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公开(公告)号:US08729264B2
公开(公告)日:2014-05-20
申请号:US12680484
申请日:2008-09-26
申请人: Keisuke Yamamoto , Seiji Aratake , Daisuke Nakashima , Kimihisa Ueno , Mirai Mizutani , Daisuke Harada , Katsuya Kobayashi , Kazuki Hemmi
发明人: Keisuke Yamamoto , Seiji Aratake , Daisuke Nakashima , Kimihisa Ueno , Mirai Mizutani , Daisuke Harada , Katsuya Kobayashi , Kazuki Hemmi
IPC分类号: C07D487/00
CPC分类号: C07D487/04 , A61K31/519 , A61K31/5377
摘要: Provided is an agent for the prevention and/or treatment of a skin disease containing, as an active ingredient, a pyrazolopyrimidine derivative represented by the formula (I) (wherein each symbol is as defined in the specification), or a pharmacologically acceptable salt thereof, and the like.
摘要翻译: 本发明提供含有式(I)表示的吡唑并嘧啶衍生物(其中各符号如说明书中的定义)作为活性成分的皮肤病的预防和/或治疗药剂或其药理学上可接受的盐 ,等等。
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公开(公告)号:US08486980B2
公开(公告)日:2013-07-16
申请号:US13057599
申请日:2009-08-06
申请人: Arata Yanagisawa , Keiji Uehara , Masahiro Matsubara , Kimihisa Ueno , Michihiko Suzuki , Takeshi Kuboyama , Keisuke Yamamoto , Tomohiro Tamura
发明人: Arata Yanagisawa , Keiji Uehara , Masahiro Matsubara , Kimihisa Ueno , Michihiko Suzuki , Takeshi Kuboyama , Keisuke Yamamoto , Tomohiro Tamura
IPC分类号: A61K31/4245 , A61K31/335 , A61K31/4184 , A61K31/4188 , C07D271/07 , C07D313/10 , C07D235/00 , C07D235/04
CPC分类号: C07D471/04 , A61K31/335 , A61K31/4184 , A61K31/422 , A61K31/4353 , A61K31/4409 , C07C255/34 , C07C255/44 , C07D235/08 , C07D235/16 , C07D257/04 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14
摘要: Provided is a tricyclic compound having a PPAR γ agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:
摘要翻译: 本发明提供具有PPARγ激动剂活性的三环化合物,其通式(I)表示,其中Z表示单键等,Y表示氢原子,任选具有取代基的低级烷基等, X表示氢原子等,A表示芳基等,B和C相同或不同,各自表示芳香族碳环等,R4-R9相同或不同,表示氢等, V表示单键等,R 10和R 11相同或不同,各自表示氢等,或其药学上可接受的盐等:
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公开(公告)号:US07005430B2
公开(公告)日:2006-02-28
申请号:US10149423
申请日:2000-12-22
申请人: Kimihisa Ueno , Akira Ogawa , Yoshihisa Ohta , Yuji Nomoto , Kotaro Takasaki , Hideaki Kusaka , Hiroshi Yano , Chiharu Nakagawa , Satoshi Nakanishi
发明人: Kimihisa Ueno , Akira Ogawa , Yoshihisa Ohta , Yuji Nomoto , Kotaro Takasaki , Hideaki Kusaka , Hiroshi Yano , Chiharu Nakagawa , Satoshi Nakanishi
IPC分类号: C07D487/14 , C07D473/24 , C07D473/22 , A61K31/519 , A61P3/10
CPC分类号: C07D487/14
摘要: A condensed purine derivative represented by Formula (I): wherein X—Y-Z represents R1N—C═O or N═C—W, R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, n represents an integer of from 0 to 3, V1 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, V2 represents a substituted lower alkyl group or a substituted or unsubstituted aromatic heterocyclic group, and when V1 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and for example, X—Y-Z represents R1aN—C═O and R2 represents a substituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted alicyclic heterocyclic group, a halogen atom, a lower alkylthio group, —NR7R8, —CO2H, a lower alkoxycarbonyl group, —COHal, —CONR9R10 or —CHO, V2 may represent a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group; or a pharmacologically acceptable salt thereof.
