Quinoline derivatives, their production and use

Details Quinoline derivatives, their production and use Quinoline derivatives, their production and use

1997-01-07

1998-09-15

Huang, Evelyn

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546156, A61K 3147, C07D21556

Patent

active

058078690

ABSTRACT:
The present quinoline derivatives and compositions having gonadotropin-releasing hormone antagonistic activity are useful as propylactics or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, uterine or cervical cancer, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; are effective as a fertility controlling agent in both sexes (e.g. a pregnancy controlling agent and a menstrual cycle controlling agent); can be used as a male or female contraceptive, as an ovulation-inducing agent; can be used as an infertility treating agent by using a rebound effect owing to a stoppage of administration thereof; and are useful for modulating estrous cycles in animals in the field of animal husbandry, as agents for improving the quality of edible meat or promoting the growth of animals, and as agents for promoting spawning in fish.

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Reissmann TH et al. Human Reproduction, 10 (8), 1974-1981, 1995.
P. M. Gillis et al., "Synthesis and Antibacterial Evaluation of Chem., No. 3, 1978, pp. 265-269.
R. J. Bienstock et al., "Conformational Analysis of a Highly Potent Dicyclic Gonadotropin-Releasing Hormone Antagonist by Nuclear Magnetic Resonance and Molecular Dynamics", J. Med. Chem. vol. 36, (1993), pp. 3265-3273.
Seirigaku 2, Bunkodo, (1986), pp. 610-618., {English abstract}.
Receptor Kiso to Risho, Asakurashoten, (1993), pp. 297-304., {English abstract}.

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