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1. 发明授权

US07482358B2 Imidazoline compounds 失效
标题翻译：咪唑啉化合物
公开(公告)号：US07482358B2
公开(公告)日：2009-01-27
申请号：US11348459
申请日：2006-02-07
申请人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
发明人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
IPC分类号： A61K31/435 , C07D401/00
CPC分类号： C07D401/04 , C07D233/26 , C07D401/14 , C07D403/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds represented by the general formula (I): wherein Ar1 and Ar2 are each aryl or heteroaryl; R1 is lower cycloalkyl, —Ar3, or a group of the general formula (a), (b) or (c): and R2 and R3are each hydrogen, lower cycloalkyl, lower alkenyl, or optionally substituted lower alkyl (with the proviso that when R2 and R3 are simultaneously hydrogen, Ar1, Ar2 and R1 do not simultaneously represent unsubstituted phenyl). The compounds are useful as treating agents for various NPY-related diseases, for example, circulatory diseases including hypertension, kidney diseases, cardiac diseases, vasospasm and arteriosclerosis; central nervous system diseases including hyperphagia, depression, anxiety, convulsion, epilepsy, dementia, pain, alcohol dependence, and withdrawal symptoms due to abstinence from drugs; metabolic diseases including obesity, diabetes, hormonal disorders, hypercholesterolemia, and hyperlipidemia; sexual dysfunction and reproductive function disorders; digestive diseases including enterokinetic disorders; respiratory diseases; inflammation; or glaucoma.
摘要翻译：由通式（I）表示的化合物：其中Ar1和Ar2各自为芳基或杂芳基; R 1是低级环烷基，-Ar 3或通式（a），（b）或（c）的基团：R 2和R 3各自为氢，低级环烷基，低级烯基或任选取代的低级烷基（条件是当R2和R3同时为氢时，Ar1，Ar2和R1不同时表示未取代的苯基）。这些化合物可用作各种NPY相关疾病的治疗剂，例如包括高血压，肾脏疾病，心脏病，血管痉挛和动脉硬化的循环系统疾病; 中枢神经系统疾病，包括食欲过多，抑郁，焦虑，惊厥，癫痫，痴呆，疼痛，酒精依赖以及戒毒症状; 代谢疾病包括肥胖，糖尿病，激素失调，高胆固醇血症和高脂血症; 性功能障碍和生殖功能障碍; 消化疾病包括肠动力障碍; 呼吸疾病; 炎; 或青光眼。

2. 发明申请

US20060135559A1 Novel imidazoline compounds 失效
标题翻译：新型咪唑啉化合物
公开(公告)号：US20060135559A1
公开(公告)日：2006-06-22
申请号：US11348459
申请日：2006-02-07
申请人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
发明人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
IPC分类号： A61K31/4709 , A61K31/4439 , A61K31/4178 , C07D409/02 , C07D403/02
CPC分类号： C07D401/04 , C07D233/26 , C07D401/14 , C07D403/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds represented by the general formula (I): wherein Ar1 and Ar2 are each aryl or heteroaryl; R1 is lower cycloalkyl, —Ar3, or a group of the general formula (a), (b) or (c): and R2 and R3are each hydrogen, lower cycloalkyl, lower alkenyl, or optionally substituted lower alkyl (with the proviso that when R2 and R3 are simultaneously hydrogen, Ar1, Ar2 and R1 do not simultaneously represent unsubstituted phenyl). The compounds are useful as treating agents for various NPY-related diseases, for example, circulatory diseases including hypertension, kidney diseases, cardiac diseases, vasospasm and arteriosclerosis; central nervous system diseases including hyperphagia, depression, anxiety, convulsion, epilepsy, dementia, pain, alcohol dependence, and withdrawal symptoms due to abstinence from drugs; metabolic diseases including obesity, diabetes, hormonal disorders, hypercholesterolemia, and hyperlipidemia; sexual dysfunction and reproductive function disorders; digestive diseases including enterokinetic disorders; respiratory diseases; inflammation; or glaucoma.
摘要翻译：由通式（I）表示的化合物：其中Ar 1和Ar 2各自为芳基或杂芳基; R 1是低级环烷基，-Ar 3或通式（a），（b）或（c）的基团：R 2， R 3和R 3各自为氢，低级环烷基，低级烯基或任选取代的低级烷基（条件是当R 2和R 3' / SUP>同时为氢，Ar 1，Ar 2和R 1不同时表示未取代的苯基）。这些化合物可用作各种NPY相关疾病的治疗剂，例如包括高血压，肾脏疾病，心脏病，血管痉挛和动脉硬化的循环系统疾病; 中枢神经系统疾病，包括食欲过多，抑郁，焦虑，惊厥，癫痫，痴呆，疼痛，酒精依赖以及戒毒症状; 代谢疾病包括肥胖，糖尿病，激素失调，高胆固醇血症和高脂血症; 性功能障碍和生殖功能障碍; 消化疾病包括肠动力障碍; 呼吸疾病; 炎; 或青光眼。

