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1. 发明申请

WO2022067100A2 PLK1 POLO BOX DOMAIN INHIBITORS AND METHOD OF TREATING CANCER 审中-公开
公开(公告)号：WO2022067100A2
公开(公告)日：2022-03-31
申请号：PCT/US2021/052054
申请日：2021-09-24
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , LEE, Kyung, S. , JACOBSON, Kenneth, A. , ALVEREZ, Celeste, N. , PARK, Jung-Eun , OLIVA, Paola , LEE, Hobin , PONGORNE KIRSCH, Klara
发明人： LEE, Kyung, S. , JACOBSON, Kenneth, A. , ALVEREZ, Celeste, N. , PARK, Jung-Eun , OLIVA, Paola , LEE, Hobin , PONGORNE KIRSCH, Klara
IPC分类号： A61K31/519 , A61P35/00
摘要： Provided is a method of treating cancer, particularly cancers associated with an overexpression of polo-like kinase (Plk1), comprising administering a compound of formula (I) or a pharmaceutically acceptable salt thereof in which ring A, X1, X2, X3, X4, X5, R2, R3, R4, n, bond a, and bond b are described herein. Exemplary compounds of formula (I) and pharmaceutically acceptable salts thereof, especially those that selectively inhibit the polo box domain of Plk1, also are provided.

2. 发明申请

WO2011103552A3 AMP DERIVATIVES FOR TREATING CARDIAC DISEASES 审中-公开
公开(公告)号：WO2011103552A3
公开(公告)日：2011-08-25
申请号：PCT/US2011/025680
申请日：2011-02-22
申请人： UNIVERSITY OF CONNECTICUT , THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , LIANG, Bruce , JACOBSON, Kenneth A. , JOSHI, Bhalchandra V. , KUMAR, Thatikonda Santhosh
发明人： LIANG, Bruce , JACOBSON, Kenneth A. , JOSHI, Bhalchandra V. , KUMAR, Thatikonda Santhosh
IPC分类号： C07F9/6561 , A61K31/675 , A61P9/04
摘要： Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)- methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C-P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded.

3. 发明申请

WO2010014921A2 A3 ADENOSINE RECEPTOR ANTAGONISTS AND PARTIAL AGONISTS 审中-公开
标题翻译： A3腺苷受体拮抗剂和部分激动剂
公开(公告)号：WO2010014921A2
公开(公告)日：2010-02-04
申请号：PCT/US2009/052439
申请日：2009-07-31
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , JACOBSON, Kenneth, A. , MELMAN, Artem , WANG, Ben, Bih-Ren
发明人： JACOBSON, Kenneth, A. , MELMAN, Artem , WANG, Ben, Bih-Ren
CPC分类号： C07D473/34
摘要： Disclosed are A 3 adenosine receptor antagonists and/or partial agonists of formula (I): wherein R 1 to R 5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The antagonists or partial agonists find use in treating a number of diseases including cancer, glaucoma, inflammatory diseases, asthma, stroke, myocardial infarction, allergic reactions, rhinitis, poison ivy induced responses, urticaria, scleroderma, arthritis, brain arteriole diameter constriction, bronchoconstriction, and myocardial ischemia, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs.
摘要翻译：公开了式（I）的A 3 - 腺苷受体拮抗剂和/或部分激动剂：其中R 1至R 5各自独立地选自：如本文所述，以及其药物组合物及其使用方法。拮抗剂或部分激动剂可用于治疗许多疾病，包括癌症，青光眼，炎性疾病，哮喘，中风，心肌梗塞，过敏反应，鼻炎，毒葛诱发的反应，荨麻疹，硬皮病，关节炎，小脑小动脉直径收缩，支气管收缩，和心肌缺血，以及预防心脏缺血。还公开了放射性标记的式（I）化合物及其在组织和器官诊断成像中的用途。

4. 发明申请

WO2009123881A1 PURINE DERIVATIVES AS A3 RECEPTOR- SELECTIVE AGONISTS 审中-公开
标题翻译：作为A3受体选择性激素的嘌呤衍生物
公开(公告)号：WO2009123881A1
公开(公告)日：2009-10-08
申请号：PCT/US2009/038026
申请日：2009-03-24
申请人： THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , JACOBSON, Kenneth, A. , MELMAN, Artem
发明人： JACOBSON, Kenneth, A. , MELMAN, Artem
IPC分类号： C07D473/34 , A61K31/52 , A61P25/00 , A61P3/00 , A61P29/00 , A61P35/00
CPC分类号： C07D473/34
摘要： Disclosed are (N)-methanocarba adenine nucleosides, e.g., of formula (I) as highly potent A 3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R 1 -R 6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A 3 versus the A 1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.
摘要翻译：本发明公开了（N） - 甲烷卡巴腺嘌呤核苷，例如式（I）作为高效A3腺苷受体激动剂，包含这种核苷的药物组合物，以及这些核苷的使用方法，其中R1-R6如说明书中所定义。这些核苷显示出与人类和小鼠腺苷受体的A3相对于A1受体的激动剂相似的选择性，并且被考虑用于治疗许多疾病，例如炎症，心脏缺血，中风，哮喘，糖尿病和心律失常。

