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Beta-lactam vasopressin v1a antagonists
专利权人:
Inc.;Azevan Pharmaceuticals
发明人:
BRUNS, Robert,GUILLON, Christophe D.,HEINDEL, Ned,KOPPEL, Gary,LU, Shifang,MILLER, Marvin
申请号:
ES02776210
公开号:
ES2666188T3
申请日:
2002.10.11
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
Compound that has the formula ** (See formula) ** where: n is an integer from 0 to 2; A is XNH- or R5XN-, where R5 is selected from the group consisting of hydroxy, C1-C6 alkyl, C1-C4 alkoxycarbonyl and benzyl and where X is optionally substituted aryl (C1-C4 alkyl); A 'is R5'X'N-, where R5' and X 'are taken together with the nitrogen atom to which they are attached to form a piperidinyl optionally substituted in position 4 by hydroxy, C1-C6 alkyl, C3-C8 cycloalkyl , C1-C4 alkoxy, (C1-C4 alkoxy) carbonyl, hydroxy (C1-C4 alkoxy) (C1-C4 alkyl), R7R8N-, R7R8N- (C1-C4 alkyl), phenyl, phenyl (C1-C4 alkyl), optionally substituted phenyl (C1-C4 alkyl), furyl (C1-C4 alkyl), pyridinyl (C1-C4 alkyl), thienyl (C1-C4 alkyl) or piperidin-1-yl (C1-C4 alkyl); R2 is hydrogen or C1-C6 alkyl; R3 is oxazolidin-2-on-3-yl-4-substituted; R4 is optionally substituted arileten-1-yl; R7 is hydrogen or C1-C6 alkyl; R8 is C1-C6 alkyl, C3-C8 cycloalkyl, optionally substituted aryl or optionally substituted aryl (C1-C4 alkyl) or R7 and R8 are taken together with the nitrogen atom to which they are attached to form a heterocycle selected from the group consisting in pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl and homopiperazinyl; wherein said piperazinyl or homopiperazinyl is optionally N-substituted by R12; R12 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, C1-C4 alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aryl (C1-C4 alkyl) and optionally substituted aryloyl and hydrates, solvates and salts of addition of pharmaceutically acceptable acids thereof.Compuesto que tiene la fórmula **(Ver fórmula)** donde: n es un número entero de 0 a 2; A es XNH- o R5XN-, donde R5 se selecciona del grupo que consiste en hidroxi, alquilo C1-C6, alcoxicarbonilo C1-C4 y bencilo y donde X es aril(alquilo C1-C4) opcionalmente sustituido; A' es R5'X'N-, donde R5' y X' se toman junto con el átomo de nitrógeno al que están unidos p
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