公开(公告)号：US20050222175A1

公开(公告)日：2005-10-06

申请号：US10947995

申请日：2004-09-23

申请人： Dale Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar Reddy ,  Srinivasa Cheruku ,  Rosa Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

发明人： Dale Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar Reddy ,  Srinivasa Cheruku ,  Rosa Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

IPC分类号： A61K31/519 ,  C07D495/04 ,  C07D498/02

CPC分类号： C07D495/04

摘要： The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno [2,3-d]pyrimidine compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as pulmonary arterial hypertension, migraine, hypertension, disorders of the gastrointestinal tract, restenosis, asthma, obstructive airway disease, prostatic hyperplasia and priapism, anxiety, depression, schizophrenia, neural injury and stroke. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also provided.

摘要翻译： 本发明涉及5-HT受体拮抗剂。 公开了由式I表示的新型哌啶基氨基 - 噻吩并[2,3-d]嘧啶化合物及其用于治疗由5-HT受体直接或间接介导的疾病的合成和用途。 这些病症包括中枢神经系统疾病如肺动脉高压，偏头痛，高血压，胃肠道疾病，再狭窄，哮喘，阻塞性气道疾病，前列腺增生和阴茎异常勃起，焦虑，抑郁，精神分裂症，神经损伤和中风。 还提供了制备方法和新型中间体及其药用盐。

公开(公告)号：US20050222176A1

公开(公告)日：2005-10-06

申请号：US11075565

申请日：2005-03-08

申请人： Dale Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar Alla ,  Srinivasa Cheruku ,  Rosa Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

发明人： Dale Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar Alla ,  Srinivasa Cheruku ,  Rosa Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

IPC分类号： A61K31/519 ,  C07D495/04 ,  C07D498/02

CPC分类号： C07D495/04

摘要： The invention relates to 5-HT receptor modulators, particularly 5-HT2B antagonists. Novel piperidinylamino-thieno [2,3-d] pyrimidine compounds represented by Formula I, II and III, and uses thereof for treating conditions including pulmonary arterial hypertension, congestive heart failure, and hypertension.

摘要翻译： 本发明涉及5-HT受体调节剂，特别是5-HT 2BA拮抗剂。 由式I，II和III表示的新型哌啶基氨基 - 噻吩并[2,3-d]嘧啶化合物及其用于治疗包括肺动脉高压，充血性心力衰竭和高血压的病症的用途。