06-02-2020 дата публикации
Номер: US20200039921A1
Принадлежит:
The present invention provides novel antifibrinilytic compounds, processes for their preparation, pharmaceutical and veterinary compositions thereof, and their use in medicine, in particular for the treatment of bleeding. 1. A compound of formula III:{'br': None, 'sup': 1', '1', '5, 'sub': '2', 'R—CH—X—R\u2003\u2003(III)'} [{'sup': 1', '6', '6', '7', '+', '6', '7', '8', '+', '9', '10, 'sub': '2', 'Ris —NH, —NHR, NRR—NRRRor —SRR;'}, {'sup': 5', '12', '13', '14', '15, 'sub': '2', 'Ris —C(O)R, —SOR, —P(O)RR, nitro or nitroso;'}, {'sup': 6', '7', '9', '10', '6', '7, 'sub': 1', '4', '1', '4, 'R, R, R8, Rand Rare independently (C-C)alkyl or halo(C-C)alkyl, or Rand R, together with the N atom to which they are attached form an aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, or pyrrolyl group;'}, {'sup': 12', '13', '14', '15, 'sub': 1', '4', '1', '4, 'R, R, Rand Rare independently hydroxyl, —O—(C-C)alkyl or —(C-C)alkyl; and'}, {'sup': '1', 'Xis trans cyclohexan-1,4-diyl;'}, {'sup': 1', '2, 'sub': '2', 'with the proviso that Rin not NHwhen Ris COOH, or'}, 'a pharmaceutically acceptable salt thereof., 'wherein2. The compound of claim 1 , of formula IIIa:{'br': None, 'sup': 9', '10', '+', '5, 'sub': '2', 'RRS—CH—X—R\u2003\u2003(IIIa)'}or a pharmaceutically acceptable salt thereof.3. The compound of claim 1 , of formula IIIb:{'br': None, 'sup': 9', '10', '+', '1', '12, 'sub': '2', 'RRS—CH—X—C(O)R\u2003\u2003(IIIb)'}or a pharmaceutically acceptable salt thereof.4. The compound of claim 1 , wherein Ris hydroxyl or —O—(C-C)alkyl or a pharmaceutically acceptable salt thereof.5. The compound of claim 4 , wherein Ris hydroxyl claim 4 , or a pharmaceutically acceptable salt thereof.6. The compound according to claim 1 , wherein. Rand Rare independently (C-C)alkyl or halo(C-C)alkyl claim 1 , or a pharmaceutically acceptable salt thereof.7. The compound of claim 6 , wherein Rand Rare both methyl claim 6 , or a pharmaceutically acceptable salt thereof. This application claims priority ...
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