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    • 4. 发明申请
    • CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V
    • 羧酰胺化合物及其作为钙抑制剂V
    • WO2013149800A1
    • 2013-10-10
    • PCT/EP2013/055291
    • 2013-03-14
    • ABBVIE DEUTSCHLAND GMBH & CO. KGABBVIE INC.
    • KLING, AndreasJANTOS, KatjaMACK, HelmutMÖLLER, AchimHORNBERGER, WilfriedBACKFISCH, GiselaLAO, YanbinNIJSEN, Marjoleen
    • C07D401/14C07D405/14C07D401/04C07D471/04C07D487/04A61K31/4439A61P25/00A61P31/00A61P33/00A61P35/00
    • C07D401/14C07D401/04C07D405/14C07D413/14C07D471/04C07D487/04C07D491/048C07D491/107
    • The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R 1 , R 2 and n have the meanings mentioned in the claims and the description, Y is a radical of the formulae (Y1) or (Y2) where # indicates the point of attachment of Y to the pyridine ring, R 3 , R 4 , R 5 , R y and m have the meanings mentioned in the claims and the description, A is is (CH 2 ) p with p being 1, 2, 3 or 4, where one or two hydrogen atoms may be replaced by a radical R 6 , where A is attached to the 3-or 4-positon of the pyrazole radical and R 6 has the meaning mentioned in the claims and the description; A 1 is (CH 2 )q with q being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C 1 -C 4 -alkyl; and A 2 is (CH 2 )r with r being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C 1 -C 4 -alkyl, provided that that r + q is 2, 3, 4, 5 or 6; their tautomers, the hydrates thereof, the pharmaceutically suitable salts of the carbox-amide compounds (I), the prodrugs of (I) and the pharmaceutically suitable salts of the prodrugs, tautomers or hydrates of (I).
    • 本发明涉及新的羧酰胺化合物及其用于制备药物的用途。 羧酰胺化合物是钙蛋白酶(钙依赖性半胱氨酸蛋白酶)的抑制剂。 因此,本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。 羧酰胺化合物是通式(I)的化合物,其中R 1,R 2和n具有权利要求书和描述中所述的含义,Y是式(Y1)或(Y2)的基团,其中#表示 Y连接到吡啶环,R3,R4,R5,Ry和m具有权利要求和说明书中提及的含义,A是(CH 2)p,其中p是1,2,3或4,其中一个或两个 氢原子可以被基团R6代替,其中A连接到吡唑基的3-或4-位,R6具有权利要求书和说明书中提到的含义; A 1是(CH 2)q,其中q是0,1,2或3,其中一个或两个氢原子可以被卤素或C 1 -C 4 - 烷基取代; 并且A 2为(CH 2)r,其中r为0,1,2或3,其中一个或两个氢原子可被卤素或C 1 -C 4 - 烷基取代,条件是该r + q为2,3,4,5 或6; 其互变异构体,其水合物,羧酰胺化合物(I)的药学上合适的盐,(I)的前药和(I)的前药,互变异构体或水合物的药学上合适的盐。
    • 9. 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
    • WO2015173393A1
    • 2015-11-19
    • PCT/EP2015/060763
    • 2015-05-15
    • ABBVIE DEUTSCHLAND GMBH & CO. KG
    • GENESTE, HervéHORNBERGER, WilfriedJANTOS, KatjaKLING, AndreasVAN GAALEN, Marcel
    • C07D471/10C07D487/10C07D295/135C07D305/08
    • 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 R 6 and optionally one substituent R 7 ;B is a ring selected from phenyland a monocyclic or bicyclic het- eroaromatic 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 R 8 ;X 1 , X 2 , X 3 and X 4 , independently of each other, are selected from -CH 2 -, -O-, -S(O) c -, -NH-, -C(O)-, -CH 2 CH 2 -,-CH 2 O-, -OCH 2 -, -S(O) c CH 2 -, -CH 2 S(O)c-, CH 2 NH-,-NHCH 2 -, -CH 2 C(O)-andC(O)CH 2 -;X 5 is NH,CH 2 or O,;and wherein c, R 1 , R 2 , (R 3 )a, (R 4 )b, R 5 , R 6 , R 7 , and R 8 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的新的取代的羟基吲哚衍生物,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作为环成员的杂原子的单环或双环环芳族环的环,其中环B可以带有1,2或3个取代基R8; X1,X2,X3 和X 4彼此独立地选自-CH 2 - , - O - , - S(O)c - , - NH - , - C(O) - , - CH 2 CH 2 - , - CH 2 O-,-OCH 2 - -S(O)cCH 2 - , - CH 2 S(O)c - ,CH 2 NH-, - NHCH 2 - , - CH 2 C(O) - 和C(O)CH 2 - ; X 5是NH,CH 2或O,并且其中c, R2,(R3)a,(R4)b,R5,R6,R7和R8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病症的用途。