公开(公告)号：US20120094990A1

公开(公告)日：2012-04-19

申请号：US12672762

申请日：2008-08-11

申请人： Atsushi Naganawa ,  Toshihiko Nagase

发明人： Atsushi Naganawa ,  Toshihiko Nagase

IPC分类号： A61K31/538 ,  A61P37/08 ,  A61P11/08 ,  A61P29/00 ,  A61P9/10 ,  A61P7/02 ,  A61P25/00 ,  A61P35/00 ,  A61P1/00 ,  A61P17/00 ,  A61P17/10 ,  C07D265/36 ,  A61P37/06

CPC分类号： C07D265/36 ,  A61K31/00 ,  A61K31/538 ,  A61K45/06 ,  A61K2300/00

摘要： A compound represented by formula (I), wherein R1 represents a hydrogen atom, etc., R2 and R3 each independently represents a hydrogen atom, optionally oxidized C1-4 alkyl group or optionally protected hydroxyl group, or R2 and R3 taken together represent optionally oxidized C2-5 alkylene group, R4 represents an optionally oxidized C1-6 alkyl group, etc., R5 represents an optionally oxidized C1-6 alkyl group, etc., R6 represents an optionally oxidized C1-6 alkyl group, etc., m represents 0 or an integer from 1 to 3, n represents 0 or an integer from 1 to 4, and i represents 0 or an integer from 1 to 7.

摘要翻译： 由式（I）表示的化合物，其中R 1表示氢原子等，R 2和R 3各自独立地表示氢原子，任选被氧化的C 1-4烷基或任选被保护的羟基，或者R 2和R 3一起代表任选地 氧化的C 2-5亚烷基，R 4表示任选氧化的C 1-6烷基等，R 5表示任选氧化的C 1-6烷基等，R 6表示任选氧化的C 1-6烷基等，m 表示0或1〜3的整数，n表示0或1〜4的整数，i表示0或1〜7的整数。

公开(公告)号：US20100041708A1

公开(公告)日：2010-02-18

申请号：US12603194

申请日：2009-10-21

申请人： Atsushi NAGANAWA ,  Tetsuji Saito ,  Kaoru Kobayashi ,  Takayuki Maruyama ,  Yoshihiko Nakai ,  Shinsuke Hashimoto

发明人： Atsushi NAGANAWA ,  Tetsuji Saito ,  Kaoru Kobayashi ,  Takayuki Maruyama ,  Yoshihiko Nakai ,  Shinsuke Hashimoto

IPC分类号： A61K31/18 ,  C07D307/64 ,  C07D277/36 ,  C07D213/70 ,  C07D401/12 ,  A61K31/341 ,  A61K31/426 ,  A61K31/4406 ,  A61K31/4439 ,  A61P13/00

CPC分类号： C07D213/70 ,  C07D277/36 ,  C07D307/64 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.

摘要翻译： 式（I）的N-苯基芳基磺酰胺化合物（R1是COOH等; R2是氢，甲基等; R3和R4是甲基和甲基的组合等; R5是异丙基等; Ar是噻唑基， 吡啶基，5-甲基-2-呋喃基，各自任选被甲基取代; n为0或1），化合物的合成中间体及其制备方法。 式（I）化合物结合前列腺素E2受体，特别是EP1亚型受体，并拮抗它。 蛋白质结合的影响较小，因此具有令人满意的体内活性。 因此，认为可用作止痛剂，解热剂，治疗尿频（尿频）和/或下尿路疾病综合征或抗肿瘤药物的药剂。

