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    • 4. 发明申请
    • NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
    • 新型的磷酸二酯酶抑制剂化合物10A
    • WO2014079995A2
    • 2014-05-30
    • PCT/EP2013/074532
    • 2013-11-25
    • ABBVIE INC.ABBVIE DEUTSCHLAND GMBH & CO. KG
    • GENESTE, HervéTURNER, SeanOCHSE, MichaelDRESCHER, KarlaBLACK, Lawrence A.JANTOS, Katja
    • C07D401/14A61K31/4353A61K31/4427C07D401/04C07D401/10C07D471/04C07D487/04
    • C07D401/14C07D401/04C07D401/10C07D471/04C07D487/04
    • The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders wherein Y 1 and Y 2 are adjacent atoms in Het 1 , which are independently selected from the group consisting of carbon and nitrogen; k is 0, 1, 2 or 3; Het 1 is a bivalent monocyclic 5- or 6-membered heteroaromatic radical, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N-R a as ring members, or a bivalent fused bicyclic 8-, 9- or 10-membered heteroaromatic radical, having 1, 2, 3 or 4 heteroatoms or heteroatom moieties selected from O, S, N and N-R a as ring members; Het 2 is inter alia monocyclic 5- or 6-membered hetaryl, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N-R 1a as ring members, Cyc is inter alia optionally substituted monocyclic 5- or 6-membered hetaryl or optionally substituted fused 8-, 9- or 10-membered bicyclic hetaryl; Ar is optionally substituted phenylene or optionally substituted bivalent 6-membered hetaryl; R is attached to a carbon atom of Het 1 and inter alia - halogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -alkoxy, C 1 -C 6 -fluoroalkyl, C 1 -C 6 -fluoroalkoxy, C 3 -C 6 -cycloalkyl etc.
    • 本发明涉及作为磷酸二酯酶10A型抑制剂的式I化合物及其盐等,并涉及它们在制备药物中的应用,因此适用于治疗或控制 选自神经障碍和精神障碍的医学病症,用于改善与这种病症相关的症状,以及用于降低这种病症的风险,其中Y 1和Y 2是相邻的原子 Het 1,它们独立地选自由碳和氮组成的组; k是0,1,2或3; Het 1是具有1,2或3个选自O,S,N和NR a的杂原子或杂原子部分的二价单环5-或6-元杂芳族基团,其为 环成员或具有1,2,3或4个选自O,S,N和NR a的杂原子或杂原子部分的二价稠合双环8,9或10元杂芳族基团作为 戒指成员; Het 2尤其是单环5-或6-元杂芳基,其具有1,2或3个选自O,S,N和NR 1a的杂原子或杂原子部分作为环 Cyc特别是任选取代的单环5-或6-元杂芳基或任选取代的稠合的8-,9-或10-元双环杂芳基; Ar是任选取代的亚苯基或任选取代的二价6-元杂芳基; R连接到Het 1 1的碳原子上,尤其是 - 卤素,C 1 -C 6 - 烷基,C≡2 C 6 -C 6 - 烯基,C 2 -C 6 - 炔基,C 1 -C 6 - C 1-6 - 烷氧基,C 1 -C 6 - 氟代烷基,C 1 -C 6 - 烷氧基,C 1 -C 6 - C 1-3 - 烷氧基,C 3-6 - 环烷基等。
    • 6. 发明申请
    • NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
    • 磷酸二酯酶类型10A的新型抑制剂化合物
    • WO2014140086A1
    • 2014-09-18
    • PCT/EP2014/054810
    • 2014-03-12
    • ABBVIE DEUTSCHLAND GMBH & CO. KGABBVIE INC.
    • JANTOS, KatjaOCHSE, MichaelGENESTE, HervéFROGGETT, JayneJAKOB, ClarissaDRESCHER, KarlaDINGES, Jürgen
    • C07D495/04A61K31/5025A61P25/00
    • C07D495/04
    • The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: (I). In formula I the variables X 1 is CH or N, X 2 is O or S and where R 1 , R 2 , R 3 , R 4 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    • 本发明涉及式I化合物,其N-氧化物,互变异构体,其前药及其药学上可接受的盐:(I)。 在式I中,变量X1是CH或N,X2是O或S,其中R1,R2,R3,R4和Q如权利要求中所定义。 式I化合物,N-氧化物,互变异构体,其前药和药学上可接受的盐是10A型磷酸二酯酶的抑制剂。 因此,本发明还涉及式I化合物,N-氧化物,互变异构体,前药和其药学上可接受的盐在制备药物中的用途,因此其适用于治疗或控制医学病症 选自神经障碍和精神障碍,用于改善与这种障碍相关的症状并降低这种障碍的风险。
    • 9. 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。