公开(公告)号：WO2005108949A3

公开(公告)日：2006-07-20

申请号：PCT/EP2005052186

申请日：2005-05-12

Applicant: GALAPAGOS NV ,  LAENEN WENDY ,  SPITTAELS KOENRAAD FREDERIK FL ,  HOFFMANN MARCEL ,  MERCHIERS PASCAL GERARD

Inventor： SPITTAELS KOENRAAD FREDERIK FL ,  HOFFMANN MARCEL ,  MERCHIERS PASCAL GERARD

IPC: G01N33/68 ,  A61K48/00 ,  C12Q1/00 ,  C12Q1/25 ,  C12Q1/48 ,  C12Q1/68 ,  G01N20060101 ,  G01N33/53 ,  G01N33/567 ,  G01N33/74

CPC classification number: C12Q1/37 ,  A61K48/00 ,  C12Q1/25 ,  C12Q1/485 ,  G01N33/6896 ,  G01N33/74 ,  G01N2333/4709 ,  G01N2333/726 ,  G01N2333/9015 ,  G01N2500/00 ,  G01N2500/02 ,  G01N2500/04 ,  G01N2800/2821

Abstract: A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a PROTEASE polypeptide, or fragment thereof, and measuring a compound-PROTEASE property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including cleaved protease substrate and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of PROTEASE expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimer's disease.

Abstract translation: 一种用于鉴定抑制细胞中淀粉样蛋白β前体蛋白加工的化合物的方法，包括使测试化合物与PROTEASE多肽或其片段接触，并测量与淀粉状蛋白-β肽的产生相关的化合物-PRTETEASE性质。 所述方法的细胞测定测量指标，包括切割的蛋白酶底物和/或淀粉样蛋白β肽水平。 包括有效的淀粉样蛋白β前体加工抑制量的PROTEASE表达抑制剂的治疗方法和药物组合物可用于治疗涉及认知障碍的症状如阿尔茨海默病。

公开(公告)号：WO2005109002A3

公开(公告)日：2006-05-04

申请号：PCT/EP2005052188

申请日：2005-05-12

Applicant: GALAPAGOS NV ,  LAENEN WENDY ,  SPITTAELS KOENRAAD FREDERIK FL ,  HOFFMANN MARCEL ,  MERCHIERS PASCAL GERARD

Inventor： SPITTAELS KOENRAAD FREDERIK FL ,  HOFFMANN MARCEL ,  MERCHIERS PASCAL GERARD

IPC: A61K48/00 ,  C12Q1/00 ,  C12Q1/25 ,  C12Q1/48 ,  C12Q1/68 ,  G01N20060101 ,  G01N33/53 ,  G01N33/567 ,  G01N33/68 ,  G01N33/74

CPC classification number: C12Q1/37 ,  A61K48/00 ,  C12Q1/25 ,  C12Q1/485 ,  G01N33/6896 ,  G01N33/74 ,  G01N2333/4709 ,  G01N2333/726 ,  G01N2333/9015 ,  G01N2500/00 ,  G01N2500/02 ,  G01N2500/04 ,  G01N2800/2821

Abstract: A method for identifying compounds that inhibit aberrant amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a LIGASE polypeptide, or fragment thereof, and measuring a compound-LIGASE property related to the production of amyloid-beta peptide. Cellular assays of the method measure amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of LIGASE DNA expression agents or LIGASE agonists, are useful for treating conditions involving cognitive impairment such as Alzheimers Disease.

Abstract translation: 一种用于鉴定抑制细胞中异常淀粉样蛋白β前体蛋白加工的化合物的方法，包括使测试化合物与LIGASE多肽或其片段接触，并测量与淀粉状蛋白-β肽的生产相关的化合物-LIGASE性质。 该方法的细胞测定法测量淀粉样β肽水平。 包括有效的淀粉样蛋白β前体加工抑制量的LIGASE DNA表达剂或LIGASE激动剂的治疗方法和药物组合物可用于治疗涉及认知障碍的疾病如阿尔茨海默病。

