IP Library Granted Patent US 11,702,424
Granted Patent B2
US 11,702,424 · App. 16/996,117 · Granted Jul 18, 2023

Bicyclic-fused heteroaryl or aryl compounds

Inventors: John David Trzupek (Arlington, MA); Katherine Lin Lee (West Newton, MA); Mark Edward Bunnage (Concord, MA); Seungil Han (Mystic, CT); David Hepworth (Concord, MA); Frank Eldridge Lovering (Acton, MA); John Paul Mathias (Concord, MA); Nikolaos Papaioannou (Newton, MA); Betsy Susan Pierce (East Lyme, CT); Joseph Walter Strohbach (Wentzville, MO); Stephen Wayne Wright (Old Lyme, CT); Christoph Wolfgang Zapf (Marlborough, MA); Lori Krim Gavrin (Villanova, PA); Arthur Lee (San Carlos, CA); David Randolph Anderson (Salem, CT); Kevin Joseph Curran (Somerset, NJ); Christoph Martin Dehnhardt (Burnaby, CA); Eddine Saiah (Brookline, MA); Joel Adam Goldberg (New Orleans, LA); Xiaolun Wang (San Diego, CA); Horng-Chih Huang (Chesterfield, MO); Richard Vargas (Bedford, MA); Michael Dennis Lowe (White Plains, NY); Akshay Patny (Waltham, MA)
Assignee: Pfizer Inc.
C07D491/056A61K31/40A61K31/4015A61K31/47A61K31/4709A61K31/4725A61K31/517A61K31/5377A61K31/541A61K45/06C07C69/94C07D207/08C07D207/26C07D207/267C07D207/273C07D209/52C07D215/48C07D217/02C07D217/22C07D217/24C07D239/86C07D239/88C07D263/24C07D401/12C07D401/14C07D403/12C07D405/12C07D405/14C07D407/14C07D413/12C07D417/12C07D487/04C07D498/04C07F7/1804
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Quick Facts
Patent No.
US 11,702,424
App. No.
16/996,117
Granted
Jul 18, 2023
Kind
B2
Abstract

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Claims (8)

1. A pharmaceutical combination comprising 1-(((2S,3S,4S)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-yl)methoxy)-7-methoxyisoquinoline-6-carboxamide, or a pharmaceutically acceptable salt thereof, and a JAK1 inhibitor, or a pharmaceutically acceptable salt thereof.

2. A method for treating rheumatoid arthritis in a human comprising administering to the human the pharmaceutical combination according to claim 1 .

3. A pharmaceutical combination comprising 1-(((2S,3S,4S)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-yl)methoxy)-7-methoxyisoquinoline-6-carboxamide, or a pharmaceutically acceptable salt thereof, a JAK1 inhibitor, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, vehicle, or diluent.

4. A method for treating rheumatoid arthritis in a human comprising administering to the human in need of rheumatoid arthritis treatment a therapeutically effective amount of the pharmaceutical combination according to claim 3 .

5. A pharmaceutical combination comprising 1-(((2S,3S,4S)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-yl)methoxy)-7-methoxyisoquinoline-6-carboxamide, or a pharmaceutically acceptable salt thereof, and N-{cis-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}-propane-1-sulfonamide, or a pharmaceutically acceptable salt thereof.

6. A method for treating rheumatoid arthritis in a human comprising administering to the human the pharmaceutical combination according to claim 5 .

7. A pharmaceutical combination comprising 1-(((2S,3S,4S)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-yl)methoxy)-7-methoxyisoquinoline-6-carboxamide, or a pharmaceutically acceptable salt thereof, N-{cis-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}-propane-1-sulfonamide, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier, vehicle, or diluent, or a combination thereof.

8. A method for treating rheumatoid arthritis in a human comprising administering to the human the pharmaceutical combination according to claim 7 .

Assignments (1)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: PFIZER INC.
To: PFIZER INC.
Reel/Frame 063119/0087 →
Continuity (6)
Continuation 16411679 · May 14, 2019
Continuation 15862691 · Jan 5, 2018
Continuation 15232892 · Aug 10, 2016
Continuation 14678114 · Apr 3, 2015
Provisional Application 61975473 · Apr 4, 2014
Related Publication 20200377511A1 · Dec 3, 2020
Cited By (1)
US 12,202,836