5. 发明申请

WO2008108508A1 ADENOSINE DERIVATIVES, METHOD FOR THE SYNTHESIS THEREOF, AND THE PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF THE INFLAMMATORY DISEASES CONTAINING THE SAME AS AN ACTIVE INGREDIENT 审中-公开
标题翻译：腺苷衍生物，其合成方法和用于预防和治疗含有作为活性成分的炎症疾病的药物组合物
公开(公告)号：WO2008108508A1
公开(公告)日：2008-09-12
申请号：PCT/KR2007/001131
申请日：2007-03-07
申请人： FM THERAPEUTICS Co., Ltd. , JEONG, Lak Shin , KIM, Hea Ok , JACOBSON, Kenneth A. , CHOE, Seung Ah
发明人： JEONG, Lak Shin , KIM, Hea Ok , JACOBSON, Kenneth A. , CHOE, Seung Ah
IPC分类号： C07D473/34 , A61K31/4985
CPC分类号： C07D473/34 , C07H19/16
摘要： Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A3 adenosine receptors and act as A3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.
摘要翻译：公开了腺苷衍生物，其合成方法和用于预防和治疗炎性疾病的药物组合物，其包含与活性成分相同的物质。腺苷衍生物对腺苷受体具有高结合亲和力和选择性，特别是A3腺苷受体，作为A3腺苷受体拮抗剂，具有抗炎活性。因此，腺苷衍生物可用于预防和治疗炎性疾病。

6. 发明申请

WO2008045330A2 EFFECTIVE DELIVERY OF CROSS-SPECIES A3 ADENOSINE-RECEPTOR ANTAGONISTS TO REDUCE INTRAOCULAR PRESSURE 审中-公开
标题翻译：有效递送交叉物种A3腺苷受体拮抗剂降低内分泌压
公开(公告)号：WO2008045330A2
公开(公告)日：2008-04-17
申请号：PCT/US2007021409
申请日：2007-10-05
申请人： UNIV PENNSYLVANIA , MORTIMER CIVAN M , JACOBSON KENNETH A
发明人： MORTIMER CIVAN M , JACOBSON KENNETH A , AVILA MARCEL Y , STONE RICHARD
IPC分类号： A61K38/00
CPC分类号： A61K31/52
摘要： Provided are methods for reducing intraocular pressure in an individual having an ocular disorder causing elevated intraocular pressure, such as glaucoma. The method comprises administering to the individual an effective intraocular pressure-reducing amount of a pharmaceutical composition comprising an A3 subtype adenosine receptor (A 3 AR) antagonist, including dihydropyridine, pyridine, pyridinium salt or triazoloquinazoline, and derivatives thereof expressly having A 3 AR antagonist activity, including, e.g., the nucleoside- based A 3 AR antagonist, MRS-3820. Further provided is a method for ensuring the delivery of a topically administered therapeutic composition for reducing intraocular pressure, wherein the method expressly requires physically opening a channel through the corneal barrier of the patient's eye by a microneedle or micropipette to permit transport of the topical composition to the anterior chamber of the eye.
摘要翻译：本发明提供了降低眼内压引起眼内压升高的患者眼内压的方法，例如青光眼。该方法包括向个体施用有效降低眼内压的药物组合物，其包含A3亚型腺苷受体（Aβ3 AR）拮抗剂，包括二氢吡啶，吡啶，吡啶鎓盐或三唑并喹唑啉，以及衍生物其明确具有Aβ3拮抗剂活性，包括例如基于核苷的Aβ3拮抗剂MRS-3820。还提供了一种用于确保局部施用的用于降低眼内压的治疗组合物的递送的方法，其中所述方法明确地要求通过微针或微量移液管物理性地打开穿过患者眼睛的角膜屏障的通道，以允许将局部组合物运输到眼睛的前房。

