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1. 发明授权

US07825160B2 (Biphenyl) carboxylic acids and derivatives thereof 有权
标题翻译：（联苯）羧酸及其衍生物
公开(公告)号：US07825160B2
公开(公告)日：2010-11-02
申请号：US11665760
申请日：2005-10-21
申请人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline Leformal , Andrew Cansfield , Svenja Burckhardt
发明人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline Leformal , Andrew Cansfield , Svenja Burckhardt
IPC分类号： A01N37/10 , A61K31/19 , A01N37/08 , A01N53/00 , A61K31/557 , C07C63/00 , C07C65/00 , C07C63/33 , C07C63/333 , C07C61/04 , C07C61/16 , C07C62/00
CPC分类号： C07C59/68 , C07C59/72 , C07C233/54 , C07C235/42 , C07C311/29 , C07C317/22 , C07C317/46 , C07C2601/02 , C07C2601/14 , C07D261/08 , C07D295/192 , C07D295/26 , C07D309/06
摘要： The present invention relates to compounds having the general formula (I) with the definitions of A, X, R1-R6 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.
摘要翻译：本发明涉及具有通式（I）的具有下述A，X，R 1 -R 6的定义的化合物和/或其盐或酯。此外，本发明涉及所述化合物用于治疗阿尔茨海默氏病及其用于调节γ-分泌酶活性的用途。

2. 发明申请

US20090220992A1 METHODS FOR THE IDENTIFICATION OF LRRK2 INTERACTING MOLECULES AND FOR THE PURIFICATION OF LRRK2 失效
标题翻译： LRRK2相互作用分子鉴定方法及LRRK2纯化方法
公开(公告)号：US20090220992A1
公开(公告)日：2009-09-03
申请号：US12282851
申请日：2007-03-13
申请人： Gerard Drewes , Carsten Hopf , Valerie Reader
发明人： Gerard Drewes , Carsten Hopf , Valerie Reader
IPC分类号： G01N33/573 , C07D403/04 , C12N9/12
CPC分类号： C12Q1/485 , G01N2800/2835
摘要： The invention provides in a first aspect a method for the identification of an LRRK2 interacting compound, comprising the steps of providing a protein preparation containing LRRK2, contacting the protein preparation with indol ligand 91 immobilized on a solid support under conditions allowing the formation of an indol ligand 91-LRRK2 complex, incubating the indol ligand 91-LRRK2 complex with a given compound, and determining whether the compound is able to separate LRRK2 from the immobilized indol ligand 91. Furthermore, the invention relates to a method for the identification of an LRRK2 interacting compound, comprising the steps of providing a protein preparation containing LRRK2, contacting the protein preparation with indol ligand 91 immobilized on a solid support and with a given compound under conditions allowing the formation of an indol ligand 91-LRRK2 complex, and detecting the indol ligand 91-LRRK2 complex. Additionally, the invention provides a method for the identification of an LRRK2 interacting compound, comprising the steps of providing two aliquots of a protein preparation containing LRRK2, contacting one aliquot with indol ligand 91 immobilized on a solid support under conditions allowing the formation of an indol ligand 91-LRRK2 complex, contacting the other aliquot with indol ligand 91 immobilized on a solid support and with a given compound under conditions allowing the formation of an indol ligand 91-LRRK2 complex, and determining the amount of indol ligand 91-LRRK2 complex. Furthermore, the invention relates to a method for the purification of LRRK2, comprising the steps of providing a protein preparation containing LRRK2, contacting the protein preparation with indol ligand 91 immobilized on a solid support under conditions allowing the formation of an indol ligand 91-LRRK2 complex, and separating LRRK2 from the immobilized indol ligand 91.
摘要翻译：本发明在第一方面提供了一种用于鉴定LRRK2相互作用化合物的方法，包括以下步骤：提供含有LRRK2的蛋白质制剂，使所述蛋白质制剂与固定在固体支持物上的吲哚配体91接触，所述条件允许形成吲哚配体91-LRRK2复合物，将吲哚配体91-LRRK2复合物与给定化合物一起温育，并测定化合物是否能够从固定的吲哚配体91分离LRRK2。此外，本发明涉及用于鉴定LRRK2的方法包括以下步骤：提供含有LRRK2的蛋白质制剂，使蛋白质制备物与固定在固体载体上的吲哚配体91与允许形成吲哚配体91-LRRK2复合物的条件下的给定化合物接触，并检测吲哚配体91-LRRK2复合物。另外，本发明提供了一种用于鉴定LRRK2相互作用化合物的方法，包括以下步骤：提供含有LRRK2的蛋白质制剂的两个等分试样，将一个等分试样与固定在固体支持物上的吲哚配体91接触，形成吲哚配体91-LRRK2复合物，使其它等分试样与固定在固体载体上的吲哚配体91与给定化合物在允许形成吲哚配体91-LRRK2复合物的条件下接触，并测定吲哚配体91-LRRK2复合物的量。此外，本发明涉及LRRK2的纯化方法，包括以下步骤：提供含有LRRK2的蛋白质制剂，使蛋白质制剂与固定在固体支持物上的吲哚配体91接触，形成吲哚配体91-LRRK2 复合物，并将LRRK2与固定的吲哚配体91分离。

