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1. 发明授权

US07754728B2 Adenine compound and use thereof 失效
标题翻译：腺嘌呤化合物及其用途
公开(公告)号：US07754728B2
公开(公告)日：2010-07-13
申请号：US10528343
申请日：2003-09-26
申请人： Yoshiaki Isobe , Haruo Takaku , Haruhisa Ogita , Masanori Tobe , Ayumu Kurimoto , Tetsuhiro Ogino , Hitoshi Fujita
发明人： Yoshiaki Isobe , Haruo Takaku , Haruhisa Ogita , Masanori Tobe , Ayumu Kurimoto , Tetsuhiro Ogino , Hitoshi Fujita
IPC分类号： C07D473/18 , C07D473/16 , A61K31/522 , A61P11/06 , A61P37/08
CPC分类号： A61K31/5377 , A61K31/522 , A61K31/55
摘要： A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.
摘要翻译：用作局部给药的药物，其作为抗过敏剂有效。用于局部给药的药物含有作为活性成分的由通式（1）表示的腺嘌呤化合物：[其中环A表示6至10元，单或双环，芳族烃或5至10元，单或双环，含有1至3个选自0至2个氮原子，0或1个氧原子和0或1个硫原子的杂原子的芳族杂环; n为0〜2的整数， m为0〜2的整数; R代表卤代，（取代）烷基等; X1代表氧，硫，NR1（R1代表氢或烷基）或单键; Y1表示单键，亚烷基等; Y2表示单键，亚烷基等; Z表示亚烷基; 并且Q1和Q2中的至少一个表示-COOR 10（其中R 10表示（un）取代的烷基等）等）或该化合物的药学上可接受的盐。

2. 发明授权

US08148371B2 Adenine compound and use thereof 失效
标题翻译：腺嘌呤化合物及其用途
公开(公告)号：US08148371B2
公开(公告)日：2012-04-03
申请号：US12793649
申请日：2010-06-03
申请人： Yoshiaki Isobe , Haruo Takaku , Haruhisa Ogita , Masanori Tobe , Ayumu Kurimoto , Tetsuhiro Ogino , Hitoshi Fujita
发明人： Yoshiaki Isobe , Haruo Takaku , Haruhisa Ogita , Masanori Tobe , Ayumu Kurimoto , Tetsuhiro Ogino , Hitoshi Fujita
IPC分类号： C07D473/18 , A61K31/522 , A61P37/08 , A61P11/06 , C07D473/40 , C07D473/16
CPC分类号： A61K31/5377 , A61K31/522 , A61K31/55
摘要： A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.
摘要翻译：用作局部给药的药物，其作为抗过敏剂有效。用于局部给药的药物含有作为活性成分的由通式（1）表示的腺嘌呤化合物：[其中环A表示6至10元，单或双环，芳族烃或5至10元，单或双环，含有1至3个选自0至2个氮原子，0或1个氧原子和0或1个硫原子的杂原子的芳族杂环; n为0〜2的整数， m为0〜2的整数; R代表卤代，（取代）烷基等; X1代表氧，硫，NR1（R1代表氢或烷基）或单键; Y1表示单键，亚烷基等; Y2表示单键，亚烷基等; Z表示亚烷基; 并且Q1和Q2中的至少一个表示-COOR 10（其中R 10表示（un）取代的烷基等）等）或该化合物的药学上可接受的盐。

3. 发明申请

US20060052403A1 Novel adenine compound and use thereof 失效
标题翻译：新型腺嘌呤化合物及其用途
公开(公告)号：US20060052403A1
公开(公告)日：2006-03-09
申请号：US10528343
申请日：2003-09-26
申请人： Yoshiaki Isobe , Haruo Takaku , Haruhisa Ogita , Masanori Tobe , Ayumu Kurimoto , Tetsuhiro Ogino , Hitoshi Fujita
发明人： Yoshiaki Isobe , Haruo Takaku , Haruhisa Ogita , Masanori Tobe , Ayumu Kurimoto , Tetsuhiro Ogino , Hitoshi Fujita
IPC分类号： A61K31/52 , C07D473/12 , C07D473/14
CPC分类号： A61K31/5377 , A61K31/522 , A61K31/55
摘要： A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.
摘要翻译：用作局部给药的药物，其作为抗过敏剂有效。用于局部给药的药物含有由通式（1）表示的腺嘌呤化合物作为活性成分：

