US2007179132A1PendingUtilityA1
Inhibitors of macrophage migration inhibitory factor and methods for identifying the same
Est. expiryFeb 14, 2023(expired)· nominal 20-yr term from priority
A61P 37/08A61P 3/10A61P 9/00A61P 37/00A61P 37/06A61P 43/00A61P 25/00A61P 35/00A61P 29/00A61P 31/04A61P 11/06A61P 11/00A61P 1/04A61P 19/02A61P 1/00A61K 31/496C07D 401/12A61K 31/56A61K 31/52C07D 409/12A61K 31/54C07D 405/12C07D 215/54C07D 413/12C07D 417/12C07D 401/04
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Claims
Abstract
Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R 1 , R 2 , R 3 , R 4 , X, and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.
Claims
exact text as granted — not AI-modified1 . A compound having a structure selected from the group consisting of:
or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein:
X is oxygen or sulfur;
Z is —CH 2 — or —C(═O)—;
R 1 is selected from the group consisting of C 1-10 alkyl, aryl C 1-10 alkyl, aryl, 5- to 7-membered monocyclic heterocyclic ring, and 7- to 14-membered polycyclic heterocyclic ring, wherein R 1 is unsubstituted or substituted with at least one substitutent selected from the group consisting of halogen, alkyl, alkoxy, hydroxy, amino, alkylamino, dialkylamino, and keto;
R 2 and R 3 are independently selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, hydroxy, amino, alkylamino, dialkylamino, and keto;
R 4 is selected from the group consisting of —CH 2 R 7 , —C(═O)NR 5 R 6 , and —C(═O)R 7 ;
R 5 and R 6 are independently selected from the group consisting of C 1-10 alkyl, aryl, aryl C 1-10 alkyl, 5- to 7-membered monocyclic heterocyclic ring, and 7- to 14-membered polycyclic heterocyclic ring, wherein R 5 and R 6 are independently unsubstituted or substituted with at least one substitutent selected from the group consisting of halogen, alkoxy, hydroxy, amino, alkylamino, dialkylamino, and keto, or R 5 and R 6 taken together with a nitrogen atom to which they are attached form a 5- to 7-membered monocyclic heterocyclic ring or a 7- to 14-membered polycyclic heterocyclic ring, wherein the ring is unsubstituted or substituted with at least one substitutent selected from the group consisting of halogen, alkyl, alkoxy, hydroxy, amino, alkylamino, dialkylamino, and keto;
R 7 is selected from the group consisting of C 1-10 alkyl, aryl, aryl C 1-10 alkyl, 5- to 7-membered monocyclic heterocyclic ring, and 7- to 14-membered polycyclic heterocyclic ring, wherein R 7 is unsubstituted or substituted with at least one substitutent selected from the group consisting of halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, and keto; and
n is 0, 1 or 2, with the proviso that when n is 0, Z is —C(═O)—.
2 . The compound of claim 1 , wherein X is oxygen.
3 . The compound of claim 1 , wherein Z is —CH 2 —.
4 . The compound of claim 1 , wherein Z is —CH 2 — and n is 1.
5 . The compound of claim 1 , wherein n is 1.
6 . The compound of claim 1 , wherein R 1 is —CH 2 Ph.
7 . The compound of claim 1 , wherein R 1 is —CH 2 (2-pyridyl).
8 . The compound of claim 1 , wherein R 4 is —C(═O)R 7 , and wherein R 7 is methyl.
9 . A compound having a structure selected from the group consisting of:
or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein:
X is oxygen or sulfur;
Z is —CH 2 — or —C(═O)—;
R 1 is selected from the group consisting of C 1-10 alkyl, aryl C 1-10 alkyl, aryl, 5- to 7-membered monocyclic heterocyclic ring, and 7- to 14-membered polycyclic heterocyclic ring, wherein R 1 is unsubstituted or substituted with at least one substitutent selected from the group consisting of halogen, alkyl, alkoxy, hydroxy, amino, alkylamino, dialkylamino, and keto;
R 2 and R 3 are independently selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, hydroxy, amino, alkylamino, dialkylamino, and keto;
R 4 is selected from the group consisting of hydrogen, methyl, and methyl substituted by keto; and
n is 0, 1 or 2, with the proviso that when n is 0, Z is —C(═O)—.
10 . The compound of claim 9 , wherein X is oxygen.
11 . The compound of claim 9 , wherein Z is —CH 2 —.
12 . The compound of claim 9 , wherein Z is —CH 2 — and n is 1.
13 . The compound of claim 9 , wherein n is 1.
14 . The compound of claim 9 , wherein R 1 is —CH 2 (2-pyridyl).
15 . The compound of claim 9 , wherein R 1 is —CH 2 Ph.
16 . The compound of claim 9 , wherein R 4 is hydrogen.
17 . The compound of claim 16 , wherein Z is —CH 2 — and n is 1.
18 . The compound of claim 16 , wherein R 1 is CH 3 .
19 . The compound of claim 16 , wherein R 1 is CH 2 Ph.
20 . The compound of claim 16 , wherein R 1 is 4-FCH 2 Ph.
21 . The compound of claim 16 , wherein R 2 is F and R 3 is H.
22 . The compound of claim 9 , wherein R 4 is methyl.
23 . The compound of claim 22 , wherein Z is —CH 2 — and n is 1.
24 . The compound of claim 22 , wherein R 1 is CH 3 .
25 . The compound of claim 22 , wherein R 1 is CH 2 Ph.
26 . The compound of claim 22 , wherein R 1 is 4-FCH 2 Ph.
27 . The compound of claim 22 , wherein R 2 is F and R 3 is H.
28 . The compound of claim 9 , wherein R 4 is methyl substituted by keto.
29 . The compound of claim 28 , wherein Z is —CH 2 — and n is 1.
30 . The compound of claim 28 , wherein R 1 is CH 3 .
31 . The compound of claim 28 , wherein R 1 is CH 2 Ph.
32 . The compound of claim 28 , wherein R 1 is 4-FCH 2 Ph.
33 . The compound of claim 28 , wherein R 21s F and R 3 is H.
34 . The compound of claim 9 , having a formula selected from the group consisting of:
35 . The compound of claim 9 , having a formula selected from the group consisting of:
36 . The compound of claim 9 , having a formula selected from the group consisting of:Cited by (0)
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