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12. 发明授权

EP2648731B1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 有权
标题翻译： CARBOXAMIDVERBINDUNGEN UND IHRE VERWENDUNG ALS CALPAIN-HEMMER V
公开(公告)号：EP2648731B1
公开(公告)日：2017-01-25
申请号：EP11796664.8
申请日：2011-12-08
申请人： Abbvie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , LAO, Yanbin , BACKFISCH, Gisela , NIJSEN, Marjoleen
IPC分类号： A61K31/4439 , C07D401/04 , A61P25/28
CPC分类号： C07D401/04 , A61K31/4439 , C07D401/14 , Y02A50/411
摘要： 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 R1, R2, R3, R4, X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R2 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or CH2—C(O)OCH3, R3 and R4 independently of one another are halogen, CN, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.
摘要翻译：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，R 3，R 4，X，m和n具有权利要求书和说明书中所述的含义，其互变异构体，其水合物和药学上合适的盐它们。在这些化合物中，优选其中R 1为任选取代的苄基或杂芳基 - 甲基，X为单键或氧原子，R 2为C 1 -C 4烷基，C 1 -C 4卤代烷基，C 2 -C 4 - 烯基，C 3 -C 6 环烷基，C 3 -C 6 - 环烷基-C 1 -C 2 - 烷基，C 3 -C 6 - 杂环烷基-C 1 -C 2烷基，苯基，苯基-C 1 -C 3烷基，吡啶-2-基-C 1 -C 3 - 烷基或CH 2 -C（O）OCH 3，R 3和R 4彼此独立地是卤素，CN，CF 3，CHF 2，CH 2 F，C 1 -C 2烷基或C 1 -C 2烷氧基，m和n彼此独立地为0或1。

13. 发明公开

EP2970328A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 失效
标题翻译： NEUARTIGE INHIBITORVERBINDUNGEN DER PHOSPHODIESTERASE TYP 10A
公开(公告)号：EP2970328A1
公开(公告)日：2016-01-20
申请号：EP14709320.7
申请日：2014-03-12
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： JANTOS, Katja , OCHSE, Michael , GENESTE, Hervé , FROGGETT, Jayne , JAKOB, Clarissa , DRESCHER, Karla , DINGES, Jürgen
IPC分类号： C07D495/04 , A61K31/5025 , A61P25/00
CPC分类号： C07D495/04
摘要： 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.
摘要翻译：本发明涉及式I化合物，N-氧化物，互变异构体，前药及其药学上可接受的盐：在式I中，变量X1是CH或N，X2是O或S，并且其中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。

14. 发明公开

EP2922842A2 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 无效
标题翻译：化合物作为磷酸二酯酶10A型抑制剂
公开(公告)号：EP2922842A2
公开(公告)日：2015-09-30
申请号：EP13798625.3
申请日：2013-11-25
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co KG
发明人： GENESTE, Hervé , TURNER, Sean , OCHSE, Michael , DRESCHER, Karla , BLACK, Lawrence A. , JANTOS, Katja , JAKOB, Clarissa
IPC分类号： C07D401/14 , A61K31/4353 , A61K31/4427 , C07D401/04 , C07D401/10 , C07D471/04 , C07D487/04 , A61P25/00
CPC分类号： C07D401/14 , C07D401/04 , C07D401/10 , C07D471/04 , C07D487/04
摘要： 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.

15. 发明公开

EP3988555A1 MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE 审中-实审
公开(公告)号：EP3988555A1
公开(公告)日：2022-04-27
申请号：EP21197248.4
申请日：2018-08-15
申请人： AbbVie Inc. , Abbvie Deutschland GmbH & Co. KG
发明人： BRAJE, Wilfried , DOHERTY, George , JANTOS, Katja , JI, Cheng , JUDD, Andrew , KUNZER, Aaron , MASTRACCHIO, Anthony , SONG, Xiaohong , SOUERS, Andrew , SULLIVAN, Gerard , TAO, Zhi-Fu , TESKE, Jesse , WANG, Xilu , WENDT, Michael , PENNING, Thomas , LAI, Chunqiu , KLING, Andreas , POHKLI, Frauke
IPC分类号： C07D515/22 , A61K31/395 , A61P35/00
摘要： The present disclosure provides for compounds of formula (I)

wherein A 2 , A 3 , A 4 , A 6 , A 7 , A 8 , A 15 , R A , R 5 , R 9 , R 10A , R 10B , R 11 , R 12 , R 13 , R 14 , R 16 , W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of formula (I).

16. 发明授权

EP2922842B1 INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 无效
标题翻译： VERBINDUNGEN ALS磷酸二酯酶类型10A-HEMMER
公开(公告)号：EP2922842B1
公开(公告)日：2017-06-14
申请号：EP13798625.3
申请日：2013-11-25
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co KG
发明人： GENESTE, Hervé , TURNER, Sean , OCHSE, Michael , DRESCHER, Karla , BLACK, Lawrence A. , JANTOS, Katja , JAKOB, Clarissa
IPC分类号： C07D401/14 , A61K31/4353 , A61K31/4427 , C07D401/04 , C07D401/10 , C07D471/04 , C07D487/04 , A61P25/00
CPC分类号： C07D401/14 , C07D401/04 , C07D401/10 , C07D471/04 , C07D487/04

18. 发明授权

EP2970328B1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 失效
标题翻译：新型的磷酸二酯酶抑制剂化合物10A
公开(公告)号：EP2970328B1
公开(公告)日：2017-04-26
申请号：EP14709320.7
申请日：2014-03-12
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： JANTOS, Katja , OCHSE, Michael , GENESTE, Hervé , FROGGETT, Jayne , JAKOB, Clarissa , DRESCHER, Karla , DINGES, Jürgen
IPC分类号： C07D495/04 , A61K31/5025 , A61P25/00
CPC分类号： C07D495/04

19. 发明公开

EP2726479A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
标题翻译： NEU抑制剂DEN磷酸二酯酶类型10A
公开(公告)号：EP2726479A1
公开(公告)日：2014-05-07
申请号：EP12731416.9
申请日：2012-06-28
申请人： AbbVie Deutschland GmbH & Co KG , AbbVie Inc.
发明人： GENESTE, Hervé , OCHSE, Michael , DRESCHER, Karla , BEHL, Berthold , LAPLANCHE, Loic , DINGES, Jürgen , JAKOB, Clarissa , JANTOS, Katja
IPC分类号： C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , A61K31/44
CPC分类号： C07D471/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling 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.
摘要翻译：本发明涉及新的羧酰胺化合物，含有它们的药物组合物及其在治疗中的用途。该化合物具有有价值的治疗性质，并且特别适用于治疗或控制选自神经障碍和精神疾病的医学病症，用于改善与此类疾病相关的症状并降低此类疾病的风险。

20. 发明公开

EP2648731A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 有权
标题翻译：甲酰胺化合物和它们作为钙蛋白酶抑制剂V选用
公开(公告)号：EP2648731A1
公开(公告)日：2013-10-16
申请号：EP11796664.8
申请日：2011-12-08
申请人： Abbvie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , LAO, Yanbin , BACKFISCH, Gisela , NIJSEN, Marjoleen
IPC分类号： A61K31/4439 , C07D401/04 , A61P25/28
CPC分类号： C07D401/04 , A61K31/4439 , C07D401/14 , Y02A50/411
摘要： 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 R1, R2, R3, R4, X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R2 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or CH2—C(O)OCH3, R3 and R4 independently of one another are halogen, CN, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.

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