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公开(公告)号:US07875633B2
公开(公告)日:2011-01-25
申请号:US11990889
申请日:2006-08-23
申请人: Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
发明人: Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
IPC分类号: A61K31/444 , A61K31/4439 , A61K31/5377 , A61K31/4545 , A61P9/00 , A61P25/00 , A61P3/00 , C07D213/64 , C07D401/02 , C07D413/02 , C07D401/14
CPC分类号: C07D213/69 , C07D213/64 , C07D401/10 , C07D413/10
摘要: A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents —CH2—O—, —CH═CH— or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
摘要翻译: 作为活性成分,含有式(I)所示的化合物:其中,R 1和R 2分别独立地表示氢原子,低级烷基等,或者与连接有L,Z 2和R 1的氮原子一起形成 可以形成脂族氮杂环基,并且R 1和R 2与它们所连接的氮原子一起形成脂族氮杂环基; X表示次甲基或氮原子; Y表示-CH 2 -O-,-CH = CH-等; Z1表示单键,C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基,C3-8亚环烷基等; Ar表示芳族碳环基等。 该化合物可用作中枢神经系统疾病,心血管疾病或代谢疾病的药物。
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公开(公告)号:US07700611B2
公开(公告)日:2010-04-20
申请号:US11988780
申请日:2006-07-24
申请人: Russell R. Ferlita , Yuji Haga , Makoto Ishikawa , Keisuke Kamei , Shinji Kato , Hisaki Kojima , Aaron Moment , Nobuaki Nonoyama , Nobuya Satake , Kazuki Shigemori , Toshihiro Wada , Yaling Wang , Steven A. Weissman , Robert M. Wenslow
发明人: Russell R. Ferlita , Yuji Haga , Makoto Ishikawa , Keisuke Kamei , Shinji Kato , Hisaki Kojima , Aaron Moment , Nobuaki Nonoyama , Nobuya Satake , Kazuki Shigemori , Toshihiro Wada , Yaling Wang , Steven A. Weissman , Robert M. Wenslow
IPC分类号: A61K31/4355 , C07D491/048
CPC分类号: C07D491/10
摘要: The present invention relates to a process for producing crystalline trans-N-[1-(2-fluorophenyl)-S-pyrazoly]-3-ox-ospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide and novel salts, hydrates and polymorphs thereof.
摘要翻译: 本发明涉及一种制备结晶反式-N-〔1-(2-氟苯基)-S-吡唑基〕-3-氧 - 环螺[6-氮杂苯并呋喃-1(3H),1'-环己烷〕-4 ' - 甲酰胺及其新型盐,水合物及其多晶型物。
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公开(公告)号:US20090124648A1
公开(公告)日:2009-05-14
申请号:US11988780
申请日:2006-07-24
申请人: Russell R. Ferlita , Yuji Haga , Makoto Ishikawa , Keisuke Kamei , Shinji Kato , Hisaki Kojima , Aaron Moment , Nobuaki Nonoyama , Nobuya Satake , Kazuki Shigemori , Toshihiro Wada , Yaling Wang , Steven A. Weissman , Robert M. Wenslow
发明人: Russell R. Ferlita , Yuji Haga , Makoto Ishikawa , Keisuke Kamei , Shinji Kato , Hisaki Kojima , Aaron Moment , Nobuaki Nonoyama , Nobuya Satake , Kazuki Shigemori , Toshihiro Wada , Yaling Wang , Steven A. Weissman , Robert M. Wenslow
IPC分类号: A61K31/4355 , C07D491/048 , A61P3/04
CPC分类号: C07D491/10
摘要: The present invention relates to a process for producing crystalline trans-N-[1-(2-fluorophenyl)-S-pyrazoly]-3-ox-ospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide and novel salts, hydrates and polymorphs thereof.