4. 发明授权

US07521454B2 Adenine derivatives 失效
标题翻译：腺嘌呤衍生物
公开(公告)号：US07521454B2
公开(公告)日：2009-04-21
申请号：US11582452
申请日：2006-10-18
申请人： Yoshiaki Isobe , Haruhisa Ogita , Masanori Tobe , Haruo Takaku , Tetsuhiro Ogino , Ayumu Kurimoto , Hajime Kawakami
发明人： Yoshiaki Isobe , Haruhisa Ogita , Masanori Tobe , Haruo Takaku , Tetsuhiro Ogino , Ayumu Kurimoto , Hajime Kawakami
IPC分类号： A61P11/06 , A61P17/00 , A61P35/00 , C07D473/16 , C07D473/18 , C07D473/24 , A61K31/52 , A61K31/522
CPC分类号： C07D473/00 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/34
摘要： This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): wherein X represents NR3 (wherein R3 represents a hydrogen atom or C1-3 alkyl) or the like; R1 represents substituted or unsubstituted alkyl or the like; R2 represents hydroxyl or the like; and Y represents a substituted or unsubstituted aromatic hetero ring or the like. Also, the present invention relates to pharmaceuticals such as an interferon inducer, antiviral agent, anticancer agent, type 2 helper T cell selective immune response inhibitor, antiallergic agent, and immune response modulator comprising the above derivative as an active ingredient.
摘要翻译：本发明涉及由通式（I）表示的腺嘌呤衍生物，其互变异构体或其药学上可接受的盐：其中X表示NR 3（其中R 3表示氢原子或C 1-3烷基）等; R 1表示取代或未取代的烷基等; R2表示羟基等; Y表示取代或未取代的芳族杂环等。此外，本发明涉及包含上述衍生物作为活性成分的药物，例如干扰素诱导剂，抗病毒剂，抗癌剂，2型辅助T细胞选择性免疫应答抑制剂，抗过敏剂和免疫应答调节剂。

5. 发明授权

US07157465B2 Adenine derivatives 失效
标题翻译：腺嘌呤衍生物
公开(公告)号：US07157465B2
公开(公告)日：2007-01-02
申请号：US10474199
申请日：2002-04-15
申请人： Yoshiaki Isobe , Haruhisa Ogita , Masanori Tobe , Haruo Takaku , Tetsuhiro Ogino , Ayumu Kurimoto , Hajime Kawakami
发明人： Yoshiaki Isobe , Haruhisa Ogita , Masanori Tobe , Haruo Takaku , Tetsuhiro Ogino , Ayumu Kurimoto , Hajime Kawakami
IPC分类号： C07D473/16 , C07D473/18 , C07D473/24 , A61K31/52 , A61K31/522
CPC分类号： C07D473/00 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/34
摘要： This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): wherein X represents NR3 (wherein R3 represents a hydrogen atom or C1-3 alkyl) or the like; R1 represents substituted or unsubstituted alkyl or the like; R2 represents hydroxyl or the like; and Y represents a substituted or unsubstituted aromatic hetero ring or the like. Also, the present invention relates to pharmaceuticals such as an interferon inducer, antiviral agent, anticancer agent, type 2 helper T cell selective immune response inhibitor, antiallergic agent, and immune response modulator comprising the above derivative as an active ingredient.
摘要翻译：本发明涉及由通式（I）表示的腺嘌呤衍生物，其互变异构体或其药学上可接受的盐：其中X表示NR 3（其中R 3表示氢原子或C 1-3烷基）等; R 1表示取代或未取代的烷基等; R 2表示羟基等; Y表示取代或未取代的芳族杂环等。此外，本发明涉及包含上述衍生物作为活性成分的药物，例如干扰素诱导剂，抗病毒剂，抗癌剂，2型辅助T细胞选择性免疫应答抑制剂，抗过敏剂和免疫应答调节剂。

