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1. 发明授权

US08026273B2 8-azaprostaglandin derivative compound and agent comprising the compound as active ingredient 失效
标题翻译： 8-氮杂的前列腺素衍生物化合物和包含该化合物作为活性成分的试剂
公开(公告)号：US08026273B2
公开(公告)日：2011-09-27
申请号：US12683609
申请日：2010-01-07
申请人： Kousuke Tani , Kaoru Kobayashi , Toru Maruyama , Tohru Kambe , Mikio Ogawa , Tsutomu Shiroya
发明人： Kousuke Tani , Kaoru Kobayashi , Toru Maruyama , Tohru Kambe , Mikio Ogawa , Tsutomu Shiroya
IPC分类号： A61K31/40 , A61K31/405 , C07D207/00 , C07D209/00
CPC分类号： C07D413/06 , C07D207/26 , C07D263/24 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12
摘要： An 8-azaprostaglandin represented by formula (I) (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof. Since the compound represented by formula (I) binds to EP2 subtype among PGE receptor strongly, it is useful for preventive and/or treatment for immune diseases, allergic diseases, neuronal cell death, dysmenorrhea, premature birth, abortion, baldness, retinal neuropathy such as glaucoma, erectile dysfunction, arthritis, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, hepatic injury, acute hepatitis, liver cirrhosis, shock, nephritis, renal failure, circulatory diseases, systemic inflammatory response syndrome, sepsis, hemophagocytosis syndrome, macrophage activation syndrome, still disease, Kawasaki Disease, burn, systemic granuloma, ulcerative colitis, Crohn disease, hypercytokinemia at dialysis, multiple organ failure, or bone diseases etc.
摘要翻译：由式（I）（其中所有符号具有与说明书中所述相同的含义）表示的8-氮杂前列腺素，其药学上可接受的盐或其环糊精包合物。由于式（I）表示的化合物强烈地与PGE受体中的EP2亚型结合，因此可用于免疫疾病，过敏性疾病，神经元细胞死亡，痛经，早产，流产，秃发，视网膜神经病变等的预防和/或治疗青光眼，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，肝损伤，急性肝炎，肝硬化，休克，肾炎，肾衰竭，循环系统疾病，全身性炎症反应综合征，败血症，血细胞增多综合征，巨噬细胞活化综合征，静止病，川崎病，烧伤，全身肉芽肿，溃疡性结肠炎，克罗恩病，透析中的高细胞因子血症，多器官功能衰竭或骨骼疾病等。

2. 发明申请

US20050124577A1 8-Azaprostaglandin derivative compounds and drugs containing the compounds as the active ingredient 失效
标题翻译： 8-Azaprostaglandin衍生物化合物和含有这些化合物作为活性成分的药物
公开(公告)号：US20050124577A1
公开(公告)日：2005-06-09
申请号：US10506536
申请日：2003-03-04
申请人： Kousuke Tani , Kaoru Kobayashi , Toru Maruyama , Tohru Kambe , Mikio Ogawa , Tsutomu Shiroya
发明人： Kousuke Tani , Kaoru Kobayashi , Toru Maruyama , Tohru Kambe , Mikio Ogawa , Tsutomu Shiroya
IPC分类号： C07D207/27 , A61P1/00 , A61P1/16 , A61P7/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P15/06 , A61P15/10 , A61P19/02 , A61P19/08 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D207/26 , C07D263/24 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , A61K31/724 , A61K31/557 , C07D413/02 , C07D417/02
CPC分类号： C07D413/06 , C07D207/26 , C07D263/24 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12
摘要： An 8-azaprostaglandin represented by formula (I) (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof. Since the compound represented by formula (I) binds to EP2 subtype among PGE receptor strongly, it is useful for preventive and/or treatment for immune diseases, allergic diseases, neuronal cell death, dysmenorrhea, premature birth, abortion, baldness, retinal neuropathy such as glaucoma, erectile dysfunction, arthritis, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, hepatic injury, acute hepatitis, liver cirrhosis, shock, nephritis, renal failure, circulatory diseases, systemic inflammatory response syndrome, sepsis, hemophagocytosis syndrome, macrophage activation syndrome, still disease, Kawasaki Disease, burn, systemic granuloma, ulcerative colitis, Crohn disease, hypercytokinemia at dialysis, multiple organ failure, or bone diseases etc.
摘要翻译：由式（I）（其中所有符号具有与说明书中所述相同的含义）表示的8-氮杂前列腺素，其药学上可接受的盐或其环糊精包合物。由于式（I）表示的化合物强烈地与PGE受体中的EP2亚型结合，因此可用于免疫疾病，过敏性疾病，神经元细胞死亡，痛经，早产，流产，秃发，视网膜神经病变等的预防和/或治疗青光眼，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，肝损伤，急性肝炎，肝硬化，休克，肾炎，肾衰竭，循环系统疾病，全身性炎症反应综合征，败血症，血细胞增多综合征，巨噬细胞活化综合征，静止病，川崎病，烧伤，全身肉芽肿，溃疡性结肠炎，克罗恩病，透析中的高细胞因子血症，多器官功能衰竭或骨骼疾病等。

