US2019119204A1PendingUtilityA1

ROR GAMMA (RORy) MODULATORS

66
Assignee: LEAD PHARMA HOLDING BVPriority: Dec 5, 2016Filed: Dec 19, 2018Published: Apr 25, 2019
Est. expiryDec 5, 2036(~10.4 yrs left)· nominal 20-yr term from priority
C07C 2601/02A61P 17/00C07C 315/04C07C 317/46C07C 317/44A61P 25/00A61K 31/10A61K 31/167A61P 1/00A61P 19/02C07C 317/32A61K 45/00A61P 29/00A61K 45/06C07C 317/50A61P 17/06Y02A50/30
66
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Claims

Abstract

The compounds can be used as inhibitors of RORγ and are useful for the treatment of RORγ mediated diseases.

Claims

exact text as granted — not AI-modified
1 - 13 . (canceled) 
     
     
         14 . A compound having the absolute configuration corresponding to Formula (IA), 2-}4-[(cyclopropylmethyl)sulfonyl]phenyl}-N-{4-[(1R)-1-(difluoromethyl)-2,2,2-trifluoro-1-hydroxyethyl]phenyl}acetamide: 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         15 . A process of preparing the compound of Formula (IA) according to  claim 14  comprising:
 i) reacting an amine of formula (II) 
 
       
         
           
           
               
               
           
         
       
       with a compound of Formula (III): 
       
         
           
           
               
               
           
         
       
       to give a compound of Formula (I): 
       
         
           
           
               
               
           
         
       
       and
 ii) obtaining the compound of Formula (IA) by chiral separation. 
 
     
     
         16 . A method of therapeutically treating at least one condition selected from the group consisting of ROR-γ mediated autoimmune diseases, ROR-γ mediated inflammatory diseases and ROR-γ mediated infectious diseases, comprising administering an effective amount of a compound having the absolute configuration corresponding to Formula (IA), or a pharmaceutically acceptable salt thereof, to a person in need of a therapeutic treatment, wherein the compound of Formula (IA) is 2-{4-[(cyclopropylmethyl)sulfonyl]phenyl}-N-{4-[(1R)-1-(difluoromethyl)-2,2,2-trifluoro-1-hydroxyethyl]phenyl}acetamide: 
       
         
           
           
               
               
           
         
       
     
     
         17 . The method according to  claim 16 , wherein the at least one condition is selected from the group consisting of rheumatoid arthritis, psoriasis, inflammatory bowel disease, Crohn's disease and multiple sclerosis. 
     
     
         18 . The method according to  claim 16 , wherein the at least one condition is selected from the group consisting of osteoarthritis and asthma. 
     
     
         19 . The method according to  claim 16 , wherein the at least one condition is mucosal leishmaniasis. 
     
     
         20 . A method of prophylactically treating at least one condition selected from the group consisting of ROR-γ mediated autoimmune diseases, ROR-γ mediated inflammatory diseases and ROR-γ mediated infectious diseases, comprising administering an effective amount of a compound having the absolute configuration corresponding to Formula (IA), or a pharmaceutically acceptable salt thereof, to a patient, wherein the compound of Formula (IA) is 2-{4-[(cyclopropylmethyl)sulfonyl]phenyl}-N-{4-[(1R)-1-(difluoromethyl)-2,2,2-trifluoro-1-hydroxyethyl]phenyl}acetamide: 
       
         
           
           
               
               
           
         
       
     
     
         21 . The method according to  claim 20 , wherein the at least one condition is selected from the group consisting of rheumatoid arthritis, psoriasis, inflammatory bowel disease, Crohn's disease and multiple sclerosis. 
     
     
         22 . The method according to  claim 20 , wherein the at least one condition is selected from the group consisting of osteoarthritis and asthma. 
     
     
         23 . The method according to  claim 20 , wherein the at least one condition is mucosal leishmaniasis. 
     
     
         24 . A method of therapeutically treating at least one condition selected from the group consisting of Kawaski disease and Hashimoto's thyroiditis, comprising administering an effective amount of a compound having the absolute configuration corresponding to Formula (IA), or a pharmaceutically acceptable salt thereof, to a person in need of a therapeutic treatment, wherein the compound of Formula (IA) is 2-{4-[(cyclopropylmethyl)sulfonyl]phenyl}-N-{4-[(1R)-1-(difluoromethyl)-2,2,2-trifluoro-1-hydroxyethyl]phenyl}acetamide: 
       
         
           
           
               
               
           
         
       
     
     
         25 . A method of prophylactically treating at least one condition selected from the group consisting of Kawaski disease and Hashimoto's thyroiditis, comprising administering an effective amount of a compound having the absolute configuration corresponding to Formula (IA), or a pharmaceutically acceptable salt thereof, to a patient, wherein the compound of Formula (IA) is 2-{4-[(cyclopropylmethyl)sulfonyl]phenyl}-N-{4-[(1R)-1-(difluoromethyl)-2,2,2-trifluoro-1-hydroxyethyl]phenyl}acetamide: 
       
         
           
           
               
               
           
         
       
     
     
         26 . A pharmaceutical composition comprising the compound according to  claim 14 , or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable excipients.

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