6. 发明申请

US20070037832A1 Novel adenine derivatives 失效
标题翻译：新型腺嘌呤衍生物
公开(公告)号：US20070037832A1
公开(公告)日：2007-02-15
申请号：US11582452
申请日：2006-10-18
申请人： Yoshiaki Isobe , Haruhisa Ogita , Masanori Tobe , Haruo Takaku , Tetsuhiro Ogino , Ayumu Kurimoto , Hajime Kawakami
发明人： Yoshiaki Isobe , Haruhisa Ogita , Masanori Tobe , Haruo Takaku , Tetsuhiro Ogino , Ayumu Kurimoto , Hajime Kawakami
IPC分类号： A61K31/52
CPC分类号： C07D473/00 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/34
摘要： This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): wherein X represents NR3 (wherein R3 represents a hydrogen atom or C1-3 alkyl) or the like; R1 represents substituted or unsubstituted alkyl or the like; R2 represents hydroxyl or the like; and Y represents a substituted or unsubstituted aromatic hetero ring or the like. Also, the present invention relates to pharmaceuticals such as an interferon inducer, antiviral agent, anticancer agent, type 2 helper T cell selective immune response inhibitor, antiallergic agent, and immune response modulator comprising the above derivative as an active ingredient.
摘要翻译：本发明涉及由通式（I）表示的腺嘌呤衍生物，其互变异构体或其药学上可接受的盐：其中X表示NR 3（其中R 3表示氢原子或C 1-3烷基）等; R 1表示取代或未取代的烷基等; R 2表示羟基等; Y表示取代或未取代的芳族杂环等。此外，本发明涉及包含上述衍生物作为活性成分的药物，例如干扰素诱导剂，抗病毒剂，抗癌剂，2型辅助T细胞选择性免疫应答抑制剂，抗过敏剂和免疫应答调节剂。

7. 发明授权

US06376501B1 Type 2 helper T cell-selective immune response suppressors 失效
标题翻译： 2型辅助性T细胞选择性免疫应答抑制剂
公开(公告)号：US06376501B1
公开(公告)日：2002-04-23
申请号：US09582176
申请日：2000-06-21
申请人： Yoshiaki Isobe , Haruhisa Ogita , Masanori Tobe , Haruo Takaku , Hiroyuki Matsui , Hideyuki Tomizawa
发明人： Yoshiaki Isobe , Haruhisa Ogita , Masanori Tobe , Haruo Takaku , Hiroyuki Matsui , Hideyuki Tomizawa
IPC分类号： A61K3152
CPC分类号： A61K31/522 , A61K31/52 , C07D473/00 , C07D473/34
摘要： The present invention relates to a type 2 helper T cell-selective immune response inhibitor, an immune response regulator and an anti-allergic agent, individually comprising, as an active ingredient, a purine derivative represented by General Formula (I): wherein R2 is hydrogen or a hydrocarbon group in which —CH2— not directly bound to the purine skeleton may be substituted by CO, SO2, O or S, and C—H not directly bound to the purine skeleton may be substituted by N, C-halogen or C—CN; R6 is hydroxyl, amino or amino which is mono- or di-substituted by a hydrocarbon group(s); R8 is hydroxyl, mercapto, acyloxy or hydrocarbon group-substituting oxycarbonyloxy; and R9 is a hydrocarbon group in which —CH2— not directly bound to the purine skeleton may be substituted by CO, SO2, O or S, and C—H not directly bound to the purine skeleton may be substituted by N, C-halogen or C—CN; or its tautomer or a salt of the purine derivative or the tautomer.
摘要翻译：本发明涉及一种2型辅助性T细胞选择性免疫应答抑制剂，免疫应答调节剂和抗过敏剂，其各自包含作为活性成分的由通式（I）表示的嘌呤衍生物：其中R 2为氢或其中不直接结合嘌呤骨架的-CH 2可以被CO，SO 2，O或S取代的烃基，并且不直接键合到嘌呤骨架上的CH可以被N，C-卤素或C-CN R6是羟基，被一个或多个烃基单取代或二取代的氨基或氨基; R8是羟基，巯基，酰氧基或烃基取代的氧羰基氧基; 并且R 9是其中不直接结合嘌呤骨架的-CH 2可以被CO，SO 2，O或S取代的烃基，并且不直接键合到嘌呤骨架上的CH可以被N，C-卤素或C- CN;或其互变异构体或嘌呤衍生物或互变异构体的盐。

8. 发明申请

US20090192153A1 NOVEL ADENINE COMPOUND 审中-公开
标题翻译：新颖的化合物
公开(公告)号：US20090192153A1
公开(公告)日：2009-07-30
申请号：US12067780
申请日：2006-09-21
申请人： Kazuki Hashimoto , Tomoaki Nakamura , Kei Nakamura , Ayumu Kurimoto , Yoshiaki Isobe , Haruhisa Ogita , Ian Millichip , Thomas Mcinally , Roger Bonnert
发明人： Kazuki Hashimoto , Tomoaki Nakamura , Kei Nakamura , Ayumu Kurimoto , Yoshiaki Isobe , Haruhisa Ogita , Ian Millichip , Thomas Mcinally , Roger Bonnert
IPC分类号： A61K31/5377 , C07D473/34 , A61K31/522 , A61P37/08
CPC分类号： C07D473/18
摘要： An adenine compound or its pharmaceutically acceptable salt as a medicament as shown following formula (1): wherein R1 is optionally substituted alkyl group, etc., X is oxygen atom, etc., A is 4 to 8 membered optionally substituted saturated or unsaturated heterocyclic group containing 1 to 2 hetero atoms selected from 1 to 3 nitrogen atoms, 0 to 1 oxygen atom and 0 to 1 sulfur atom, L1 and L2 are independently straight or branched chain alkylene, or a single bond, R2 is optionally substituted alkyl group, etc.
摘要翻译：腺嘌呤化合物或其药学上可接受的盐作为如下式（1）所示的药物：其中R 1是任选取代的烷基等，X是氧原子等，A是4至8元任选取代的饱和或不饱和杂环含有1至2个选自1至3个氮原子，0至1个氧原子和0至1个硫原子的杂原子的基团，L1和L2独立地为直链或支链亚烷基或单键，R2为任选取代的烷基，等等

