US2019119204A1PendingUtilityA1
ROR GAMMA (RORy) MODULATORS
Est. expiryDec 5, 2036(~10.4 yrs left)· nominal 20-yr term from priority
Inventors:Joseph Maria Gerardus Barbara CalsDavid MachnikSander Bernardus NabuursJean-Francois Sabuco
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
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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-modified1 - 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.Cited by (0)
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