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公开(公告)号:US07229986B2
公开(公告)日:2007-06-12
申请号:US10276288
申请日:2001-05-15
申请人: Yuji Ishihara , Jun Terauchi , Nobuhiro Suzuki , Shiro Takekawa , Kazuyoshi Aso
发明人: Yuji Ishihara , Jun Terauchi , Nobuhiro Suzuki , Shiro Takekawa , Kazuyoshi Aso
IPC分类号: C07D209/08 , C07D209/14 , C07D401/12 , A61K31/404 , A61P3/04
CPC分类号: C07D223/16 , A61K31/404 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/538 , A61K31/541 , A61K31/55 , A61K31/551 , C07D209/08 , C07D215/12 , C07D215/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D265/36 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/12 , C07D417/06
摘要: A melanin-concentrating hormone antagonist comprising a compound of the formula: wherein R is hydrogen atom or a cyclic group which may be substituted; X is a bond or a spacer having a main chain of 1 to 10 atoms; Y is a spacer having a main chain of 1 to 6 atoms; ring A is benzene ring which may be further substituted; ring B is a 5- to 9-membered nitrogen-containing non-aromatic heterocyclic ring which may be further substituted; R1 and R2 are the same or different and are hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; or R1 and R2, together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic ring which may be substituted; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing heterocyclic ring which may be substituted; or a salt thereof is useful as a preventive or therapeutic agent for obesity, etc.
摘要翻译: 一种黑色素浓缩激素拮抗剂,其包含下式化合物:其中R为氢原子或可被取代的环状基团; X是具有1至10个原子的主链的键或间隔基; Y是具有1至6个原子的主链的间隔物; 环A是可以被进一步取代的苯环; 环B是可以进一步取代的5至9元含氮非芳族杂环; R 1和R 2相同或不同,为氢原子,可被取代的烃基或可被取代的杂环基; 或R 1和R 2以及相邻的氮原子可以形成可以被取代的含氮杂环; 或R 2与相邻的氮原子和Y一起形成可以被取代的含氮杂环; 或其盐可用作肥胖症等的预防或治疗剂。
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公开(公告)号:US07115750B1
公开(公告)日:2006-10-03
申请号:US10088771
申请日:2000-09-19
申请人: Kaneyoshi Kato , Jun Terauchi , Masaaki Mori , Nobuhiro Suzuki , Yukio Shimomura , Shiro Takekawa , Yuji Ishihara
发明人: Kaneyoshi Kato , Jun Terauchi , Masaaki Mori , Nobuhiro Suzuki , Yukio Shimomura , Shiro Takekawa , Yuji Ishihara
IPC分类号: C09B5/00 , A61K3/41 , C07D209/56 , C07D487/00 , C07D491/00
CPC分类号: C07D207/277 , C07C217/74 , C07C219/28 , C07C233/29 , C07C233/44 , C07C233/80 , C07C235/42 , C07C235/50 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C271/28 , C07C275/42 , C07C311/21 , C07C2602/10 , C07C2602/12 , C07D209/18 , C07D209/22 , C07D209/42 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/32 , C07D211/52 , C07D211/62 , C07D211/70 , C07D213/56 , C07D213/81 , C07D213/82 , C07D215/14 , C07D215/38 , C07D233/24 , C07D239/28 , C07D239/30 , C07D261/18 , C07D263/14 , C07D263/34 , C07D265/28 , C07D271/06 , C07D295/096 , C07D295/13 , C07D295/185 , C07D307/68 , C07D307/81 , C07D311/58 , C07D317/60 , C07D319/20 , C07D333/24 , C07D333/28 , C07D333/38 , C07D335/16 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/12 , C07D493/04
摘要: A melanin-concentrating hormone antagonist which comprises a compound of the formula: wherein Ar1 is a cyclic group which may have substituents; X is a spacer having a main chain of 1 to 6 atoms; Y is a bond or a spacer having a main chain of 1 to 6 atoms; Ar is a monocyclic aromatic ring which may be condensed with a 4 to 8 membered non-aromatic ring, and may have further substituents; R1 and R2 are independently hydrogen atom or a hydrocarbon group which may have substituents; R1 and R2, together with the adjacent nitrogen atom, may form a nitrogen-containing hetero ring which may have substituents; R2 may form a spiro ring together with Ar; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing hetero ring which may have substituents; or a salt thereof; which is useful as an agent for preventing or treating obesity, etc.
