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    • 2. 发明申请
      WO2004002986A2 NOVEL BENZIMIDAZOLE DERIVATIVES 审中-公开
    • NOVEL BENZIMIDAZOLE DERIVATIVES
    • 新型苯并咪唑衍生物
    • WO2004002986A2
    • 2004-01-08
    • PCT/JP2003/008161
    • 2003-06-26
    • BANYU PHARMACEUTICAL CO., LTD. , OTAKE, Norikazu , MORIYA, Minoru , OGINO, Yoshio , MATSUDA, Kenji , NAGAE, Yoshikazu , KANATANI, Akio , FUKAMI, Takehiro
    • OTAKE, Norikazu , MORIYA, Minoru , OGINO, Yoshio , MATSUDA, Kenji , NAGAE, Yoshikazu , KANATANI, Akio , FUKAMI, Takehiro
    • C07D471/04
    • C07D473/30 , C07D405/04 , C07D471/04 , C07D471/10 , C07D473/00 , C07D491/04
    • A compound of the formula (I): (wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is - N(S0 2 R 4 )-, - N (COR 5 ) - or - CO-; Y is -C (R 6 ) (R 7 )_, -0- or -N (R 8 )_, provided that the compound (I) when E is nitrogen, n is 0, X is -CO-, and Y is - 0- is excluded) is useful as an agent 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, arteriosclerosis, etc., central 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, hypercholesterolemia, hyperlipidemia, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorder, inflammatory diseases or glaucoma, and the like, also for example, atherosclerosis, hypogonadism, hyperandrogenism, polycystic ovary syndrome, hirsutism, gastro-intestinal motility disorder, obesity-related gastro-esophageal reflux, obesity hypoventilation (Pickwickian syndrome), sleep apnea, inflammation, systemic inflammation of the vasculature, osteoarthritis, insulin resistance, bronchoconstriction, alcohol preference, metabolic syndrome, Alzheimer's disease, cardiac hypertrophy, left ventricular hypertrophy, hypertriglyceridemia, low HDL cholesterol, cardiovascular disorders such as coronary heart disease (CHD), cerebrovascular disease, stroke, peripheral vascular disease, sudden death, gallbladder diseases, cancer (breast, endometrial, colon), breathlessness, hyperuricemia, impaired fertility, low back pain, and increased anesthetic risk.
    • 式（I）的化合物：其中A，B，C和D独立地为氮或任选取代的次甲基; E为氮，次甲基或羟基取代的次甲基; n为0或1; T，U，V和W为 独立的氮或任选取代的次甲基; X是-N（SO 2 R 4） - ， - N（COR 5） - 或 - CO-; Y是-C（R 6） 其中当E为氮时，化合物（I）为n，n为0，X为-CO-，Y为0〜 - 被排除）可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病如心绞痛，急性或充血性心力衰竭，心肌梗塞，高血压，肾病，电解质异常，血管痉挛，动脉硬化等， 中枢神经系统疾病如贪食症，抑郁症，焦虑症，癫痫发作，癫痫症，痴呆症，酗酒，戒酒，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，高胆固醇血症，高脂血症，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，胃肠疾病，呼吸系统疾病，炎性疾病或青光眼，以及 例如动脉粥样硬化，性腺机能减退，雄激素过多症，多囊卵巢综合征，多毛症，胃肠动力障碍，肥胖相关的胃食管反流，肥胖低通气（皮克维克综合征），睡眠呼吸暂停，炎症，脉管系统的全身炎症， 骨关节炎，胰岛素抵抗，支气管收缩，酒精偏爱，代谢综合征，阿尔茨海默病，心脏肥大，左心室肥大，高甘油三酯血症，低HDL胆固醇，心血管疾病如冠心病（CHD），脑血管疾病，中风，外周血管疾病，突发 死亡，胆囊疾病，癌症（乳腺癌，子宫内膜癌，结肠癌） ），呼吸困难，高尿酸血症，生育能力受损，腰痛，麻醉风险增加。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 4. 发明申请
      WO2004031175A2 N-SUBSTITUTE-2-OXODIHYDROPYRIDINE DERIVATES 审中-公开
    • N-SUBSTITUTE-2-OXODIHYDROPYRIDINE DERIVATES
    • N-取代-2-氧代二氢吡啶衍生物
    • WO2004031175A2
    • 2004-04-15
    • PCT/JP2003/012290
    • 2003-09-25
    • BANYU PHARMACEUTICAL CO., LTD. , SATO, Nagaaki , ANDO, Makoto , ISHIKAWA, Shiho , NAGASE, Tsuyoshi , NAGAI, Keita , KANATANI, Akio
    • SATO, Nagaaki , ANDO, Makoto , ISHIKAWA, Shiho , NAGASE, Tsuyoshi , NAGAI, Keita , KANATANI, Akio
    • C07D401/14
    • C07D213/80 , C07D401/04 , C07D401/14
    • A compound of the formula (I): (wherein Ar 1l and Ar 2 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; R 1 and R 2 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, f ormyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl; R 1 , R 4 and R 5 are independently hydrogen, cyano, halogen 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.
    • 式（I）的化合物：其中Ar 11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，芳基，低级 低级烷基氨基甲酰基和二低级烷基氨基甲酰基; R 1，R 4和R 5独立地是氢，氰基，卤素羟基或低级烷基，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，也可用 作为治疗贪食症，肥胖症或糖尿病的药物。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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