NR5R6;
- R4 chosen from C7 to C24 hydrocarbon, —(C7 to C24 hydrocarbon)-COOH and —(C7 to C24 hydrocarbon)-NR9R10;
- R5 hydrogen or C7 to C24 hydrocarbon;
- R6 is chosen from C7 to C24 hydrocarbon and —(C7 to C24 hydrocarbon)-COOH;
- R9 is hydrogen or C1 to C17 hydrocarbon;
- R10 is hydrogen or C1 to C17 hydrocarbon;
- R11 is —OR2;
- and
- X and Y are independently hydrogen or halogen.
A method for treating inflammatory conditions comprising administering a β2 adrenergic agonist and a compound of Formula I:
- wherein
- R1 and R2, independently for each occurrence, represent lower alkyl or lower acyl, or taken together R1 and R2 form a substituted or unsubstituted ketal;
- R3 is —OR4 or —NR5R6;
- R4 is chosen from C7 to C24 hydrocarbon, —(C7 to C24 hydrocarbon)-COOH and —(C7 to C24 hydrocarbon)-NR9R10;
- R5 hydrogen or C7 to C24 hydrocarbon;
- R6 is chosen from C7 to C24 hydrocarbon and —(C7 to C24 hydrocarbon)-COOH;
- R9 hydrogen or C1 to C17 hydrocarbon;
- R10 is hydrogen or C1 to C17 hydrocarbon;
- R11 is —OR2;
- and
- X and Y are independently hydrogen or halogen.
Dependencies are inferred from the claim text.