3. 发明申请

US20100113388A1 8-AZAPROSTAGLANDIN DERIVATIVE COMPOUND AND AGENT COMPRISING THE COMPOUND AS ACTIVE INGREDIENT 失效
标题翻译： 8-AZAPROSTAGLANDIN衍生化合物和包含化合物作为活性成分的试剂
公开(公告)号：US20100113388A1
公开(公告)日：2010-05-06
申请号：US12683609
申请日：2010-01-07
申请人： Kousuke Tani , Kaoru Kobayashi , Toru Maruyama , Tohru Kambe , Mikio Ogawa , Tsutomu Shiroya
发明人： Kousuke Tani , Kaoru Kobayashi , Toru Maruyama , Tohru Kambe , Mikio Ogawa , Tsutomu Shiroya
IPC分类号： A61K31/724 , A61K31/427 , A61K31/422 , A61K31/4015 , C07D277/36 , C07D263/32 , C07D207/46 , A61P19/08 , A61P1/04 , A61P17/14
CPC分类号： C07D413/06 , C07D207/26 , C07D263/24 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12
摘要： An 8-azaprostaglandin represented by formula (I) (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof. Since the compound represented by formula (I) binds to EP2 subtype among PGE receptor strongly, it is useful for preventive and/or treatment for immune diseases, allergic diseases, neuronal cell death, dysmenorrhea, premature birth, abortion, baldness, retinal neuropathy such as glaucoma, erectile dysfunction, arthritis, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, hepatic injury, acute hepatitis, liver cirrhosis, shock, nephritis, renal failure, circulatory diseases, systemic inflammatory response syndrome, sepsis, hemophagocytosis syndrome, macrophage activation syndrome, still disease, Kawasaki Disease, burn, systemic granuloma, ulcerative colitis, Crohn disease, hypercytokinemia at dialysis, multiple organ failure, or bone diseases etc.
摘要翻译：由式（I）（其中所有符号具有与说明书中所述相同的含义）表示的8-氮杂前列腺素，其药学上可接受的盐或其环糊精包合物。由于式（I）表示的化合物强烈地与PGE受体中的EP2亚型结合，因此可用于免疫疾病，过敏性疾病，神经元细胞死亡，痛经，早产，流产，秃发，视网膜神经病变等的预防和/或治疗青光眼，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，肝损伤，急性肝炎，肝硬化，休克，肾炎，肾衰竭，循环系统疾病，全身性炎症反应综合征，败血症，血细胞增多综合征，巨噬细胞活化综合征，静止病，川崎病，烧伤，全身肉芽肿，溃疡性结肠炎，克罗恩病，透析中的高细胞因子血症，多器官功能衰竭或骨骼疾病等。

