IP Library Granted Patent US 9,290,485
Granted Patent B2
US 9,290,485 · App. 13/194,009 · Granted Mar 22, 2016

N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides

Inventors: Trixi Brandl (Basel, CH); Stefanie Flohr (Basel, CH); Sebastian Kopec (Basel, CH); Julie Lachal (Basel, CH); Christian Markert (Basel, CH); Kenji Namoto (Basel, CH); Perle Nganga (Basel, CH); Bernard Pirard (Basel, CH); Martin Renatus (Basel, CH); Richard Sedrani (Basel, CH); Thomas Zoller (Basel, CH)
Assignee: NOVARTIS AG
C07D409/14C07D403/12C07D403/14C07D405/14C07D413/12C07D417/14
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Quick Facts
Patent No.
US 9,290,485
App. No.
13/194,009
Granted
Mar 22, 2016
Kind
B2
Abstract

The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

Claims (27)

1. A compound, or salt thereof, of Formula 1 A:

wherein

R 1 and R 3 are C 1-4 alkyl;

A is a ring system selected from

wherein the bond marked with the asterisk is attached to the carboxamide group and wherein each R 8 is hydrogen;

L is —C(R 10 ) 2 —; and each R 10 is hydrogen;

B is a quinolinyl, wherein the quinolinyl may be substituted once or more than once by R 12 ;

and wherein a substituent on a nitrogen in a heterocyclic ring system may not be halogen;

each R 12 independently is halogen; —X 2 —R 13 ;

X 2 is selected from bond; and

R 13 is C 1-6 alkyl; C 1-6 halogenalkyl.

2. A compound, or salt thereof, of claim 1

wherein

R 1 and R 3 are C 1-4 alkyl;

A is a ring system selected from

wherein the bond marked with the asterisk is attached to the carboxamide group and wherein each R 8 is hydrogen;

L is —C(R 10 ) 2 - ; and each R 10 is hydrogen;

B is a quinolin-2-yl, quinol-3-yl, quinol-6-yl, wherein the quinolinyl may be substituted once or more than once by R 12 ; and wherein a substituent on a nitrogen in a heterocyclic ring system may not be halogen;

each R 12 independently is halogen; —X 2 —R 13 ;

X 2 is selected from bond; and

R 13 is C 1-6 alkyl; C 1-6 halogenalkyl.

3. A compound, or salt thereof, of claim 1 selected from:

N-((6-amino-2,4-dimethylpyridin-3-yl)methyl)-1-((2-methylquinolin-6-yl)methyl)-1H-1,2,3-triazole-4-carboxamide;

N-((6-amino-2,4-dimethylpyridin-3-yl)methyl)-1-((7-methylquinolin-3-yl)methyl)-1H-1,2,3-triazole-4-carboxamide; and

N-((6-amino-2,4-dimethylpyridin-3-yl)methyl)-1-((7-chloroquinolin-2-yl)methyl)-1H-1,2,3-triazole-4-carboxamide.

4. A compound, or salt thereof, of claim 1 wherein the compound is

5. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 in free form or in pharmaceutically acceptable salt form and one or more pharmaceutically acceptable carriers.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 2, 2011
From: BRANDL, TRIXI; FLOHR, STEFANIE; KOPEC, SEBASTIAN; LACHAL, JULIE; MARKERT, CHRISTIAN; NAMOTO, KENJI; NGANGA, PERLE; PIRARD, BERNARD; RENATUS, MARTIN; SEDRANI, RICHARD; ZOLLER, THOMAS
To: NOVARTIS AG
Reel/Frame 027160/0952 →
Continuity (2)
Provisional Application 61370612 · Aug 4, 2010
Related Publication 20120035168A1 · Feb 9, 2012