3. 发明授权

US07064142B2 Imidazonline compounds 失效
标题翻译：咪唑啉化合物
公开(公告)号：US07064142B2
公开(公告)日：2006-06-20
申请号：US10204267
申请日：2001-02-22
申请人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
发明人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
IPC分类号： A61K31/415 , C07D233/26
CPC分类号： C07D401/04 , C07D233/26 , C07D401/14 , C07D403/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds represented by the general formula (I): wherein Ar1 and Ar2 are each aryl or heteroaryl; R1 is lower cycloalkyl, —Ar3, or a group of the general formula (a), (b) or (c): and R2 and R3 are each hydrogen, lower cycloalkyl, lower alkenyl, or optionally substituted lower alkyl (with the proviso that when R2 and R3 are simultaneously hydrogen, Ar1, Ar2 and R1 do not simultaneously represent unsubstituted phenyl). The compounds are useful as treating agents for various NPY-related diseases, for example, circulatory diseases including hypertension, kidney diseases, cardiac diseases, vasospasm and arteriosclerosis; central nervous system diseases including hyperphagia, depression, anxiety, convulsion, epilepsy, dementia, pain, alcohol dependence, and withdrawal symptoms due to abstinence from drugs; metabolic diseases including obesity, diabetes, hormonal disorders, hypercholesterolemia, and hyperlipidemia; sexual dysfunction and reproductive function disorders; digestive diseases including enterokinetic disorders; respiratory diseases; inflammation; or glaucoma.
摘要翻译：由通式（I）表示的化合物：其中Ar 1和Ar 2各自为芳基或杂芳基; R 1是低级环烷基，-Ar 3或通式（a），（b）或（c）的基团：R 2， R 3和R 3各自为氢，低级环烷基，低级烯基或任选取代的低级烷基（条件是当R 2和R 3' / SUP>同时为氢，Ar 1，Ar 2和R 1不同时表示未取代的苯基）。这些化合物可用作各种NPY相关疾病的治疗剂，例如包括高血压，肾脏疾病，心脏病，血管痉挛和动脉硬化的循环系统疾病; 中枢神经系统疾病，包括食欲过多，抑郁，焦虑，惊厥，癫痫，痴呆，疼痛，酒精依赖以及戒毒症状; 代谢疾病包括肥胖，糖尿病，激素失调，高胆固醇血症和高脂血症; 性功能障碍和生殖功能障碍; 消化疾病包括肠动力障碍; 呼吸疾病; 炎; 或青光眼。