摘要翻译: 一种黑色素浓缩激素拮抗剂,其包含下式化合物:其中Ar 1是可以具有取代基的环状基团; X是具有1至6个原子的主链的间隔物; Y是具有1至6个原子的主链的键或间隔基; Ar是可以与4至8元非芳族环稠合的单环芳环,并且可以具有其它取代基; R 1和R 2独立地是氢原子或可以具有取代基的烃基; R 1和R 2与相邻的氮原子一起可以形成可以具有取代基的含氮杂环; R 2可以与Ar一起形成螺环; 或R 2连同相邻的氮原子和Y可以形成可具有取代基的含氮杂环; 或其盐; 其可用作预防或治疗肥胖症等的药剂。
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公开(公告)号:US20070173498A1
公开(公告)日:2007-07-26
申请号:US11224744
申请日:2005-09-12
申请人: Kaneyoshi Kato , Jun Terauchi , Masaaki Mori , Nobuhiro Suzuki , Yukio Shimomura , Shiro Takekawa , Yuji Ishihara
发明人: Kaneyoshi Kato , Jun Terauchi , Masaaki Mori , Nobuhiro Suzuki , Yukio Shimomura , Shiro Takekawa , Yuji Ishihara
IPC分类号: A61K31/538 , A61K31/4706 , A61K31/40 , A61K31/165 , A61K31/353
CPC分类号: C07D207/277 , C07C217/74 , C07C219/28 , C07C233/29 , C07C233/44 , C07C233/80 , C07C235/42 , C07C235/50 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C271/28 , C07C275/42 , C07C311/21 , C07C2602/10 , C07C2602/12 , C07D209/18 , C07D209/22 , C07D209/42 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/32 , C07D211/52 , C07D211/62 , C07D211/70 , C07D213/56 , C07D213/81 , C07D213/82 , C07D215/14 , C07D215/38 , C07D233/24 , C07D239/28 , C07D239/30 , C07D261/18 , C07D263/14 , C07D263/34 , C07D265/28 , C07D271/06 , C07D295/096 , C07D295/13 , C07D295/185 , C07D307/68 , C07D307/81 , C07D311/58 , C07D317/60 , C07D319/20 , C07D333/24 , C07D333/28 , C07D333/38 , C07D335/16 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/12 , C07D493/04
摘要: A melanin-concentrating hormone antagonist which comprises a compound of the formula: wherein Ar1 is a cyclic group which may have substituents; X is a spacer having a main chain of 1 to 6 atoms; Y is a bond or a spacer having a main chain of 1 to 6 atoms; Ar is a monocyclic aromatic ring which may be condensed with a 4 to 8 membered non-aromatic ring, and may have further substituents; R1 and R2 are independently hydrogen atom or a hydrocarbon group which may have substituents; R1 and R2, together with the adjacent nitrogen atom, may form a nitrogen-containing hetero ring which may have substituents; R2 may form a spiro ring together with Ar; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing hetero ring which may have substituents; or a salt thereof; which is useful as an agent for preventing or treating obesity, etc.
摘要翻译: 一种黑色素浓缩激素拮抗剂,其包含下式化合物:其中Ar 1是可以具有取代基的环状基团; X是具有1至6个原子的主链的间隔物; Y是具有1至6个原子的主链的键或间隔基; Ar是可以与4至8元非芳族环稠合的单环芳环,并且可以具有其它取代基; R 1和R 2独立地是氢原子或可以具有取代基的烃基; R 1和R 2与相邻的氮原子一起可以形成可以具有取代基的含氮杂环; R 2可以与Ar一起形成螺环; 或R 2连同相邻的氮原子和Y可以形成可具有取代基的含氮杂环; 或其盐; 其可用作预防或治疗肥胖症等的药剂。
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公开(公告)号:US06930185B2
公开(公告)日:2005-08-16
申请号:US10258492
申请日:2001-04-26
申请人: Yuji Ishihara , Nobuhiro Suzuki , Shiro Takekawa
发明人: Yuji Ishihara , Nobuhiro Suzuki , Shiro Takekawa
IPC分类号: C07C233/80 , C07C235/66 , C07C237/48 , C07C271/30 , C07D207/06 , C07D209/12 , C07D215/38 , C07D295/096 , C07D295/135 , C07D401/06 , C07D401/12 , C07D401/14 , C07D417/06 , C07D471/04 , A61K31/47 , C07D215/16
CPC分类号: C07D295/096 , C07C233/80 , C07C235/66 , C07C237/48 , C07C271/30 , C07D207/06 , C07D209/12 , C07D215/38 , C07D295/135 , C07D401/06 , C07D401/12 , C07D401/14 , C07D417/06 , C07D471/04
摘要: A melanin-concentrating hormone antagonist comprising a compound of the formula (I): wherein Ar1 is a cyclic group which may be substituted; X and Y are the same or different and are a spacer having a main chain of 1 to 6 atoms; Ar is a condensed polycyclic aromatic ring which may be substituted; R1 and R2 are the same or different and are hydrogen atom or a hydrocarbon group which may be substituted; or R1 and R2, together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic ring which may be substituted; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing heterocyclic ring which may be substituted; or R2, together with the adjacent nitrogen atom, Y and Ar, may form a condensed ring; or a salt thereof is useful as an agent for preventing or treating obesity, etc.
