# US 10,118,923 B2 · Compositions and methods for inhibiting kinases

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- Number: US 10,118,923 B2
- Document ID: US10118923B2
- Status: Granted
- Kind: B2
- Application number: 15/805,693
- Filed: 2017-11-07
- Published: 2018-03-01
- Granted: 2018-11-06
- Earliest claimed: 2015-04-23
- Assignees: Inhibikase Therapeutics, Inc.
- Applicants: Inhibikase Therapeutics, Inc.
- Inventors: Milton H. Werner; Terence A. Kelly
- Web page: https://patentgrep.com/patent/US10118923B2

## CPC

- C07D 417/14: containing three or more hetero rings
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 31/04: Antibacterial agents
- A61P 31/12: Antivirals
- A61P 31/18: for HIV
- A61P 31/22: for herpes viruses
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 401/14: containing three or more hetero rings
- C07D 403/14: containing three or more hetero rings
- C07D 413/14: containing three or more hetero rings
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present invention provides compounds for the prevention or treatment of cancer or a bacterial or viral infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the prevention or treatment of cancer or a bacterial or viral infection in a subject.

## Claims

### Claim 1

A method of treating a mammal suffering from a bacterial infection or a viral infection, comprising administering to the mammal an effective amount of a compound of Formula (I) or a pharmaceutical composition thereof:
wherein, independently for each occurrence,
R1 is hydrogen, lower alkyl, —CH3, —CDH2, —CD2H, or —CD3; and
Cy1 is heterocyclyl or substituted or unsubstituted 5-membered heteroaryl,
wherein the bacterial infection is caused by Pseudomonas aeruginosa, Chlamydia trachomatis, Escherichia coli, Helicobacter pylori, Salmonella typhimurium, Shigella flexneri, or Mycobacterium tuberculosis; and
the viral infection is caused by a Vaccinia virus, a variola virus, a polyoma virus, a Pox virus, a Herpes virus, cytomegalovirus, a human immunodeficiency virus, JC polyomavirus, BK polyomavirus, Simian virus 40, Monkeypox virus, Ebola virus, Marburg virus, Flavivirus, or West Nile virus.

### Claim 2 (depends on 1)

The method of claim 1, wherein Cy1 is selected from:
wherein, independently for each occurrence,
R2 and R3 are selected from hydrogen, alkyl, amino, monoalkylamino, dialkylamino, cycloalkyl, halo, cyano, alkoxy, —C(O)OH, and —C(O)N(R4)(R4);
n is 1, 2, 3 or 4;
X is C(R4)2, S, O, or NR4;
R4 is selected from hydrogen and substituted or unsubstituted alkyl, aralkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, heteroaralkyl, cycloalkylalkyl, or heterocyclylalkyl.

### Claim 3 (depends on 1)

The method of claim 1, wherein Cy1 is selected from:
wherein, independently for each occurrence,
R1 is selected from hydrogen or lower alkyl;
R2 and R3 are selected from hydrogen, alkyl, amino, monoalkylamino, dialkylamino, cycloalkyl, halo, cyano, alkoxy, —C(O)OH, and —C(O)N(R4)(R4);
R4 is selected from hydrogen and substituted or unsubstituted alkyl, aralkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, heteroaralkyl, cycloalkylalkyl, or heterocyclylalkyl.

### Claim 4 (depends on 1)

The method of claim 1, wherein Cy1 is a substituted or unsubstituted 5-membered heteroaryl.

### Claim 5 (depends on 4)

The method of claim 4, wherein Cy1 is selected from:

### Claim 6 (depends on 4)

The method of claim 4, wherein Cy1 is selected from:

### Claim 7 (depends on 4)

The method of claim 4, wherein Cy1 is selected from:

### Claim 8 (depends on 1)

The method of claim 1, wherein Cy1 is selected from:

### Claim 9 (depends on 1)

The method of claim 1, wherein R1 is —CH3, —CDH2, —CD2H, or —CD3.

### Claim 10 (depends on 1)

The method of claim 1, comprising administering to the mammal an effective amount of a pharmaceutical composition comprising the compound of claim 1.

### Claim 11 (depends on 10)

The method of claim 10, wherein the pharmaceutical composition further comprises one or more pharmaceutically acceptable excipients.

### Claim 12 (depends on 1)

The method of claim 1, wherein the mammal is suffering from a lytic infection of JC polyomavirus in the brain.

### Claim 13 (depends on 1)

The method of claim 1, wherein the compound or composition is conjointly administered with one or more compounds independently selected from central nervous system drugs, analgesics, narcotic agonists, narcotic antagonists, nonsteroidal anti-inflammatory/analgesic agents, behavior-modifying agents, tranquilizers/sedatives, anesthetic agents, inhalants, narcotics, reversal agents, anticonvulsants, skeletal muscle relaxants, smooth muscle relaxants, cardiovascular agents, inotropic agents, antiarrhythmic drugs, anticholinergics, vasodilating agents, agents used in treatment of shock, alpha-adrenergic blocking agents, beta-adrenergic blocking agents, respiratory drugs, bronchodilators, sympathomimetics, antihistamines, antitussives, agents for urinary incontinence/retention, urinary alkalinizers, urinary acidifiers, cholinergic stimulants, agents for urolithiasis, gastrointestinal agents, antiemetic agents, antacids, histamine H2 antagonists, gastromucosal protectants, proton pump inhibitors, appetite stimulants, GI antispasmodics-anticholinergics, GI stimulants, laxatives, saline, lubricant, surfactant, antidiarrheals, hormones/endocrine/reproductive agents, sex hormones, anabolic steroids, posterior pituitary hormones, adrenal cortical steroids, glucocorticoids, antidiabetic agents, thyroid drugs, thyroid hormones, endocrine/reproductive drugs, prostaglandins, antiinfective drugs, antiparasitics, anticoccidial agents, antibiotics, anti-tuberculosis, aminocyclitols, cephalosporins, macrolides, penicillins, tetracyclines, lincosamides, quinolones, sulfonamides, antibacterials, antifungal agents, antiviral agents, blood modifying agents, clotting agents, anticoagulants, erythropoietic agents, antineoplastics/immunosuppressives, alkylating agents, antidotes, bone/joint agents, dermatologic agents (systemic), vitamins and minerals/nutrients, systemic acidifiers, systemic alkalinizers, anti-cancer agents, or anti-viral agents.
