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1. 发明申请

WO1996040706A1 ORALLY ACTIVE ADENOSINE KINASE INHIBITORS 审中-公开
标题翻译： ORALLY ACTIVE ADENOSIN KINASE INHIBITORS
公开(公告)号：WO1996040706A1
公开(公告)日：1996-12-19
申请号：PCT/US1996010919
申请日：1996-06-07
申请人： GENSIA INC.
发明人： GENSIA INC. , UGARKAR, Gheemarao, G. , ERION, Mark, D. , GALENO, Jorge, E., Gomez , CASTELLINO, Angelo, J. , BROWNE, Clinton, E.
IPC分类号： C07H19/14
CPC分类号： C07H19/04 , A61K31/00 , A61K31/7064 , A61K31/7076 , C07D487/04 , C07H19/052 , C07H19/06 , C07H19/14 , C07H19/16
摘要： This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to orally active, substituted 5-aryl pyrrolo[2,3-d] pyrimidine and 3-aryl pyrazolo[3,4-d] pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention also relates to the preparation and use of these and other adenosine kinase inhibitors in the treatment of cardiovascular and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.
摘要翻译：本发明涉及腺苷激酶抑制剂和核苷类似物，特别是具有作为腺苷激酶活性的口服活性的取代的5-芳基吡咯并[2,3-d]嘧啶和3-芳基吡唑并[3,4-d]嘧啶核苷类似物抑制剂。本发明还涉及这些和其它腺苷激酶抑制剂在治疗心血管和脑血管疾病，炎症等疾病中的制备和应用，可以通过增加腺苷的局部浓度来调节。

2. 发明申请

WO9314807A3 METHOD AND APPARATUS FOR CLOSED LOOP DRUG DELIVERY 审中-公开
标题翻译：闭环式药物递送的方法和装置
公开(公告)号：WO9314807A3
公开(公告)日：1994-12-08
申请号：PCT/US9300676
申请日：1993-01-19
申请人： GENSIA INC
发明人： VALCKE CHRISTIAN PAUL , BOCHENKO WALTER JOHN , HILLMAN ROBERT STEVEN
IPC分类号： A61M5/00 , A61M5/172 , A61M31/00
CPC分类号： A61M5/1723 , A61M2230/06 , G06F19/3468 , G06F19/3481 , G16H50/50 , Y10S128/12 , Y10S128/13 , A61M2230/005
摘要： A closed-loop drug delivery system uses patient response and rule based decision making methods to achieve operator specified responses for diagnostic purposes. In the preferred embodiment, cardiac diagnosis is performed by pharmacologically stressing the heart by administration of an exercise simulating agent drug. In the preferred method, a protocol is defined, which preferably includes a target for a physiologic variable, such as heart rate, and a plan to achieve that target value. Preferably, the plan includes a specification of the desired rate of increase in that variable, such as the rate of increase in the heart rate per minute. The plan comprises the desired changes in the physiologic variable as a function of time. While any desired function may be used, the more common modes include RAMP, HOLD, LEVEL and TARGET mode. In one aspect of this invention, the protocol may be varied by the operator after drug administration has begun. Further, in one embodiment, the protocol includes a definition of an acceptable zone of deviation from the plan, such that if the patient physiologic variable deviates from the permissible zone, alternate control rules are implemented. Preferably, saturation detection and avoidance is implemented.

