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1. 发明申请

WO2004110375A2 COMBINATION THERAPY FOR THE TREATMENT OF DIABETES 审中-公开
标题翻译：用于治疗糖尿病的组合治疗
公开(公告)号：WO2004110375A2
公开(公告)日：2004-12-23
申请号：PCT/US2004/017291
申请日：2004-06-02
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , ERONDU, Ngozi, E. , FONG, Tung, M. , MACNEIL, Douglas, J. , VAN DER PLOEG, Leonardus, H. T. , KANATANI, Akio
发明人： ERONDU, Ngozi, E. , FONG, Tung, M. , MACNEIL, Douglas, J. , VAN DER PLOEG, Leonardus, H. T. , KANATANI, Akio
IPC分类号： A61K
CPC分类号： A61K31/4747 , A61K31/353 , A61K31/4196 , A61K31/498 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compositions comprising an anti-obesity agent and an anti-diabetic agent useful for the treatment of diabetes, diabetes associated with obesity and diabetes-related disorders. The present invention further relates to methods of treating or preventing obesity, and obesity-related disorders, in a subject in need thereof by administering a composition of the present invention. The present invention further provides for pharmaceutical compositions, medicaments, and kits useful in carrying out these methods.
摘要翻译：本发明涉及包含抗肥胖剂和用于治疗糖尿病的抗糖尿病药物，与肥胖相关的糖尿病和糖尿病相关疾病的组合物。本发明还涉及通过给予本发明的组合物来治疗或预防有需要的受试者中肥胖和肥胖相关疾病的方法。本发明进一步提供可用于实施这些方法的药物组合物，药物和试剂盒。

2. 发明申请

WO03076443A9 SPIRO COMPOUNDS WITH NPY ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有NPY拮抗活性的SPIRO化合物
公开(公告)号：WO03076443A9
公开(公告)日：2005-01-20
申请号：PCT/JP0302611
申请日：2003-03-05
申请人： BANYU PHARMA CO LTD , FUKAMI TAKEHIRO , KANATANI AKIO , ISHIHARA AKANE , ISHII YASUYUKI , TAKAHASHI TOSHIYUKI , HAGA YUJI , SAKAMOTO TOSHIHIRO , ITOH TAKAHIRO , CHIBA MASATO
发明人： FUKAMI TAKEHIRO , KANATANI AKIO , ISHIHARA AKANE , ISHII YASUYUKI , TAKAHASHI TOSHIYUKI , HAGA YUJI , SAKAMOTO TOSHIHIRO , ITOH TAKAHIRO , CHIBA MASATO
IPC分类号： C07D491/107 , A61K31/438 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/04 , A61P9/10 , 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 , C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10 , C07D519/00
CPC分类号： C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10
摘要： A compound represented by the general formula (I): wherein Ar represents an aryl or heteroaryl which may be substituted, n represents 0 or 1: T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen, and a salt, ester or N-oxide derivative thereof exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis and the like.
摘要翻译：由通式（I）表示的化合物：其中Ar 1表示可被取代的芳基或杂芳基，n表示0或1：T，U，V和W各自独立地表示氮原子或次甲基，可以具有选自卤素，低级烷基，羟基和低级烷氧基的取代基，其中至少两个表示所述次甲基; X表示次甲基，羟基取代的次甲基或氮原子; Y表示可被低级烷基或氧取代的亚氨基，其盐，酯或N-氧化物衍生物表现出NPY拮抗活性，可用作治疗与NPY有关的各种疾病的药剂，例如心血管疾病如高血压，肾病，心脏病，血管痉挛，动脉硬化等。

3. 发明申请

WO2004002986A2 NOVEL BENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译：新型苯并咪唑衍生物
公开(公告)号：WO2004002986A2
公开(公告)日：2004-01-08
申请号：PCT/JP2003/008161
申请日：2003-06-26
申请人： BANYU PHARMACEUTICAL CO., LTD. , OTAKE, Norikazu , MORIYA, Minoru , OGINO, Yoshio , MATSUDA, Kenji , NAGAE, Yoshikazu , KANATANI, Akio , FUKAMI, Takehiro
发明人： OTAKE, Norikazu , MORIYA, Minoru , OGINO, Yoshio , MATSUDA, Kenji , NAGAE, Yoshikazu , KANATANI, Akio , FUKAMI, Takehiro
IPC分类号： C07D471/04
CPC分类号： C07D473/30 , C07D405/04 , C07D471/04 , C07D471/10 , C07D473/00 , C07D491/04
摘要： 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.
摘要翻译：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。

