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1. 发明申请

WO2005119252A2 GPR35 AND MODULATORS THEREOF FOR THE TREATMENT OF METABOLIC-RELATED DISORDERS 审中-公开
标题翻译： GPR35的调节剂用于治疗与代谢相关的疾病
公开(公告)号：WO2005119252A2
公开(公告)日：2005-12-15
申请号：PCT/US2005/018082
申请日：2005-05-23
申请人： ARENA PHARMACEUTICALS, INC. , LEONARD, James N. , CHU, Zhi Liang , UNETT, David J. , GATLIN, Joel E. , GAIDAROV, Ibragim , QIU, Jun , SKINNER, Philip J. , BOATMAN, P. Douglas
发明人： LEONARD, James N. , CHU, Zhi Liang , UNETT, David J. , GATLIN, Joel E. , GAIDAROV, Ibragim , QIU, Jun , SKINNER, Philip J. , BOATMAN, P. Douglas
IPC分类号： G01N33/50
CPC分类号： G01N33/6893 , A61K31/425 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR35, and b) determining whether GPR35 functionality is increased, wherein an increase in GPR35 functionality is indicative of the candidate compound being a metabolic stabilizing compound. The invention further relates to use of a GPR35 modulator for the manufacture of a medicament for use as a metabolic stabilizing agent. In addition, the invention relates to a method for increasing GPR35 function, comprising contacting GPR35 with an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein X is O or S; and R1, R2, R3, R4, and R5 are each independently selected from the group consisting of H, C1-4 alkoxy, C1-4 alkyl, halogen, hydroxyl, and nitro; wherein said C1-4 alkoxy is optionally substituted with carbo-C1-4-alkoxy or carboxy.
摘要翻译：本发明涉及用于鉴定代谢稳定化合物的方法，包括：a）使候选化合物与GPR35接触，和b）确定GPR35的功能是否增加，其中GPR35功能的增加指示候选化合物是代谢稳定化合物。本发明还涉及GPR35调节剂在制备用作代谢稳定剂的药物中的用途。另外，本发明涉及增加GPR35功能的方法，包括使GPR35与有效量的式（I）化合物或其可药用盐接触，其中X为O或S; R 1，R 2，R 3，R 4和R 5各自独立地选自H，C 1-4烷氧基，C 1-4烷基，卤素，羟基和硝基; 其中所述C 1-4烷氧基任选被C 1-4 - 烷氧基或羧基取代。

2. 发明申请

WO2009074477A1 EXTRUSION PROCESS FOR GRAFTING RUBBERS 审中-公开
标题翻译：挤压挤出工艺
公开(公告)号：WO2009074477A1
公开(公告)日：2009-06-18
申请号：PCT/EP2008/066534
申请日：2008-12-01
申请人： DSM IP ASSETS B.V. , OLIVIER, Errol, Joseph , MEESSEN, Patric , HOUTVAST, Franciscus, Victoire, Paulus , GEESINK, Johannes, Hendrik , QIU, Jun
发明人： MEESSEN, Patric , HOUTVAST, Franciscus, Victoire, Paulus , GEESINK, Johannes, Hendrik , QIU, Jun
IPC分类号： C08F255/04 , B29C47/00 , B29C47/78 , C08F255/00 , C08F255/02
CPC分类号： C08F255/04 , B29C47/0011 , B29C47/822 , B29C47/8895 , C08F255/00 , C08F255/02 , C08F291/00
摘要： The invention relates to a process for producing a grafted rubber comprising: a) providing an ethylene propylene rubber having a weight average molecular weight (Mw) of at least 80 kg/mol in a continuous extrusion reactor by feeding the rubber in a slab/melt dosing unit and transporting the rubber to the continuous extrusion reactor by a melt pump; b) drying the rubber in the continuous extrusion reactor to a moisture content of between about 0.2 and about 0.5 wt%; c) providing the dried rubber to a first injection zone of the continuous extrusion reactor at a temperature of between 190 and 250°C, d) in the first injection zone, providing successively a first amount of maleic anhydride and a first free-radical initiator to the dried rubber; e) reacting maleic anhydride with the rubber in a first reaction zone of the continuous extrusion reactor to produce a grafted rubber; f) in a second injection zone, providing successively a second amount of maleic anhydride and a second free-radical initiator,the first and the second free radical initiator is an organic peroxide with a half-life (ty2) of more than 1 second if measured in mono-chlorobenzene at 220°C. g) applying shear to the grafted rubber in a second reaction zone of the continuous extrusion reactor, the shear sufficient to reduce the weight average molecular weight (Mw) of the grafted rubber by a factor of at least 2.
摘要翻译：本发明涉及一种生产接枝橡胶的方法，包括：a）在连续挤出反应器中通过将橡胶进料到板/熔体中提供重均分子量（Mw）至少为80kg / mol的乙丙橡胶并通过熔体泵将橡胶输送到连续挤出反应器; b）将连续挤出反应器中的橡胶干燥至约0.2至约0.5重量％的水分含量; c）在190-250℃的温度下将干燥的橡胶提供给连续挤出反应器的第一注入区，d）在第一注入区中，连续提供第一量的马来酸酐和第一自由基引发剂到干燥的橡胶; e）在连续挤出反应器的第一反应区中使马来酸酐与橡胶反应，生产接枝橡胶; f）在第二注射区域中，连续提供第二量的马来酸酐和第二自由基引发剂，第一和第二自由基引发剂是半衰期（ty2）大于1秒的有机过氧化物，如果在220℃的单氯苯中测定。 g）在连续挤出反应器的第二反应区中对接枝橡胶施加剪切力，剪切力足以将接枝橡胶的重均分子量（Mw）降低至少2倍。