公开(公告)号：WO2005109000A2

公开(公告)日：2005-11-17

申请号：PCT/EP2005/052173

申请日：2005-05-12

Applicant: GALAPAGOS GENOMICS N.V. ,  LAENEN, Wendy ,  SPITTAELS, Koenraad, Frederik, Florentina ,  HOFFMANN, Marcel ,  MERCHIERS, Pascal, Gerard

Inventor： SPITTAELS, Koenraad, Frederik, Florentina ,  HOFFMANN, Marcel ,  MERCHIERS, Pascal, Gerard

IPC: G01N33/68

CPC classification number: C12Q1/37 ,  A61K48/00 ,  C12Q1/25 ,  C12Q1/485 ,  G01N33/6896 ,  G01N33/74 ,  G01N2333/4709 ,  G01N2333/726 ,  G01N2333/9015 ,  G01N2500/00 ,  G01N2500/02 ,  G01N2500/04 ,  G01N2800/2821

Abstract: A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a GPCR polypeptide, or fragment thereof, and measuring a compound-GPCR property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including second messenger and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of GPCR expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimers Disease.

Abstract translation: 鉴定抑制细胞中淀粉样蛋白β前体蛋白加工的化合物的方法，包括使测试化合物与GPCR多肽或其片段接触，并测量与淀粉状蛋白-β肽的生产相关的化合物-GPCR性质。 该方法的细胞测定法测量包括第二信使和/或淀粉样蛋白β肽水平的指标。 包括有效的淀粉样蛋白-β前体加工抑制量的GPCR表达抑制剂的治疗方法和药物组合物可用于治疗涉及认知障碍的疾病如阿尔茨海默病。

公开(公告)号：WO2005103715A2

公开(公告)日：2005-11-03

申请号：PCT/EP2005/051882

申请日：2005-04-26

Applicant: GALAPAGOS GENOMICS N.V. ,  SPITTAELS, Koenraad, Frederik, Florentina ,  HOFFMANN, Marcel ,  MERCHIERS, Pascal, Gerard

Inventor： SPITTAELS, Koenraad, Frederik, Florentina ,  HOFFMANN, Marcel ,  MERCHIERS, Pascal, Gerard

IPC: G01N33/68

CPC classification number: C12N15/1138 ,  C12N2310/111 ,  C12N2310/14 ,  C12N2310/53 ,  G01N2333/4709 ,  G01N2500/04

Abstract: A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a melanocortin receptor polypeptide, or fragment thereof, and measuring a compound-polypeptide property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including second messenger and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of melanocortin receptor inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimers Disease.

Abstract translation: 一种用于鉴定抑制细胞中淀粉样蛋白β前体蛋白处理的化合物的方法，包括使测试化合物与黑皮质素受体多肽或其片段接触，并测量与淀粉状蛋白-β肽的产生相关的化合物 - 多肽性质。 该方法的细胞测定法测量包括第二信使和/或淀粉样蛋白β肽水平的指标。 包括有效的淀粉样蛋白β前体加工抑制量的黑皮质素受体抑制剂的治疗方法和药物组合物可用于治疗涉及认知障碍的疾病如阿尔茨海默病。

公开(公告)号：WO2005024057A1

公开(公告)日：2005-03-17

申请号：PCT/EP2003/010160

申请日：2003-09-10

Applicant: GALAPAGOS GENOMICS N.V. ,  MERCHIERS, Pascal, Gerard ,  SPITTAELS, Koenraad, Frederik, Florentina ,  HOFFMANN, Marcel ,  THYS, Kim ,  LAENEN, Wendy

Inventor： MERCHIERS, Pascal, Gerard ,  SPITTAELS, Koenraad, Frederik, Florentina ,  HOFFMANN, Marcel ,  THYS, Kim ,  LAENEN, Wendy

IPC: C12Q1/68

CPC classification number: C12N15/113 ,  A61K38/00 ,  C07K7/06 ,  C07K14/605 ,  C07K14/705 ,  C12N15/1138 ,  C12N2310/111 ,  C12N2310/14 ,  C12N2310/53 ,  C12Q1/6883 ,  C12Q2600/136 ,  C12Q2600/158 ,  G01N33/6896 ,  G01N2800/2821

Abstract: The present invention relates to methods of identifying a compound that changes the amyloid-beta precursor protein processing in a cell. The invention also relates to methods for changing the amyloid-beta precursor protein processing of a cell, and a method for diagnosing a pathological condition involving cognitive impairment or susceptibility to this condition in a subject.

