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SPIRO-5, 6-DIHYDRO-4H-2, 3, 5, 10B-TETRA-AZA-BENZO[E]AZULENES

2025-06-18 08:293370下载
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FIELD : medicine, pharmaceutics. SUBSTANCE : invention relates to spiro-5, 6-dihydro-4H-2, 3, 5, 10b-tetra-aza-benzo[e]azulene derivatives of formula I, where X-Y represents C(RaRb)-O, where each of Ra and Rb independently represents H or C1-4-alkyl, C(RcRd)-S(O)p, where each of Rc and Rd independently represents H, C(O)O, CH2OCH2, CH2CH2O, Z represents CH or N; R1 represents halogeno, R2 represents H, C1-6-alkyl, non-substituted or having as substituents one OH, -(CH2)q-Re, where Re represents pyridyl, -C(O)-C1-6-alkyl, -C(O)(CH2)qNRiRii, -C(O)O-C1-6-alkyl, -S(O)2NRiRii, each of Ri and Rii independently represents C1-6-alkyl, R3 represents Cl or F, n has value 1 or 2, m has value 0, 1, p has value 0 or 2, q has value 1, or to their pharmaceutically acceptable salts. Invention also relates to pharmaceutical composition, possessing antagonistic activity with respect to receptors V1a, on the basis of said compounds. EFFECT : obtained are novel compounds and pharmaceutical composition on their basis, which can be applied in medicine as drugs of peripheral and central action in case of the following states : dysmenorrhea, male or female sexual disfunction, hypertension, chronic heart failure, inadequate secretion of vasopressin, liver cirrhosis, nephritic syndrome, anxiety, depressive disorders, obsessive-compulsive disorder, autism spectrum disorders, schizophrenia and aggressive behaviour. 20 cl, 10 tbl, 37 ex


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