Quinazolinone and benzoxazine derivatives as progesterone receptor modulators

作者: Eugene A. Terefenko , James P. Edwards , Puwen Zhang , Jay E. Wrobel , Todd K. Jones

DOI:

关键词:

摘要: This invention provides compounds which are agonists and antagonists of the progesterone receptor having general structure: wherein: R1 R2 independently selected from H, CORA, or NRBCORA, optionally substituted alkyl, alkenyl, alknyl, cycloalklyl, aryl, heterocyclic moieties; fused to form: 3 8 membered spirocyclic alkenyl rings; RA is H alkoxy, aminoalkyl groups; RB C1 C3 alkyl; R3 OH, NH2, CORC alkynyl; RC aminoalkyl; R4 halogen, CN, NO2, alkynyl, amino R5 an benzene five six ring with 1, 2, heteroatoms O, S, SO, SO2 NR6; R6 G1 NR7, CR7R8; G2 CO, CS, provided that when CR7R8, cannot both be R7 R8 moiety; pharmaceutically acceptable salt thereof, methods using these in mammals as receptor.

参考文章(86)
Hartmann Rj, Geller I, Effects of brofoxine, a new anxiolytic, on experimentally induced conflict in rats. Proceedings of the Western Pharmacology Society. ,vol. 21, pp. 51- ,(1978)
Bella Luigi C, Ermanno C, Aldo C, Franco c, Bojidar C, Contraceptive and menstrual cycle controlling drug having oncostatic properties ,(1991)
Atsumi Kamochi, Akihiko Yanagi, Hiroshi Miyauchi, Tadao Asami, Toyohiko Kume, Toshio Goto, Herbicidal novel benzothiazolonyl pyrroles ,(1989)
L. Michael Kettel, Ana A. Murphy, Joseph F. Mortola, James H. Liu, Andre Ulmann, Samuel S.C. Yen, Endocrine responses to long-term administration of the antiprogesterone RU486 in patients with pelvic endometriosis. Fertility and Sterility. ,vol. 56, pp. 402- 407 ,(1991) , 10.1016/S0015-0282(16)54531-2