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公开(公告)号：EP3112362B1
公开(公告)日：2018-09-26
申请号：EP15756097.0
申请日：2015-02-26
发明人： OGAWA, Seiji , WATANABE, Toshihide , SUGIMOTO, Isamu , TANI, Kousuke , MORIYUKI, Kazumi , GOTO, Yoshikazu , YAMANE, Shinsaku
IPC分类号： C07D407/04 , A61K31/352 , A61K31/427 , A61K31/4709 , A61P1/00 , A61P1/04 , A61P1/16 , A61P7/00 , A61P11/00 , A61P13/12 , A61P15/00 , A61P17/14 , A61P19/04 , A61P19/08 , A61P25/00 , A61P27/02
CPC分类号： C07D417/04 , A61K45/06 , C07D407/04 , C07D417/12
摘要： To provide an excellent selective EP2 agonist in a safe manner. A compound represented by general formula (I): (wherein all symbols are as defined in the specification), a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has a selective EP2 agonist activity and is highly safe, and is therefore useful as a drug, especially as a therapeutic agent for EP2 receptor-related diseases including immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases, cartilage injury and others.
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公开(公告)号：EP3409658A1
公开(公告)日：2018-12-05
申请号：EP17744379.3
申请日：2017-01-27
IPC分类号： C07C229/46 , A61K31/197 , A61K31/397 , A61K31/402 , A61K31/472 , A61K31/55 , A61P21/00 , A61P25/00 , A61P25/18 , A61P25/28 , A61P27/02 , A61P31/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D205/04 , C07D207/16 , C07D217/04 , C07D217/16 , C07D223/06
CPC分类号： A61K31/197 , A61K31/397 , A61K31/402 , A61K31/472 , A61K31/55 , C07C229/46 , C07D205/04 , C07D207/16 , C07D217/04 , C07D217/16 , C07D223/06 , C07D223/16 , C07D405/12
摘要： A compound shown by general formula (I-1) (in the formula, all symbols are as stated in the specification.) has selective S1P5 receptor-binding activity. Adjusting this activity make s it possible to obtain a therapeutic agent for S1P5-mediated diseases, for example, neurod egenerative diseases such as schizophrenia and Binswanger's disease.
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公开(公告)号：EP4431157A2
公开(公告)日：2024-09-18
申请号：EP24190856.5
申请日：2019-02-21
发明人： WATANABE, Toshihide , KUSUMI, Kensuke , IMAIDE, Satomi , ENDO, Toshimitsu , KOMIYA, Takaki , TSUBURAYA, Naomi
IPC分类号： A61P43/00
CPC分类号： A61P37/06 , C07D205/04 , C07D207/16 , C07D403/04 , Y02P20/55
摘要： Provided is a compound in which the balance of the agonist activity against the S1P5 receptor relative to the SIPi receptor has been improved in order to develop a pharmaceutical useful for the treatment of S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases. This compound represented by general formula (V) (in the formula, all symbols are as defined in the specification) has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic for SIPs-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.
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公开(公告)号：EP3327018B1
公开(公告)日：2020-11-25
申请号：EP16827875.2
申请日：2016-07-22
发明人： OGAWA, Seiji , WATANABE, Toshihide , SUGIMOTO, Isamu , TANI, Kousuke , MORIYUKI, Kazumi , GOTO, Yoshikazu , YAMANE, Shinsaku
IPC分类号： C07D417/04 , C07D417/14 , C07D409/04 , C07D407/04 , A61K31/427 , A61K31/352 , A61K31/381 , A61K31/428 , A61P27/02 , A61P27/06 , A61P27/10 , A61P27/12
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公开(公告)号：EP3327018A1
公开(公告)日：2018-05-30
申请号：EP16827875.2
申请日：2016-07-22
发明人： OGAWA, Seiji , WATANABE, Toshihide , SUGIMOTO, Isamu , TANI, Kousuke , MORIYUKI, Kazumi , GOTO, Yoshikazu , YAMANE, Shinsaku
IPC分类号： C07D407/04 , A61K31/352 , A61K31/381 , A61K31/427 , A61K31/428 , A61P1/04
CPC分类号： C07D417/04 , A61K31/352 , A61K31/381 , A61K31/427 , A61K31/428 , C07D407/04 , C07D409/04 , C07D417/14
摘要： Provided is an EP2 agonist having excellent safety. A compound represented by general formula (I)
(wherein all symbols are as defined in the description), a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has an EP2 agonist activity and is highly safe, and is therefore useful as a medicine, particularly a therapeutic agent for diseases associated with EP2 receptors, such as immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases and cartilage injury.-
6.发明公开COMPOUND EXHIBITING SELECTIVE EP2 AGONIST ACTIVITY 审中-公开VERBINDUNG MIT SELEKTIVER EP2-AGONISTISCHERAKTIVITÄT
公开(公告)号：EP3112362A1
公开(公告)日：2017-01-04
申请号：EP15756097.0
申请日：2015-02-26
发明人： OGAWA, Seiji , WATANABE, Toshihide , SUGIMOTO, Isamu , TANI, Kousuke , MORIYUKI, Kazumi , GOTO, Yoshikazu , YAMANE, Shinsaku
IPC分类号： C07D407/04 , A61K31/352 , A61K31/427 , A61K31/4709 , A61P1/00 , A61P1/04 , A61P1/16 , A61P7/00 , A61P11/00 , A61P13/12 , A61P15/00 , A61P17/14 , A61P19/04 , A61P19/08 , A61P25/00 , A61P27/02
CPC分类号： C07D417/04 , A61K45/06 , C07D407/04 , C07D417/12
摘要： To provide an excellent selective EP2 agonist in a safe manner. A compound represented by general formula (I):
(wherein all symbols are as defined in the specification), a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has a selective EP2 agonist activity and is highly safe, and is therefore useful as a drug, especially as a therapeutic agent for EP2 receptor-related diseases including immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases, cartilage injury and others.摘要翻译： 以安全的方式提供优异的选择性EP2激动剂。 由通式（I）表示的化合物（其中所有符号如说明书中所定义），化合物的盐或N-氧化物，或化合物或其盐或N-氧化物的溶剂合物或前药具有选择性 EP2激动剂活性高度安全，因此可用作药物，特别是作为EP2受体相关疾病的治疗剂，包括免疫疾病，过敏性疾病，神经元死亡，痛经，早产，流产，秃发，眼部疾病，勃起 功能障碍，关节炎，肺损伤，肺纤维化，肺气肿，支气管炎，慢性阻塞性肺病，骨病，软骨损伤等。
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