7. 发明申请

WO2006031505A1 PURINE DERIVATIVES AS A3 AND A1 ADENOSINE RECEPTOR AGONISTS 审中-公开
标题翻译：作为A3和A1腺嘌呤受体激动剂的嘌呤衍生物
公开(公告)号：WO2006031505A1
公开(公告)日：2006-03-23
申请号：PCT/US2005/031678
申请日：2005-09-02
申请人： GOVERNMENT OF THE UNITED STATES OF AMERICA, REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , JACOBSON, Kenneth A. , JOSHI, Bhalchandra V. , TCHILIBON, Susanna
发明人： JACOBSON, Kenneth A. , JOSHI, Bhalchandra V. , TCHILIBON, Susanna
IPC分类号： C07D473/00 , A61K31/52 , A61P9/00
CPC分类号： C07D473/00
摘要： Disclosed are (N)-methanocarba adenine nucleosides of the formula: [Formula] as highly potent A 3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R 1 -R 6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A 1 and A 3 adenosine receptors for use in cardioprotection.
摘要翻译：公开了下式的（N） - 甲烷卡巴腺嘌呤核苷：[Formula]作为高效A

8. 发明申请

WO0073307A8 SUBSTITUTED 8-PHENYLXANTHINES USEFUL AS ANTAGONISTS OF A2B ADENOSINE RECEPTORS 审中-公开
标题翻译：作为A2B腺苷受体拮抗剂有用的替代8-苯丙氨酸
公开(公告)号：WO0073307A8
公开(公告)日：2002-02-28
申请号：PCT/US0015233
申请日：2000-06-01
申请人： UNIV VIRGINIA , NAT INST HEALTH , LINDEN JOEL M , JACOBSON KENNETH A , KIM YONG CHUL
发明人： LINDEN JOEL M , JACOBSON KENNETH A , KIM YONG-CHUL
IPC分类号： A61K31/522 , A61P1/12 , A61P3/10 , A61P9/10 , A61P9/14 , A61P11/06 , A61P27/02 , A61P35/00 , A61P43/00 , C07D473/06 , A61K31/505
CPC分类号： C07D473/06
摘要： The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
摘要翻译：本发明提供了作为A2B腺苷受体（AR）的选择性拮抗剂的化合物和药物组合物。这些化合物和组合物可用作药剂。

9. 发明申请

WO9818430A3 P2Y RECEPTOR ANTAGONISTS 审中-公开
标题翻译： P2Y受体拮抗剂
公开(公告)号：WO9818430A3
公开(公告)日：1998-06-18
申请号：PCT/US9719922
申请日：1997-10-23
申请人： UNIV NORTH CAROLINA , BOYER JOSE L , HARDEN T KENDALL , JACOBSON KENNETH A , CAMAIONI EMIDIO
发明人： BOYER JOSE L , HARDEN T KENDALL , JACOBSON KENNETH A , CAMAIONI EMIDIO
IPC分类号： G01N33/566 , A61K31/7072 , A61K31/7076 , A61P5/00 , A61P9/08 , A61P13/10 , A61P43/00 , C07H19/10 , C07H19/16 , C07H19/20 , A61K
CPC分类号： C07H19/16 , C07H19/20
摘要： Novel P2Y receptor antagonists derived from ATP and UTP are described. P2Y receptor antagonists with competitive antagonist activity at the P2Y receptor are described in particular, as are P2Y receptor antagonists that bind selectively to the P2Y1 receptor. Also described herein are methods of detecting a P2Y receptor in a biological sample. 00000
摘要翻译：描述了衍生自ATP和UTP的新型P2Y受体拮抗剂。 P2Y受体具有竞争性拮抗剂活性的P2Y受体拮抗剂特别描述，P2Y受体拮抗剂选择性结合P2Y1受体。本文还描述了检测生物样品中P2Y受体的方法。 00000

10. 发明申请

WO1998018430A2 P2Y RECEPTOR ANTAGONISTS 审中-公开
标题翻译： P2Y受体拮抗剂
公开(公告)号：WO1998018430A2
公开(公告)日：1998-05-07
申请号：PCT/US1997019922
申请日：1997-10-23
申请人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , BOYER, José, L. , HARDEN, T., Kendall , JACOBSON, Kenneth, A. , CAMAIONI, Emidio
发明人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
IPC分类号： A61K00/00
CPC分类号： C07H19/16 , C07H19/20
摘要： Novel P2Y receptor antagonists derived from ATP and UTP are described. P2Y receptor antagonists with competitive antagonist activity at the P2Y receptor are described in particular, as are P2Y receptor antagonists that bind selectively to the P2Y1 receptor. Also described herein are methods of detecting a P2Y receptor in a biological sample.
摘要翻译：描述了源自ATP和UTP的新型P2Y受体拮抗剂。 P2Y受体具有竞争性拮抗剂活性的P2Y受体拮抗剂特别描述，P2Y受体拮抗剂选择性结合P2Y1受体。本文还描述了检测生物样品中P2Y受体的方法。

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