4. 发明申请

WO1998025908A1 NOVEL AMINOPYRAZOLE DERIVATIVES 审中-公开
标题翻译：新型氨基吡唑衍生物
公开(公告)号：WO1998025908A1
公开(公告)日：1998-06-18
申请号：PCT/JP1997004571
申请日：1997-12-12
申请人： BANYU PHARMACEUTICAL CO., LTD. , FUKAMI, Takehiro , FUKURODA, Takahiro , KANATANI, Akio , IHARA, Masaki
发明人： BANYU PHARMACEUTICAL CO., LTD.
IPC分类号： C07D231/40
CPC分类号： C07D401/12 , C07D231/40
摘要： Compounds represented by general formula (I), (wherein Ar represents an aryl group which may be substituted with a group selected among halogen atoms and lower alkyl and halogenated lower alkyl groups; Ar represents an aryl group or a heteroaromatic group which may be substituted with a group selected among halogen atoms and lower alkyl, lower alkenyl, halogenated lower alkyl, lower alkoxy, lower alkylthio, lower alkylamino, di(lower alkyl)amino, and aryl groups; R and R , which may be the same or different, represent each a hydrogen atom or a lower alkyl group; R and R , which may be the same or different, represent each a hydrogen atom or a lower alkyl group, or R and R combine with each other to form an alkylene group bearing 2 to 4 carbon atoms and optionally having a lower alkyl group; and R represents a hydrogen atom or a lower alkyl or lower alkoxy group) or salts thereof; a process for preparing the same; and a therapeutic agent for bulimia, obesity, or diabetes, comprising the compound or salt thereof as the active ingredient.
摘要翻译：由通式（I）表示的化合物（其中Ar 1表示可以被选自卤素原子和低级烷基和卤代低级烷基的基团取代的芳基; Ar 2表示芳基或杂芳族可以被选自卤素原子和低级烷基，低级烯基，卤代低级烷基，低级烷氧基，低级烷硫基，低级烷基氨基，二（低级烷基）氨基和芳基的基团取代的基团; R 1和R 2' 2'可以相同或不同，表示氢原子或低级烷基; R 3和R 4可以相同或不同，表示氢原子或低级烷基或R 3和R 4彼此结合形成具有2至4个碳原子并且任选具有低级烷基的亚烷基; R 5表示氢原子或低级烷基或低级烷氧基基团）或其盐; 其制备方法; 以及包含其化合物或其盐作为活性成分的贪食症，肥胖症或糖尿病的治疗剂。

5. 发明申请

WO2004031175A3 N-SUBSTITUTED-2-OXODIHYDROPYRIDINE DERIVATIVES AS NPY ANTAGONISTS 审中-公开
标题翻译： N-取代的2-氧代二氢吡啶衍生物作为NPY拮抗剂
公开(公告)号：WO2004031175A3
公开(公告)日：2005-02-24
申请号：PCT/JP0312290
申请日：2003-09-25
申请人： BANYU PHARMA CO LTD , SATO NAGAAKI , ANDO MAKOTO , ISHIKAWA SHIHO , NAGASE TSUYOSHI , NAGAI KEITA , KANATANI AKIO
发明人： SATO NAGAAKI , ANDO MAKOTO , ISHIKAWA SHIHO , NAGASE TSUYOSHI , NAGAI KEITA , KANATANI AKIO
IPC分类号： A61P3/04 , C07D213/80 , C07D401/04 , C07D401/14 , A61K31/444
CPC分类号： C07D213/80 , C07D401/04 , C07D401/14
摘要： A compound of the formula (I): (wherein Ar and Ar 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 and R 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 , R and R 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.
摘要翻译：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。

6. 发明申请

WO2003076443A1 SPIRO COMPOUNDS WITH NPY ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有NPY拮抗活性的SPIRO化合物
公开(公告)号：WO2003076443A1
公开(公告)日：2003-09-18
申请号：PCT/JP2003/002611
申请日：2003-03-05
申请人： BANYU PHARMACEUTICAL CO., LTD. , FUKAMI, Takehiro , KANATANI, Akio , ISHIHARA, Akane , ISHII, Yasuyuki , TAKAHASHI, Toshiyuki , HAGA, Yuji , SAKAMOTO, Toshihiro , ITOH, Takahiro , CHIBA, Masato
发明人： FUKAMI, Takehiro , KANATANI, Akio , ISHIHARA, Akane , ISHII, Yasuyuki , TAKAHASHI, Toshiyuki , HAGA, Yuji , SAKAMOTO, Toshihiro , ITOH, Takahiro , CHIBA, Masato
IPC分类号： C07D491/10
CPC分类号： C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10
摘要： A compound represented by the general formula (I): wherein Ar 1 represents an aryl or heteroaryl which may be substituted, n represents 0 or 1: T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen, and a salt, ester or N-oxide derivative thereof exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis and the like.
摘要翻译：由通式（I）表示的化合物：其中Ar1表示可被取代的n的芳基或杂芳基，表示0或1：T，U，V和W各自独立地表示可以具有取代基的氮原子或次甲基选自卤素，低级烷基，羟基和低级烷氧基，其中至少两个表示所述次甲基; X表示次甲基，羟基取代的次甲基或氮原子; Y表示可以被低级烷基或氧取代的亚氨基，其盐，酯或N-氧化物衍生物表现出NPY拮抗活性，可用作治疗与NPY有关的各种疾病的药剂，例如心血管疾病如高血压，肾病，心脏病，血管痉挛，动脉硬化等。

