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公开(公告)号：US11291681B2
公开(公告)日：2022-04-05
申请号：US17003191
申请日：2020-08-26
发明人： Pnina Fishman , Shira Cohen
IPC分类号： A61K31/7076 , A61P1/16 , A61K9/00
摘要： Provided is an A3AR ligand for reducing ectopic fat accumulation, particularly in fatty liver. Further provided is the use of A3AR ligand for the preparation of a pharmaceutical composition for reducing such fat accumulation, method of treating a condition associates with fat accumulation making use of the ligand and kits including pharmaceutical compositions including the ligand, and instructions for use of same, for treating a condition associated with ectopic fat accumulation. Further provided is the use of an A3AR agonist, such as 2-Chloro-N6-(3-iodobenzyl)-adenosine-5′-N-methyluronamide (CI-IB-MECA, CF102) for treating fatty liver, specifically, non-alcoholic fatty liver disease (NAFLD).
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公开(公告)号：US10265337B2
公开(公告)日：2019-04-23
申请号：US15160462
申请日：2016-05-20
发明人： Pnina Fishman
IPC分类号： A01N43/04 , A61K31/70 , A61K31/7076 , A61K31/00 , A61K31/519 , A61K9/00 , A61K31/706 , A61K45/06
摘要： Provided is an A3 adenosine receptor agonist (A3AR agonist) for the preparation of a pharmaceutical composition for the treatment of a mammal subject having osteoarthritis (OA), as well as to a method for the treatment of OA in a mammal subject, the method includes administering to said subject in need of said treatment an amount of A3AR agonist, the amount being effective to treat or prevent the development of OA. Preferred but not exclusive A3AR agonists in accordance with the present subject matter are IB-MECA and Cl-IB-MECA. The A3AR agonist may be administered in combination with another drug, such as Methotrexate (MTX). Also provided are pharmaceutical compositions for treatment of osteoarthritis including an amount of an A3AR agonist.
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公开(公告)号：US20040137477A1
公开(公告)日：2004-07-15
申请号：US10689550
申请日：2003-10-21
发明人： Pnina Fishman , Lea Madi , Sara Bar Yehuda
IPC分类号： C12Q001/68 , G01N033/574
CPC分类号： G01N33/57484 , G01N2333/726
摘要： The invention concerns a method of detecting a disease, for example cancer, by determining a change in the expression level of the A3 adenosine receptor as compared to the expression level in a non-diseased control.
摘要翻译： 本发明涉及一种通过与非病变对照中的表达水平相比，通过确定A3腺苷受体的表达水平的变化来检测疾病，例如癌症的方法。
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4.发明申请C2,5'-disubstituted and N6,C2,5'-trisubstituted adenosine derivatives and pharmaceutical compositions containing them 失效C2,5'-二取代的和N6，C2,5'-三取代的腺苷衍生物和含有它们的药物组合物公开(公告)号：US20040127452A1
公开(公告)日：2004-07-01
申请号：US10653464
申请日：2003-09-03
发明人： Erica Van Tilburg , Ad Ijzerman
IPC分类号： A61K031/7076 , C07H019/16
CPC分类号： C07H19/16
摘要： The present invention concerns novel C2,5null-disubstituted and N6,C2,5null-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adenosine receptor agonists and thus are of a therapeutic value in the treatment and prophylaxis of diseases and disorders affected by adenosine receptor agonists.
摘要翻译： 本发明涉及新的C2,5'-二取代和N6，C2,5'-三取代的腺苷衍生物及其不同用途。 发现这些腺苷衍生物是有效的腺苷受体激动剂，因此在治疗和预防受腺苷受体激动剂影响的疾病和病症方面具有治疗价值。
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公开(公告)号：US20230049415A1
公开(公告)日：2023-02-16
申请号：US17758920
申请日：2021-01-14
发明人： Pnina FISHMAN , Inbal ITZHAK
IPC分类号： A61K36/185 , A61K31/352 , A61K31/05 , A61K31/60
摘要： Cannabinoids are used to treat diseases or disorders treatable by an activator of the A3 adenosine receptor (A3AR). The cannabinoid effect is exerted through the A3AR. The cannabinoids may be selected from natural, phytocannabinoids, synthetic derivatives of phytocannabinoids, extracts of cannabis plant, and others.
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6.发明授权公开(公告)号：US09549943B2
公开(公告)日：2017-01-24
申请号：US14420439
申请日：2013-08-08
发明人： Pnina Fishman
IPC分类号： A61K31/4745 , A61K31/7076
CPC分类号： A61K31/7076 , A61K31/4745
摘要： The present disclosure provides an A3 adenosine receptor (A3AR) ligand for the treatment of sexual dysfunction. In some embodiments the A3AR ligand is selected from an A3AR agonist and A3AR allosteric enhancer. The present disclosure also provides a method a method and pharmaceutical composition for treating a sexual dysfunction, the method comprises administering to a subject having the sexual dysfunction an amount of an A3 adenosine receptor (A3AR) ligand. In some embodiments, the A3AR ligand is an A3AR agonist and more specifically, IB-MECA.
