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11. 发明申请

WO2022155037A1 HETEROCYCLIC P2Y 14 RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2022155037A1
公开(公告)日：2022-07-21
申请号：PCT/US2022/011226
申请日：2022-01-05
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , JACOBSON, Kenneth A. , JUNG, Young-Hwan , WEN, Zhiwei
发明人： JACOBSON, Kenneth A. , JUNG, Young-Hwan , WEN, Zhiwei
IPC分类号： C07D211/18 , C07D249/06 , C07D205/04 , C07D209/02 , C07D211/34 , C07D211/70 , C07D223/04 , C07D255/02 , C07D261/08 , C07D403/10 , A61P29/00 , A61P25/00 , A61P3/10 , A61K31/4192 , A61K31/44
摘要： Disclosed are compounds for treating or preventing a disease or disorder responsive to antagonism of a P2Y14R receptor agonist in a mammal in need thereof, for example, compounds of formulas (I) and (II), wherein R1‑R8, X, Y, Z, X', Y', Z', and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.

12. 发明申请

WO2009006089A2 A2 ADENOSINE RECEPTOR AGONISTS 审中-公开
标题翻译： A2腺苷受体激动剂
公开(公告)号：WO2009006089A2
公开(公告)日：2009-01-08
申请号：PCT/US2008/067978
申请日：2008-06-24
申请人： GOVERNMENT OF THE UNITED STATES OF AMERICA, REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , SOUTH ALABAMA MEDICAL SCIENCE FOUNDATION , JACOBSON, Kenneth, A. , GAO, Zhan-guo , ADACHI, Hayamitsu , DOWNEY, James, M. , LIU, Yanping
发明人： JACOBSON, Kenneth, A. , GAO, Zhan-guo , ADACHI, Hayamitsu , DOWNEY, James, M. , LIU, Yanping
IPC分类号： C07H19/167 , A61K31/7076 , A61P9/10
CPC分类号： C07H19/167
摘要： Disclosed are A ZB adenosine receptor (AR) agonists of formula (I), in which R 1 , R 2 , R 3 , R 4 , Z, and n are defined herein. The invention also provides compositions comprising at least one compound of formula I and methods of use thereof, for example, in the treatment of septic shock, cystic fibrosis, restenosis, erectile dysfunction, inflammation, myocardial ischemia, and reperfusion injury.
摘要翻译：公开了式（I）的AβZBα腺苷受体（AR）激动剂，其中R 1，R 2， R 3，R 4，Z和n在本文中定义。本发明还提供了包含至少一种式I化合物的组合物及其使用方法，例如用于治疗败血性休克，囊性纤维化，再狭窄，勃起功能障碍，炎症，心肌缺血和再灌注损伤。

13. 发明申请

WO0073307A3 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：WO0073307A3
公开(公告)日：2001-05-31
申请号：PCT/US0015233
申请日：2000-06-01
申请人： UNIV VIRGINIA , 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。

14. 发明申请

WO1997027177A2 DIHYDROPYRIDINE-, PYRIDINE-, BENZOPYRAN- ONE- AND TRIAZOLOQUINAZOLINE DERIVATIVE, THEIR PREPARATION AND THEIR USE AS ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：二氢吡啶，吡啶，苯并噻唑和三唑并噻唑衍生物，其制备及其用作腺苷受体拮抗剂
公开(公告)号：WO1997027177A2
公开(公告)日：1997-07-31
申请号：PCT/US1997001252
申请日：1997-01-29
申请人： THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , JACOBSON, Kenneth, A. , JIANG, Ji-Long , KIM, Yong-Chul , KARTON, Yishai , VAN RHEE, Albert, M.
发明人： THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
IPC分类号： C07D211/90
CPC分类号： C07D401/04 , C07D211/90 , C07D311/22 , C07D311/30 , C07D311/32 , C07D317/70 , C07D405/04 , C07D409/04 , C07D487/04 , C07D493/04 , C07F7/0812
摘要： The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R1 to R4 are as defined in the description, and M is -CH(OH)-CH(R2) or -C(OH)=C(R2)- and R1, R2 are as defined in the description; or dihydropyridines of formula (III), wherein R2 to R6 are as defined in the description; or pyridines of formula (IV), wherein R2 to R6 are as defined in the description, or triazoloquinazolines of formula (V) wherein R1 and R2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供某些新的化合物，组合物和通过阻断其腺苷受体来治疗哺乳动物的方法，包括施用至少一种本发明的化合物。本发明化合物的实例包括式（I）和（II）的某些类黄酮，其中R 1至R 4如说明书中所定义，M为-CH（OH）-CH（R 2）或-C（OH）= C（R 2） - 和R 1，R 2如说明书中所定义; 或式（III）的二氢吡啶类，其中R2至R6如说明书中所定义; 或式（Ⅳ）的吡啶，其中R 2至R 6如说明书中所定义，或式（Ⅴ）的三唑并喹唑啉其中R 1和R 2如说明书中所定义; 及其衍生物或其药学上可接受的盐。

