IP Library Granted Patent US 9,840,496
Granted Patent B2
US 9,840,496 · App. 15/529,120 · Granted Dec 12, 2017

CD38 inhibitors and methods of treatment

Inventors: J. David Becherer (Research Triangle Park, NC); Rodolfo Cadilla (King of Prussia, PA); David Norman Deaton (King of Prussia, PA); Curt Haffner (King of Prussia, PA); Brad Richard Henke (Research Triangle Park, NC); Frank Preugschat (Research Triangle Park, NC); Christie Schulte (King of Prussia, PA)
Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
C07D403/04
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Quick Facts
Patent No.
US 9,840,496
App. No.
15/529,120
Granted
Dec 12, 2017
Kind
B2
Abstract

Compounds of Formula I and methods of treating diseases of metabolism by modulating cellular NAD+ levels through the inhibition of the CD38 enzyme, are disclosed.

Claims (12)

1. A compound of Formula I

wherein Q is O, NH, N(H)C(O), or C(O)N(H);

R 1 is C 1-5 alkylS(O) 2 CH 3 , or C 1-6 alkyl wherein said alkyl can comprise straight-chain portions, branched chain portions, cycloalkyl portions, and wherein said C 1-6 alkyl is optionally substituted by one OH or OCH 3 and wherein said C 1-6 alkyl is optionally further substituted by 1 to 3 Fluorine atoms; and

R 2 is H, C 1-3 alkyl, or halogen.

2. A pharmaceutically acceptable salt of a compound of Formula I

wherein Q is O, NH, N(H)C(O), or C(O)N(H);

R 1 is C 1-5 alkylS(O) 2 CH 3 , or C 1-6 alkyl wherein said alkyl can comprise straight-chain portions, branched chain portions, cycloalkyl portions, and wherein said C 1-6 alkyl is optionally substituted by one OH or OCH 3 and wherein said C 1-6 alkyl is optionally further substituted by 1 to 3 Fluorine atoms; and

R 2 is H, C 1-3 alkyl, or halogen.

3. A compound according to claim 1 wherein R 2 is H or Cl.

4. A compound according to claim 1 wherein R 2 is H.

5. A compound according to claim 1 wherein the orientation on the cyclohexyl ring is trans as depicted below

6. The compound

Assignments (2)
CHANGE OF ADDRESS Recorded Apr 16, 2025
From: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
Reel/Frame 070854/0469 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 24, 2017
From: CADILLA, RODOLFO; SCHULTE, CHRISTIE; DEATON, DAVID NORMAN; HENKE, BRAD RICHARD; PREUGSCHAT, FRANK; HAFFNER, CURT; BECHERER, J. DAVID
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
Reel/Frame 042551/0204 →
Continuity (2)
Provisional Application 62086844 · Dec 3, 2014
Related Publication 20170260164A1 · Sep 14, 2017