US 12,247,028 B2
Azabicyclo and diazepine derivatives
David Ellis, Durham, NC (US); and Howard Allen Ketelson, Dallas, TX (US)
Assigned to Alcon Inc., Fribourg (CH)
Filed by Alcon Inc., Fribourg (CH)
Filed on Nov. 30, 2023, as Appl. No. 18/524,807.
Application 18/524,807 is a division of application No. 17/699,606, filed on Mar. 21, 2022, granted, now 11,884,666.
Application 17/699,606 is a division of application No. 16/760,192, granted, now 11,306,090, issued on Apr. 19, 2022, previously published as PCT/IB2018/058631, filed on Nov. 2, 2018.
Claims priority of provisional application 62/749,610, filed on Oct. 23, 2018.
Claims priority of provisional application 62/581,073, filed on Nov. 3, 2017.
Prior Publication US 2024/0132497 A1, Apr. 25, 2024
Int. Cl. A61P 27/10 (2006.01); A61K 9/00 (2006.01); C07D 243/38 (2006.01); C07D 471/04 (2006.01); C07D 471/08 (2006.01)
CPC C07D 471/08 (2013.01) [A61K 9/0048 (2013.01); A61P 27/10 (2018.01); C07D 243/38 (2013.01); C07D 471/04 (2013.01)] 16 Claims
OG exemplary drawing
 
1. An ophthalmic pharmaceutical composition for treating a mammalian subject having or at risk of having an ocular disorder associated with modulation of a muscarinic receptor, which is ophthalmically compatible and comprises:
(1) a compound and/or a pharmaceutically acceptable salt, wherein the compound is represented by formula (I)

OG Complex Work Unit Chemistry
wherein
Me=CH3;
A=O;
X=-OH;
R1 and R2 are independently a phenyl or benzyl group being optionally substituted with one or more substituents selected from C1-C20 straight, branched or cyclo alkyl groups, halo alkyl groups, hydroxyl, alkoxy, nitrile, nitro, amino, amide, ester, sulfone, sulfoxide, sulfonamide, and halogen atoms;
R3 and R4 are independently hydrogen, C1-C10 straight or branched or cyclo alkyl or halo alkyl groups; and
(2) one or more pharmaceutically acceptable carriers.