US2021188836A1PendingUtilityA1
6-AMINOPYRIDIN-3-YL THIAZOLES AS MODULATORS OF RORyT
Est. expiryApr 27, 2036(~9.7 yrs left)· nominal 20-yr term from priority
Inventors:Steven GoldbergKelly J. McclureVirginia M. TanisElizabeth G. FennemaAlec D. LebsackConnor L. MartinHariharan VenkatesanXiaohua XueCraig R. Woods
C07D 417/14C07D 417/04C07D 491/107C07D 487/08A61P 1/04A61P 3/00A61P 19/02C07D 491/08C07D 498/08C07B 59/002C07B 2200/05A61P 25/00A61K 31/4439A61P 37/00A61P 11/00A61P 29/00A61P 11/06A61P 37/02A61P 17/06A61P 43/00A61P 25/24
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Claims
Abstract
The present invention comprises compounds of Formula I.wherein:A1, A2, A3, A4, A5, R1, and R2 are defined in the specification.The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
Claims
exact text as granted — not AI-modifiedWe claim:
1 . A compound of Formula I.
wherein
R 1 is H, —C (1-3) alkyl, —CHF 2 , —CF 3 , —CN, —OCH 3 , —OCH2CH 3 , cyclopropyl, OCF 3 , or OCHF 2 ;
R 2 is H, F, —CHF 2 , —CF 3 , —CN, —OCH 3 , —OCHF 2 , or OCF3; provided that R 2 may not be H if 1e is H;
A l and A 2 are taken together with their attached nitrogen to form a ring selected from the group consisting of
or A 3 may be —CH 2 C(CH 3 ) 2 OH, when A 1 and A 2 are
A 4 is —H, or —CH 3 ;
or A 3 and A 4 may be taken together with their attached nitrogen to form a ring selected from the group consisting of
A 5 is
wherein said —C (1-6) alkyl and —C (4-6) cycloalkyl are optionally substituted with up to three fluorine atoms; and said —C (1-6) alkyl is independently optionally substituted with one cyclobutyl, or up to two cyclopropyl groups;
and pharmaceutically acceptable salts thereof.
2 . The compound of claim 1 wherein:
A 5 is
wherein said —C (3-6) alkyl and —C (4-6) cycloalkyl are optionally substituted with up to three fluorine atoms;
and pharmaceutically acceptable salts thereof.
3 . The compound of claim 2 wherein:
R 1 is H, —C (1-3) alkyl, —CHF 2 , —CF 3 , —CN, —OCH 3 , —OCH 2 CH 3 , or cyclopropyl;
R 2 is H, F, —CHF 2 , —CF 3 , —CN, —OCH 3 , or —OCHF2; provided that R 2 may not be H if R 1 is H;
and pharmaceutically acceptable salts thereof.
4 . The compound of claim 3 wherein:
A 3 and A 4 may be taken together with their attached nitrogen to form a ring selected from the group consisting of
and pharmaceutically acceptable salts thereof.
5 . The compound of claim 4 wherein:
A 1 and A 2 are taken together with their attached nitrogen to form a ring selected from the group consisting of
and pharmaceutically acceptable salts thereof.
6 . The compound of claim 3 selected from the group consisting of:
and pharmaceutically acceptable salts thereof.
7 . The compound of claim 3 selected from the group consisting of:
and pharmaceutically acceptable salts thereof.
8 . The compound of claim 4 selected from the group consisting of:
and pharmaceutically acceptable salts thereof.
9 . The compound of claim 5 selected from the group consisting of:
and pharmaceutically acceptable salts thereof.
10 . A pharmaceutical composition, comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
11 . A method for treating or ameliorating a RORγt mediated inflammatory syndrome, disorder or disease selected from the group consisting of: inflammatory bowel diseases, rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disorder, psoriatic arthritis, ankylosing spondylitis, neutrophilic asthma, steroid resistant asthma, multiple sclerosis, and systemic lupus erythematosus, comprising administering to a subject in need thereof an effective amount of a compound of claim 1 .
12 . A method for treating or ameliorating a RORγt mediated inflammatory syndrome, disorder or disease selected from the group consisting of: depression and metabolic syndrome, comprising administering to a subject in need thereof an effective amount of a compound of claim 1 .
13 . The method of claim 11 , wherein the disease is psoriasis.
14 . The method of claim 11 , wherein the disease is rheumatoid arthritis.
15 . The method of claim 11 , wherein the inflammatory bowel disease is ulcerative colitis.
16 . The method of claim 11 , wherein the inflammatory bowel disease is Crohn's disease.
17 . The method of claim 11 , wherein the disease is multiple sclerosis.
18 . The method of claim 11 , wherein the disease is neutrophilic asthma.
19 . The method of claim 11 , wherein the disease is steroid resistant asthma.
20 . The method of claim 11 , wherein the disease is psoriatic arthritis.
21 . The method of claim 11 , wherein the disease is ankylosing spondylitis.
22 . The method of claim 11 , wherein the disease is systemic lupus erythematosus.
23 . The method of claim 11 , wherein the disease is chronic obstructive pulmonary disorder.
24 . The method of claim 12 , wherein the disease is depression.
25 . The method of claim 12 , wherein the disease is metabolic syndrome.
26 . A method of inhibiting production of interleukin-17, comprising administering to a subject in need thereof an effective amount of a compound of claim 1 .Join the waitlist — get patent alerts
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