US2019015377A1PendingUtilityA1
Compositions for Use in Treating Pulmonary Arterial Hypertension
Est. expiryMar 11, 2035(~8.6 yrs left)· nominal 20-yr term from priority
Inventors:Darryl David DixonJonas GrinaJohn A. JoseyJames P. RizziStephen T. SchlachterEli M. WallaceBin WangPaul WehnRui XuHanbiao Yang
A61K 31/451A61K 31/275A61P 9/12A61K 2300/00A61K 31/185A61K 31/4245A61K 31/47A61K 31/10A61K 31/381A61K 31/435
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Claims
Abstract
The present disclosure provides methods of treating pulmonary arterial hypertension (PAH) in a subject in need thereof. Compositions for use in these methods are also provided.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound of Formula I:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is CR 5 ;
Y is CR 6 ;
Z is O, S, or NR B ;
R 1 is alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;
R 2 and R 3 taken together form a 5-membered heterocycle;
R 4 is nitro, halo, cyano, alkyl, fluoroalkyl, cycloalkyl, heteroaryl, carboxyl, sulfinyl, sulfonamidyl, sulfonyl, sulfoximinyl, or fluoroalkyl sulfonyl; and
R 5 , R 6 , and R 8 are independently hydrogen, halo, hydroxy, cyano, alkyl, or alkoxy.
2 . The compound of claim 1 , wherein Z is O.
3 . The compound of claim 1 , wherein R 1 is phenyl substituted with at least one substituent selected from the group consisting of halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, and cyano.
4 . The compound of claim 3 , wherein the halo is fluoro.
5 . The compound of claim 1 , wherein the 5-membered heterocycle contains an oxygen atom.
6 . The compound of claim 5 , wherein the 5-membered heterocycle is substituted with at least one substituent selected from the group consisting of halo, hydroxy, C 1 -C 4 alkoxy, alkyl, heteroalkyl, and cyano.
7 . The compound of claim 1 , wherein Z is O, R 1 is phenyl, and the 5-membered heterocycle contains an oxygen atom.
8 . The compound of claim 7 , wherein said 5-membered heterocycle is substituted with at least one substituent selected from the group consisting of halo and hydroxy.
9 . The compound of claim 8 , wherein said 5-membered heterocycle is substituted with fluoro.
10 . The compound of claim 8 , wherein R 4 is selected from the group consisting of sulfonyl, fluoroalkyl sulfonyl, fluoroalkyl, and trifluoromethyl.
11 . A compound of Formula I:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is CR 5 ;
Y is CR 6 ;
Z is O, S, or NR B ;
R 1 is alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;
R 2 and R 3 taken together form a cyclic moiety;
R 4 is cycloalkyl or heteroaryl; and
R 5 , R 6 , and R 8 are independently hydrogen, halo, hydroxy, cyano, alkyl, or alkoxy.
12 . The compound of claim 11 , wherein Z is O.
13 . The compound of claim 11 , wherein R 1 is phenyl substituted with at least one substituent selected from the group consisting of halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, and cyano.
14 . The compound of claim 13 , wherein the halo is fluoro.
15 . The compound of claim 11 , wherein R 2 and R 3 taken together form a 5- or 6-membered carbocycle with at least one sp 3 hybridized carbon.
16 . The compound of claim 15 , wherein the carbocycle is substituted with at least one substituent selected from the group consisting of halo, hydroxy, alkyl, heteroalkyl, C 1 -C 4 alkoxy, cyano, cycloalkyl, heterocycloalkyl, and oxo.
17 . The compound of claim 16 , wherein the carbocycle is substituted with at least one substituent selected from the group consisting of fluoro and hydroxy.
18 . The compound of claim 17 , wherein R 4 is heteroaryl.
19 . The compound of claim 15 , wherein the R 4 is pyrazolyl and the carbocycle is substituted with fluoro and hydroxy.
20 . The compound of claim 11 , wherein R 4 is selected from the group consisting of pyrazolyl, pyrrolyl, thiazolyl, and thiophenyl.Join the waitlist — get patent alerts
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