公开(公告)号：US07745489B2

公开(公告)日：2010-06-29

申请号：US10506059

申请日：2003-03-07

Applicant: Edward Dennis ,  Tony Yaksh ,  Karin Killermann Lucas ,  Camilla Svensson ,  David A. Six ,  George Kokotos ,  Violetta Constantinou-Kokotou

Inventor： Edward Dennis ,  Tony Yaksh ,  Karin Killermann Lucas ,  Camilla Svensson ,  David A. Six ,  George Kokotos ,  Violetta Constantinou-Kokotou

IPC: A61K31/185 ,  A61K31/195 ,  C07F9/28 ,  C07C229/00 ,  C07C205/00

CPC classification number: C07C235/80 ,  C07C233/56 ,  C07C237/22 ,  C07C271/12 ,  C07D207/08 ,  C07D309/30

Abstract: Specific, highly potent 2-oxo-amide based inhibitors of phospholipase A2 (PLA2) activity are provided. A role for PLA2 activity in spinally mediated inflammatory processes is established, and a method for treating hyperalgesia and other inflammatory conditions associated with PLA2 activity is provided.

Abstract translation: 提供了特异的，高效的2-氧代 - 酰胺基磷脂酶A2（PLA2）活性抑制剂。 建立了PLA2活性在脊髓介导炎症过程中的作用，并提供了一种治疗与PSA2活性相关的痛觉过敏和其他炎性病症的方法。

公开(公告)号：US20080319065A1

公开(公告)日：2008-12-25

申请号：US12064013

申请日：2006-08-17

Applicant: Edward Dennis ,  Tony Yaksh ,  Karin Killerman Lucas ,  Camilla Svensson ,  David A. Six ,  George Kokots ,  Violetta Constantinou-Kokotou

Inventor： Edward Dennis ,  Tony Yaksh ,  Karin Killerman Lucas ,  Camilla Svensson ,  David A. Six ,  George Kokots ,  Violetta Constantinou-Kokotou

IPC: A61K31/221 ,  C07C69/003 ,  A61K31/195 ,  A61P25/00 ,  C07C53/00

CPC classification number: C07C235/78 ,  C07C237/22

Abstract: Phospholipase A2 (PLA2) forins are expressed in spinal cord whose inhibition induces a potent antihyperalgesia. PLA2 inhibitor compounds are provided that include a common motif consisting of a 2-oxoamide with a hydrocarbon tail and a four carbon tether. The compounds block Group IVA calcium dependent PLA2 (cPLA2) and/or Group VIA calcium independent PLA2 (iPLA2) and/or Group V secreted PLA2 (sPLA2).

Abstract translation: 磷脂酶A2（PLA2）forins在脊髓中表达，其抑制诱导有效的抗痛觉过敏。 提供PLA2抑制剂化合物，其包括由具有烃尾部的2-氧代酰胺和四碳系链组成的共同基序。 化合物阻断IVA类钙依赖性PLA2（cPLA2）和/或VIA钙独立PLA2（iPLA2）和/或V组分泌的PLA2（sPLA2）。

公开(公告)号：US06996429B2

公开(公告)日：2006-02-07

申请号：US09765063

申请日：2001-01-17

Applicant: Tony Yaksh ,  George Ozaki

Inventor： Tony Yaksh ,  George Ozaki

IPC: A61B5/05

CPC classification number: A61B5/4884 ,  A61B5/1105 ,  A61B5/6824 ,  A61B2503/40 ,  A61B2503/42 ,  G01D5/2046

Abstract: An apparatus and method for measuring spatial displacement of an animal's paw injected with irritant. This apparatus comprises an electromagnetic detecting assembly having (1) a transmitting oscillator for generating electrical current (2) an electromagnetic transmitter coil coupled to the oscillator for generating an electromagnetic field (3) an electromagnetic receiving coil placed in axial plane directly below the transmitter coil (4) a first, receiving amplifier connected to the receiving coil (5) an amplitude detector connected to the receiving amplifier (6) a second amplifier connected to the amplitude detector (7) a metal object attached to the animal's paw (8) and a cylindrical observation chamber of a diameter not greater than the diameter of the generated magnetic field.

Abstract translation: 用于测量注射有刺激物的动物爪的空间位移的装置和方法。 该装置包括电磁检测组件，其具有（1）用于产生电流的发射振荡器（2）耦合到所述振荡器的电磁发射器线圈，用于产生电磁场（3）放置在发射器线圈正下方的轴向平面中的电磁接收线圈 （4）连接到接收线圈（5）的第一接收放大器，连接到接收放大器（6）的振幅检测器，连接到振幅检测器（7）的第二放大器，附接到动物爪（8）的金属物体和 直径不大于所产生的磁场直径的圆柱形观察室。

公开(公告)号：US20050148549A1

公开(公告)日：2005-07-07

申请号：US10506059

申请日：2003-03-07

Applicant: Edward Dennis ,  Tony Yaksh ,  Karin Lucas ,  Camilla Svensson ,  David Six ,  George Kokotos ,  Violetta Constaninou-Kokotou

Inventor： Edward Dennis ,  Tony Yaksh ,  Karin Lucas ,  Camilla Svensson ,  David Six ,  George Kokotos ,  Violetta Constaninou-Kokotou

IPC: C07D309/30 ,  A61K31/16 ,  A61K31/197 ,  A61K31/22 ,  A61K31/325 ,  A61K31/366 ,  A61K31/40 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07C233/56 ,  C07C235/74 ,  C07C235/78 ,  C07C235/80 ,  C07C237/22 ,  C07C271/12 ,  C07C271/22 ,  C07D207/08 ,  A61K31/66 ,  A61K31/195 ,  A61K31/41 ,  C07C233/46 ,  C07D257/04 ,  C07F9/28

CPC classification number: C07C235/80 ,  C07C233/56 ,  C07C237/22 ,  C07C271/12 ,  C07D207/08 ,  C07D309/30

Abstract: Specific, highly potent 2-oxo-amide based inhibitors of phospholipase A2 (PLA2) activity are provided. A role for PLA2 activity in spinally mediated inflammatory processes is established, and a method for treating hyperalgesia and other inflammatory conditions associated with PLA2 activity is provided.

Abstract translation: 提供了特异的，高效的2-氧代 - 酰胺基磷脂酶A 2（PLA 2 N 2）活性的抑制剂。 建立了在脊髓介导的炎性过程中PLA 2活性的作用，并且提供了治疗与PSA 2活性相关的痛觉过敏和其它炎性病症的方法。

公开(公告)号：US20080039461A1

公开(公告)日：2008-02-14

申请号：US11648226

申请日：2006-12-28

Applicant: Andrew Protter ,  Camilla Svensson ,  Tony Yaksh ,  Barbara Cordell ,  Sundeep Dugar

Inventor： Andrew Protter ,  Camilla Svensson ,  Tony Yaksh ,  Barbara Cordell ,  Sundeep Dugar

IPC: A61K31/535 ,  A61K31/415 ,  A61K31/445 ,  A61P25/00 ,  A61K31/505

CPC classification number: A61K31/381 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/496

Abstract: The present invention relates to methods for the prevention or treatment of pain by the inhibition of p38 MAP kinase.

Abstract translation: 本发明涉及通过抑制p38 MAP激酶预防或治疗疼痛的方法。