公开(公告)号：WO2007146085A3

公开(公告)日：2008-04-17

申请号：PCT/US2007013454

申请日：2007-06-06

Applicant: XENOPORT INC ,  ZERANGUE NOA ,  GAO QINGZHI ,  DOWER WILLIAM J

Inventor： ZERANGUE NOA ,  GAO QINGZHI ,  DOWER WILLIAM J

IPC: C07F9/24 ,  A61K31/661 ,  A61K31/665 ,  A61P21/00 ,  A61P25/28 ,  C07F9/655

CPC classification number: C07F9/65515 ,  C07F9/2408 ,  C07F9/2458

Abstract: Membrane permeable prodrugs of creatine phosphate, pharmaceutical compositions comprising membrane permeable prodrugs of creatine phosphate, and methods of treating diseases such as ischemia, heart failure, and neurodegenerative disorders comprising administering prodrugs of creatine phosphate or pharmaceutical compositions thereof are disclosed. In the Formula (I) wherein: Y and Z are each independently selected from Formula (1), Formula (2), and Formula (3).

Abstract translation: 本发明公开了磷酸肌酸的可渗透膜的前体药物，包含可渗透磷酸肌酸前药的药物组合物，以及治疗疾病如缺血，心力衰竭和神经变性疾病的方法，包括施用磷酸肌酸前药或其药物组合物。 在其中：Y和Z各自独立地选自式（1），式（2）和式（3）的式（I）中。

公开(公告)号：WO2007016161A2

公开(公告)日：2007-02-08

申请号：PCT/US2006/029039

申请日：2006-07-25

Applicant: XENOPORT, INC. ,  ZERANGUE, Noa

Inventor： ZERANGUE, Noa

IPC: G01N33/50

CPC classification number: G01N33/5064 ,  A61K49/0002 ,  G01N33/5008 ,  G01N33/5011 ,  G01N33/5014 ,  G01N33/5058 ,  G01N33/566 ,  G01N33/94 ,  G01N2333/705 ,  G01N2500/10

Abstract: OCT3 is consistently expressed at high levels in brain microvessel endothelial cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is actively transported by, the OCT3 transporter, and therefore a candidate substrate for crossing the blood brain barrier. The assays are useful in screening for therapeutic, cytotoxic or imaging compounds used in the treatment or diagnosis of neurological diseases.

Abstract translation: OCT3在脑微血管内皮细胞中一直以高水平表达。 本文公开了用于确定测试材料/分子是否为OCT3转运蛋白的基质和/或由OCT3转运蛋白主动转运的测定法，因此用于跨越血脑屏障的候选底物。 该测定法可用于筛选用于治疗或诊断神经疾病的治疗性，细胞毒性或成像化合物。

公开(公告)号：WO2007016159A2

公开(公告)日：2007-02-08

申请号：PCT/US2006/029033

申请日：2006-07-25

Applicant: XENOPORT, INC. ,  ZERANGUE, Noa

Inventor： ZERANGUE, Noa

IPC: G01N33/68

CPC classification number: G01N33/5008 ,  A61K47/50 ,  G01N33/5011 ,  G01N33/5014 ,  G01N33/5035 ,  G01N33/5058 ,  G01N33/5064 ,  G01N33/6872 ,  G01N33/9426 ,  G01N2500/10 ,  G01N2800/24

Abstract: GAT2 is consistently expressed at high levels in brain microvessel endothelial cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is actively transported by, the GAT2 transporter, and therefore a candidate substrate for crossing the blood brain barrier. The assays are useful in screening for therapeutic, cytotoxic or imaging compounds used in the treatment or diagnosis of neurological diseases.

