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公开(公告)号:US20070208046A1
公开(公告)日:2007-09-06
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: A61K31/513 , A61K31/444 , A61K31/4412 , C07D403/02 , 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 alkylene, 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[在式中,R 1和R 2可以相同或不同,代表H等, 或R 1和R 2可以与它们所键合的N一起形成脂族含氮杂环基; X 1 -X 3可以相同或不同,代表次甲基或N,但并不全部同时代表氮; X 4 -X 7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个不同时代表N; Y 1和Y 3可以相同或不同,代表单键,-O-,-NR-,-S-等; Y 2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R 1,L和Z 2可以与R 1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:US20060178375A1
公开(公告)日:2006-08-10
申请号:US10561115
申请日:2004-06-24
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: A61K31/506 , C07D413/14 , C07D403/14
CPC分类号: C07D401/12 , A61K31/4545 , A61K31/501 , A61K31/506 , C07D401/14 , C07D403/12 , C07D413/14 , C07D471/04
摘要: Compound of the formula: (I) [wherein each of X1, X2, and X3 independently represents N or CH, W represents the formula (II):(II) or the formula (III):(III) and Y represents a group of the formula (IV):(IV)], or a pharmacologically acceptable salt thereof. This compound exhibits histamine receptor H3 antagonist or inverse agonist activity and is useful of the treatment and/or prevention of obesity, diabetes, hormonal secretion abnormality, sleep, disorder, etc.
摘要翻译: 式(I)的化合物[其中X 1,X 2和X 3各自独立地表示N或CH,W表示 式(II):(II)或式(III):III),Y表示式(IV):(IV)]的基团,或其药理学上可接受的盐。 该化合物显示组胺受体H3拮抗剂或反向激动剂活性,并且可用于治疗和/或预防肥胖症,糖尿病,激素分泌异常,睡眠,障碍等。
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公开(公告)号:US20050032820A1
公开(公告)日:2005-02-10
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: C07D491/107 , A61K31/438 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/06 , A61P29/00 , A61P43/00 , C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10 , C07D519/00 , C07D487/14 , A61K31/4747 , A61K31/519
CPC分类号: C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10
摘要: A Compound represented by the general formula (I): wherein AR1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of hydroxy, 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; Ar2represents 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, 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 exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis and the like, central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal and the like, metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia and the like, sexual and reproductive dysfunction, gastro-intestinal disorder, respiratory disorder, inflammation or glaucoma, and the like.
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公开(公告)号:US06462053B1
公开(公告)日:2002-10-08
申请号:US10101221
申请日:2002-03-20
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: A61K34355
CPC分类号: C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要: A method for treating a cardiovascular 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: 一种治疗心血管疾病的方法,其涉及向需要的患者施用治疗有效量的式(I)化合物:其中Ar1表示可被取代的芳基或杂芳基,所述取代基选自 卤素,硝基,低级烷基,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, 任选被氧代取代的基团和由式-Q-Ar 2表示的基团; Ar 2表示可被取代的芳基或杂芳基,所述取代基选自卤素,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, W各自独立地表示硝基 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表示可以被取代的亚氨基 与低级烷基或氧; 或其盐或酯。
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公开(公告)号:US20120035155A1
公开(公告)日:2012-02-09
申请号:US13263801
申请日:2010-04-17
申请人: Yuji Haga , Sayaka Mizutani , Nagaaki Sato
发明人: Yuji Haga , Sayaka Mizutani , Nagaaki Sato
IPC分类号: A61K31/4725 , C07D401/14 , A61P9/12 , A61P9/10 , A61P13/12 , A61P9/00 , A61P3/04 , A61P3/10 , A61P5/00 , A61P3/06 , A61P19/06 , A61P1/16 , A61P29/00 , A61P1/04 , C07D401/12
CPC分类号: C07D403/06 , C07D403/12 , C07D403/14
摘要: To provide an indole compound having a human QRFP receptor antagonistic activity and useful as a preventive or a remedy for various disorders. A compound of a formula (I) or a pharmaceutically-acceptable salt thereof is provided: [wherein, R1 represents a hydrogen atom, a halogen, a C1-6 alkyl, etc,; R2 represents a C1-6 alkyl, or a halo-C1-6 alkyl; R3 represents a hydrogen atom, a C1-6 alkyl, etc.; R4 represents a hydrogen atom, a C1-6 alkyl, a halo-C1-6 alkyl, etc.; or R3 and R4, taken together with the nitrogen atom to which they bond, form a 3- to 6-membered aliphatic nitrogen-containing hetero ring; or R3 and Y3, taken together, form —CH2—CH2—; Y1 and Y2 are both hydrogen atoms; or Y1 and Y2, taken together, form —CH2—CH2—; and Y3 represents a hydrogen atom; or Y3 and R3, taken together, form —CH2—CH2—].