摘要翻译: 由式(I)表示的稠合嘌呤衍生物:化学式id =“CHEM-US-00001”num =“000”
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公开(公告)号:US20140163008A1
公开(公告)日:2014-06-12
申请号:US14236545
申请日:2011-08-03
IPC分类号: C07D495/04 , C07D471/04 , C07D487/04 , C07D413/14
CPC分类号: C07D495/04 , A61K31/335 , A61K31/4245 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4985 , A61K31/5025 , A61K31/519 , C07D413/14 , C07D471/04 , C07D487/04
摘要: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPARγ agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
摘要翻译: 由以下通式(I)表示的二苯并氧杂环己烷衍生物,其中Y为氢原子等,RA为氢原子等,X为式(b3),其中RB为氢原子等, A是式(a18),其中R1是氢原子等,RC和RD相同或不同,各自是具有PPARγ激动剂活性的氢原子等,以及 作为2型糖尿病等的治疗剂和/或预防剂等,或其药学上可接受的盐等有用。
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公开(公告)号:US5539112A
公开(公告)日:1996-07-23
申请号:US464093
申请日:1995-06-05
申请人: Tsutomu Akama , Shun-ichi Ikeda , Yasushi Shida , Masaji Kasai , Hiroyuki Ishida , Uichiro Kimura , Katsushige Gomi , Hiromitsu Saito , Kimihisa Ueno
发明人: Tsutomu Akama , Shun-ichi Ikeda , Yasushi Shida , Masaji Kasai , Hiroyuki Ishida , Uichiro Kimura , Katsushige Gomi , Hiromitsu Saito , Kimihisa Ueno
IPC分类号: C07D311/30 , C07D413/12
CPC分类号: C07D311/30
摘要: 5-Aminoflavone derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and represent hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, halogen-substituted or unsubstituted lower alkanoyl or lower alkoxycarbonyl, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 are the same or different and represent hydrogen, halogen or lower alkyl, at least one of X.sup.1 and X.sup.2 represents halogen or lower alkyl, X.sup.3 represents hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, halogen, hydroxy, substituted or unsubstituted lower alkoxy, NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or substituted or unsubstituted lower alkyl, or R.sup.5 and R.sup.6 are taken together to form a heterocyclic group containing the nitrogen atom in the ring), lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, lower alkoxycarbonyl, lower alkanoyl, adizo, cyano, substituted or unsubstituted carbamoyl or lower alkylthiothiocarbonyl: or pharmaceutically acceptable salts thereof.
摘要翻译: 由式(I)表示的5-氨基黄酮衍生物:其中R 1,R 2,R 3和R 4相同或不同,表示氢,取代或未取代的低级烷基,低级烯基,卤素取代或未取代的低级 烷酰基或低级烷氧基羰基,X 1,X 2,Y 1和Y 2相同或不同,表示氢,卤素或低级烷基,X 1和X 2中的至少一个表示卤素或低级烷基,X 3表示氢,取代或未取代的低级烷基,低级 烯基,低级炔基,卤素,羟基,取代或未取代的低级烷氧基,NR5R6(其中R5和R6相同或不同,代表氢,或取代或未取代的低级烷基,或R5和R6一起形成含有 环中的氮原子),低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,羧基,低级烷氧基羰基,低级烷酰基,二唑基,氰基,取代或未取代的氨基甲酰基或低级烷硫基硫代 辛基或其药学上可接受的盐。
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公开(公告)号:US08242151B2
公开(公告)日:2012-08-14
申请号:US12162119
申请日:2008-02-07
申请人: Arata Yanagisawa , Takeshi Kuboyama , Seiji Aratake , Kazuki Hemmi , Kimihisa Ueno , Michihiko Suzuki , Masahiro Matsubara , Kozo Yao , Akinori Hamaguchi , Yukihito Tsukumo
发明人: Arata Yanagisawa , Takeshi Kuboyama , Seiji Aratake , Kazuki Hemmi , Kimihisa Ueno , Michihiko Suzuki , Masahiro Matsubara , Kozo Yao , Akinori Hamaguchi , Yukihito Tsukumo
CPC分类号: C07D403/14 , A61K31/4245 , A61K31/437 , A61K31/55 , C07D413/10 , C07D413/14 , C07D471/04
摘要: The present invention provides a PPAR γ agonist comprising, as an active ingredient, a tricyclic compound represented by the formula (I) (wherein R1 represents lower alkyl optionally having substituent(s) or the like, R2 and R3 are the same or different and each represents lower alkyl optionally having substituent(s) or the like, R4 and R5 are the same or different and each represents a hydrogen atom or the like, Q1-Q2-Q3 represents CH═CH—CH═CH or the like, Y represents a single bond or the like, Z1-Z2 represents C═CR13 (wherein R13 represents a hydrogen atom or the like), or the like, and A represents —COOH or the like), or a pharmaceutically acceptable salt thereof and the like.
