Pyrrolidinyl sulfone rorgamma modulators
US-2015191483-A1 · Jul 9, 2015 · US
RORγ modulators
US9725443B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9725443-B2 |
| Application number | US-201415022673-A |
| Country | US |
| Kind code | B2 |
| Filing date | Sep 18, 2014 |
| Priority date | Sep 20, 2013 |
| Publication date | Aug 8, 2017 |
| Grant date | Aug 8, 2017 |
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Abstract
Official abstract text for this publication.
Described are RORγ modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
First claim
Opening claim text (preview).
We claim: 1. A compound which is (S)—N′-(2-(1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)acetyl)-2-hydroxy-2-methylpropanehydrazide, (S)-2-(5-((1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)-1,3,4-oxadiazol-2-yl)acetonitrile, (S,E)-1-(1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)propan-2-one O-phenyl oxime, (S,E)-1-(1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)propan-2-one O-ethyl oxime, (S,Z)-1-(1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)propan-2-one O-ethyl oxime, (S)-1,1,1,3,3,3-hexafluoro-2-(1-((4-fluorophenyl)sulfonyl)-2-((5-(methylthio)-1,3,4-thiadiazol-2-yl)methyl)-1,2,3,4-tetrahydroquinolin-6-yl)propan-2-ol, (S)-1,1,1,3,3,3-hexafluoro-2-(1-((4-fluorophenyl)sulfonyl)-2-((5-(methylsulfonyl)-1,3,4-thiadiazol-2-yl)methyl)-1,2,3,4-tetrahydroquinolin-6-yl)propan-2-ol, (S)-1,1,1,3,3,3-hexafluoro-2-(1-((4-fluorophenyl)sulfonyl)-2-((5-(2-hydroxypropan-2-yl)-1,3,4-oxadiazol-2-yl)methyl)-1,2,3,4-tetrahydroquinolin-6-yl)propan-2-ol, (S)-2-(2-((5-(2-amino-2-methylpropyl)-1,3,4-oxadiazol-2-yl)methyl)-1-((4-fluorophenyl)sulfonyl)-1,2,3,4-tetrahydroquinolin-6-yl)-1,1,1,3,3,3-hexafluoropropan-2-ol, (S)-3-amino-N′-(2-(1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)acetyl)-3-methylbutanehydrazide, (S)—N′-(2-(1-((4-fluorophenyl)sulfonyl)-6-(1, 1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)acetyl)isonicotinohydrazide, (S)-2-(2-((5-(1-aminocyclopropyl)-1,3,4-oxadiazol-2-yl)methyl)-1-((4-fluorophenyl)sulfonyl)-1,2,3,4-tetrahydroquinolin-6-yl)-1,1,1,3,3,3-hexafluoropropan-2-ol, (S)-1,1,1,3,3,3-hexafluoro-2-(1-((4-fluorophenyl)sulfonyl)-2-((5-(pyri din-4-yl)-1,3,4-oxadiazol-2-yl)methyl)-1,2,3,4-tetrahydroquinolin-6-yl)propan-2-ol, 2-(5-(((S)-1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)-1,3,4-oxadiazol-2-yl)propane-1,2-diol, 1-(3-(((S)-1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)-1H-pyrazol-1-yl)butan-2-ol, (S)-1,1,1,3,3,3-hexafluoro-2-(2-((1-((4-fluorobenzyl)-1H-pyrazol-5-yl)methyl)-1-((4-fluorophenyl)sulfonyl)-1,2,3,4-tetrahydroquinolin-6-yl)propan-2-ol, 3-(5-(((S)-1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)-1,3,4-oxadiazol-2-yl)propane-1,2-diol, 3-(5-(((S)-1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)-1H-pyrazol-1-yl)propane-1,2-diol, 3-(3-(((S)-1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)-1H-pyrazol-1-yl)propane-1,2-diol, (S)-benzyl 2-(5-((1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)-1,3,4-oxadiazol-2-yl)acetate, (S)-2-(5-((1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)-1,3,4-oxadiazol-2-yl)-N,N-dimethyl acetamide, (S)-2-(5-((1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)-1,3,4-oxadiazol-2-yl)acetamide, (S)-4-fluoro-N-((1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)benzenesulfonamide, (S)-6-chloro-N-((1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)pyridine-3-sulfonamide, (S)—N-((1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)cyclopropanesulfonamide, (S)-ethyl 2-(((1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)amino)acetate, (S)-2-(2-((benzylamino)methyl)-1-((4-fluorophenyl)sulfonyl)-1,2,3,4-tetrahydroquinolin-6-yl)-1,1,1,3,3,3-hexafluoropropan-2-ol, (±) 1-cyclopropyl-3-((1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)urea, (±) 1-((1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)-3-phenylurea, and (±) 1-benzyl-3-((1-((4-fluorophenyl)sulfonyl)-6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,2,3,4-tetrahydroquinolin-2-yl)methyl)urea, or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof. 2. A pharmaceutical composition comprising a compound, stereoisomeric form, N-oxide, or pharmaceutically acceptable salt according to claim 1 , and a pharmaceutically acceptable carrier, excipient or diluent.
Assignees
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Classifications
Immunomodulators · CPC title
Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title
Drugs for immunological or allergic disorders · CPC title
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Antineoplastic agents · CPC title
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- What does patent US9725443B2 cover?
- Described are RORγ modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and com…
- Who is the assignee on this patent?
- Bristol Myers Squibb Co
- What technology area does this patent fall under?
- Primary CPC classification C07D417/06. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Aug 08 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 1 related publication on this page (citations in our corpus or others sharing the same primary CPC).