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71. 发明申请

US20090029406A1 Npy Y4 Agonist as Therapeutic Agent for Disease Accompanied by Intestinal Tract Dysfunction 审中-公开
标题翻译： Npy Y4激动剂作为伴随肠道功能障碍的疾病治疗剂
公开(公告)号：US20090029406A1
公开(公告)日：2009-01-29
申请号：US12223573
申请日：2007-02-23
申请人： Jun Suzuki , Ryuichi Moriya , Hiroyasu Hirose , Tetsuya Kanno , Akio Kanatani
发明人： Jun Suzuki , Ryuichi Moriya , Hiroyasu Hirose , Tetsuya Kanno , Akio Kanatani
IPC分类号： G01N33/68 , G01N33/53 , C12Q1/02 , C07K2/00
CPC分类号： C07K14/57545 , A61K38/00 , A61K38/22 , G01N33/5023 , G01N33/5041 , G01N2333/5755 , G01N2800/06
摘要： The present invention has its object to provide an agent capable of ameliorating the intestinal tract dysfunction through a novel mechanism of action. It also has its object to provide a method for the evaluation of a compound, including the screening of the agent. A disease accompanied by intestinal tract dysfunction can be ameliorated or treated by using an NPY Y4 agonist as a therapeutic agent. A compound capable of ameliorating or treating a disease accompanied by intestinal tract dysfunction can be evaluated or screened by evaluating a compound targeting to an NPY Y4 receptor.
摘要翻译：本发明的目的是提供能够通过新的作用机制改善肠道功能障碍的药剂。本发明的目的还在于提供一种化合物的评估方法，包括筛选试剂。伴随肠道功能障碍的疾病可以通过使用NPY Y4激动剂作为治疗剂来改善或治疗。可以通过评估靶向NPY Y4受体的化合物来评估或筛选能够改善或治疗伴随肠道功能障碍的疾病的化合物。

72. 发明申请

US20070031833A1 Method For Examining Obesity Or Leanness 失效
标题翻译：检查肥胖或瘦身的方法
公开(公告)号：US20070031833A1
公开(公告)日：2007-02-08
申请号：US10548772
申请日：2004-03-12
申请人： Hidehito Kotani , Hiraku Itadani , Hiromitsu Araki , Kazuhiko Takahashi , Satoshi Mashiko , Akane Ishihara , Akio Kanatani
发明人： Hidehito Kotani , Hiraku Itadani , Hiromitsu Araki , Kazuhiko Takahashi , Satoshi Mashiko , Akane Ishihara , Akio Kanatani
IPC分类号： C12Q1/68 , G01N33/567
CPC分类号： C12Q1/6883 , C12Q2600/136 , C12Q2600/156 , C12Q2600/158 , G01N33/5088 , G01N33/6893 , G01N2800/044 , G01N2800/52
摘要： In the examination of obesity or leanness, the examination is based on the expression level of the MCP-1 gene or the MCP-1 protein in a tissue or cell analyte, or on the polymorphism in the gene. In the evaluation of compounds, including screening for therapeutic agents for obesity or leanness, the properties of the MCP-1 gene or the MCP-1 protein are utilized to carry out the evaluation.
摘要翻译：在检查肥胖或瘦身时，检查是基于组织或细胞分析物中MCP-1基因或MCP-1蛋白的表达水平，或基于该基因的多态性。在化合物的评价中，包括筛选肥胖或瘦身的治疗剂，使用MCP-1基因或MCP-1蛋白的性质进行评价。

73. 发明授权

US07105526B2 Benzimidazole derivatives 失效
标题翻译：苯并咪唑衍生物
公开(公告)号：US07105526B2
公开(公告)日：2006-09-12
申请号：US10463390
申请日：2003-06-18
申请人： Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
发明人： Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
IPC分类号： A61K31/52 , C07D239/70
CPC分类号： C07D473/30 , C07D405/04 , C07D471/04 , C07D471/10 , C07D473/00 , C07D491/04
摘要： The present invention relates to novel benzimidazole derivatives which are useful as neuropeptide Y receptor antagonists.
摘要翻译：本发明涉及可用作神经肽Y受体拮抗剂的新型苯并咪唑衍生物。

74. 发明申请

US20060106046A1 Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient 失效
标题翻译：黑色素浓缩激素受体拮抗剂含有哌啶衍生物作为活性成分
公开(公告)号：US20060106046A1
公开(公告)日：2006-05-18
申请号：US10544261
申请日：2004-02-09
申请人： Minoru Moriya , Toshihiro Sakamoto , Makoto Ishikawa , Akio Kanatani , Takehiro Fukami
发明人： Minoru Moriya , Toshihiro Sakamoto , Makoto Ishikawa , Akio Kanatani , Takehiro Fukami
IPC分类号： A61K31/4747 , A61K31/4545 , C07D471/10 , C07D401/02
CPC分类号： C07D401/04 , A61K31/438 , A61K31/4439 , A61K31/445 , C07D211/26 , C07D491/10
摘要： The invention provides melanin-concentrating hormone receptor antagonists containing as the active ingredient piperidine derivatives represented by the general formula [I]: [wherein R1 is hydrogen, hydroxyl, lower alkyl, or the like; R2, R3a, R3b, R4a, R4b, R5a, R5b and R6 each stands for hydrogen, halogen, or the like; W1 and W2 each independently stands for —O—, —CH2—, or the like; Y1, Y2, Y3 and Y4 stand for —CH—, —CF—, —N—, or the like; Z stands for lower alkyl, an aliphatic heterocyclic 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：本发明提供了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 3，R 3b，R 4a，R 4b，R 4b， R 5a，R 5b和R 6各自代表氢，卤素等; W 1和W 2各自独立地代表-O-，-CH 2 - 等; Y 1，Y 2，Y 3和Y 4代表-CH - ， - CF - ， - N-等; Z代表低级烷基，脂族杂环基等; 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素浓缩激素受体的拮抗剂，可用作中枢疾病，循环系统疾病或代谢疾病的药物。

