IP Library › Granted Patent US 10,596,174
Granted Patent B2
US 10,596,174 · App. 15/435,722 · Granted Mar 24, 2020

Pyrrolopyrimidine compounds as inhibitors of protein kinases

Inventors: Xiao Xu (San Diego, CA); Xiaobo Wang (San Diego, CA); Long Mao (San Diego, CA); Li Zhao (San Diego, CA); Biao Xi (San Diego, CA)
Assignee: ACEA THERAPEUTICS, INC.
A61K31/519A61K31/506A61K31/52A61K45/06C07D239/42C07D239/46C07D239/47C07D239/48C07D401/12C07D401/14C07D403/12C07D473/16C07D473/24C07D473/32C07D473/34C07D473/40C07D487/02C07D487/04
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Quick Facts
Patent No.
US 10,596,174
App. No.
15/435,722
Granted
Mar 24, 2020
Kind
B2
Abstract

The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways.

Claims (8)

1. A method for curative treatment of a proliferation disorder, cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, or dry eye, comprising administering to a subject in need of such treatment an effective amount of N-(3-((2-((3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the proliferation disorder is selected from the group consisting of sarcoma, epidermoid cancer, fibrosarcoma, cervical cancer, gastric carcinoma, skin cancer, leukemia, lymphoma, lung cancer, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, breast cancer, liver cancer, head and neck cancers, and pancreatic cancer.

3. The method of claim 1 , further comprising administering an effective amount of a second therapeutic agent for the curative treatment of a proliferation disorder in a subject.

4. The method of claim 1 , wherein the pharmaceutically acceptable salt is a HCl salt, a maleate salt, a HBr salt, a hydroxybutanedioic acid salt or a fumaric acid salt.

5. A method for curative treatment of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, or dry eye in a subject, comprising administering to a subject in need thereof an effective amount of a combination comprising an effective amount of N-(3-((2-((3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide or a pharmaceutically acceptable salt thereof,

and an effective amount of a second therapeutic agent for curative treatment of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease in a subject.

6. The method of claim 1 , wherein the compound inhibits EGFR, BLK, BMX/ETK, BTK, FLT3, ITK, JAK1, JAK2, JAK3, TEC, or TXK in the subject.

7. The method of claim 1 , wherein the compound inhibits BTK in the subject.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 14, 2018
From: ACEA BIOSCIENCES, INC.
To: ACEA THERAPEUTICS, INC.
Reel/Frame 047492/0140 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2017
From: XU, XIAO; WANG, XIAOBO; MAO, LONG; ZHAO, LI; XI, BIAO
To: ACEA BIOSCIENCES INC.
Reel/Frame 043264/0365 →
Continuity (6)
Division 14420341
Continuation In Part 13917514 · Jun 13, 2013
Continuation In Part 13842554 · Mar 15, 2013
Provisional Application 61814147 · Apr 19, 2013
Provisional Application 61680230 · Aug 6, 2012
Related Publication 20170224689A1 · Aug 10, 2017