Pharmaceutical Gallium Compositions and Methods
AssigneeGenta Incorporated
InventorThomas N. Julian
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Abstract
Novel pharmaceutical gallium compositions, including gallium complexes having increased oral bioavailablity relative to uncomplexed gallium salts are disclosed. Such compositions are useful in the treatment of conditions and diseases in which inhibition of abnormally increased calcium resorption is desired, including cancer, hypercalcemia, osteoporosis, osteopenia and Paget's disease. Methods for preparation and treatment are also provided.
Claims20
A complex comprising a metal ion and a compound represented by structural formula I:
- 2-OH—Ar—CR1—NR2—R3—COOH I
- wherein 2-OH—Ar is an optionally substituted 2-hydroxyaryl;
- R1 is —OH or ═O;
- R2 is hydrogen, hydroxyl or an optionally substituted C1-C4 alkyl, C1-C4 alkoxy, or C2-C4 alkenyl;
- and
- R3 is an optionally substituted aryl, heteroaryl, cycloalkyl, heterocyclyl, C1-C24 alkyl, C2-C20 alkenyl, C2-C20 alkynl, C1-C10 alkylaryl, C1-C10 arylalkyl, C2-C10 alkenylaryl, C2-C10 arylalkenyl, C2-C10 alkynylaryl or C2-C10 arylalkynyl, which optionally is interrupted by O, N, S or any combination thereof.
A method for preparing a complex comprising reacting a metal ion with a compound represented by structural formula I:
- 2-OH—Ar—CR1—NR2—R3—COOH I
- wherein 2-OH—Ar is an optionally substituted 2-hydroxyaryl;
- R1 is —OH or ═O;
- R2 is hydrogen, hydroxyl or an optionally substituted C1-C4 alkyl, C1-C4 alkoxy, or C2-C4 alkenyl;
- and
- R3 is an optionally substituted aryl, heteroaryl, cycloalkyl, heterocyclyl, C1-C24 alkyl, C2-C20 alkenyl, C2-C20 alkynl, C1-C10 alkylaryl, C1-C10 arylalkyl, C2-C10 alkenylaryl, C2-C10 arylalkenyl, C2-C10 alkynylaryl or C2-C10 arylalkynyl, which optionally is interrupted by O, N, S or any combination thereof,
- under conditions sufficient to form said complex.
A composition comprising a metal ion, a compound represented by structural formula I:
- 2-OH—Ar—CR1—NR2—R3—COOH I
- wherein 2-OH—Ar is an optionally substituted 2-hydroxyaryl;
- R1 is —OH or ═O;
- R2 is hydrogen, hydroxyl or an optionally substituted C1-C4 alkyl, C1-C4 alkoxy, or C2-C4 alkenyl;
- and
- R3 is an optionally substituted aryl, heteroaryl, cycloalkyl, heterocyclyl, C1-C24 alkyl, C2-C20 alkenyl, C2-C20 alkynl, C1-C10 alkylaryl, C1-C10 arylalkyl, C2-C10 alkenylaryl, C2-C10 arylalkenyl, C2-C10 alkynylaryl or C2-C10 arylalkynyl, which optionally is interrupted by O, N, S or any combination thereof,
- and at least one pharmaceutically acceptable excipient.
A method for removing an unwanted metal ion from body tissue or blood comprising treating the body tissue or blood with a compound represented by structural formula I:
- 2-OH—Ar—CR1—NR2—R3—COOH I
- wherein 2-OH—Ar is an optionally substituted 2-hydroxyaryl;
- R1 is —OH or ═O;
- R2 is hydrogen, hydroxyl or an optionally substituted C1-C4 alkyl, C1-C4 alkoxy, or C2-C4 alkenyl;
- and
- R3 is an optionally substituted aryl, heteroaryl, cycloalkyl, heterocyclyl, C1-C24 alkyl, C2-C20 alkenyl, C2-C20 alkynl, C1-C10 alkylaryl, C1-C10 arylalkyl, C2-C10 alkenylaryl, C2-C10 arylalkenyl, C2-C10 alkynylaryl or C2-C10 arylalkynyl, which optionally is interrupted by O, N, S or any combination thereof, whereby the unwanted metal ion is removed from the body tissue or blood.
Dependencies are inferred from the claim text.