4. 发明授权

US07683094B2 8-azaprostaglandin derivative compound and agent comprising the compound as active ingredient 失效
标题翻译： 8-氮杂的前列腺素衍生物化合物和包含该化合物作为活性成分的试剂
公开(公告)号：US07683094B2
公开(公告)日：2010-03-23
申请号：US12139260
申请日：2008-06-13
申请人： Kousuke Tani , Kaoru Kobayashi , Toru Maruyama , Tohru Kambe , Mikio Ogawa , Tsutomu Shiroya
发明人： Kousuke Tani , Kaoru Kobayashi , Toru Maruyama , Tohru Kambe , Mikio Ogawa , Tsutomu Shiroya
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D413/06 , C07D207/26 , C07D263/24 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12
摘要： An 8-azaprostaglandin represented by formula (I) (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof. Since the compound represented by formula (I) binds to EP2 subtype among PGE receptor strongly, it is useful for preventive and/or treatment for immune diseases, allergic diseases, neuronal cell death, dysmenorrhea, premature birth, abortion, baldness, retinal neuropathy such as glaucoma, erectile dysfunction, arthritis, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, hepatic injury, acute hepatitis, liver cirrhosis, shock, nephritis, renal failure, circulatory diseases, systemic inflammatory response syndrome, sepsis, hemophagocytosis syndrome, macrophage activation syndrome, still disease, Kawasaki Disease, burn, systemic granuloma, ulcerative colitis, Crohn disease, hypercytokinemia at dialysis, multiple organ failure, or bone diseases etc.
摘要翻译：由式（I）（其中所有符号具有与说明书中所述相同的含义）表示的8-氮杂前列腺素，其药学上可接受的盐或其环糊精包合物。由于式（I）表示的化合物强烈地与PGE受体中的EP2亚型结合，因此可用于免疫疾病，过敏性疾病，神经元细胞死亡，痛经，早产，流产，秃发，视网膜神经病变等的预防和/或治疗青光眼，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，肝损伤，急性肝炎，肝硬化，休克，肾炎，肾衰竭，循环系统疾病，全身性炎症反应综合征，败血症，血细胞增多综合征，巨噬细胞活化综合征，静止病，川崎病，烧伤，全身肉芽肿，溃疡性结肠炎，克罗恩病，透析中的高细胞因子血症，多器官功能衰竭或骨骼疾病等。

5. 发明授权

US07402605B2 8-azaprostaglandin derivative compounds and drugs containing the compounds as the active ingredient 失效
标题翻译： 8-氮杂的前列腺素衍生物化合物和含有这些化合物作为活性成分的药物
公开(公告)号：US07402605B2
公开(公告)日：2008-07-22
申请号：US10506536
申请日：2003-03-04
申请人： Kousuke Tani , Kaoru Kobayashi , Toru Maruyama , Tohru Kambe , Mikio Ogawa , Tsutomu Shiroya
发明人： Kousuke Tani , Kaoru Kobayashi , Toru Maruyama , Tohru Kambe , Mikio Ogawa , Tsutomu Shiroya
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D413/06 , C07D207/26 , C07D263/24 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12
摘要： An 8-azaprostaglandin represented by formula (I) (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof. Since the compound represented by formula (I) binds to EP2 subtype among PGE receptor strongly, it is useful for preventive and/or treatment for immune diseases, allergic diseases, neuronal cell death, dysmenorrhea, premature birth, abortion, baldness, retinal neuropathy such as glaucoma, erectile dysfunction, arthritis, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, hepatic injury, acute hepatitis, liver cirrhosis, shock, nephritis, renal failure, circulatory diseases, systemic inflammatory response syndrome, sepsis, hemophagocytosis syndrome, macrophage activation syndrome, still disease, Kawasaki Disease, burn, systemic granuloma, ulcerative colitis, Crohn disease, hypercytokinemia at dialysis, multiple organ failure, or bone diseases etc.
摘要翻译：由式（I）（其中所有符号具有与说明书中所述相同的含义）表示的8-氮杂前列腺素，其药学上可接受的盐或其环糊精包合物。由于式（I）表示的化合物强烈地与PGE受体中的EP2亚型结合，因此可用于免疫疾病，过敏性疾病，神经元细胞死亡，痛经，早产，流产，秃发，视网膜神经病变等的预防和/或治疗青光眼，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，肝损伤，急性肝炎，肝硬化，休克，肾炎，肾衰竭，循环系统疾病，全身炎症反应综合征，败血症，血细胞增多综合征，巨噬细胞活化综合征，静止病，川崎病，烧伤，全身肉芽肿，溃疡性结肠炎，克罗恩病，透析中的高细胞因子血症，多器官功能衰竭或骨骼疾病等。

