US 2017/0247357 A1 · PYRIDINE DERIVATIVES AS SOFT ROCK INHIBITORS

Abstract

The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including Respiratory and Gastro-Intestinal diseases.

Claims8

Dependent claims

-12. (canceled)

A method of treatment of fibrosis, wherein the method comprises administering to a patient in need thereof, a therapeutically effective amount of a compound of Formula I or a stereoisomer, tautomer, racemic, salt, hydrate, or solvate thereof,

Wherein
R1 is selected from hydrogen and C1-20alkyl;
X1 is hydrogen or halo;
X2 is —C(═O)—NH— or —NH—C(═O)—;
Cy is an optionally substituted group selected from aryl and heteroaryl;
X3 is selected from the group consisting of —S—, —O—, and —NR2—;
R2 is hydrogen or C1-6alkyl;
Het1 is 2-oxotetrahydrofuranyl optionally substituted with one or more C1-6alkyl-;
and
A1 and A2 are each independently a direct bond or an optionally substituted C1-6alkylene.

7 more elements

Dependencies are inferred from the claim text.

Facts

Application

15/595,219Filed 15 May 2017

Priority

EP 13153094.129 Jan 2013

Published

31 Aug 2017

Term ends

Not estimatedThe source records don’t support an estimate.

Classification13 codes

C07D 405/12
Containing two hetero rings: linked by a chain containing hetero atoms as chain links
A61K 31/33
Medicinal preparations containing organic active ingredients: heterocyclic compounds
A61K 31/435
Having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins: having six-membered rings with one nitrogen as the only ring hetero atom
A61K 31/4355
Ortho- or peri-condensed with heterocyclic ring systems: the heterocyclic ring system containing a five-membered ring having oxygen as a ring…

Pyridine derivatives as soft rock inhibitors

Life of this patent

Pyridine derivatives as soft rock inhibitors

Life of this patent

Abstract

Claims8