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公开(公告)号:US08778944B2
公开(公告)日:2014-07-15
申请号:US13543207
申请日:2012-07-06
申请人: Takahiko Taniguchi , Akira Kawada , John F. Quinn , Jun Kunitomo , Masato Yoshikawa , Makoto Fushimi
发明人: Takahiko Taniguchi , Akira Kawada , John F. Quinn , Jun Kunitomo , Masato Yoshikawa , Makoto Fushimi
IPC分类号: A61K31/50 , A61K31/501
CPC分类号: C07D403/04 , A61K9/2059 , C07D401/14 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14
摘要: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
摘要翻译: 本发明提供具有PDE抑制作用的化合物,其可用作预防或治疗精神分裂症等的药物。 式(I0)的化合物,其中R1表示取代基; R2表示氢原子或取代基; R3表示氢原子或取代基; 环A表示可被取代的芳环,环B表示可被取代的5元杂芳环或其盐。
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公开(公告)号:US20130331409A1
公开(公告)日:2013-12-12
申请号:US14002439
申请日:2012-03-15
申请人: Takahiko Taniguchi , Jun Kunitomo , Masato Yoshikawa , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Haruhi Kamisaki , Shinkichi Suzuki , Kasei Miura
发明人: Takahiko Taniguchi , Jun Kunitomo , Masato Yoshikawa , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Haruhi Kamisaki , Shinkichi Suzuki , Kasei Miura
IPC分类号: C07D471/14 , C07D471/04
CPC分类号: C07D471/14 , C07D471/04 , C07D519/00
摘要: The present invention provides a compound having a superior PDE10A inhibitory action and use thereof. The compound is a compound represented by the following formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
摘要翻译: 本发明提供具有优异的PDE10A抑制作用的化合物及其用途。 化合物是由下式(I)表示的化合物:其中各符号如本说明书中所定义,或其盐。
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公开(公告)号:US20130172292A1
公开(公告)日:2013-07-04
申请号:US13814073
申请日:2011-08-03
IPC分类号: C07D471/04 , C07D471/14 , C07D519/00
CPC分类号: C07D471/04 , C07D471/14 , C07D519/00
摘要: The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound represented by the formula (1′): wherein, Ring A′ represents an optionally substituted pyridine ring, an optionally substituted pyridazine ring, a pyrimidine ring, or 10 a pyrazine ring, R1′ represents (1) wherein, R1a′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2 represents a bond, —S—, -0-, —CO—, an optionally substituted methylene group, or —NRa′-(Ra′ represents a hydrogen atom, or an optionally substituted C1-6 alkyl group), and Ring B1′ represents an optionally further substituted 6- to 10-membered aromatic hydrocarbon ring, or an optionally further substituted 5- to 10-membered aromatic heterocyclic ring, or alternatively, L′ and R1a′ may be taken together to form an optionally substituted bicyclic or tricyclic fused heterocyclic group, or (2), wherein, R1b′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2′ represents an optionally substituted benzene ring, an optionally substituted pyridine ring, an optionally substituted pyrimidine ring, an optionally substituted pyrazine ring, or an optionally substituted pyridazine ring, Ring D′ represents an optionally further substituted 5- or 6-membered ring, R2′ represents a hydrogen atom, or a substituent, X′ represents ═N— or ═CRb′—(Rb′ represents a hydrogen atom, or a substituent), - - - - - represents that Rb′ and R2′ may form, taken together with the carbon atom and the nitrogen atom to which they are each adjacent, an optionally substituted 5- to 7-membered ring when.X′ is ═CRb′, or a salt thereof.