6. 发明申请

US20090318703A1 CARBOXYLIC ACID DERIVATIVES AND PHARMACEUTICAL AGENT COMPRISING THE SAME AS ACTIVE INGREDIENT 有权
标题翻译：羧酸衍生物和包含它们的药物代谢作为活性成分
公开(公告)号：US20090318703A1
公开(公告)日：2009-12-24
申请号：US12259012
申请日：2008-10-27
申请人： Kousuke Tani , Masaki Asada , Kaoru Kobayashi , Masami Narita , Mikio Ogawa
发明人： Kousuke Tani , Masaki Asada , Kaoru Kobayashi , Masami Narita , Mikio Ogawa
IPC分类号： C07D213/62 , C07C229/34 , C07D307/02 , C07D231/10
CPC分类号： C07D231/12 , C07C59/68 , C07C69/734 , C07C69/736 , C07C69/738 , C07C229/34 , C07C309/66 , C07C309/67 , C07C309/73 , C07C311/06 , C07C311/08 , C07C311/19 , C07C311/29 , C07C311/51 , C07C317/18 , C07C317/22 , C07C317/40 , C07C317/50 , C07C323/19 , C07C323/42 , C07C323/59 , C07C323/60 , C07D233/56 , C07D249/08
摘要： A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.
摘要翻译：式（I）的羧酸衍生物：其中R 1是-COOH，-COOR 6等; A是单键，亚烷基等; R2是烷基，烷氧基等; B是碳环或杂环; Q是亚烷基-Si 2等; D是连接链; 和R 3是烷基，碳环或杂环，或其无毒盐。式（I）化合物与PGE2受体结合，特别是亚型EP3和/或EP4并显示拮抗活性，可用于预防和/或治疗疾病诱发的疼痛，瘙痒，荨麻疹，过敏，尿频，尿紊乱，阿尔茨海默病，癌症，痛经，子宫内膜异位症等

