# US 5,703,085 A · Xanthine derivatives

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- Number: US 5,703,085 A
- Document ID: US5703085A
- Status: Granted
- Kind: A
- Application number: 08/537,770
- Filed: 1995-10-20
- Granted: 1997-12-30
- Earliest claimed: 1994-02-23
- Assignees: Kyowa Hakko Kogyo Co., Ltd.
- Inventors: Fumio Suzuki; Nobuaki Koike; Junichi Shimada; Joji Nakamura; Shizuo Shiozaki; Shigeto Kitamura; Shunji Ichikawa; Hiroshi Kase; Hiromi Nonaka
- Web page: https://patentgrep.com/patent/US5703085A

## CPC

- C07D 473/06: with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention relates to novel xanthine derivatives and pharmaceutically acceptable salts thereof, represented by Formula (I): ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, R.sup.4 represents lower alkyl, or substituted or unsubstituted aryl, R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, and lower alkoxy, or R.sup.5 and R.sup.6 are combined together to represent --O--(CH.sub.2)p--O-- (p is an integer of 1 to 3), n represents 0, 1, or 2, and m represents 1 or 2. The compounds of the present invention have an adenosine A.sub.2 receptor antagonistic activity, and are useful for the treatment or prevention of various kinds of diseases caused by hyperergasia of adenosine A.sub.2 receptors (for example, Parkinson's disease, senile dementia, depression, asthma, and osteoporosis).

## Claims

### Claim 1

A xanthine derivative represented by Formula (I) or its pharmaceutically acceptable salt: ##STR33## wherein R.sup.1 and R.sup.2 independently represent lower alkyl, lower alkenyl, or lower alkynyl; R.sup.3 represents hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; R.sup.4 represents lower alkyl, or aryl which is optionally substituted with 1 to 4 substituents independently selected from the group consisting of lower alkyl, hydroxy, lower alkoxy, halogen, nitro, amino, lower alkylamino, di-lower alkylamino, benzyloxy, phenyl and phenoxy, wherein said lower alkyl substituent and lower alkoxy substituent are each optionally substituted with 1 to 3 substituents independently selected from the group consisting of halogen, nitro, lower alkoxy and amino; R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, or lower alkoxy, or R.sup.5 and R.sup.6 are combined together to represent --O--(CH.sub.2).sub.p --O-- (where p is an integer of 1 to 3); n represents 0, 1 or 4; and m represents 1 or 2, with the proviso that R.sup.1 and R.sup.2 are not methyl.

### Claim 2 (depends on 1)

A compound of claim 1 wherein R.sup.1, R.sup.2, and R.sup.3 independently represent lower alkyl or lower alkenyl.

### Claim 3 (depends on 1)

A compound of claim 1 wherein R.sup.3 represents lower alkyl.

### Claim 4 (depends on 3)

A compound of claim 3 wherein R.sup.1 and R.sup.2 independently represent ethyl, propyl or allyl.

### Claim 5 (depends on 4)

A compound of claim 4 wherein R.sup.3 represents methyl.

### Claim 6 (depends on 5)

A compound of claim 5 wherein R.sup.4 represents methyl, ethyl, tert-butyl or phenyl.

### Claim 7 (depends on 6)

A compound of claim 6 wherein R.sup.5 and R.sup.6 independently represent hydrogen, methoxy, or R.sup.5 and R.sup.6 are combined together to represent --O--CH.sub.2 --O--.

### Claim 8 (depends on 2)

A compound of claim 2, wherein R.sup.3 represents lower alkyl.

### Claim 9 (depends on 1, 2, 3, 4, 5, 6, 7, 8)

A method for treatment of Parkinson's disease, comprising:
selecting a pharmaceutical composition containing at least one of the compounds of claims 1 to 7 or 8 and a pharmaceutically acceptable excipient; and
administering said composition to a patient in need thereof.

### Claim 10 (depends on 1, 2, 3, 4, 5, 6, 7, 8)

A composition comprising at least one of the compounds of claims 1 to 7 or 8 and a pharmaceutically acceptable carrier.

### Claim 11 (depends on 1, 2, 3, 4, 5, 6, 7, 8)

A method of producing a pharmaceutical composition, comprising the steps of:
selecting a compound according to any of claims 1 to 7 or 8, and
blending said compound with a pharmaceutically acceptable excipient.

### Claim 12 (depends on 1, 2, 3, 4, 5, 6, 7, 8)

A method of treating depression, comprising
selecting a pharmaceutical composition containing at least one of the compounds of claims 1 to 7 or 8 and a pharmaceutically acceptable excipient; and
administering said composition to a patient in need thereof.