Abstract translation: 本发明涉及鉴定改变细胞中淀粉样蛋白β前体蛋白处理的化合物的方法。 本发明还涉及用于改变细胞的淀粉样蛋白β前体蛋白加工的方法，以及用于诊断受试者涉及认知障碍或对该病症的敏感性的病理状态的方法。

公开(公告)号：WO2008101985A2

公开(公告)日：2008-08-28

申请号：PCT/EP2008/052119

申请日：2008-02-21

Applicant: ABLYNX N.V. ,  MERCHIERS, Pascal Gerard ,  VERHEESEN, Peter ,  HOOGENBOOM, Hendricus Renerus Jacobus Mattheus

Inventor： MERCHIERS, Pascal Gerard ,  VERHEESEN, Peter ,  HOOGENBOOM, Hendricus Renerus Jacobus Mattheus

IPC: C07K16/22 ,  A61K39/395

CPC classification number: C07K16/22 ,  C07K2317/22 ,  C07K2317/569 ,  C07K2317/73 ,  C07K2317/76 ,  C07K2317/92

Abstract: The present invention relates to amino acid sequences that are directed against vascular endothelial growth factor (VEGF), as well as to compounds or constructs, and in particular proteins and polypeptides, that comprise or essentially consist of one or more such amino acid sequences. The amino acid sequences, compounds and constructs can be used for prophylactic, therapeutic or diagnostic purposes, such as for the treatment of conditions and diseases characterized by excessive and/or pathological angiogenesis or neovascularization.

Abstract translation: 本发明涉及针对血管内皮生长因子（VEGF）的氨基酸序列以及化合物或构建体，特别是蛋白质和多肽，其包含一种或基本上由一种 或更多这样的氨基酸序列。 氨基酸序列，化合物和构建体可用于预防，治疗或诊断目的，例如用于治疗以过度和/或病理性血管生成或新血管形成为特征的病症和疾病。

公开(公告)号：WO2005109001A3

公开(公告)日：2006-07-13

申请号：PCT/EP2005052182

申请日：2005-05-12

Applicant: GALAPAGOS NV ,  LAENEN WENDY ,  SPITTAELS KOENRAAD FREDERIK FL ,  HOFFMANN MARCEL ,  MERCHIERS PASCAL GERARD

Inventor： SPITTAELS KOENRAAD FREDERIK FL ,  HOFFMANN MARCEL ,  MERCHIERS PASCAL GERARD

IPC: G01N33/68 ,  A61K31/00 ,  A61K48/00 ,  C12Q1/00 ,  C12Q1/25 ,  C12Q1/48 ,  C12Q1/68 ,  G01N20060101 ,  G01N33/53 ,  G01N33/567 ,  G01N33/74

CPC classification number: C12Q1/37 ,  A61K48/00 ,  C12Q1/25 ,  C12Q1/485 ,  G01N33/6896 ,  G01N33/74 ,  G01N2333/4709 ,  G01N2333/726 ,  G01N2333/9015 ,  G01N2500/00 ,  G01N2500/02 ,  G01N2500/04 ,  G01N2800/2821

Abstract: A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a KINASE polypeptide, or fragment thereof, and measuring a compound-KINASE property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including phosphorylated kinase substrate and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing­inhibiting amounts of KINASE expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimer's disease.

Abstract translation: 一种用于鉴定抑制细胞中淀粉样蛋白β前体蛋白处理的化合物的方法，包括使测试化合物与KINASE多肽或其片段接触，并测量与淀粉状蛋白-β肽的产生相关的化合物 - KINASE性质。 所述方法的细胞测定法包括磷酸化激酶底物和/或淀粉状蛋白β肽水平。 包括有效的淀粉状蛋白-β前体加工抑制量的KINASE表达抑制剂的治疗方法和药物组合物可用于治疗涉及认知障碍的症状如阿尔茨海默病。