4. 发明申请

US20050154025A1 Novel pyridone derivatives 失效
标题翻译：新型吡啶酮衍生物
公开(公告)号：US20050154025A1
公开(公告)日：2005-07-14
申请号：US10505476
申请日：2003-03-14
申请人： Nagaaki Sato , Tsuyoshi Nagase , Keita Nagai , Makoto Ando , Akio Kanatani
发明人： Nagaaki Sato , Tsuyoshi Nagase , Keita Nagai , Makoto Ando , Akio Kanatani
IPC分类号： A61K31/444 , A61P1/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/06 , A61P29/00 , A61P43/00 , C07D401/14 , C07D41/14
CPC分类号： C07D401/14 , A61K31/444
摘要： A compound of the formula (I): wherein R1 is hydrogen, halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy, lower alkoxy or aralkyloxy; R2 and R3 are each independently hydrogen, halogen or halo-lower alkyl; and R4 and R are each independently hydrogen or halogen, is useful as a pharmaceutical composition for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, etc., nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译：式（I）的化合物：其中R 1是氢，卤素，氰基，低级烷基，卤代低级烷基，羟基，低级烷氧基或芳烷氧基; R 2和R 3各自独立地为氢，卤素或卤代低级烷基; R 4和R 4各自独立地为氢或卤素，可用作治疗与NPY相关的各种疾病的药物组合物，例如心血管疾病如心绞痛，急性或充血性心力衰竭，心肌梗死，高血压，肾病，电解质异常，血管痉挛等，神经系统疾病如贪食症，抑郁症，焦虑症，癫痫，癫痫，痴呆，疼痛，酒精中毒，药物戒断，昼夜节律紊乱，精神分裂症，记忆障碍，睡眠障碍，认知障碍等，代谢疾病如肥胖，糖尿病，激素异常，痛风，脂肪肝等，生殖器官或生殖障碍如不育症，早产，性功能障碍等，胃肠道疾病，呼吸系统疾病，炎症性疾病或青光眼等。

5. 发明授权

US06869966B2 N-substituted-2-oxodihydropyridine derivatives 失效
标题翻译： N-取代-2-氧代二氢吡啶衍生物
公开(公告)号：US06869966B2
公开(公告)日：2005-03-22
申请号：US10641017
申请日：2003-08-15
申请人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
发明人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
IPC分类号： A61P3/04 , C07D213/80 , C07D401/04 , C07D401/14 , C07D401/02 , A61K31/44 , C07D213/02
CPC分类号： C07D213/80 , C07D401/04 , C07D401/14
摘要： A compound of the formula (I): (wherein Ar1 and Ar2 are independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl; R1 and R2 are independently lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl or lower alkoxy, any of which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl;R3, R4 and R5 are independently hydrogen, cyano, halogen or hydroxy, or lower alkyl, lower alkoxy or lower alkylthio, the last three groups being optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl), or a salt or ester thereof is useful as a neuropeptide Y receptor antagonist agent and is also useful as an agent for the treatment of bulimia, obesity or diabetes.
摘要翻译：式（I）的化合物（其中Ar 1和Ar 2独立地是芳基或杂芳基，其中任何一个任选被选自氰基，卤素，硝基，低级烷基，卤代低级烷基，羟基 - 低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基，低级烯基，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，低级烷基磺酰基氨基，芳基磺酰基氨基，羟基，低级烷氧基，低级烷氧基，芳氧基，杂芳氧基，低级烷硫基，羧基，甲酰基，低级烷酰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，二低级烷基氨基甲酰基，低级烷基磺酰基，芳基磺酰基，芳基和杂芳基; R 1和R 2独立地为低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基或低级烷氧基，其中任何一个任选被选自卤素，低级烷基氨基，二低级烷基氨基，低级烷酰氨基，羟基，低级烷氧基，甲酰基，低级烷基氧羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基; R 3，R 4和R 5独立地是氢，氰基，卤素或羟基，或低级烷基，低级烷氧基或低级烷硫基，最后三个基团是任选的被选自卤素，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，羟基，低级烷氧基，甲酰基，低级烷氧基羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基的取代基取代）或其盐或酯是有用的作为神经肽Y受体拮抗剂，也可用作治疗贪食症，肥胖症或糖尿病的药剂。

