IP Library Granted Patent US 9,758,521
Granted Patent B2
US 9,758,521 · App. 15/388,178 · Granted Sep 12, 2017

Kinase inhibitors

Inventors: Carmelida Capaldi (Parma, IT); Elisabetta Armani (Parma, IT); Andrew Steven Robert Jennings (Harlow, GB); Christopher Hurley (Harlow, GB)
Assignee: CHIESI FARMACEUTICI S.p.A.
C07D471/04
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Quick Facts
Patent No.
US 9,758,521
App. No.
15/388,178
Granted
Sep 12, 2017
Kind
B2
Abstract

Compounds of formulae (I), (II), and (III), defined herein, are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.

Claims (24)

1. A compound of formula (I):

wherein

R 1 is a group of one of the following formulae:

or a pharmaceutically acceptable salt thereof.

2. A compound or pharmaceutically acceptable salt according to claim 1 , which is:

1-(3-tert-Butyl-1′-methyl-1′H-[1,4′]bipyrazolyl-5-yl)-3-{(1S,4R)-4-[3-(1-dimethylamino-1-methyl-ethyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalenyl}-urea hydrochloride salt;

1-(3-tert-Butyl-1′-methyl-1′H-[1,4′]bipyrazolyl-5-yl)-3-{(1S,4R)-4-[3-((S)-1,2-dimethyl-pyrrolidin-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalenyl}-urea hydrochloride salt;

1-(3-tert-Butyl-1′-methyl-1′H-[1,4′]bipyrazolyl-5-yl)-3-{(1S,4R)-4-[3-((S)-1-isopropyl-pyrrolidin-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalenyl}-urea hydrochloride salt; or

1-(3-tert-Butyl-1′-methyl-1′H-[1,4′]bipyrazolyl-5-yl)-3-{(1S,4R)-4-[3-((S)-1-isopropyl-piperidin-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea hydrochloride salt.

3. A compound of formula (II):

wherein

R 1 is a group of one of the following formulae:

or a pharmaceutically acceptable salt thereof.

4. A compound or pharmaceutically acceptable salt according to claim 3 , which is:

1-(5-tert-Butyl-2-methyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-((S)-1,2-dimethyl-pyrrolidin-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea hydrochloride salt; or

1-(5-tert-Butyl-2-methyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-(1-dimethylamino-1-methyl-ethyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea hydrochloride salt.

5. A compound of formula (III):

wherein

R 1 is a group of one of the following formulae:

or a pharmaceutically acceptable salt thereof.

6. A compound or pharmaceutically acceptable salt according to claim 5 , which is:

1-(5-tert Butyl-isoxazol-3-yl)-3-{(1S,4R)-4-[3-((S)-1-isopropyl-pyrrolidin-2-yl)-[1,2,4]triazolo[4,3-a]pyridine-6-yloxy]-1,2,3,4-tetrahydronaphthalen-1-yl)}-urea hydrochloride salt; or

1-(5-tert Butyl-isoxazol-3-yl)-3-{(1S,4R)-4-[3-((S)-1-methyl-pyrrolidin-2-yl)-[1,2,4]triazolo[4,3-a]pyridine-6-yloxy]-1,2,3,4-tetrahydronaphthalen-1-yl}-urea hydrochloride salt.

7. A pharmaceutical composition, comprising a compound or a pharmaceutically acceptable salt according to claim 1 and one or more pharmaceutically acceptable carriers.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 17, 2017
From: ARGENTA DISCOVERY 2009 LIMITED
To: CHIESI FARMACEUTICI S.P.A.
Reel/Frame 042026/0933 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 12, 2017
From: CAPALDI, CARMELIDA; ARMANI, ELISABETTA
To: CHIESI FARMACEUTICI S.P.A.
Reel/Frame 041978/0938 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 12, 2017
From: JENNINGS, ANDREW STEVEN ROBERT; HURLEY, CHRISTOPHER
To: ARGENTA DISCOVERY 2009 LIMITED
Reel/Frame 041978/0957 →
Priority Claims (1)
EP 15202350 · Dec 23, 2015 · regional
Continuity (1)
Related Publication 20170183344A1 · Jun 29, 2017