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1. 发明申请

WO2004011440A1 ベンズイミダゾール誘導体を有効成分とするメラニン凝集ホルモン受容体拮抗剤审中-公开
标题翻译：含有苯并咪唑衍生物作为活性成分的茂金属浓度激素受体拮抗剂
公开(公告)号：WO2004011440A1
公开(公告)日：2004-02-05
申请号：PCT/JP2003/009610
申请日：2003-07-29
申请人：萬有製薬株式会社 , 守谷実 , 金谷章生 , 岩浅央 , 石原あかね , 深見竹広
发明人：守谷実 , 金谷章生 , 岩浅央 , 石原あかね , 深見竹広
IPC分类号： C07D235/30
CPC分类号： C07D403/12 , A61K31/4184 , A61K31/4196 , A61K31/4245 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/55 , C07D235/30 , C07D401/04 , C07D401/12 , C07D403/04
摘要： Benzimidazole derivative of the general formula: [I] wherein each of B , B and B represents a hydrogen atom or a lower alkyl; R and R may be identical with or different from each other and represent lower alkyls, etc.; each of R and R represents a hydrogen atom, etc.; W represents a 3 to 8-membered aromatic or aliphatic heterocycle, etc.; and Ar represents a substituted or unsubstituted aromatic heterocycle, etc. This compound functions as an antagonist of melanin-concentrating hormone receptor and is useful as a drug for central diseases, circulatory diseases and metabolic diseases.
摘要翻译：苯并咪唑衍生物，其通式为：[I]其中B 1，B 2和B 3各自表示氢原子或低级烷基; R 1和R 2可以相同或不同，表示低级烷基等; R 3和R 4各自表示氢原子等; W表示3至8元芳族或脂族杂环等; 并且Ar表示取代或未取代的芳族杂环等。该化合物用作黑色素浓缩激素受体的拮抗剂，可用作中枢疾病，循环系统疾病和代谢性疾病的药物。

2. 发明申请

WO2002094825A1 新規スピロピペリジン誘導体审中-公开
标题翻译：新型螺吡啶衍生物
公开(公告)号：WO2002094825A1
公开(公告)日：2002-11-28
申请号：PCT/JP2002/004954
申请日：2002-05-22
申请人：萬有製薬株式会社 , 深見竹広 , 守谷実 , 菅卓哉
发明人：深見竹広 , 守谷実 , 菅卓哉
IPC分类号： C07D471/10
CPC分类号： C07D471/10 , A61K31/438 , A61K31/444 , A61K31/4709 , A61K31/4747 , A61K31/497 , A61K31/506
摘要： A compound represented by the general formula (I): (I) [wherein A means optionally substituted C 1−3 linear alkylene; Ar 1 means optionally substituted aryl or heteroaryl; n is 0 or 1; T, U, V, and W each means an optionally substituted methine group or a nitrogen atom, provided that at least two of these mean the methine group; X means a group represented by −N(SO 2 R 1 )−, −N(COR 2 )−, or −CO−; and Y means a group represented by −C(R 3 )(R 4 )−, −O−, or −N(R 5 )−]. The compound has NPY antagonism and is hence useful as a remedy for various diseases in which NPY participates, i.e., circulatory diseases such as hypertension, central diseases such as hyperphagia, metabolic diseases such as obesity and diabetes, sexual and reproductive dysfunction, digestive diseases such as movement disorders of the digestive tract, respiratory diseases, inflammation, glaucoma, etc.
摘要翻译：由通式（I）表示的化合物：（I）[其中A表示任选取代的C 1〜3 直链亚烷基; Ar 1表示任选取代的芳基或杂芳基; n为0或1; T，U，V和W各自表示任选取代的次甲基或氮原子，条件是它们中的至少两个表示次甲基; X表示由-N（SO 3）2，-S（CO 2） - 或 - -CO-表示的基团。并且Y表示由-C（R 3）3 - ， - O-或-N（R 5）5表示的基团。） - ]。该化合物具有NPY拮抗作用，因此可用作NPY参与的各种疾病的补救措施，即循环系统疾病如高血压，中枢性疾病如食欲过盛，代谢性疾病如肥胖和糖尿病，性和生殖功能障碍，消化性疾病作为消化道的运动障碍，呼吸系统疾病，炎症，青光眼等

