IP Library Granted Patent US 12686667
Granted Patent B2
US 12686667 · App. 17/537,266 · Granted Jul 21, 2026

Methods and compositions for gamma-glutamyl cycle modulation

Inventors: David Rubin (San Diego, CA); Eyal Rubin (San Diego, CA)
Assignee: CANCER RESEARCH TECHNOLOGIES LLC
C07D277/06A61K31/426C07D277/04C07B2200/13
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Quick Facts
Patent No.
US 12686667
App. No.
17/537,266
Granted
Jul 21, 2026
Kind
B2
Abstract

The present disclosure provides pharmaceutical compositions comprising Gamma-glutamyl cycle inhibitors (GGCI) and certain pharmaceutically acceptable salts thereof, and methods of use.

Claims (32)

1 . A compound represented by formula (I):

or a pharmaceutically acceptable salt thereof, wherein:

R is independently selected from optionally substituted aryl, heteroaryl, para- methoxyphenyl, ortho-hydroxy phenyl, and phenyl;

R 2 is COOH;

R 3 and R 4 are each independently selected from methyl, ethyl, and propyl; and

* is independently selected from selenium and tellurium.

2 . A pharmaceutical composition consisting essentially of a stereoisomeric compound, or salt thereof, of claim 1 , and a pharmaceutically acceptable excipient,

wherein the pharmaceutically acceptable excipient is selected from sterile saline, buffers, antioxidants, preservatives, alkyl parabens, sugars, and non-ionic surfactants.

3 . A composition for selectively inhibiting the synthesis of glutamic acid in the gamma-glutamyl cycle in tumor cells, comprising a therapeutically effective amount of a compound of claim 1 .

4 . The compound of claim 1 or a pharmaceuitcally acceptable salt thereof, wherein R 3 and R 4 are each methyl.

5 . A pharmaceutical composition consisting essentially of a stereoisomeric compound of claim 4 or a pharmaceutically acceptable salt thereof,

and comprising a pharmaceutically acceptable excipient;

wherein the pharmaceutically acceptable excipient is selected from sterile saline, buffers, antioxidants, preservatives, alkyl parabens, hydrophilic polymers, sugars, and non-ionic surfactants.

6 . The pharmaceutical composition of claim 5 , wherein the composition is in a form selected from: tablets, capsules, solutions and suspensions.

7 . The pharmaceutical composition of claim 5 , wherein the buffer is selected from: phosphate, citrate, ascorbate, and Ringer's solution.

8 . A pharmaceutical composition consisting essentially of a stereoisomeric compound represented by formula (I):

or a pharmaceutically acceptable salt thereof, wherein:

R is independently selected from optionally substituted aryl, heteroaryl, para- methoxyphenyl, ortho-hydroxy phenyl, and phenyl;

R 2 is COOH;

R 3 and R 4 are each independently selected from methyl, ethyl, and propyl; and

* is independently selected from sulfur, selenium and tellurium;

and a pharmaceutically acceptable excipient, wherein the pharmaceutically acceptable excipient is:

selected from an antioxidant selected from ascorbic acid and methionine;

a preservative selected from octadecyldimethylbenzyl ammonium chloride, hexamethonium chloride, benzalkonium chloride, benzethonium chloride, phenol, butyl alcohol, and benzyl alcohol;

an alkyl paraben selected from methyl paraben and propyl paraben;

a sugar selected from: glucose, mannose, sucrose, mannitol, trehalose, sorbitol, and dextrin; or

a non-ionic surfactant selected from: Tween (Polyoxyethylene (20) sorbitan monolaurate), Pluronic (poly (ethylene oxide)-co-(poly (propylene oxide))), and polyethylene glycol.

9 . The pharmaceutical composition of claim 5 , wherein the hydrophilic polymer is polyvinylpyrrolidone.

10 . The pharmaceutical composition of claim 5 , wherein the pharmaceutically acceptable salt is selected from: sulfate, citrate, acetate, oxalate, chloride, bromide, iodide, nitrate, bisulfate, phosphate, acid phosphate, isonicotinate, lactate, salicylate, tartrate, oleate, tannate, pantothenate, bitartrate, ascorbate, succinate, maleate, gentisinate, fumarate, fluconate, glucuronate, saccharate, formate, benzoate, glutamate, methanesulfonate “mesylate”, ethansulfonate, benzenesulfonate, p-toluenesulfonate, and pamoate, which is 1′-methylene-bis(2-hydroxy-3-napthoate).

11 . A pharmaceutical composition consisting essentially of a stereoisomeric compound of claim 1 and an anti-hormonal agent.

12 . The pharmaceutical composition of claim 11 , wherein the anti-hormonal agent is selected from: anti-estrogens and selective estrogen receptor modulators.

13 . The pharmaceutical composition of claim 12 , wherein the anti-hormonal agent is selected from: tamoxifen, tamoxifen citrate, raloxifene, droloxifene, 4-hydroxytamoxifen, trioxifene, keoxifene, LY117018, onapristone, and toremifene citrate.