IP Library Granted Patent US 8,158,646
Granted Patent B2
US 8,158,646 · App. 11/394,158 · Granted Apr 17, 2012

Antifungal and antiparasitic indoloquinoline derivates

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Quick Facts
Patent No.
US 8,158,646
App. No.
11/394,158
Granted
Apr 17, 2012
Kind
B2
Abstract

An indoloquinoline wherein the quarternary N-5 atom is a straight C(1-5) chain, a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring; the 10 position is N—R 10 , O, S, S═O, CH 2 , or C═O, where R 10 is a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring. In one embodiment the quarternary N-5 atom is —CH 3 and the 10 position is N—(CH 2 ) 5 —Ph.

Claims (11)

1. A compound having the formula:

wherein:

R 5 is —CH 3 ; and

Z is N—(CH 2 ) 5 —Ph.

2. The compound of claim 1 , wherein said compound is a quaternary salt.

3. A pharmaceutical composition comprising a pharmacologically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.

4. The pharmaceutical composition of claim 3 comprising a pharmacologically antimycobacterial, antimalarial, or antifungal effective amount of a compound and a pharmaceutically acceptable carrier.

5. A method of treating a mammal in need of antimycobacterial, antimalarial, or antifungal therapy comprising administering thereto a pharmacologically effective amount of a compound of claim 1 .

6. An article of manufacture comprising packaging material and a pharmaceutical agent contained within said packaging material, wherein said pharmaceutical agent is effective for the treatment of a subject suffering from one or more of conditions of a fungal infection, a mycobacterial infection, or malaria, and wherein said packaging material comprises a label which indicates that said pharmaceutical agent can be used for ameliorating the symptoms associated with said condition and wherein said pharmaceutical agent is a compound of claim 1 .

7. The compound of claim 2 wherein said quaternary salt has the formula:

wherein: X is an anion, wherein X is I or tosylate.

Assignments (3)
CONFIRMATORY LICENSE Recorded Jun 20, 2017
From: FLORIDA AGRICULTURAL AND MECHANICAL UNIV
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 042754/0073 →
CONFIRMATORY LICENSE Recorded Jun 9, 2015
From: FLORIDA AGRICULTURAL AND MECHANICAL UNIV
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 035871/0791 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 20, 2006
From: ABLORDEPPEY, SETH Y.
To: FLORIDA AGRICULTURAL AND MECHANICAL UNIVERSITY
Reel/Frame 018002/0614 →