3. 发明授权

US5721356A Orally active adenosine kinase inhibitors 失效
标题翻译：口服活性腺苷激酶抑制剂
公开(公告)号：US5721356A
公开(公告)日：1998-02-24
申请号：US473491
申请日：1995-06-07
申请人： Bheemarao G. Ugarkar , Mark D. Erion , Jorge E. Gomez Galeno , Angelo J. Castellino , Clinton E. Browne
发明人： Bheemarao G. Ugarkar , Mark D. Erion , Jorge E. Gomez Galeno , Angelo J. Castellino , Clinton E. Browne
IPC分类号： C12N9/99 , A61K31/00 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61P25/04 , A61P25/08 , A61P29/00 , A61P43/00 , C07D487/04 , C07D519/00 , C07H19/04 , C07H19/052 , C07H19/06 , C07H19/14 , C07H19/16 , C07H19/23
CPC分类号： C07H19/04 , A61K31/00 , A61K31/7064 , A61K31/7076 , C07D487/04 , C07H19/052 , C07H19/06 , C07H19/14 , C07H19/16
摘要： This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to orally active, substituted 5-aryl pyrrolo�2,3-d!pyrimidine and 3-aryl pyrazolo�3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention also relates to the preparation and use of these and other adenosine kinase inhibitors in the treatment of cardiovascular and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.
摘要翻译：本发明涉及腺苷激酶抑制剂和核苷类似物，特别是具有作为腺苷激酶活性的口服活性的取代的5-芳基吡咯并[2,3-d]嘧啶和3-芳基吡唑并[3,4-d]嘧啶核苷类似物抑制剂。本发明还涉及这些和其它腺苷激酶抑制剂在治疗心血管和脑血管疾病，炎症等疾病中的制备和应用，可以通过增加腺苷的局部浓度来调节。

4. 发明授权

US5573772A Methods for protecting tissues and organs from ischemic damage 失效
标题翻译：保护组织和器官免受缺血损伤的方法
公开(公告)号：US5573772A
公开(公告)日：1996-11-12
申请号：US214942
申请日：1994-03-17
申请人： James M. Downey , Kevin M. Mullane
发明人： James M. Downey , Kevin M. Mullane
IPC分类号： A61F2/02 , A61K9/14 , A61K9/20 , A61K9/48 , A61M31/00 , C07H20060101
CPC分类号： A61K31/70 , Y10S514/936
摘要： Methods for protecting tissues and organs including the heart central nervous system, and kidney from ischemic damage are described and claimed based upon the recognition that protection against infarction is mediated by A3 rather than A1 adenosine receptors, as was previously thought, and that the receptor mediating protection in other organs and tissues has not been defined. Methods for selectively stimulating A3 adenosine receptors are described and claimed, as such selection is shown to prevent or substantially reduce cell death resulting from ischemia with or without reperfusion in humans. According to this invention, the A3 adenosine receptor is selectively stimulated by administering a compound which is an A3 adenosine receptor-selective agonist. Prevention of tissue death is also achieved by administering a compound which is a non-selective adenosine receptor agonist together with compounds that act as antagonists to the A1 and A2 adenosine receptor.
摘要翻译：基于以前认为由APC而不是A1腺苷受体介导的对梗塞的保护的认识描述和要求保护包括心脏中枢神经系统在内的组织和器官以及来自缺血性损伤的肾脏的方法，并且受体介导其他器官和组织的保护尚未定义。描述和要求保护选择性刺激A3腺苷受体的方法，因为这样的选择被证明可预防或显着减少由于在人或不伴有再灌注的局部缺血导致的细胞死亡。根据本发明，通过给予作为A3腺苷受体选择性激动剂的化合物来选择性地刺激A3腺苷受体。还通过将作为非选择性腺苷受体激动剂的化合物与作为Aβ和腺苷受体的拮抗剂的化合物一起施用来预防组织死亡。

5. 发明申请

WO1996040705A1 C-4' MODIFIED ADENOSINE KINASE INHIBITORS 审中-公开
标题翻译： C-4'修饰的腺苷激酶抑制剂
公开(公告)号：WO1996040705A1
公开(公告)日：1996-12-19
申请号：PCT/US1996010404
申请日：1996-06-07
申请人： GENSIA INC.
发明人： GENSIA INC. , BOYER, Serge, H. , ERION, Mark, D. , UGARKAR, Bheemarao, G.
IPC分类号： C07H19/14
CPC分类号： C07H19/04 , C07H19/06 , C07H19/14
摘要： This invention relates to adenosine kinase inhibitors and to nucleoside analogs, C-4' modified pyrrolo[2,3-d] pyrimidine and pyrazolo[3,4-d] pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention relates to nucleoside analogs of this kind, having zero substitutions or two substitutions at the C-4' position of the furanose (sugar) moiety. The invention also relates to the preparation and use of these adenosine kinase inhibitors in the treatment of cardiovascular, and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.
摘要翻译：本发明涉及具有作为腺苷激酶抑制剂活性的腺苷激酶抑制剂和核苷类似物C-4'修饰的吡咯并[2,3-d]嘧啶和吡唑并[3,4-d]嘧啶核苷类似物。本发明涉及这样的核苷类似物，其在呋喃糖（糖）部分的C-4'位置具有零取代或两个取代。本发明还涉及这些腺苷激酶抑制剂在治疗心血管和脑血管疾病，炎症等疾病中的制备和应用，可以通过增加腺苷的局部浓度来调节。

