Gold complexes
AssigneeNational University of Singapore
InventorsPak Hing Leung, Soh Ha Chan, Yongcheng Song
Life of this patent
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Abstract
Novel phosphino-gold (I) compounds, a process for their preparation, pharmaceutical compositions containing such phosphino-gold (I) compounds and their use in the treatment of cancer disease.
Claims49
A phosphino-gold(I) compound of formula (1):
- 5
- wherein R1, R2, R3, R4 and R5, each of which may be the same or different, are selected from the group consisting of hydrogen, optionally substituted alkyl, aryl, alkenyl, alkynyl, hydroxyalkyl, alkoxy, aryloxy, carboxyalkyl, alkoxycarbonyl, hydroxy, alkylthio, alkylsulfinyl and alkylsulfonyl;
- Z is hydrogen or a functional group;
- Y is hydrogen or a functional group;
- W is hydrogen or a functional group;
- and
- X is a halogen or C(F)3 or C(CI)3;
- in an optically active or racemic form;
- or salt thereof:
A phosphino-gold(I) compound of formula (II)
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- wherein R1=aryl or alkyl
- R2=aryl or alkyl
- R3=aryl or alkyl
- R4=aryl or alkyl
- R5=aryl or alkyl
- Z=H or functional group
- Y=H or functional group
- W=H or functional group
- X=halogen or C(F3) or C(CI)3 in an optically active or racemic form;
- or a salt thereof.
A process for the preparation of a phosphinogold(I) compound of formula (I)
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- wherein R1, R2, R3, R4 and R5, each of which may be the same or different, are selected from the group consisting of hydrogen, optionally substituted alkyl, aryl, alkenyl, alkynyl, hydroxyalkyl, alkoxy, aryloxy, carboxyalkyl, alkoxycarbonyl, hydroxy, alkylthio, alkylsulfinyl and alkylsulfonyl;
- Z is hydrogen or a functional group;
- Y is hydrogen or a functional group;
- W is hydrogen or a functional group;
- and
- X is a halogen C(F)3 or C(CI)3;
- in an optically active or racemic form;
- or a salt thereof;
- which process comprises reacting a compound of formula (III) with a halo gold(I) compound to form a phosphino-gold(I) compound
- 8
- wherein R1, R2, R3, R4 and R5, each of which may be the same or different, are selected from the group consisting of hydrogen, optionally substituted alkyl, aryl, alkenyl, alkynyl, hydroxyalkyl, alkoxy, aryloxy, carboxyalkyl, alkoxycarbonyl, hydroxy, alkylthio, alkylsulfinyl and alkylsulfonyl;
- Z is hydrogen or a functional group;
- Y is hydrogen or a functional group;
- and
- W is hydrogen or a functional group;
A pharmaceutical composition comprising an effective amount of a phosphino-gold(I) compound of formula (I) in an optically active or racemic form, or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable diluent or carrier.
Use of a phosphino-gold(I) compound of formula (I) in an optically active or racemic form, or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the production of an anti-proliferative effect in a warm blooded animal.
Use of a phosphino-gold(I)compound of formula (I) in an optically active or racemic form, or a pharmaceutically acceptable salt for the production of an anti-proliferative effect in a warm blooded animal.
Use of a phosphinogold(I) compound of formula (I) in an optically active or racemic form, or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of cancer.
Use of a phosphino-gold(I) compound of formula (I) in an optically active or racemic form, or a pharmaceutically acceptable salt thereof in the treatment of cancer.
A process for producing an anti-proliferative effect in a warm-blooded animal in need of such treatment comprising
- administering to said animal an effective amount of a compound of a phosphinogold(I) compound of formula (I) in an optically active or racemic form, or a pharmaceutically-acceptable salt thereof.
A process for treating cancer of a patient comprising administering to said patient an effective amount of a phosphino-gold(I) compound of formula (I) in an optically active or racemic form, or a pharmaceutically-acceptable salt thereof.
Dependencies are inferred from the claim text.