7. 发明授权

US06835752B2 Carboxylic acid derivatives, processes for the preparation thereof and pharmaceutical agents comprising the same as active ingredient 失效
标题翻译：羧酸衍生物，其制备方法和包含其作为活性成分的药剂
公开(公告)号：US06835752B2
公开(公告)日：2004-12-28
申请号：US10344989
申请日：2003-02-20
申请人： Kousuke Tani , Masaki Asada , Kaoru Kobayashi , Masami Narita , Mikio Ogawa
发明人： Kousuke Tani , Masaki Asada , Kaoru Kobayashi , Masami Narita , Mikio Ogawa
IPC分类号： C07C23343
CPC分类号： C07D213/75 , C07B2200/07 , C07C233/44 , C07C233/55 , C07C235/38 , C07C255/60 , C07C311/51 , C07C323/52 , C07C323/60 , C07C2601/02 , C07C2601/10 , C07C2602/10 , C07D209/18 , C07D261/10 , C07D319/18 , C07D333/60
摘要： A carboxylic acid derivative of formula (1) wherein R1 is COOH, COOR6 etc.; A is alkylene etc.; R2 is alkyl, alkenyl, alkynyl etc.; B is carbocyclic ring or heterocyclic ring; R4 is alkyl, cycloalkyl etc.; R6 is carbocyclic ring or heterocyclic ring; or non-toxic salts thereof, a process for the preparation thereof and a pharmaceutical agent comprising the same as active ingredient. The compound of the formula (I) can bind to Prostaglandin E2 receptors, especially, EP3 receptor and/or EP4 receptor and show the antagonizing activity, and useful for the prevention and/or treatment of disease, for example, pain, allergy, Alzheimer's disease, cancer.
摘要翻译：式（1）的羧酸衍生物，其中R 1是COOH，COOR 6等; A是亚烷基等; R 2是烷基，烯基，炔基等; B是碳环或杂环; R 4是烷基，环烷基等; R 6是碳环或杂环;或其无毒盐，其制备方法和包含与活性成分相同的药剂。式（I）化合物可与前列腺素E2受体结合，特别是EP3受体和/或EP4受体，并显示拮抗活性，并且可用于预防和/或治疗疾病，例如疼痛，过敏，阿尔茨海默病，癌症。

8. 发明申请

US20060258728A1 Carboxylic acid derivative compounds and drugs comprising these compounds as the active ingredient 失效
标题翻译：羧酸衍生物化合物和包含这些化合物作为活性成分的药物
公开(公告)号：US20060258728A1
公开(公告)日：2006-11-16
申请号：US10486220
申请日：2002-08-08
申请人： Kousuke Tani , Masaki Asada , Kaoru Kobayashi , Masami Narita , Mikio Ogawa
发明人： Kousuke Tani , Masaki Asada , Kaoru Kobayashi , Masami Narita , Mikio Ogawa
IPC分类号： A61K31/4178 , A61K31/4172 , A61K31/4152 , A61K31/192 , A61K31/4035 , A61K31/325
CPC分类号： C07D231/12 , C07C59/68 , C07C69/734 , C07C69/736 , C07C69/738 , C07C229/34 , C07C309/66 , C07C309/67 , C07C309/73 , C07C311/06 , C07C311/08 , C07C311/19 , C07C311/29 , C07C311/51 , C07C317/18 , C07C317/22 , C07C317/40 , C07C317/50 , C07C323/19 , C07C323/42 , C07C323/59 , C07C323/60 , C07D233/56 , C07D249/08
摘要： A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.
摘要翻译：式（I）的羧酸衍生物：其中R 1是-COOH，-COOR 6等; A是单键，亚烷基等; R 2是烷基，烷氧基等; B是碳环或杂环; Q是亚烷基-Si 2等; D是连接链; 和R 3是烷基，碳环或杂环，或其无毒盐。式（I）化合物与PGE2受体结合，特别是亚型EP 3和/或EP 4，并显示出拮抗活性，用于预防和/或治疗疾病引起的疼痛，瘙痒，荨麻疹，过敏，尿频，尿失调，阿尔茨海默病，癌症，痛经，子宫内膜异位症等。

