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1. WO2018005812 - DIPROVOCIMS: A NEW AND POTENT CLASS OF TLR AGONISTS

Publication Number WO/2018/005812
Publication Date 04.01.2018
International Application No. PCT/US2017/040028
International Filing Date 29.06.2017
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
4025
not condensed and containing further heterocyclic rings, e.g. cromakalim
C07D 403/10 (2006.01)
A61K 31/40 (2006.01)
A61K 31/4025 (2006.01)
CPC
A61K 31/40
A61K 31/4025
C07D 207/16
C07D 403/10
Applicants
  • THE SCRIPPS RESEARCH INSTITUTE [US/US]; 10550 North Torrey Pines Road La Jolla, CA 92037, US
  • THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM [US/US]; 201 West 7th Street Austin, TX 78701, US
  • BEUTLER, Bruce [US/US]; US (US)
  • BOGER, Dale, L. [US/US]; US (US)
Inventors
  • BEUTLER, Bruce; US
  • BOGER, Dale, L.; US
Agents
  • GAMSON, Edward, P.; US
  • RHEINTGEN, Kathleen, A.; US
  • SCHEER, James, A.; US
  • SHEKLETON, Gerald, T.; US
Priority Data
62/356,31429.06.2016US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) DIPROVOCIMS: A NEW AND POTENT CLASS OF TLR AGONISTS
(FR) DIPROVOCIMS: UNE NOUVELLE CLASSE PUISSANTE D'AGONISTES TLR
Abstract
(EN)
A diprovocim compound that corresponds in structure to structural Formula V is disclosed, wherein A, W, Z, R1, R2, R3 and R4 (when present) are defined within. A diprovocim compound has immune-adjuvant properties on human and mouse cells in culture and on in vivo immunization of mice. A composition containing a diprovocim and a method of using a compound are also disclosed. The immunostimulatory activity of a diprovocim compound is similar to that of LPS, to which there is no apparent structural similarity. A contemplated compound bears no structural similarity to either the TLR1/TLR2 lipoprotein agonists nor to any other synthetic TLR agonist, and is remarkably easy to prepare and synthetically modify.
(FR)
L'invention concerne un composé de diprovocim qui correspond en structure à la formule structurale V, dans laquelle A, W, Z, R 1 , R 2 , R 3 et R 4 (quand ils existent) sont définis à l'intérieur. Un composé de diprovocim possède des propriétés immuno-adjuvantes sur des cellules humaines et des cellules de souris en culture et sur l'immunisation in vivo de souris. L'invention porte également sur une composition contenant du diprovocim et sur un procédé d'utilisation d'un composé. L'activité immunostimulante d'un composé de diprovocim est similaire à celle du LPS, à laquelle il n'y a pas de similarité structurale apparente. Un composé selon l'invention ne présente aucune similarité structurale avec les agonistes des lipoprotéines TLR1/TLR2, ni sur tout autre agoniste synthétique de TLR, et est remarquablement facile à préparer et à modifier de manière synthétique.
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