7. 发明申请

WO9847505A9 NEUROPEPTIDE Y RECEPTOR ANTAGONIST 审中-公开
标题翻译：神经元Y受体拮抗剂
公开(公告)号：WO9847505A9
公开(公告)日：1999-03-25
申请号：PCT/JP9801855
申请日：1998-04-22
申请人： BANYU PHARMA CO LTD , FUKAMI TAKEHIRO , FUKURODA TAKAHIRO , KANATANI AKIO , IHARA MASAKI , OKABE TAKAYOSHI
发明人： FUKAMI TAKEHIRO , FUKURODA TAKAHIRO , KANATANI AKIO , IHARA MASAKI , OKABE TAKAYOSHI
IPC分类号： A61K31/352 , C07D311/82 , A61K31/35
CPC分类号： C07D311/82 , A61K31/352
摘要： A neuropeptide Y receptor antagonist containing the compound of formula (I) as the active ingredient.
摘要翻译：含有式（I）化合物作为活性成分的神经肽Y受体拮抗剂。

8. 发明申请

WO1998027063A1 AMINOPYRAZOLE DERIVATIVES 审中-公开
标题翻译：氨基吡唑衍生物
公开(公告)号：WO1998027063A1
公开(公告)日：1998-06-25
申请号：PCT/JP1997004569
申请日：1997-12-12
申请人： BANYU PHARMACEUTICAL CO., LTD. , FUKAMI, Takehiro , FUKURODA, Takahiro , KANATANI, Akio , IHARA, Masaki
发明人： BANYU PHARMACEUTICAL CO., LTD.
IPC分类号： C07D231/40
CPC分类号： C07D231/38 , C07D231/40 , C07D401/04
摘要： Compounds represented by general formula (I): wherein Ar represents an aryl group or a heteroaromatic group which may be substituted with a group selected among halogen atoms and lower alkyl, lower alkenyl, halogenated lower alkyl, lower alkoxy, lower alkylthio, lower alkylamino, di(lower alkyl)amino, acyl, and aryl groups; Ar represents an aryl group or heteroaromatic group which may be substituted with a group selected among halogen atoms and lower alkyl, lower alkenyl, halogenated lower alkyl, lower alkoxy, lower alkylthio, lower alkylamino; di(lower alkyl)amino, and aryl groups; n is 0, 1, or 2; and R and R , which may be the same or different, represent each a hydrogen atom or a lower alkyl group or a salts thereof; a process for preparing the same; and a therapeutic agent for bulimia, obesity, or diabetes, comprising the compound or salt thereof as the active ingredient.
摘要翻译：由通式（I）表示的化合物：其中Ar 1表示可以被选自卤素原子和低级烷基，低级烯基，卤代低级烷基，低级烷氧基，低级烷硫基，低级烷氧基，低级烷基氨基，二（低级烷基）氨基，酰基和芳基; Ar 2表示可以被选自卤素原子和低级烷基，低级烯基，卤代低级烷基，低级烷氧基，低级烷硫基，低级烷基氨基的基团取代的芳基或杂芳基; 二（低级烷基）氨基和芳基; n为0,1或2; 和R 1和R 2可以相同或不同，表示氢原子或低级烷基或其盐; 其制备方法; 以及包含其化合物或其盐作为活性成分的贪食症，肥胖症或糖尿病的治疗剂。

