US2020222442A1PendingUtilityA1
2'-substituted-n6-substituted purine nucleotides for rna virus treatment
Est. expirySep 7, 2036(~10.2 yrs left)· nominal 20-yr term from priority
C07H 19/20C07H 19/16A61P 31/14A61K 31/7076C07H 23/00C07H 19/207Y02A50/30A61P 1/00A61K 31/675A61K 9/0043
66
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Claims
Abstract
The use of described compounds or pharmaceutically acceptable salts or compositions thereof for the treatment of a host infected with an RNA virus other than HCV, or other disorder more fully described herein.
Claims
exact text as granted — not AI-modifiedWe claim:
1 . A method to treat or prevent a Coronaviridae viral infection in a human in need thereof comprising administering an effective amount of a compound of the formula:
or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier,
wherein
R 1 is C 1 -C 5 alkyl, —(C 0 -C 2 alkyl)(C 3 -C 6 cycloalkyl), or —C(O)R 3C ;
R 3C is alkyl;
R 7 is hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, heteroaryl, heterocyclyl, or aryl;
R 8 is hydrogen or C 1-6 alkyl;
R 9a and R 9b are independently selected from hydrogen, C 1-6 alkyl, and cycloalkyl; and
R 10 is hydrogen, C 1-6 alkyl, C 1-6 haloalkyl, C 3-7 cycloalkyl, heterocycloalkyl, aminoacyl, aryl, heteroaryl, aryl, or heteroaryl.
2 . The method of claim 1 , wherein R 1 is C 1 -C 5 alkyl.
3 . The method of claim 2 , wherein R 1 is selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec-butyl, tert-butyl and pentyl.
4 . The method of claim 3 , wherein R 1 is selected from methyl and ethyl.
5 . The method of claim 1 , wherein R 1 is —(C 0 -C 2 alkyl)(C 3 -C 6 cycloalkyl).
6 . The method of claim 5 , wherein R 1 is cyclopropyl.
7 . The method of claim 1 , wherein R 1 is —C(O)R 3C .
8 . The method of claim 7 , wherein R 1 is selected from —C(O)CH 3 , —C(O)CH 2 CH 3 —C(O)CH(CH 3 ) 2 , —C(O)OCH 3 , —C(O)OC 2 H 5 , —C(O)OC 3 H 7 , —C(O)OC 4 H 9 , and —C(O)OC 5 H 11 .
9 . The method of claim 1 , wherein R 7 is phenyl.
10 . The method of claim 1 , wherein R 7 is napthyl.
11 . The method of claim 1 , wherein R 8 is hydrogen.
12 . The method of claim 1 , wherein R 9a is methyl and R 9b is hydrogen.
13 . The method of claim 1 , wherein R 10 is methyl, ethyl, or iso-propyl.
14 . The method of claim 13 , wherein R 10 is isopropyl.
15 . The method of claim 1 ,
wherein R 7 is aryl; R 8 is hydrogen; R 9a and R 9b are independently selected from methyl and hydrogen; and R 10 is alkyl.
16 . The method of claim 15 ,
wherein R 7 is phenyl; R 8 is hydrogen; R 9a and R 9b are independently selected from methyl and hydrogen; and R 10 is isopropyl.
17 . The method of claim 1 , wherein the Coronaviridae viral infection is a virus of the genus Alphacoronavirus.
18 . The method of claim 1 , wherein the Coronaviridae viral infection is a virus of the genus Betacoronavirus.
19 . The method of claim 1 , wherein the Coronaviridae viral infection is a virus of the genus Gammacoronavirus.
20 . The method of claim 1 , wherein the Coronaviridae viral infection is a virus of the genuses Deltacoronavirus.
21 . The method of claim 1 , wherein the compound is administered in a dosage form suitable for oral administration.
22 . The method of claim 21 , wherein the dosage form is a solid oral dosage form.
23 . The method of claim 22 , wherein the solid oral dosage form is a tablet or capsule.
24 . The method of claim 21 , wherein the dosage form is a liquid oral dosage form.
25 . The method of claim 24 , wherein the liquid oral dosage form is a solution or a suspension.
26 . The method of claim 1 , wherein the compound is administered in a dosage form suitable for intravenous administration.
27 . The method of claim 1 , wherein the compound is administered in a dosage form suitable for parenteral administration.
28 . The method of claim 1 comprising administering an effective amount of a compound of the formula:
or a pharmaceutically acceptable salt thereof.
29 . The method of claim 28 , comprising administering an effective amount of a compound of the formula
or a pharmaceutically acceptable salt thereof.
30 . The method of claim 28 , comprising administering an effective amount of a compound
or a pharmaceutically acceptable salt thereof.
31 . The method of claim 28 , wherein the Coronaviridae viral infection is a virus of the genus Alphacoronavirus.
32 . The method of claim 28 , wherein the Coronaviridae viral infection is a virus of the genus Betacoronavirus.
33 . The method of claim 28 , wherein the Coronaviridae viral infection is a virus of the genus Gammacoronavirus.
34 . The method of claim 28 , wherein the Coronaviridae viral infection is a virus of the genuses Deltacoronavirus.
35 . The method of claim 28 , wherein the compound is administered in a dosage form suitable for oral administration.
36 . The method of claim 35 , wherein the dosage form is a solid oral dosage form.
37 . The method of claim 36 , wherein the solid oral dosage form is a tablet or capsule.
38 . The method of claim 35 , wherein the dosage form is a liquid oral dosage form.
39 . The method of claim 38 , wherein the liquid oral dosage form is a solution or a suspension.
40 . The method of claim 28 , wherein the compound is administered in a dosage form suitable for intravenous administration.
41 . The method of claim 28 , wherein the compound is administered in a dosage form suitable for parenteral administration.
42 . The method of claim 1 comprising administering an effective amount of a compound of the formula:
or a pharmaceutically acceptable salt thereof.
43 . The method of claim 42 , comprising administering an effective amount of a compound of the formula
or a pharmaceutically acceptable salt thereof.
44 . The method of claim 42 , comprising administering an effective amount of a compound
or a pharmaceutically acceptable salt thereof.
45 . The method of claim 42 , wherein the Coronaviridae viral infection is a virus of the genuses Alphacoronavirus.
46 . The method of claim 42 , wherein the Coronaviridae viral infection is a virus of the genuses Betacoronavirus.
47 . The method of claim 42 , wherein the Coronaviridae viral infection is a virus of the genuses Gammacoronavirus.
48 . The method of claim 42 , wherein the Coronaviridae viral infection is a virus of the genuses Deltacoronavirus.
49 . The method of claim 42 , wherein the compound is administered in a dosage form suitable for oral administration.
50 . The method of claim 49 , wherein the dosage form is a solid oral dosage form.
51 . The method of claim 50 , wherein the solid oral dosage form is a tablet or capsule.
52 . The method of claim 49 , wherein the dosage form is a liquid oral dosage form.
53 . The method of claim 52 , wherein the liquid oral dosage form is a solution or a suspension.
54 . The method of claim 42 , wherein the compound is administered in a dosage form suitable for intravenous administration.
55 . The method of claim 42 , wherein the compound is administered in a dosage form suitable for parenteral administration.Cited by (0)
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