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1. WO2020118139 - A1 ADENOSINE RECEPTOR AGONISTS AND METHODS OF USE THEREOF

Publication Number WO/2020/118139
Publication Date 11.06.2020
International Application No. PCT/US2019/064844
International Filing Date 06.12.2019
IPC
C07D 249/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
249Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
10with 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
C07D 471/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 473/34 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
26with an oxygen, sulfur, or nitrogen atom directly attached in position 2 or 6, but not in both
32Nitrogen atom
34attached in position 6, e.g. adenine
C07H 19/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen as ring hetero atom
C07H 19/16 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen as ring hetero atom
16Purine radicals
A61P 43/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
CPC
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07D 249/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
249Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
10with 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
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 473/34
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
26with an oxygen, sulfur or nitrogen atom directly attached in position 2 or 6, but not in both
32Nitrogen atom
34attached in position 6, e.g. adenine
C07H 19/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides ; Anhydro-derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
C07H 19/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides ; Anhydro-derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
16Purine radicals
Applicants
  • THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES [US]/[US]
Inventors
  • JACOBSON, Kenneth A.
  • TOSH, Dilip K.
  • REITMAN, Marc L.
  • GAVRILOVA, Oksana
Agents
  • KOSZYK, Francis J.
  • PILLAI, Xavier
Priority Data
62/776,52807.12.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) A1 ADENOSINE RECEPTOR AGONISTS AND METHODS OF USE THEREOF
(FR) AGONISTES DU RÉCEPTEUR DE L'ADÉNOSINE A1 ET LEURS MÉTHODES D'UTILISATION
Abstract
(EN)
Disclosed are compounds of the formulas (I), (II), and (II): which are A1 adenosine receptor agonists, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein Y, R1‑R6, R10‑R15, and R20‑R22 are as defined in the specification. These compounds are selective to the A1 adenosine receptor, and are contemplated for use in the treatment or prevention of a number of diseases or conditions, for example, for inducing and/or maintaining a hypothermic and/or hypometabolic state for treatment of a mammal.
(FR)
La présente invention concerne des composés de formules (I) et (II) qui sont des agonistes du récepteur de l'adénosine A1 , des compositions pharmaceutiques comprenant ces composés, et un procédé d'utilisation de ces composés, Y, R1‑R6, R10‑R15, et R20‑R22 étant tels que définis dans la description. Ces composés sont sélectifs vis-à-vis du récepteur de l'adénosine A1, et il est envisagé de les utiliser dans le traitement ou la prévention d'un certain nombre de maladies ou d'états, par exemple, pour induire et/ou maintenir un état hypothermique et/ou hypométabolique pour le traitement d'un mammifère.
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