3. 发明申请

WO2009063067A2 HIGH PERFORMANCE MEMBRANE 审中-公开
标题翻译：高性能膜
公开(公告)号：WO2009063067A2
公开(公告)日：2009-05-22
申请号：PCT/EP2008/065593
申请日：2008-11-14
申请人： DSM IP ASSETS BV , QIU, Jun , RULKENS, Rudy , KAMP, OP DEN, Johannes Leonardus Maria , THIES, Jens Christoph
发明人： QIU, Jun , RULKENS, Rudy , KAMP, OP DEN, Johannes Leonardus Maria , THIES, Jens Christoph
IPC分类号： B01D67/00 , B01D69/12
CPC分类号： B01D67/0088 , B01D69/02 , B01D71/26 , B01D71/56 , B01D2323/02 , B01D2325/22 , B01D2325/24 , H01M2/145 , H01M2/1653
摘要： The invention relates to a micro-porous membrane comprising a porous membrane carrier made of a first polymeric material (A) and comprising a second polymeric material (B) intimately divided throughout the porous membrane carrier, wherein the porous membrane carrier comprises a plurality of interconnected polymeric fibers, fibrils, filaments and/or lamellae having a thickness of less than 1 µm, the porous membrane carrier has an interconnected open porous structure formed by the plurality of interconnected polymeric fibers, fibrils, filaments and/or lamellae and a porosity of at least 50%; and the polymeric material (B) comprises a thermoplastic polycondensation polymer and is present in an amount of at most 30 wt.%, relative to the total weight of (A) and (B). The invention also relates to a process for preparing such a micro-porous membrane comprising steps wherein (i) a porous membrane carrier made of a first polymeric material (A) is impregnated with a polymer solution comprising a second polymeric material (B) in a solvent system (X), and (ii) the resulting impregnated membrane carrier is quenched in a non-solvent system (Y), thereby precipitating at least part of the second polymeric material (B).
摘要翻译：本发明涉及一种微孔膜，其包括由第一聚合物材料（A）制成的多孔膜载体，并且包括在整个多孔膜载体上密切分配的第二聚合材料（B），其中多孔膜载体包括多个互连的聚合物纤维，原纤维，细丝和/或薄片，其厚度小于1μm，多孔膜载体具有由多个互连的聚合物纤维，原纤维，长丝和/或薄片形成的互连的开放多孔结构，至少50％; 聚合物材料（B）包含热塑性缩聚聚合物，相对于（A）和（B）的总重量，其含量至多为30重量％。本发明还涉及一种制备这种微孔膜的方法，其包括以下步骤：（i）由第一聚合物材料（A）制成的多孔膜载体用包含第二聚合物材料（B）的聚合物溶液浸渍溶剂体系（X），和（ii）所得浸渍的膜载体在非溶剂系统（Y）中骤冷，从而沉淀至少部分第二聚合物材料（B）。

