IP Library Granted Patent US 10,954,195
Granted Patent B2
US 10,954,195 · App. 16/566,659 · Granted Mar 23, 2021

Substituted triazenes protected from degradation by carboxylation of N1

Inventors: John C. Jewett (Tucson, AZ); Lindsay E. Guzman (Tucson, AZ); Bereketab T. Mehari (Tucson, AZ); Jie He (Tucson, AZ)
Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
C07D233/88C07D233/60
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Quick Facts
Patent No.
US 10,954,195
App. No.
16/566,659
Granted
Mar 23, 2021
Kind
B2
Abstract

Triazabutadiene molecules, such as those according to Formula B, which can yield aryl diazonium species, and methods of use of triazabutadiene molecules, for example methods and compositions for yielding an aryl diazonium species from a triazabutadiene molecule, e.g., a protected aryl diazonium species in the form of a triazabutadiene. In some embodiments, an enzyme catalyzes the reaction yielding the aryl diazonium species from the triazabutadiene molecule. As an example, the methods and compositions herein may be used for delivery of drugs.

Claims (30)

1. A compound of Formula B:

wherein:

A is —N—;

D is H;

E is H;

X 1 is alkyl or aryl, wherein the alkyl is optionally substituted with one or more substituents independently selected from the group consisting of C(O)OH, NH 2 , and OH, and further wherein the aryl is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, C(O)OH, NH 2 , and OH;

Y 1 is alkyl or aryl, wherein the alkyl is optionally substituted with one or more substituents independently selected from the group consisting of C(O)OH, NH 2 , and OH, and further wherein the aryl is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, C(O)OH, NH 2 , and OH;

Z 1 is aryl, wherein the aryl is optionally substituted with a substituent selected from the group consisting of NO 2 , C 1-6 alkyl, C 1-6 haloalkyl, C(O)OH, C(O)OC 1-6 alkyl, and OC 1-6 alkyl; and

Z 2 is C(O)OC 1-16 alkyl, wherein the C 1-16 alkyl is optionally substituted with a substituent selected from the group consisting of heterocyclyl and aryl, and further wherein the heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of oxo, NO 2 , C(O)O − , NHC(O)CH 2 Ph, and OC 1-6 alkyl, and the aryl is optionally substituted with one or more substituents independently selected from the group consisting of NO 2 , C(O)O − , NHC(O)CH 2 Ph, OC 1-6 alkyl, and OC(O)alkyl.

2. A compound of Formula B:

wherein:

A is —N—;

D is H;

E is H;

X 1 is alkyl or aryl, wherein the alkyl is optionally substituted with one or more substituents independently selected from the group consisting of C(O)OH, NH 2 , and OH, and further wherein the aryl is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, C(O)OH, NH 2 , and OH;

Y 1 is alkyl or aryl, wherein the alkyl is optionally substituted with one or more substituents independently selected from the group consisting of C(O)OH, NH 2 , and OH, and further wherein the aryl is optionally substituted with one or more substituents independently selected from the group consisting of alkyl, C(O)OH, NH 2 , and OH;

Z 1 is aryl, wherein the aryl is optionally substituted with a substituent selected from the group consisting of NO 2 , C 1-6 alkyl, C 1-6 haloalkyl, C(O)OH, C(O)OC 1-6 alkyl, and OC 1-6 alkyl; and

Z 2 is C(O)OC 1-6 alkyl, wherein the C 1-6 alkyl is optionally substituted with a substituent selected from the group consisting of heterocyclyl and aryl, and further wherein the heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of oxo, NO 2 , C(O)O − , NHC(O)CH 2 Ph, and OC 1-6 alkyl, and the aryl is optionally substituted with one or more substituents independently selected from the group consisting of NO 2 , C(O)O − , NHC(O)CH 2 Ph, OC 1-6 alkyl, and OC(O)alkyl.

3. The compound of claim 2 , wherein X 1 is CH 3 .

4. The compound of claim 2 , wherein Y 1 is CH 3 .

5. The compound of claim 2 , wherein Y 1 is C(CH 3 ) 3 .

6. The compound of claim 2 , wherein:

X 1 is alkyl; and

Y 1 is alkyl.

7. The compound of claim 2 , wherein:

X 1 is CH 3 ; and

Y 1 is CH 3 .

8. The compound of claim 2 , wherein:

X 1 is C(CH 3 ) 3 ; and

Y 1 is C(CH 3 ) 3 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 8, 2020
From: JEWETT, JOHN C.; GUZMAN, LINDSAY E.; MEHARI, BEREKETAB T.; HE, JIE
To: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
Reel/Frame 054574/0523 →
CONFIRMATORY LICENSE Recorded Oct 11, 2019
From: UNIVERSITY OF ARIZONA
To: NATIONAL SCIENCE FOUNDATION
Reel/Frame 050714/0335 →
Continuity (6)
Continuation In Part PCTUS2018022046 · Mar 12, 2018
Continuation In Part 15751555
Provisional Application 62469677 · Mar 10, 2017
Provisional Application 62203667 · Aug 11, 2015
Provisional Application 62203725 · Aug 11, 2015
Related Publication 20200002290A1 · Jan 2, 2020