摘要翻译: 提供具有人QRFP受体拮抗活性的吲哚化合物,并且可用作各种疾病的预防或补救。 提供式(I)化合物或其药学上可接受的盐:[其中,R 1表示氢原子,卤素,C 1-6烷基等; R 2表示C 1-6烷基或卤代C 1-6烷基; R3代表氢原子,C1-6烷基等; R 4表示氢原子,C 1-6烷基,卤代C 1-6烷基等; 或R 3和R 4与它们键合的氮原子一起形成3至6元脂族含氮杂环; 或R 3和Y 3一起形成-CH 2 -CH 2 - ; Y1和Y2都是氢原子; 或Y1和Y2一起形成-CH 2 -CH 2 - ; Y 3表示氢原子; 或Y 3和R 3一起形成-CH 2 -CH 2 - ]。
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公开(公告)号:US20100210637A1
公开(公告)日:2010-08-19
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: A61K31/5377 , C07D403/12 , A61K31/506 , A61P3/10 , A61P3/04 , A61P1/16 , A61P3/06 , A61P9/10 , C07D401/12 , A61K31/4545 , C07D413/14 , A61K31/501
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:US07595316B2
公开(公告)日:2009-09-29
申请号:US10561115
申请日:2004-06-24
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: A01N43/58 , A61K31/50 , C07D239/00 , C07D239/02
CPC分类号: C07D401/12 , A61K31/4545 , A61K31/501 , A61K31/506 , C07D401/14 , C07D403/12 , C07D413/14 , C07D471/04
摘要: Compound of the formula: (I) [wherein each of X1, X2 and X3 independently represents N or CH, W represents the formula (II):(II) or the formula (III):(III) and Y represents a group of the formula (IV):(IV)], or a pharmacologically acceptable salt thereof. This compound exhibits histamine receptor H3 antagonist or inverse agonist activity and is useful of the treatment and/or prevention of obesity, diabetes, hormonal secretion abnormality, sleep, disorder, etc.
摘要翻译: 式(I)的化合物[其中X1,X2和X3各自独立地表示N或CH,W表示式(II):(II)或式(III):III),Y表示 式(IV):(IV)]或其药理学上可接受的盐。 该化合物显示组胺受体H3拮抗剂或反向激动剂活性,并且可用于治疗和/或预防肥胖症,糖尿病,激素分泌异常,睡眠,障碍等。
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公开(公告)号:US07589096B2
公开(公告)日:2009-09-15
申请号:US12071808
申请日:2008-02-26
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: A61K31/438 , A61K31/506 , A61K31/4545 , C07D233/96 , C07D401/14 , C07D401/02
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, wherein a methine may be optionally substituted by a substituent, and at least two of T, U, V and W are 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, gastro-intestinal 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独立地是次甲基或氮,其中次甲基可以任选地被取代基取代,并且T,U,V和W中的至少两个是次甲基; 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,呼吸障碍 ,炎症性疾病或青光眼等。
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公开(公告)号:US20080188507A1
公开(公告)日:2008-08-07
申请号:US12071808
申请日:2008-02-26
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 , C07D491/14
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, gastro-intestinal 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,呼吸障碍 ,炎症性疾病或青光眼等。
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公开(公告)号:US07365079B2
公开(公告)日:2008-04-29
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: A61K31/4355 , C07D471/04
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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