# US 7,612,053 B2 · 7-Substituted fused ring tetracycline compounds

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- Number: US 7,612,053 B2
- Document ID: US7612053B2
- Status: Granted
- Kind: B2
- Application number: 11/305,048
- Filed: 2005-12-16
- Published: 2006-07-06
- Granted: 2009-11-03
- Earliest claimed: 2000-05-15
- Assignees: Paratek Pharmaceuticals, Inc.
- Inventors: Mark L. Nelson; Laura McIntyre
- Web page: https://patentgrep.com/patent/US7612053B2

## CPC

- C07D 323/02: Five-membered rings
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- C07C 237/26: of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
- C07D 317/60: Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07C 2603/46: 1,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

7-substituted fused ring tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted fused ring tetracycline compounds are described.

## Claims

### Claim 1

A method for treating a tetracycline responsive state in a mammal, comprising administering to said mammal a 7-substituted fused ring tetracycline compound of formula (I):
wherein:
X is CR6R6′;
R4 and R4′ are each alkyl;
R5 is hydrogen or hydroxyl;
R6 and R6′ are each independently hydrogen, hydroxyl, alkyl, or taken together, alkenyl;
Y and Y′ are each independently optionally substituted C, N, O, or S;
m is 1 or 2; and pharmaceutically acceptable salts thereof; such that the tetracycline responsive state is a bacterial infection that is selected from the group consisting of S. pnuemoniae, E. hirae, H influenzae, and M catarrhalis.

### Claim 2 (depends on 1)

The method of claim 1 wherein R5, R6 and R6′ are each hydrogen and R4 and R4′ are each methyl.

### Claim 3 (depends on 1)

The method of claim 1, wherein Y and Y′ are each oxygen.

### Claim 4 (depends on 1)

The method of claim 1, wherein m is 1.

### Claim 5

A method for treating a tetracycline responsive state in a mammal, comprising administering to said mammal 7-(3′,4′-methylene dioxyphenyl)sancycline or a pharmaceutically acceptable salt thereof, such that the tetracycline responsive state is a bacterial infection that is selected from the group consisting of S. pnuemoniae, E. hirae, H influenzae, and M catarrhalis.

### Claim 6 (depends on 2)

The method of claim 2, wherein said bacterial infection is associated with S. pnuemoniae.

### Claim 7 (depends on 2)

The method of claim 2, wherein said bacterial infection is associated with E. hirae.

### Claim 8 (depends on 2)

The method of claim 2, wherein said bacterial infection is associated with H influenzae.

### Claim 9 (depends on 2)

The method of claim 2, wherein said bacterial infection is associated with M catarrhalis.

### Claim 10 (depends on 2)

The method of claim 2, wherein said bacterial infection is resistant to other tetracycline antibiotics.

### Claim 11 (depends on 2)

The method of claim 2, wherein said compound is administered with a pharmaceutically acceptable carrier.

### Claim 12 (depends on 5)

The method of claim 5, wherein said bacterial infection is associated with S. pnuemoniae.

### Claim 13 (depends on 5)

The method of claim 5, wherein said bacterial infection is associated with E. hirae.

### Claim 14 (depends on 5)

The method of claim 5, wherein said bacterial infection is associated with H influenzae.

### Claim 15 (depends on 5)

The method of claim 5, wherein said bacterial infection is associated with M catarrhalis.

### Claim 16 (depends on 5)

The method of claim 5, wherein said bacterial infection is resistant to other tetracycline antibiotics.

### Claim 17 (depends on 5)

The method of claim 5, wherein said compound is administered with a pharmaceutically acceptable carrier.