6. 发明授权

US07138525B2 N-substituted-2-oxodihydropyridine derivatives 失效
标题翻译： N-取代-2-氧代二氢吡啶衍生物
公开(公告)号：US07138525B2
公开(公告)日：2006-11-21
申请号：US10899162
申请日：2004-07-27
申请人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
发明人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
IPC分类号： C07D211/80
CPC分类号： C07D213/80 , C07D401/04 , C07D401/14
摘要： A compound of the formula (I): (wherein Ar1 and Ar2 are independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl; R1 and R2 are independently lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl or lower alkoxy, any of which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl; R3, R4 and R5 are independently hydrogen, cyano, halogen or hydroxy, or lower alkyl, lower alkoxy or lower alkylthio, the last three groups being optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl), or a salt or ester thereof is useful as a neuropeptide Y receptor antagonist agent and is also useful as an agent for the treatment of bulimia, obesity or diabetes.
摘要翻译：式（I）的化合物：其中Ar 1和Ar 2独立地为芳基或杂芳基，其中任何一个任选被选自以下的取代基取代：氰基，卤素，硝基，低级烷基，卤代低级烷基，羟基 - 低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基，低级烯基，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，低级烷基磺酰基氨基，芳基磺酰基氨基，羟基，低级烷氧基，卤代低级烷氧基，芳氧基，杂芳氧基，低级烷硫基，羧基，甲酰基，低级烷酰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，二低级烷基氨基甲酰基，低级烷基磺酰基，芳基磺酰基，芳基和杂芳基; R R 1和R 2独立地是低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基或低级烷氧基，其中任何一个任选被选定的取代基取代由卤素，低级烷基氨基，二低级烷基氨基，低级烷酰氨基，低级烷基氨基，低级烷氧基，甲酰基，低级烷氧基羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基; R 3，R 4和R 5独立地是氢，氰基，卤素或羟基，或低级烷基，低级烷氧基或低级烷硫基，最后三个基团任选被选自卤素，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，羟基，低级烷氧基，甲酰基，低级烷氧基羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基的取代基取代）或盐或其酯可用作神经肽Y受体拮抗剂，并且也可用作治疗贪食症，肥胖症或糖尿病的药剂。

7. 发明授权

US07119107B2 Pyridone derivatives 失效
标题翻译：吡啶酮衍生物
公开(公告)号：US07119107B2
公开(公告)日：2006-10-10
申请号：US10505476
申请日：2003-03-14
申请人： Nagaaki Sato , Tsuyoshi Nagase , Keita Nagai , Makoto Ando , Akio Kanatani
发明人： Nagaaki Sato , Tsuyoshi Nagase , Keita Nagai , Makoto Ando , Akio Kanatani
IPC分类号： A61K31/4439 , C07D401/14
CPC分类号： C07D401/14 , A61K31/444
摘要： A compound of the formula (I): wherein R1 is hydrogen, halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy, lower alkoxy or aralkyloxy; R2 and R3 are each independently hydrogen, halogen or halo-lower alkyl; and R4 and R5 are each independently hydrogen or halogen, is useful as a pharmaceutical composition for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, etc., nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译：式（I）的化合物：其中R 1是氢，卤素，氰基，低级烷基，卤代低级烷基，羟基，低级烷氧基或芳烷氧基; R 2和R 3各自独立地为氢，卤素或卤代低级烷基; R 4和R 5各自独立地为氢或卤素，可用作治疗与NPY相关的各种疾病的药物组合物，例如心血管疾病如心绞痛，急性或充血性心力衰竭，心肌梗死，高血压，肾病，电解质异常，血管痉挛等，神经系统疾病如贪食症，抑郁症，焦虑症，癫痫症，痴呆症，疼痛，酒精中毒，药物戒断，昼夜节律紊乱，精神分裂症，记忆障碍，睡眠障碍，认知障碍等，代谢疾病如肥胖，糖尿病，激素异常，痛风，脂肪肝等，生殖器或生殖障碍如不孕，早产，性功能障碍等。，胃肠道疾病，呼吸系统疾病，炎性疾病或青光眼等。

