# US 5,348,950 A · Platinum(II) complex and antitumor agent

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- Number: US 5,348,950 A
- Document ID: US5348950A
- Status: Granted
- Kind: A
- Application number: 07/894,779
- Filed: 1992-06-05
- Granted: 1994-09-20
- Earliest claimed: 1991-06-10
- Assignees: Toray Industries, Inc.
- Inventors: Go Hata; Tatsuya Kaneko; Hideki Kawai; Masato Mutoh; Hideyuki Hashimoto
- Web page: https://patentgrep.com/patent/US5348950A

## CPC

- C07F 15/0093: {without a metal-carbon linkage}
- A61P 35/00: Antineoplastic agents
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A platinum(II) complex represented by the general formula (A), ##STR1## in which R.sub.1 represents a hydrocarbon radical having 1 to 10 carbon atoms, R.sub.2 and R.sub.3 each represent a hydrogen atom or a hydrocarbon radical of 1 to 10 carbon atoms, or R.sub.2 and R.sub.3, together, may form --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --, and X and Y each represent an ammonia molecule or a monodentate amine having 1 to 7 carbon atoms or X and Y, together, may form a bidentate diamine having 2 to 10 carbon atoms. The compounds are useful for treating a tumor.

## Claims

### Claim 1

A platinum(II) complex represented by the general formula (A), ##STR18## in which R.sub.1 represents an aliphatic hydrocarbon radical having 1 to 10 carbon atoms, R.sub.2 and R.sub.3 each represent a hydrogen atom or an aliphatic hydrocarbon radical having 1 to 10 carbon atoms, or R.sub.2 and R.sub.3, together, may form --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --, and X and Y each represent an ammonia molecule or an aliphatic primary amine having 1 to 10 carbon atoms or X and Y, together, may form a diamine selected from the group consisting of unsubstituted 1,2-diaminoethane, 1,3-diaminopropane, 1,4-diaminobutane and 2-aminomethylpyridine, and 1,2-diaminoethane, 1,3-diaminopropane, 1,4-diaminobutane and 2-aminomethylpyridine substituted by an aliphatic hydrocarbon radical or aliphatic hydrocarbon ether radical having 1 to 10 carbon atoms.

### Claim 2 (depends on 1)

A complex set forth in claim 1, wherein R.sub.1 is alkyl having 1 to 10 carbon atoms, alkenyl having 2 to 10 carbon atoms, cycloalkyl having 3 to 10 carbon atoms, or cycloalkylalkyl having 4 to 10 carbon atoms and R.sub.2 and R.sub.3 are independently hydrogen, alkyl having 1 to 10 carbon atoms, alkenyl having 2 to 10 carbon atoms, cycloalkyl having 3 to 10 carbon atoms, or cycloalkylalkyl having 4 to 10 carbon atoms.

### Claim 3 (depends on 1)

A complex as set forth in claim 1, wherein R.sub.1 is methyl.

### Claim 4 (depends on 1)

A complex as set forth in claim 1, wherein R.sub.2 is hydrogen or methyl.

### Claim 5 (depends on 1)

A complex as set forth in claim 1, wherein R.sub.3 is hydrogen or methyl.

### Claim 6 (depends on 1)

An agent for treating tumor comprising an effective amount of platinum(II) complex as defined in claim 1 in a pharmaceutically acceptable vehicle.

### Claim 7 (depends on 6)

An agent as set forth in claim 6, wherein R.sub.1 is methyl.

### Claim 8 (depends on 6)

An agent as set forth in claim 6, wherein R.sub.2 is hydrogen or methyl.

### Claim 9 (depends on 6)

An agent as set forth in claim 6, wherein R.sub.3 is hydrogen or methyl.

### Claim 10 (depends on 1)

A complex as defined in claim 1 wherein said amine is selected from the group consisting of n-propylamine, iso-propylamine, n-butylamine, n-hexylamine, n-octylamine, cyclopropylamine, cyclobutylamine, cyclopentylamine and cyclohexylamine.

### Claim 11 (depends on 1)

A complex as set forth in claim 1, wherein x and y each represent an ammonia molecule or an aliphatic primary amine having alkyl having 1 to 10 carbon atoms, alkenyl having 2 to 10 carbon atoms, cycloalkyl having 3 to 10 carbon atoms, or cycloalkylalkyl having 4 to 10 carbon atoms.

### Claim 12

A platinum(II) complex represented by the general formula: ##STR19## in which R.sub.1 represents an aliphatic hydrocarbon radical having 1 to 10 carbon atoms, R.sub.2 and R.sub.3 each represent a hydrogen atom or an aliphatic hydrocarbon radical having 1 to 10 carbon atoms, or R.sub.2 and R.sub.3, together, form --(CH.sub.2).sub.4 -- or (CH.sub.2).sub.5 --, R.sub.4 and R.sub.5 each represent a hydrogen atom or an aliphatic hydrocarbon radical or aliphatic hydrocarbon ether radical having 1 to 6 carbon atoms, the carbon atoms of the moiety ##STR20## being not more than 10, or R.sub.4 and R.sub.5, together, form --(CH.sub.2).sub.l --, in which l is an integer of 3 to 5, or --(CH.sub.2 ).sub.2 --O--(CH.sub.2).sub.2 --, and m is 1 or 2.

### Claim 13

An agent for treating tumor comprising an anti-tumor effective amount of platinum(II) complex represented by the general formula: ##STR21## in which R.sub.1 represents an aliphatic hydrocarbon radical having 1 to 10 carbon atoms, R.sub.2 and R.sub.3 each represent a hydrogen atom or an aliphatic hydrocarbon radical having 1 to 10 carbon atoms, or R.sub.2 and R.sub.3, together, form --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --, R.sub.4 and R.sub.5 each represent a hydrogen atom or an aliphatic hydrocarbon radical or aliphatic hydrocarbon ether radical having 1 to 6 carbon atoms, the carbon atoms or the moiety ##STR22## being not more than 10, or R.sub.4 and R.sub.5, together, form --(CH.sub.2).sub.l --, in which l is an integer of 3 to 5, or --(CH.sub.2 ).sub.2 --O--(CH.sub.2).sub.2 --, and m is 1 or 2 is a pharmaceutically acceptable vehicle.