3. 发明申请

US20070254957A1 TRIARYL COMPOUNDS AND DERIVATES THEREOF 有权
标题翻译：三环化合物及其衍生物
公开(公告)号：US20070254957A1
公开(公告)日：2007-11-01
申请号：US11737475
申请日：2007-04-19
申请人： Francis WILSON , Alison Reid , Valerie Reader , Richard Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Yan Zhang , Chih Ho
发明人： Francis WILSON , Alison Reid , Valerie Reader , Richard Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Yan Zhang , Chih Ho
IPC分类号： A61K31/192 , C07C59/40 , C07C62/30
CPC分类号： C07D257/04 , C07C51/09 , C07C57/38 , C07C57/58 , C07C59/56 , C07C59/64 , C07C63/331 , C07C69/65
摘要： The present invention relates to compounds having the general formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, R10 given below, and solvates, hydrates, esters, and pharmaceutically acceptable salts thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.
摘要翻译：本发明涉及具有通式（I）的化合物，其具有X，Y，R 1，R 2，R 3，R 3， R 4，R 9，R 10，及其溶剂合物，水合物，酯和药学上可接受的盐。此外，本发明涉及所述化合物用于治疗阿尔茨海默氏病及其用于调节γ-分泌酶活性的用途。

4. 发明申请

US20090118289A1 (Biphenyl) Carboxylic Acids and Derivatives Thereof 有权
标题翻译：（联苯）羧酸及其衍生物
公开(公告)号：US20090118289A1
公开(公告)日：2009-05-07
申请号：US11665760
申请日：2005-10-21
申请人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline Leformal , Andrew Cansfield , Svenja Burckhardt
发明人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline Leformal , Andrew Cansfield , Svenja Burckhardt
IPC分类号： A61K31/19 , C07C59/68 , C07D207/12 , C07D261/06 , C07D265/30 , A61P25/28 , A61K31/5375 , A61K31/40 , A61K31/42
CPC分类号： C07C59/68 , C07C59/72 , C07C233/54 , C07C235/42 , C07C311/29 , C07C317/22 , C07C317/46 , C07C2601/02 , C07C2601/14 , C07D261/08 , C07D295/192 , C07D295/26 , C07D309/06
摘要： The present invention relates to compounds having the general formula (I) with the definitions of A, X, R1-R6 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.
摘要翻译：本发明涉及具有通式（I）的具有下述A，X，R 1 -R 6的定义的化合物和/或其盐或酯。此外，本发明涉及所述化合物用于治疗阿尔茨海默氏病及其用于调节γ-分泌酶活性的用途。

5. 发明申请

US20070293567A1 SUBSTITUTED BIPHENYL CARBOXYLIC ACIDS AND DERIVATIVES THEREOF 失效
标题翻译：取代的联苯二羧酸及其衍生物
公开(公告)号：US20070293567A1
公开(公告)日：2007-12-20
申请号：US11737938
申请日：2007-04-20
申请人： Francis WILSON , Alison Reid , Valerie Reader , Richard Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Chih Ho , Yan Zhang
发明人： Francis WILSON , Alison Reid , Valerie Reader , Richard Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Chih Ho , Yan Zhang
IPC分类号： A61K31/196 , A61K31/24 , A61P25/28 , C07C229/28
CPC分类号： C07C229/42 , C07C59/68
摘要： The present invention relates to compounds having the general Formula (I) with the definitions of X, Y, R1, R2, R3, R4 R9, and R10 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.
摘要翻译：本发明涉及具有通式（I）的化合物，其具有X，Y，R 1，R 2，R 3，，R 4 R 9和R 10，和/或其盐或酯。此外，本发明涉及所述化合物用于治疗阿尔茨海默氏病及其用于调节γ-分泌酶活性的用途。

6. 发明授权

US08106236B2 Triaryl compounds and derivates thereof 有权
标题翻译：三芳基化合物及其衍生物
公开(公告)号：US08106236B2
公开(公告)日：2012-01-31
申请号：US11737475
申请日：2007-04-19
申请人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Yan Zhang , Chih Yung Ho
发明人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Yan Zhang , Chih Yung Ho
IPC分类号： C07C63/00
CPC分类号： C07D257/04 , C07C51/09 , C07C57/38 , C07C57/58 , C07C59/56 , C07C59/64 , C07C63/331 , C07C69/65
摘要： The present invention relates to compounds having the general formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, R10 given below, and solvates, hydrates, esters, and pharmaceutically acceptable salts thereof.Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.
摘要翻译：本发明涉及具有以下给出的X，Y，R 1，R 2，R 3，R 4，R 9，R 10的定义的通式（I）的化合物及其溶剂化物，水合物，酯和药学上可接受的盐。此外，本发明涉及所述化合物用于治疗阿尔茨海默氏病及其用于调节γ-分泌酶活性的用途。

