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BICYCLIC INHIBITORS
专利权人:
KALVISTA FARMASYUTIKALZ LIMITED
发明人:
EDVARDS Khannakh Dzhoj (GB),ЭДВАРДС Ханнах Джой (GB),EVANS Devid Majkl (GB),ЭВАНС Дэвид Майкл (GB),DEJVI Rebekka Luiz (GB),ДЭЙВИ Ребекка Луиз (GB),RUKER Devid Filip (GB),РУКЕР Дэвид Филип (GB),KHYUISO
申请号:
RU2016108762
公开号:
RU0002672582C2
申请日:
2014.08.14
申请国别(地区):
RU
年份:
2018
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (I)Formula (I) in which W is selected from CH and N; X is selected from CH, CH2-CH2, CH = CH, N and NH; Y is selected from CH2, CH, N, NH and O; in which the bond between X and Y is either saturated, unsaturated or aromatic; B is selected from: i) a radical of formula II (II) and ii) a condensed 6,5- or 6,6-heteroaromatic bicyclic ring structure containing N and, optionally, one or two additional heteroatoms, which are independently selected from N, which is optionally monosubstituted with NR8R9; P is H and Q is -C(R20)(R21)NH2 or P is -C(R20)(R21)NH2 and Q is H; U and V, independently of each other, are selected from C and N, thus the aromatic ring containing U and V is phenyl, pyridine or pyridazine; R1 is absent provided that U is N; R2 is absent provided that V is N; or, if present, R1 and R2, independently of one another, are selected from H and alkyl; R3 is selected from H, alkyl, alkoxy, CN, halogen and CF3; A is selected from -(CH2)0-9-heteroaryl and -(CH2)0-9-aryl; R8 and R9 are H; R20 and R21, independently of each other, are selected from H and alkyl, which are directly related to plasma kallikrein activity.EFFECT: these compounds are potentially useful in the treatment of impaired visual acuity, diabetic retinopathy, macular edema, hereditary angioedema, diabetes, pancreatitis, cerebral haemorrhage, nephropathy, cardiomyopathy, neuropathy, inflammatory bowel disease, arthritis, inflammation, septic shock, hypotension, cancer, adult respiratory distress syndrome, disseminated intravascular coagulation, cardiopulmonary bypass surgery and bleeding from post operative surgery.22 cl, 5 tbl, 10 exИзобретение относится к соединениям формулы (I)Формула (I)в которой W выбирают из CH и N; X выбирают из CH, CH2-CH2, CH=CH, N и NH; Y выбирают из CH2, CH, N, NH и O; в которой связь между X и Y представляет собой либо насыщенную, либо ненасыщенную или ароматическую; B выбирают из: i) радикал форм
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http://www.ckcest.cn/home/
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