US 9,040,540 B2 · 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use

Abstract

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionizing radiation.

Claims39

Dependent claims

A compound of the following formula, or a pharmaceutically acceptable salt thereof:

wherein:
—RB3 is independently:
each —RB3A is independently —H or saturated aliphatic C1-3alkyl;
—RA4 is independently —NHRA4A, —NRA4A2, or —ORA4A;
each —RA4A is independently saturated aliphatic C1-3alkyl;
—RA5 is independently —RA5A, —RA5B, —RA5C, —RA5D, —RA5E, or —RA5F;
—RA5A is independently:
—RA5AA is saturated aliphatic C1-3alkyl;
—RA5B is —CF3;
—RA5C is independently —F, —Cl, —Br, or —I;
—RA5D is independently —C≡CH, —C≡C—RA5DA, or —C≡C—RA5DB—OH;
—RA5DA is saturated aliphatic C1-4alkyl;
—RA5DB is saturated aliphatic C1-4alkylene;
—RA5E is independently saturated C3-6cycloalkyl;
—RA5F is —C(═O)O—RA5FA;
and
—RA5FA is saturated aliphatic C1-3alkyl.

14 more elements

Dependencies are inferred from the claim text.

Facts

Application

14/356,626Filed 9 Nov 2012 · us provisional application

Priority

9 Nov 2011

Published

US 2014/0315925 A123 Oct 2014

Granted

26 May 2015

Term ends

Not estimatedThe source records don’t support an estimate.

Classification14 codes

C07D 401/14
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a…:…
A61K 9/0053
Galenical forms characterised by the site of application: mouth and digestive tract, i.e. intraoral and peroral administration
A61K 31/497
Non-condensed pyrazines: containing further heterocyclic rings
A61K 45/06
Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00: mixtures of active ingredients without…

5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use

Life of this patent

5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use

Life of this patent

Abstract

Claims39