IP Library Granted Patent US 11,819,505
Granted Patent B2
US 11,819,505 · App. 17/866,942 · Granted Nov 21, 2023

Heterocyclylamines as PI3K inhibitors

Inventors: Yun-Long Li (Chadds Ford, PA); Andrew P. Combs (Kennett Square, PA); Eddy W. Yue (Landenberg, PA); Brent Douty (Fallowfield, PA); Song Mei (Wilmington, DE)
Assignees: Incyte Corporation; Incyte Holdings Corporation
A61K31/519A61P29/00C07D471/04C07D487/04C07D519/00
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Quick Facts
Patent No.
US 11,819,505
App. No.
17/866,942
Granted
Nov 21, 2023
Kind
B2
Abstract

The present invention provides heterocyclylamine derivatives of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.

Claims (6)

1. A method of inhibiting or ameliorating eczema in a patient, comprising administering to the patient a compound which is 4-{3-[1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-fluorophenyl}pyrrolidin-2-one, or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the compound is 4-{3-[1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-fluorophenyl}pyrrolidin-2-one.

3. The method of claim 1 , wherein the compound is (S)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one.

4. The method of claim 1 , wherein the compound is (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one.

5. The method of claim 1 , wherein the compound is (S)-4-(3-((R)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one.

6. The method of claim 1 , wherein the compound is (R)-4-(3-((R)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 28, 2022
From: LI, YUN-LONG; YAO, WENQING; COMBS, ANDREW P.; YUE, EDDY W.; MEI, SONG; ZHU, WENYU; GLENN, JOSEPH; MADUSKUIE, THOMAS P.; SPARKS, RICHARD B.; DOUTY, BRENT; HE, CHUNHONG
To: INCYTE CORPORATION
Reel/Frame 060653/0442 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 28, 2022
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 060653/0568 →
Continuity (10)
Continuation 16828315 · Mar 24, 2020
Continuation 16446098 · Jun 19, 2019
Continuation 16112160 · Aug 24, 2018
Continuation 15673529 · Aug 10, 2017
Continuation 14872881 · Oct 1, 2015
Continuation 13601349 · Aug 31, 2012
Provisional Application 61677445 · Jul 30, 2012
Provisional Application 61594882 · Feb 3, 2012
Provisional Application 61530866 · Sep 2, 2011
Related Publication 20230121440A1 · Apr 20, 2023
Cited By (1)
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