1073435-67-2Relevant academic research and scientific papers
The condensed heterocyclic derivative and its intermediate
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Paragraph 0027, (2018/05/03)
Provided are an industrially useful method for producing a fused-heterocyclic derivative or salt thereof which is useful as a preventive agent, therapeutic agent, reproductive adjustment agent, contraceptive, ovulation-inducing agent, or sex-hormone-dependent-cancer-post-operation-recurrence preventive agent which target sex-hormone-dependent diseases and the like such as prostate enlargement, uterine myoma, endometriosis, uterine fibroma, precocious puberty, amenorrhea, premenstrual syndrome, dysmenorrhea, polycystic ovary syndrome, lupus erythematosus, hypertrichosis, dwarfism, sleep disorders, acne, baldness, Alzheimer's disease, infertility, irritable bowel syndrome, prostate cancer, uterine cancer, ovarian cancer, breast cancer, and pituitary tumors; and a production intermediate thereof. The present invention makes it possible to produce a compound or salt thereof represented by general formula (A) in high yield and purity by using a compound represented by general formula (D) (R1 and R2 represent identical or different C1-6 alkyl groups, and R3 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a nitro group).
NITROGENATED FUSED RING DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND USE OF THE SAME FOR MEDICAL PURPOSES
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Page/Page column 23, (2010/01/29)
[Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, -OW1, -SW1, -COW2, -NW3W4, -SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, -CO-Y, -SO2-Y -S-(alkylene)-Y, -O-(alkylene)-Y, -SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.
