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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 i> 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。
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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。
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公开(公告)号:US07192969B2
公开(公告)日:2007-03-20
申请号:US10983613
申请日:2004-11-09
申请人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
发明人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号: A61K31/46 , C07D451/02
CPC分类号: C07D207/08 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10
摘要: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].
摘要翻译: 本发明涉及具有选择性毒蕈碱M 3受体拮抗作用,副作用小,适用于吸入治疗的化合物,并且可用作通式(I)的呼吸系统疾病的治疗剂; [其中A表示由式(a
0 SUB>)或(b 0>)表示的组; Ar表示任选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2,R 3和R 4表示低级烷基,单键或与B 1连接的亚烷基,或 R 2和R 3结合起来表示亚烷基; R 5和R 7表示氢,低级烷基或键合到B 2的单键或亚烷基; R 6表示氢,低级烷基或以-N(R 8)R 9表示的基团; 和X - 表示阴离子]。 -
公开(公告)号:US20070129397A1
公开(公告)日:2007-06-07
申请号:US11648614
申请日:2007-01-03
申请人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
发明人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号: A61K31/46 , C07D451/00 , C07D211/34 , A61K31/445 , A61K31/40 , C07D207/04
CPC分类号: C07D207/08 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10
摘要: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X−signifies an anion].
摘要翻译: 本发明涉及具有选择性毒蕈碱M 3受体拮抗作用,副作用小,适用于吸入治疗的化合物,并且可用作通式(I)的呼吸系统疾病的治疗剂; [其中A表示由式(a
0 SUB>)或(b 0>)表示的组; Ar表示任选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2,R 3和R 4表示低级烷基,单键或与B 1连接的亚烷基,或 R 2和R 3结合起来表示亚烷基; R 5和R 7表示氢,低级烷基或键合到B 2的单键或亚烷基; R 6表示氢,低级烷基或以-N(R 8)R 9表示的基团; 和X - 表示阴离子]。 -
公开(公告)号:US07504432B2
公开(公告)日:2009-03-17
申请号:US11648614
申请日:2007-01-03
申请人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
发明人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号: A01N43/36 , C07D207/00
CPC分类号: C07D207/08 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10
摘要: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].
摘要翻译: 本发明涉及具有选择性毒蕈碱M3受体拮抗作用,副作用小,适用于吸入治疗的化合物,并且可用作通式(I)的呼吸系统疾病的治疗剂; [其中A表示由式(a0)或(b0)表示的组; Ar表示任选取代的芳基或杂芳基; B1和B2表示脂族烃; R1表示氟取代的环烷基; R2,R3和R4表示低级烷基,单键或与B1键合的亚烷基,或者R2和R3相连,表示亚烷基; R5和R7表示氢,低级烷基或键合到B2的单键或亚烷基; R6表示氢,低级烷基或表示为-N(R8)R9的基团; 和X-表示阴离子]。
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公开(公告)号:US20050065211A1
公开(公告)日:2005-03-24
申请号:US10983613
申请日:2004-11-09
申请人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
发明人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号: A61P11/00 , A61P11/06 , A61P27/16 , A61P43/00 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/08 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10 , C07D498/10 , A61K31/445 , A61K31/24 , C07C229/52
CPC分类号: C07D207/08 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10
摘要: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].
摘要翻译: 本发明涉及具有选择性毒蕈碱M3受体拮抗作用,副作用小,适用于吸入治疗的化合物,并且可用作通式(I)的呼吸系统疾病的治疗剂; [其中A表示由式(a0)或(b0)表示的组; Ar表示任选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2,R 3和R 4表示低级烷基,单键或与B 1键合的亚烷基,或R 2和R 3一起表示亚烷基; R 5和R 7表示氢,低级烷基或与B 2键合的单键或亚烷基; R 6表示氢,低级烷基或以-N(R 8)R 9表示的基团; 而X - 表示阴离子]。
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公开(公告)号:US06846835B2
公开(公告)日:2005-01-25
申请号:US10332617
申请日:2001-07-10
申请人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
发明人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号: A61P11/00 , A61P11/06 , A61P27/16 , A61P43/00 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/08 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10 , C07D498/10 , A61K31/445 , A61K31/4465 , C07D211/04 , C07D221/02
CPC分类号: C07D207/08 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10
摘要: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].
摘要翻译: 本发明涉及具有选择性毒蕈碱性M3受体拮抗作用,副作用小,适用于吸入治疗的化合物,并且可用作通式(I)的呼吸系统疾病的治疗剂; [其中A表示一组表达 通式(a0)或(b0); Ar表示任选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2,R 3和R 4表示低级烷基,单键或与B 1键合的亚烷基,或R 2和R 3一起表示亚烷基; R 5和R 7表示氢,低级烷基或与B 2键合的单键或亚烷基; R 6表示氢,低级烷基或以-N(R 8)R 9表示的基团; 而X - 表示阴离子]。
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