摘要翻译: 本发明提供一种PPARγ激动剂,其包含作为活性成分的由式(I)表示的三环化合物(其中R 1表示任选具有取代基的低级烷基等),R2和R3相同或不同, 各自表示任选具有取代基等的低级烷基,R4和R5相同或不同,各自表示氢原子等,Q1-Q2-Q3表示CH = CH-CH = CH等,Y 表示单键或类似物,Z1-Z2表示C = CR13(其中R13表示氢原子等)等,A表示-COOH等)或其药学上可接受的盐等 。
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公开(公告)号:US20070191402A1
公开(公告)日:2007-08-16
申请号:US10514119
申请日:2003-05-16
申请人: Hiroki Ishiguro , Yuko Saeki , Seiji Sugimoto , Masahiro Matsubara , Kimihisa Ueno , Kiyotoshi Mori , Satoshi Nakanishi , Hiroshi Yano
发明人: Hiroki Ishiguro , Yuko Saeki , Seiji Sugimoto , Masahiro Matsubara , Kimihisa Ueno , Kiyotoshi Mori , Satoshi Nakanishi , Hiroshi Yano
IPC分类号: A61K31/519 , A61K31/53 , C07D487/12 , G01N33/53
CPC分类号: C12Q1/32 , A61K31/53 , A61K31/5377 , A61K31/55 , C07D487/14 , G01N33/56966 , G01N2333/90209 , G01N2500/00
摘要: The present invention provides a screening method of a substance which inhibits binding of a condensed purine derivative to a pancreatic β cell or a treated product of the cell, a substance which inhibits binding of a condensed purine derivative to a protein capable of the condensed purine derivative, and a substance which inhibits the expression or enzymatic activity of a protein capable of a condensed purine derivative, which comprises using the condensed purine derivative and a pancreatic β cell or a treated product of the cell or a protein capable of binding to the condensed purine derivative.
摘要翻译: 本发明提供了抑制冷凝的嘌呤衍生物与胰腺β细胞或细胞的处理产物的结合的物质的筛选方法,抑制结合的嘌呤衍生物与能够产生缩合嘌呤衍生物的蛋白质结合的物质 以及抑制能够结合嘌呤衍生物的蛋白质的表达或酶活性的物质,其包括使用稠合的嘌呤衍生物和胰β细胞或能够结合浓缩的嘌呤的细胞或蛋白质的处理产物 衍生物。
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公开(公告)号:US20070037834A1
公开(公告)日:2007-02-15
申请号:US10516750
申请日:2003-06-06
申请人: Hitoshi Arai , Tsutomu Matsumura , Hiroshi Ishida , Yosuke Yamaura , Seiji Aratake , Etsuo Ohshima , Koji Yanagawa , Motoki Miyama , Koji Suzuki , Ari Kawabe , Satoshi Nakanishi , Katsuya Kobayashi , Takashi Sato , Ichiro Miki , Kimihisa Ueno , Shinya Fujii , Miho Iwase
发明人: Hitoshi Arai , Tsutomu Matsumura , Hiroshi Ishida , Yosuke Yamaura , Seiji Aratake , Etsuo Ohshima , Koji Yanagawa , Motoki Miyama , Koji Suzuki , Ari Kawabe , Satoshi Nakanishi , Katsuya Kobayashi , Takashi Sato , Ichiro Miki , Kimihisa Ueno , Shinya Fujii , Miho Iwase
IPC分类号: A61K31/519 , C07D487/02
CPC分类号: C07D263/58 , C07D471/04 , C07D487/04
摘要: [wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m+n is 4 or less; R1 represents —NR4R5 (wherein R4 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R2 represents the above Formula (II), Formula (IV) or the like; A represents a single bond, —C(═O)—, —SO2—, —OC(═O)— or the like; and R3 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like]Bicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided. These have anti-inflammatory activities or modulation activities on the functions of TARC and/or MDC and are useful for treating and/or preventing a disease which is related to T cells, such as an allergic disease, an autoimmune disease or transplant rejection.
