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1. 发明授权

US08012964B2 9-substituted 8-oxoadenine compound 有权
标题翻译： 9-取代的8-氧代腺嘌呤化合物
公开(公告)号：US08012964B2
公开(公告)日：2011-09-06
申请号：US10593691
申请日：2005-03-24
申请人： Ayumu Kurimoto , Yoshiaki Isobe , Stephen Brough , Hiroki Wada , Roger Bonnert , Thomas McInally
发明人： Ayumu Kurimoto , Yoshiaki Isobe , Stephen Brough , Hiroki Wada , Roger Bonnert , Thomas McInally
IPC分类号： C07D473/18 , A61K31/522 , A61P37/06 , A61P37/08 , A61P11/06
CPC分类号： C07D473/18 , A61K31/522 , A61K31/5377
摘要： The present invention provides an 8-oxoadenine compound having immunemodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1): [wherein the ring A represents a 6-10 membered aromatic carbocyclic ring and the like, R represents a halogen atom, an alkyl group and the like, n represents an integer of 0-2, Z1 represents alkylene, X2 represents oxygen atom, sulfur atom, SO2, NR5, CO, CONR5, NR5CO and the like, Y1, Y2 and Y3 represent independently a single bond or an alkylene group, X1 represents oxygen atom, sulfur atom, NR4 (R4 is hydrogen atom or an alkyl group) or a single bond, R2 represents a substituted or unsubstituted alkyl group, R1 represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group] or its pharmaceutically acceptable salt.
摘要翻译：本发明提供具有免疫调节活性的8-氧代腺嘌呤化合物，例如干扰素诱导活性，可用作抗病毒剂和抗变应性剂，其由下式（1）表示：[其中环A表示6-10元芳香族碳环等，R表示卤素原子，烷基等，n表示0-2的整数，Z1表示亚烷基，X2表示氧原子，硫原子，SO2，NR5，CO，CONR5，NR5CO 等等，Y1，Y2和Y3独立地表示单键或亚烷基，X1表示氧原子，硫原子，NR4（R4是氢原子或烷基）或单键，R2表示取代或未取代的烷基基团，R 1表示氢原子，羟基，烷氧基，烷氧基羰基或卤代烷基]或其药学上可接受的盐。

2. 发明申请

US20110054168A1 METHOD FOR PREPARING ADENINE COMPOUND 审中-公开
标题翻译：制备腺嘌呤化合物的方法
公开(公告)号：US20110054168A1
公开(公告)日：2011-03-03
申请号：US12863297
申请日：2009-01-16
申请人： Ayumu Kurimoto , Wataru Katoda , Kazuki Hashimoto , Kazuhiko Takashi
发明人： Ayumu Kurimoto , Wataru Katoda , Kazuki Hashimoto , Kazuhiko Takashi
IPC分类号： C07D473/18
CPC分类号： C07D473/18
摘要： A method for preparing compound (4): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, thiomorpholine, etc., and R4 is C1-3 alkyl group, or a pharmaceutically acceptable salt, which is useful as a medicament, which comprises step (a) for preparing compound (2): wherein m, n, R1, R2 and R3 are the same as defined above, or its salt which comprises subjecting compound (1): wherein k is an integer of 1 or 2, R is hydrogen atom, halogen atom, etc., or a salt thereof to debenzylation reaction, and then step (b) for preparing compound (4) or a pharmaceutically acceptable salt which comprises reacting compound (2) or its salt prepared in the above step (a) or salt thereof and compound (3): wherein R4 is C1-3 alkyl group, in the presence of a boron-containing reducing agent.
摘要翻译：一种制备化合物（4）的方法：其中m和n独立地为2至5的整数，R 1为C 1-6烷基，R 2和R 3与相邻的氮原子结合形成吡咯烷，吗啉，硫代吗啉等。，和R4为C1-3烷基，或其药学上可接受的盐，其可用作药物，其包含用于制备化合物（2）的步骤（a）：其中m，n，R 1，R 2和R 3相同或其盐，其包括使化合物（1）：其中k为1或2的整数，R为氢原子，卤素原子等或其盐进行脱苄基化反应，然后步骤（b）为制备化合物（4）或其药学上可接受的盐，其包括使上述步骤（a）中制备的化合物（2）或其盐或其盐与化合物（3）反应：其中R 4为C 1-3烷基，在含硼还原剂。

3. 发明申请

US20100256118A1 NOVEL ADENINE COMPOUND AND USE THEREOF 失效
标题翻译：新颖的化合物及其用途
公开(公告)号：US20100256118A1
公开(公告)日：2010-10-07
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： A61K31/52 , C07D473/18 , A61K31/5377 , C07D473/24 , C07D473/16 , A61K31/55 , A61P11/06 , A61P17/00 , A61P37/02
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。