摘要翻译: 本发明提供了具有PDE 10A抑制作用的化合物,其可用作预防或治疗精神分裂症等的药物。 由式(1')表示的化合物:其中环A'表示任选取代的吡啶环,任选取代的哒嗪环,嘧啶环或吡嗪环,R1'表示(1)其中R1a'表示 任选取代的苯基或任选取代的5至10元杂环基,环B2表示键,-S - , - O-,-CO-,任选取代的亚甲基或-NR a' - (R a '表示氢原子或任选取代的C 1-6烷基),并且环B1'表示任选进一步取代的6至10元芳族烃环或任选进一步取代的5至10元芳族杂环 ,或者可选地,L'和R 1a'可以一起形成任选取代的双环或三环稠合杂环基,或(2),其中,R 1b'表示任选取代的苯基,或任选取代的5-至10- 环B2'表示 任选取代的苯环,任选取代的吡啶环,任选取代的嘧啶环,任选取代的吡嗪环或任选取代的哒嗪环,环D'表示任选进一步取代的5-或6-元环,R 2' 表示氢原子或取代基,X'表示= N-或= CRb' - (Rb'表示氢原子或取代基), - - - 表示Rb'和R2'可以一起形成 与它们各自相邻的碳原子和氮原子,当X'= CRb'或其盐时,任选取代的5-至7-元环。
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公开(公告)号:US20110319394A1
公开(公告)日:2011-12-29
申请号:US13166212
申请日:2011-06-22
申请人: Takahiko TANIGUCHI , Masato YOSHIKAWA , Kasei MIURA , Tomoaki HASUI , Eiji HONDA , Keisuke IMAMURA , Makoto KAMATA , Haruhi KAMISAKI , John F. QUINN , Joseph RAKER , Fatoumata CAMARA , Yi WANG
发明人: Takahiko TANIGUCHI , Masato YOSHIKAWA , Kasei MIURA , Tomoaki HASUI , Eiji HONDA , Keisuke IMAMURA , Makoto KAMATA , Haruhi KAMISAKI , John F. QUINN , Joseph RAKER , Fatoumata CAMARA , Yi WANG
IPC分类号: A61K31/437 , C07D498/04 , A61P25/18 , C07D487/14 , A61K31/522 , A61K31/551 , C07D471/04 , C07D473/00
CPC分类号: A61K31/4353 , A61K31/4355 , A61K31/437 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/551 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D471/04 , C07D471/14 , C07D473/00 , C07D473/28 , C07D487/04 , C07D495/04 , C07D498/04 , C07D498/08 , C07D519/00 , C07F7/10
摘要: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.
摘要翻译: 本发明提供具有PDE抑制作用的化合物,其可用作预防或治疗精神分裂症的药剂。 化合物由式(I)表示:其中符号在说明书中定义。
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公开(公告)号:US20100069351A1
公开(公告)日:2010-03-18
申请号:US12449320
申请日:2008-02-05
申请人: Takahiko Taniguchi , Kenichi Miyata , Osamu Kubo
发明人: Takahiko Taniguchi , Kenichi Miyata , Osamu Kubo
IPC分类号: A61K31/397 , C07D237/02 , A61K31/50 , C07D265/12 , A61K31/537 , C07D239/72 , A61K31/527 , C07D245/04 , A61P3/00 , A61P9/00
CPC分类号: C07D401/04 , C07D409/14 , C07D417/14 , C07D471/10 , C07D487/10 , C07D491/107 , C07D498/10
摘要: The present invention aims to provide a novel SCD inhibitor.The present invention relate to SCD inhibitor comprising A compound represented by the formula (I) wherein R is an optionally substituted cyclic group or an optionally substituted carbamoyl group, provided that R is not an optionally substituted 7-pyrido[2,3-d]pyrimidyl group; ring A is an optionally further substituted pyridazine ring; R1, R2, R3, R4, R11, R12, R13 and R14 are each independently a hydrogen atom or a substituent, or R1 and R11 in combination, R2 and R12 in combination, R3 and R13 in combination, or R4 and R14 in combination optionally form an oxo group, or R2 and R4 in combination optionally form a bond or an alkylene cross-linkage; m and n are each independently an integer of 0 to 2; ring B is an optionally substituted ring, provided that the two atoms constituting ring B, which are adjacent to the spiro carbon atom, are not oxygen atoms at the same time, or a salt thereof, or a prodrug thereof.
