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11. 发明申请

US20060094737A1 Novel uracil derivatives and medicinal use thereof 审中-公开
标题翻译：新型尿嘧啶衍生物及其药用
公开(公告)号：US20060094737A1
公开(公告)日：2006-05-04
申请号：US10528373
申请日：2003-09-17
申请人： Yoshiaki Isobe , Masanori Tobe , Yoshifumi Inoue , Masakazu Isobe
发明人： Yoshiaki Isobe , Masanori Tobe , Yoshifumi Inoue , Masakazu Isobe
IPC分类号： A61K31/513 , C07D405/02 , C07D239/54
CPC分类号： C07D239/545 , A61K31/513 , C07D405/06 , C07D405/12 , C07D405/14
摘要： It is intended to provide an uracil derivative represented by the following general formula (I): (I) wherein X represents a group selected from among NHCO, NHCH2, CO, CONH and CH2NH; R1 represents hydrogen or optionally substituted C1-6 alkyl; R2 represents a group of the following general formula (II) or (III): (II) (III) (wherein m is 0 or 1; n is an integer of from 1 to 3; Y represents OH or NH2; and a dotted line shows a binding position), provided that when R2 is a group of the general formula (III), X represents NHCO or NHCH2; R3 and R4 independently represent each hydrogen or C1-6 alkyl; and Ar represents phenyl substituted by C1-6 alkyl at the o- and m-positions, optionally substituted heteroaryl or a bicyclic aromatic group; its pharmaceutically acceptable salt, and a remedy containing the above uracil derivative or its pharmaceutically acceptable salt as the active ingredient for, in particular, allergic diseases relating to a type IV allergic reaction, i.e., a novel compound useful in treating diseases in which a type IV allergic reaction participates and a remedy for allergic diseases containing the same as the active ingredient.
摘要翻译：旨在提供由以下通式（I）表示的尿嘧啶衍生物：（I）其中X表示选自NHCO，NHCH 2，CO，CONH和CH 2的基团 NH; R 1表示氢或任选取代的C 1-6烷基; R 2表示下述通式（II）或（III）的基团：（II）（III）（其中m为0或1; n为1至3的整数; Y 表示OH或NH 2，虚线表示结合位置），条件是当R 2为通式（III）的基团时，X表示NHCO或 NHCH 2

12. 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。

13. 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。

14. 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：

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