Evangelos N Moudrianakis from 3415 Guilford Ter, Baltimore, MD 21218, age 85, Phone: 4104678420

Heterocyclic And Carbonate Derivatives Of Ndga And Their Use As New Anti-Hiv And Anti-Cancer Agents
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US Patent:

8420692, Apr 16, 2013
Filed:

Apr 6, 2010
Appl. No.:

12/755077
Inventors:

Ru Chih C. Huang - Baltimore MD, US
Apostolos Gittis - Baltimore MD, US
Evangelos Moudrianakis - Baltimore MD, US
Julie A. Dohm - Oak Lawn IL, US
Jih Ru Hwu - Hsinchu, TW
Ming-Hua Hsu - Hsinchu, TW
Assignee:

The Johns Hopkins University - Baltimore MD
International Classification:

A01N 43/36
A61K 31/40
US Classification:

514408, 5142312, 514315
Abstract:

Reaction of nordihydroguaiaretic acid with various alkyl chlorides, 1-piperidinecarbonyl chloride, methyl chloroformate, or 1,1′-carbonyldiimidazole under alkaline conditions produced the corresponding phenol ethers, carbamates and carbonates, respectively, in 67-83% yields (Scheme 1 and Scheme 2). Among these derivatives, the nitrogen-containing compounds were converted to the corresponding hydrochloride salts. Having good solubility, these NDGA derivatives were found to be stable in aqueous solution. These new compounds exerted potent activities against HIV Tat-regulated transactivation in cos-7 cells. The most active transcription inhibitor compound of this series 5b (PN, Tetrapiperidino NDGA, meso-2,3-dimethyl-1,4-bis(3,4-[2-(piperidino)ethoxypehnyl])butane tetrakishydrochloride salt) has an ICof 0. 88 μ.

Heterocyclic And Carbonate Derivatives Of Ndga And Their Use As New Anti-Hiv And Anti-Cancer Agents
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US Patent:

7741357, Jun 22, 2010
Filed:

Apr 13, 2007
Appl. No.:

11/783970
Inventors:

Ru Chih C. Huang - Baltimore MD, US
Apostolos Gittis - Baltimore MD, US
Evangelos Moudrianakis - Baltimore MD, US
Julie A. Dohm - Oak Lawn IL, US
Jih Ru Hwu - Hsinchu, TW
Ming-Hua Hsu - Hsinchu, TW
Assignee:

Johns Hopkins University - Baltimore MD
International Classification:

A01N 43/36
US Classification:

514408, 5142312, 514315, 548400, 548560, 544106, 546184
Abstract:

Reaction of nordihydroguaiaretic acid with various alkyl chlorides, 1-piperidinecarbonyl chloride, methyl chloroformate, or 1,1′-carbonyldiimidazole under alkaline conditions produced the corresponding phenol ethers, carbamates and carbonates, respectively, in 67-83% yields (Scheme 1 and Scheme 2). Among these derivatives, the nitrogen-containing compounds were converted to the corresponding hydrochloride salts. Having good solubility, these NDGA derivatives were found to be stable in aqueous solution. These new compounds exerted potent activities against HIV Tat-regulated transactivation in cos-7 cells. The most active transcription inhibitor compound of this series 5b (PN, Tetrapiperidino NDGA, meso-2,3-dimethyl-1,4-bis(3,4-[2-(piperidino)ethoxyphenyl])butane tetrakishydrochloride salt) has an ICof 0. 88 μ.

Evangelos N Moudrianakis