# US 10,946,033 B2 · 2′-substituted-N6-substituted purine nucleotides for RNA virus treatment

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- Number: US 10,946,033 B2
- Document ID: US10946033B2
- Status: Granted
- Kind: B2
- Application number: 16/293,423
- Filed: 2019-03-05
- Published: 2019-07-04
- Granted: 2021-03-16
- Earliest claimed: 2016-09-07
- Assignees: Atea Pharmaceuticals, Inc.
- Applicants: Atea Pharmaceuticals, Inc.
- Inventors: Jean-Pierre Sommadossi; Adel Moussa
- Web page: https://patentgrep.com/patent/US10946033B2

## CPC

- A61K 31/7076: containing purines, e.g. adenosine, adenylic acid
- A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 31/14: for RNA viruses
- C07H 19/16: Purine radicals
- C07H 19/20: with the saccharide radical esterified by phosphoric or polyphosphoric acids
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## 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

### Claim 1

A method to treat a host infected with Dengue Fever comprising administering an effective amount of a compound of the formula:
or a pharmaceutically acceptable salt thereof to treat the host in need thereof;
wherein:
R7 is C1-6alkyl, C3-7cycloalkyl, or aryl;
R8 is hydrogen or C1-6alkyl;
R9a and R9b are independently selected from hydrogen, C1-6alkyl, cycloalkyl, aryl and aryl(C1-3alkyl)-;
R10 is hydrogen, C1-6alkyl, C1-6haloalkyl, or C3-7cycloalkyl; and
R11 is C1-6alkyl, cycloalkyl, C2-6alkynyl, C2-6alkenyl, or acyl.

### Claim 2 (depends on 1)

The method of claim 1, wherein R7 is aryl.

### Claim 3 (depends on 1)

The method of claim 1, wherein R8 is hydrogen.

### Claim 4 (depends on 1)

The method of claim 1, wherein R10 is C1-C6alkyl.

### Claim 5 (depends on 1)

The method of claim 1,
wherein
R7 is phenyl;
R8 is hydrogen;
R9a and R9b are independently selected from methyl and hydrogen; and
R10 is isopropyl.

### Claim 6 (depends on 5)

The method of claim 5, wherein:
R7 is phenyl;
R8 is hydrogen;
R9a is methyl;
R9b is hydrogen;
R10 is isopropyl; and
the phosphoramidate is in the L-configuration.

### Claim 7 (depends on 1)

The method of claim 1, wherein the host is a human.

### Claim 8 (depends on 7)

The method of claim 7, wherein the Dengue fever is Dengue fever 2.

### Claim 9 (depends on 7)

The method of claim 7, wherein the Dengue fever is Dengue fever 3.

### Claim 10

A method to treat a human infected with Dengue Fever comprising administering an effective amount of a compound of the formula:
or a pharmaceutically acceptable salt thereof to treat the human in need thereof.

### Claim 11 (depends on 10)

The method of claim 10, comprising administering a compound of the formula
or a pharmaceutically acceptable salt thereof.

### Claim 12 (depends on 10)

The method of claim 10, comprising administering a compound of the formula
or a pharmaceutically acceptable salt thereof.

### Claim 13 (depends on 10)

The method of claim 10, wherein the Dengue fever is Dengue fever 2.

### Claim 14 (depends on 10)

The method of claim 10, wherein the Dengue fever is Dengue fever 3.

### Claim 15 (depends on 11)

The method of claim 11, wherein the Dengue fever is Dengue fever 2.

### Claim 16 (depends on 11)

The method of claim 11, wherein the Dengue fever is Dengue fever 3.

### Claim 17

A method to treat a human infected with Dengue Fever comprising administering an effective amount of a compound of the formula:
or a pharmaceutically acceptable salt thereof to treat the human in need thereof.

### Claim 18 (depends on 17)

The method of claim 17, comprising administering a compound of the formula
or a pharmaceutically acceptable salt thereof.

### Claim 19 (depends on 17)

The method of claim 17, comprising administering a compound of the formula
or a pharmaceutically acceptable salt thereof.

### Claim 20 (depends on 17)

The method of claim 17, wherein the Dengue fever is Dengue fever 2.

### Claim 21 (depends on 17)

The method of claim 17, wherein the Dengue fever is Dengue fever 3.

### Claim 22 (depends on 18)

The method of claim 18, wherein the Dengue fever is Dengue fever 2.

### Claim 23 (depends on 18)

The method of claim 18, wherein the Dengue fever is Dengue fever 3.