IP Library › Granted Patent US 9,567,320
Granted Patent B2
US 9,567,320 · App. 14/766,671 · Granted Feb 14, 2017

Pyridazinone-amides derivatives

Inventors: Catherine Jorand-Lebrun (Contamine-Sarzin, FR); Santosh Kulkarni (Bangalore, IN); Stefano Crosignani (Nivelles, BE)
Assignee: MERCK PATENT GmbH
C07D403/14A61K31/501A61K31/506A61K45/06C07D401/14
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Quick Facts
Patent No.
US 9,567,320
App. No.
14/766,671
Granted
Feb 14, 2017
Kind
B2
Abstract

The present invention relates to compounds of formula (I) wherein R1, Ra, Rb and Z have the meaning given in claim 1 , and their use in the prophylaxis and treatment of diseases.

Claims (35)

1. A compound of formula (I):

wherein Ra is H, Hal or Al, wherein Hal is F, Cl, Br, or I, and wherein Al is a branched or linear alkyl having 1 to 12 C-atoms, wherein one or more H atoms may be replaced by Hal, ORb, COORb, CN or N(Rb) 2 and wherein one or more CH 2 -groups may be replaced by O, CO, NRb or S, SO, SO 2 , 1,2-, 1,3- or 1,4- phenylen, —CH═CH— or —C══C—,

wherein Rb is H or alkyl,

wherein R1 is H, Hal or Al, and

wherein Z is a group:

wherein in said group:

X is CH or N,

Y is CH or N, and

Rc is H, Hal or Al,

and a pharmaceutically acceptable solvate, pharmaceutically acceptable salt, or stereoisomer thereof.

2. The compound of Formula (I) according to claim 1 , wherein Ra is Hal, ORd, or alkyl, and wherein Rd is H, alkyl or COH or COalkyl.

3. The compound of Formula (I) according to claim 1 , wherein R1 denotes H, alkyl, Hal, Oalkyl, ORd, (CH 2 )nCONHRb or (CH2)nCOORb, wherein n is 0, 1, 2, 3, 4, 5, or 6 and Rd is H, alkyl or CORb.

4. The compound of Formula (I) according to claim 1 , wherein Z is pyridinyl or pyrimidinyl.

5. The compound of Formula (I) according to claim 1 , selected from the group consisting of compounds 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17 and a pharmaceutically acceptable solvate, pharmaceutically acceptable salt, or stereoisomer thereof,

wherein compounds 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17 are:

1

2

3

4

5

6

7

8

9

10

11

12

13

14

15

16

17

6. A pharmaceutical composition, comprising:

the compound of Formula (I) according to claim 1 and a pharmaceutically acceptable solvate, salt, hydrate or stereoisomer thereof, including mixtures thereof in all ratios.

7. A method for the treatment of rheumatoid arthritis, lupus nephritis, and systemic lupus erythematosus comprising administering the composition according to claim 6 to a subject in need thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 11, 2015
From: JORAND-LEBRUN, CATHERINE; KULKARNI, SANTOSH; CROSIGNANI, STEFANO
To: MERCK PATENT GMBH
Reel/Frame 037010/0539 →
Priority Claims (1)
EP 13154390 · Feb 7, 2013 · regional
Continuity (1)
Related Publication 20150376167A1 · Dec 31, 2015