9. 发明申请

WO1997034873A1 AMINOPYRIDINE DERIVATIVES 审中-公开
标题翻译：氨基吡啶衍生物
公开(公告)号：WO1997034873A1
公开(公告)日：1997-09-25
申请号：PCT/JP1997000890
申请日：1997-03-19
申请人： BANYU PHARMACEUTICAL CO., LTD. , FUKAMI, Takehiro , MASE, Toshiaki , TSUCHIYA, Yoshimi , KANATANI, Akio , FUKURODA, Takahiro
发明人： BANYU PHARMACEUTICAL CO., LTD.
IPC分类号： C07D213/74
CPC分类号： C07D417/06 , C07D213/74 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12 , C07D417/14
摘要： Compounds of general formula [I] or pharmaceutically acceptable salts thereof; and agents for the treatment of hyperphagia, obesity or diabetes, comprising the same as the active ingredient wherein Ar is aryl or hetero-aryl which may be substituted with a radical selected from the group consisting of lower alkyl, lower hydroxyalkyl, lower alkylene and -NR R ; R is hydrogen or lower alkyl; R and R are each independently lower alkyl, or alternatively R and R are united to form alkylene which may be interrupted by oxygen or sulfur and may be substituted with one or two lower alkyl radicals; R is hydrogen or lower alkyl which may be substituted with a radical selected from the group consisting of hydroxyl, amino, carbamoyl and lower alkoxycarbonyl; Ar is aryl or hetero-aryl which may be substituted with a radical selected from the group consisting of halogeno, hydroxyl, lower alkyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower hydroxyalkyl, lower alkoxy lower alkyl, -NR Rc and -NR -CO-NR R ; and W is oxygen, sulfur, -CHR - or -NR -.
摘要翻译：通式[I]的化合物或其药学上可接受的盐; 以及用于治疗肥胖，肥胖或糖尿病的药物，其包含与活性成分相同的活性成分，其中Ar 1是可以被选自下列的基团取代的芳基或杂芳基：低级烷基，低级羟烷基，低级亚烷基和-NR a R b; R 1是氢或低级烷基; R 2和R 3各自独立地为低级烷基，或者R 2和R 3相互结合形成可被氧或硫中断的亚烷基并且可以被一个或两个低级烷基取代 ; R 4是氢或可以被选自羟基，氨基，氨基甲酰基和低级烷氧基羰基的基团取代的低级烷基; Ar 2是可以被选自卤代，羟基，低级烷基，低级卤代烷基，低级烷氧基，低级烷硫基，低级羟烷基，低级烷氧基低级烷基，-NR' c> R c和-NR e -CO-NR f R g; W是氧，硫，-CHR j - 或-NR k - 。

10. 发明申请

WO2005028438A9 NOVEL PIPERIDINE DERIVATIVE 审中-公开
标题翻译：新型哌啶衍生物
公开(公告)号：WO2005028438A9
公开(公告)日：2005-05-26
申请号：PCT/JP2004013768
申请日：2004-09-21
申请人： BANYU PHARMA CO LTD , OHTAKE NORIKAZU , MIZUTANI SAYAKA , YOSHIMOTO RYO , TOKITA SHIGERU , KANATANI AKIO
发明人： OHTAKE NORIKAZU , MIZUTANI SAYAKA , YOSHIMOTO RYO , TOKITA SHIGERU , KANATANI AKIO
IPC分类号： A61K31/454 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P19/06 , A61P25/02 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/36 , A61P43/00 , C07D211/58 , A61K31/4523 , A61K31/4535 , A61K31/4545 , A61K31/496 , A61K31/506 , C07D401/02 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/12
CPC分类号： C07D211/58 , A61K31/454
摘要： A histamine H3-receptor antagonist; and a therapeutic and/or preventive agent for metabolic diseases, e.g., obesity and diabetes, various diseases such as, e.g., angina pectoris and acute/congestive heart failure, circulatory diseases such as, e.g., idiopathic narcolepsy and recurrent narcolepsy, and central and peripheral nerve diseases such as, e.g., bulimia, affective disorders, and depression. The histamine H3-receptor antagonist is characterized by containing a piperidine derivative represented by the general formula (I) [wherein X and X each independently represents nitrogen or CH; Y represents a specific group; X represents Os-(CH2)m; R and R each independently represents hydrogen, halogeno, linear or branched lower alkyl, lower alkoxy, or acetyl substituted by 2 or 3 fluorine atoms; s is 0 or 1; and m is such an integer that (m+s) is 0 to 4] or a pharmaceutically acceptable salt of the derivative.
摘要翻译：组胺H3受体拮抗剂; 以及用于代谢疾病例如肥胖和糖尿病的治疗和/或预防剂，各种疾病，例如心绞痛和急性/充血性心力衰竭，循环系统疾病例如特发性发作性睡病和复发性发作性睡病，以及中枢和周围神经疾病，例如贪食症，情感障碍和抑郁症。组胺H3受体拮抗剂的特征在于含有由通式（I）表示的哌啶衍生物[其中X 1和X 2各自独立地表示氮或CH; Y表示特定组; X 3表示Os-（CH 2）m; R 1和R 2各自独立地表示氢，卤素，直链或支链的低级烷基，低级烷氧基或被2或3个氟原子取代的乙酰基; s为0或1; m是（m + s）为0〜4的整数]或该衍生物的药学上可接受的盐。

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