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    • 6. 发明申请
    • OXINDOLE COMPOUNDS CARRYING A NITROGEN-BOUND SPIRO SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSIN-RELATED DISEASES
    • 携带氮离子螺旋体替代物的氧化合物及其用于治疗相关疾病的用途
    • US20150329551A1
    • 2015-11-19
    • US14713909
    • 2015-05-15
    • AbbVie Deutschland GmbH & Co. KG
    • Hervé GenesteWilfried HornbergerKatja JantosAndreas KlingMarcel Van Gaalen
    • C07D487/10
    • C07D471/10C07D295/135C07D305/08C07D487/10
    • The present invention relates to novel substituted oxindole derivatives of the formula I wherein A is a ring selected from phenyl and 6-membered hetaryl containing 1 or 2 nitrogen atoms as ring members, where ring A carries one substituent R6 and optionally one substituent R7; B is a ring selected from phenyl and a monocyclic or bicyclic heteroaromatic ring containing 1, 2 or 3 heteroatoms selected from O, N and S as ring members, where ring B may carry 1, 2 or 3 substituents R8; X1, X2, X3 and X4, independently of each other, are selected from —CH2—, —O—, —S(O)c—, —NH—, —C(O)—, —CH2CH2—, —CH2O—, —OCH2—, —S(O)cCH2—, —CH2S(O)c—, CH2NH—, —NHCH2—, —CH2C(O)— and C(O)CH2—; X5 is NH, CH2 or O; and wherein c, R1, R2, (R3)a, (R4)b, R5, R6, R7, and R8 are as defined in the claims. The present invention also relates to pharmaceutical compositions comprising the novel substituted oxindole derivatives of the formula I, and to their use for the treatment of vasopressin-related disorders
    • 本发明涉及式I的新的取代羟吲哚衍生物,其中A是选自苯基和含有1或2个氮原子作为环成员的6元杂芳基的环,其中环A携带一个取代基R6和任选的一个取代基R7; B是选自苯基和含有1,2或3个选自O,N和S的环成员的单环或双环杂芳族环的环,其中环B可以带有1,2或3个取代基R8; X1,X2,X3和X4彼此独立地选自-CH 2 - , - O - , - S(O)c - , - NH - , - C(O) - , - CH 2 CH 2 - ,-OCH 2 - , - S(O)cCH 2 - , - CH 2 S(O)c - ,CH 2 NH - , - NHCH 2 - , - CH 2 C(O) - 和C(O) X 5是NH,CH 2或O; 并且其中c,R 1,R 2,(R 3)a,(R 4)b,R 5,R 6,R 7和R 8如权利要求中所定义。 本发明还涉及包含式I的新型取代的羟吲哚衍生物的药物组合物及其用于治疗加压素相关疾病的用途