9. 发明申请

US20050026908A1 Carboxylic acid derivatives, processes for the preparation thereof and pharmaceutical aggents comprising the same as active ingredient 审中-公开
标题翻译：羧酸衍生物，其制备方法和包含其作为活性成分的药物组合物
公开(公告)号：US20050026908A1
公开(公告)日：2005-02-03
申请号：US10924924
申请日：2004-08-25
申请人： Kousuke Tani , Masaki Asada , Kaoru Kobayashi , Masami Narita , Mikio Ogawa
发明人： Kousuke Tani , Masaki Asada , Kaoru Kobayashi , Masami Narita , Mikio Ogawa
IPC分类号： A61P1/12 , A61P3/12 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/00 , A61P13/02 , A61P13/12 , A61P15/00 , A61P15/06 , A61P17/00 , A61P17/02 , A61P17/04 , A61P19/02 , A61P25/02 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/06 , A61P37/08 , C07C233/44 , C07C233/55 , C07C235/38 , C07C255/60 , C07C311/51 , C07C323/52 , C07C323/60 , C07D209/18 , C07D213/75 , C07D261/10 , C07D319/18 , C07D333/60 , A61K31/55 , A61K31/40 , A61K31/445
CPC分类号： C07D213/75 , C07B2200/07 , C07C233/44 , C07C233/55 , C07C235/38 , C07C255/60 , C07C311/51 , C07C323/52 , C07C323/60 , C07C2601/02 , C07C2601/10 , C07C2602/10 , C07D209/18 , C07D261/10 , C07D319/18 , C07D333/60
摘要： A carboxylic acid derivative of formula (I) wherein R1 is COOH, COOR6 etc.; A is alkylene etc.; R2 is alkyl, alkenyl, alkynyl etc.; B is carbocyclic ring or heterocyclic ring; R4 is alkyl, cycloalkyl etc.; R6 is carbocyclic ring or heterocyclic ring; or non-toxic salts thereof, a process for the preparation thereof and a pharmaceutical agent comprising the same as active ingredient. The compound of the formula (I) can bind to Prostaglandin E2 receptors, especially, EP3 receptor and/or EP4 receptor and show the antagonizing activity, and useful for the prevention and/or treatment of disease, for example, pain, allergy, Alzheimer's disease, cancer.
摘要翻译：式（I）的羧酸衍生物，其中R 1是COOH，COOR 6等; A是亚烷基等; R 2是烷基，烯基，炔基等; B是碳环或杂环; R 4是烷基，环烷基等; R 6是碳环或杂环; 或其无毒盐，其制备方法和包含其作为活性成分的药剂。式（I）化合物可以结合前列腺素E2受体，特别是EP3受体和/或EP4受体，并显示拮抗活性，并且可用于预防和/或治疗疾病，例如疼痛，过敏，阿尔茨海默病疾病，癌症。

10. 发明授权

US07786161B2 Carboxylic acid derivatives and pharmaceutical agent comprising the same as active ingredient 有权
标题翻译：羧酸衍生物和包含与活性成分相同的药剂
公开(公告)号：US07786161B2
公开(公告)日：2010-08-31
申请号：US12259012
申请日：2008-10-27
申请人： Kousuke Tani , Masaki Asada , Kaoru Kobayashi , Masami Narita , Mikio Ogawa
发明人： Kousuke Tani , Masaki Asada , Kaoru Kobayashi , Masami Narita , Mikio Ogawa
IPC分类号： A61K31/415 , C07D231/12
CPC分类号： C07D231/12 , C07C59/68 , C07C69/734 , C07C69/736 , C07C69/738 , C07C229/34 , C07C309/66 , C07C309/67 , C07C309/73 , C07C311/06 , C07C311/08 , C07C311/19 , C07C311/29 , C07C311/51 , C07C317/18 , C07C317/22 , C07C317/40 , C07C317/50 , C07C323/19 , C07C323/42 , C07C323/59 , C07C323/60 , C07D233/56 , C07D249/08
摘要： A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.
摘要翻译：式（I）的羧酸衍生物：其中R 1是-COOH，-COOR 6等; A是单键，亚烷基等; R2是烷基，烷氧基等; B是碳环或杂环; Q是亚烷基-Si 2等; D是连接链; 和R 3是烷基，碳环或杂环，或其无毒盐。式（I）化合物与PGE2受体结合，特别是亚型EP3和/或EP4并显示拮抗活性，可用于预防和/或治疗疾病诱发的疼痛，瘙痒，荨麻疹，过敏，尿频，尿紊乱，阿尔茨海默病，癌症，痛经，子宫内膜异位症等

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