Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-03-31
1997-12-23
Dees, Jose G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5483137, A61K 31415, C07D23395, C07D23391
Patent
active
057008256
ABSTRACT:
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.
REFERENCES:
patent: 4282232 (1981-08-01), Agrawal
patent: 4323689 (1982-04-01), Vogel et al.
patent: 4371540 (1983-02-01), Lee et al.
patent: 4456610 (1984-06-01), Hofheinz et al.
patent: 4462992 (1984-07-01), Agrawal et al.
patent: 4665191 (1987-05-01), Waddill et al.
patent: 4995898 (1991-02-01), Nasu et al.
patent: 5073566 (1991-12-01), Lifer et al.
patent: 5073639 (1991-12-01), Suto
patent: 5215738 (1993-06-01), Lee et al.
patent: 5236944 (1993-08-01), Distelmans et al.
patent: 5270330 (1993-12-01), Suzuki et al.
patent: 5371101 (1994-12-01), Itoh et al.
patent: 5389661 (1995-02-01), Sircar et al.
Hay et al., Hypoxia-selective antitumor agents. 10. Bis (nitroimidazoles) and related Bis(nitroheterocycles): Development of derivatives with higher rates of metabolic activation under hypoxia and improved aqueous solubility. J. Med. Chem., vol. 38, No. 11, pp. 1928-1941; May 26, 1995.
Gatenby et al., "Oxygen Distribution in Squamous Cell Carcinoma Metastases And Its Relationship to Outcome of Radiation Therapy", Int. J. Radiat. Oncol. Biol. Phys.14; 831-822(1988).
Berg and Sharp, "Derivatives of 4- and 5-nitro-2-methylimidazol-1-yl-acetaldehyde", European Journal of Med. Chemistry 10:171-177 (1975).
Huang and Swern, "Oxidation of Long-Chain and Related Alcohols to Carbonyls by Dimethyl Sulfoxide Activated by Oxalyl Chloride.sup.1 ", J. Organic Chemistry 43:2480-2482 (1978).
Holley et al., Biochem. Pharmacology, 43(4) 763-769 (1992).
Carminati et al., Biochem. Pharmacology, 38(14) 2253-2258 (1989).
Hofer Kurt G.
Yang Li-Xi
Cross Laura R.
Dees Jos,e G.
Florida State University
LandOfFree
Radiosensitizing diamines and their pharmaceutical preparations does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Radiosensitizing diamines and their pharmaceutical preparations, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Radiosensitizing diamines and their pharmaceutical preparations will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1803094