US2021069182A1PendingUtilityA1
Ror-gamma modulators
Est. expiryOct 27, 2036(~10.3 yrs left)· nominal 20-yr term from priority
A61P 17/10A61P 17/06A61P 17/02A61P 17/00A61K 31/496C07D 401/06A61K 31/495A61Q 19/08A61P 17/08A61K 9/0014
69
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Claims
Abstract
Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing RORγ modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound having the structure of Formula (I):
wherein:
is phenyl, or a 5-membered or 6-membered heteroaryl ring;
is phenyl, or a 5-membered or 6-membered heteroaryl ring;
is phenyl, or a 5-membered or 6-membered heteroaryl ring;
X is a bond, C 1 -C 6 alkyl, or C 1 -C 6 heteroalkyl;
R 1 is —C(═O)OR 6 or —C(═O)N(R 6 ) 2 ;
each R 2 is independently halogen, C 1 -C 6 alkyl, or C 1 -C 6 alkoxy;
each R 3 , each R 4 , and each R 5 are each independently halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 heteroalkyl, —OR 7 , —N(R 7 ) 2 , —CN, —C(═O)R 8 , —C(═O)OR 7 , —C(═O)N(R 7 ) 2 , —NR 7 C(═O)R 8 , —NR 7 SO 2 R 8 , —SO 2 R 8 , or —SO 2 N(R 7 ) 2 ;
each R 6 is independently hydrogen, C 1 -C 6 alkyl, or —C 1 -C 6 alkyl-Y—R 9 ;
each Y is independently —O—, —S—, or —N(R 10 )—;
each R 7 is independently hydrogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, or C 1 -C 6 heteroalkyl;
each R 8 is independently C 1 -C 6 alkyl or C 1 -C 6 heteroalkyl;
each R 9 is independently hydrogen or C 1 -C 6 alkyl;
each R 10 is independently hydrogen or C 1 -C 6 alkyl;
m is 0, 1, 2, 3, or 4;
n is 0, 1, 2, 3, or 4;
p is 0, 1, 2, 3, or 4; and
q is 0, 1, 2, or 3;
or a pharmaceutically acceptable salt or solvate thereof.
2 . The compound of claim 1 wherein
is phenyl or a 6-membered heteroaryl ring.
3 . The compound of claim 2 wherein
is phenyl.
4 . The compound of claim 2 wherein
is a 6-membered heteroaryl ring.
5 . The compound of claim 4 wherein
is pyridyl.
6 . The compound of any one of claims 1 - 5 wherein
is phenyl or a 6-membered heteroaryl ring.
7 . The compound of any one of claims 1 - 5 wherein
is phenyl.
8 . The compound of any one of claims 1 - 5 wherein
is a 6-membered heteroaryl ring.
9 . The compound of any one of claims 1 - 5 wherein
is pyridyl.
10 . The compound of any one of claims 1 - 9 wherein
is phenyl or a 6-membered heteroaryl ring.
11 . The compound of any one of claims 1 - 9 wherein
is phenyl.
12 . The compound of any one of claims 1 - 9 wherein
is a 6-membered heteroaryl ring.
13 . The compound of any one of claims 1 - 9 wherein
is pyridyl.
14 . The compound of claim 1 having the structure of Formula (Ia):
15 . The compound of any one of claims 1 - 14 wherein R 1 is —C(═O)OR 6 .
16 . The compound of claim 15 wherein R 6 is C 1 -C 6 alkyl.
17 . The compound of claim 16 wherein R 1 is —C(═O)OCH 3 , —C(═O)OCH 2 CH 3 , or —C(═O)OCH(CH 3 ) 2 .
18 . The compound of claim 16 wherein R 1 is —C(═O)OCH 3 or —C(═O)OCH 2 CH 3 .
19 . The compound of claim 15 wherein R 6 is —C 1 -C 6 alkyl-Y—R 9 .
20 . The compound of claim 19 wherein Y is —O—.
21 . The compound of claim 20 wherein R 9 is hydrogen.
22 . The compound of claim 21 wherein R 1 is —C(═O)OCH 2 CH 2 OH.
23 . The compound of claim 20 wherein R 9 is C 1 -C 6 alkyl.
24 . The compound of claim 23 wherein R 1 is —C(═O)OCH 2 CH 2 OCH 2 CH 3 .
25 . The compound of claim 19 wherein Y is —N(R 10 )—.
26 . The compound of claim 25 wherein R 9 is hydrogen.
27 . The compound of claim 26 wherein R 1 is —C(═O)OCH 2 CH 2 NH 2 .
28 . The compound of any one of claims 1 - 14 wherein R 1 is —C(═O)N(R 6 ) 2 .
29 . The compound of claim 28 wherein R 6 is C 1 -C 6 alkyl.
30 . The compound of any one of claims 1 - 29 wherein X is a bond.
31 . The compound of any one of claims 1 - 29 wherein X is a C 1 -C 6 alkyl.
32 . The compound of claim 31 wherein X is a —CH 2 —.
33 . The compound of any one of claims 1 - 32 wherein each R 3 , each R 4 , and each R 5 are each independently halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, or C 1 -C 6 alkoxy.
34 . The compound of any one of claims 1 - 33 wherein m is 0 or 1, and n is 0 or 1.
35 . The compound of any one of claims 1 - 33 wherein m is 0, and n is 0.
36 . The compound of any one of claims 1 - 33 wherein m is 0, n is 0, and q is 0.
37 . The compound of any one of claims 1 - 35 wherein p is 0 or 1, and q is 0.
