# US 5,708,015 A · Method for using pharmaceutical compositions containing 2-(2-alkyphenyl-amino)-thiazolines as adrenergic agents

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- Number: US 5,708,015 A
- Document ID: US5708015A
- Status: Granted
- Kind: A
- Application number: 08/739,232
- Filed: 1996-10-29
- Granted: 1998-01-13
- Earliest claimed: 1993-10-22
- Assignees: Allergan, Inc.
- Inventors: Michael E. Garst; James E. Burke; Larry A. Wheeler
- Web page: https://patentgrep.com/patent/US5708015A

## CPC

- A61K 31/415: 1,2-Diazoles
- A61K 31/4168: having a nitrogen attached in position 2, e.g. clonidine
- A61K 31/42: Oxazoles
- A61K 31/421: 1,3-Oxazoles, e.g. pemoline, trimethadione
- A61K 31/425: Thiazoles
- A61K 31/426: 1,3-Thiazoles
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 9/08: Vasodilators for multiple indications
- A61P 9/12: Antihypertensives
- A61P 23/00: Anaesthetics
- A61P 25/02: for peripheral neuropathies
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/20: Hypnotics; Sedatives
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

A pharmaceutical composition, useful for treating animals of the mammalian species, including humans, to treat diseases and conditions which normally respond to treatment with alpha.sub.2 adrenergic agents, contains as its active alpha.sub.2 adrenergic agent ingredient one or more compounds of the formula ##STR1## where X is O, S or NH; n is an integer with the values of 0, 1 or 2; when n is 0 then R.sub.1 is lower alkyl having 1 to 6 carbon atoms and R.sub.2 is H or lower alkyl having 1 to 6 carbon atoms; when n is 1 or 2, then R.sub.1 and R.sub.2 both are methylene (CH.sub.2), or methylene substituted with an R.sub.5 group where R.sub.5 is lower alkyl of 1 to 6 carbons; R.sub.3 and R.sub.4 independently are H or lower alkyl having 1 to 6 carbons; R.sub.6 is H or lower alkyl of 1 to 6 carbons.

## Claims

### Claim 1

A method of treating diseases or conditions of an animal of the mammalian species, the disease or condition being of the type which responds to treatment with alpha.sub.2 adrenergic agents, the method of treatment comprising the steps of administering to the mammal a pharmaceutical composition which comprises as its active ingredient an effective amount of one or more compounds of the formula ##STR9## where X is S;
n is an integer with the values of 0, 1 or 2;
R.sub.3 and R.sub.4 independently are H or lower alkyl having 1 to 6 carbons;
R.sub.6 is H or lower alkyl of 1 to 6 carbons, with the proviso that when n is 0 then R.sub.1 is lower alkyl having 1 to 6 carbon atoms and R.sub.2 is H or lower alkyl having 1 to 6 carbon atoms, when n is 1 or 2, then R.sub.1 and R.sub.2 both are CHR.sub.5, where R.sub.5 independently is H or lower alkyl of 1 to 6 carbons, or salts of compounds of said formula.

### Claim 2 (depends on 1)

The method of treatment of claim 1 wherein in the formula of the active ingredient n is zero.

### Claim 3 (depends on 1)

The method of treatment of claim 1 wherein in the formula of the active ingredient n is 2.

### Claim 4

A method of treating animals of the mammalian species, which are afflicted with a disease or condition of the type which is treated with an .alpha..sub.2 adrenergic agent having effect of altering the rate of fluid flow in the gastrointestinal tract, or anti-spastic, anti-hypertensive, anti-ischemic, anti-epileptic, anesthetic, memory-enhancing or sleep aiding effect, or the effect of increasing fluid flow in at least one kidney, the method of treatment comprising the steps of administering to the mammal a pharmaceutical composition which comprises as its active ingredient an effective amount of one or more compounds of the formula ##STR10## where X is S;
n is an integer with the values of 0, 1 or 2, with the proviso that when n is 0 then R.sub.1 is lower alkyl having 1 to 6 carbon atoms and R.sub.2 is H or lower alkyl having 1 to 6 carbon atoms, when n is 1 or 2, then R.sub.1 and R.sub.2 both are CH.sub.2, or salts of compounds of said formula.

### Claim 5 (depends on 4)

The method of treatment of claim 4 wherein in the formula of the active ingredient n is zero.

### Claim 6 (depends on 4)

The method of treatment of claim 4 wherein in the formula of the active ingredient n is 2.