Abstract translation: GAT2在脑微血管内皮细胞中始终以高水平表达。 本文公开了用于确定测试材料/分子是否为GAT2转运蛋白的底物和/或由GAT2转运蛋白主动转运以及因此穿过血脑屏障的候选底物的测定。 该测定法可用于筛选用于治疗或诊断神经疾病的治疗剂，细胞毒素或成像化合物。

公开(公告)号：WO2005117998A2

公开(公告)日：2005-12-15

申请号：PCT/US2005/020070

申请日：2005-06-06

Applicant: XENOPORT, INC. ,  ZERANGUE, Noa

Inventor： ZERANGUE, Noa

IPC: A61K49/00

CPC classification number: G01N33/5035 ,  A61K49/0004 ,  G01N33/5011 ,  G01N33/574 ,  G01N33/57492 ,  G01N2500/00

Abstract: SMVT is consistently expressed at high levels in cancer cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is transported by, the SMVT transporter, and therefore a candidate substrate for transport into cancer cells. The assays are useful in screening for cytotoxic agents or imaging components used in the treatment or diagnosis of cancer.

Abstract translation: SMVT在癌细胞中一直以高水平表达。 本文公开了用于确定测试材料/分子是否用于由SMVT转运蛋白和/或由SMVT转运蛋白转运和/或由SMVT转运蛋白转运的测定，因此用于转运到癌细胞中的候选底物。 该测定法可用于筛选用于治疗或诊断癌症的细胞毒剂或成像组件。

公开(公告)号：WO2004033655A2

公开(公告)日：2004-04-22

申请号：PCT/US2003/032087

申请日：2003-10-08

Applicant: XENOPORT, INC. ,  ZERANGUE, Noa ,  PADDON, Christopher

Inventor： ZERANGUE, Noa ,  PADDON, Christopher

IPC: C12N

CPC classification number: C07K14/47

Abstract: The invention provides several new transporter proteins, nucleic acids encoding them and methods of using the transporters to screen agents, conjugates or conjugate moieties, linked or linkable to agents, for capacity to be transported as substrates through the transporters. The invention also provides methods of treatment involving oral delivery of agents that either alone, or as a result of linkage to a conjugate moiety, are substrates of one of the transporter.

Abstract translation: 本发明提供几种新的转运蛋白，编码它们的核酸和使用转运蛋白筛选与试剂连接或可连接的试剂，缀合物或缀合物部分，以及通过转运蛋白作为底物转运的能力的方法。 本发明还提供涉及口服递送药物的方法，所述药物单独或作为与缀合物部分连接的结果是转运蛋白之一的底物。

公开(公告)号：WO2010022177A2

公开(公告)日：2010-02-25

申请号：PCT/US2009/054349

申请日：2009-08-19

Applicant: XENOPORT, INC. ,  GANGAKHEDKAR, Archana ,  DAI, Xuedong ,  ZERANGUE, Noa ,  VIRSIK, Peter A.

Inventor： GANGAKHEDKAR, Archana ,  DAI, Xuedong ,  ZERANGUE, Noa ,  VIRSIK, Peter A.

IPC: A61P17/06

CPC classification number: C07C235/06 ,  C07C69/60 ,  C07C69/75 ,  C07C69/78 ,  C07C69/96 ,  C07C235/08 ,  C07C235/10 ,  C07C235/12 ,  C07C259/06 ,  C07C271/64 ,  C07C275/50 ,  C07C2601/14 ,  C07D207/16 ,  C07D263/20 ,  C07D285/12 ,  C07D295/18 ,  C07D295/185

Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.

Abstract translation: 富马酸氢盐的前体药物，包含富马酸氢盐的前体药物的药物组合物，以及使用富马酸氢甲酯的前体药物及其药物组合物用于治疗牛皮癣，哮喘，多发性硬化症，炎性肠病 疾病和关节炎。披露。

公开(公告)号：WO2007016160A3

公开(公告)日：2007-05-31

申请号：PCT/US2006029034

申请日：2006-07-25

Applicant: XENOPORT INC ,  ZERANGUE NOA

Inventor： ZERANGUE NOA

IPC: C12Q1/68 ,  A61K47/46 ,  A61P25/00 ,  G01N33/68 ,  G01N33/82

CPC classification number: G01N33/82 ,  G01N33/5064 ,  G01N33/6872 ,  G01N33/6896 ,  G01N33/94 ,  G01N2500/10 ,  G06Q30/06 ,  G06Q30/0621 ,  Y10S977/716

Abstract: SVCT2 is consistently expressed at high levels in brain microvessel endothelial cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is actively transported by, the SVCT2 transporter, and therefore a candidate substrate for crossing the blood brain barrier. The assays are useful in screening for therapeutic, cytotoxic or imaging compounds used in the treatment or diagnosis of neurological diseases.