公开(公告)号：US08318729B2

公开(公告)日：2012-11-27

申请号：US12672762

申请日：2008-08-11

申请人： Atsushi Naganawa ,  Toshihiko Nagase

发明人： Atsushi Naganawa ,  Toshihiko Nagase

IPC分类号： C07D265/36 ,  A61K31/00

CPC分类号： C07D265/36 ,  A61K31/00 ,  A61K31/538 ,  A61K45/06 ,  A61K2300/00

摘要： A compound represented by formula (I), wherein R1 represents a hydrogen atom, etc., R2 and R3 each independently represents a hydrogen atom, optionally oxidized C1-4 alkyl group or optionally protected hydroxyl group, or R2 and R3 taken together represent optionally oxidized C2-5 alkylene group, R4 represents an optionally oxidized C1-6 alkyl group, etc., R5 represents an optionally oxidized C1-6 alkyl group, etc., R6 represents an optionally oxidized C1-6 alkyl group, etc., m represents 0 or an integer from 1 to 3, n represents 0 or an integer from 1 to 4, and i represents 0 or an integer from 1 to 7.

摘要翻译： 由式（I）表示的化合物，其中R 1表示氢原子等，R 2和R 3各自独立地表示氢原子，任选被氧化的C 1-4烷基或任选被保护的羟基，或者R 2和R 3一起代表任选地 氧化的C 2-5亚烷基，R 4表示任选氧化的C 1-6烷基等，R 5表示任选氧化的C 1-6烷基等，R 6表示任选氧化的C 1-6烷基等，m 表示0或1〜3的整数，n表示0或1〜4的整数，i表示0或1〜7的整数。

公开(公告)号：US08088802B2

公开(公告)日：2012-01-03

申请号：US12603194

申请日：2009-10-21

申请人： Atsushi Naganawa ,  Tetsuji Saito ,  Kaoru Kobayashi ,  Takayuki Maruyama ,  Yoshihiko Nakai ,  Shinsuke Hashimoto

发明人： Atsushi Naganawa ,  Tetsuji Saito ,  Kaoru Kobayashi ,  Takayuki Maruyama ,  Yoshihiko Nakai ,  Shinsuke Hashimoto

IPC分类号： A61K31/41 ,  C07D421/00 ,  C07D417/00 ,  C07D413/00 ,  C07D285/08 ,  C07D271/06 ,  C07D257/04 ,  C07D307/00

CPC分类号： C07D213/70 ,  C07D277/36 ,  C07D307/64 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.

摘要翻译： 式（I）的N-苯基芳基磺酰胺化合物（R1是COOH等; R2是氢，甲基等; R3和R4是甲基和甲基的组合等; R5是异丙基等; Ar是噻唑基， 吡啶基，5-甲基-2-呋喃基，各自任选被甲基取代; n为0或1），化合物的合成中间体及其制备方法。 式（I）化合物结合前列腺素E2受体，特别是EP1亚型受体，并拮抗它。 蛋白质结合的影响较小，因此具有令人满意的体内活性。 因此，认为可用作止痛剂，解热剂，治疗尿频（尿频）和/或下尿路疾病综合征或抗肿瘤药物的药剂。

公开(公告)号：US20070004716A1

公开(公告)日：2007-01-04

申请号：US10572578

申请日：2004-09-16

申请人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  SeijiKoji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

发明人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  SeijiKoji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

IPC分类号： A61K31/538 ,  C07D265/36

CPC分类号： C07D307/80 ,  A61K31/343 ,  A61K31/538 ,  C07D265/36 ,  C07D317/48

摘要： A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g., scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis, etc. Since it specifically binds to DP receptor and binds weakly to other prostaglandins receptors, they can be pharmaceuticals having little side effect.

摘要翻译： 由式（I）表示的化合物，其中式中的符号与说明书中的符号相同，其盐，溶剂合物或其前药与DP受体结合并显示DP受体的拮抗活性。 因此，它可用于预防和/或治疗过敏性疾病（例如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），系统性肥大细胞增多症，伴有全身性肥大细胞活化的病症，过敏性休克， 支气管收缩，荨麻疹，湿疹，伴有瘙痒的疾病（例如特应性皮炎和荨麻疹），伴随瘙痒的行为的结果产生的疾病（例如白内障，视网膜脱离，炎症，感染和睡眠障碍）（例如， 搔抓和殴打），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿关节炎，胸膜炎，溃疡性结肠炎等。由于其特异性结合DP受体并且弱结合到其他前列腺素受体，它们可以是具有 小副作用。

