Certain n-(1-cyan0-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating chronic rhinosinusitis
OwnerAriel TEPER, Carlos FERNANDEZ +1inventors
InventorsAriel TEPER, Carlos FERNANDEZ, David CIPOLLA
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Abstract
The present disclosure relates to methods for treating chronic rhinosinusitis with a composition comprising an effective amount of a N-(1-cyano-2-phenylethyl)-1,4-oxazepane-2-carboxamide DPP1 inhibitor compound of Formula (I) or a pharmaceutically acceptable salt thereof. In one embodiment, the compound of Formula (I) is (2S)-N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihyd ro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide (brensocatib).
Claims212
A method of inhibiting dipeptidyl peptidase (DPP1) in a subject having chronic rhinosinusitis (CRS) or at risk of developing CRS, comprising,
- administering to the subject for an administration period, a pharmaceutical composition comprising an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt thereof,
- wherein,
- R1 is
- R2 is hydrogen, F, Cl, Br, OSO2C1-3alkyl, or C1-3alkyl;
- R3 is hydrogen, F, Cl, Br, CN, CF3, SO2C1-3alkyl, CONH2 or SO2NR4R5,
- wherein R4 and R5 together with the nitrogen atom to which they are attached form an azetidine, pyrrolidine or piperidine ring;
- or
- X is O, S or CF2;
- Y is O or S;
- Q is CH or N;
- R6 is C1-3alkyl, wherein said C1-3alkyl is optionally substituted by 1, 2 or 3 F and optionally by one substituent selected from the group consisting of OH, OC1-3alkyl, N(C1-3alkyl)2, cyclopropyl, and tetrahydropyran;
- and
- R7 is hydrogen, F, Cl or CH3,
- thereby inhibiting DPP1 in the subject.
A method of treating chronic rhinosinusitis (CRS) in a subject in need thereof, comprising,
- administering to the subject for an administration period, a pharmaceutical composition comprising an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt thereof,
- wherein,
- R1 is
- R2 is hydrogen, F, Cl, Br, OSO2C1-3alkyl, or C1-3alkyl;
- R3 is hydrogen, F, Cl, Br, CN, CF3, SO2C1-3alkyl, CONH2 or SO2NR4R5,
- wherein R4 and R5 together with the nitrogen atom to which they are attached form an azetidine, pyrrolidine or piperidine ring;
- or
- X is O, S or CF2;
- Y is O or S;
- Q is CH or N;
- R6 is C1-3alkyl, wherein said C1-3alkyl is optionally substituted by 1, 2 or 3 F and optionally by one substituent selected from the group consisting of OH, OC1-3alkyl, N(C1-3alkyl)2, cyclopropyl, and tetrahydropyran;
- and
- R7 is hydrogen, F, Cl or CH3,
- thereby treating chronic rhinosinusitis in the subject.
Dependencies are inferred from the claim text.