# US 7,745,442 B2 · Methods of reducing risk of infection from pathogens

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- Number: US 7,745,442 B2
- Document ID: US7745442B2
- Status: Granted
- Kind: B2
- Application number: 10/920,484
- Filed: 2004-08-18
- Published: 2005-04-14
- Granted: 2010-06-29
- Earliest claimed: 2003-08-20
- Assignees: Parion Sciences, Inc.
- Inventors: Michael R. Johnson; Samuel E. Hopkins
- Web page: https://patentgrep.com/patent/US7745442B2

## CPC

- C07D 241/30: in which said hetero-bound carbon atoms are part of a substructure —C(=X)—X—C(=X)—X— in which X is an oxygen or sulphur atom or an imino radical, e.g. imidoylguanidines
- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/4965: Non-condensed pyrazines
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 31/06: for tuberculosis
- A61P 31/14: for RNA viruses
- A61P 31/16: for influenza or rhinoviruses
- C07D 253/07: with hetero atoms, or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- 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

Prophylactic treatment methods are provided for protection of individuals and/or populations against infection from airborne pathogens. In particular, prophylactic treatment methods are provided including administering a sodium channel blocker or pharmaceutically acceptable salts thereof to one or more members of a population at risk of exposure to or already exposed to one or more airborne pathogens, either from natural sources or from intentional release of pathogens into the environment.

## Claims

### Claim 1

A treatment method for delaying and/or reducing the risk of infection from one or more airborne pathogens comprising:
administering an effective amount of a sodium channel blocker or a pharmaceutically acceptable salt thereof to an individual in need thereof, wherein said one or more airborne pathogens are retained in lung mucous secretions and are thus removed by mucociliary clearance, wherein the sodium channel blocker is a compound according to Formula III:
where X is hydrogen, halogen, trifluoromethyl, lower alkyl, unsubstituted or substituted phenyl, lower alkyl-thio, phenyl-lower alkyl-thio, lower alkyl-sulfonyl, or phenyl-lower alkyl-sulfonyl;
Y is hydrogen, hydroxyl, mercapto, lower alkoxy, lower alkyl-thio, halogen, lower alkyl, unsubstituted or substituted mononuclear aryl, or —N(R2)2;
R1 is hydrogen or lower alkyl;
each R2 is, independently, —R7, —(CH2)m—OR8, —(CH2)m—NR7R10, —(CH2)n(CHOR8)(CHOR8)n—CH2OR8, —(CH2CH2O)m—R8, —(CH2CH2O)m—CH2CH2NR7R10, —(CH2)n—C(═O)NR7R10, —(CH2)n—Zg—R7, —(CH2)m—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —(CH2)n—CO2R7, or
R3″ and R4″ are each, independently, hydrogen, a group represented by formula (A″), lower alkyl, hydroxy lower alkyl, phenyl, phenyl-lower alkyl, (halophenyl)-lower alkyl, lower-(alkylphenylalkyl), lower (alkoxyphenyl)-lower alkyl, naphthyl-lower alkyl, or pyridyl-lower alkyl, with the proviso that at least one of R3″ and R4″ is a group represented by formula (A″):
where each RL is, independently, —R7, —(CH2)n—OR8, —O—(CH2)m—OR8, —(CH2)n—NR7R10, —O—(CH2)m—NR7R10, —(CH2)n(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)m(CHOR8)(CHOR8)n—CH2OR8, —(CH2CH2O)m—R8, —O—(CH2CH2O)m—R8, —(CH2CH2O)m—CH2CH2NR7R10, —O—(CH2CH2O)m—CH2CH2NR7R10 , —(CH2)n—C(═O)NR7R10, —O—(CH2)m—C(═O)NR7R10, —(CH2)n—(Z)g—R7, —O—(CH2)m—(Z)g—R7, —(CH2)n—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)m—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —(CH2)n—CO2R7, —O—(CH2)m—CO2R7, —OSO3H, —O—glucuronide, —O—glucose,
each o is, independently, an integer from 0 to 10;
each p is an integer from 0 to 10;
with the proviso that the sum of o and p in each contiguous chain is from 1 to 10;
each x is, independently, O, NR10, C(═O), CHOH, C(═N—R10), CHNR7R10, or represents a single bond;
each R5′ is, independently, —(CH2)m—OR8, —O—(CH2)m—OR8, —(CH2)n—NR7R10, —O—(CH2)m—NR7R10, —(CH2)n(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)m(CHOR8)(CHOR8)n—CH2OR8, —(CH2CH2O)m—R8, —O—(CH2CH2O)m—R8, —(CH2CH2O)m—CH2CH2NR7R10, —O—(CH2CH2O)m—CH2CH2NR7R10, —(CH2)n—C(═O)NR7R10, —O—(CH2)m—C(═O)NR7R10, —(CH2)n—(Z)g—R7, —O—(CH2)m—(Z)g—R7, —(CH2)n—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)m—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —(CH2)n—CO2R7, —O—(CH2)mCO2R7, —OSO3H, —O—glucuronide, —O—glucose,
each R6″ is, independently, —R7, —OR11, —N(R7)2, —(CH2mOR8, —O—(CH2)m—OR8, —(CH2)n—NR7R10, —O—(CH2)m—NR7R10, —(CH2)n(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)m(CHOR8)(CHOR8)n—CH2OR8, —(CH2CH2O)m—R8, —O—(CH2CH2O)m—R8, —(CH2CH2O)m—CH2CH2NR7R10, —O—(CH2CH2O)m—CH2CH2NR7R10, —(CH2)n—C(═O)NR7R10, —O—(CH2)m—C(═O)NR7R10, —(CH2)n—(Z)g—R7, —O—(CH2)m—(Z)g—R7, —(CH2)m—NR10—CH2(CHOR8)(CHOR8)n,—CH2OR8, —O—(CH2)m—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —(CH2)m—CO2R7, —O—(CH2)m—CO2R7, —OSO3H, —O—glucuronide, —O—glucose,
where when two R6″ are —OR11 and are located adjacent to each other on a phenyl ring, the alkyl moieties of the two R6″ may be bonded together to form a methylenedioxy group;
each R7 is, independently, hydrogen or lower alkyl;
each R8 is, independently, hydrogen, lower alkyl, —C(═O)—R11, glucuronide, 2-tetrahydropyranyl, or
each R9 is, independently, —CO2R7, —CON(R7)2, —SO2CH3, or —C(═O)R7;
each R10 is, independently, —H, —SO2CH3, —CO2R7, —C(═O)NR7R9, —C(═O)R7, or —CH2—(CHOH)n—CH2OH;
each Z is, independently, CHOH, C(═O), CHNR7R10, C═NR10, or NR10;
each R11 is, independently, lower alkyl;
each g is, independently, an integer from 1 to 6;
each m is, independently, an integer from 1 to 7;
each n is, independently, an integer from 0 to 7;
each Q″ is, independently, C—R5′, C—R6″, or a nitrogen atom, wherein at most three Q″ in a ring are nitrogen atoms and wherein at least one Q″ in a ring is C-R5″; or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The treatment method of claim 1 wherein the pathogen is Bacillus anthracis.

### Claim 3 (depends on 1)

The treatment method of claim 1 wherein the sodium channel blocker or pharmaceutically acceptable salt thereof is administered in an aerosol suspension of respirable particles which the individual inhales.

### Claim 4 (depends on 1)

The treatment method of claim 1 wherein the sodium channel blocker or a pharmaceutically acceptable salt is administered post-exposure to the one or more airborne pathogens.

### Claim 5 (depends on 1)

The treatment method of claim 1 wherein the sodium channel blocker is