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公开(公告)号:US09181233B2
公开(公告)日:2015-11-10
申请号:US13040159
申请日:2011-03-03
IPC分类号: C07D235/04 , A61K31/4184 , C07D417/04 , C07D403/04 , C07D413/04
CPC分类号: C07D417/04 , A61K31/4184 , C07D235/04 , C07D403/04 , C07D413/04
摘要: The invention relates to novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
摘要翻译: 本发明涉及作为谷氨酰胺酰环化酶抑制剂的新型杂环衍生物(QC,EC 2.3.2.5)。 QC在氨释放下催化N-末端谷氨酰胺残基在焦谷氨酸(5-氧代 - 脯氨酰基,pGlu *)中的分子内环化,并且在释放水下将N-末端谷氨酸残基分子内环化成焦谷氨酸。
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公开(公告)号:US20110262388A1
公开(公告)日:2011-10-27
申请号:US13091276
申请日:2011-04-21
申请人: Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
发明人: Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
IPC分类号: A61K38/20 , C07D405/14 , C07D409/14 , C07D417/14 , C07D401/14 , C07D409/12 , C07D417/12 , A61K31/4184 , A61K31/428 , A61K31/433 , A61K31/4709 , A61K39/395 , A61K31/4409 , A61K38/21 , A61P35/00 , A61P25/18 , A61P35/04 , A61P17/06 , A61P29/00 , A61P25/00 , A61P5/00 , A61P25/28 , A61P9/10 , A61P19/02 , A61P9/00 , A61P15/08 , A61P3/00 , C07D235/08
CPC分类号: C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14
摘要: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
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公开(公告)号:US20110092501A1
公开(公告)日:2011-04-21
申请号:US12880369
申请日:2010-09-13
申请人: Ulrich Heiser , Daniel Ramsbeck , Robert Sommer , Antje Meyer , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
发明人: Ulrich Heiser , Daniel Ramsbeck , Robert Sommer , Antje Meyer , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
IPC分类号: A61K31/535 , C07D403/02 , A61K31/4184 , A61K31/454 , C07D401/02 , C07D413/14 , C07D471/04 , A61K31/437 , A61P35/00 , A61P29/00 , A61P25/00 , A61P35/04 , A61P3/00 , A61P5/00
CPC分类号: C07D403/04 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5355 , A61K31/5377 , A61K45/06 , C07D235/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
摘要翻译: 本发明涉及式(I)的新型吡咯烷衍生物:其中R1,R2和R3如本文所定义,作为谷氨酰胺酰环化酶抑制剂(QC,EC 2.3.2.5)。 QC在氨释放下催化N-末端谷氨酰胺残基在焦谷氨酸(5-氧代 - 脯氨酰基,pGlu *)中的分子内环化,并且在释放水下将N-末端谷氨酸残基分子内环化成焦谷氨酸。
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公开(公告)号:US08541596B2
公开(公告)日:2013-09-24
申请号:US13091276
申请日:2011-04-21
申请人: Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
发明人: Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
IPC分类号: A61K31/4184 , C07D235/08
CPC分类号: C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14
摘要: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
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公开(公告)号:US08486940B2
公开(公告)日:2013-07-16
申请号:US12880369
申请日:2010-09-13
申请人: Ulrich Heiser , Daniel Ramsbeck , Robert Sommer , Antje Meyer , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
发明人: Ulrich Heiser , Daniel Ramsbeck , Robert Sommer , Antje Meyer , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
IPC分类号: A61K31/535 , A61K31/497 , A61K31/42 , A61K31/415 , A61K31/40 , C07D211/06 , C07D265/30 , C07D241/02 , C07D263/02 , C07D233/02
CPC分类号: C07D403/04 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5355 , A61K31/5377 , A61K45/06 , C07D235/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
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公开(公告)号:US20080267912A1
公开(公告)日:2008-10-30
申请号:US12105874
申请日:2008-04-18
申请人: Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
发明人: Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
