Amide-substituted pyridinyltriazole derivatives and uses thereof

Patent metadata

Field	Value
Publication number	US-10472348-B2
Application number	US-201815969222-A
Country	US
Kind code	B2
Filing date	May 2, 2018
Priority date	May 3, 2016
Publication date	Nov 12, 2019
Grant date	Nov 12, 2019

Abstract

The present invention relates to novel 5-(carboxamide)-1-pyridinyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.

First claim

The invention claimed is:

1. A compound 3-({3-(4-Chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-[3-(trifluoromethyl) pyridin-2-yl]-1H-1,2,4-triazole-5-carboxamide, having the following formula

or a pharmaceutically acceptable salt, hydrate, and/or solvate thereof.

2. The compound of claim 1 , wherein the compound is 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-[3-(trifluoro-methyl)pyridin-2-yl]-1H-1,2,4-triazole-5-carboxamide having the following formula

3. The compound of claim 1 for use in a method for treatment of at least one disease selected from the group consisting of acute and chronic kidney diseases, acute and chronic heart failure, preeclampsia, peripheral arterial disease (PAD), coronary microvascular dysfunction (CMD), Raynaud's syndrome, and dysmenorrhea.

4. The compound of claim 1 for use in a method for treatment of diabetic nephropathy.

5. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt, hydrate, and/or solvate thereof, and one or more pharmaceutically acceptable excipients.

6. The pharmaceutical composition of claim 5 comprising one or more further active ingredients selected from the group consisting of diuretics, angiotensin All antagonists, ACE inhibitors, beta-receptor blockers, mineralocorticoid receptor antagonists, antidiabetics, organic nitrates and NO donors, activators and stimulators of the soluble guanylate cyclase (sGC), antiinflammatory agents, immunosuppressive agents, phosphate binders, and compounds that modulate vitamin D metabolism.

7. The pharmaceutical composition of claim 5 for treatment of at least one disease selected from the group consisting of acute kidney disease, chronic kidney disease, acute heart failure, chronic heart failure, preeclampsia, peripheral arterial disease (PAD), coronary microvascular dysfunction (CMD), Raynaud's syndrome, and dysmenorrhea.

8. The pharmaceutical composition of claim 5 for treatment of diabetic nephropathy.

9. A method for treatment of at least one disease selected from the group consisting of acute kidney disease, chronic kidney disease, acute heart failure, chronic heart failure, preeclampsia, peripheral arterial disease (PAD), coronary microvascular dysfunction (CMD), Raynaud's syndrome, and dysmenorrhea in a human or other mammal in need thereof, comprising administering to the human or other mammal in need thereof a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt, hydrate, and/or solvate thereof.

10. A method for treatment of at least one disease selected from the group consisting of acute kidney disease, chronic kidney disease, acute heart failure, chronic heart failure, preeclampsia, peripheral arterial disease (PAD), coronary microvascular dysfunction (CMD), Raynaud's syndrome, and dysmenorrhea in a human or other mammal in need thereof, comprising administering to the human or other mammal in need thereof a therapeutically effective amount of a pharmaceutical composition comprising (i) a compound of claim 1 or a pharmaceutically acceptable salt, hydrate, and/or solvate thereof and (ii) one or more pharmaceutically acceptable excipients.

11. A method for treatment of diabetic nephropathy in a human or other mammal in need thereof, comprising administering to the human or other mammal in need thereof a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt, hydrate, and/or solvate thereof.

12. A method for treatment of diabetic nephropathy in a human or other mammal in need thereof, comprising administering to the human or other mammal in need thereof a therapeutically effective amount of a pharmaceutical composition comprising (i) a compound of claim 1 or a pharmaceutically acceptable salt, hydrate, and/or solvate thereof and (ii) one or more pharmaceutically acceptable excipients.

Assignees

• Bayer Pharma AG

Inventors

• Collin Marie-Pierre
• Kolkhof Peter
• Neubauer Thomas
• Fürstner Chantal
• Pook Elisabeth
• Wittwer Matthias Beat
• Lustig Klemens
• Buchmüller Anja
• Tinel Hanna
• DRÖBNER Karoline
• Mondritzki Thomas
• Schirmer Heiko
• Kretschmer Axel
• Schmeck Carsten
• Wasnaire Pierre
• Cernecka Hana

Classifications

• A61P13/12

  of the kidneys · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61K31/4439 Primary

  containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465) · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• C07D401/14 Primary

  containing three or more hetero rings · CPC title