4. 发明申请

WO2008116345A1 METHOD AND APPARATUS OF TESTING DATA COMMUNICATION PERFORMANCE OF A NETWORK SYSTEM 审中-公开
标题翻译：测试网络系统数据通信性能的方法与装置
公开(公告)号：WO2008116345A1
公开(公告)日：2008-10-02
申请号：PCT/CN2007/000969
申请日：2007-03-26
申请人： INTEL COPORATION , SU, Yu , QIU, Jun , ZHANG, Xu
发明人： SU, Yu , QIU, Jun , ZHANG, Xu
IPC分类号： H04L7/04
CPC分类号： H04L1/24 , H04J3/0638 , H04L1/205 , H04L43/106 , H04L43/50 , H04W24/00
摘要： Machine-readable media, methods, apparatus and system for testing a data communication performance of a network system are described. In some embodiments, an apparatus may comprise a first channel to synchronize a local clock of the apparatus with another local clock of another apparatus by communicating a synchronization message with the another apparatus through a first connection. The apparatus may further comprise a second channel to analyze a transceiving activity performed by the apparatus through a second connection and a timestamp of the transceiving activity, wherein the timestamp is made based upon the local clock.
摘要翻译：描述了用于测试网络系统的数据通信性能的机器可读介质，方法，装置和系统。在一些实施例中，装置可以包括通过第一连接与另一装置通信同步消息来将装置的本地时钟与另一装置的另一本地时钟同步的第一信道。该装置还可以包括第二信道，用于通过第二连接和收发活动的时间戳来分析由装置执行的收发活动，其中基于本地时钟进行时间戳。

5. 发明申请

WO2005116653A2 HUMAN G PROTEIN-COUPLED RECEPTOR AND MODULATORS THEREOF FOR THE TREATMENT OF HYPERGLYCEMIA AND RELATED DISORDERS 审中-公开
标题翻译：人G蛋白偶联受体及其调节剂治疗高血压和相关疾病
公开(公告)号：WO2005116653A2
公开(公告)日：2005-12-08
申请号：PCT/US2005/012447
申请日：2005-04-12
申请人： ARENA PHARMACEUTICALS, INC. , QIU, Jun , WEBB, Robert R. , UNETT, David J. , GATLIN, Joel E. , CONNOLLY, Daniel T.
发明人： QIU, Jun , WEBB, Robert R. , UNETT, David J. , GATLIN, Joel E. , CONNOLLY, Daniel T.
IPC分类号： G01N33/566
CPC分类号： C07D417/04 , A61K31/427 , A61K31/4439 , G01N33/76 , G01N2333/726
摘要： The present invention relates to methods of identifying whether one or more candidate compounds is a modulator of a G protein-coupled receptor (GPCR) or a modulator of blood glucose concentration. In certain embodiments, the GPCR is human. The present invention also relates to methods of using a modulator of the GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for lowering blood glucose concentration, for preventing or treating certain metabolic disorders, such as insulin resistance, impaired glucose tolerance, and diabetes, and for preventing or treating a complication of an elevated blood glucose concentration, such as atherosclerosis, heart disease, stroke, hypertension and peripheral vascular disease.
摘要翻译：本发明涉及鉴定一种或多种候选化合物是G蛋白偶联受体（GPCR）或血糖浓度调节剂的调节剂的方法。在某些实施方案中，GPCR是人。本发明还涉及使用GPCR调制器的方法。优选的调节剂是激动剂。本发明的激动剂可用作降低血糖浓度的治疗剂，用于预防或治疗某些代谢紊乱，例如胰岛素抵抗，葡萄糖耐量异常和糖尿病，以及用于预防或治疗血糖浓度升高的并发症，作为动脉粥样硬化，心脏病，中风，高血压和外周血管疾病。

