IP Library Granted Patent US 9,469,650
Granted Patent B2
US 9,469,650 · App. 14/537,389 · Granted Oct 18, 2016

Melampomagnolide B derivatives

Inventors: Venumadhav Janganati (Little Rock, AR); Narsimha Reddy Penthala (Little Rock, AR); Peter A. Crooks (Little Rock, AR); Craig T. Jordan (Little Rock, AR)
Assignees: BOARD OF TRUSTEES OF THE UNIVERSITY OF ARKANSAS; UNIVERSITY OF ROCHESTER
C07D493/04
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Quick Facts
Patent No.
US 9,469,650
App. No.
14/537,389
Granted
Oct 18, 2016
Kind
B2
Abstract

The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.

Claims (15)

1. A compound comprising Formula (I) or (II):

wherein:

X is O or S;

R 1 and R 2 are independently selected from the group consisting of —OR 3 , —O-alkyl-NR 3 R 4 , —SR 3 , —S-alkyl-NR 3 R 4 , alkyl-C(O)NR 3 R 4 , and -alkyl-R 5 or when X is S, R 1 is —NR 3 R 4 ;

R 3 is selected from the group consisting of hydrocarbyl, substituted hydrocarbyl, and R 5 ;

R 4 is selected from the group consisting of hydrogen, hydrocarbyl, and substituted hydrocarbyl;

R 5 is an optionally substituted nitrogen-containing heterocyclic ring;

one or more of R 3 and R 4 may form part of a ring or ring system chosen from the group consisting of heterocyclic, substituted heterocyclic, and combinations thereof; and

when R 4 is hydrogen, R 3 is selected from the group consisting of alkyl, R 5 , and substituted hydrocarbyl having at least one hydroxyl or R 5 .

2. The compound of claim 1 , wherein R 1 and R 2 are selected from the group consisting of alkoxy, alkylamino, dialkylamino, dialkylaminoalkoxy, heterocyclylalkoxy, hydroxyalkylamino, heterocycylamino, and heterocycylalkylamino.

3. The compound of claim 2 , wherein R 1 and R 2 are selected from the group consisting of methylamino, dimethylamino, hydroxyhexylamino, hydroxyethylamino, pyrrolyl, pyrrolidinyl, pyridinyl, piperdinyl, pyrazinyl, piperazinyl, pyrimidinyl, imidazolyl, triazolyl, hydroxypiperdinyl, difluoropiperdinyl, triazolylamino, methylthiotriazolylamino, morpholinyl, morpholinylethylamino, pyridinylmethylamino, piperdinylethylamino, pyridinylethylamino, morpholinylpropylamino, imidiazolylpropylamino, methoxy, dimethylaminoethoxy, piperdinylpropoxy, piperdinylethoxy, pyrrolidinylethoxy, morpholinylethyoxy, piperidinylethoxyhydroxyethylthio, and piperdinylethyl.

4. The compound of claim 2 , wherein R 1 and R 2 are independently selected from the group consisting of imidazolylpropylaminocarbonylethylcarbonyl, difluoropiperinylcarbonylethylcarbonyl, methylthiotriazolylaminocarbonylethylcarbonyl, chloropyridinylmethylaminocarbonylethylcarbonyl, methylpiperdinylcarbonylethylcarbonyl, and methyl piperazinylcarbonylethylcarbonyl.

5. The compound of claim 1 , wherein R 1 is R 5 , and R 2 is dialkylamino.

6. The compound of claim 1 , wherein one or more R 1 , R 2 , R 3 , R 4 , or R 5 is substituted with at least one selected from the group consisting of methyl, ethyl, propyl, cyano, C 1 -C 3 -alkylamino, carboxyl, hydroxyl, trifluoromethyl, thio, alkylthio, and halogen.

7. A pharmaceutically acceptable salt comprising a compound of claim 1 .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 4, 2018
From: BOARD OF TRUSTEES OF THE UNIVERSITY OF ARKANSAS
To: BIOVENTURES, LLC
Reel/Frame 047667/0515 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 28, 2015
From: JORDAN, CRAIG T.
To: UNIVERSITY OF ROCHESTER
Reel/Frame 035736/0777 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 31, 2015
From: JANGANATI, VENUMADHAV; PENTHALA, NARSIMHA REDDY; CROOKS, PETER A.; JORDAN, CRAIG T.
To: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ARKANSAS
Reel/Frame 034859/0936 →
Continuity (2)
Provisional Application 61901714 · Nov 8, 2013
Related Publication 20150133444A1 · May 14, 2015