摘要翻译: 包含式(I)化合物的黑色素浓缩激素拮抗剂:其中Ar 1是可被取代的环状基团; X和Y相同或不同,是具有1至6个原子的主链的间隔基; Ar是可以被取代的稠合多环芳香环; R 1和R 2相同或不同,为氢原子或可被取代的烃基; 或R 1和R 2以及相邻的氮原子可以形成可以被取代的含氮杂环; 或R 2与相邻的氮原子和Y一起形成可以被取代的含氮杂环; 或R 2与相邻的氮原子Y和Ar一起形成稠环; 或其盐可用作预防或治疗肥胖症等的药剂。
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公开(公告)号:US20050209213A1
公开(公告)日:2005-09-22
申请号:US10493427
申请日:2002-10-24
申请人: Yuji Ishihara , Makoto Kamata , Shiro Takekawa , Nobuhiro Suzuki , Koki Kato
发明人: Yuji Ishihara , Makoto Kamata , Shiro Takekawa , Nobuhiro Suzuki , Koki Kato
IPC分类号: A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/55 , A61P3/04 , A61P5/04 , A61P25/22 , A61P25/24 , A61P43/00 , C07D215/38 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D413/02 , C07D41/02
CPC分类号: C07D401/06 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D215/38 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04
摘要: A compound, which has a melanin-concentrating hormone antagonistic action and useful as an agent for preventing or treating obesity, and which is represented by the formula: wherein Ar is a cyclic group optionally having substituent(s); X is a bond or a spacer having a main chain of 1 to 6 atoms; R1 and R2 are the same or different and each is a hydrogen atom or a hydrocarbon group optionally having substituent(s), or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocycle optionally having substituent(s); Y is a divalent hydrocarbon group optionally having substituent(s) (except CO); R3 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); and ring A and ring B may further have substituents, and when ring B further has a substituent, the substituent may be linked to R1 to form a ring, or a salt thereof, or a prodrug thereof, is provided.
摘要翻译: 一种化合物,其具有黑色素浓集激素拮抗作用并且可用作预防或治疗肥胖症的药剂,并且其由下式表示:其中Ar是任选具有取代基的环状基团; X是具有1至6个原子的主链的键或间隔基; R 1和R 2相同或不同,各自为氢原子或任选具有取代基的烃基,或R 1〜 >和R 2可以与相邻的氮原子一起形成任选具有取代基的含氮杂环; Y是任选具有取代基(CO除外)的二价烃基; R 3是氢原子或任选具有取代基的烃基; 并且环A和环B可以进一步具有取代基,并且当环B还具有取代基时,取代基可以与R 1连接形成环,或其盐或其前药, 被提供。
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公开(公告)号:US07183415B2
公开(公告)日:2007-02-27
申请号:US10493427
申请日:2002-10-24
申请人: Yuji Ishihara , Makoto Kamata , Shiro Takekawa , Nobuhiro Suzuki , Koki Kato
发明人: Yuji Ishihara , Makoto Kamata , Shiro Takekawa , Nobuhiro Suzuki , Koki Kato
IPC分类号: C07D215/38 , C07D215/14
CPC分类号: C07D401/06 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D215/38 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04
摘要: A compound, which has a melanin-concentrating hormone antagonistic action and useful as an agent for preventing or treating obesity, and which is represented by the formula: wherein Ar is a cyclic group optionally having substituent(s); X is a bond or a spacer having a main chain of 1 to 6 atoms; R1 and R2 are the same or different and each is a hydrogen atom or a hydrocarbon group optionally having substituent(s), or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocycle optionally having substituent(s); Y is a divalent hydrocarbon group optionally having substituent(s) (except CO); R3 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); and ring A and ring B may further have substituents, and when ring B further has a substituent, the substituent may be linked to R1 to form a ring, or a salt thereof, or a prodrug thereof, is provided.