6. 发明申请

WO2009149258A3 CRYSTALLINE FORM OF 6-[(4S)-2-METHYL-4-(2-NAPHTHYL)-1,2,3,4-TETRAHYDROISOQUINOLIN-7-YL]PYRIDAZIN-3-AMINE 审中-公开
标题翻译： 6 - [（4S）-2-甲基-4-（2-萘基）-1,2,3,4-四氢喹啉-7-YL]吡啶-3-胺的晶体形式
公开(公告)号：WO2009149258A3
公开(公告)日：2010-02-04
申请号：PCT/US2009046256
申请日：2009-06-04
申请人： SQUIBB BRISTOL MYERS CO , ALBANY MOLECULAR RES INC , QIU JUN , GAO QI , LIU SHUANG , HU MIN , YANG YUH-LIN ALLEN , ISHERWOOD MATTHEW , AMIN RASIDUL
发明人： QIU JUN , GAO QI , LIU SHUANG , HU MIN , YANG YUH-LIN ALLEN , ISHERWOOD MATTHEW , AMIN RASIDUL
IPC分类号： C07D401/04 , A61K31/501 , A61P3/04 , A61P25/24
CPC分类号： C07F5/04 , C07C215/20 , C07C217/58 , C07C223/02 , C07D217/04 , C07D237/20 , C07D401/04 , C07D413/10 , C07F5/022 , C07F5/025
摘要： The present disclosure generally relates to a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form, as well of methods of using a crystalline form in the treatment of depression and other conditions and methods for obtaining such crystalline form.
摘要翻译：本公开内容通常涉及6 - [（4S）-2-甲基-4-（萘基）-1,2,3,4-四氢异喹啉-7-基]哒嗪-3-胺的结晶形式。本公开还通常涉及包含结晶形式的药物组合物，以及在治疗抑郁症和其它病症中使用结晶形式的方法以及获得这种结晶形式的方法。

7. 发明申请

WO2009063067A3 HIGH PERFORMANCE MEMBRANE 审中-公开
标题翻译：高性能膜
公开(公告)号：WO2009063067A3
公开(公告)日：2009-07-30
申请号：PCT/EP2008065593
申请日：2008-11-14
申请人： DSM IP ASSETS BV , QIU JUN , RULKENS RUDY , KAMP OP DEN JOHANNES LEONARDUS MARIA , THIES JENS CHRISTOPH
发明人： QIU JUN , RULKENS RUDY , KAMP OP DEN JOHANNES LEONARDUS MARIA , THIES JENS CHRISTOPH
IPC分类号： B01D67/00 , B01D69/12
CPC分类号： B01D67/0088 , B01D69/02 , B01D71/26 , B01D71/56 , B01D2323/02 , B01D2325/22 , B01D2325/24 , H01M2/145 , H01M2/1653
摘要： The invention relates to a micro-porous membrane comprising a porous membrane carrier made of a first polymeric material (A) and comprising a second polymeric material (B) intimately divided throughout the porous membrane carrier, wherein the porous membrane carrier comprises a plurality of interconnected polymeric fibers, fibrils, filaments and/or lamellae having a thickness of less than 1 µm, the porous membrane carrier has an interconnected open porous structure formed by the plurality of interconnected polymeric fibers, fibrils, filaments and/or lamellae and a porosity of at least 50%; and the polymeric material (B) comprises a thermoplastic polycondensation polymer and is present in an amount of at most 30 wt.%, relative to the total weight of (A) and (B). The invention also relates to a process for preparing such a micro-porous membrane comprising steps wherein (i) a porous membrane carrier made of a first polymeric material (A) is impregnated with a polymer solution comprising a second polymeric material (B) in a solvent system (X), and (ii) the resulting impregnated membrane carrier is quenched in a non-solvent system (Y), thereby precipitating at least part of the second polymeric material (B).
摘要翻译：本发明涉及一种微孔膜，其包含由第一聚合物材料（A）制成的多孔膜载体并且包含紧密分散在整个多孔膜载体中的第二聚合物材料（B），其中所述多孔膜载体包含多个互连的厚度小于1μm的聚合物纤维，原纤维，长丝和/或薄片，多孔膜载体具有由多个相互连接的聚合物纤维，原纤维，长丝和/或薄片形成的互连的开放多孔结构，孔隙率为至少50％; 并且聚合物材料（B）包含热塑性缩聚聚合物并且以相对于（A）和（B）的总重量计至多30重量％的量存在。本发明还涉及制备这种微孔膜的方法，其包括以下步骤：（i）用包含第二聚合物材料（B）的聚合物溶液浸渍由第一聚合物材料（A）制成的多孔膜载体，溶剂系统（X），和（ii）所得浸渍膜载体在非溶剂体系（Y）中骤冷，由此沉淀至少部分第二聚合物材料（B）。

