IP Library › Granted Patent US 11,851,419
Granted Patent B2
US 11,851,419 · App. 17/530,300 · Granted Dec 26, 2023

GLP-1R modulating compounds

Inventors: Gediminas J. Brizgys (San Carlos, CA); James S. Cassidy (San Francisco, CA); Chienhung Chou (Dublin, CA); Jeromy J. Cottell (Redwood City, CA); Chao-I Hung (San Mateo, CA); Kavoos Kolahdouzan (San Francisco, CA); James G. Taylor (Burlingame, CA); Nathan E. Wright (San Diego, CA); Zheng-Yu Yang (Palo Alto, CA)
Assignee: Gilead Sciences, Inc.
C07D401/14A61K45/06C07D405/14
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Quick Facts
Patent No.
US 11,851,419
App. No.
17/530,300
Granted
Dec 26, 2023
Kind
B2
Abstract

The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition in a human.

Claims (4)

1. A compound, or a pharmaceutically acceptable salt thereof, wherein the compound has the structure:

2. A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient.

3. The pharmaceutical composition of claim 2 further comprising one or more additional therapeutic agents.

4. The pharmaceutical composition of claim 3 , wherein the additional therapeutic agent comprises an anti-obesity agent selected from peptide YY , a neuropeptide Y receptor type 2 (NPYR2) agonist, a N PYR 1 agonist, an NPYR5 antagonist, a cannabinoid receptor type 1 (CB1 R) antagonist, a lipase inhibitor, a human proislet peptide (HIP), a melanocortin receptor 4 agonist (MC4R), a melanin concentrating hormone receptor 1 antagonist, a farnesoid X receptor (FXR) agonist, an apoptotic signal-regulating kinase (ASK-1) inhibitor, zonisamide, phentermine (alone or in combination with topiramate), a norepinephrine/dopa mine reuptake inhibitor, an opioid receptor antagonist, a combination of a norepinephrine/dopa mine reuptake inhibitor and an opioid receptor antagonist, sibutramine, a cholecystokinin agonist, amylin, leptin , a serotonergic agent, a methionine aminopeptidase 2 (MetAP2) inhibitor, phendimetrazine, diethylpropion, benzphetamine, an SGLT2 inhibitor , an SGLTL1 inhibitor, a dual SGLT2/SGLT1 inhibitor, a fibroblast growth factor receptor (FGFR) modulator, an AMP-activated protein kinase (AMPK) activator, biotin, a MAS receptor modulator, a glucagon receptor agonist (alone or in combination with another GLP-1R agonist , a peroxisome proliferator-activated receptor alpha (PPARα) agonist, fish oil, an acetyl-coA carboxylase (ACC) inhibitor, a TGFβ antagonist, GFRAL agonist, and/or a pharmaceutically acceptable salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 22, 2021
From: BRIZGYS, GEDIMINAS J.; CASSIDY, JAMES S.; CHOU, CHIENHUNG; COTTELL, JEROMY J.; HUNG, CHAO-I; KOLAHDOUZAN, KAVOOS; TAYLOR, JAMES G.; WRIGHT, NATHAN E.; YANG, ZHENG-YU
To: GILEAD SCIENCES, INC.
Reel/Frame 058181/0044 →
Continuity (3)
Provisional Application 63134505 · Jan 6, 2021
Provisional Application 63116630 · Nov 20, 2020
Related Publication 20220177449A1 · Jun 9, 2022
Cited By (3)
US 12,473,271 US 12,497,382 US 12,570,642