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1. WO2020118206 - BUTENOLIDE ANTAGONISTS OF THE CGAS/STING PATHWAY

Publication Number WO/2020/118206
Publication Date 11.06.2020
International Application No. PCT/US2019/064990
International Filing Date 06.12.2019
IPC
C07D 307/58 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02not condensed with other rings
34having two or three double bonds between ring members or between ring members and non-ring members
56with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
58One oxygen atom, e.g. butenolide
C07D 307/60 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02not condensed with other rings
34having two or three double bonds between ring members or between ring members and non-ring members
56with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
60Two oxygen atoms, e.g. succinic anhydride
C07D 307/83 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
77ortho- or peri-condensed with carbocyclic rings or ring systems
78Benzo furans; Hydrogenated benzo furans
82with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
83Oxygen atoms
C07D 307/88 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
77ortho- or peri-condensed with carbocyclic rings or ring systems
87Benzo furans; Hydrogenated benzo furans
88with one oxygen atom directly attached in position 1 or 3
A61P 37/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
A61K 31/341 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
34having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
341not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
CPC
A61P 37/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
C07D 307/58
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02not condensed with other rings
34having two or three double bonds between ring members or between ring members and non-ring members
56with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
58One oxygen atom, e.g. butenolide
C07D 307/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02not condensed with other rings
34having two or three double bonds between ring members or between ring members and non-ring members
56with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
60Two oxygen atoms, e.g. succinic anhydride
C07D 307/83
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
77ortho- or peri-condensed with carbocyclic rings or ring systems
78Benzo [b] furans; Hydrogenated benzo [b] furans
82with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
83Oxygen atoms
C07D 307/88
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
77ortho- or peri-condensed with carbocyclic rings or ring systems
87Benzo [c] furans; Hydrogenated benzo [c] furans
88with one oxygen atom directly attached in position 1 or 3
Applicants
  • THE SCRIPPS RESEARCH INSTITUTE [US]/[US]
Inventors
  • LAIRSON, Luke L.
  • CHIN, Emily
  • SHENVI, Ryan
  • HUFFMAN, Benjamin
  • SCHWARZ, Jonas Luca
Agents
  • PERDOK, Monique M.
  • SCHEER, Bradley W.
  • ARORA, Suneel
  • BEEKMAN, Marvin L.
  • BIANCHI, Timothy E.
  • BLACK, David W.
  • LANG, Allen R.
Priority Data
62/776,30606.12.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) BUTENOLIDE ANTAGONISTS OF THE CGAS/STING PATHWAY
(FR) ANTAGONISTES DU BUTÉNOLIDE DE LA VOIE CGAS/STING
Abstract
(EN)
A series of butenolide heterodimers were found to be inhibitors of the cGAS/STING pathway. They can be useful in therapies for treating a range of chronic interferon (IFN) associated autoimmune diseases and inflammation.
(FR)
La présente invention concerne une série d'hétérodimères de buténolide qui s'est avérée être des inhibiteurs de la voie cGAS/STING. Lesdits hétérodimères de buténolide peuvent être utiles dans des thérapies pour traiter une gamme de maladies auto-immunes associées à l'interféron chronique (IFN) et une inflammation.
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