公开(公告)号：US20070191337A1

公开(公告)日：2007-08-16

申请号：US11547874

申请日：2005-04-29

申请人： Alexander Ivashchenko ,  Vladimir Vvedensky ,  Aleksei Ilyin ,  Volodymyr Kysil ,  Alexander Khvat ,  Yulia Kuzovkova ,  Sergey Kutepov ,  Irina Dmitrieva ,  Denis Zolotarev ,  Sergey Tkachenko ,  Llya Okun ,  Dmitri Kravchenko ,  Vladimir Kobak ,  Andrei Trifilenkov ,  Yulia Mishunina ,  Marina Loseva ,  Elena Rizhova ,  Vladislav Parchinsky ,  Sergey Tsirulnikov ,  Alexandr Kyseley

发明人： Alexander Ivashchenko ,  Vladimir Vvedensky ,  Aleksei Ilyin ,  Volodymyr Kysil ,  Alexander Khvat ,  Yulia Kuzovkova ,  Sergey Kutepov ,  Irina Dmitrieva ,  Denis Zolotarev ,  Sergey Tkachenko ,  Llya Okun ,  Dmitri Kravchenko ,  Vladimir Kobak ,  Andrei Trifilenkov ,  Yulia Mishunina ,  Marina Loseva ,  Elena Rizhova ,  Vladislav Parchinsky ,  Sergey Tsirulnikov ,  Alexandr Kyseley

IPC分类号： A61K31/554 ,  A61K31/551 ,  A61K31/498 ,  C07D498/14 ,  C07D487/14

CPC分类号： C40B40/04 ,  A61K31/4985 ,  A61K31/5513 ,  A61K31/5517 ,  A61K31/554 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14 ,  C07D493/14 ,  C07D495/14 ,  C07D513/04

摘要： This invention relates to novel annellated carbamyl-aza-heterocyclic compounds that are potential physiologically active compounds (agonists, antagonists, and receptor modulators, enzyme inhibitors, oncolytics, antibacterial and antiparasitic agents, and so on), to a focused library comprising annellated carbamyl-aza-heterocyclic compounds, a pharmaceutical composition comprising annellated carbamyl-aza-heterocyclic compounds as the active ingredient, and to methods of producing and using the same. The invention relates to annellated carbamyl-aza-heterocyclic compounds of general formula 1: wherein: W is 6-oxopiperazine, [1,4]diazepan, [1,4]thiazepan or [1,4]oxazepan compound annellated to at least one optionally substituted and optionally condensed heterocyclic compound Q; R1, R2 and R3 are, independently of one another, a hydrogen atom, an inert substituent, an optionally substituted C1-C6 alkyl, an optionally substituted C3-C8 cycloalkyl, an optionally substituted phenyl, an optionally substituted aryl, or an optionally substituted heterocyclyl; and Q is a pyrrole, pyrazole, imidazole, thiazole, pyrrolidine, indole, benzofuran, 4,5,6,7-tetrahydrobenzothiophene, thieno[3,2-b]pyrrole, furo[3,2-b]pyrrole, thieno[2,3-b]pyrrole, benzimidazole, pyridine, quinoline, or 1,2,3,4-tetrahydroisoquinoline cyclic compound.

摘要翻译： 本发明涉及一种聚焦文库的新型环状氨基甲酰基 - 氮杂杂环化合物，其是潜在的生理活性化合物（激动剂，拮抗剂，受体调节剂，酶抑制剂，溶瘤剂，抗细菌剂和抗寄生虫剂等） 氮杂杂环化合物，包含环状氨基甲酰基 - 氮杂杂环化合物作为活性成分的药物组合物及其制备和使用方法。 本发明涉及通式1的环状氨基甲酰基 - 氮杂杂环化合物：其中：W是6-氧代哌嗪，[1,4]二氮杂环庚烷，[1,4]硫杂环庚烷或[1,4]氧氮杂环素化合物，其至少一个 任选取代的和任选稠合的杂环化合物Q; R 1，R 2和R 3彼此独立地为氢原子，惰性取代基，任选取代的C