3. 发明申请

WO2004069798A1 ピペリジン誘導体を有効成分とするメラニン凝集ホルモン受容体拮抗剤审中-公开
标题翻译：含有作为活性成分的哌啶衍生物的富含MELANIN浓度的HORMONE受体拮抗剂
公开(公告)号：WO2004069798A1
公开(公告)日：2004-08-19
申请号：PCT/JP2004/001326
申请日：2004-02-09
申请人：萬有製薬株式会社 , 守谷実 , 坂本俊浩 , 石川誠 , 金谷章生 , 深見竹広
发明人：守谷実 , 坂本俊浩 , 石川誠 , 金谷章生 , 深見竹広
IPC分类号： C07D211/26
CPC分类号： C07D401/04 , A61K31/438 , A61K31/4439 , A61K31/445 , C07D211/26 , C07D491/10
摘要： Melanin-concentrating hormone receptor antagonists containing as the active ingredient piperidine derivatives represented by the general formula [I]: [wherein R is hydrogen, hydroxyl, lower alkyl, or the like; R , R , R , R , R , R , R and R are each hydrogen, halogeno, or the like; W and W are each independently -O-, -CH2-,or the like; Y , Y , Y and Y are each -CH-, -CF-, -N-, or the like; Z is lower alkyl, a hetero-alicyclic group, or the like; Ar is a mono- or bi-cyclic aliphatic heterocycle or an aromatic heterocycle; and n is an integer of 1 to 8]. The compounds act as antagonist against melanin -concentrating hormone receptor and are useful as drugs for central diseases, circulatory diseases, or metabolic diseases.
摘要翻译：含有作为活性成分的通式[I]表示的哌啶衍生物的黑色素浓缩激素受体拮抗剂：其中R 1是氢，羟基，低级烷基等; R 2，R 3a，R 3b，R 4a，R 4b，R 5a，R 5b和R 6各自为氢，卤素等; W 1和W 2各自独立地为-O - ， - CH 2 - 等; Y 1，Y 2，Y 3和Y 4各自为-CH-，-CF-，-N-等; Z是低级烷基，杂脂环基等; Ar是单环或双环脂族杂环或芳族杂环; n为1〜8的整数]。该化合物作为拮抗黑色素浓度激素受体的拮抗剂，可用作中枢性疾病，循环系统疾病或代谢疾病的药物。

4. 发明申请

WO2003014083A1 スピロ化合物审中-公开
标题翻译： SPIRO化合物
公开(公告)号：WO2003014083A1
公开(公告)日：2003-02-20
申请号：PCT/JP2002/007922
申请日：2002-08-02
申请人：萬有製薬株式会社 , 深見竹広 , 野々下克昌 , 相良武 , 岸野博之
发明人：深見竹広 , 野々下克昌 , 相良武 , 岸野博之
IPC分类号： C07D209/96
CPC分类号： C07D401/12 , A61K31/4747 , C07D209/96 , C07D307/94 , C07D403/12 , C07D405/12 , C07D471/10 , C07D491/10
摘要： The invention relates to compounds represented by the general formula (‖) or the like: (‖) [wherein A is a linear C 1−6 hydrocarbon group which may be substituted or interrupted by oxygen or nitrogen; Ar 1 is an aryl or heteroaryl group which may be substituted; n is 0 or 1; R 0 is hydrogen or lower alkylene attached to an arbitrary binding site of A; T, U, V and W are each optionally substituted methine or nitrogen, with the proviso that at least two of them are each methine; X is −N(SO 2 R 1 )−, −N(COR 2 )−, or −CO−; Y is −C(R 3 )(R 4 )−, −O−, or −N(R 5 )−; and Z is methine or nitrogen]. The compounds exhibit NPY antagonism and are therefore useful as treating agents for various diseases in which NPY participates, e.g., circulatory diseases, central nervous system diseases such as hyperphagia, metabolic diseases such as obesity and diabetes, and so on.
摘要翻译：本发明涉及由通式（‖）等表示的化合物：（‖）[其中A是可以被氧或氮取代或中断的直链C 16-18烃基; Ar 1是可以被取代的芳基或杂芳基; n为0或1; R 0是氢或连接到A的任意结合位点的低级亚烷基; T，U，V和W各自是任选取代的次甲基或氮，条件是它们中的至少两个都是次甲基; X是-N（SO 2）n - ， - （COR 2） - 或-CO-; Y是-C（R 3）3， - 或-O-（R 5）。 Z是次甲基或氮]。化合物表现出NPY拮抗作用，因此可用作NPY参与的各种疾病的治疗剂，例如循环系统疾病，中枢神经系统疾病如食欲过盛，代谢疾病如肥胖症和糖尿病等。

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