38 . The compound of any one of claims 1 - 35 wherein p is 1, R 4 is C 1 -C 6 alkyl, and q is 0.
39 . The compound of any one of claims 1 - 33 wherein m is 0 or 1, n is 0 or 1, p is 0 or 1, and q is 0 or 1.
40 . The compound of any one of claims 1 - 32 wherein m is 0, n is 0, p is 0, and q is 0.
41 . A compound having the structure of Formula (Ib):
wherein:
X is a bond, C 1 -C 6 alkyl, or C 1 -C 6 heteroalkyl;
R 1 is —C(═O)OR 6 or —C(═O)N(R 6 ) 2 ;
each R 2 is independently halogen, C 1 -C 6 alkyl, or C 1 -C 6 alkoxy;
each R 3 is independently halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 heteroalkyl, —OR 7 , —N(R 7 ) 2 , —CN, —C(═O)R 8 , —C(═O)OR 7 , —C(═O)N(R 7 ) 2 , —NR 7 C(═O)R 8 , —NR 7 SO 2 R 8 , —SO 2 R 8 , or —SO 2 N(R 7 ) 2 ;
R 4 is hydrogen or C 1 -C 6 alkyl;
each R 5 is independently halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 heteroalkyl, —OR 7 , —N(R 7 ) 2 , —CN, —C(═O)R 8 , —C(═O)OR 7 , —C(═O)N(R 7 ) 2 , —NR 7 C(═O)R 8 , —NR 7 SO 2 R 8 , —SO 2 R 8 , or —SO 2 N(R 7 ) 2 ;
each R 6 is independently hydrogen, C 1 -C 6 alkyl, or —C 1 -C 6 alkyl-Y—R 9 ;
each Y is independently —O—, —S—, or —N(R 10 )—;
each R 7 is independently hydrogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, or C 1 -C 6 heteroalkyl;
each R 8 is independently C 1 -C 6 alkyl or C 1 -C 6 heteroalkyl;
each R 9 is independently hydrogen or C 1 -C 6 alkyl;
each R 10 is independently hydrogen or C 1 -C 6 alkyl;
m is 0, 1, 2, 3, or 4;
n is 0, 1, 2, 3, or 4; and
q is 0, 1, 2, or 3;
or a pharmaceutically acceptable salt or solvate thereof.
42 . The compound of claim 41 wherein R 1 is —C(═O)OR 6 .
43 . The compound of claim 42 wherein R 6 is C 1 -C 6 alkyl.
44 . The compound of claim 43 wherein R 1 is —C(═O)OCH 3 , —C(═O)OCH 2 CH 3 , or —C(═O)OCH(CH 3 ) 2 .
45 . The compound of claim 43 wherein R 1 is —C(═O)OCH 3 or —C(═O)OCH 2 CH 3 .
46 . The compound of claim 42 wherein R 6 is —C 1 -C 6 alkyl-Y—R 9 .
47 . The compound of claim 46 wherein Y is —O—.
48 . The compound of claim 47 wherein R 9 is hydrogen.
49 . The compound of claim 48 wherein R 1 is —C(═O)OCH 2 CH 2 OH.
50 . The compound of claim 47 wherein R 9 is C 1 -C 6 alkyl.
51 . The compound of claim 50 wherein R 1 is —C(═O)OCH 2 CH 2 OCH 2 CH 3 .
52 . The compound of claim 46 wherein Y is —N(R 10 )—.
53 . The compound of claim 52 wherein R 9 is hydrogen.
54 . The compound of claim 53 wherein R 1 is —C(═O)OCH 2 CH 2 NH 2 .
55 . The compound of claim 41 wherein R 1 is —C(═O)N(R 6 ) 2 .
56 . The compound of claim 55 wherein R 6 is C 1 -C 6 alkyl.
57 . The compound of any one of claims 41 - 56 wherein X is a bond.
58 . The compound of any one of claims 41 - 56 wherein X is a C 1 -C 6 alkyl.
59 . The compound of claim 58 wherein X is a —CH 2 —.
60 . The compound of any one of claims 41 - 59 wherein each R 3 and each R 5 are each independently halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, or C 1 -C 6 alkoxy.
61 . The compound of any one of claims 41 - 60 wherein m is 0 or 1, n is 0 or 1, and q is 0 or 1.
62 . The compound of any one of claims 41 - 60 wherein m is 0, n is 0, and q is 0.
63 . The compound of any one of claims 41 - 62 wherein R 4 is hydrogen.
64 . The compound of any one of claims 41 - 62 wherein R 4 is C 1 -C 6 alkyl.
65 . The compound of any one of claims 41 - 62 wherein R 4 is —CH 3 .
66 . A compound selected from:
or a pharmaceutically acceptable salt or solvate thereof.
67 . A compound selected from:
or a pharmaceutically acceptable salt or solvate thereof.
68 . A pharmaceutical composition comprising a pharmaceutically acceptable diluent, excipient or binder, and a compound of any one of claims 1 - 67 ; or a pharmaceutically acceptable salt or solvate thereof.
69 . A method of treating a disease, disorder or condition in an individual in need thereof comprising administering to the individual a therapeutically effective amount of a compound of any one of claims 1 - 67 , or a pharmaceutically acceptable salt or solvate thereof, wherein the disease, disorder or condition is a dermal disease, disorder or condition is selected from the group consisting of skin aging, scarring, psoriasis, dermatitis, eczema, urticaria, rosacea, burns, and acne.Cited by (0)
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