Autotaxin inhibitors

Patent metadata

Field	Value
Publication number	US-9763957-B2
Application number	US-201414906161-A
Country	US
Kind code	B2
Filing date	Jul 16, 2014
Priority date	Jul 18, 2013
Publication date	Sep 19, 2017
Grant date	Sep 19, 2017

Abstract

The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.

First claim

The invention claimed is:

1. A compound which is selected from the group consisting of:
(E)-1-(4-(5-methyl-1,3,4-oxadiazol-2-yl)piperidin-1-yl)-3-(2-((5-methyl-2H-tetrazol-2-yl)methyl)-4-(trifluoromethyl)phenyl)prop-2-en-1-one;
(E)-1-(4-(3-methyl-1H-1,2,4-triazol-1-yl)piperidin-1-yl)-3-(2-((5-methyl-2H-tetrazol-2-yl)methyl)-4-(trifluoromethyl)phenyl)prop-2-en-1-one;
1-(4-(5-Methyl-1,3,4-oxadiazol-2-yl)piperidin-1-yl)-3-(2-((5-methyl-2H-tetrazol-2-yl)methyl)-4-(trifluoromethyl)phenyl)propan-1-one;

or a pharmaceutically acceptable salt thereof.

2. The compound which is (E)-1-(4-(5-methyl-1,3,4-oxadiazol-2-yl)piperidin-1-yl)-3-(2-((5-methyl-2H-tetrazol-2-yl)methyl)-4-(trifluoromethyl)phenyl)prop-2-en-1-one; or a pharmaceutically acceptable salt thereof.

3. The compound which is (E)-1-(4-(3-methyl-1H-1,2,4-triazol-1-yl)piperidin-1-yl)-3-(2-((5-methyl-2H-tetrazol-2-yl)methyl)-4-(trifluoromethyl)phenyl)prop-2-en-1-one; or a pharmaceutically acceptable salt thereof.

4. The compound which is 1-(4-(5-Methyl-1,3,4-oxadiazol-2-yl)piperidin-1-yl)-3-(2-((5-methyl-2H-tetrazol-2-yl)methyl)-4-(trifluoromethyl)phenyl)propan-1-one; or a pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

6. A pharmaceutical combination comprising a therapeutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and one or more therapeutically active co-agent.

7. A method of treating an autotaxin dependent or an autotaxin mediated disease or condition, wherein the disease or condition is idiopathic pulmonary fibrosis, comprising administering to a subject a therapeutically effective amount of a compound according to claim 1 .

Assignees

• Novartis Ag

Inventors

• Beattie David
• Baettig Urs
• Legrand Darren Mark
• Lister Andrew Stuart
• Mckenna Jeffrey
• Pearce David William
• Sandham David Andrew
• Steward Oliver Ross
• Thomson Christopher

Classifications

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title

• A61P1/16

  for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics · CPC title