公开(公告)号：US20100029631A1

公开(公告)日：2010-02-04

申请号：US12551860

申请日：2009-09-01

申请人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  Seiji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

发明人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  Seiji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

IPC分类号： A61K31/538 ,  C07D265/36 ,  A61P37/08 ,  A61P11/06

CPC分类号： C07D307/80 ,  A61K31/343 ,  A61K31/538 ,  C07D265/36 ,  C07D317/48

摘要： A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g., scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis, etc. Since it specifically binds to DP receptor and binds weakly to other prostaglandins receptors, they can be pharmaceuticals having little side effect.

摘要翻译： 由式（I）表示的化合物，其中式中的符号与说明书中的符号相同，其盐，溶剂合物或其前药与DP受体结合并显示DP受体的拮抗活性。 因此，它可用于预防和/或治疗过敏性疾病（例如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），系统性肥大细胞增多症，伴有全身性肥大细胞活化的病症，过敏性休克， 支气管收缩，荨麻疹，湿疹，伴有瘙痒的疾病（例如特应性皮炎和荨麻疹），伴随瘙痒的行为的结果产生的疾病（例如白内障，视网膜脱离，炎症，感染和睡眠障碍）（例如， 搔抓和殴打），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿关节炎，胸膜炎，溃疡性结肠炎等。由于其特异性结合DP受体并且弱结合到其他前列腺素受体，它们可以是具有 小副作用。

公开(公告)号：US07629369B2

公开(公告)日：2009-12-08

申请号：US11239406

申请日：2005-09-30

申请人： Atsushi Naganawa ,  Tetsuji Saito ,  Kaoru Kobayashi ,  Takayuki Maruyama ,  Yoshihiko Nakai ,  Shinsuke Hashimoto

发明人： Atsushi Naganawa ,  Tetsuji Saito ,  Kaoru Kobayashi ,  Takayuki Maruyama ,  Yoshihiko Nakai ,  Shinsuke Hashimoto

IPC分类号： C07D285/08 ,  C07D271/06 ,  C07D257/04 ,  A61K31/41

CPC分类号： C07D213/70 ,  C07D277/36 ,  C07D307/64 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.

摘要翻译： 式（I）的N-苯基芳基磺酰胺化合物（R1是COOH等; R2是氢，甲基等; R3和R4是甲基和甲基的组合等; R5是异丙基等; Ar是噻唑基， 吡啶基，5-甲基-2-呋喃基，各自任选被甲基取代; n为0或1），化合物的合成中间体及其制备方法。 式（I）化合物结合前列腺素E2受体，特别是EP1亚型受体，并拮抗它。 蛋白质结合的影响较小，因此具有令人满意的体内活性。 因此，认为可用作止痛剂，解热剂，治疗尿频（尿频）和/或下尿路疾病综合征或抗肿瘤药物的药剂。

公开(公告)号：US07601712B2

公开(公告)日：2009-10-13

申请号：US10572578

申请日：2004-09-16

申请人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  Seiji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

发明人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  Seiji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

IPC分类号： A61K31/535 ,  A61K31/36 ,  A61K31/34 ,  A61K31/335 ,  C07D265/36 ,  C07D317/44 ,  C07D307/00 ,  C07D319/14

CPC分类号： C07D307/80 ,  A61K31/343 ,  A61K31/538 ,  C07D265/36 ,  C07D317/48

摘要： A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g., scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis, etc. Since it specifically binds to DP receptor and binds weakly to other prostaglandins receptors, they can be pharmaceuticals having little side effect.