Abstract translation: SVCT2在脑微血管内皮细胞中一直以高水平表达。 本文公开了用于确定测试材料/分子是否为SVCT2转运蛋白和/或由SVCT2转运蛋白主动转运的测定材料/分子以及因此用于穿过血脑屏障的候选底物的测定。 该测定法可用于筛选用于治疗或诊断神经疾病的治疗性，细胞毒性或成像化合物。

公开(公告)号：WO2007016178A3

公开(公告)日：2007-04-19

申请号：PCT/US2006029063

申请日：2006-07-26

Applicant: XENOPORT INC ,  ZERANGUE NOA

Inventor： ZERANGUE NOA

IPC: G01N33/50 ,  G01N33/68 ,  G01N33/94

CPC classification number: A61K38/17 ,  G01N33/502 ,  G01N33/5064 ,  G01N33/6872 ,  G01N33/9426

Abstract: BGTl is consistently expressed at high levels in brain microvessel endothelial cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is actively transported by, the BGTl transporter, and therefore a candidate substrate for crossing the blood brain barrier. The assays are useful in screening for therapeutic, cytotoxic or imaging compounds used in the treatment or diagnosis of neurological diseases.

Abstract translation: BGT1在脑微血管内皮细胞中始终以高水平表达。 本文公开了用于确定测试材料/分子是否为BGT1转运蛋白的底物和/或由BGT1转运蛋白主动转运以及因此穿过血脑屏障的候选底物的测定。 该测定可用于筛选用于治疗或诊断神经疾病的治疗剂，细胞毒性剂或成像化合物。

公开(公告)号：WO2007041268A2

公开(公告)日：2007-04-12

申请号：PCT/US2006/038003

申请日：2006-09-27

Applicant: XENOPORT, INC. ,  ZERANGUE, Noa ,  DOWER, William, J.

Inventor： ZERANGUE, Noa ,  DOWER, William, J.

IPC: C12Q1/68

CPC classification number: G01N33/5011 ,  A61K51/04 ,  A61K51/0402 ,  A61K51/0491 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/136 ,  C12Q2600/158 ,  G01N33/5023 ,  G01N33/57492 ,  G01N33/6872

Abstract: Methods of treating a disease in a patient, methods of determining the presence of a disease in a patient, methods of determining whether a disease in a patient is suitable to be treated with a therapeutic agent, and methods of monitoring treatment of a disease in a patient comprising determining a level of expression of a transporter in cells of a tissue associated with the disease are disclosed. The methods include administering to a patient a diagnostic conjugate and/or therapeutic conjugate that are substrates for a transporter expressed by cells of a tissue associated with the disease. Kits comprising a diagnostic composition comprising a diagnostic conjugate that is a transporter substrate are also disclosed. In particular, methods and kits useful for diagnosing and treating cancer are disclosed.

Abstract translation: 治疗患者疾病的方法，确定患者疾病存在的方法，确定患者疾病是否适合用治疗剂治疗的方法，以及监测患者疾病治疗方法 公开了包括确定与该疾病相关的组织的细胞中的转运蛋白的表达水平的患者。 所述方法包括向患者施用作为由与该疾病相关的组织的细胞表达的转运蛋白底物的诊断缀合物和/或治疗缀合物。 还公开了包含诊断组合物的试剂盒，其包含作为转运体底物的诊断缀合物。 特别地，公开了用于诊断和治疗癌症的方法和试剂盒。

公开(公告)号：WO2005119261A3

公开(公告)日：2005-12-15

申请号：PCT/US2005/020077

申请日：2005-06-06

Applicant: XENOPORT, INC. ,  ZERANGUE, Noa

Inventor： ZERANGUE, Noa

IPC: G01N33/574 ,  A61K31/00 ,  A61K33/24

Abstract: GLUT5 is consistently expressed at high levels in cancer cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is transported by, the GLUT5 transporter, and therefore a candidate substrate for transport into cancer cells. The assays are useful in screening for cytotoxic agents or imaging components used in the treatment or diagnosis of cancer.