# US 2010/0168089 A1 · Utilization of tace inhibitors for the treatment of acne

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- Number: US 2010/0168089 A1
- Document ID: US20100168089A1
- Status: Published application
- Kind: A1
- Application number: 12/640,029
- Filed: 2009-12-17
- Published: 2010-07-01
- Earliest claimed: 2007-06-18
- Assignees: Galderma Research & Development
- Inventors: JÉRÔME AUBERT; ISABELLE CARLAVAN; JOHANNES VOEGEL
- Web page: https://patentgrep.com/patent/US20100168089A1

## CPC

- C12Q 1/37: involving peptidase or proteinase
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 17/10: Anti-acne agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- G01N 2500/00: Screening for compounds of potential therapeutic value
- C12Q: MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS (immunoassay G01N33/53); COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

An in vitro method of screening for candidate compounds for the preventive or curative treatment of acne entails determination of the ability of a compound to inhibit the expression or the activity of TACE, and also to the administration of inhibitors of the expression or of the activity of this enzyme, in the treatment of acne.

## Claims

### Claim 1

An in vitro method of screening for candidate compounds for the preventive and/or curative treatment of acne, comprising determining the ability of a compound to inhibit the expression or the activity of the TACE enzyme, or the expression of its gene or the activity of at least one of the promoters thereof, and thus identifying such candidate compound.

### Claim 2 (depends on 1)

The in vitro method as defined by claim 1, comprising the following steps:
a. preparing at least two biological samples or reaction mixtures;
b. contacting one of the samples or reaction mixtures with one or more of the test compounds;
c. measuring the expression or the activity of the TACE enzyme, the expression of its gene or the activity of at least one of the promoters thereof, in the biological samples or reaction mixtures;
d. selecting the compounds for which an inhibition of the expression or of the activity of the TACE enzyme, or an inhibition of the expression of its gene or an inhibition of the activity of at least one of the promoters thereof, is measured in the sample or the mixture treated in b), compared with the untreated sample or mixture.

### Claim 3

A regime or regimen for the preventive and/or curative treatment of acne, comprising administering to an individual in need of such treatment, a medicament which comprises a thus effective amount of at least one inhibitor of the TACE enzyme, said medicament being devoid of cyclooxygenase-2 inhibitor.

### Claim 4 (depends on 3)

The regime or regimen as defined by claim 3, said at least one inhibitor of the TACE enzyme being selected from among E-3-[3-[N-(4-methoxyphenylsulfonyl)-N-isopropylamino]phenyl]-3-(3-pyridyl)-2(E)-propenohydroxamic acid, (2R,3S,5E)-3-[(hydroxyamino)carbonyl]-2-(2-methylpropyl)-6-phenyl-5-hexenoic acid 2-(2-methylpropyl)-2-(methylsulfonyl)hydrazide, (2R,3S)-3-(formylhydroxyamino)-4-methyl-2-(2-methylpropyl)-N-[(1S,2S)-2-methyl-1-[(2-pyridinylamino)carbonyl]butyl]pentanamide, apratastat, (2R,3S)-3-(formylhydroxyamino)-N-[(1S)-4-[[imino(nitroamino)methyl]amino]-1-[(2-thiazolylamino)carbonyl]butyl]-2-(2-methylpropyl)hexanamide, (αR,1α,4 β)-α-[[(4-ethoxyphenyl)sulfonyl](4-pyridinylmethyl)amino]-N-hydroxy-4-propoxycyclohexaneacetamide, (αR)-N-hydroxy-α,3-dimethyl-2-oxo-3-[4-(2-methyl-4-quinolinylmethoxy)phenyl]-1-pyrrolidineacetamide, TNF-484, WTACE2, (8S,11R,12S)-N12-hydroxy-11-(2-methylpropyl)-N8-[2-(4-morpholinyl)-2-oxoethyl]-2,10-dioxo-1-oxa-3,9-diazacyclopentadecane-8,12-dicarboxamide, (6S,7R,10S)-N-6-hydroxy-N10-[2-(methylamino)-2-oxoethyl]-7-(2-methylpropyl)-8-oxo-2-oxa-9-azabicyclo[10.2.2]hexadeca-12,14,15-triene-6,10-dicarboxamide, [2R-[1(S*),2R*,3S*]]-N-1-[1-[[4-(aminoiminomethyl)amino]phenyl]methyl]-2-(methylamino)-2-oxoethyl]-N4-hydroxy-2-(2-methylpropyl)-3-(3-phenylpropyl)butanediamide monoacetate, (2S,3R)-N1-hydroxy-2-methyl-N-4-[(1S)-2-(methylamino)-2-oxo-1-phenylethyl]-3-(2-methylpropyl)butanediamide, 3-[3-[N-isopropyl-N-(4-methoxyphenylsulfonyl)amino]phenyl]-3-(3-pyridyl)-2(E)-propenohydroxamic acid, (2R,3S)-3-(formylhydroxyamino)-4-methyl-2-(2-methylpropyl)-N-[(1S,2S)-2-methyl-1-[(2-pyridinylamino)carbonyl]butyl]pentanamide, (2R,3S)-3-(formylhydroxyamino)-N-[(1S)-4-[[imino(nitroamino)methyl]amino]-1-[(2-thiazolylamino)carbonyl]butyl]-2-(2-methylpropyl)hexanamide, (αR,1α,4β)-α-[[(4-ethoxyphenyl)sulfonyl](4-pyridinylmethyl)amino]-N-hydroxy-4-propoxycyclohexaneacetamide, and (αR)-N-hydroxy-α3-dimethyl-2-oxo-3-[4-(2-methyl-4-quinolinylmethoxy)phenyl]-1-pyrrolidineacetamide.

### Claim 5 (depends on 3)

The regime or regimen as defined by claim 3, said at least one TACE-enzyme inhibitor comprising the only active ingredient(s) in said medicament.

### Claim 6 (depends on 3)

The regime or regimen for the prevention and/or curative treatment of acne as defined by claim 3, said at least one TACE-enzyme inhibitor comprising a compound identified by determining the ability of such compound to inhibit the expression or the activity of the TACE enzyme, or the expression of its gene or the activity of at least one of the promoters thereof.

### Claim 7 (depends on 3)

The regime or regimen as defined by claim 3, said medicament being formulated for topical application.