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US 5,700,825 AGranted
Radiosensitizing diamines and their pharmaceutical preparations
AssigneeFlorida State University
InventorsKurt G. Hofer, Li-xi Yang
Life of this patent
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AssigneeFlorida State University
InventorsKurt G. Hofer, Li-xi Yang
Estimating the term…
A compound comprising a diamine containing from 2-4 electron-affinic radiosensitizing functional groups or a salt thereof is provided. In a preferred embodiment the compound has the formula ##STR1## wherein A comprises a carbon chain having from about 2-10 carbons in the chain, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are H, or T, T is ##STR2## wherein A' comprises a carbon chain having from about 1-8 carbons in the chain, R.sup.5 is H, lower alkyl, or halo, and R.sup.6 is H, lower alkyl, halo or nitro, provided that at least one of R.sup.1 and R.sup.2, and at least one of R.sup.3 and R.sup.4 is T. Intermediates for, pharmaceutical compositions containing, methods for making and methods for using such compounds to radiosensitize and kill hypoxic tumor cells are also provided.
A compound having the formula ##STR26## wherein A comprises a carbon chain having from about 4-10 carbons in the chain, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are ##STR27## wherein A' comprises a carbon chain having from about 1-8 carbons in the chain, R.sup.5 is H, lower alkyl, or halo, and R.sup.6 is H, lower alkyl, halo or nitro, or a salt of said compound.
A compound having the formula ##STR28## wherein A comprises a carbon chain having from about 2-10 carbons in the chain, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are ##STR29## wherein A' comprises a carbon chain having from about 1-8 carbons in the chain, R.sup.5 is H, lower alkyl, or halo, and R.sup.6 is H, lower alkyl, halo or nitro, or a salt of said compound.
A compound or a salt thereof, the compound having the formula:
A compound or a salt thereof, the compound being N, N'-di2'-(2-methyl-5-nitro-1-imidazolyl)ethyl!-1,4-butanediamine.
A compound or a salt thereof, the compound being N, N'-di2'-(2-methyl-5-nitro-1-imidazolyl)ethyl!-1,5-pentanediamine.
A compound or a salt thereof, the compound being N, N'-di2'-(2-methyl-5-nitro-1-imidazolyl)ethyl!-1,8-octanediamine.
A pharmaceutical composition for radiosensitizing hypoxic cells comprising a radiosensitizing amount of a compound or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable carrier, the compound having the formula ##STR32## wherein A comprises a carbon chain having from about 2-10 carbons in the chain, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are ##STR33## wherein A' comprises a carbon chain having from about 1-8 carbons in the chain, R.sup.5 is H, lower alkyl, or halo, and R.sup.6 is hydrogen, lower alkyl, halo or nitro.
A pharmaceutical composition for radiosensitizing hypoxic cells comprising a radiosensitizing amount of a compound or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable carrier, the compound having the formula:
Dependencies are inferred from the claim text.