8. 发明申请

WO2008034581A1 GASTRENN-MEMBRAN 审中-公开
标题翻译： GUEST RACING REED
公开(公告)号：WO2008034581A1
公开(公告)日：2008-03-27
申请号：PCT/EP2007/008112
申请日：2007-09-18
申请人： GKSS-FORSCHUNGSZENTRUM GEESTHACHT GMBH , QIU, Jun , PEINEMANN, Klaus-Viktor , WIND, Jan , PINGEL, Holger
发明人： QIU, Jun , PEINEMANN, Klaus-Viktor , WIND, Jan , PINGEL, Holger
IPC分类号： B01D71/00 , B01D71/02
CPC分类号： B01D69/10 , B01D53/228 , B01D71/08 , B01D71/12 , B01D71/16 , B01D2256/12 , C01B13/0255 , C01B2210/0046 , Y10S55/05
摘要： Die Erfindung betrifft eine Membran zur Gastrennung, ein Verfahren zur Herstellung einer entsprechenden Membran, ein Gastrennmodul mit einer entsprechenden Membran sowie ein Verfahren zum Betrieb eines solchen Gastrennmoduls. Die Membran umfasst: eine poröse Trägerschicht aus Polymer oder anorganischem Material, insbesondere keramischem Material, eine Trennschicht, umfassend eine Mischung aus Saccharid- Derivaten und Homopolymer, insbesondere umfassend Ethylzellulose, Zelluloseacetat oder Poly-4-Methyl-1-Penten, wobei die Saccharid-Derivate eine zyklische Struktur mit fünf oder sechs Ringatomen oder eine lineare Struktur aufweisen oder Monosaccharid-Derivate sind, die über Glykosidbindungen verbunden sind, wobei die Anzahl der auf diese Weise verbundenen Monosaccharide zwischen 2 und 1.000 liegt. Dabei hat sich überraschenderweise herausgestellt, dass der Sauerstofffluss durch eine solche Membran erheblich ansteigt, wenn der Membran Saccharid-Derivate zugesetzt werden.
摘要翻译：本发明涉及一种气体分离膜，用于产生相应的膜，具有相应的隔膜以及用于操作这种气体分离组件的方法的气体分离组件的方法。所述膜包括：聚合物或无机材料制成的多孔载体层，特别是陶瓷材料，剥离层，其包含糖衍生物和均聚物，特别是包括乙基纤维素，醋酸纤维素或聚-4-甲基-1-戊烯的混合物，其中糖衍生物的环状结构具有五个或六个环原子或一个直链结构或包括单糖衍生物，其通过糖苷键连接，其中的连接在位于这样的单糖2-1000数。在这种情况下，已经令人惊奇地发现，当添加显著氧气流量的增加通过这样的膜的膜糖衍生物。

