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公开(公告)号:US07799775B2
公开(公告)日:2010-09-21
申请号:US10590707
申请日:2005-02-25
申请人: Michitaka Sato , Teruaki Matsui , Akira Asagarasu , Hiroyuki Hayashi , Sei-ichi Araki , Satoru Tamaoki , Nobuyuki Takahashi , Yukinao Yamauchi , Yoshiko Yamamoto , Norio Yamamoto , Chisato Ogawa
发明人: Michitaka Sato , Teruaki Matsui , Akira Asagarasu , Hiroyuki Hayashi , Sei-ichi Araki , Satoru Tamaoki , Nobuyuki Takahashi , Yukinao Yamauchi , Yoshiko Yamamoto , Norio Yamamoto , Chisato Ogawa
IPC分类号: A01N43/54 , A01N43/90 , A01N43/04 , A01N43/58 , A01N43/60 , A61K31/54 , A61K31/505 , A61K31/519 , A61K31/535 , A61K31/675 , A61K31/50 , A61K31/495
CPC分类号: C07D495/14 , A61K31/496 , A61K31/4985 , A61K31/517 , A61K31/519 , A61K31/5395 , A61K45/06 , C07D401/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04 , A61K2300/00
摘要: This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X1 stands for hydrogen, lower alkyl, amino, etc., X2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0-4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT1A agonistic activity and 5-HT3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT1A agonistic activity and 5-HT3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT3 antagonistic agent which concurrently exhibits 5-HT1A agonistic activity, or administering 5-HT1A agonistic agent and 5-HT3 antagonistic agent simultaneously, in sequence or at an interval.
摘要翻译: 本发明提供下式所示的嘧啶衍生物,式中环A代表碳环基或杂环基,X1代表氢,低级烷基,氨基等,X2代表氢或低级烷基,Y代表直链 键或硫或氮,n表示0-4的整数,Ar表示下式的基团或其盐,其同时表现出5-HT1A激动活性和5-HT 3拮抗活性,并且可用于 治疗和治疗IBS等疾病。 本发明还提供了IBS的治疗方法,其特征在于在体内同时和协同地具有5-HT1A激动活性和5-HT3拮抗活性,其包括施用同时显示5-HT1A激动活性的5-HT3拮抗剂,或 同时按照或间隔施用5-HT1A激动剂和5-HT3拮抗剂。
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公开(公告)号:US20070197551A1
公开(公告)日:2007-08-23
申请号:US10590707
申请日:2005-02-25
申请人: Michitaka Sato , Teruaki Matsui , Akira Asagarasu , Hiroyuki Hayashi , Sei-ichi Araki , Satoru Tamaoki , Nobuyuki Takahashi , Yukinao Yamauchi , Yoshiko Yamamoto , Norio Yamamoto , Chisato Ogawa
发明人: Michitaka Sato , Teruaki Matsui , Akira Asagarasu , Hiroyuki Hayashi , Sei-ichi Araki , Satoru Tamaoki , Nobuyuki Takahashi , Yukinao Yamauchi , Yoshiko Yamamoto , Norio Yamamoto , Chisato Ogawa
IPC分类号: A61K31/497 , C07D239/06
CPC分类号: C07D495/14 , A61K31/496 , A61K31/4985 , A61K31/517 , A61K31/519 , A61K31/5395 , A61K45/06 , C07D401/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04 , A61K2300/00
摘要: This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X1 stands for hydrogen, lower alkyl, amino, etc., X2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0-4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT1A agonistic activity and 5-HT3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT1A agonistic activity and 5-HT3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT3 antagonistic agent which concurrently exhibits 5-HT1A agonistic activity, or administering 5-HT1A agonistic agent and 5-HT3 antagonistic agent simultaneously, in sequence or at an interval.
摘要翻译: 本发明提供由下式表示的嘧啶衍生物,式中,环A代表碳环基或杂环基,X 1代表氢,低级烷基,氨基等,X 2 代表氢或低级烷基,Y表示直接键或硫或氮,n表示0-4的整数,Ar表示下式的基团或其盐,其同时 表现出5-HT 1A激动活性和5-HT 3拮抗活性,并且可用于治疗和治疗诸如IBS的疾病。 本发明还提供IBS的治疗方法,其特征在于具有5-HT 1A激动活性和5-HT 3拮抗活性同时并且在体内协同作用,其包括 施用同时具有5-HT 1A激动活性的5-HT 3拮抗剂,或施用5-HT 1A激动剂和5-HT 同时按照或间隔进行。
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