IP Library › Granted Patent US 9,714,236
Granted Patent B2
US 9,714,236 · App. 15/272,554 · Granted Jul 25, 2017

Compounds and methods for inhibiting JAK

Inventors: Neil Grimster (Waltham, MA); Sameer Kawatkar (Waltham, MA); Jason Grant Kettle (Macclesfield, GB); Qibin Su (Waltham, MA); Melissa Vasbinder (Waltham, MA); Claudio Edmundo Chuaqui (Waltham, MA)
Assignee: ASTRAZENECA AB
C07D403/14
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Quick Facts
Patent No.
US 9,714,236
App. No.
15/272,554
Granted
Jul 25, 2017
Kind
B2
Abstract

Disclosed are compounds of formula (I), pharmaceutical compositions comprising such compounds and methods/uses of using the same, for example, for treating a JAK-related disorder, such as cancer, cancer cachexia or an immune disorder: wherein R 1 is methyl or ethyl; R 2 is selected from methyl, ethyl, methoxy and ethoxy; R 3 is selected from hydrogen, chlorine, fluorine, bromine and methyl; R 4 is selected from methyl, ethyl and —CH 2 OCH 3 ; R 5 and R 6 are each individually methyl or hydrogen; and R 7 is selected from methyl, ethyl, —(CH 2 ) 2 OH and —(CH 2 ) 2 OCH 3 , or a pharmaceutically acceptable salt thereof.

Claims (5)

1. A compound which is (2R)—N-(3-{2-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]pyrimidin-4-yl}-1H-indol-7-yl)-2-(4-methylpiperazin-1-yl)propanamide, or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , which is (2R)—N-(3-{2-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]pyrimidin-4-yl}-1H-indol-7-yl)-2-(4-methylpiperazin-1-yl)propanamide.

3. The compound of claim 1 , which is a pharmaceutically acceptable salt of (2R)—N-(3-{2-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]pyrimidin-4-yl}-1H-indol-7-yl)-2-(4-methylpiperazin-1-yl)propanamide.

4. A solid form of (2R)—N-(3-{2-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]pyrimidin-4-yl}-1H-indol-7-yl)-2-(4-methylpiperazin-1-yl)propanamide, or a pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition comprising a compound of any one of claims 1 - 3 , and a pharmaceutically acceptable diluent, excipient or carrier.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 16, 2017
From: ASTRAZENECA AB
To: DIZAL (JIANGSU) PHARMACEUTICAL CO., LTD.
Reel/Frame 044149/0172 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 17, 2017
From: CHUAQUI, CLAUDIO EDMUNDO; VASBINDER, MELISSA MARIE; GRIMSTER, NEIL PATRICK; KAWATKAR, SAMEER; SU, QIBIN; WU, DEDONG; YANG, WENZHAN; WOESSNER, RICHARD DONALD
To: ASTRAZENECA PHARMACEUTICALS LP
Reel/Frame 041605/0363 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 17, 2017
From: ASTRAZENECA PHARMACEUTICALS LP
To: ASTRAZENECA UK LIMITED
Reel/Frame 041605/0542 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 17, 2017
From: ASTRAND, ANNIKA BIRGITTA MARGARETA; NILSSON, MAGNUS K
To: ASTRAZENECA AB
Reel/Frame 041605/0786 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 17, 2017
From: ASTRAZENECA UK LIMITED
To: ASTRAZENECA AB
Reel/Frame 041605/0915 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 17, 2017
From: KETTLE, JASON GRANT; RUSTON, LINETTE; WINTER-HOLT, JON JAMES; GRECU, TUDOR; MCCABE, JAMES
To: ASTRAZENECA UK LIMITED
Reel/Frame 042039/0074 →
Continuity (2)
Provisional Application 62232629 · Sep 25, 2015
Related Publication 20170088543A1 · Mar 30, 2017