摘要翻译： 本公开提供了用于治疗性功能障碍的A3腺苷受体（A3AR）配体。 在一些实施方案中，A3AR配体选自A3AR激动剂和A3AR变构增强子。 本公开还提供了用于治疗性功能障碍的方法和药物组合物的方法，所述方法包括向具有性功能障碍的受试者施用一定量的A3腺苷受体（A3AR）配体。 在一些实施方案中，A3AR配体是A3AR激动剂，更具体地，IB-MECA。
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公开(公告)号：US10780106B2
公开(公告)日：2020-09-22
申请号：US15986332
申请日：2018-05-22
发明人： Pnina Fishman , Shira Cohen
IPC分类号： A61K31/7076 , A61P1/16 , A61K9/00
摘要： Provided is an A3AR ligand for reducing ectopic fat accumulation, particularly in fatty liver. Further provided is the use of A3AR ligand for the preparation of a pharmaceutical composition for reducing such fat accumulation, method of treating a condition associates with fat accumulation making use of the ligand and kits including pharmaceutical compositions including the ligand, and instructions for use of same, for treating a condition associated with ectopic fat accumulation. Further provided is the use of an A3AR agonist, such as 2-Chloro-N6-(3-iodobenzyl)-adenosine-5′-N-methyluronamide (Cl-IB-MECA, CF102) for treating fatty liver, specifically, non-alcoholic fatty liver disease (NAFLD).
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公开(公告)号：US20130345163A1
公开(公告)日：2013-12-26
申请号：US13973595
申请日：2013-08-22
发明人： Pnina FISHMAN , Sara BAR-YEHUDA , Lea MADI
IPC分类号： G01N33/68 , A61K31/7076
CPC分类号： G01N33/6872 , A61K31/7076 , G01N33/564 , G01N2800/52
摘要： Inflammatory state in a subject is assayed by determining the level of expression of A3 adenosine receptor (A3AR) in white blood cells (WBC), e.g. circulating WBCs, from the subject. A high level of expression of A3AR is indicative of an inflammatory state in the subject. This assay can be used for determining whether a patient known to have an inflammatory state should be treated with an A3AR agonist to reduce the inflammatory state. The patient will be so treated only if the level of A3AR in the WBC of the subject is above a predefined threshold, which is about twice the level of A3AR in WBC of healthy subjects. The inflammatory state may particularly be rheumatoid arthritis or uveitis.
摘要翻译： 通过测定白细胞（WBC）中的A3腺苷受体（A3AR）的表达水平来测定受试者的炎症状态。 流通WBC，从主题。 A3AR的高水平表达表明受试者的炎症状态。 该测定可以用于确定是否应该用A3AR激动剂治疗已知具有炎性状态的患者以减少炎症状态。 只有当受试者的白细胞中的A3AR水平高于预定阈值时，患者才会受到治疗，这是健康受试者的白细胞计数值的三倍。 炎症状态可能特别是类风湿性关节炎或葡萄膜炎。
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9.发明申请USE OF A3 ADENOSINE RECEPTOR AGONIST IN OSTEOARTHRITIS TREATMENT 审中-公开A3腺苷受体激动剂在OSTEOARTHRITIS治疗中的应用公开(公告)号：US20160263142A1
公开(公告)日：2016-09-15
申请号：US15160462
申请日：2016-05-20
发明人： Pnina FISHMAN
IPC分类号： A61K31/7076 , A61K31/519 , A61K31/706 , A61K9/00 , A61K45/06
CPC分类号： A61K31/7076 , A61K9/0053 , A61K31/00 , A61K31/519 , A61K31/706 , A61K45/06 , A61K2300/00
摘要： Provided is an A3 adenosine receptor agonist (A3AR agonist) for the preparation of a pharmaceutical composition for the treatment of a mammal subject having osteoarthritis (OA), as well as to a method for the treatment of OA in a mammal subject, the method includes administering to said subject in need of said treatment an amount of A3AR agonist, the amount being effective to treat or prevent the development of OA. Preferred but not exclusive A3AR agonists in accordance with the present subject matter are IB-MECA and Cl-IB-MECA. The A3AR agonist may be administered in combination with another drug, such as Methotrexate (MTX). Also provided are pharmaceutical compositions for treatment of osteoarthritis including an amount of an A3AR agonist.
摘要翻译： 本发明提供了用于制备用于治疗患有骨关节炎（OA）的哺乳动物受试者的药物组合物的A3腺苷受体激动剂（A3AR激动剂）以及哺乳动物受试者中OA治疗方法， 对需要所述治疗的所述受试者施用一定量的有效治疗或预防OA发展的量的A3AR激动剂。 根据本主题的优选但不排他的A3AR激动剂是IB-MECA和Cl-IB-MECA。 A3AR激动剂可以与另一种药物如甲氨蝶呤（MTX）组合施用。 还提供了用于治疗骨关节炎的药物组合物，其包括一定量的A3AR激动剂。
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公开(公告)号：US20140364388A1
公开(公告)日：2014-12-11
申请号：US14464970
申请日：2014-08-21
发明人： Pnina FISHMAN , Shira COHEN
IPC分类号： A61K31/7076
CPC分类号： A61K31/7076 , A61K31/52 , A61K31/522
摘要： The present application provides methods and compositions for inducing hepatocyte proliferation and liver regeneration, the latter being mainly dependent on hepatocyte proliferation even if all the other cell types divide to reconstitute the organ specific-lobular-architecture. The methods and compositions provided herein make use of an A3AR agonist. A preferred A3AR agonist disclosed herein is Cl-IB-MECA.
摘要翻译： 本申请提供诱导肝细胞增殖和肝再生的方法和组合物，后者主要依赖于肝细胞增殖，即使所有其他细胞类型分裂以重建器官特异性小叶结构。 本文提供的方法和组合物使用A3AR激动剂。 本文公开的优选的A3AR激动剂是Cl-IB-MECA。
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