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1. 发明申请

US20090054476A1 A3 Adenosine receptor allosteric modulators 有权
标题翻译： A3腺苷受体变构调节剂
公开(公告)号：US20090054476A1
公开(公告)日：2009-02-26
申请号：US12219772
申请日：2008-07-28
申请人： Aniko Goblyos , Johannes Brussee , Adriaan P. Ijzerman , Zhan-Guo Gao , Kenneth Jacobson
发明人： Aniko Goblyos , Johannes Brussee , Adriaan P. Ijzerman , Zhan-Guo Gao , Kenneth Jacobson
IPC分类号： A61K31/4745 , C07D471/04
CPC分类号： A61K31/4745 , A61K31/00 , C07D471/04
摘要： The present invention relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions comprising the same and therapeutic methods comprising administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to the invention are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. The invention also provides some of such novel 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.
摘要翻译：本发明涉及A3腺苷受体（A3AR）的变构调节，并提供使用A3腺苷受体调节剂（A3RM），用于制备用于调节受试者中的A3AR的药物组合物，以及包含相同和治疗方法包括向受试者施用一定量的有效调节A3AR活性的量的A3RM。根据本发明的A3RM是1H-咪唑并[4,5-c]喹啉-4-胺衍生物。本发明还提供了一些这样的新颖的1H-咪唑并〔4,5-c〕喹啉-4-胺衍生物。

2. 发明授权

US07135568B2 Substituted pyrazolopyrimidines and thiazolopyrimidines 失效
标题翻译：取代的吡唑并嘧啶和噻唑并嘧啶
公开(公告)号：US07135568B2
公开(公告)日：2006-11-14
申请号：US10660794
申请日：2003-09-12
申请人： Matthias Gerlach , Corrinna Sundermann , Utz-Peter Jagusch , Bernd Sundermann , Martin Fuhr , Adriaan P. Ijzerman , Miriam Dissen-De Groote
发明人： Matthias Gerlach , Corrinna Sundermann , Utz-Peter Jagusch , Bernd Sundermann , Martin Fuhr , Adriaan P. Ijzerman , Miriam Dissen-De Groote
IPC分类号： C07D471/04 , C07D513/04 , A61K31/519 , A61P25/04 , A61P25/28
CPC分类号： C07D487/04 , C07D513/04
摘要： Substituted pyrazolopyrimidines and thiazolopyrimidines, specifically, compounds corresponding to the structure (I A), (I B) or (II) processes for their preparation, substance libraries containing them, pharmaceutical formulations containing these compounds, the use of these compounds for the production of medicaments for the treatment and/or prophylaxis of pain and related treatment methods are provided.
摘要翻译：取代的吡唑并嘧啶和噻唑并嘧啶，具体地，对应于结构（IA），（IB）或（II）的制备方法，含有它们的物质文库，含有这些化合物的药物制剂，使用这些化合物用于制备药物提供了治疗和/或预防疼痛和相关治疗方法。

