IP Library Granted Patent US 11,420,929
Granted Patent B2
US 11,420,929 · App. 17/196,873 · Granted Aug 23, 2022

Phenoxy acetic acids and phenyl propionic acids as PPAR delta agonists

Inventors: Per Sauerberg (Farum, DK); Pavel Pihera (Prague, CZ); Zdenek Polivka (Prague, CZ); Miroslav Havranek (Prague, CZ); Ingrid Pettersson (Frederiksberg, DK); John Patrick Mogensen (Herlev, DK)
Assignee: VTV THERAPEUTICS LLC
C07C69/736A61K31/192A61K31/195A61K31/343A61K31/381A61K31/40A61K31/4025A61K31/415A61K31/4402A61K31/445A61K31/495A61K31/5375A61K31/5377C07C59/70C07C217/48C07C323/16C07C323/32C07D211/46C07D213/30C07D213/36C07D231/12C07D265/30C07D295/096C07D295/112C07D307/79C07D307/81C07D333/16C07D333/20C07D333/54C07C2601/02
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Quick Facts
Patent No.
US 11,420,929
App. No.
17/196,873
Granted
Aug 23, 2022
Kind
B2
Abstract

Phenoxy acetic acids and phenyl propionic acids and their use in improving mitochondrial energy output in a subject are provided herein. The present compounds are activators of PPARδ and may be useful for treating conditions mediated by the same.

Claims (18)

1. A process for the preparation of a compound of the following formula:

or a pharmaceutically acceptable salt thereof,

comprising saponification of a compound of formula (I):

or a salt thereof, wherein:

is a double bond, with either E or Z substitution;

X 1 is C 1-6 alkyl substituted with morpholino;

X 2 is phenylene;

X 3 is phenyl substituted with one or more halogens;

Ar is phenylene optionally substituted with methyl;

Y 1 is O;

Y 2 is O;

Z is CH 2 ;

R 1 is hydrogen; and

R 2 is C 1-6 alkyl.

2. The process of claim 1 , wherein X 1 is morpholin-4-ylmethyl.

3. The process of claim 2 , wherein R 2 is methyl or ethyl.

4. The process of claim 1 , wherein the compound of formula (I) is methyl (Z)-[4-[3-(4-fluorophenyl)-3-[4-[3-(morpholin-4-yl) propynyl]phenyl]allyloxy]-2-methylphenoxy]acetate, or a salt thereof.

5. The process of claim 1 , wherein the compound of formula (I) is methyl (E)-[4-[3-(4-fluorophenyl)-3-[4-[3-(morpholin-4-yl) propynyl]phenyl]allyloxy]-2-methylphenoxy]acetate, or a salt thereof.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 9, 2021
From: TRANSTECH PHARMA, INC.
To: HIGH POINT PHARMACEUTICALS, LLC
Reel/Frame 055540/0704 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 9, 2021
From: NOVO NORDISK A/S
To: TRANSTECH PHARMA, INC.
Reel/Frame 055540/0711 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 9, 2021
From: TRANSTECH PHARMA, INC.
To: HIGH POINT PHARMACEUTICALS, LLC
Reel/Frame 055540/0727 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 9, 2021
From: VTVX HOLDINGS II LLC
To: VTV THERAPEUTICS LLC
Reel/Frame 055540/0733 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 9, 2021
From: SAUERBERG, PER; PIHERA, PAVEL; POLIVKA, ZDENEK; HAVRANEK, MIROSLAV; PETTERSSON, INGRID; MOGENSEN, JOHN PATRICK
To: TRANSTECH PHARMA, INC.
Reel/Frame 055542/0490 →
CHANGE OF NAME Recorded Mar 9, 2021
From: HIGH POINT PHARMACEUTICALS, LLC
To: VTVX HOLDINGS II LLC
Reel/Frame 055543/0526 →
Priority Claims (2)
EP 05112758 · Dec 22, 2005 · regional
EP 06115631 · Jun 19, 2006 · regional
Continuity (9)
Continuation 16679026 · Nov 8, 2019
Continuation 15817470 · Nov 20, 2017
Continuation 15490205 · Apr 18, 2017
Continuation 14016442 · Sep 3, 2013
Division 13708163 · Dec 7, 2012
Continuation 13708163 · Dec 7, 2012
Continuation 13079460 · Apr 4, 2011
Continuation 12097564
Related Publication 20210188758A1 · Jun 24, 2021