IP Library Granted Patent US 10,308,597
Granted Patent B2
US 10,308,597 · App. 15/307,178 · Granted Jun 4, 2019

Inhibitors of creatine transport and uses thereof

Inventors: Eduardo J. Martinez (Bryn Mawr, PA); Sohail F. Tavazoie (New York, NY)
Assignee: Rgenix, Inc.
C07C279/14A61K31/00A61K31/155A61K31/337A61K31/397A61K31/40A61K31/4168A61K31/4402A61K31/4427A61K31/505A61K31/53A61K31/704A61K31/7068A61K31/7105A61K45/06C07C257/14C07C259/14C07C275/70C07C279/16C07C279/26C07C279/36C07C281/16C07C281/18C07C309/15C07C313/34C07D205/04C07D205/08C07D207/16C07D207/22C07D213/74C07D213/76C07D231/12C07D233/26C07D233/46C07D233/52C07D233/64C07D233/88C07D239/06C07D239/14C07D249/08C07D249/14C07D253/06C07D257/08C07D295/32C07D401/04C07D405/04C07D487/04C07F9/097C07F9/2458C07F9/3808C07F9/4006C07F9/48C07F9/568C07F9/572C07F9/6506C07H19/06C07B2200/05C07C2601/02C07C2601/04
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,308,597
App. No.
15/307,178
Granted
Jun 4, 2019
Kind
B2
Abstract

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

Claims (32)

1. A compound having the structure:

wherein Q1 is

m is 1 or 2;

R7 is hydrogen;

one R8 combines with R12 with the atoms to which they are attached to form an optionally substituted C3-C4 heterocycle;

a second R8, if present, is hydrogen, deuterium, halo, NH2, optionally substituted C1-C3 alkyl, or combines with an R9 and with the atoms to which they are attached to form an optionally substituted C3-C6 cycloalkyl ring; or combines with R10 or R11 and with the atoms to which they are attached to form an optionally substituted C3-C4 cycloalkyl ring;

each R9 is independently hydrogen, deuterium, halo, NH2, optionally substituted C1-C3 alkyl or combines with the second R8, if present, and with the atoms to which they are attached to form an optionally substituted C3-C6 cycloalkyl ring; or combines with R10 or R11 and with the atoms to which they are attached to form an optionally substituted C3-C4 cycloalkyl ring;

R10 and R11 are independently hydrogen, deuterium, optionally substituted C1-C4 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl or R10 and R11 combine with the atoms to which they are attached to form an optionally substituted C3-C6 cycloalkyl ring; or R10 or R11 combine with R8 or R9 with the atoms to which they are attached to form an optionally substituted C3-C4 cycloalkyl ring; or R10 or R11 combine with R12 with the atoms to which they are attached to form an optionally substituted C3-C4 heterocycle;

R12 is hydrogen, optionally substituted C1-C6 alkyl, or R12 combines with R8 or R9 with the atoms to which they are attached to form an optionally substituted C3-C4 heterocycle, or R12 combines with R10 or R11 with the atoms to which they are attached to form an optionally substituted C3-C4 heterocycle;

wherein if m is 1 and R10 is methyl then at least one of R9, and R11 is not hydrogen;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein R 10 is optionally substituted C 1 -C 4 alkyl, optionally substituted C 2 -C 6 alkenyl, optionally substituted C 2 -C 6 alkynyl.

3. The compound of claim 2 , wherein R 10 is methyl, ethyl, n-propyl, iso-propyl, —CD 3 , —CF 3 , —CH 2 F, —CHF 2 , —CH═CH 2 , or —C≡CH.

4. The compound of claim 2 , wherein R 11 is hydrogen or methyl.

5. The compound of claim 2 , wherein m is 2 and the second R 8 is hydrogen.

6. The compound of claim 2 , wherein R 9 is hydrogen, NH 2 , or methyl.

7. The compound of claim 1 , wherein said optionally substituted C3-C4 heterocycle is an optionally substituted C4 heterocycle.

8. A compound having the structure of Formula VIII:

wherein b is 0 or 1 and c is 0;

Q1 is

R9 is hydrogen, deuterium, halo, NH2, optionally substituted C1-C3 alkyl; and

R10 and R11 are, independently, hydrogen, deuterium, optionally substituted C1-C4 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, or a pharmaceutically acceptable salt thereof.

9. The compound of claim 1 , wherein R10 is hydrogen or optionally substituted C1-C4 alkyl.

10. The compound of claim 9 , wherein R10 is hydrogen or methyl.

11. The compound of claim 1 , wherein R11 is hydrogen.

12. The compound of claim 1 , wherein R9 is hydrogen, halo, hydroxyl, NH2, optionally substituted C1-C3 alkyl.

13. The compound of claim 12 , wherein R9 is hydrogen, fluoro, hydroxyl, NH2, or methyl.

14. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

15. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

16. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable excipient.

Assignments (2)
CHANGE OF NAME Recorded Sep 17, 2021
From: RGENIX, INC.
To: INSPIRNA, INC.
Reel/Frame 057537/0973 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 30, 2018
From: MARTINEZ, EDUARDO J.; TAVAZOIE, SOHAIL F.
To: RGENIX, INC.
Reel/Frame 045669/0645 →
Continuity (2)
Provisional Application 61986723 · Apr 30, 2014
Related Publication 20170050924A1 · Feb 23, 2017