公开(公告)号：US09651520B2

公开(公告)日：2017-05-16

申请号：US13988055

申请日：2011-02-25

Applicant: Philippe M. Dekleva ,  Jonathan A. Vickers ,  James T. Palmer

Inventor： Philippe M. Dekleva ,  Jonathan A. Vickers ,  James T. Palmer

IPC: G01N27/447 ,  B01L3/00 ,  B81B1/00 ,  B01L9/00

CPC classification number: G01N27/44791 ,  B01L3/502715 ,  B01L3/502753 ,  B01L3/502776 ,  B01L9/527 ,  B01L2300/0816 ,  B01L2300/0867 ,  B01L2400/0421 ,  B81B1/00

Abstract: A capillary electrophoresis system which provides a microfluidic chip for capillary electrophoresis and a microfluidic interface module which fluidicly couples the microfluidic chip to external fluid sources and or external repositories.

公开(公告)号：US20120101065A1

公开(公告)日：2012-04-26

申请号：US13335713

申请日：2011-12-22

Applicant: Orion D. Jankowski ,  James T. Palmer ,  Lee Honigberg

Inventor： Orion D. Jankowski ,  James T. Palmer ,  Lee Honigberg

IPC: A61K31/675 ,  A61P37/06 ,  A61K31/497

CPC classification number: C07D471/04 ,  C07F9/65685 ,  C07F9/65846

Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.

公开(公告)号：US20100130447A1

公开(公告)日：2010-05-27

申请号：US12515250

申请日：2007-11-15

Applicant: Christopher John Burns ,  Michael Francis Harte ,  James T. Palmer

Inventor： Christopher John Burns ,  Michael Francis Harte ,  James T. Palmer

IPC: A61K31/497 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D403/12 ,  C07F9/09 ,  C07D241/26 ,  A61K31/5377 ,  A61K31/675 ,  A61P29/00 ,  A61P35/00 ,  A61P13/00 ,  A61P19/00 ,  A61P3/00 ,  A61P7/00 ,  C12N9/99

CPC classification number: C07D241/20 ,  C07D213/75 ,  C07D213/82 ,  C07D241/18 ,  C07D241/24 ,  C07D241/28 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07F9/65583

Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFRβ, PDGFRα or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.

Abstract translation: 本发明涉及抑制激酶的吡啶或吡嗪。 特别是本发明的化合物抑制III类PTK受体家族成员如FMS（CSF-IR），c-KIT，PDGFR＆bgr，PDGFRα或FLT3和KDR，SRC，EphA2，EphA3，EphA8，FLT1，FLT4， HCK，LCK，PTK5（FRK），SYK，DDR1和DDR2和RET。 本发明的化合物可用于治疗激酶相关疾病如免疫和炎性疾病; 过度增生性疾病，包括癌症和涉及新血管生成的疾病; 肾肾疾病; 骨重塑疾病; 代谢疾病; 和血管疾病。

公开(公告)号：US06593327B2

公开(公告)日：2003-07-15

申请号：US10017851

申请日：2001-12-14

Applicant: Clifford M. Bryant ,  James T. Palmer ,  Robert M. Rydzewski ,  Eduardo L. Setti ,  Zong-Qiang Tian ,  Shankar Venkatraman ,  Dan-Xiong Wang

Inventor： Clifford M. Bryant ,  James T. Palmer ,  Robert M. Rydzewski ,  Eduardo L. Setti ,  Zong-Qiang Tian ,  Shankar Venkatraman ,  Dan-Xiong Wang

IPC: A61K314439

CPC classification number: C07D213/70 ,  C07B2200/07 ,  C07C255/24 ,  C07C255/29 ,  C07C255/60 ,  C07C271/22 ,  C07C275/24 ,  C07C311/06 ,  C07C311/09 ,  C07C317/50 ,  C07C323/60 ,  C07C323/62 ,  C07C2601/14 ,  C07D207/16 ,  C07D209/06 ,  C07D209/26 ,  C07D209/52 ,  C07D211/60 ,  C07D213/81 ,  C07D213/82 ,  C07D233/26 ,  C07D239/28 ,  C07D277/30 ,  C07D277/42 ,  C07D277/56 ,  C07D295/155 ,  C07D295/215 ,  C07D307/68 ,  C07D333/20 ,  C07D333/38 ,  C07D417/04 ,  C07D417/12

Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

公开(公告)号：US06287840B1

公开(公告)日：2001-09-11

申请号：US09376267

申请日：1999-08-18

Applicant: James T. Palmer ,  David Rasnick ,  Jeffrey Lee Klaus

Inventor： James T. Palmer ,  David Rasnick ,  Jeffrey Lee Klaus

IPC: C12N950

CPC classification number: C07D295/215 ,  A61K38/00 ,  C07C317/28 ,  C07F9/6533 ,  C07K5/0205 ,  C07K5/06043 ,  C07K5/0812 ,  Y02A50/411

Abstract: Irreversible cysteine protease inhibitors based upon an alkene bond being conjugated to an electron withdrawing group are disclosed. The inhibitor structure also provides a targeting peptide which is specific for different cysteine proteases. The method of making the inhibitors, and methods of using the inhibitors to inhibit cysteine proteases and for therapy are disclosed.

Abstract translation: 公开了基于与吸电子基团共轭的烯键的不可逆半胱氨酸蛋白酶抑制剂。 抑制剂结构还提供了针对不同半胱氨酸蛋白酶特异性的靶向肽。 公开了制备抑制剂的方法，以及使用抑制剂抑制半胱氨酸蛋白酶和治疗的方法。

公开(公告)号：US5976858A

公开(公告)日：1999-11-02

申请号：US700518

申请日：1996-08-23

Applicant: James T. Palmer ,  David Rasnick ,  Jeffrey Lee Klaus

Inventor： James T. Palmer ,  David Rasnick ,  Jeffrey Lee Klaus

IPC: A61K38/00 ,  C07C317/28 ,  C07D295/215 ,  C07F9/6533 ,  C07K5/02 ,  C07K5/06 ,  C07K5/087 ,  C12N9/50 ,  C12N9/99

CPC classification number: C07D295/215 ,  C07C317/28 ,  C07F9/6533 ,  C07K5/0205 ,  C07K5/06043 ,  C07K5/0812 ,  A61K38/00

Abstract: Irreversible cysteine protease inhibitors based upon an alkene bond being conjugated to an electron withdrawing group are disclosed. The inhibitor structure also provides a targeting peptide which is specific for different cysteine proteases. The method of making the inhibitors, and methods of using the inhibitors to inhibit cysteine proteases and for therapy are disclosed.

Abstract translation: PCT No.PCT / US95 / 02252 Sec。 371日期：1996年8月23日 102（e）日期1996年8月23日PCT提交1995年2月24日PCT公布。 WO95 / 23222 PCT公开号 日期1995年8月31日公开了基于与吸电子基团共轭的烯键的可逆半胱氨酸蛋白酶抑制剂。 抑制剂结构还提供了针对不同半胱氨酸蛋白酶特异性的靶向肽。 公开了制备抑制剂的方法，以及使用抑制剂抑制半胱氨酸蛋白酶和治疗的方法。

公开(公告)号：US09511073B2

公开(公告)日：2016-12-06

申请号：US14112735

申请日：2012-04-20

Applicant: David John Haydon ,  Lloyd George Czaplewski ,  Neil Robert Stokes ,  David Davies ,  Ian Collins ,  James T. Palmer ,  Jeffrey Peter Mitchell ,  Gary Robert William Pitt ,  Daniel Offermann

Inventor： David John Haydon ,  Lloyd George Czaplewski ,  Neil Robert Stokes ,  David Davies ,  Ian Collins ,  James T. Palmer ,  Jeffrey Peter Mitchell ,  Gary Robert William Pitt ,  Daniel Offermann

IPC: C07D263/32 ,  C07D417/06 ,  C07D413/06 ,  C07D277/24 ,  C07D417/12 ,  C07D413/12 ,  C07D285/08 ,  C07D513/04 ,  C07D413/10 ,  C07D271/06 ,  A61K31/5377 ,  A61K31/166 ,  A61K31/4245 ,  A61K31/421 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  C07D277/30

CPC classification number: A61K31/5377 ,  A61K31/166 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/30 ,  C07D285/08 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D513/04

Abstract: The present invention provides compounds of Formula (I): and salts, racemates, isomers, diastereoisomers, enantiomers, hydrates, solvates, N-oxides, pharmaceutically acceptable derivatives or prodrugs thereof. Also provided the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.