IPC分类号: A61K38/20 , C07D233/54 , A61K31/4164 , A61K38/21 , A61P31/00 , A61P3/00 , A61P9/00 , A61P25/00 , A61P35/00 , A61K31/4178 , A61K39/395
CPC分类号: C07D233/61 , C07D233/64 , C07D235/06 , C07D405/12 , C07D417/12
摘要: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
摘要翻译: 式(I)化合物,其用于疾病治疗的组合和用途,或其药学上可接受的盐,溶剂化物或多晶型物,包括所有互变异构体和立体异构体,其中:A表示和B,R 1,R R 3,R 4,R 4,R 5,R 6和Z 3, 在整个说明书和权利要求书中都是定义的。
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公开(公告)号:US08227498B2
公开(公告)日:2012-07-24
申请号:US12105874
申请日:2008-04-18
申请人: Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
发明人: Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
IPC分类号: A61K31/417 , C07D233/64 , C07D235/06
CPC分类号: C07D233/61 , C07D233/64 , C07D235/06 , C07D405/12 , C07D417/12
摘要: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
摘要翻译: 式(I)化合物,其用于疾病治疗的组合和用途,或其药学上可接受的盐,溶剂化物或多晶型物,包括所有互变异构体和立体异构体,其中:A表示和B,R1,R2,R3,R4,R5,R6 和Z如在说明书和权利要求书中所定义。
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公开(公告)号:US07803810B2
公开(公告)日:2010-09-28
申请号:US12045163
申请日:2008-03-10
IPC分类号: C07D471/04 , A61K31/437 , A61P25/00
CPC分类号: C07D471/04
摘要: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoisomers and polymorphs thereof wherein: R1 represents C2-8alkyl; C2-8alkenyl; —(C1-6alkyl)-aryl; —(C1-6alkyl)-heteroaryl; —(C1-6alkyl)-carbocyclyl; —(C1-6alkyl)-heterocyclyl; -aryl; -heteroaryl; -carbocyclyl or -heterocyclyl; wherein said aryl or heteroaryl groups may be optionally substituted by one or more substituents selected from, C1-4alkyl, C1-4-fluoroalkyl, C1-4alkoxy, C1-4-fluoroalkoxy, hydroxy, —SO2(C1-4alkyl), —SO2N(C1-4alkyl)(C1-4alkyl), —SOC1-4alkyl, —SOC3-6cycloalkyl —C(O)O(C1-4alkyl), benzyloxy and phenyl; and wherein said carbocyclyl and heterocyclyl groups may be optionally substituted by one or more substituents selected from —C1-4 alkyl, —C1-4 alkoxy, hydroxyl, halogen and oxo; R2 represents H; C1-4alkyl or halogen; R3 represents H; C1-4alkyl or halogen; and R4 represents H; C1-4alkyl or halogen.
摘要翻译: 式(I)的化合物,其用于疾病治疗的组合和用途,或其药学上可接受的盐或溶剂合物,包括所有互变异构体,立体异构体和多晶型物,其中:R1代表C2-8烷基; C2-8烯基; - (C 1-6烷基) - 芳基; - (C 1-6烷基) - 杂芳基; - (C 1-6烷基) - 碳环基; - (C 1-6烷基) - 杂环基; 芳基 杂芳基 碳环基或杂环基; 其中所述芳基或杂芳基可以任选地被一个或多个选自C 1-4烷基,C 1-4 - 氟烷基,C 1-4烷氧基,C 1-4 - 氟烷氧基,羟基,-SO 2(C 1-4烷基),-SO 2 N (C 1-4烷基)(C 1-4烷基),-SOC 1-4烷基,-SOC 3 - 6环烷基-C(O)O(C 1-4烷基),苄氧基和苯基; 并且其中所述碳环基和杂环基可任选被一个或多个选自-C 1-4烷基,-C 1-4烷氧基,羟基,卤素和氧代的取代基取代; R2表示H; C 1-4烷基或卤素; R3表示H; C 1-4烷基或卤素; 且R 4表示H; C 1-4烷基或卤素。
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公开(公告)号:US20120237475A1
公开(公告)日:2012-09-20
申请号:US13422619
申请日:2012-03-16
申请人: Ulrich Heiser , Daniel Ramsbeck
发明人: Ulrich Heiser , Daniel Ramsbeck
IPC分类号: A61K38/20 , A61K31/4184 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/454 , C07D417/14 , A61K31/541 , C07D405/14 , C07D409/14 , C07D403/14 , A61K31/496 , A61K33/14 , A61K39/395 , A61K38/21 , A61K31/4409 , A61K38/10 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/22 , A61P25/18 , A61P37/02 , A61P37/06 , A61P1/04 , A61P35/00 , A61P31/04 , A61P15/08 , A61P29/00 , A61P35/04 , A61P17/06 , A61P37/00 , A61P3/00 , A61P5/00 , A61P7/00 , A61P25/28 , A61P19/02 , A61P9/10 , A61P1/18 , A61P9/00 , C07D403/10
CPC分类号: C07D403/04 , A61K31/4184 , A61K31/4409 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K38/2026 , A61K38/21 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要: Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).
