IP Library Granted Patent US 10,308,609
Granted Patent B2
US 10,308,609 · App. 14/855,102 · Granted Jun 4, 2019

Bicyclic compounds

Inventors: Kevin Duane Bunker (Escondido, CA); Chuangxing Guo (San Diego, CA); Mark Charles Grier (San Diego, CA); Chad Daniel Hopkins (San Diego, CA); Joseph Robert Pinchman (San Diego, CA); Deborah Helen Slee (Encinitas, CA); Qinhua Huang (San Diego, CA); Mehmet Kahraman (San Diego, CA)
Assignee: Zeno Royalties & Milestones, LLC
C07D213/89A61K31/13A61K31/145A61K31/16A61K31/164A61K31/27A61K31/444A61K45/06C07C211/38C07C215/42C07C233/05C07C233/06C07C233/09C07C233/13C07C233/14C07C233/23C07C317/30C07C2601/02C07C2602/38C07C2603/62
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Quick Facts
Patent No.
US 10,308,609
App. No.
14/855,102
Granted
Jun 4, 2019
Kind
B2
Abstract

Disclosed herein are compounds of Formulae (I) and (II), methods of synthesizing compounds of Formulae (I) and (II), and methods of using compounds of Formulae (I) and (II) as an analgesic.

Claims (37)

1. A method for reducing pain or fever comprising administering to a subject an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt thereof, in a subject in need thereof, wherein Formula (I) has the structure:

wherein:

R 1 is selected from the group consisting of H, D, a substituted or unsubstituted C 1-6 alkyl and a substituted or unsubstituted C 1-6 haloalkyl;

R 2 is H;

R 3 is selected from the group consisting of D, halo, hydroxy, a substituted or unsubstituted C 1-8 alkyl, a substituted or unsubstituted C 2-8 alkenyl, a substituted or unsubstituted C 2-8 alkynyl, a substituted or unsubstituted C 3-20 cycloalkyl, a substituted or unsubstituted C 3-20 cycloalkenyl, a substituted or unsubstituted C 8-20 cycloalkynyl, a substituted or unsubstituted C 6-20 aryl, a substituted or unsubstituted heteroaryl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl(C 1-6 alkyl), a substituted or unsubstituted heteroaryl(C 1-6 alkyl), a substituted or unsubstituted heterocyclyl(C 1-6 alkyl), a substituted or unsubstituted C 1-8 haloalkyl and a substituted or unsubstituted sulfonyl;

m is 0; and

provided that when R 1 is H, then R 3 is not t-butyl; and provided that a compound of Formula (I), or a pharmaceutically salt thereof, is not

2. A compound of Formula (I), or a pharmaceutically acceptable salt thereof,

wherein:

R 1 is selected from the group consisting of H, D, a substituted or unsubstituted C 1-6 alkyl and a substituted or unsubstituted C 1-6 haloalkyl;

R 2 is H;

R 3 is selected from the group consisting of D, hydroxy, an unsubstituted C 1-8 alkyl, a substituted or unsubstituted C 2-8 alkenyl, a substituted or unsubstituted C 2-8 alkynyl, a substituted or unsubstituted C 3-20 cycloalkenyl, a substituted or unsubstituted C 8-20 cycloalkynyl, a substituted or unsubstituted heteroaryl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl(C 1-6 alkyl), a substituted or unsubstituted heteroaryl(C 1-6 alkyl), a substituted or unsubstituted heterocyclyl(C 1-6 alkyl), CHF 2 , CH 2 F, CF 2 CH 3 and a substituted or unsubstituted sulfonyl; and

m is 0; and

provided that when R 1 is H then R 3 is not selected from the group consisting of CH 3 , hydroxy and an unsubstituted t-butyl; and provided that a compound of Formula (I), or a pharmaceutically salt thereof, cannot be N,N-diethyl-alpha-methyl-bicyclo[1.1.1]pentane-1-methanamine or

3. A pharmaceutical composition comprising an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt thereof, as recited in claim 2 , and a pharmaceutically acceptable carrier, diluent, excipient or combination thereof.

4. The compound of claim 2 , wherein R 1 is H.

5. The compound of claim 2 , wherein R 3 is an unsubstituted C 1-8 alkyl.

6. The compound of claim 2 , wherein R 3 is a substituted or unsubstituted sulfonyl.

7. The compound of claim 2 , wherein R 3 is a substituted or unsubstituted C 2-8 alkenyl, a substituted or unsubstituted C 2-8 alkynyl, a substituted or unsubstituted C 3-20 cycloalkenyl, a substituted or unsubstituted C 8-20 cycloalkynyl, a substituted or unsubstituted heteroaryl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl(C 1-6 alkyl), a substituted or unsubstituted heteroaryl(C 1-6 alkyl) or a substituted or unsubstituted heterocyclyl(C 1-6 alkyl).

8. The compound of claim 2 , wherein the compound is selected from

or a pharmaceutically acceptable salt of any of the foregoing.

9. The compound of claim 2 , wherein R 1 is an unsubstituted C 1-6 alkyl.

10. The compound of claim 2 , wherein R 1 is H; and R 3 is CHF 2 , CH 2 F or CF 2 CH 3 .

11. The compound of claim 2 , wherein R 3 is a substituted or unsubstituted C 3-20 cycloalkenyl.

12. The compound of claim 2 , wherein R 3 is a substituted or unsubstituted C 8-20 cycloalkynyl.

13. The compound of claim 2 , wherein R 3 is a substituted or unsubstituted heteroaryl.

14. The compound of claim 2 , wherein R 3 is a substituted or unsubstituted heterocyclyl.

15. The compound of claim 2 , wherein R 3 is a substituted or unsubstituted aryl(C 1-6 alkyl).

16. The compound of claim 2 , wherein R 3 is a substituted or unsubstituted heteroaryl(C 1-6 alkyl).

17. The compound of claim 2 , wherein R 3 is a substituted or unsubstituted heterocyclyl(C 1-6 alkyl).

18. The method of claim 1 , wherein the compound is selected from

or a pharmaceutically acceptable salt of any of the foregoing.

19. The method of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

20. The compound of claim 2 , wherein R 3 is CHF 2 , CH 2 F or CF 2 CH 3 .

21. The method of claim 1 , wherein R 3 is CHF 2 , CH 2 F or CF 2 CH 3 .

22. The method of claim 21 , wherein R 1 is H.

Assignments (3)
CHANGE OF NAME Recorded Jan 3, 2020
From: ZENO ROYALTIES & MILESTONES, LLC
To: RECURIUM IP HOLDINGS, LLC
Reel/Frame 051479/0848 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 6, 2018
From: KALYRA PHARMACEUTICALS, INC.
To: ZENO ROYALTIES & MILESTONES, LLC
Reel/Frame 047423/0493 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2015
From: BUNKER, KEVIN DUANE; GUO, CHUANGXING; GRIER, MARK CHARLES; HOPKINS, CHAD DANIEL; PINCHMAN, JOSEPH ROBERT; SLEE, DEBORAH HELEN; HUANG, QINHUA; KAHRAMAN, MEHMET
To: KALYRA PHARMACEUTICALS, INC.
Reel/Frame 037181/0376 →
Continuity (2)
Provisional Application 62051760 · Sep 17, 2014
Related Publication 20160075654A1 · Mar 17, 2016