6. 发明申请

WO1996040621A1 METHODS AND COMPOUNDS FOR DIAGNOSING CORONARY ARTERY DISEASE 审中-公开
标题翻译：用于诊断冠状动脉疾病的方法和化合物
公开(公告)号：WO1996040621A1
公开(公告)日：1996-12-19
申请号：PCT/US1996007811
申请日：1996-05-31
申请人： GENSIA, INC.
发明人： GENSIA, INC. , METZNER, Ernest, K. , ERION, Mark, D.
IPC分类号： C07C247/04
CPC分类号： C07C323/25 , C07C217/02 , C07C247/04 , C07C255/24 , C07C317/28
摘要： The present invention relates generally to methods of diagnosis, evaluation and treatment of coronary artery disease in mammals using substituted catecholamines and compounds therefore. It also relates to the preparation, use and administration of these compounds which are useful in the diagnosis, evaluation and treatment of coronary artery disease by means of a feedback controlled drug delivery system that delivers exercise simulating agents which are capable of eliciting acute responses similar to those elicited by aerobic exercise.
摘要翻译：本发明一般涉及使用取代的儿茶酚胺和化合物来诊断，评价和治疗哺乳动物冠状动脉疾病的方法。它还涉及这些化合物的制备，使用和给药，其可用于通过反馈控制的药物递送系统诊断，评估和治疗冠状动脉疾病，所述反馈控制药物递送系统递送能够引起类似于那些由有氧运动引起的。

7. 发明申请

WO1996025186A2 FEEDBACK CONTROLLED DRUG DELIVERY SYSTEM 审中-公开
标题翻译：反馈控制药物递送系统
公开(公告)号：WO1996025186A2
公开(公告)日：1996-08-22
申请号：PCT/US1996001221
申请日：1996-01-30
申请人： GENSIA, INC.
发明人： GENSIA, INC. , HILLMAN, Robert, Steven , VALCKE, Christian, P. , GAUTHIER, Robert, T. , GORIN, Michael, Morduch
IPC分类号： A61M00/00
CPC分类号： G01N33/4905 , A61M5/1723 , A61M39/105 , A61M39/16 , A61M2005/1403 , A61M2202/0478 , A61M2230/20 , G01N33/48707 , G06F19/00 , A61M2202/0007
摘要： A feedback controlled drug delivery system includes automated blood sampling and analysis and dosing of the patient. Automated sampling is performed by direct analysis of patient blood, such as for measurement of its coagulation state. A novel manifold includes a fluid input port, a patient port adapted to output fluid and to receive a blood sample from the patient, and a fluid pathway connecting the fluid port and the patient port. A sample line is connected to the fluid pathway to provide the sample to an analyzer. In one aspect of this invention, the sample is forced through the sample line by isolating the patient port, such as by a valve, and non-drug fluid is forced into the manifold causing the blood to cross through the sample line. In another embodiment, an integrated assembly includes an integrated peristaltic pump, valve assembly, selectively movable actuator and integrated waste container. In one aspect, the peristaltic pump permits retraction of the rollers away from the inner circumference of the pump, so as to reduce deformation of the peri-pump tube and to permit sterilization.
摘要翻译：反馈控制的药物递送系统包括患者的自动血液取样和分析和给药。通过直接分析患者血液进行自动采样，例如用于测量其凝血状态。新颖的歧管包括流体输入端口，适于输出流体并从患者接收血液样本的患者端口以及连接流体端口和患者端口的流体通路。样品管线连接到流体通道以将样品提供给分析仪。在本发明的一个方面，样品通过例如通过阀门隔离患者端口而被迫通过样品管线，并且非药物流体被迫进入歧管中，导致血液穿过样品管线。在另一个实施例中，集成组件包括集成的蠕动泵，阀组件，选择性地可移动致动器和集成的废物容器。在一个方面，蠕动泵允许辊离开泵的内周回缩，以便减少周围泵管的变形并允许灭菌。