15. 发明申请

WO2011103552A9 AMP DERIVATIVES FOR TREATING CARDIAC DISEASES 审中-公开
标题翻译：用于治疗心脏病的AMP衍生物
公开(公告)号：WO2011103552A9
公开(公告)日：2012-04-26
申请号：PCT/US2011025680
申请日：2011-02-22
申请人： UNIV CONNECTICUT , US HEALTH , 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
CPC分类号： A61K31/675 , A61K31/683 , C07F9/65616
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.
摘要翻译：描述了磷酸酯和膦酸盐的N-甲基钴胺衍生物，包括它们的前药类似物。含有（N） - 甲氰胺（二环[3.1.0]己烷）环体系的2-氯-AMP衍生物代替核糖的MRS2339激活P2X受体，配体门控离子通道。基于由于C-P键的稳定性增加体内半衰期的期望，使用Michaelis-Arbuzov和Wittig反应合成MRS2339的膦酸酯类似物。当通过小型渗透泵（Alzet）将其转运给小鼠（心力衰竭的遗传模型）时，一些类似物通过超声心动图来源的分数缩短（FS）评估，显着增加了体内完整的心脏收缩功能车辆输注小鼠。用于治疗心力衰竭的碳环核苷酸类似物的范围已经扩大。

16. 发明申请

WO2011068978A1 METHANOCARBA ADENOSINE DERIVATIVES AND DENDRIMER CONJUGATES THEREOF 审中-公开
标题翻译：甲磺酸腺苷衍生物及其结合物
公开(公告)号：WO2011068978A1
公开(公告)日：2011-06-09
申请号：PCT/US2010/058746
申请日：2010-12-02
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , JACOBSON, Kenneth A. , TOSH, Dilip K.
发明人： JACOBSON, Kenneth A. , TOSH, Dilip K.
IPC分类号： C07D473/34 , A61K31/52 , A61P27/00 , A61P35/00
CPC分类号： C07D473/34
摘要： Disclosed are (N)-methanocarba adenine nucleosides, e.g., of the formula (I): as A 3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein A, a, R 2 , and R 3 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. Also disclosed are conjugates comprising a dendrimer and one or more ligands, which are functionalized congeners of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily. Such conjugates are have the potential of being used as dual agonists, dual antagonists, or agonist/antagonist combinations.
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A，a，R 2和R 3为如说明书中所定义。这些核苷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。还公开了包含树状聚合物和一种或多种配体的缀合物，其是G-蛋白偶联受体（GPCR）超家族的受体的激动剂或拮抗剂的功能化同系物。这样的缀合物具有用作双重激动剂，双重拮抗剂或激动剂/拮抗剂组合的潜力。

17. 发明申请

WO9727177A3 DIHYDROPYRIDINE-, PYRIDINE-, BENZOPYRAN- ONE- AND TRIAZOLOQUINAZOLINE DERIVATIVE, THEIR PREPARATION AND THEIR USE AS ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：二氢吡啶，吡啶，苯并噻唑和三唑并噻唑衍生物，其制备及其用作腺苷受体拮抗剂
公开(公告)号：WO9727177A3
公开(公告)日：1997-11-13
申请号：PCT/US9701252
申请日：1997-01-29
申请人： US HEALTH , JACOBSON KENNETH A , JIANG JI LONG , KIM YONG CHUL , KARTON YISHAI , RHEE ALBERT M VAN
发明人： JACOBSON KENNETH A , JIANG JI-LONG , KIM YONG-CHUL , KARTON YISHAI , VAN RHEE ALBERT M
IPC分类号： A61K31/4422 , A61K31/4545 , A61P7/02 , A61P9/10 , A61P25/22 , A61P43/00 , C07D211/90 , C07D311/22 , C07D311/30 , C07D311/32 , C07D317/70 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D487/04 , C07D493/04 , C07F7/08 , A61K31/44 , C07D407/04
CPC分类号： C07D401/04 , C07D211/90 , C07D311/22 , C07D311/30 , C07D311/32 , C07D317/70 , C07D405/04 , C07D409/04 , C07D487/04 , C07D493/04 , C07F7/0812
摘要： The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R1 to R4 are as defined in the description, and M is -CH(OH)-CH(R2)- or -C(OH)= C(R2)- and R1, R2 are as defined in the description; or dihydropyridines of formula (III), wherein R2 to R6 are as defined in the description; or pyridines of formula (IV), wherein R2 to R6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R1 and R2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供某些新的化合物，组合物和通过阻断其腺苷受体来治疗哺乳动物的方法，包括施用至少一种本发明的化合物。本发明化合物的实例包括式（I）和（II）的某些类黄酮，其中R 1至R 4如说明书中所定义，M为-CH（OH）-CH（R 2） - 或-C （OH）= C（R 2） - 和R 1，R 2如说明书中所定义; 或式（III）的二氢吡啶类，其中R 2至R 6如说明书中所定义; 或式（Ⅳ）的吡啶，其中R 2至R 6如说明书中所定义，或式（Ⅴ）的三唑并喹唑啉，其中R 1和R 2如说明书中所定义; 及其衍生物或其药学上可接受的盐。