摘要翻译: 一种化合物,其具有黑色素浓集激素拮抗作用并且可用作预防或治疗肥胖症的药剂,并且其由下式表示:其中Ar是任选具有取代基的环状基团; X是具有1至6个原子的主链的键或间隔基; R 1和R 2相同或不同,各自为氢原子或任选具有取代基的烃基,或R 1〜 >和R 2可以与相邻的氮原子一起形成任选具有取代基的含氮杂环; Y是任选具有取代基(CO除外)的二价烃基; R 3是氢原子或任选具有取代基的烃基; 并且环A和环B可以进一步具有取代基,并且当环B还具有取代基时,取代基可以与R 1连接形成环,或其盐或其前药, 被提供。
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公开(公告)号:US20060128690A1
公开(公告)日:2006-06-15
申请号:US10545120
申请日:2004-02-12
申请人: Yuji Ishihara , Makoto Kamata , Shiro Takekawa
发明人: Yuji Ishihara , Makoto Kamata , Shiro Takekawa
IPC分类号: A61K31/55 , A61K31/401 , A61K31/445
CPC分类号: C07D211/16 , A61K31/55 , C07C233/73 , C07C235/42 , C07D207/09 , C07D207/12 , C07D211/14 , C07D213/82 , C07D233/24 , C07D295/135
摘要: The present invention provides a compound represented by the formula wherein Ar1 is a cyclic group optionally having substituent(s); R is a hydrogen atom, an optionally halogenated C1-6 alkyl, a phenyl optionally having substituent(s) or a pyridyl optionally having substituent(s); Ra1, Ra2, Ra3 and Ra4 are the same or different and each is a hydrogen atom, an optionally halogenated C1-6 alkyl or the like; Ar is a monocyclic aromatic ring optionally having substituent(s); Y is an optionally halogenated alkylene group; and R1 and R2 are (1) the same or different and each is a hydrogen atom or a C1-6 alkyl, (2) R1 and R2 form a nitrogen-containing heterocycle optionally having substituent(s) together with the adjacent nitrogen atom, or (3) R1 and Y form a nitrogen-containing heterocycle optionally having substituent(s) together with the adjacent nitrogen atom, and R2 is a hydrogen atom or a C1-6 alkyl; provided that when the nitrogen-containing heterocycle formed by R1 and R2 together with the adjacent nitrogen atom is a piperazine, or when R is a C1-4 alkyl, Ar1 is a cyclic group having substituent(s), or a salt thereof, having a melanin-concentrating hormone antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like.
摘要翻译: 本发明提供由下式表示的化合物:其中Ar 1是任选具有取代基的环状基团; R是氢原子,任选卤代的C 1-6烷基,任选具有取代基的苯基或任选具有取代基的吡啶基; Ra 1,R 2,R 3,R 3和R 4相同或不同,各自为氢原子 ,任选卤代的C 1-6烷基等; Ar是任选具有取代基的单环芳环; Y是任选卤代的亚烷基; 且R 1和R 2均为(1)相同或不同,并且各自为氢原子或C 1-6烷基,( 2)R 1和R 2 2形成任选具有取代基的氮杂环与相邻的氮原子,或(3)R 1, Y和Y形成任选具有取代基的氮杂环与相邻的氮原子一起形成,R 2是氢原子或C 1-6 烷基; 条件是当由R 1和R 2与相邻氮原子一起形成的含氮杂环是哌嗪时,或当R是C 1〜 4个烷基,Ar 1是具有取代基的环状基团或其盐,其具有黑色素浓缩激素拮抗作用并且可用作预防或治疗的药剂 肥胖等。
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公开(公告)号:US07601868B2
公开(公告)日:2009-10-13
申请号:US10545120
申请日:2004-02-12
申请人: Yuji Ishihara , Makoto Kamata , Shiro Takekawa
发明人: Yuji Ishihara , Makoto Kamata , Shiro Takekawa
IPC分类号: C07C233/65 , C07D207/06 , A61K31/165 , A61K31/40
CPC分类号: C07D211/16 , A61K31/55 , C07C233/73 , C07C235/42 , C07D207/09 , C07D207/12 , C07D211/14 , C07D213/82 , C07D233/24 , C07D295/135
摘要: The present invention provides a compound represented by the formula or salts thereof, wherein, Ar1, Ar, R, R1, R2, Ra1, Ra2, Ra3, Ra4 and Y have meanings described in the specification, having a melanin-concentrating hormone antagonistic, action and useful as an agent for the prophylaxis or treatment of obesity and the like.