7. 发明申请

US20110070595A1 METHODS FOR THE IDENTIFICATION OF PARP INTERACTING MOLECULES AND FOR PURIFICATION OF PARP PROTEINS 审中-公开
标题翻译：用于鉴定PARP相互作用分子和用于纯化PARP蛋白的方法
公开(公告)号：US20110070595A1
公开(公告)日：2011-03-24
申请号：US12993071
申请日：2009-05-14
申请人： Gerard Drewes , Valerie Reader
发明人： Gerard Drewes , Valerie Reader
IPC分类号： G01N33/573 , C07D471/04 , C12N9/10 , C08B37/00
CPC分类号： G01N33/573 , C07D471/04 , G01N2333/9125 , G01N2500/04
摘要： The present invention relates to immobilization compounds and methods useful for the identification of PARP interacting compounds or for the purification or identification of PARP proteins.
摘要翻译：本发明涉及用于鉴定PARP相互作用化合物或用于纯化或鉴定PARP蛋白质的固定化合物和方法。

8. 发明授权

US07557244B2 Substituted biphenyl carboxylic acids and derivatives thereof 失效
标题翻译：取代的联苯羧酸及其衍生物
公开(公告)号：US07557244B2
公开(公告)日：2009-07-07
申请号：US11737938
申请日：2007-04-20
申请人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernadez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Chih Yung Ho , Yan Zhang
发明人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernadez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Chih Yung Ho , Yan Zhang
IPC分类号： C07C321/00 , C07C229/00 , C07C59/00 , C07D249/08 , A01N43/64 , A01N37/10
CPC分类号： C07C229/42 , C07C59/68
摘要： The present invention relates to compounds having the general Formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, and R10 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.
摘要翻译：本发明涉及具有以下给出的X，Y，R 1，R 2，R 3，R 4，R 9和R 10的定义的通式（I）的化合物和/或其盐或酯。此外，本发明涉及所述化合物用于治疗阿尔茨海默氏病及其用于调节γ-分泌酶活性的用途。

9. 发明申请

US20140179664A1 Heterocyclyl Pyrimidine Analogues As JAK Inhibitors 审中-公开
标题翻译：杂环嘧啶类似物作为JAK抑制剂
公开(公告)号：US20140179664A1
公开(公告)日：2014-06-26
申请号：US14234662
申请日：2012-07-24
申请人： Jay Freeman , Valerie Reader , Glynn Addison , Nigel Ramsden , Jane Elizabeth Scanlon , Richard John Harrison
发明人： Jay Freeman , Valerie Reader , Glynn Addison , Nigel Ramsden , Jane Elizabeth Scanlon , Richard John Harrison
IPC分类号： C07D491/107 , C07D403/14 , C07D413/14 , C07D403/12
CPC分类号： C07D491/107 , C07D403/12 , C07D403/14 , C07D413/14 , C07D491/10
摘要： The present invention relates to compounds of formula (I) wherein X1 to X5, Z1 to Z3, Y0, RY1, RY2 and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及其中X1至X5，Z1至Z3，Y0，RY1，RY2和R具有在说明书和权利要求书中引用的含义的式（I）化合物。所述化合物可用作JAK抑制剂，用于治疗或预防免疫学，炎症，自身免疫，过敏性疾病和免疫介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

10. 发明授权

US08163511B2 Methods for the identification of LRRK2 interacting molecules 失效
标题翻译：鉴定LRRK2相互作用分子的方法
公开(公告)号：US08163511B2
公开(公告)日：2012-04-24
申请号：US12282851
申请日：2007-03-13
申请人： Gerard Drewes , Carsten Hopf , Valerie Reader
发明人： Gerard Drewes , Carsten Hopf , Valerie Reader
IPC分类号： G01N33/53 , G01N33/542 , G01N33/566 , G01N33/567
CPC分类号： C12Q1/485 , G01N2800/2835
摘要： The invention features methods for the identification of leucine-rich kinase 2 (LRRK2) inhibitors using indol ligand 91. Generally, these methods include identifying compounds that compete with indol ligand 91 for binding to LRRK2.
摘要翻译：本发明的特征在于使用吲哚配体91鉴定富含亮氨酸激酶2（LRRK2）抑制剂的方法。通常，这些方法包括鉴定与吲哚配体91竞争结合LRRK2的化合物。

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