公开(公告)号：US07452908B2

公开(公告)日：2008-11-18

申请号：US10838340

申请日：2004-05-05

申请人： Yufu Sagara ,  Minaho Uchiyama ,  Akira Naya ,  Toshifumi Kimura ,  Tomoshige Numazawa ,  Toru Fujikawa ,  Norikazu Otake ,  Kazuhito Noguchi

发明人： Yufu Sagara ,  Minaho Uchiyama ,  Akira Naya ,  Toshifumi Kimura ,  Tomoshige Numazawa ,  Toru Fujikawa ,  Norikazu Otake ,  Kazuhito Noguchi

IPC分类号： A61K31/445 ,  C07D211/32

CPC分类号： C07D401/12 ,  C07D207/16 ,  C07D211/26 ,  C07D401/14 ,  C07D471/10 ,  C07D493/10

摘要： This invention relates to compounds which are represented by the general formula [I] [in which A stands for a group of the following formula [ao] or [b0] Ar1, Ar2 and Ar3 stand for optionally substituted phenyl; k stands for 0 or 1; m, n and s stand for 0, 1 or 2; R1 stands for hydrogen or optionally substituted lower alkyl; R2, R3, R4 and R5 either stand for hydrogen or optionally substituted lower alkyl, or R2 and R3, or R4 and R5 together stand for trimethylene and the like; R60 stands for hydrogen, alkyl, or the like; R61 and R71 either stand for alkyl and the like, or together stand for trimethylene and the like; X stands for carbonyl or methylene; Y stands for nitrogen or methine; and Q− stands for anion], and the like. The compounds of the invention exhibit selective antagonism to muscarinic M3 receptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.

摘要翻译： 本发明涉及由通式[I]表示的化合物[其中A代表下列通式[a]或[b] 0 Ar 1，Ar 2和Ar 3代表任选取代的苯基; k代表0或1; m，n和s代表0,1或2; R 1表示氢或任选取代的低级烷基; R 2，R 3，R 4和R 5均代表氢或任选取代的低级烷基，或 R 2和R 3，或R 4和R 5一起代表三亚甲基等; R 60代表氢，烷基等; R 61和R 71均代表烷基等，或一起代表三亚甲基等; X代表羰基或亚甲基; Y代表氮或次甲基; 和Q ^{代表阴离子]等。 本发明的化合物对毒蕈碱M 3受体表现出选择性拮抗作用，因此可用作治疗呼吸，泌尿和消化系统疾病的副作用小的安全有效的药剂。}

公开(公告)号：US06809108B1

公开(公告)日：2004-10-26

申请号：US10031716

申请日：2002-03-26

申请人： Yufu Sagara ,  Minaho Uchiyama ,  Akira Naya ,  Toshifumi Kimura ,  Tomoshige Numazawa ,  Toru Fujikawa ,  Norikazu Otake ,  Kazuhito Noguchi

发明人： Yufu Sagara ,  Minaho Uchiyama ,  Akira Naya ,  Toshifumi Kimura ,  Tomoshige Numazawa ,  Toru Fujikawa ,  Norikazu Otake ,  Kazuhito Noguchi

IPC分类号： A61K31445

CPC分类号： C07D401/12 ,  C07D207/16 ,  C07D211/26 ,  C07D401/14 ,  C07D471/10 ,  C07D493/10

摘要： This invention relates to compounds which are represented by the general formula [I] [in which A stands for a group of the following formula [a0] or [b0] Ar1, Ar2 and Ar3 stand for optionally substituted phenyl; k stands for 0 or 1; m, n and a stand for 0, 1 or 2; R1 stands for hydrogen or optionally substituted lower alkyl; R2, R3, R4 and R5 either stand for hydrogen or optionally substituted lower alkyl, or R2 and R3, or R4 and R5 together stand for trimethylene and the like; R60 stands for hydrogen, alkyl, or the like; R61 and R71 either stand for alkyl and the like, or together stand for trimethylene and the like; X stands for carbonyl or methylene; Y stands for nitrogen or methine; and Q− stands for anion], and the like. The compounds of the invention exhibit selective antagonism to muscarinic M3 receptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.

摘要翻译： 本发明涉及由通式[I]表示的化合物[其中A代表下式[a0]或[b0] Ar 1的基团，Ar 2和Ar 3代表 任选取代的苯基; k代表0或1; m，n和a代表0,1或2; R 1代表氢或任选取代的低级烷基; R 2，R 3，R 4和R 5分别代表氢或任选取代的低级烷基，或者R 2和R 3，或R 4和R 5， 一起代表三亚甲基等; R 60代表氢，烷基等; R 61和R 71代表烷基等，或一起代表三亚甲基等; X代表羰基或亚甲基; Y代表氮或次甲基; 并且Q 1表示阴离子]等。本发明的化合物对毒蕈碱性M3受体表现出选择性拮抗作用，因此可用作治疗副作用小的安全有效药物，用于治疗呼吸道，尿和尿的疾病 消化系统。