3. 发明申请

US20110144156A1 A3 ADENOSINE RECEPTOR ALLOSTERIC MODULATORS 审中-公开
标题翻译： A3腺苷受体免疫调节剂
公开(公告)号：US20110144156A1
公开(公告)日：2011-06-16
申请号：US13059836
申请日：2009-08-12
申请人： Adriaan P. Ijzerman , Aniko Goblyos , Johannes Brussee
发明人： Adriaan P. Ijzerman , Aniko Goblyos , Johannes Brussee
IPC分类号： A61K31/4709 , A61K31/47 , C07D215/38 , A61P35/00
CPC分类号： A61K31/4709 , C07D215/38 , C07D215/42 , C07D405/12
摘要： Provided are 2,4-disubstituted quinoline derivatives that are A3 adenosine receptor modulators (A3RM), for use in the treatment of a condition which is treatable by adenosine, an A3 adenosine receptor (A3AR) agonist, or an A3 adenosine receptor antagonist. The 2,4-disubstituted quinoline derivatives can be used in the treatment of a condition treatable by an adenosine or an A3AR agonist, by enhancing activity of a protein (by binding of said 2,4-disubstituted quinoline derivative to the A3AR). Some conditions treatable by the 2,4-disubstituted quinoline derivative when used for enhancing activity include, malignancy, an immuno-compromised affliction, high intraocular pressure, or a condition associated with high intraocular pressure. Further provided is a method for treatment of a subject having a condition treatable by adenosine, an A3AR agonist, or an A3AR antagonist making use of the defined 2,4-disubstituted quinoline derivative (s), and pharmaceutical composition and comprising said derivative and a kit comprising the derivative and instructions for use thereof. One specific 2,4-disubstituted quinoline derivative includes N-{2-[(3,4-dichlorophenyl)amino]quinolin-4-yl}cyclohexanecarboxamide. The 2,4-disubstituted quinoline derivatives can be formulated in a form suitable for oral administration.
摘要翻译：提供作为可用腺苷，A3腺苷受体（A3AR）激动剂或A3腺苷受体拮抗剂治疗的病症的A3腺苷受体调节剂（A3RM）的2,4-二取代喹啉衍生物。 2,4-二取代喹啉衍生物可用于通过增强蛋白质的活性（通过将所述2,4-二取代喹啉衍生物与A3AR结合）来治疗由腺苷或A3AR激动剂可治疗的病症。当用于增强活性时，2,4-二取代喹啉衍生物可治疗的一些病症包括恶性肿瘤，免疫受损的痛苦，高眼内压或与高眼内压相关的病症。还提供了一种用于治疗具有可由腺苷治疗的病症的受试者的方法，使用所定义的2,4-二取代喹啉衍生物的A3AR激动剂或A3AR拮抗剂，以及包含所述衍生物和包含衍生物的试剂盒和使用说明书。一种特定的2,4-二取代喹啉衍生物包括N- {2 - [（3,4-二氯苯基）氨基]喹啉-4-基}环己烷甲酰胺。 2,4-二取代喹啉衍生物可以配制成适于口服给药的形式。

4. 发明申请

US20130197025A1 A3 ADENOSINE RECEPTOR ALLOSTERIC MODULATORS 审中-公开
标题翻译： A3腺苷受体免疫调节剂
公开(公告)号：US20130197025A1
公开(公告)日：2013-08-01
申请号：US13800560
申请日：2013-03-13
申请人： Anikó GÖBLYÖS , Johannes BRUSSEE , Adriaan P. IJZERMAN , Zhan-Guo GAO , Kenneth JACOBSON
发明人： Anikó GÖBLYÖS , Johannes BRUSSEE , Adriaan P. IJZERMAN , Zhan-Guo GAO , Kenneth JACOBSON
IPC分类号： A61K31/4745
CPC分类号： A61K31/4745 , A61K31/00 , C07D471/04
摘要： The claimed subject matter relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions including the same and therapeutic methods including administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to claimed subject matter are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. Also provided are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.
摘要翻译：所要求保护的主题涉及A3腺苷受体（A3AR）的变构调节并提供使用A3腺苷受体调节剂（A3RM）用于制备用于调节受试者中的A3AR的药物组合物，以及药物组合物，包括相同和治疗方法，包括向受试者施用一定量的有效调节A3AR活性的量的A3RM。根据要求保护的主题的A3RM是1H-咪唑并[4,5-c]喹啉-4-胺衍生物。还提供了1H-咪唑并[4,5-c]喹啉-4-胺衍生物。

