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1. WO2022109182 - POLYHETEROCYCLIC GLP-1 R MODULATING COMPOUNDS

Publication Number WO/2022/109182
Publication Date 27.05.2022
International Application No. PCT/US2021/059960
International Filing Date 18.11.2021
IPC
C07D 401/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
C07D 401/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 405/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14containing three or more hetero rings
A61K 31/4545 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
4545containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61P 1/16 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
CPC
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 9/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
C07D 401/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • GILEAD SCIENCES, INC. [US]/[US]
Inventors
  • 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
Agents
  • ROMEO, Russell J.
  • AMIRGHOLIZADEH, Tashica T.
  • BAJPAI, Reena
  • BOSS, Brandon
  • BRINKER, Achim
  • CHEN, Wenlan
  • CHOI, Lydia B.
  • DAMMANN, Yu-Ming
  • DOZZO, Paola
  • EDWARDS, Mary J.
  • GHOSH, Samantak
  • GINAH, Francis O.
  • GRESSLER, Donna
  • HARTRUM, J. Elin
  • HUTCHISON, Andrea
  • LAI, Shelley
  • LIU, Jiangqiong
  • MARQUART, Timothy A.
  • MUNTEAN, Lucia N.
  • NAKASHIMA, Richard A.
  • POLSTER, Philip B.
  • RICE, Katharine R.
  • SILVER, Joel
  • SIMPSON, Alexis N.
  • STUART, Tara C.
  • WAHLSTEN, Jennifer L.
  • YANG, Liuchun
Priority Data
63/116,63020.11.2020US
63/134,50506.01.2021US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) POLYHETEROCYCLIC GLP-1 R MODULATING COMPOUNDS
(FR) COMPOSÉS MODULATEURS DE GLP-1R POLYHÉTÉROCYCLIQUES
Abstract
(EN) The present disclosure provides glucagon-like peptide-1 receptor (GLP-1R) agonists of Formula (l-A), as well as pharmaceutical compositions and therapeutic uses thereof. The compounds are generally useful for treating a GLP-1R mediated disease or condition in a human such as non-alcoholic steatohepatitis (NASH), obesity or type 2 diabetes.
(FR) La présente invention concerne des agonistes du récepteur de peptide 1 de type glucagon (GLP-1R) de formule (l-A), ainsi que des compositions pharmaceutiques et leurs utilisations thérapeutiques. Les composés sont généralement utiles pour traiter une maladie ou un état à médiation par GLP-1R chez un être humain tel que la stéatohépatite non alcoolique (NASH), l'obésité ou le diabète de type 2.
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