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1. 发明授权

US06638942B1 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：US06638942B1
公开(公告)日：2003-10-28
申请号：US10228250
申请日：2002-08-26
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： C07D47110
CPC分类号： C07D221/20 , C07D471/10
摘要： Compounds of general structural formula I are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.
摘要翻译：通用结构式的化合物Iare选择性NPY Y5受体拮抗剂，可用于治疗肥胖及其相关并发症。

2. 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 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。

8. 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。

9. 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。

10. 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。

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