5. 发明授权

US08420664B2 A3 adenosine receptor allosteric modulators 有权
标题翻译： A3腺苷受体变构调节剂
公开(公告)号：US08420664B2
公开(公告)日：2013-04-16
申请号：US12219772
申请日：2008-07-28
申请人： Aniko Goblyos , Johannes Brussee , Adriaan P. Ijzerman , Zhan-Guo Gao , Kenneth Jacobson
发明人： Aniko Goblyos , Johannes Brussee , Adriaan P. Ijzerman , Zhan-Guo Gao , Kenneth Jacobson
IPC分类号： A61K31/4745 , C07D471/04
CPC分类号： A61K31/4745 , A61K31/00 , C07D471/04
摘要： The present invention relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions comprising the same and therapeutic methods comprising administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to the invention are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. The invention also provides some of such novel 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.
摘要翻译：本发明涉及A3腺苷受体（A3AR）的变构调节，并提供使用A3腺苷受体调节剂（A3RM），用于制备用于调节受试者中的A3AR的药物组合物，以及包含相同和治疗方法包括向受试者施用一定量的有效调节A3AR活性的量的A3RM。根据本发明的A3RM是1H-咪唑并[4,5-c]喹啉-4-胺衍生物。本发明还提供了一些这样的新颖的1H-咪唑并〔4,5-c〕喹啉-4-胺衍生物。

6. 发明授权

US09326978B2 A3 adenosine receptor allosteric modulators 有权
标题翻译： A3腺苷受体变构调节剂
公开(公告)号：US09326978B2
公开(公告)日：2016-05-03
申请号：US13800560
申请日：2013-03-13
申请人： Anikó Göblyös , Johannes Brussee , Adriaan P. Ijzerman , Zhan-Guo Gao , Kenneth Jacobson
发明人： Anikó Göblyös , Johannes Brussee , Adriaan P. Ijzerman , Zhan-Guo Gao , Kenneth Jacobson
IPC分类号： A61K31/4745 , A61K31/00 , C07D471/04
CPC分类号： A61K31/4745 , A61K31/00 , C07D471/04
摘要： The claimed subject matter relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions including the same and therapeutic methods including administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to claimed subject matter are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. Also provided are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.
摘要翻译：所要求保护的主题涉及A3腺苷受体（A3AR）的变构调节并提供使用A3腺苷受体调节剂（A3RM）用于制备用于调节受试者中的A3AR的药物组合物，以及药物组合物，包括相同和治疗方法，包括向受试者施用一定量的有效调节A3AR活性的量的A3RM。根据要求保护的主题的A3RM是1H-咪唑并[4,5-c]喹啉-4-胺衍生物。还提供了1H-咪唑并[4,5-c]喹啉-4-胺衍生物。

7. 发明授权

US07449470B2 Substituted pyrimidines as ligands of adenosine receptors 失效
标题翻译：取代的嘧啶作为腺苷受体的配体
公开(公告)号：US07449470B2
公开(公告)日：2008-11-11
申请号：US10574436
申请日：2004-10-01
申请人： Lisa Chung Wai Chang , Adriaan P. Ijzerman , Johannes Brussee
发明人： Lisa Chung Wai Chang , Adriaan P. Ijzerman , Johannes Brussee
IPC分类号： C07D239/42 , A61K31/505 , A61P9/00 , A61P11/00 , A61P25/00 , A61P35/00
CPC分类号： C07D239/42
摘要： The invention provides a compound of formula (I) wherein R and R′ are selected from hydrogen, alkyl, alkenyl, alkynyl, or aryl; R″ and R′″ are selected from hydrogen, acyl, thio-acyl, seleno-acyl, alkyl, alkenyl, alkynyl, or aryl; or a pharmaceutically acceptable salt thereof, to interact with the adenosine receptors in the beneficial treatment and/or prevention of a (dis)order arising from the said receptors. The invention further provides pharmaceutical compositions comprising said compounds. The invention also relates to the use of said compositions for treating an/or preventing a variety of diseases.
摘要翻译：本发明提供式（I）化合物，其中R和R'选自氢，烷基，烯基，炔基或芳基; R“和R”'选自氢，酰基，硫代酰基，硒酰基，烷基，烯基，炔基或芳基; 或其药学上可接受的盐在有益治疗和/或预防由所述受体产生的（dis）顺序的情况下与腺苷受体相互作用。本发明还提供包含所述化合物的药物组合物。本发明还涉及所述组合物用于治疗/或预防各种疾病的用途。

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