9. 发明申请

US20070225303A1 8-Oxoadenine Compound 审中-公开
标题翻译： 8-氧基腺嘌呤化合物
公开(公告)号：US20070225303A1
公开(公告)日：2007-09-27
申请号：US10594074
申请日：2005-03-25
申请人： Haruhisa Ogita , Tomoaki Nakamura , Yoshiaki Isobe , Kazuki Hashimoto , Ayumu Kurimoto
发明人： Haruhisa Ogita , Tomoaki Nakamura , Yoshiaki Isobe , Kazuki Hashimoto , Ayumu Kurimoto
IPC分类号： A61K31/522 , C07D473/34
CPC分类号： C07D473/16 , A61K31/522 , A61K31/5377 , C07D473/18 , C07D473/24 , C07D473/34
摘要： An 8-oxoadenine compound useful as an immuno-modulator having specific activity against Th1/Th2, specifically a prophylactic and therapeutic agent for a topical application for allergic diseases, viral diseases and cancers, which is represented by the following formula (1): wherein A is a group of a formula represented by the formula (2): wherein R2 is a substituted or unsubstituted alkyl group and so on, R3 is hydrogen atom or an alkyl group, R is a halogen atom and so on, n is 0˜2, X1 is oxygen atom, Z is straight or branched chain alkylene, and R1 is an alkyl group which is optionally substituted by hydroxy group, an alkoxy group, alkoxycarbonyl group and so on, or its pharmaceutically acceptable salt.
摘要翻译：可用作对Th1 / Th2具有比活性的免疫调节剂的8-氧基腺嘌呤化合物，特别是用于过敏性疾病，病毒性疾病和癌症的局部应用的预防和治疗剂，其由下式（1）表示：其中 A是由式（2）表示的式的基团：其中R 2是取代或未取代的烷基等，R 3是氢原子或烷基，R为卤素原子等，n为0〜2，X 1为氧原子，Z为直链或支链亚烷基，R 1为任选被羟基，烷氧基，烷氧基羰基等取代的烷基或其药学上可接受的盐。

10. 发明授权

US06028076A Purine derivative 失效
标题翻译：嘌呤衍生物
公开(公告)号：US06028076A
公开(公告)日：2000-02-22
申请号：US29076
申请日：1998-03-03
申请人： Kohsaku Hirota , Yoshiaki Isobe , Nobuyoshi Chiba , Harumi Satoh , Haruo Takaku , Hiroyuki Matsui , Haruhisa Ogita
发明人： Kohsaku Hirota , Yoshiaki Isobe , Nobuyoshi Chiba , Harumi Satoh , Haruo Takaku , Hiroyuki Matsui , Haruhisa Ogita
IPC分类号： C07D473/00 , C07D473/30 , C07D473/34 , A61K31/52 , C07D473/38
CPC分类号： C07D473/00 , C07D473/30 , C07D473/34
摘要： This invention relates to novel purine derivatives of formula (I): ##STR1## where R.sup.2 and R.sup.9 are hydrocarbon groups, R.sup.6 is an amino group and R.sup.8 is a hydroxyl, or acyloxy group. These purine derivatives are effective at promoting secretion of interferon in patients, and can be used to treat diseases against which interferon is effective.
摘要翻译： PCT No.PCT / JP97 / 02310 Sec。 371日期1998年3月3日 102（e）1998年3月3日PCT PCT 1997年7月3日PCT公布。出版物WO98 / 01448 日本1998年1月15日本发明涉及式（I）的新型嘌呤衍生物：其中R2和R9为烃基，R6为氨基，R8为羟基或酰氧基。这些嘌呤衍生物有效促进患者的干扰素分泌，并可用于治疗干扰素有效的疾病。

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