Complement pathway modulators and uses thereof

Patent metadata

Field	Value
Publication number	US-9550755-B2
Application number	US-201314409914-A
Country	US
Kind code	B2
Filing date	Jun 27, 2013
Priority date	Jul 12, 2012
Publication date	Jan 24, 2017
Grant date	Jan 24, 2017

Abstract

The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

First claim

What is claimed is:

1. A compound, or salt thereof, represented by formula (V) or (VI):

wherein
Z 2 is CR 2 or N;
R 2 is hydrogen, C 1 -C 4 alkyl, or halogen;
R 3 is hydrogen, C 1 -C 4 alkyl, or pyrimidinylmethoxy;
R 5 is methyl or amino; and
R 10 is C 1 -C 4 alkyl, C 3 -C 6 cycloalkyl-methyl or C 1 -C 2 haloalkyl.

2. The compound of claim 1 , or a salt thereof, selected from the group consisting of:
1-(2-oxo-2-((1R,3S,5R)-3-(1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-ylcarbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl)ethyl)-1H-indazole-3-carboxamide;
1-(2-oxo-2-((1R,3S,5R)-3-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl)carbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl)ethyl)-1H-pyrazolo[3,4-c]pyridine-3-carboxamide;
(1R,3S,5R)-2-(2-(3-acetyl-1H-pyrazolo[3,4-c]pyridin-1-yl)acetyl)-N-(1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl)-2-azabicyclo[3.1.0] hexane-3-carboxamide; and
(1R,3S,5R)-N2-(1-carbamoyl-1H-indol-3-yl)-N3-(1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl)-2-azabicyclo[3.1.0] hexane-2,3-dicarboxamide.

3. The compound of claim 1 , or a salt thereof, which is 1-(2-((1R,3S,5R)-3-(1-isopropyl-1H-pyrazol-3-ylcarbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)-1H-indazole-3-carboxamide.

4. A pharmaceutical composition comprising one or more pharmaceutically acceptable carriers and a therapeutically effective amount of a compound of claim 1 .

Assignees

• Novartis Ag

Inventors

• Hommel Ulrich
• Lorthiois Edwige Liliane Jeanne
• Maibaum Jeurgen Klaus
• Ostermann Nils
• Randl Stefan Andreas
• Rogel Olivier
• Vulpetti Anna

Classifications

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title

• A61P37/02

  Immunomodulators · CPC title