摘要翻译: 本发明涉及一种制备结晶反式-N-〔1-(2-氟苯基)-S-吡唑基〕-3-氧 - 环螺[6-氮杂苯并呋喃-1(3H),1'-环己烷〕-4 ' - 甲酰胺及其新型盐,水合物及其多晶型物。
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公开(公告)号:US20060111380A1
公开(公告)日:2006-05-25
申请号:US10536360
申请日:2003-11-25
申请人: Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
发明人: Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
IPC分类号: A61K31/4747 , C07D471/10
CPC分类号: C07D491/10
摘要: The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译: 本发明涉及式(I)化合物:其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T,U,V和W独立为次甲基或氮,所述次甲基任选被取代基取代,T,U,V和W中的至少两个为所述次甲基; X是氮或次甲基。 本发明的化合物可用作治疗与NPY相关的各种疾病的药剂,例如心血管疾病,神经系统疾病,基因疾病,代谢疾病,生殖器或生殖障碍,胃肠道疾病,呼吸系统疾病,炎症性疾病 疾病或青光眼等。
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公开(公告)号:US20050275498A1
公开(公告)日:2005-12-15
申请号:US11143880
申请日:2005-06-01
申请人: Yuji Haga
发明人: Yuji Haga
CPC分类号: H01F5/02 , H01F5/04 , H01F41/076 , H01F41/10 , H01F2027/297
摘要: A coil bobbin for preventing coil lead wires to terminal pins from being loosened, and a transformer employing such coil bobbin. The coil bobbin made of a thermosetting resin is provided with a secondary side terminal base including a first surface to which lead wires of secondary coil wound on the bobbin are led and a second surface provided with terminal pins and perpendicular to the first surface, and with projections projected continuously from both of the first and second surfaces for catching the lead wires to be connected to the terminal pins. The transformer includes primary and secondary coils wound on the bobbin and an iron core mounted about the coils. The lead wires of the secondary coil are led out of the first surface of the secondary side terminal base, caught by the projections and wound on the terminal pins on the second surface of the base.
摘要翻译: 用于防止线圈引线到端子销松动的线圈架,以及采用这种线圈架的变压器。 由热固性树脂制成的线圈架设有二次侧端子座,该二次侧端子座具有:第一面,该第一面被卷绕在筒管上的次级线圈的引线被引导;第二面,设置有端子销并与第一面垂直; 从第一和第二表面两端连续突出的突起,用于捕捉要连接到端子销的引线。 变压器包括缠绕在绕线管上的初级线圈和次级线圈以及围绕线圈安装的铁芯。 次级线圈的引线从次级侧端子座的第一表面引出,被突起卡住,并缠绕在基座的第二表面上的端子销上。
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公开(公告)号:US06649624B2
公开(公告)日:2003-11-18
申请号:US10226225
申请日:2002-08-23
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: A61K31438
CPC分类号: C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要: A method for treating a central nervous system disorder, which involves administering to a patient in need a therapeutically effective amount of a compound of formula (I): wherein Ar1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, nitro, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, cyclo(lower) alkyl, lower alkenyl, lower alkoxy, halo(lower) alkoxy, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylene optionally substituted with oxo, and a group represented by the formula —Q—Ar2; Ar2 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, cyano, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, hydroxy, lower alkoxy, halo(lower) alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl: n represents 0 or 1; Q represents a single bond or carbonyl; 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; Y represents an imino which may be substituted with lower alkyl, or oxygen; or a salt or ester thereof
摘要翻译: 一种治疗中枢神经系统疾病的方法,其涉及向需要的患者施用治疗有效量的式(I)化合物:其中Ar 1表示可被取代的芳基或杂芳基,所选择的取代基 卤代低级烷基,羟基(低级)烷基,环(低级)烷基,低级烯基,低级烷氧基,卤代(低级)烷氧基,低级烷硫基,羧基,低级烷酰基, 低级烷氧基羰基,任选被氧代取代的低级亚烷基和由式-Q-Ar 2表示的基团; Ar 2表示可被取代的芳基或杂芳基,该取代基选自卤素, 氰基,低级烷基,卤代(低级)烷基,羟基(低级)烷基,羟基,低级烷氧基,卤代(低级)烷氧基,低级烷基氨基,二低级烷基氨基,低级烷酰基和芳基:n表示0或1; Q表示 单键或羰基; T,U,V和W各自独立地表示 反应可以具有选自卤素,低级烷基,羟基和低级烷氧基的取代基的氮原子或次甲基,其中至少两个表示所述次甲基; X表示次甲基; Y表示亚氨基, 被低级烷基或氧取代; 或其盐或酯
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公开(公告)号:US08044070B2
公开(公告)日:2011-10-25
申请号:US12540534
申请日:2009-08-13
申请人: Norikazu Ohtake , Akira Naya , Yuji Haga , Makoto Jitsuoka , Takuya Suga , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani
发明人: Norikazu Ohtake , Akira Naya , Yuji Haga , Makoto Jitsuoka , Takuya Suga , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani
IPC分类号: A61K31/445 , C07D211/00
CPC分类号: C07D401/12 , A61K31/4545 , A61K31/501 , A61K31/506 , C07D401/14 , C07D403/12 , C07D413/14 , C07D471/04
摘要: Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II): or the following formula (III): Y represents a group of a formula (IV): The compounds have a histamine-H3 receptor antagonistic or inverse-agonistic activity and are useful for remedy and/or prevention of obesity, diabetes, hormone secretion disorders, sleep disorders, etc.