75. 发明授权

US06495559B2 NPY Y5 receptor antagonists 失效
标题翻译： NPY Y5受体拮抗剂
公开(公告)号：US06495559B2
公开(公告)日：2002-12-17
申请号：US09896940
申请日：2001-06-29
申请人： Ying-Duo Gao , Douglas J. MacNeil , Lihu Yang , Nancy R. Morin , Takehiro Fukami , Akio Kanatani , Takahiro Fukuroda , Yasuyuki Ishii , Masaki Ihara
发明人： Ying-Duo Gao , Douglas J. MacNeil , Lihu Yang , Nancy R. Morin , Takehiro Fukami , Akio Kanatani , Takahiro Fukuroda , Yasuyuki Ishii , Masaki Ihara
IPC分类号： C07D22120
CPC分类号： C07D221/20 , C07D471/10
摘要： Compounds of general structural formula I such as that shown in structural formula II are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.
摘要翻译：一般结构式I的化合物如结构式II所示的化合物是选择性NPY Y5受体拮抗剂，可用于治疗肥胖症及其相关并发症。

76. 发明授权

US06258837B1 Neuropeptide Y receptor antagonist 失效
标题翻译：神经肽Y受体拮抗剂
公开(公告)号：US06258837B1
公开(公告)日：2001-07-10
申请号：US09403031
申请日：1999-12-08
申请人： Takehiro Fukami , Takahiro Fukuroda , Akio Kanatani , Masaki Ihara , Takayoshi Okabe
发明人： Takehiro Fukami , Takahiro Fukuroda , Akio Kanatani , Masaki Ihara , Takayoshi Okabe
IPC分类号： A01N4316
CPC分类号： C07D311/82 , A61K31/352
摘要： The present invention relates to a neuropeptide Y receptor antagonist comprising a compound represented by the formula [I]: as an active ingredient.
摘要翻译：本发明涉及包含由式[I]表示的化合物作为活性成分的神经肽Y受体拮抗剂。

77. 发明授权

US06191160B1 Spiro-indolines as Y5 receptor antagonists 失效
标题翻译：螺吲哚啉作为Y5受体拮抗剂
公开(公告)号：US06191160B1
公开(公告)日：2001-02-20
申请号：US09436120
申请日：1999-11-08
申请人： Ying-Duo Gao , Douglas J. MacNeil , Lihu Yang , Nancy R. Morin , Takehiro Fukami , Akio Kanatani , Takahiro Fukuroda , Yasuyuki Ishii , Masaki Ihara
发明人： Ying-Duo Gao , Douglas J. MacNeil , Lihu Yang , Nancy R. Morin , Takehiro Fukami , Akio Kanatani , Takahiro Fukuroda , Yasuyuki Ishii , Masaki Ihara
IPC分类号： A61K31495
CPC分类号： C07D221/20 , C07D471/10
摘要： Compounds of the general structural formula I are selective NPY Y5 receptor antagonists. The compounds and compositions of the present invention are useful in the treatment of obesity and complications associated therewith.
摘要翻译：化合物的一般结构式Iare选择性NPY Y5受体拮抗剂。本发明的化合物和组合物可用于治疗与其相关的肥胖症和并发症。

78. 发明授权

US06180653B2 Aminopyrazole derivatives 失效
标题翻译：氨基吡唑衍生物
公开(公告)号：US06180653B2
公开(公告)日：2001-01-30
申请号：US09319912
申请日：1999-07-28
申请人： Takehiro Fukami , Takahiro Fukuroda , Akio Kanatani , Masaki Ihara
发明人： Takehiro Fukami , Takahiro Fukuroda , Akio Kanatani , Masaki Ihara
IPC分类号： C07D40104
CPC分类号： C07D231/38 , C07D231/40 , C07D401/04
摘要： The present invention relates to a compound represented by the general formula [I]: wherein Ar1 represents an aryl or heteroaryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino, acyl and aryl groups; Ar2 represents an aryl or heteroaryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino and aryl groups; n is zero, 1 or 2; and R1 and R2 may be the same or different and each represents a hydrogen atom or a lower alkyl group, or its salt, a method for its preparation as well as an agent for the treatment of bulimia, obesity or diabetes comprising it as an active ingredient.
摘要翻译：本发明涉及由通式[I]表示的化合物：其中Ar 1表示可以具有选自卤素原子和低级烷基，低级链烯基，低级卤代烷基，低级烷氧基，低级烷硫基，低级烷基氨基，低级二烷基氨基，酰基和芳基; Ar2表示可以具有选自卤素原子和低级烷基，低级烯基，低级卤代烷基，低级烷氧基，低级烷硫基，低级烷基氨基，低级二烷基氨基和芳基的取代基的芳基或杂芳基; n为零，1或2; 并且R 1和R 2可以相同或不同，并且各自表示氢原子或低级烷基，或其盐，其制备方法以及用于治疗贪食，肥胖症或糖尿病的药物，其包含其作为活性物质成分。

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