PYRAZOLOPYRIMIDONE OR PYRROLOTRIAZONE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL APPLICATIONS THEREOF

FIELD: chemistry.SUBSTANCE: present invention relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof having the properties of gonadotropin-releasing hormone (GnRH) antagonists. In formula (I)when G is N, D is C and E is CH-; when G is C, D and E are N; Ris selected...

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Hauptverfasser: GUJ Bin, LYUJ Khetszyun, SUN Pyaoyan, DUN Tsin
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: chemistry.SUBSTANCE: present invention relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof having the properties of gonadotropin-releasing hormone (GnRH) antagonists. In formula (I)when G is N, D is C and E is CH-; when G is C, D and E are N; Ris selected from the group consisting of phenyl and pyridazinyl, wherein independently of each other, each of phenyl and pyridazinyl is optionally further substituted with one or more groups selected from the group consisting of halogen and -OR; Ris C-Calkyl, wherein C-Calkyl is further substituted with phenyl, wherein phenyl is optionally further substituted with one or more groups selected from the group consisting of halogen, C-Calkyl and C-Chaloalkyl; Ris phenyl, wherein the phenyl is optionally further substituted with one or more groups selected from the group consisting of -NRR, -NHC(O)R, -NHC(O)OR, -NHC(O)NHRand -NHC(O)NHOR; Ris C-Calkyl; Ris hydrogen; Ris selected from the group consisting of hydrogen and C-Calkyl; independently of each other, each Rand Ris selected from the group consisting of hydrogen and C-Calkyl; n is 1, 2, 3, or 4. Invention also relates to versions of the method of producing a compound of formula (I), intermediates of formula (IVc) and formula (IB) for obtaining a compound of formula (I) and methods for production thereof.,.EFFECT: compounds can be used in preparation of medicaments for the treatment or prevention of diseases associated with the GnRH receptor, where the disease is selected from a group of sex-hormone dependent cancer, bone metastasis of sex hormone-dependent cancer, prostatic hypertrophy, uterine fibroids, endometriosis, uterine fibroids, precocious puberty, amenorrhea, premenstrual syndrome, dysmenorrhea, multilocular ovary syndrome, polycystic ovary syndrome, acne, alopecia, Alzheimer's disease, infertility, irritable bowel syndrome, benign or malignant tumours that are hormone-independent and sensitive to luteinizing hormone-release hormone (LH-RH), or flushes; to obtain a reproductive regulator, a birth control pill, an ovulation evacerator; or for the preparation of medicaments for the prevention of postoperative relapse of a sex hormone-dependent cancer selected from the group consisting of prostate cancer, uterine cancer, breast cancer and pituitary cancer.22 cl, 7 tbl, 18 ex Настоящее изобретение относится к новому соединению формулы (I) или его фармацевтически приемлемой соли, обладающему свойствами антагонистов гона