IP Library Granted Patent US 9,238,647
Granted Patent B2
US 9,238,647 · App. 13/259,040 · Granted Jan 19, 2016

P2X3 receptor antagonists for treatment of pain

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Quick Facts
Patent No.
US 9,238,647
App. No.
13/259,040
Granted
Jan 19, 2016
Kind
B2
Abstract

The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.

Claims (175)

1. A compound represented in Tables 9 and 10:

TABLE 9

Example

R 3a

B

9.1

9.2

9.3

9.4

9.5

9.6

9.7

9.8

9.9

9.10

9.11

9.12

9.13

9.14

9.15

9.16

9.17

9.18

9.19

9.20

9.21

9.22

9.23

9.24

9.25

9.26

9.27

9.28

9.29

9.30

9.31

9.32

9.33

9.34

9.35

9.36

9.37

9.38

9.39

9.40

9.41

9.42

9.43

9.44

9.45

9.46

9.47

9.48

9.49

9.50

9.51

9.52

9.53

9.54

9.55

9.56

9.57

9.58

9.59

9.60

9.61

9.62

9.63

Example

R 6

R 6a

9.1

H

9.2

H

9.3

H

9.4

H

9.5

9.6

H

9.7

H

9.8

9.9

9.10

9.11

H

9.12

H

9.13

9.14

H

9.15

H

9.16

H

9.17

9.18

9.19

H

9.20

H

9.21

H

9.22

9.23

9.24

9.25

9.26

9.27

H

9.28

9.29

9.30

9.31

9.32

H

9.33

9.34

9.35

9.36

H

9.37

H

9.38

9.39

9.40

H

9.41

9.42

9.43

9.44

9.45

9.46

9.47

9.48

H

9.49

H

9.50

9.51

9.52

9.53

9.54

9.55

9.56

9.57

9.58

9.59

9.60

9.61

9.62

9.63

TABLE 10

Example

R 3a

B

10.1

10.2

Example

R 6a

R 6

10.1

10.2

or pharmaceutically acceptable salts and individual enantiomers thereof.

2. The compound according to claim 1 which is:

TABLE 9

R 3a

B

R 6

R 6a

or pharmaceutically acceptable salts and individual enantiomers thereof.

3. A pharmaceutical composition comprising an inert carrier and an effective amount of a compound according to claim 1 .

Assignments (3)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
CORRECTIVE ASSIGNMENT TO CORRECT THE INVENTOR JOHN J. LIN, SHOULD BE CORRECTED TO JOHN J. LIM PREVIOUSLY RECORDED ON REEL 031388 FRAME 0365. ASSIGNOR(S) HEREBY CONFIRMS THE INVENTOR JOHN J. LIN, SHOULD BE CORRECTED TO JOHN J. LIM. Recorded Jan 23, 2014
From: SEGERDELL, CAROLYN; BURGERY, CHRISTOPHER S; DENG, ZHENGWU J; NGUYEN, DIEM N; PAONE, DANIEL V; POTTEIGER, CRAIG M; NOMLAND, ASHLEY; LIM, JOHN J.; STAUFFER, SHAUN R.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 032123/0113 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 11, 2013
From: SEGERDELL, CAROLYN; BURGEY, CHRISTOPHER S.; DENG, ZHENGWU J.; NGUYEN, DIEM N.; PAONE, DANIEL V.; POTTEIGER, CRAIG M.; NOMLAND, ASHLEY; LIN, JOHN J.; STAUFFER, SHAUN R.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 031388/0365 →