18. 发明申请

WO2019157417A1 HETEROCYCLIC P2Y14 RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2019157417A1
公开(公告)日：2019-08-15
申请号：PCT/US2019/017422
申请日：2019-02-11
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , JACOBSON, Kenneth A. , YU, Jinha , CIANCETTA, Antonella , WEN, Zhiwei , JUNG, Young-Hwan
发明人： JACOBSON, Kenneth A. , YU, Jinha , CIANCETTA, Antonella , WEN, Zhiwei , JUNG, Young-Hwan
IPC分类号： C07D235/18 , A61K31/439 , A61K31/44 , C07D403/04 , C07D409/10 , C07D249/06 , C07D471/08 , C07D209/10 , C07D211/18 , C07D211/70 , A61P29/00 , A61P13/12 , A61P11/06
摘要： Disclosed are compounds of formulas (I)-(IX) for treating or preventing a disease or disorder responsive to antagonism of a P2Y 14 R receptor agonist in a mammal in need thereof, wherein R 1 -R 8 , X, Y, Z, X', Y', Z', and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.

19. 发明申请

WO2011103552A2 COMPOSITIONS AND METHODS TO TREAT CARDIAC DISEASES 审中-公开
标题翻译：组合物和治疗心脏病的方法
公开(公告)号：WO2011103552A2
公开(公告)日：2011-08-25
申请号：PCT/US2011025680
申请日：2011-02-22
申请人： UNIV CONNECTICUT , US HEALTH , LIANG BRUCE , JACOBSON KENNETH A , JOSHI BHALCHANDRA V
发明人： LIANG BRUCE , JACOBSON KENNETH A , JOSHI BHALCHANDRA V
IPC分类号： C07F9/6561
CPC分类号： A61K31/675 , A61K31/683 , C07F9/65616
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.
摘要翻译：描述了膦酸盐和次膦酸盐，其包括其前体药物类似物的N-甲基碳酰胺衍生物。含有（N） - 甲氰胺（双环[3.1.0]己烷）环系的2-氯-AMP衍生物MRS2339代替核糖，活化P2X受体，配体门控离子通道。基于由于C-P键的稳定性而增加的体内半衰期的期望，使用Michaelis-Arbuzov和Wittig反应合成MRS2339的膦酸酯类似物。当通过小型渗透泵（Alzet）将氯雷斯特林过度表达的小鼠（心力衰竭的遗传模型）施用时，一些类似物显着增加体内完整的心脏收缩功能，如通过超声心动图来源的分数缩短（FS）评估的，与车辆输注小鼠。用于治疗心力衰竭的碳环核苷酸类似物的范围已经扩大。

20. 发明申请

WO2009006089A3 A2 ADENOSINE RECEPTOR AGONISTS 审中-公开
标题翻译： A2腺苷受体激动剂
公开(公告)号：WO2009006089A3
公开(公告)日：2009-04-09
申请号：PCT/US2008067978
申请日：2008-06-24
申请人： US GOV HEALTH & HUMAN SERV , UNIV SOUTH ALABAMA , JACOBSON KENNETH A , GAO ZHAN-GUO , ADACHI HAYAMITSU , DOWNEY JAMES M , LIU YANPING
发明人： JACOBSON KENNETH A , GAO ZHAN-GUO , ADACHI HAYAMITSU , DOWNEY JAMES M , LIU YANPING
IPC分类号： C07H19/167 , A61K31/7076 , A61P9/10
CPC分类号： C07H19/167
摘要： Disclosed are AZB adenosine receptor (AR) agonists of formula (I), in which R1, R2, R3, R4, Z, and n are defined herein. The invention also provides compositions comprising at least one compound of formula I and methods of use thereof, for example, in the treatment of septic shock, cystic fibrosis, restenosis, erectile dysfunction, inflammation, myocardial ischemia, and reperfusion injury.
摘要翻译：公开了式（I）的AZB腺苷受体（AR）激动剂，其中R1，R2，R3，R4，Z和n如本文所定义。本发明还提供了包含至少一种式I化合物及其使用方法的组合物，例如治疗败血性休克，囊性纤维化，再狭窄，勃起功能障碍，炎症，心肌缺血和再灌注损伤。

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