摘要翻译: 本发明旨在提供一种新型的SCD抑制剂。 本发明涉及包含由式(I)表示的化合物的SCD抑制剂,其中R是任选取代的环状基团或任选取代的氨基甲酰基,条件是R不是任选取代的7-吡啶并[2,3-d] 嘧啶基; 环A是任选进一步取代的哒嗪环; R 1,R 2,R 3,R 4,R 11,R 12,R 13和R 14各自独立地为氢原子或取代基,或R 1和R 11组合,R 2和R 12组合,R 3和R 13组合,或R 4和R 14组合 任选地形成氧代基团,或者R 2和R 4组合任选地形成键或亚烷基交联; m和n各自独立地为0〜2的整数。 环B是任选取代的环,条件是与螺环碳原子相邻的构成环B的两个原子不是同时为氧原子,或其盐或其前药。
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公开(公告)号:US20080217936A1
公开(公告)日:2008-09-11
申请号:US12038244
申请日:2008-02-27
IPC分类号: B60R19/30
CPC分类号: B60R19/18 , B60R2019/1873
摘要: A bumper absorber (2) includes an upper leg (2b) and a lower leg (2c), each of which extends in a longitudinal direction of an automobile, and a spanning portion (2d). The spanning portion (2d) connects the upper leg (2b) and the lower leg (2c), and faces an outer surface side of the bumper absorber (2) in a longitudinal direction of the automobile. Each of the upper leg (2b) and the lower leg (2c) includes a buckling inductive portion (2f that serves as a starting point of the buckling that is caused when the spanning portion (2d) receives an impact load. The buckling inductive portion (2f) is formed as an angular transition portion in which the angle of inclination between inner side surfaces changes. The inner side surfaces mutually face between the upper leg (2b) and the lower leg (2c) that include the buckling inductive portion (2f).
摘要翻译: 保险杠吸收器(2)包括上部腿部(2b)和一个小腿部(2c),每个腿部沿着汽车的纵向方向延伸,并且跨越部分(2d)。 跨越部分(2d)连接上腿部(2b)和下腿部(2c),并且在汽车的纵向方向上面对保险杠吸收器(2)的外表面侧。 上腿部(2b)和下腿部(2c)中的每一个都包括一个屈曲感应部分(2f),用于当跨越部分(2d)接收冲击载荷时引起的屈曲起始点。 弯曲感应部(2f)形成为内侧面的倾斜角度变化的角度过渡部,内侧面相互面对上腿(2b)与小腿(2c)之间, 包括屈曲感应部分(2f)。
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公开(公告)号:US20070284896A1
公开(公告)日:2007-12-13
申请号:US11811008
申请日:2007-06-07
IPC分类号: B60R19/03
CPC分类号: B60R19/18 , B60R2019/184 , B60R2019/188
摘要: The present invention discloses a bumper absorber that is provided on an automobile between a bumper reinforcement and a bumper fascia, comprising a first energy absorbing portion formed by foaming a resin molded material; the first energy absorbing portion extending from the bumper reinforcement toward the bumper fascia; a second energy absorbing portion formed by a resin molded material; the second energy absorbing portion extending from the bumper reinforcement toward the bumper fascia at a position where a space that permits buckling is formed between the first energy absorbing portion and the second energy absorbing portion on the bumper reinforcement side; a crosslinking portion disposed facing a vehicle interior side of the bumper fascia; and the crosslinking portion fastening the first energy absorbing portion and the second energy absorbing portion together while sealing an opening between the first energy absorbing portion and the second energy absorbing portion on the bumper fascia side.
