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US 2012/0234316 A1Published application
Isoxazolidine derivatives
AssigneeChiesi Farmaceutici S.p.A.
InventorsEleonora GHIDINI, Andrea Rizzi
Life of this patent
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Abstract
Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, according to formula (I) according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.
Claims18
A compound of formula (I):
- wherein
- R1 is —(CH2)n—Z—(CH2)n′—R2, —R3 wherein n and n′ are each independently 0, 1 or 2;
- Z is a single bond or is selected from —S—, —O— and —OC(R4R5)—;
- R3 is selected from the group consisting of:
- H, halogen, —CN, —OH, —CONH2, (C1-C6)alkyl, (C2-C4)alkenyl, (C1-C6)haloalkyl, (C2-C4)alkynyl, (C1-C6)alkylsulfonyl, and (C1-C6)alkylcarbonyl;
- —NR4R5, wherein R4 and R5 are independently selected from the group consisting of (C1-C6)alkyl and (C1-C6)alkoxy;
- (C3-C8)cycloalkyl, (C3-C8)heterocycloalkyl, ary,1 and heteroaryl, each of which is optionally substituted by one or more halogen atoms or oxo groups or —CN groups;
- and
- R2 is selected from the group consisting of:
- linear or branched (C1-C8)alkyl, (C1-C6)alkoxy, and (C1-C6)haloalkyl, optionally substituted by one or more CN groups or halogen atoms;
- —(CH2)mR6, wherein R6 is selected from the group consisting of (C3-C8)cycloalkyl, (C3-C8)heterocycloalkyl, aryl, (C1-C6)arylalkyl, aryloxy, arylthio, and heteroaryl, each of which optionally substituted by one or more substituents selected from the group consisting of oxo, —OH, halogen, —CN, —NH2, —CONH2, —NO2, —NHC(O)H, linear or branched (C1-C6)alkyl, linear or branched (C1-C6)haloalkyl, linear or branched (C1-C6)alkoxy, linear or branched (C1-C6)haloalkoxy, (C1-C6)hydroxyalkoxy, (C1-C6)haloalkoxy, (C1-C6)alkoxycarbonyl, (C1-C6)alkylcarboxyl, (C1-C6)alkylsulfonyl and (C1-C6)alkylsulfanyl, (C1-C6)alkyloxysulfonyl, (C1-C6)haloalkylsulfonyloxy, aminosulfonyl, (C3-C8)cycloalkyl, (C3-C6)heterocycloalkyl, and heteroaryl, wherein m is 0 or an integer from 1 to 3;
- and
- X and Y are independently H or halogen,
- or a pharmaceutically acceptable salt thereof,
- with the proviso that when R1 is a group —CH2OH and R2 is (C1-C6)alkyl or (C3-C8)cycloalkyl, then X and Y are fluorine atoms;
- or pharmaceutically acceptable salts thereof.
13 more elements
Dependencies are inferred from the claim text.