US 12,344,587 B2 · Synthetic retinoids for use in RAR activation

Abstract

The present invention relates to compounds of formula I: in which A1-A7 and R1 to R5 are defined herein, for use in the treatment of a condition or disease which is alleviated by the activation of retinoic acid receptors (RAR). The invention also relates to pharmaceutical compounds comprising such compounds, and related methods of treatment. In an aspect, the invention relates to a method of screening compounds for therapeutic potential in the treatment of a condition or disease which is alleviated by the activation of retinoic acid receptors (RAR). Aspects of the invention relate to novel compounds of formula I in which at least one of A1 to A3 is N or at least one of A4 is CR12 or A5 is CR13 in which R12/R13 is halogen.

Claims14

Dependent claims

A compound of formula I:

in which:
A1 is Nor CR6;
A2 is N or CR7;
A3 is N or CR8;
R6 and R8, are each independently hydrogen, C1-C10 alkyl, F, Br or Cl;
R9 is independently hydrogen, C1-C10 alkyl, F, Br, Cl or —OCR9 in which R9 is H or C3-C6 alkyl;
R1 to R4 are each independently C1-C10 alkyl, or R1 and R2 and/or R3 and R4 join to form a 3-membered ring;
A3 is N or CR12;
A5 is N or CR13;
A6 is N or CR14;
A7 is N or CR15;
each R13 to R15 is independently H, halogen or haloalkyl C1-C10, and
R5 is —C(═O)R16 or —C(═O)OR16 in which R16 is H or C1-10 alkyl;
with the proviso that at least one of A1 to A3 is N;
in free or in salt form.

12 more elements

Dependencies are inferred from the claim text.

Facts

Application

17/435,939Filed 11 Mar 2020

Priority

GB 190324211 Mar 2019

Published

US 2022/0144783 A112 May 2022

Granted

1 Jul 2025

Term ends

Not estimatedThe source records don’t support an estimate.

Classification25 codes

A61K 31/192
Carboxylic acids, e.g. valproic acid: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/203
Having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids: retinoic acids ; Salts thereof
A61K 31/47
Having six-membered rings with one nitrogen as the only ring hetero atom: quinolines; Isoquinolines
A61K 31/495
Having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins: having six-membered rings with two or more nitrogen atoms as the only ring…

Synthetic retinoids for use in RAR activation

Life of this patent

Synthetic retinoids for use in RAR activation

Life of this patent

Abstract

Claims14