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US 7,622,467 B2Granted
Aryl aniline derivatives as β2 adrenergic receptor agonists
AssigneeTheravance, Inc.
InventorsRobert M. McKinnell, John R. Jacobsen, Sean G. Trapp, Daisuke R. Saito
Life of this patent
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Abstract
The invention provides novel β2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
Claims16
A compound of formula (I):
- wherein:
- R1 and R2 taken together are selected from —NHC(═O)CH═CH—, —CH═CHC(═O)NH—, —NHC(═O)S—, and —SC(═O)NH—;
- R3 is hydroxy and R4 is hydrogen;
- one of R5 and R6 is —[X—C1-6alkylenyl]n—NR10R11 or C1-6alkylenyl-NR12R13,
- and the other of R5 and R6 is selected from hydrogen, hydroxy, C1-4alkoxy, and C1-4alkyl,
- wherein C1-4alkyl is optionally substituted with halo,
- wherein
- each X is independently selected from —O—, —NH—, —S—, —NHSO2—, —SO2NH—, —NHC(═O)—, and —C(═O)NH—;
- each of R10 , R11, R12, and R13 is independently hydrogen or C1-4alkyl;
- or
- R10 and R11, together with the nitrogen atom to which they are attached, or R10, together with the nitrogen atom to which it is attached and a carbon atom of the adjacent C1-6alkylenyl, or R12 and R13, together with the nitrogen atom to which they are attached, or R12, together with the nitrogen atom to which it is attached and a carbon atom of the adjacent C1-6alkylenyl, form a heterocyclic or heteroaryl ring having from 5 to 7 ring atoms, and optionally containing an additional heteroatom selected from oxygen, nitrogen, and sulfur, wherein nitrogen is optionally substituted with —S(O)2—C1-4alkyl;
- and
- n is 1,2, or 3;
- and
- each of R7, R8, and R9 is independently hydrogen or C1-6alkyl;
- or a pharmaceutically-acceptable salt or solvate or stereoisomer thereof.
13 more elements
Dependencies are inferred from the claim text.