# US 5,708,019 A · Methods of treating hyperlipidemia using azaspirane derivatives

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- Number: US 5,708,019 A
- Document ID: US5708019A
- Status: Granted
- Kind: A
- Application number: 08/295,777
- Filed: 1995-05-04
- Granted: 1998-01-13
- Earliest claimed: 1993-04-28
- Assignees: SmithKline Beecham Corporation
- Inventors: Alsion Mary Badger
- Web page: https://patentgrep.com/patent/US5708019A

## CPC

- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- 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)

## Abstract

Invented is a method of treatment of hyperlipidemia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of an azaspirane derivative. Also invented are pharmaceutical compositions containing an azaspirane derivative.

## Claims

### Claim 1

A method of treatment of hyperlipidemia in a mammal in need thereof which comprises administering to such mammal an effective amount of a compound of Formula I ##STR4## wherein: n is 1 or 2;
R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen or straight chain, branched chain or cyclic alkyl, provided that the total number of carbon atoms contained in R.sub.1 and R.sub.2 when taken together is 0-10; or R.sup.1 and R.sup.2 are joined together to from a cyclic alkyl group having 3-7 carbon atoms; and
R.sup.3 and R.sup.4 are the same or different and are selected from hydrogen or methyl; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

### Claim 2 (depends on 1)

The method of claim 1 wherein the compound is 2-2-(dimethylamino)ethyl!-8,8-dipropyl-2-azaspiro4.5!decane.

### Claim 3 (depends on 1)

The method of claim 1 wherein the mammal is a human.

### Claim 4 (depends on 1)

The method of claim 1 wherein the mammal is afflicted with hyperlipidemic syndrome.

### Claim 5 (depends on 1)

The method of claim 1 wherein the mammal is afflicted with atherosclerosis.

### Claim 6 (depends on 1)

The method of claim 1 wherein the mammal is afflicted with transplant arteriolosclerosis.

### Claim 7 (depends on 1)

The method of claim 1 wherein the mammal is in need of lower cholesterol and triglyceride levels.

### Claim 8 (depends on 1)

The method of claim 1 wherein the mammal is in need of lower cholesterol levels.

### Claim 9 (depends on 1)

The method of claim 1 wherein the mammal is in need of lower triglyceride levels.

### Claim 10 (depends on 1)

The method of claim 1 wherein the mammal is in need of lower low-density lipoprotein levels.

### Claim 11 (depends on 1)

The method of claim 1 wherein the compound is administered orally.

### Claim 12 (depends on 11)

The method of claim 11 wherein from about 0.01 mg/kg to about 30 mg/kg of compound is administered per day.

### Claim 13 (depends on 1)

The method of claim 1 wherein the compound is administered parenteraly.

### Claim 14 (depends on 13)

The method of claim 13 wherein from about 0.01 mg/kg to about 30 mg/kg of compound is administered per day.

### Claim 15

A pharmaceutical composition comprising a compound of the structure: ##STR5## wherein: n is 1 or 2;
R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen or straight chain, branched chain or cyclic alkyl, provided that the total number of carbon atoms contained in R.sub.1 and R.sub.2 when taken together is 0-10; or R.sup.1 and R.sup.2 are joined together to from a cyclic alkyl group having 3-7 carbon atoms; and
R.sup.3 and R.sup.4 are the same or different and are selected from hydrogen or methyl; or a pharmaceutically acceptable salt, hydrate or solvate thereof; and a pharmaceutically acceptable carrier.

### Claim 16 (depends on 15)

A composition according to claim 15 wherein the compound is 2-2-(dimethylamino)ethyl!-8,8 -dipropyl-2-azaspiro4.5!decane.

### Claim 17 (depends on 15)

A composition according to claim 15 wherein the mammal being treated is a human.

### Claim 18 (depends on 15)

A composition according to claim 15 wherein the mammal is afflicted with hyperlipidemic syndrome.

### Claim 19 (depends on 15)

A composition according to claim 15 wherein the mammal is afflicted with atherosclerosis.

### Claim 20 (depends on 15)

A composition according to claim 15 wherein the mammal is afflicted with transplant arteriolosclerosis.

### Claim 21 (depends on 15)

A composition according to claim 15 wherein the mammal is in need of lower cholesterol and triglyceride levels.

### Claim 22 (depends on 15)

A composition according to claim 15 wherein the mammal is in need of lower cholesterol levels.

### Claim 23 (depends on 15)

A composition according to claim 15 wherein the mammal is in need of lower triglyceride levels.

### Claim 24 (depends on 15)

A composition according to claim 15 wherein the mammal is in need of lower low-density lipoprotein levels.

### Claim 25 (depends on 15)

A composition according to claim 15 wherein the compound is administered orally.

### Claim 26 (depends on 25)

A composition according to claim 25 wherein from about 0.01 mg/kg to about 30 mg/kg of compound is administered per day.

### Claim 27 (depends on 15)

A composition according to claim 15 wherein the compound is administered parenterally.

### Claim 28 (depends on 27)

A composition according to claim 27 wherein from about 0.01 mg/kg to about 30 mg/kg of compound is administered per day.

### Claim 29

A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of the structure ##STR6##