摘要翻译: 式(I)的新型杂环衍生物:或其药学上可接受的盐,溶剂化物或多晶型物,包括其所有互变异构体和立体异构体,其中R a,n,R 1和R 2如本文所定义,作为谷氨酰胺酰环化酶抑制剂(QC,EC2.3 .2.5)。
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公开(公告)号:US20080234313A1
公开(公告)日:2008-09-25
申请号:US12045163
申请日:2008-03-10
IPC分类号: A61K31/437 , C07D471/04 , A61P25/00
CPC分类号: C07D471/04
摘要: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoisomers and polymorphs thereof wherein: R1 represents C2-8alkyl; C2-8alkenyl; —(C1-6alkyl)-aryl; —(C1-6alkyl)-heteroaryl; —(C1-6alkyl)-carbocyclyl; —(C1-6alkyl)-heterocyclyl; -aryl; -heteroaryl; -carbocyclyl or -heterocyclyl; wherein said aryl or heteroaryl groups may be optionally substituted by one or more substituents selected from, C1-4alkyl, C1-4-fluoroalkyl, C1-4alkoxy, C1-4-fluoroalkoxy, hydroxy, —SO2(C1-4alkyl), —SO2N(C1-4alkyl)(C1-4alkyl), —SOC1-4alkyl, —SOC3-6cycloalkyl —C(O)O(C1-4alkyl), benzyloxy and phenyl; and wherein said carbocyclyl and heterocyclyl groups may be optionally substituted by one or more substituents selected from —C1-4 alkyl, —C1-4 alkoxy, hydroxyl, halogen and oxo; R2 represents H; C1-4alkyl or halogen; R3 represents H; C1-4alkyl or halogen; and R4 represents H; C1-4alkyl or halogen.
摘要翻译: 式(I)的化合物,其用于疾病治疗的组合和用途,或其药学上可接受的盐或溶剂合物,包括所有互变异构体,立体异构体和多晶型物,其中:R 1表示C 2- 8烷基; C 2〜C 8链烯基; - (C 1-6烷基) - 芳基; - (C 1-6烷基) - 杂芳基; - (C 1-6烷基) - 碳环基; - (C 1-6烷基) - 杂环基; 芳基 杂芳基 碳环基或杂环基; 其中所述芳基或杂芳基可以任选被一个或多个选自C 1-4 - 烷基,C 1-4 - 氟代烷基,C 1 - -4个烷氧基,C 1-4 1-4氟烷氧基,羟基,-SO 2(C 1-4烷基), - SO 2 N(C 1-4烷基)(C 1-4烷基),-SOC 1-4, 烷基,-SOC 3 -C 3-6环烷基-C(O)O(C 1-4烷基),苄氧基和苯基; 并且其中所述碳环基和杂环基可以任选被一个或多个选自-C 1-4烷基,-C 1-4烷氧基,羟基,卤素和 氧代 R 2表示H; C 1-4烷基或卤素; R 3表示H; C 1-4烷基或卤素; R 4表示H; C 1-4烷基或卤素。
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