# US 2010/0168189 A1 · Therapeutic substituted lactams

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- Number: US 2010/0168189 A1
- Document ID: US20100168189A1
- Status: Published application
- Kind: A1
- Application number: 12/527,155
- Filed: 2008-02-08
- Published: 2010-07-01
- Earliest claimed: 2007-02-15
- Assignees: Allergan, Inc.
- Inventors: David W. Old; Wha Bin Im; Vinh X. Ngo
- Web page: https://patentgrep.com/patent/US20100168189A1

## CPC

- C07D 409/12: linked by a chain containing hetero atoms as chain links
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61P 27/12: for cataracts
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Therapeutic compounds, compositions, methods, and medicaments related thereto are disclosed herein.

## Claims

### Claim 1

A compound having a formula
or a pharmaceutically acceptable salt thereof;
Y is an organic acid functional group, or an amide or ester thereof comprising up to 14 carbon atoms; or Y is hydroxymethyl or an ether thereof comprising up to 14 carbon atoms; or Y is a tetrazolyl functional group;
A is —(CH2)6—, cis —CH2CH═CH—(CH2)3—, or —CH2C≡C—(CH2)3—, wherein 1 or 2 carbon atoms may be replaced by S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is 1, 2, 3, or 4, and wherein 1 —CH2— may be replaced by S or O, and 1 —CH2—CH2— may be replaced by —CH═CH— or —C≡C—; and
B is substituted aryl or heteroaryl.

### Claim 2 (depends on 1)

The compound of claim 1 having a formula
or a pharmaceutically acceptable salt thereof;
wherein a dashed line indicates the presence or absence of a bond; and
G is —CH—, —CH2—, O, or S.

### Claim 3 (depends on 2)

The compound of claim 2 wherein G is O.

### Claim 4 (depends on 2)

The compound of claim 2 wherein G is —CH2—.

### Claim 5 (depends on 1)

The compound of claim 1 wherein B is substituted phenyl.

### Claim 6 (depends on 5)

The compound of claim 5 wherein B is dichlorophenyl.

### Claim 7 (depends on 2)

The compound of claim 2 having a formula
or a pharmaceutically acceptable salt thereof;
wherein Ra is H, alkyl of from 1 to 6 carbon atoms, or phenyl.

### Claim 8 (depends on 1)

A method of treating glaucoma or elevated intraocular pressure comprising administering a compound according to claim 1 to a mammal in need thereof.

### Claim 9 (depends on 1)

Use of a compound according claim 1 in the manufacture of a medicament for the treatment of glaucoma or elevated intraocular pressure.