Nova Patents
EP4403560A2

Macrocyclic compounds and uses thereof

Abstract

The present invention provides novel compounds (e.g., compounds of Formulae (I), (II), (III), (IV)) having tumor vascular remodeling effect and/or anti-CAF (Cancer Associated Fibroblasts) activity, or pharmaceutically acceptable salts thereof, optionally in a pharmaceutically acceptable carrier, and a medical uses thereof.

EP4403560A2, drawing sheet 1
Sheet 1 of 252

Term

Projected expiry 15 November 2038.

  1. Priority
  2. Filed
  3. Published
  4. Today
  5. Projected expiry

15 claims: 4 independent, 11 dependent

  1. 1
    A compound of Formula (II):or a pharmaceutically acceptable salt or stereoisomer thereof, wherein: R N1 and R N2 are independently hydrogen, optionally substituted alkyl, optionally substituted acyl, or a nitrogen protecting group, or wherein R N1 and R N2 are joined together with the intervening atoms to form optionally substituted heterocyclyl or optionally substituted heteroaryl;R P1 and R P2 are independently hydrogen, optionally substituted alkyl, optionally substituted acyl, or an oxygen protecting group;R X is hydrogen or -OR Xa ;R Y is hydrogen or -OR Ya ;R Xa and R Ya are independently hydrogen, optionally substituted alkyl, optionally substituted acyl, or an oxygen protecting group, or wherein R Xa and R Ya are joined together with the intervening atoms to form optionally substituted heterocyclyl;and m is 0 or 1.
  2. 5
    A compound of Formula (III):or a pharmaceutically acceptable salt or stereoisomer thereof, wherein: R O is hydrogen, optionally substituted alkyl, optionally substituted acyl, or an oxygen protecting group;R P1 is hydrogen, optionally substituted alkyl, optionally substituted acyl, or an oxygen protecting group;R X is hydrogen or -OR Xa ;R Y is hydrogen or -OR Ya ;R Xa and R Ya are independently hydrogen, optionally substituted alkyl, optionally substituted acyl, or an oxygen protecting group, or wherein R Xa and R Ya are joined together with the intervening atoms to form optionally substituted heterocyclyl;and n is 1 or 2, provided that the compound is not the following: or a pharmaceutically acceptable salt thereof.
  3. 9
    A compound of Formula ( IV ):or a pharmaceutically acceptable salt or stereoisomer thereof, wherein: R O is hydrogen, optionally substituted alkyl, optionally substituted acyl, or an oxygen protecting group;R P1 is hydrogen, optionally substituted alkyl, optionally substituted acyl, or an oxygen protecting group;R X is hydrogen or -OR Xa ;R Y is hydrogen or -OR Ya ;and R Xa and R Ya are independently hydrogen, optionally substituted alkyl, optionally substituted acyl, or an oxygen protecting group, or wherein R Xa and R Ya are joined together with the intervening atoms to form optionally substituted heterocyclyl.
  4. 12
    A pharmaceutical composition comprising a compound of any one of claims 1-11, or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically acceptable carrier.
Independent claims4