8. 发明申请

US20050009879A1 N-substituted-2-oxodihydropyridine derivatives 失效
标题翻译： N-取代-2-氧代二氢吡啶衍生物
公开(公告)号：US20050009879A1
公开(公告)日：2005-01-13
申请号：US10899162
申请日：2004-07-27
申请人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
发明人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
IPC分类号： A61P3/04 , C07D213/80 , C07D401/04 , C07D401/14 , A61K31/4439 , C07
CPC分类号： C07D213/80 , C07D401/04 , C07D401/14
摘要： A compound of the formula (I): (wherein Ar1 and Ar2 are independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl; R1 and R2 are independently lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl or lower alkoxy, any of which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl; R3, R4 and R5 are independently hydrogen, cyano, halogen or hydroxy, or lower alkyl, lower alkoxy or lower alkylthio, the last three groups being optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl), or a salt or ester thereof is useful as a neuropeptide Y receptor antagonist agent and is also useful as an agent for the treatment of bulimia, obesity or diabetes.
摘要翻译：式（I）的化合物：其中Ar 1和Ar 2独立地为芳基或杂芳基，其中任何一个任选被选自氰基，卤素，硝基，低级烷基，卤代低级烷基，羟基 - 低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基，低级烯基，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，低级烷基磺酰基氨基，芳基磺酰基氨基，羟基，低级烷氧基，低级烷氧基，芳氧基，杂芳氧基，低级烷硫基，羧基，甲酰基，低级烷酰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，二低级烷基氨基甲酰基，低级烷基磺酰基，芳基磺酰基，芳基和杂芳基; R 1和R 2独立地为低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基或低级烷氧基，其中任何一个任选被选自卤素，低级烷基氨基，二低级烷基氨基，低级烷酰氨基，羟基，低级烷氧基，甲酰基，低级烷基低级烷基氨基甲酰基和二低级烷基氨基甲酰基; R 3，R 4和R 5独立地是氢，氰基，卤素或羟基，或低级烷基，低级烷氧基或低级烷硫基，最后三个基团任选地被选自以下的取代基取代：卤素，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，羟基，低级烷氧基，甲酰基，低级烷氧基羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基）或其盐或酯可用作神经肽Y受体拮抗剂，可用作治疗贪食症，肥胖症或糖尿病的药剂。

