IP Library Granted Patent US 8,927,586
Granted Patent B2
US 8,927,586 · App. 13/780,458 · Granted Jan 6, 2015

Thromboxane A2 (TP) receptor antagonists

Inventors: John Q. Trojanowski (Philadelphia, PA); Virginia M. Y. Lee (Philadelphia, PA); Kurt R. Brunden (Media, PA); Amos B. Smith (Merion, PA); Donna M. Huym (Allentown, NJ); Carlo Ballatore (Philadelphia, PA); Anne-Marie Hogan (Mount Merrion, IE); Francesco Piscitelli (Marina di Strongoll, IT); Sugiyama Shimpei (Shizuoka, JP); Xiaozhao Wang (Drexel Hill, PA)
Assignee: The Trustees of the University of Pennsylvania
A61K31/18A61K31/196A61K31/216A61K31/357A61K31/41A61K31/4174A61K31/421A61K31/426A61K45/06C07C311/20C07D233/64C07D257/04C07D263/32C07D277/28C07D317/28
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Quick Facts
Patent No.
US 8,927,586
App. No.
13/780,458
Granted
Jan 6, 2015
Kind
B2
Abstract

The present invention relates to novel TP receptor antagonists, which optionally cross the blood-brain barrier of a mammal. The invention also provides methods for treating a disorder related to activation of TP receptor utilizing the compounds of the invention.

Claims (9)

1. A composition comprising a compound of Formula (I), or a salt or solvate thereof:

wherein:

R 1 is selected from the group consisting of

the bond between carbons 1 and 2 is either a single bond (C 1 -C 2 ) or a double bond (C 1 ═C 2 );

R 2 is selected from the group consisting of F, Cl, Br, I, and CF 3 ;

R 3 is selected from the group consisting of NR 4 , S, and O;

R 4 is selected from the group consisting of H, —(C 1 -C 6 alkyl), —(C 1 -C 6 fluoroalkyl), —(C 1 -C 6 heteroalkyl), —(C 1 -C 3 alkyl)-(C 3 -C 6 cycloalkyl), —(C 1 -C 3 alkyl)-aryl, —(C 1 -C 3 alkyl)-heteroaryl, —C(═O)R 5 , —CO 2 R 5 , and —CH(R) 2 ; and,

each occurrence of R 5 is independently selected from the group consisting of H, —(C 1 -C 6 alkyl), —(C 1 -C 6 heteroalkyl), and —(C 1 -C 3 alkyl)-(C 3 -C 6 cycloalkyl), wherein the alkyl, heteroalkyl, or cycloalkyl group is optionally substituted.

2. The composition of claim 1 , wherein the compound is selected from the group consisting of 4-chloro-N-(5-(2-(oxazol-2-yl)ethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)benzenesulfonamide, 4-chloro-N-(5-(2-(thiazol-2-yl)ethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)benzenesulfonamide, 4-chloro-N-(5-(2-(2-methylthiazol-4-yl)ethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)benzenesulfonamide, 4-chloro-N-(5-(2-(oxazol-4-yl)ethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)benzenesulfonamide, N-(5-(2-(1H-imidazol-2-yl)ethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)-4-chlorobenzenesulfonamide, N-(5-(2-(1H-imidazol-5-yl)ethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)-4-chlorobenzenesulfonamide, 4-fluoro-N-(5-(2-(thiazol-2-yl)ethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)benzenesulfonamide, a salt thereof, a solvate thereof, and any combinations thereof.

Assignments (2)
CONFIRMATORY LICENSE Recorded Jul 9, 2014
From: UNIVERSITY OF PENNSYLVANIA
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 033282/0605 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 12, 2013
From: TROJANOWSKI, JOHN Q.; LEE, VIRGINIA M.Y.; BRUNDEN, KURT R.; SMITH, AMOS B., III; HURYN, DONNA M.; BALLATORE, CARLO; HOGAN, ANNE-MARIE; PISCITELLI, FRANCESCO; SUGIYAMA, SHIMPEI; WANG, XIAOZHAO
To: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
Reel/Frame 031774/0359 →
Continuity (3)
Continuation In Part 13812793
Provisional Application 61368884 · Jul 29, 2010
Related Publication 20130165488A1 · Jun 27, 2013