# US 5,703,069 A · Method for inhibiting and controlling viral growth

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- Number: US 5,703,069 A
- Document ID: US5703069A
- Status: Granted
- Kind: A
- Application number: 08/712,063
- Filed: 1996-09-11
- Granted: 1997-12-30
- Earliest claimed: 1994-03-07
- Assignees: Warner-Lambert Company
- Inventors: David Thomas Connor; Stephen Joseph Gracheck
- Web page: https://patentgrep.com/patent/US5703069A

## CPC

- C07D 495/04: Ortho-condensed systems
- A61K 31/551: having two nitrogen atoms, e.g. dilazep
- A61K 31/553: having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
- A61K 31/554: having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/12: Antivirals
- A61P 31/18: for HIV
- A61P 31/22: for herpes viruses
- A61P 37/04: Immunostimulants
- C07D 513/04: Ortho-condensed systems
- 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

## Abstract

Benzothiophene, benzofuran and indole-thiazepinones, oxazepinones, and diazepinones are effective therapeutic agents for treating viral diseases, including those caused by herpesvirus and HIV.

## Claims

### Claim 1

A method for substantially inhibiting HIV or the activation of HIV in an HIV-infected individual or suppressing the immune system which comprises administering a therapeutically effective amount of a compound of the following formula: ##STR3## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each independently hydrogen, hydroxy, halogen, lower alkyl, lower alkoxy, benzyloxy, trifluoromethyl, nitro, or -NR.sub.8 R.sub.9, in which R.sub.8 and R.sub.9 are each independently hydrogen or lower alkyl;
R.sub.5 and R.sub.6 are each independently hydrogen, lower alkyl or phenyl;
X is O, S(O).sub.n or NR.sub.7 ;
Y is O, S(O).sub.n or NR.sub.8 ;
R.sub.7 is hydrogen, lower alkyl, phenyl, benzyl, CH.sub.2 OR.sub.8 or lower alkyl, phenyl, benzyl substituted with halo;
R.sub.8 is hydrogen, lower alkyl or phenyl;
n is an integer of 0, 1 or 2;
with the provisos that
1) when X is NH, Y is NH, R.sub.1 is H, R.sub.3 is H and R.sub.4 is Br, R.sub.2 is not methyl;
2) when X is NH, Y is NH, R.sub.1, R.sub.3 and R.sub.4 are H, R.sub.2 is not methoxy or ethoxy, and
3) when X is NH, Y is S, at least one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is not H.

### Claim 2 (depends on 1)

A method of claim 1 employing a compound, wherein R.sub.1, R.sub.3 , and R.sub.4 are hydrogen.

### Claim 3 (depends on 2)

A method of claim 2 employing a compound, wherein R.sub.2 is hydrogen or lower alkoxy; X is O, S(O).sub.n or NR.sub.7 ; Y is O or S(O).sub.n ; R.sub.7 is hydrogen or lower alkyl, and n is 0, 1 or 2.

### Claim 4 (depends on 3)

A method of claim 3 employing 2,3 -dihydro-9-methoxy-›1!benzothieno›2,3-f!-1,4-thiazepin-5(4H) -one.

### Claim 5 (depends on 3)

A method of claim 3 employing 2,3-dihydro-›1!benzothieno-›2,3-f!-1,4-oxazepin-5(4H)-one.

### Claim 6 (depends on 3)

A method of claim 3 employing 2,3 -dihydro-9-methoxy-›1!benzothieno›2,3-f!-1,4-thiazepin-5(4H)-one-1-oxide.

### Claim 7 (depends on 3)

A method of claim 3 employing 3,4-dihydro-9-methoxy-6-methyl-2H-1,4-oxazepino›6,7-b!-indol-5(6H)-one.

### Claim 8 (depends on 3)

A method of claim 3 employing 2,3-dihydro-1H-benzothieno-›3,2-e!-1,4-diazepine-5-one.

### Claim 9 (depends on 3)

A method of claim 3 employing 2,3-dihydro-9-methoxy-1H-benzothieno-›2,3-f!-1,4-oxazepin-5-one.

### Claim 10 (depends on 3)

A method of claim 3 employing 2,3-dihydro-9-methoxy-6-oxide-1H-benzothieno-›2,3-f!-1,4-oxazepin-5-one.

### Claim 11 (depends on 3)

A method of claim 3 employing 2,3-dihydro-9-methoxy-2-methyl-1H-benzothieno-›2,3-f!-1,4-oxazepin-5-one.