公开(公告)号：US09121824B2

公开(公告)日：2015-09-01

申请号：US13677036

申请日：2012-11-14

Applicant: James T. Palmer ,  Philippe M. Dekleva

Inventor： James T. Palmer ,  Philippe M. Dekleva

IPC: G01N27/447 ,  B81B1/00 ,  B01L3/00 ,  B01L9/00 ,  G01N35/00

CPC classification number: G01N27/44791 ,  B01L3/502715 ,  B01L3/50273 ,  B01L9/527 ,  B01L2300/0816 ,  B01L2400/0421 ,  B01L2400/049 ,  B81B1/00 ,  G01N35/00069 ,  Y10T29/49117

Abstract: A microfluidic chip interface for providing fluid communication with external fluid sources and external fluid waste containers, and for providing electrical contact with voltage sources and voltage and current measuring devices, is described. The microchip is first placed into electrical communication with at least one electrical source and at least one electronic measurement device, and reversibly secured in place. Chosen fluids are provided into the microchip and directed through the chip using a fluid manifold having dispensing tubes and fluid aspiration tubes, which is brought into the vicinity of the secured microchip. The distance between the fluid manifold and the microchip is chosen such that the injection tubes are located within wells in the microchip connected to microfluidic channels, and the aspiration tubes are located near the surface of the microchip in the vicinity of the wells such that fluid spillage onto the surface of the microchip during fluid transfer is avoided. The fluid manifold is removed from fluid communication with the microchip during electrical measurements.

Abstract translation: 描述了用于提供与外部流体源和外部流体废物容器的流体连通以及用于提供与电压源和电压和电流测量装置的电接触的微流体芯片接口。 微芯片首先被放置成与至少一个电源和至少一个电子测量装置电连通，并且可逆地固定就位。 将选择的流体提供到微芯片中并使用具有分配管和流体抽吸管的流体歧管引导到芯片中，流体歧管被带到安全的微芯片附近。 选择流体歧管和微芯片之间的距离使得注射管位于连接到微流体通道的微芯片中的孔内，并且抽吸管位于靠近孔附近的微芯片表面，使得流体溢出 在流体转移过程中避免了微芯片的表面。 在电测量期间，流体歧管与微芯片的流体连通被去除。

公开(公告)号：US20130248369A1

公开(公告)日：2013-09-26

申请号：US13988055

申请日：2011-02-25

Applicant: Philippe M. Dekleva ,  Jonathan A. Vickers ,  James T. Palmer

Inventor： Philippe M. Dekleva ,  Jonathan A. Vickers ,  James T. Palmer

IPC: G01N27/447 ,  B81B1/00 ,  B01L3/00

CPC classification number: G01N27/44791 ,  B01L3/502715 ,  B01L3/502753 ,  B01L3/502776 ,  B01L9/527 ,  B01L2300/0816 ,  B01L2300/0867 ,  B01L2400/0421 ,  B81B1/00

Abstract: A capillary electrophoresis system which provides a microfluidic chip for capillary electrophoresis and a microfluidic interface module which fluidicly couples the microfluidic chip to external fluid sources and or external repositories.

Abstract translation: 提供用于毛细管电泳的微流体芯片的毛细管电泳系统和将微流体芯片流体耦合到外部流体源和/或外部存储库的微流体界面模块。

公开(公告)号：US20120088750A1

公开(公告)日：2012-04-12

申请号：US13268154

申请日：2011-10-07

Applicant: James T. PALMER ,  Christopher James LUNNIS ,  Daniel A. OFFERMANN ,  Lorraine Claire AXFORD ,  Michael BLAIR ,  Dale MITCHELL ,  Nicholas PALMER ,  Christopher STEELE ,  John ATHERALL ,  David WATSON ,  David HAYDON ,  Lloyd CZAPLEWSKI ,  David DAVIES ,  Ian COLLINS

Inventor： James T. PALMER ,  Christopher James LUNNIS ,  Daniel A. OFFERMANN ,  Lorraine Claire AXFORD ,  Michael BLAIR ,  Dale MITCHELL ,  Nicholas PALMER ,  Christopher STEELE ,  John ATHERALL ,  David WATSON ,  David HAYDON ,  Lloyd CZAPLEWSKI ,  David DAVIES ,  Ian COLLINS

IPC: A61K31/506 ,  A01N43/54 ,  A61K31/497 ,  A01N43/60 ,  A01P1/00 ,  A01N43/84 ,  A61K31/55 ,  A01N43/78 ,  A61P31/04 ,  C07D417/14 ,  A61K31/5377

CPC classification number: C07D417/14 ,  A01N47/36 ,  C07D491/04 ,  C07D513/04

Abstract: The present invention provides a compound of the following formula and salts thereof: Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.

Abstract translation: 本发明提供下式的化合物及其盐：还提供了这些化合物作为抗菌剂的用途，包含它们的组合物及其制备方法。