4. 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

5. 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。

6. 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。

7. 发明授权

US06329381B1 Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US06329381B1
公开(公告)日：2001-12-11
申请号：US09555292
申请日：2000-05-26
申请人： Ayumu Kurimoto , Tetsuhiro Ogino , Hajime Kawakami
发明人： Ayumu Kurimoto , Tetsuhiro Ogino , Hajime Kawakami
IPC分类号： C07D47316
CPC分类号： C07D473/24 , C07D473/16 , C07D473/18
摘要： The present invention relates to a heterocyclic compound of the following general formula (I): wherein X is sulfur atom, oxygen atom or —NR3— (R3 may form a heterocyclic ring or a substituted heterocyclic ring with R1 via the nitrogen atom), R1 is alkyl group, substituted alkyl group, aryl group, substituted aryl group, heterocyclic group or substituted heterocyclic group, and R2 is hydrogen atom, halogen atom etc.; or its pharmaceutically acceptable salt and interferon inducers, antiviral agents, anticancer agents and therapeutic agents for immunologic diseases comprising the compound (I) or its pharmaceutically acceptable salt as active ingredients.
摘要翻译：本发明涉及以下通式（I）的杂环化合物：其中X是硫原子，氧原子或-NR 3 - （R 3可以通过氮原子与R 1形成杂环或取代的杂环），R 1 是烷基，取代的烷基，芳基，取代的芳基，杂环基或取代的杂环基，R 2是氢原子，卤素原子等;或其药学上可接受的盐和干扰素诱导剂，抗病毒剂，抗癌剂和治疗剂包含化合物（I）或其药学上可接受的盐作为活性成分的免疫疾病。

8. 发明授权

US08865896B2 Method for preparing adenine compound 有权
标题翻译：制备腺嘌呤化合物的方法
公开(公告)号：US08865896B2
公开(公告)日：2014-10-21
申请号：US12863291
申请日：2009-01-16
申请人： Kazuki Hashimoto , Wataru Katoda , Kazuhiko Takahashi , Ayumu Kurimoto
发明人： Kazuki Hashimoto , Wataru Katoda , Kazuhiko Takahashi , Ayumu Kurimoto
IPC分类号： C07D473/02 , C07D413/14 , C07D473/18
CPC分类号： C07D473/18
摘要： A method for producing adenine compound (1): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are the same or different, and hydrogen atom, or C1-6 alkyl group, or R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R4 is C1-3 alkyl group, which comprises a step of reacting compound (2): and compound (3): in the presence of a boron-containing reducing agent.
摘要翻译：一种腺嘌呤化合物（1）的制造方法，其中m和n分别为2〜5的整数，R1为C1-6烷基，R2和R3相同或不同，氢原子或C1-6烷基，或R2和R3与相邻的氮原子结合形成吡咯烷，吗啉，哌啶，哌嗪等，R4为C1-3烷基，其包括使化合物（2）与化合物（3）反应的步骤：：在含硼还原剂的存在下。

9. 发明申请

US20120178743A1 NOVEL ADENINE COMPOUND AND USE THEREOF 审中-公开
标题翻译：新颖的化合物及其用途
公开(公告)号：US20120178743A1
公开(公告)日：2012-07-12
申请号：US13402850
申请日：2012-02-22
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 , A61K31/5377 , A61P37/08 , A61P37/00 , A61P31/12 , A61P17/00 , C07D473/18 , A61K31/55
CPC分类号： A61K31/5377 , A61K31/522 , A61K31/55
摘要： An antiallergic agent for topical administration containing an adenine compound of 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：一种用于局部给药的抗过敏剂，其含有通式（1）的腺嘌呤化合物：[其中环A表示6至10元，单或双环，芳烃或5至10元单或双环芳族杂环，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3个杂原子; 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。

10. 发明申请

US20110046369A1 METHOD FOR PREPARING ADENINE COMPOUND 有权
标题翻译：制备腺嘌呤化合物的方法
公开(公告)号：US20110046369A1
公开(公告)日：2011-02-24
申请号：US12863291
申请日：2009-01-16
申请人： Kazuki Hashimoto , Wataru Katoda , Kazuhiko Takahashi , Ayumu Kurimoto
发明人： Kazuki Hashimoto , Wataru Katoda , Kazuhiko Takahashi , Ayumu Kurimoto
IPC分类号： C07D473/18
CPC分类号： C07D473/18
摘要： A method for producing adenine compound (1): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are the same or different, and hydrogen atom, or C1-6 alkyl group, or R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R4 is C1-3 alkyl group, which comprises a step of reacting compound (2): and compound (3): in the presence of a boron-containing reducing agent.
摘要翻译：一种腺嘌呤化合物（1）的制造方法，其中m和n分别为2〜5的整数，R1为C1-6烷基，R2和R3相同或不同，氢原子或C1-6烷基，或R2和R3与相邻的氮原子结合形成吡咯烷，吗啉，哌啶，哌嗪等，R4为C1-3烷基，其包括使化合物（2）与化合物（3）反应的步骤：：在含硼还原剂的存在下。

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