US2017157136A1PendingUtilityA1

Novel compounds

Assignee: GLAXO GROUP LTDPriority: Apr 30, 2009Filed: Feb 15, 2017Published: Jun 8, 2017
Est. expiryApr 30, 2029(~2.8 yrs left)· nominal 20-yr term from priority
A61P 3/10A61P 37/00A61P 37/06A61P 7/02A61P 43/00A61P 7/00A61P 9/00A61P 37/08A61P 9/10A61P 25/00A61P 31/10A61P 35/02A61P 25/28A61P 35/00A61P 31/04A61P 29/02A61P 25/04A61P 29/00A61P 33/02A61P 31/00A61P 31/12A61P 15/08A61P 11/00A61P 1/18A61P 11/02A61P 13/12A61P 1/00A61P 1/16A61P 17/00A61P 11/06A61P 19/02A61K 31/5375A61K 31/496A61K 31/497A61K 31/5377A61K 31/535C07D 413/14C07B 2200/13A61K 45/06Y02A50/30
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Claims

Abstract

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

Claims

exact text as granted — not AI-modified
1 - 12 . (canceled) 
     
     
         13 . A method of treating a disorder mediated by inappropriate PI3-kinase activity comprising administering a compound of formula (I): 
       
         
           
           
               
               
           
         
         wherein 
         R 1  is 9- or 10-membered bicyclic heteroaryl wherein the 9- or 10-membered bicyclic heteroaryl contains from one to three heteroatoms independently selected from oxygen and nitrogen and is optionally substituted by C 1-6 alkyl, C 3-6 cycloalkyl, halo, —CN or —NHSO 2 R 5 , or 
         pyridinyl optionally substituted by one or two substituents independently selected from C 1-6 alkyl, —OR 6 , halo and —NHSO 2 R 7 ; 
         R 2  and R 3 , together with the nitrogen atom to which they are attached, are linked to form a 6- or 7-membered heterocyclyl wherein the 6- or 7-membered heterocyclyl optionally contains an oxygen atom or a further nitrogen atom and is optionally substituted by one or two substituents independently selected from C 1-6 alkyl; 
         R 4  is hydrogen or methyl; 
         R 6  is hydrogen or C 1-4 alkyl; and 
         R 5  and R 7  are each independently C 1-6 alkyl, or phenyl optionally substituted by one or two substituents independently selected from halo; 
         or a salt thereof, to a patient having said disorder. 
       
     
     
         14 . The method according to  claim 13 , wherein R 1  is
 9-membered bicyclic heteroaryl wherein the 9-membered bicyclic heteroaryl contains one or two nitrogen atoms, or pyridinyl optionally substituted by one or two substituents independently selected from —OR 6  and —NHSO 2 R 7 .   
     
     
         15 . A method according to  claim 13 , wherein R 1  is indolyl. 
     
     
         16 . A method according to  claim 13 , wherein R 1  is pyridinyl optionally substituted by one or two substituents independently selected from —OR 6  and —NHSO 2 R 7 . 
     
     
         17 . A method according to  claim 13 , wherein R 2  and R 3 ,
 together with the nitrogen atom to which they are attached, are linked to form a 6-membered heterocyclyl wherein the 6-membered heterocyclyl optionally contains an oxygen atom or a further nitrogen atom and is optionally substituted by one or two substituents independently selected from C 1-6 alkyl.   
     
     
         18 . A method according to  claim 13 , wherein R 2  and R 3 , together with the nitrogen atom to which they are attached, are linked to form a 6-membered heterocyclyl wherein the 6-membered heterocyclyl contains an oxygen atom and is optionally substituted by one or two substituents independently selected from C 1-4 alkyl. 
     
     
         19 . A method according to  claim 13 , wherein R 2  and R 3 , together with the nitrogen atom to which they are attached, are linked to form a 6-membered heterocyclyl wherein the 6-membered heterocyclyl contains a further nitrogen atom and is optionally substituted by C 1-4 alkyl. 
     
     
         20 . A method according to  claim 13 , wherein R 4  is hydrogen. 
     
     
         21 . A method according to  claim 13  wherein the compound of formula (I) is in the form of a pharmaceutically acceptable salt thereof. 
     
     
         22 . A method according to  claim 13  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. 
     
     
         23 . A method according to  claim 13  wherein the disorder mediated by inappropriate PI3-kinase activity is asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF), 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. 
     
     
         24 . A method according to  claim 13 , wherein the disorder mediated by inappropriate PI3-kinase activity is asthma. 
     
     
         25 . A method according to  claim 13 , wherein the disorder mediated by inappropriate PI3-kinase activity is chronic obstructive pulmonary disease (COPD).

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