摘要翻译: 本发明提供由下式表示的化合物或其盐,其中Ar1,Ar,R,R1,R2,Ra1,Ra2,Ra3,Ra4和Y具有说明书中描述的具有黑色素浓缩激素拮抗作用的含义, 作用并用作预防或治疗肥胖症等的药剂。
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公开(公告)号:US08668243B2
公开(公告)日:2014-03-11
申请号:US13382467
申请日:2010-07-13
申请人: Satoshi Komiya , Kazuhito Sugimoto , Hirofumi Kondou , Yuichi Morinaka , Tomohiro Koyahata , Masato Inoue , Kenichiro Koizumi , Hitoshi Takagi , Yuji Ishihara , Kazuaki Nakajima
发明人: Satoshi Komiya , Kazuhito Sugimoto , Hirofumi Kondou , Yuichi Morinaka , Tomohiro Koyahata , Masato Inoue , Kenichiro Koizumi , Hitoshi Takagi , Yuji Ishihara , Kazuaki Nakajima
IPC分类号: B62D35/00
CPC分类号: B62D35/00 , B60Q1/0017
摘要: A vehicle boundary layer air flow control structure is provided with a vehicle body and a side view mirror. The vehicle body includes an exterior contoured surface with an air flow deflector. The side view mirror is attached to the vehicle body to provide a diagonally rearward direction to be viewed from a driver's seat. The air flow deflector has a downward air flow guiding surface provided in a vehicle body region of the exterior contoured surface of the vehicle body along which an air flow heading toward the side view mirror passes. The downward air flow guiding surface extends in an air flow direction of the air flow with respect to the side view mirror to divert the air flow underneath the side view mirror.
摘要翻译: 车辆边界层气流控制结构设置有车体和侧视镜。 车身包括具有空气导流板的外部轮廓表面。 侧视镜附接到车体以提供从驾驶员座椅观察的斜向后方向。 空气导流器具有设置在车身外部轮廓表面的车身区域中的朝向侧视镜通过的空气流的向下空气流引导表面。 向下的空气流引导表面相对于侧视镜在空气流的空气流动方向上延伸以转移侧视镜下面的空气流。
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公开(公告)号:US20130026783A1
公开(公告)日:2013-01-31
申请号:US13639211
申请日:2011-04-07
IPC分类号: B62D35/02
摘要: A front underfloor structure of a vehicle includes front deflectors disposed forward of front tires, respectively. The front deflectors each include a front apex portion disposed at a position closer to the vehicle front than a leading edge surface of each of the front tires when straight, and disposed at a position closer to a vehicle center line than an inner surface of each of the front tires when straight; an outer end portion disposed at a position closer to the vehicle rear than the front apex portion, and disposed at a position outward in the vehicle width direction of the front apex portion; and a second flow redirection surface connecting the front apex portion and the outer end portion, and being configured such that, when struck by air traveling from the vehicle front, the second flow redirection surface redirects a flow of the traveling air outward in the vehicle.
摘要翻译: 车辆的前地板结构包括分别设置在前轮胎前方的前偏转器。 前导向器各自包括设置在比前轮胎的前边缘更靠近车辆前方的位置处的前顶部部分,其在直线时位于比每个前轮胎的内表面更靠近车辆中心线的位置 前轮胎直线时; 设置在比前顶点更靠近车辆后方的位置,并且设置在前顶点部的车宽方向外侧的位置; 以及连接前顶点部和外端部的第二流向重定向面,并且被构造成当从车辆前方行进的空气撞击时,第二流向重定向面将行进空气的流动重新引导到车辆外部。
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