IP Library Granted Patent US 10,793,579
Granted Patent B2
US 10,793,579 · App. 16/411,679 · Granted Oct 6, 2020

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 10,793,579
App. No.
16/411,679
Granted
Oct 6, 2020
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 tofacitinib, or a pharmaceutically acceptable salt thereof.

2. 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, tofacitinib, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier, vehicle, or diluent, or a combination thereof.

3. A method of treating rheumatoid arthritis in a human comprising administering to the human in need of rheumatoid arthritis treatment a therapeutically effective amount of a pharmaceutical combination according to claim 1 .

4. A method of treating rheumatoid arthritis in a human comprising administering to the human in need of rheumatoid arthritis treatment a therapeutically effective amount of a pharmaceutical combination according to claim 2 .

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 a JAK3 inhibitor, or a pharmaceutically acceptable salt thereof.

6. 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 JAK3 inhibitor, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier, vehicle, or diluent, or a combination thereof.

7. A method of 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 5 .

8. A method of 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 6 .

Assignments (1)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: PFIZER INC.
To: PFIZER INC.
Reel/Frame 063119/0087 →