Back to results
US 2012/0238531 A1Published application
Isoxazolidine derivatives
AssigneeChiesi Farmaceutici S.p.A.
InventorsEleonora GHIDINI, Anna Maria Capelli
Life of this patent
Estimating the term…
Abstract
Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.
Claims20
A compound of formula (I):
- wherein
- R1 is (CH2)n—Z—(CH2)n′—R4
- n is 0, 1 or 2;
- n′ is 0, 1 or 2;
- Z is a single bond or is selected from the group consisting of —S—, —O—, —C(O)—, and —NR3;
- R3 is selected from the group consisting of H, (C1-C6)alkyl, (C1-C6)haloalkyl, (C3-C8)cycloalkyl, aryl, aryl(C1-C6)alkyl, and heteroaryl, which are optionally substituted by —CN;
- R4 is selected from the group consisting of:
- H, halogen, —OH, —SH, —CN, and —NR6R7;
- aryl(C1-C6)alkyl, (C1-C6)alkylsulfonyl, (C1-C6)alkylcarbonyl, (C1-C6)alkylcarboxyl, HO(C1-C6)alkylcarboxyl, (C1-C6)alkylamide, and (C1-C6)alkoxy, which are optionally substituted by one or more oxo groups;
- (C1-C6)alkyl which may be optionally substituted by one or more substituents selected from the group consisting of a halogen atom, —CN, —OH, —NH2, —NO2, —CF3, and —SH;
- (C2-C6)alkynyl;
- (C5-C17)alkenylcarbonyl;
- and
- a mono-, bi-, or tricyclic saturated or partially unsaturated or unsaturated ring, optionally substituted by one or more halogen atoms or oxo groups;
- R6 and R7 are independently selected from the group consisting of H, (C1-C6)alkyl, and (C1-C6)alkoxy;
- X and Y are independently H or halogen atoms;
- R2 is selected from the group consisting of:
- —(CH2)s—K-A-(CH2)t—W, —(CH2)s—K—(CH2)t—B—W, and —(CH2)s—(CHR5)—W;
- s is 0 or 1;
- t is 0 or 1;
- K is selected from the group consisting of a group —CH═CH—, arylene, and heteroarylene, where such arylene and heteroarylene groups may be optionally substituted by one or more groups independently selected from:
- halogen, (C1-C6)alkyl, —OH, (C1-C6)alkoxy, and (C1-C6)haloalkyl;
- A is selected from the group consisting of a bond, —O—, and —S—;
- B is selected from the group consisting of a bond, —O—, and —S—;
- W is aryl or heteroaryl, where such aryl and heteroaryl groups may be optionally substituted by one or more groups independently selected from:
- halogen, —OH, (C1-C6)alkyl, (C1-C6)alkoxy, and (C1-C6)haloalkyl;
- R5 is aryl or heteroaryl, where such aryl and heteroaryl groups may be optionally substituted by one or more groups independently selected from halogen, (C1-C6)alkyl, (C1-C6)alkoxy, —OH, and (C1-C6)haloalkyl;
- or a pharmaceutically acceptable salt thereof;
- with the proviso that when s is 1, K is optionally substituted heteroarylene, t is zero, and A or B is a bond, then W is optionally substituted heteroaryl.
26 more elements
Dependencies are inferred from the claim text.