摘要翻译: 本发明公开了一种保险杠吸收器,其设置在保险杠加强件和保险杠面板之间的汽车上,包括通过使树脂模制材料发泡而形成的第一能量吸收部分; 所述第一能量吸收部分从所述保险杠加强件延伸到保险杠面板; 由树脂模制材料形成的第二能量吸收部分; 所述第二能量吸收部从所述保险杠加强件朝向保险杠面板延伸,在所述保险杠加强侧的所述第一能量吸收部和所述第二能量吸收部之间形成有允许弯曲的空间的位置; 布置成面向保险杠面板的车辆内侧的交联部分; 并且所述交联部分将所述第一能量吸收部分和所述第二能量吸收部分紧固在一起,同时密封所述保险杠面板侧上的所述第一能量吸收部分和所述第二能量吸收部分之间的开口。
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公开(公告)号:US09090586B2
公开(公告)日:2015-07-28
申请号:US13813786
申请日:2011-08-03
申请人: Masato Yoshikawa , Shinkichi Suzuki , Tomoaki Hasui , Makoto Fushimi , Jun Kunitomo , Haruhi Kamisaki , Takahiko Taniguchi
发明人: Masato Yoshikawa , Shinkichi Suzuki , Tomoaki Hasui , Makoto Fushimi , Jun Kunitomo , Haruhi Kamisaki , Takahiko Taniguchi
IPC分类号: A61K31/553 , A61K31/525 , A61K31/535 , C07D401/00 , C07D498/02 , C07D413/00 , C07D241/00 , C07D413/14 , C07D498/08 , C07D417/14 , C07D403/14 , A61K9/20 , C07D403/04 , A61K9/00 , C07D401/14
CPC分类号: C07D403/04 , A61K9/00 , A61K9/2018 , A61K9/2059 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14 , C07D498/08
摘要: The present invention provides a compound represented by the formula (1): wherein each symbol is as defined in the specification, or a salt thereof, a prodrug of the compound or a salt thereof, a medicament containing the compound or a salt thereof, the medicament which is a phosphodiesterase 10A inhibitor, and a medicament which is for preventing or treating schizophrenia.
摘要翻译: 本发明提供由式(1)表示的化合物:其中各符号如说明书中所定义,或其盐,化合物或其盐的前药,含有该化合物或其盐的药物, 作为磷酸二酯酶10A抑制剂的药物,以及用于预防或治疗精神分裂症的药物。
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公开(公告)号:US09029536B2
公开(公告)日:2015-05-12
申请号:US13814073
申请日:2011-08-03
IPC分类号: C07D471/04 , C07D471/14 , C07D519/00
CPC分类号: C07D471/04 , C07D471/14 , C07D519/00
摘要: The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound represented by the formula (1′): wherein, Ring A′ represents an optionally substituted pyridine ring, an optionally substituted pyridazine ring, a pyrimidine ring, or 10 a pyrazine ring, R1′ represents (1) wherein, R1a′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2 represents a bond, —S—, -0-, —CO—, an optionally substituted methylene group, or —NRa′— (Ra′ represents a hydrogen atom, or an optionally substituted C1-6 alkyl group), and Ring B1′ represents an optionally further substituted 6- to 10-membered aromatic hydrocarbon ring, or an optionally further substituted 5- to 10-membered aromatic heterocyclic ring, or alternatively, L′ and R1a′ may be taken together to form an optionally substituted bicyclic or tricyclic fused heterocyclic group, or (2), wherein, R1b′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2′ represents an optionally substituted benzene ring, an optionally substituted pyridine ring, an optionally substituted pyrimidine ring, an optionally substituted pyrazine ring, or an optionally substituted pyridazine ring, Ring D′ represents an optionally further substituted 5- or 6-membered ring, R2′ represents a hydrogen atom, or a substituent, X′ represents ═N— or ═CRb′—(Rb′ represents a hydrogen atom, or a substituent), - - - - - represents that Rb′ and R2′ may form, taken together with the carbon atom and the nitrogen atom to which they are each adjacent, an optionally substituted 5- to 7-membered ring when.X′ is ═CRb′, or a salt thereof.
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公开(公告)号:US08563575B2
公开(公告)日:2013-10-22
申请号:US13166212
申请日:2011-06-22
申请人: Takahiko Taniguchi , Masato Yoshikawa , Kasei Miura , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Makoto Kamata , Haruhi Kamisaki
发明人: Takahiko Taniguchi , Masato Yoshikawa , Kasei Miura , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Makoto Kamata , Haruhi Kamisaki
CPC分类号: A61K31/4353 , A61K31/4355 , A61K31/437 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/551 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D471/04 , C07D471/14 , C07D473/00 , C07D473/28 , C07D487/04 , C07D495/04 , C07D498/04 , C07D498/08 , C07D519/00 , C07F7/10
摘要: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.
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