摘要翻译: [其中m和n可以相同或不同,并且各自表示1〜3的整数,其中m + n为4以下; R 1表示-NR 4 R 5(其中R 4,R 5和R 5) 可以相同或不同,各自表示氢原子,取代或未取代的低级烷基,取代或未取代的芳烷基等); R 2表示上述式(II),式(IV)等; A表示单键,-C(-O) - , - SO 2 - , - OC(-O) - 等; 和R 3表示取代或未取代的低级烷基,取代或未取代的环烷基,取代或未取代的芳烷基等〕由上式(I)表示的双环嘧啶衍生物或其季铵盐或药学上可接受的盐 可接受的盐等。 它们具有对TARC和/或MDC的功能的抗炎活性或调节活性,并且可用于治疗和/或预防与T细胞相关的疾病,例如过敏性疾病,自身免疫疾病或移植排斥反应。
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公开(公告)号:US08969345B2
公开(公告)日:2015-03-03
申请号:US14236545
申请日:2012-08-03
IPC分类号: C07D413/14 , C07D471/04 , C07D487/04 , C07D495/04 , A61K31/4245 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4985 , A61K31/5025 , A61K31/519
CPC分类号: C07D495/04 , A61K31/335 , A61K31/4245 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4985 , A61K31/5025 , A61K31/519 , C07D413/14 , C07D471/04 , C07D487/04
摘要: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPARγ agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
摘要翻译: 由以下通式(I)表示的二苯并氧杂环己烷衍生物,其中Y为氢原子等,RA为氢原子等,X为式(b3),其中RB为氢原子等, A是式(a18),其中R1是氢原子等,RC和RD相同或不同,各自是具有PPARγ激动剂活性的氢原子等,以及 作为2型糖尿病等的治疗剂和/或预防剂等,或其药学上可接受的盐等有用。
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公开(公告)号:US20100256134A1
公开(公告)日:2010-10-07
申请号:US12680484
申请日:2008-09-26
申请人: Keisuke Yamamoto , Seiji Aratake , Daisuke Nakashima , Kimihisa Ueno , Mirai Mizutani , Daisuke Harada , Katsuya Kobayashi , Kazuki Hemmi
发明人: Keisuke Yamamoto , Seiji Aratake , Daisuke Nakashima , Kimihisa Ueno , Mirai Mizutani , Daisuke Harada , Katsuya Kobayashi , Kazuki Hemmi
IPC分类号: A61K31/5377 , A61K31/519 , A61K31/497 , A61P17/00
CPC分类号: C07D487/04 , A61K31/519 , A61K31/5377
摘要: Provided is an agent for the prevention and/or treatment of a skin disease containing, as an active ingredient, a pyrazolopyrimidine derivative represented by the formula (I) (wherein each symbol is as defined in the specification), or a pharmacologically acceptable salt thereof, and the like.
摘要翻译: 本发明提供含有式(I)表示的吡唑并嘧啶衍生物(其中各符号如说明书中的定义)作为活性成分的皮肤病的预防和/或治疗药剂或其药理学上可接受的盐 ,等等。
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