8. 发明申请

WO1994018215A1 ADENOSINE KINASE INHIBITORS COMPRISING LYXOFURANOSYL DERIVATIVES 审中-公开
标题翻译：含有丝氨酸衍生物的腺苷激酶抑制剂
公开(公告)号：WO1994018215A1
公开(公告)日：1994-08-18
申请号：PCT/US1994001260
申请日：1994-02-03
申请人： GENSIA, INC.
发明人： GENSIA, INC. , ERION, Mark, David , UGARKAR, Bheemarao, Ganapatrao , CASTELLINO, Angelo, John
IPC分类号： C07H19/16
CPC分类号： C07H19/04 , C07H19/06 , C07H19/14 , C07H19/16
摘要： Novel lyxose derivatives which selectively inhibit adenosine kinase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine. The figure depicts levels of acadesine and ZMP in heart tissue after intravenous administration of compound "A" of the instant invention.
摘要翻译：提供了选择性抑制腺苷激酶的新型赖索糖衍生物和制备这些化合物的方法。这些化合物可用于治疗体内某些条件，这可以通过增加局部腺苷浓度而改善。该图描绘了静脉内施用本发明化合物“A”后心脏组织中阿卡捷定和ZMP的水平。

9. 发明申请

WO1994018200A1 NOVEL INHIBITORS OF ADENOSINE MONOPHOSPHATE DEAMINASE 审中-公开
标题翻译：腺苷单磷酸酯类杀伤剂的新型抑制剂
公开(公告)号：WO1994018200A1
公开(公告)日：1994-08-18
申请号：PCT/US1994001342
申请日：1994-02-03
申请人： GENSIA, INC.
发明人： GENSIA, INC. , ERION, Mark, David , BOOKSER, Brett, Carder , KASIBHATLA, Srinivas, Rao , GRUBER, Harry, Edward
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/00 , A61K31/55 , Y02A50/411
摘要： Novel diazepine derivatives which selectively inhibit adenosine monophosphate deaminase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine.
摘要翻译：提供选择性抑制腺苷一磷酸脱氨酶的新二氮杂衍生物及其制备方法。这些化合物可用于治疗体内某些条件，这可以通过增加局部腺苷浓度而改善。

10. 发明申请

WO1994017803A1 ADENOSINE KINASE INHIBITORS 审中-公开
标题翻译：腺苷激酶抑制剂
公开(公告)号：WO1994017803A1
公开(公告)日：1994-08-18
申请号：PCT/US1994001340
申请日：1994-02-03
申请人： GENSIA, INC.
发明人： GENSIA, INC. , FIRESTEIN, Gary, Steven , UGARKAR, Bheemarao, Ganapatrao , MILLER, Leonard, Paul , GRUBER, Harry, Edward , BULLOUGH, David, Andrew , ERION, Mark, David , CASTELLINO, Angelo, John
IPC分类号： A61K31/52
CPC分类号： A61K31/70 , A61K31/00 , A61K31/7064 , C07H19/04
摘要： Novel compounds which selectively inhibit adenosine kinase and methods of preparing adenosine kinase inhibitors are provided. Also provided are methods of treating various conditions which may be ameliorated by increased local concentrations of adenosine using adenosine kinase inhibitors.
摘要翻译：提供了选择性抑制腺苷激酶的新型化合物和制备腺苷激酶抑制剂的方法。还提供了治疗各种病症的方法，其可以通过使用腺苷激酶抑制剂增加腺苷浓度来改善。

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