公开(公告)号：US07291628B2

公开(公告)日：2007-11-06

申请号：US11029247

申请日：2005-01-04

Applicant: John L. Neumeyer ,  Jean M. Bidlack ,  Xiao-Hui Gu

Inventor： John L. Neumeyer ,  Jean M. Bidlack ,  Xiao-Hui Gu

IPC: A61K31/485

CPC classification number: C07D221/28 ,  A61K31/485 ,  A61K51/0455

Abstract: The invention is based in part on the discovery that nonselective κ agonists that possess μ receptor-mediated effects in addition to their κ agonist effects can decrease cocaine self-administration more effectively and with fewer undesirable side effects than can highly selective κ agonists. The invention includes a number of new compounds having both nonselective κ opioid receptor agonist activity and additional activity at μ opioid receptors. These compounds are useful for the treatment of cocaine abuse, and can also be radiolabeled for use as imaging agents, e.g., the N-fluoroalkyl and iodoalkyl derivatives can be used, respectively, for positron emission tomography (PET) and single photon computed tomography (SPECT) brain imaging.

Abstract translation: 本发明部分地基于以下发现：除了κ受体介导的作用以外，除了其kappa激动剂效应之外，非选择性κ激动剂可以比高选择性κ激动剂更有效地减少可卡因自身给药并且具有更少的不希望的副作用。 本发明包括许多具有非选择性κ阿片受体激动剂活性和在阿片样物质受体的另外活性的新化合物。 这些化合物可用于治疗可卡因滥用，并且也可以放射性标记用作成像剂，例如，N-氟烷基和碘代烷基衍生物可分别用于正电子发射断层摄影（PET）和单光子计算机断层摄影（ SPECT）脑成像。

公开(公告)号：US20100130505A1

公开(公告)日：2010-05-27

申请号：US12597509

申请日：2008-04-28

Applicant: Alan V. Smrcka ,  Burns C. Blaxall ,  Jean M. Bidlack

Inventor： Alan V. Smrcka ,  Burns C. Blaxall ,  Jean M. Bidlack

IPC: A61K31/498 ,  C40B30/04 ,  G01N33/53 ,  A61K31/18 ,  C07C321/00 ,  C07C211/00 ,  A61K31/135 ,  C07D311/82 ,  A61K31/35 ,  A61K31/47 ,  C07D401/12 ,  C07D403/12

CPC classification number: G01N33/74 ,  A61K31/122 ,  A61K31/4709 ,  A61K31/498 ,  G01N33/564 ,  G01N33/6893 ,  G01N33/9486 ,  G01N2333/726 ,  G01N2500/04 ,  G01N2800/32 ,  G01N2800/325 ,  Y02A50/393 ,  Y02A50/397

Abstract: Disclosed are compositions and methods for treating diseases associated with G protein βγ subunit activity.

Abstract translation: 公开了用于治疗与G蛋白和γ亚基活性相关的疾病的组合物和方法。

公开(公告)号：US4792529A

公开(公告)日：1988-12-20

申请号：US789269

申请日：1985-10-18

Applicant: Richard A. Rudick ,  Robert M. Herndon ,  Jean M. Bidlack

Inventor： Richard A. Rudick ,  Robert M. Herndon ,  Jean M. Bidlack

IPC: G01N33/564 ,  G01N33/68 ,  G01N33/534 ,  G01N33/53

CPC classification number: G01N33/564 ,  G01N33/6857 ,  G01N2800/285 ,  Y10S436/811

Abstract: Multiple sclerosis (MS) is diagnosed by determining with a quantitative immunoassay the quantity of free kappa light chains in the cerebrospinal fluid of a patient. The immunoassay is preferably a radioimmunoassay. In carrying out the immunoassay, the free kappa light chains are combined with antiserum specific thereto. This method of diagnosing MS has high sensitivity in distinguishing between normal patients and patients affected with MS.

Abstract translation: 通过定量免疫测定确定患者脑脊液中游离κ轻链的数量来诊断多发性硬化症（MS）。 免疫测定优选为放射免疫测定。 在进行免疫测定时，游离κ轻链与其特异的抗血清组合。 这种诊断MS的方法在区分正常患者和患有MS的患者方面具有很高的灵敏度。

公开(公告)号：US08975259B2

公开(公告)日：2015-03-10

申请号：US12597509

申请日：2008-04-28

Applicant: Alan V Smrcka ,  Burns C. Blaxall ,  Jean M. Bidlack

Inventor： Alan V Smrcka ,  Burns C. Blaxall ,  Jean M. Bidlack

IPC: A61K31/50 ,  A61K31/495 ,  G01N33/74 ,  G01N33/564 ,  G01N33/68 ,  G01N33/94 ,  A61K31/122 ,  A61K31/4709 ,  A61K31/498

CPC classification number: G01N33/74 ,  A61K31/122 ,  A61K31/4709 ,  A61K31/498 ,  G01N33/564 ,  G01N33/6893 ,  G01N33/9486 ,  G01N2333/726 ,  G01N2500/04 ,  G01N2800/32 ,  G01N2800/325 ,  Y02A50/393 ,  Y02A50/397

Abstract: Disclosed are compositions and methods for treating diseases associated with G protein βγ subunit activity.

Abstract translation: 公开了用于治疗与G蛋白和γ亚基活性相关的疾病的组合物和方法。

公开(公告)号：US06844438B2

公开(公告)日：2005-01-18

申请号：US10222736

申请日：2002-08-15

Applicant: John L. Neumeyer ,  Jean M. Bidlack ,  Xiao-Hui Gu

Inventor： John L. Neumeyer ,  Jean M. Bidlack ,  Xiao-Hui Gu

IPC: A61K31/485 ,  A61K51/04 ,  C07D221/28 ,  A61K51/00

CPC classification number: C07D221/28 ,  A61K31/485 ,  A61K51/0455

Abstract: The invention is based in part on the discovery that nonselective κ agonists that possess μ receptor-mediated effects in addition to their κ agonist effects can decrease cocaine self-administration more effectively and with fewer undesirable side effects than can highly selective κ agonists. The invention includes a number of new compounds having both nonselective κ opioid receptor agonist activity and additional activity at μ opioid receptors. These compounds are useful for the treatment of cocaine abuse, and can also be radiolabeled for use as imaging agents, e.g., the N-fluoroalkyl and iodoalkyl derivatives can be used, respectively, for positron emission tomography (PET) and single photon computed tomography (SPECT) brain imaging.

Abstract translation: 本发明部分地基于以下发现：除了κ受体介导的作用以外，除了其kappa激动剂效应之外，非选择性κ激动剂可以比高选择性κ激动剂更有效地减少可卡因自身给药并且具有更少的不希望的副作用。 本发明包括许多具有非选择性κ阿片受体激动剂活性和在阿片样物质受体的另外活性的新化合物。 这些化合物可用于治疗可卡因滥用，并且也可以放射性标记用作成像剂，例如，N-氟烷基和碘代烷基衍生物可分别用于正电子发射断层摄影（PET）和单光子计算机断层摄影（ SPECT）脑成像。