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公开(公告)号：US08420664B2
公开(公告)日：2013-04-16
申请号：US12219772
申请日：2008-07-28
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。
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公开(公告)号：US20090054476A1
公开(公告)日：2009-02-26
申请号：US12219772
申请日：2008-07-28
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。
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公开(公告)号：US20110144156A1
公开(公告)日：2011-06-16
申请号：US13059836
申请日：2009-08-12
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。
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