9. 发明申请

WO2005116653A3 MODULATORS OF HUMAN G PROTEIN-COUPLED RECEPTORS FOR THE TREATMENT OF HYPERGLYCEMIA AND RELATED DISORDERS 审中-公开
标题翻译：人G蛋白相关受体调节剂治疗高血压和相关疾病
公开(公告)号：WO2005116653A3
公开(公告)日：2006-05-18
申请号：PCT/US2005012447
申请日：2005-04-12
申请人： ARENA PHARM INC , QIU JUN , WEBB ROBERT R , UNETT DAVID J , GATLIN JOEL E , CONNOLLY DANIEL T
发明人： QIU JUN , WEBB ROBERT R , UNETT DAVID J , GATLIN JOEL E , CONNOLLY DANIEL T
IPC分类号： G01N33/566 , A61K31/427 , A61K31/4439 , A61K45/06 , C07D417/04 , G01N33/68 , G01N33/76
CPC分类号： C07D417/04 , A61K31/427 , A61K31/4439 , G01N33/76 , G01N2333/726
摘要： The present invention relates to methods of identifying whether one or more candidate compounds is a modulator of a G protein-coupled receptor (GPCR) or a modulator of blood glucose concentration. In certain embodiments, the GPCR is human. The present invention also relates to methods of using a modulator of the GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for lowering blood glucose concentration, for preventing or treating certain metabolic disorders, such as insulin resistance, impaired glucose tolerance, and diabetes, and for preventing or treating a complication of an elevated blood glucose concentration, such as atherosclerosis, heart disease, stroke, hypertension and peripheral vascular disease.
摘要翻译：本发明涉及鉴定一种或多种候选化合物是G蛋白偶联受体（GPCR）或血糖浓度调节剂的调节剂的方法。在某些实施方案中，GPCR是人。本发明还涉及使用GPCR的调制器的方法。优选的调节剂是激动剂。本发明的激动剂可用作降低血糖浓度的治疗剂，用于预防或治疗某些代谢紊乱，例如胰岛素抵抗，葡萄糖耐量异常和糖尿病，以及用于预防或治疗血糖浓度升高的并发症，作为动脉粥样硬化，心脏病，中风，高血压和外周血管疾病。

10. 发明申请

WO2005119252A3 MODULATORS OF GPR35 FOR THE TREATMENT OF METABOLIC-RELATED DISORDERS 审中-公开
标题翻译： GPR35的调节剂用于治疗与代谢相关的疾病
公开(公告)号：WO2005119252A3
公开(公告)日：2006-01-12
申请号：PCT/US2005018082
申请日：2005-05-23
申请人： ARENA PHARM INC , LEONARD JAMES N , CHU ZHI LIANG , UNETT DAVID J , GATLIN JOEL E , GAIDAROV IBRAGIM , QIU JUN , SKINNER PHILIP J , BOATMAN P DOUGLAS
发明人： LEONARD JAMES N , CHU ZHI LIANG , UNETT DAVID J , GATLIN JOEL E , GAIDAROV IBRAGIM , QIU JUN , SKINNER PHILIP J , BOATMAN P DOUGLAS
IPC分类号： A61K31/425 , G01N33/50 , A61P3/06 , A61P3/10
CPC分类号： G01N33/6893 , A61K31/425 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR35, and b) determining whether GPR35 functionality is increased, wherein an increase in GPR35 functionality is indicative of the candidate compound being a metabolic stabilizing compound. The invention further relates to use of a GPR35 modulator for the manufacture of a medicament for use as a metabolic stabilizing agent. In addition, the invention relates to a method for increasing GPR35 function, comprising contacting GPR35 with an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein X is O or S; and R1, R2, R3, R4, and R5 are each independently selected from the group consisting of H, C1-4 alkoxy, C1-4 alkyl, halogen, hydroxyl, and nitro; wherein said C1-4 alkoxy is optionally substituted with carbo-C1-4-alkoxy or carboxy.
摘要翻译：本发明涉及用于鉴定代谢稳定化合物的方法，包括：a）使候选化合物与GPR35接触，和b）确定GPR35的功能是否增加，其中GPR35功能的增加指示候选化合物是代谢稳定化合物。本发明还涉及GPR35调节剂在制备用作代谢稳定剂的药物中的用途。另外，本发明涉及增加GPR35功能的方法，其包括使GPR35与有效量的式（I）化合物或其药学上可接受的盐接触，其中X为O或S; 并且R 1，R 2，R 3，R 4和R 5各自独立地选自H，C 1-4烷氧基，C 1-4烷基，卤素，羟基和硝基; 其中所述C 1-4烷氧基任选被碳-C 1-4 - 烷氧基或羧基取代。

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