IP Library Granted Patent US 8,586,590
Granted Patent B2
US 8,586,590 · App. 13/633,320 · Granted Nov 19, 2013

Compounds

Inventors: Julie Nicole Hamblin (Stevenage, GB); Paul Spencer Jones (Stevenage, GB); Suzanne Elaine Keeling (Stevenage, GB); Joelle Le (Stevenage, GB); Nigel James Parr (Stevenage, GB)
Assignee: GlaxoSmithKline Intellectual Property Development Limited
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Quick Facts
Patent No.
US 8,586,590
App. No.
13/633,320
Granted
Nov 19, 2013
Kind
B2
Abstract

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.

Claims (13)

1. A method of treating a disorder mediated by inappropriate PI3-kinase activity comprising administering a safe and effective amount of a compound which is 6-(1H-Indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole

or a pharmaceutically acceptable salt thereof, to a patient having said disorder.

2. A method of treating a disorder mediated by inappropriate PI3-kinase activity comprising administering a safe and effective amount of 6-(1H-Indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole hydrochloride to a patient having said disorder.

3. A method according to claim 1 wherein the disorder mediated by inappropriate PI3-kinase activity is a respiratory disease, a viral infection, a non-viral respiratory infection, an allergic disease, an autoimmune disease, an inflammatory disorder, a cardiovascular disease, a hematologic malignancy, a neurodegenerative disease, pancreatitis, multiorgan failure, kidney disease, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection, lung injury, or pain.

4. A method according to claim 1 wherein the disorder mediated by inappropriate PI3-kinase activity is asthma, chronic obstructive pulmonary disease (COPD), viral respiratory tract infections, viral exacerbation of respiratory diseases, aspergillosis, leishmaniasis, allergic rhinitis, atopic dermatitis, rheumatoid arthritis, multiple sclerosis, inflammatory bowel disease, thrombosis, atherosclerosis, hematologic malignancy, neurodegenerative disease, pancreatitis, multiorgan failure, kidney disease, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection, lung injury, pain associated with rheumatoid arthritis or osteoarthritis, back pain, general inflammatory pain, post hepatic neuralgia, diabetic neuropathy, inflammatory neuropathic pain (trauma), trigeminal neuralgia or Central pain.

5. A method according to claim 1 wherein the disorder mediated by inappropriate PI3-kinase activity is asthma.

6. A method according to claim 1 wherein the disorder mediated by inappropriate PI3-kinase activity is COPD.

7. A method according to claim 2 wherein the disorder mediated by inappropriate PI3-kinase activity is a respiratory disease, a viral infection, a non-viral respiratory infection, an allergic disease, an autoimmune disease, an inflammatory disorder, a cardiovascular disease, a hematologic malignancy, a neurodegenerative disease, pancreatitis, multiorgan failure, kidney disease, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection, lung injury, or pain.

8. A method according to claim 2 wherein the disorder mediated by inappropriate PI3-kinase activity is asthma, chronic obstructive pulmonary disease (COPD), viral respiratory tract infections, viral exacerbation of respiratory diseases, aspergillosis, leishmaniasis, allergic rhinitis, atopic dermatitis, rheumatoid arthritis, multiple sclerosis, inflammatory bowel disease, thrombosis, atherosclerosis, hematologic malignancy, neurodegenerative disease, pancreatitis, multiorgan failure, kidney disease, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection, lung injury, pain associated with rheumatoid arthritis or osteoarthritis, back pain, general inflammatory pain, post hepatic neuralgia, diabetic neuropathy, inflammatory neuropathic pain (trauma), trigeminal neuralgia or Central pain.

9. A method according to claim 2 wherein the disorder mediated by inappropriate PI3-kinase activity is asthma.

10. A method according to claim 2 wherein the disorder mediated by inappropriate PI3-kinase activity is COPD.

11. A method of treating a respiratory disorder comprising administering a safe and effective amount of a compound which is 6-(1H-Indol-4-yl)-4-(5-{[4-(1- methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole

or a pharmaceutically acceptable salt thereof, to a patient having said disorder, wherein the respiratory disorder is selected from the group consisting of asthma and COPD.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 31, 2014
From: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
To: GLAXO GROUP LIMITED
Reel/Frame 033452/0594 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 18, 2013
From: GLAXO GROUP LIMITED
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Reel/Frame 029821/0765 →
Continuity (3)
Division 12768777 · Apr 28, 2010
Provisional Application 61174033 · Apr 30, 2009
Related Publication 20130131080A1 · May 23, 2013