IP Library Granted Patent US 8,383,683
Granted Patent B2
US 8,383,683 · App. 12/597,129 · Granted Feb 26, 2013

Pharmaceutical use of substituted amides

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Quick Facts
Patent No.
US 8,383,683
App. No.
12/597,129
Granted
Feb 26, 2013
Kind
B2
Abstract

The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydro-genase type 1 (11βHSD1) and the use of these compounds as pharmaceutical composi-tions, are described. Also a novel class of substituted amides, their use in therapy, phar-maceutical compositions comprising the compounds, as well as their use in the manufac-ture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active gluco-corticoid is desirable.

Claims (17)

1. A compound selected from the group consisting of:

N-cyclopropyl-4-(2,4-dichloro-phenoxy)-N-(5-hydroxy-adamantan-2-yl)-butyramide;

4-(2,4-dichloro-phenoxy)-N-(5-hydroxy-adamantan-2-yl)-butyramide;

4-(2,4-dichloro-phenoxy)-N-(5-hydroxy-adamantan-2-yl)-N-methyl-butyramide;

4-(2,4-dichloro-phenoxy)-N-ethyl-N-(5-hydroxy-adamantan-2-yl)-butyramide;

4-(2,4-dichloro-phenoxy)-N-(5-hydroxy-methyl-adamantan-2-yl)-butyramide;

4-(2,4-dichloro-phenoxy)-N-(5-hydroxy-adamantan-2-yl)-N-isopropyl-butyramide;

4-(2,4-dichloro-phenoxy)-N-(5-hydroxy-methyl-adamantan-2-yl)-N-methyl-butyramide;

4-(2,4-dichloro-phenoxy)-N-(5-hydroxy-adamantan-2-yl)-2,2-dimethyl-butyramide;

4-(2,4-dichloro-phenoxy)-N-(5-hydroxy-adamantan-2-yl)-2,2,N-trimethyl-butyramide;

and 4-(2,4-dichloro-phenoxy)-N-(5-hydroxy-methyl-adamantan-2-yl)-2,2-dimethyl-butyramide;

or a pharmaceutically acceptable salt thereof.

2. 4-(2,4-Dichloro-phenoxy)-N-(5-hydroxy-adamantan-2-yl)-butyramide, or a pharmaceutically acceptable salt thereof.

3. 4-(2,4-Dichloro-phenoxy)-N-(5-hydroxy-methyl-adamantan-2-yl)-butyramide, or a pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier or excipient.

5. A pharmaceutical composition comprising a compound of claim 2 and a pharmaceutically acceptable carrier or excipient.

6. A pharmaceutical composition comprising a compound of claim 3 and a pharmaceutically acceptable carrier or excipient.

Assignments (9)
CORRECTIVE ASSIGNMENT TO CORRECT THE RECEIVING PARTY DATA PREVIOUSLY RECORDED AT REEL: 036254 FRAME: 0792. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Sep 24, 2015
From: M&F TTP HOLDINGS LLC, AS COLLATERAL AGENT
To: VTVX HOLDINGS II LLC
Reel/Frame 036675/0399 →
RELEASE OF SECURITY INTEREST Recorded Aug 3, 2015
From: M&F TTP HOLDINGS LLC, AS COLLATERAL AGENT
To: VTVX HOLDINGS I LLC
Reel/Frame 036254/0792 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 31, 2015
From: VTVX HOLDINGS II LLC
To: VTV THERAPEUTICS LLC
Reel/Frame 036242/0362 →
CHANGE OF NAME Recorded Jul 30, 2015
From: HIGH POINT PHARMACEUTICALS, LLC
To: VTVX HOLDINGS II LLC
Reel/Frame 036236/0159 →
SECURITY INTEREST Recorded Feb 26, 2015
From: HIGH POINT PHARMACEUTICALS, LLC
To: M&F TTP HOLDINGS LLC, AS COLLATERAL AGENT
Reel/Frame 035103/0029 →
NOTICE OF RELEASE OF SECURITY INTEREST IN PATENTS FOR REEL/FRAME 030982/0793 Recorded Apr 7, 2014
From: M&F TTP HOLDINGS LLC
To: HIGH POINT PHARMACEUTICALS, LLC
Reel/Frame 032621/0867 →
SECURITY AGREEMENT Recorded Aug 9, 2013
From: HIGH POINT PHARMACEUTICALS, LLC
To: M&F TTP HOLDINGS LLC C/O MACANDREWS & FORBES HOLDINGS INC.
Reel/Frame 030982/0793 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 11, 2009
From: TRANSTECH PHARMA, INC.
To: HIGH POINT PHARMACEUTICALS, LLC
Reel/Frame 023502/0326 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 29, 2009
From: EBDRUP, SOREN; ANDERSEN, HENRIK SUNE
To: TRANSTECH PHARMA, INC.
Reel/Frame 023442/0982 →