公开(公告)号：WO2005103692A3

公开(公告)日：2006-06-01

申请号：PCT/EP2005004323

申请日：2005-04-20

Applicant: GALAPAGOS NV ,  MERCHIERS PASCAL GERARD ,  SPITTAELS KOENRAAD FREDERIK FL

Inventor： MERCHIERS PASCAL GERARD ,  SPITTAELS KOENRAAD FREDERIK FL

IPC: G01N33/50 ,  A61K48/00 ,  C12N15/113 ,  C12Q1/48 ,  C12Q1/68 ,  G01N33/53 ,  G01N33/68

CPC classification number: C12N15/1137 ,  C12N2310/111 ,  C12N2310/14 ,  C12N2799/022 ,  C12Q1/485 ,  C12Y207/01091 ,  G01N33/6896 ,  G01N2500/04 ,  G01N2500/10

Abstract: A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a SPHK polypeptide, or fragment thereof, and measuring a compound-SPHK property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including phosphorylated kinase substrate and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of SPHK expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimer's Disease.

Abstract translation: 用于鉴定抑制细胞中淀粉样蛋白β前体蛋白处理的化合物的方法，包括使测试化合物与SPHK多肽或其片段接触，并测量与淀粉状蛋白-β肽的产生相关的化合物-SPHK性质。 所述方法的细胞测定法包括磷酸化激酶底物和/或淀粉状蛋白β肽水平。 包括有效淀粉样蛋白β前体加工抑制量的SPHK表达抑制剂的治疗方法和药物组合物可用于治疗涉及认知障碍的症状如阿尔茨海默病。

公开(公告)号：WO2005103693A2

公开(公告)日：2005-11-03

申请号：PCT/EP2005/051883

申请日：2005-04-26

Applicant: GALAPAGOS GENOMICS N.V. ,  SPITTAELS, Koenraad, Frederik, Florentina ,  HOFFMANN, Marcel ,  MERCHIERS, Pascal, Gerard

Inventor： SPITTAELS, Koenraad, Frederik, Florentina ,  HOFFMANN, Marcel ,  MERCHIERS, Pascal, Gerard

IPC: G01N33/50

CPC classification number: C12N15/86 ,  C12N2710/10343 ,  C12N2830/002 ,  G01N33/6896 ,  G01N2333/4709

Abstract: A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a vasopressin receptor polypeptide, or fragment thereof, and measuring a compound-polypeptide property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including second messenger and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of vasopressin receptor expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimers Disease.

Abstract translation: 鉴定抑制细胞中淀粉样蛋白β前体蛋白加工的化合物的方法，包括使测试化合物与血管加压素受体多肽或其片段接触，并测量与淀粉状蛋白-β肽的产生相关的化合物 - 多肽性质。 该方法的细胞测定法测量包括第二信使和/或淀粉样蛋白β肽水平的指标。 包括有效的淀粉样蛋白β前体加工抑制量的加压素受体表达抑制剂的治疗方法和药物组合物可用于治疗涉及认知障碍的疾病如阿尔茨海默病。

公开(公告)号：WO2005119262A3

公开(公告)日：2006-06-15

申请号：PCT/EP2005052421

申请日：2005-05-27

Applicant: GALAPAGOS NV ,  MERCHIERS PASCAL GERARD ,  HINNEKINT SOFIE ,  SPITTAELS KOENRAAD FREDERIK FL

Inventor： MERCHIERS PASCAL GERARD ,  HINNEKINT SOFIE ,  SPITTAELS KOENRAAD FREDERIK FL

IPC: G01N33/68

CPC classification number: G01N33/6896

Abstract: A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a HIT polypeptide, or fragment thereof, and measuring a compound-HIT property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including cleaved protease substrates, phosphorylated kinase substrate, second messenger levels and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of HIT expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimer's disease.

Abstract translation: 用于鉴定抑制细胞中淀粉样蛋白β前体蛋白处理的化合物的方法，包括使测试化合物与HIT多肽或其片段接触，并测量与淀粉状蛋白-β肽的产生相关的化合物-HIT性质。 所述方法的细胞测定包括切割的蛋白酶底物，磷酸化激酶底物，第二信使水平和/或淀粉样蛋白β肽水平的指标。 包括有效的淀粉样蛋白β前体加工抑制量的HIT表达抑制剂的治疗方法和药物组合物可用于治疗涉及认知障碍的症状如阿尔茨海默病。