Antineoplastic .alpha.-methylene-.gamma.-butyrolactones

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514242, 544182, 544313, 544314, 544312, 544311, C07D23954, C07D239553, A61K 31505

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active

059624604

ABSTRACT:
The present invention provides antineoplastic .alpha.-methylene-.gamma.-butyrolactones represented by the general one or two groups selected from the group consisting of halide, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, phenyl, nitro and amino;.sub.2 R represents hydrogen, halide, (C.sub.1 -C.sub.4)alkyl or benzyl; X represents N; or wherein R.sub.1 is a phenyl group optionally substituted with one or two groups selected from the group consisting of halide, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4) alkoxy, nitro and amino; R.sub.2 represents Cl, F, or benzyl; X represents CH. These .alpha.-methylene-.gamma.-butyrolactones may be administered with an inert diluent or with a pharmaceutically acceptable carrier in controlling the growth of a neoplasm in a patient afflicted with a neoplasm disease. ##STR1##

REFERENCES:
Huang, B. et al. Chemical Abstract, No. 121:245284, the abstract of Gaoxiong Yixue Kexue Zazhi, vol. 9, pp. 707-711, published in 1993 (Nov. 1994).
Huang, B. et al. Chemical Abstract, No. 116:128491, the abstract of Zhonghua Yaoxue Zazhi, vol. 43, pp. 447-455, published in 1991 (Mar. 1992).
Winograd, B. Oxford Textbook of Oncology, vol. 1, ed. by Peckham, M, et al. (Oxford University Press, Oxford), pp. 486-495 (1995).
Workman, P. et al. Oxford Textbook of Oncology, vol. 1, ed. by Peckham, M. et al. (Oxford University Press, Oxford), pp. 495-513 (1995).
Crilley, P.A. et al. Basic Pharmacology in Medicine, ed. by DiPalma, J.R. et al. (Medical Surveillance Inc., West Chester), pp. 659-661 (1994).
Cleton, F.J. Oxford Textbook of Oncology, vol. 1, ed. by Peckham, M. et al. (Oxford University Press, Oxford), pp. 445-453 (1995).

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