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1. 发明申请

US20090209562A1 Fused ring 4-oxopyrimidine derivative 有权
公开(公告)号：US20090209562A1
公开(公告)日：2009-08-20
申请号：US12378163
申请日：2009-02-11
申请人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
发明人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
IPC分类号： A61K31/517 , C07D239/88 , A61P25/00
CPC分类号： C07D239/91 , A61K31/517 , A61K31/55 , A61K45/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D487/08 , A61K2300/00
摘要： The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).]

2. 发明授权

US07531668B2 2-arylcarboxamide-nitrogenous heterocycle compound 失效
标题翻译： 2-芳基羧酰胺 - 含氮杂环化合物
公开(公告)号：US07531668B2
公开(公告)日：2009-05-12
申请号：US11663038
申请日：2005-09-30
申请人： Takao Suzuki , Minoru Moriya , Shunji Sakuraba , Sayaka Mizutani , Hisashi Iwaasa , Akio Kanatani
发明人： Takao Suzuki , Minoru Moriya , Shunji Sakuraba , Sayaka Mizutani , Hisashi Iwaasa , Akio Kanatani
IPC分类号： C07D235/12 , C07D209/12 , C07D211/06 , C07D401/12 , C07D291/04 , C07D291/06 , C07D279/02 , C07D279/06 , C07D279/12 , C07D265/02 , C07D265/06 , C07D265/30 , C07D257/04 , C07D257/08 , C07D251/04 , C07D237/04
CPC分类号： C07D209/42 , C07D235/24 , C07D401/12
摘要： A compound represented by the formula [I]: [wherein R1 and R2 are the same or different and each represents C1-6 alkyl, C3-8 cycloalkyl, et al; R3a, R3b, and R4 are the same or different and each represents hydrogen, C1-6 alkyl, et al; X represents —N—, —CH—, et al; Y1 represents a single bond, C1-3 alkylene, et al; Y2 represents C1-4 alkylene, oxy(C1-4 alkylene), et al; Ar1 represents a monocyclic aromatic carbocyclic group, monocyclic aromatic heterocyclic group, et al; and Ar2 represents a 5- or 6-membered aromatic carbocyclic group, aromatic heterocyclic group, et al]. This compound functions as a melanin-concentrating hormone receptor antagonist and is useful as, e.g., a therapeutic agent for obesity, et al.
摘要翻译：由式[I]表示的化合物：其中R 1和R 2相同或不同，各自表示C 1-6烷基，C 3-8环烷基等; R3a，R3b和R4相同或不同，各自表示氢，C1-6烷基等; X表示-N-，-CH-等; Y1表示单键，C1-3亚烷基等; Y2代表C1-4亚烷基，氧基（C1-4亚烷基）等; Ar 1表示单环芳族碳环基团，单环芳族杂环基团等; 和Ar 2表示5或6元芳族碳环基团，芳族杂环基团等。该化合物起着黑色素浓缩激素受体拮抗剂的作用，可用作例如肥胖症的治疗剂等。

3. 发明申请

US20090105136A1 NPY Y2 Agonist for Use as Therapeutic Agent for Disease Accompanied by Diarrhea 审中-公开
标题翻译： NPY Y2激动剂用作腹泻伴随疾病的治疗剂
公开(公告)号：US20090105136A1
公开(公告)日：2009-04-23
申请号：US11921483
申请日：2006-06-06
申请人： Jun Suzuki , Ryuichi Moriya , Hiroyasu Hirose , Akio Kanatani
发明人： Jun Suzuki , Ryuichi Moriya , Hiroyasu Hirose , Akio Kanatani
IPC分类号： A61K38/16 , C07K14/00 , G01N33/53 , A61P1/12 , C12Q1/02 , G01N33/68
CPC分类号： G01N33/5041 , A61K38/22 , G01N33/5023 , G01N33/74 , G01N2333/5755 , G01N2800/06
摘要： An NPY Y2 agonist is used as a therapeutic agent for a disease accompanied by diarrhea. A compound capable of treating the disease can be evaluated and screened by examining the compound on the targeting to an NPY Y2 receptor. An agent capable of inhibiting the diarrhea by a novel mechanism of action; and a method for evaluation of a compound, including the screening for the agent.
摘要翻译：使用NPY Y2激动剂作为伴有腹泻的疾病的治疗剂。可以通过检查靶向化合物至NPY Y2受体来评估和筛选能够治疗该疾病的化合物。能够通过新的作用机制抑制腹泻的药剂; 以及化合物的评价方法，包括筛选试剂。

4. 发明授权

US07510833B2 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：US07510833B2
公开(公告)日：2009-03-31
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 , C07H21/04 , C12P19/34
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。

5. 发明授权

US07304072B2 Spiro compounds 失效
标题翻译：螺环化合物
公开(公告)号：US07304072B2
公开(公告)日：2007-12-04
申请号：US10922869
申请日：2004-08-23
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh , Masato Chiba
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh , Masato Chiba
IPC分类号： A61K31/4355 , C07D491/048
CPC分类号： C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10
摘要： Compounds represented by the general formula (I) wherein Ar1 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. The compounds exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases, sexual and reproductive dysfunctions, gastro-intestinal disorders, respiratory disorders, inflammation or glaucoma, and the like.
摘要翻译：由通式（I）表示的化合物

