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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 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

7. 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。

8. 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。

9. 发明申请

WO2010014921A3 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：WO2010014921A3
公开(公告)日：2010-09-16
申请号：PCT/US2009052439
申请日：2009-07-31
申请人： US HEALTH , JACOBSON KENNETH A , MELMAN ARTEM , WANG BEN BIH-REN
发明人： JACOBSON KENNETH A , MELMAN ARTEM , WANG BEN BIH-REN
IPC分类号： C07D473/34 , A61K31/52
CPC分类号： C07D473/34
摘要： Disclosed are A3 adenosine receptor antagonists and/or partial agonists of formula (I): wherein R1 to R5 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A3腺苷受体拮抗剂和/或部分激动剂：其中R 1至R 5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，炎症性疾病，哮喘，中风，心肌梗塞，过敏反应，鼻炎，毒藤素诱导的应答，荨麻疹，硬皮病，关节炎，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。还公开了式（I）的放射性标记的化合物及其在组织和器官的诊断成像中的用途。

10. 发明申请

WO2004038006A2 PURINE NUCLEOSIDES 审中-公开
标题翻译：嘌呤核苷
公开(公告)号：WO2004038006A2
公开(公告)日：2004-05-06
申请号：PCT/US0333987
申请日：2003-10-24
申请人： US GOV HEALTH & HUMAN SERV , EWHA WOMANS UNIVERSITY , JEONG LAK SHIN , JACOBSON KENNETH A , MOON HYUNG RYONG , KIM HEA OK
发明人： JEONG LAK SHIN , JACOBSON KENNETH A , MOON HYUNG RYONG , KIM HEA OK
IPC分类号： A61K31/52 , A61K31/7076 , A61P29/00 , A61P35/00 , C07D473/00 , C07D473/14 , C07D473/32 , C07D473/34 , C07H19/16 , C07H19/167 , C12N
CPC分类号： C07H5/10 , C07D473/00 , C07D473/32 , C07D473/34 , C07H19/16 , C07H19/167
摘要： Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: wherein X is sulfur or oxygen; Rl is hydrogen, alkyl, benzyl, halobenzyl, or phenylalkyl; R2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio, or thio; R3 and R3' are hydrogen, hydroxyalkyl, alkoxycarbonyl, or alkylaminocabonyl, whereas R3 and R3' do not have identical substituents simultaneously; and R4 is hydrogen or alkyl. Also disclosed are a pharmaceutical composition comprising a compound of formula (I), an isomer, or its pharmacologically acceptable salt as an active ingredient and a method for preventing or treating various diseases, state, or condition, including asthma, inflammation, cerebral ischemia, heart diseases, and cancer.
摘要翻译：公开了对A3腺苷受体具有选择性并可用于治疗癌症和炎性疾病的嘌呤核苷化合物。所述化合物由以下通式（I）表示，包括其异构体：其中X是硫或氧; R1是氢，烷基，苄基，卤代苄基或苯基烷基; R2是氢，卤素，烷氧基，烯基，炔基，烷硫基或硫代; R3和R3'是氢，羟基烷基，烷氧基羰基或烷基氨基羰基，而R3和R3'不同时具有相同的取代基; 和R4是氢或烷基。还公开了包含式（I）化合物，异构体或其药理学上可接受的盐作为活性成分的药物组合物以及用于预防或治疗各种疾病，状态或病症（包括哮喘，炎症，脑缺血，心脏疾病和癌症。

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