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31. 发明授权

US6011039A Aminopyridine derivatives 失效
标题翻译：氨基吡啶衍生物
公开(公告)号：US6011039A
公开(公告)日：2000-01-04
申请号：US142162
申请日：1998-10-13
申请人： Takehiro Fukami , Toshiaki Mase , Yoshimi Tsuchiya , Akio Kanatani , Takahiro Fukuroda
发明人： Takehiro Fukami , Toshiaki Mase , Yoshimi Tsuchiya , Akio Kanatani , Takahiro Fukuroda
IPC分类号： C07D213/74 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14 , A61K31/44
CPC分类号： C07D417/06 , C07D213/74 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12 , C07D417/14
摘要： A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for hyperphagia, obesity or diabetes, which comprises such a compound or salt as an active ingredient: ##STR1## wherein Ar.sup.1, Ar.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and W are as defined.
摘要翻译： PCT No.PCT / JP97 / 00890 Sec。 371日期：1998年10月13日 102（e）日期1998年10月13日PCT 1997年3月19日PCT公布。公开号WO97 / 34873 日期1997年9月25日由式（I）表示的化合物或其药学上可接受的盐，以及包含这样的作为活性成分的化合物或盐的食欲过盛，肥胖或糖尿病的药物组合物，其中Ar1，Ar2，R1 ，R2，R3，R4和W如上所定义。

32. 发明授权

US5114918A Endothelin antagonistic cyclic pentapeptides 失效
标题翻译：内皮素拮抗剂环糊精
公开(公告)号：US5114918A
公开(公告)日：1992-05-19
申请号：US630505
申请日：1990-12-20
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaru Nishikibe , Masaki Ihara , Mitsuo Yano
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaru Nishikibe , Masaki Ihara , Mitsuo Yano
IPC分类号： A61K38/00 , C07K7/64 , C07K14/575
CPC分类号： C07K14/57536 , A61K38/00 , Y10S514/826 , Y10S514/921 , Y10S514/922 , Y10S514/929 , Y10S530/80 , Y10S930/27
摘要： Cyclic pentapeptides of the formula:cyclo (-X.sup.1 -X.sup.2 -X.sup.3 -X.sup.4 -X.sup.5 -) (I)wherein X.sup.n (n=1-5) represents amino acid residues. These compounds are useful as hypotensive drugs.

33. 发明授权

US4988681A Phosphinic acid derivatives 失效
标题翻译：次膦酸衍生物
公开(公告)号：US4988681A
公开(公告)日：1991-01-29
申请号：US370190
申请日：1989-06-22
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Hiroshi Naganuma , Kyoko Nakamichi
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Hiroshi Naganuma , Kyoko Nakamichi
IPC分类号： C07F9/30 , C07F9/32 , C07F9/58 , C07F9/6506 , C07F9/6518
CPC分类号： C07F9/65182 , C07F9/302 , C07F9/303 , C07F9/3217 , C07F9/3223 , C07F9/582 , C07F9/65062
摘要： A phosphinic acid derivative represented by the general formula [I], or a pharmaceutically acceptable salt thereof, ##STR1## wherein R.sup.1 represents an alkyl, cycloalkyl or aralkyl group which may be substituted; R.sup.2 and R.sup.5 may be identical or different, and each represents a hydrogen atom, or an ester residue capable of forming a non-toxic ester hydrolyzable in vivo; and A represents a group of the formula ##STR2## wherein R.sup.3 represents an alkyl group, a group of the formula ##STR3## wherein R.sup.30 represents a halogen atom, a carboxyl group, a hydroxyl group, a cycloalkyl group which may be substituted, an aryl group which may be substituted, an arylthio group, a heteroarylthio group which may be substituted, an alkylthio group which may be substituted, an amino group which may be substituted, or a lower alkoxycarbonyl group; R.sup.31 represents a hydrogen atom or a lower alkyl group; and n represents an integer of 0 to 6, a cycloalkyl group which may be substituted or an aryl group which may be substituted; and the double bond at A has a Z-configuration, or a group of the formula ##STR4## wherein R.sup.4 represents a cycloalkyl group which may be substituted. Said phosphinic acid derivative is useful for reducing renal toxicity induced by a carbapenem or penem antibiotic and for inhibiting dipeptidase.

34. 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

35. 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。

36. 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。

37. 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。

38. 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。

39. 发明授权

US06057335A Pyrazole derivatives 失效
标题翻译：吡唑衍生物
公开(公告)号：US06057335A
公开(公告)日：2000-05-02
申请号：US319260
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 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D487/04 , A61K31/473 , A61K31/4155 , A61K31/4439 , C07D401/14
CPC分类号： C07D401/04 , C07D231/40 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D487/04
摘要： The present invention relates to a compound represented by the general formula [I]: ##STR1## wherein A and B rings are ortho-condensed to each other, A ring represents an aromatic carbocyclic or heterocyclic ring and B ring represents an aliphatic four- to seven-membered carbocyclic or nitrogen-containing heterocyclic ring, said nitrogen atom being possible to present at only the position where the A ring is condensed; Ar represents an aromatic carbocyclic or heterocyclic ring 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 aromatic carbocyclic ring groups; and R represents a substituent selected from the group consisting of a halogen atom and nitro, lower alkyl, lower alkoxy, aromatic carbocyclic ring groups and a carbonyl group having an aromatic carbocyclic ring group, or a hydrogen atom, provided that when the group represented by ##STR2## is the group represented by ##STR3## Ar is not a phenyl group nor a 4-chlorophenyl 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A和B环彼此原子稠合，A环表示芳族碳环或杂环，B环表示脂族四至七元碳环或含氮杂环，所述氮原子只能存在于A环稠合的位置; Ar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族碳环基团的取代基的芳族碳环或杂环基团; R表示选自卤素原子和硝基，低级烷基，低级烷氧基，芳香族碳环基团和具有芳香族碳环基团的羰基或氢原子的取代基，条件是当以是由Ar表示的基团不是苯基或4-氯苯基，或其盐，其制备方法以及用于治疗包含其作为活性成分的贪食症，肥胖症或糖尿病的药剂。

40. 发明授权

US6043246A Urea derivatives 失效
标题翻译：尿素衍生物
公开(公告)号：US6043246A
公开(公告)日：2000-03-28
申请号：US308668
申请日：1999-07-26
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 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , A61K31/415 , A61K31/496
CPC分类号： C07D401/04 , C07D231/40 , C07D401/12 , C07D403/12 , C07D405/04
摘要： The present invention relates to a compound represented by the general formula [I]: ##STR1## wherein A represents a nitrogen atom or a group represented by C--R.sup.5 ; 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 represents a hydrogen atom, a lower alkyl group or a bond formed by linking to R.sup.5 ; R.sup.2 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 hydroxyl, lower alkyl or lower alkoxy group or a bond formed by linking to R.sup.1,or its salt, a process for its preparation and an agent for the treatment of bulimia, obesity or diabetes comprising it as an active ingredient.
摘要翻译： PCT No.PCT / JP97 / 04399 Sec。 371日期：1999年7月26日 102（e）日期1999年7月26日PCT 1997年12月2日PCT公布。 WO98 / 24768 PCT公开号日期：1998年6月11日本发明涉及由通式[I]表示的化合物：其中A表示氮原子或C-R5表示的基团; Ar 1表示可以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; R1表示氢原子，低级烷基或通过连接到R5形成的键; R2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表示氢原子或羟基，低级烷基或低级烷氧基或通过连接R1或其盐形成的键，其制备方法和用于治疗贪食，肥胖或糖尿病的药物，其包含其作为有效成分。

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