摘要翻译: 提供式(I)化合物及其药学上可接受的盐:其中X1,X2和X3各自独立地表示N或CH; W表示下式(II):或下式(III):Y表示式(IV)的基团:所述化合物具有组胺H3受体拮抗或反向激动活性,可用于治疗和/或 预防肥胖,糖尿病,激素分泌障碍,睡眠障碍等
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公开(公告)号:US07732456B2
公开(公告)日:2010-06-08
申请号:US10591373
申请日:2005-03-04
申请人: Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
发明人: Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
IPC分类号: A61K31/444 , C07D401/02
CPC分类号: C07D213/69 , C07D237/16 , C07D239/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D451/02 , C07D471/04
摘要: The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].
摘要翻译: 本发明提供由通式(I)表示的吡啶酮衍生物[在该式中,R 1和R 2可以相同或不同,代表H等,或者R 1和R 2可以与脂族含氮杂环基一起形成 他们绑定的N X1-X3可以相同或不同,代替次甲基或N,但不是全部同时代表氮; X4-X7可以相同或不同,代表次甲基或N,条件是它们中的三个或更多不同时代表N; Y1和Y3可以相同或不同,代表单键,-O-,-NR-,-S-等; Y2代表低级亚烷基等; R代表H等,L代表亚甲基; Z 1和Z 2可以相同或不同,代表单键或低级亚烷基; 或R1,L和Z2可以与R1结合的N形成脂族含氮杂环基; 和Ar代表芳族碳环基团等]。
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公开(公告)号:US20090264426A1
公开(公告)日:2009-10-22
申请号:US11991334
申请日:2006-09-05
申请人: Shunji Sakuraba , Minoru Kameda , Hiroyuki Kishino , Yuji Haga , Norikazu Otake , Minoru Moriya
发明人: Shunji Sakuraba , Minoru Kameda , Hiroyuki Kishino , Yuji Haga , Norikazu Otake , Minoru Moriya
IPC分类号: A61K31/5377 , C07D401/10 , C07D413/14 , A61K31/47 , A61P9/10
CPC分类号: C07D401/14 , C07D401/04 , C07D405/04 , C07D471/04
摘要: Disclosed is a compound represented by the formula (I): Wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like; X1, X2 and X3 independently represent a methine group or a nitrogen atom; Y1 and Y3 independently represent a single bond, —O— or the like; Y2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methylene group or the like; L represents a single bond, a methylene group or the like; Z1 and Z2 independently represent a single bond, a C1-4 alkylene group or the like; Ar1 represents an aromatic carbocyclic ring or the like; and Ar2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.
摘要翻译: 公开了由式(I)表示的化合物:其中R1和R2独立地表示氢原子,低级烷基等; X1,X2和X3独立地表示次甲基或氮原子; Y1和Y3独立地表示单键,-O-等; Y2表示低级亚烷基等; W1至W4独立地表示单键,亚甲基等; L表示单键,亚甲基等; Z 1和Z 2独立地表示单键,C 1-4亚烷基等; Ar 1表示芳香族碳环等, Ar 2表示双环芳香族碳环等。 该化合物可用作中枢性疾病,心血管疾病或代谢性疾病的药物。
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公开(公告)号:US20090137587A1
公开(公告)日:2009-05-28
申请号:US11990889
申请日:2006-08-23
申请人: Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
发明人: Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
IPC分类号: A61K31/444 , C07D213/64 , C07D401/02 , C07D413/02 , A61K31/4439 , A61P9/00 , A61P25/00 , A61P3/00 , C07D401/14 , A61K31/5377 , A61K31/4545
CPC分类号: C07D213/69 , C07D213/64 , C07D401/10 , C07D413/10
摘要: A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents —CH2—O—, —CH═CH— or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
摘要翻译: 作为活性成分,含有式(I)所示的化合物:其中,R 1和R 2分别独立地表示氢原子,低级烷基等,或者与连接有L,Z 2和R 1的氮原子一起形成 可以形成脂族氮杂环基,并且R 1和R 2与它们所连接的氮原子一起形成脂族氮杂环基; X表示次甲基或氮原子; Y表示-CH 2 -O - , - CH-CH-等; Z1表示单键,C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基,C3-8亚环烷基等; Ar表示芳族碳环基等。 该化合物可用作中枢神经系统疾病,心血管疾病或代谢疾病的药物。
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