摘要翻译： 由式（I）表示的化合物，其中式中的符号与说明书中的符号相同，其盐，溶剂合物或其前药与DP受体结合并显示DP受体的拮抗活性。 因此，它可用于预防和/或治疗过敏性疾病（例如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），系统性肥大细胞增多症，伴有全身性肥大细胞活化的病症，过敏性休克， 支气管收缩，荨麻疹，湿疹，伴有瘙痒的疾病（例如特应性皮炎和荨麻疹），伴随瘙痒的行为的结果产生的疾病（例如白内障，视网膜脱离，炎症，感染和睡眠障碍）（例如， 搔抓和殴打），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿关节炎，胸膜炎，溃疡性结肠炎等。由于其特异性结合DP受体并且弱结合到其他前列腺素受体，它们可以是具有 小副作用。

公开(公告)号：US20060089353A1

公开(公告)日：2006-04-27

申请号：US10548089

申请日：2004-03-05

申请人： Maki Iwahashi ,  Atsushi Naganawa ,  Toshihiko Nishiyama ,  Toshihiko Nagase ,  Fumio Nambu

发明人： Maki Iwahashi ,  Atsushi Naganawa ,  Toshihiko Nishiyama ,  Toshihiko Nagase ,  Fumio Nambu

IPC分类号： A61K31/538 ,  C07D413/02

CPC分类号： C07D413/12

摘要： An indole derivative compound represented by formula (I) (wherein the symbols in the formula are as mentioned in the specification) and a salt thereof Since the compounds represented by formula (I) binds to PGD2 receptors and shows antagonistic activity, they are believed to be useful for prevention and/or treatment of diseases such as allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, systemic mast cell activating disorder, anaphylaxis shock, airway contraction, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis, urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleep disorder) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, autoimmune disease, chronic articular rheumatism, pleuritis, ulcerative colitis and irritable bowel syndrome.

摘要翻译： 由式（I）表示的吲哚衍生物化合物（其中式中的符号如说明书中所述）及其盐由于式（I）表示的化合物与PGD 2 N 2受体结合， 它们被认为可用于预防和/或治疗过敏性疾病（如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），系统性肥大细胞增多症，全身性肥大细胞活化障碍等疾病， 过敏性休克，气道收缩，荨麻疹，湿疹，伴有瘙痒的疾病（如特应性皮炎，荨麻疹），由于行为伴随而产生的疾病（如白内障，视网膜脱离，炎症，感染和睡眠障碍） 瘙痒（如搔痒），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，自身免疫性疾病 关节炎风湿病，胸膜炎，溃疡性结肠炎和肠易激综合征。

公开(公告)号：US20050124672A1

公开(公告)日：2005-06-09

申请号：US10471673

申请日：2002-03-11

申请人： Atsushi Naganawa ,  Tetsuji Saito ,  Kaoru Kobayashi ,  Takayuki Maruyama ,  Yoshihiko Nakai ,  Shinsuke Hashimoto

发明人： Atsushi Naganawa ,  Tetsuji Saito ,  Kaoru Kobayashi ,  Takayuki Maruyama ,  Yoshihiko Nakai ,  Shinsuke Hashimoto

IPC分类号： C07D307/64 ,  A61K31/34 ,  A61K31/341 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4439 ,  A61P1/04 ,  A61P13/00 ,  A61P13/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D213/70 ,  C07D213/71 ,  C07D277/20 ,  C07D277/36 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D213/70 ,  C07D277/36 ,  C07D307/64 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.

摘要翻译： 式（I）的N-苯基芳基磺酰胺化合物（R 1）是COOH等; R 2是氢，甲基等; R 3 O >和R 4是甲基和甲基等的组合; R 5是异丙基等; Ar是噻唑基，吡啶基，5-甲基-2-呋喃基 任选被甲基取代; n为0或1），化合物的合成中间体及其制备方法。 式（I）化合物与前列腺素E 2受体结合，特别是EP 1亚型受体，并拮抗它。 蛋白质结合的影响较小，因此具有令人满意的体内活性。 因此，认为可用作止痛剂，解热剂，治疗尿频（尿频）和/或下尿路疾病综合征或抗肿瘤药物的药剂。