6. 发明申请

US20050182045A1 Fused ring 4-oxopyrimidine derivative 有权
标题翻译：稠环4-氧代嘧啶衍生物
公开(公告)号：US20050182045A1
公开(公告)日：2005-08-18
申请号：US11058444
申请日：2005-02-14
申请人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
发明人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
IPC分类号： A61K31/4725 , A61K31/517 , A61K31/519 , A61K31/55 , A61K45/06 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P3/12 , A61P5/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P19/06 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/36 , A61P43/00 , C07D217/24 , C07D239/70 , C07D239/91 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D471/04 , C07D487/08 , C07D43/02
CPC分类号： C07D239/91 , A61K31/517 , A61K31/55 , A61K45/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D487/08 , A61K2300/00
摘要： The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).]
摘要翻译：本发明提供下述式（I）表示的化合物或其药学上可接受的盐，其具有组胺H3受体拮抗剂或反向激动剂活性，可用于预防或治疗代谢性疾病，循环系统疾病或神经系统疾病 [其中，例如，Ar为通过从苯中除去两个氢原子形成的二价基团，X 1是氮原子，硫原子或氧原子，R 1是 5-至6-元杂芳基，环A为5-至6-元杂芳基环，R 2和R 3为氨基或烷基氨基，和 X 2由式（II）表示：其中R 4和R 5是低级烷基，n是2的整数至4）。]

7. 发明授权

US06803372B2 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06803372B2
公开(公告)日：2004-10-12
申请号：US10092549
申请日：2002-03-08
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K31506
CPC分类号： C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10
摘要： Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.
摘要翻译：通式（I）的化合物：其中Ar 1表示任选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任选取代的次甲基，其中至少两个代表所述次甲基; X表示次甲基或羟基取代的次甲基; Y表示任选取代的亚氨基或氧原子。这些新颖的螺环化合物可用作神经肽Y受体拮抗剂和用作治疗各种心血管疾病，中枢神经系统疾病，代谢疾病等的药剂。

8. 发明授权

US06723847B2 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06723847B2
公开(公告)日：2004-04-20
申请号：US10453737
申请日：2003-06-04
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： C07D40514
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： The present invention is directed to novel spiro compounds useful as neuropeptide Y receptor antagonists.
摘要翻译：本发明涉及可用作神经肽Y受体拮抗剂的新型螺环化合物。

9. 发明授权

US06313298B1 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：US06313298B1
公开(公告)日：2001-11-06
申请号：US09656698
申请日：2000-09-07
申请人： Ying-Duo Gao , Lihu Yang , Douglas J. MacNeil , Nancy R. Morin , Takehiro Fukami , Takahiro Fukuroda , Akio Kanatani , Yasuyuki Ishii , Masaki Ihara
发明人： Ying-Duo Gao , Lihu Yang , Douglas J. MacNeil , Nancy R. Morin , Takehiro Fukami , Takahiro Fukuroda , Akio Kanatani , Yasuyuki Ishii , Masaki Ihara
IPC分类号： C07D47120
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。

10. 发明授权

US6166038A Aminopyrazole derivatives 失效
标题翻译：氨基吡唑衍生物
公开(公告)号：US6166038A
公开(公告)日：2000-12-26
申请号：US319270
申请日：1999-07-30
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： C07D231/40 , C07D401/12 , A61K31/445 , A61K31/415 , C07D231/38
CPC分类号： C07D401/12 , C07D231/40
摘要： The present invention relates to a compound represented by the general formula [I]: ##STR1## wherein Ar.sup.1 represents an aryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl and lower haloalkyl groups; Ar.sup.2 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; R.sup.1 and R.sup.2 may be the same or different and each represents a hydrogen atom or a lower alkyl group; R.sup.3 and R.sup.4 may be the same or different and each represents a hydrogen atom or a lower alkyl group, or R.sup.3 and R.sup.4 are linked to each other to form an alkylene group containing 2 to 4 carbon atoms which may have a lower alkyl group; and R.sup.5 represents a hydrogen atom or a lower alkyl or lower alkoxy 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： PCT No.PCT / JP97 / 04571 Sec。 371日期1999年7月30日第 102（e）1999年7月30日PCT 1997年12月12日PCT PCT。公开号WO98 / 25908 日期：1998年6月18日本发明涉及由通式[I]表示的化合物：其中Ar1表示可具有选自卤素原子和低级烷基和低级卤代烷基的取代基的芳基; 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; R 1和R 2可以相同或不同，各自表示氢原子或低级烷基; R 3和R 4可以相同或不同，各自表示氢原子或低级烷基，或者R 3和R 4相互连接形成可以具有低级烷基的含有2〜4个碳原子的亚烷基; R5代表氢原子或低级烷基或低级烷氧基，或其盐，其制备方法以及用于治疗贪食症，肥胖症或糖尿病的药物，其包含其作为活性成分。

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