9. 发明授权

US08987473B2 Ring-fused compound 有权
标题翻译：环稠合化合物
公开(公告)号：US08987473B2
公开(公告)日：2015-03-24
申请号：US13982200
申请日：2012-01-30
申请人： Keita Nagai , Koh Nagasawa , Hirobumi Takahashi , Motoaki Baba , Shinichi Fujioka , Eri Kondoh , Kenichi Tanaka , Yoshiki Itoh
发明人： Keita Nagai , Koh Nagasawa , Hirobumi Takahashi , Motoaki Baba , Shinichi Fujioka , Eri Kondoh , Kenichi Tanaka , Yoshiki Itoh
IPC分类号： C07D471/04 , C07D413/06 , C07D409/06 , C07D235/08 , C07D209/08 , C07D209/30 , C07D231/56 , C07D235/10 , C07D401/06 , C07D405/06 , C07D235/06 , C07D403/04
CPC分类号： C07D471/04 , C07D209/08 , C07D209/12 , C07D209/30 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/10 , C07D401/06 , C07D403/04 , C07D405/06 , C07D409/06 , C07D413/06
摘要： The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below. [in the formula, R1 is -Q1-A1 and the like; is a double bond or a single bond; when is a double bond, W1 is a nitrogen atom or a group represented by the general formula: ═C(Ra)—, and W2 is a nitrogen atom or a group represented by the general formula: ═C(Rb)—; when is a single bond, W1 is a group represented by the general formula: —C(Raa)(Rab)— or a group represented by the general formula: —(C═O)—, and W2 is a group represented by the general formula: —C(Rba)(Rbb)—, a group represented by the general formula: —(C═O)— or a group represented by the general formula: —N(Rbc)—; W3, W4 and W5 are each independently a nitrogen atom or a methine group and the like that may have a substituent; X is a single bond, an oxygen atom and the like; Y is a single bond or (CRYiRYi′)n; and Z is a hydroxyl group or COOR2 and the like.
摘要翻译：本发明涉及具有URAT1抑制作用的化合物和URAT1抑制剂，血液尿酸水平降低剂和包含该化合物的药物组合物。更具体地，本发明涉及由下式（I）表示的化合物。 [式中，R1为-Q1-A1等; 是双键或单键; 当是双键时，W1是氮原子或由通式：= C（Ra） - 表示的基团，并且W 2是氮原子或由通式表示的基团：= C（R b） - ; 当是单键时，W1是由通式-C（Raa）（Rab）表示的基团或由通式表示的基团 - （C = O） - ，并且W 2是由 -C（Rba）（Rbb） - ，由通式表示的基团：（C = O） - 或由通式-N（Rbc） - 表示的基团。 W3，W4和W5各自独立地为可以具有取代基的氮原子或次甲基等; X是单键，氧原子等; Y是单键或（CRYiRYi'）n; Z为羟基或COOR 2等。

10. 发明申请

US20090192174A1 Novel Aminopyridine Derivatives Having Aurora a Selective Inhibitory Action 有权
标题翻译：具有极光选择性抑制作用的新型氨基吡啶衍生物
公开(公告)号：US20090192174A1
公开(公告)日：2009-07-30
申请号：US12226639
申请日：2007-04-25
申请人： Tetsuya Kato , Nobuhiko Kawanishi , Takashi Mita , Keita Nagai , Katsumasa Nonoshita , Mitsuru Ohkubo
发明人： Tetsuya Kato , Nobuhiko Kawanishi , Takashi Mita , Keita Nagai , Katsumasa Nonoshita , Mitsuru Ohkubo
IPC分类号： A61K31/506 , C07D487/04
CPC分类号： C07D487/08
摘要： The present invention relates to a compound of general formula I: wherein: n1 and n2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; Re is hydrogen atom or lower alkyl; two groups selected from four groups consisting of (i) either one of Ra1 and Ra1′, (ii) either one of Ra2 and Ra2′, (iii) either one of Rb1 and Rb1′, and (iv) either one of Rb2 and Rb2′, are combined to form —(CH2)n— where n is 1, 2 or 3; and among Ra1, Ra1′, Ra2, Ra2′, Rb1, Rb1′, Rb2 and Rb2′, the groups which do not form —(CH2)n— are each independently hydrogen atom, etc.; X1, X2, X3 and X4 are each independently CH, N, etc.; Y1, Y2, Y3 and Y4 are the same or different and are CH or N, etc.; W is a 5-membered aromatic heterocyclic group, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及通式I的化合物：其中：n1和n2相同或不同，为0或1; R是芳基，杂芳基等; Re为氢原子或低级烷基; 选自由（i）Ra1和Ra1'中的任一个组成的四组中的两个基团，（ii）Ra2和Ra2'中的任一个，（iii）Rb1和Rb1'中的任一个，以及（iv）Rb2和 Rb2'组合形成 - （CH 2）n - ，其中n为1,2或3; 在Ra1，Ra1'，Ra2，Ra2'，Rb1，Rb1'，Rb2和Rb2'之间，不形成 - （CH2）n-的基团各自独立地为氢原子等; X1，X2，X3和X4各自独立地为CH，N等; Y1，Y2，Y3和Y4相同或不同，为CH或N等; W是5元芳杂环基或其药学上可接受的盐或酯。

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