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1. 发明授权

US08203004B2 Tetrahydroindole derivatives for treatment of alzheimer's disease 失效
标题翻译：用于治疗阿尔茨海默病的四氢吲哚衍生物
公开(公告)号：US08203004B2
公开(公告)日：2012-06-19
申请号：US12084814
申请日：2006-11-03
申请人： Frank Burkamp , Graham David Checksfield , Stephen Robert Fletcher , Stephen John Lewis , Edward Giles Mciver , Paul Joseph Oakley , Martin Richard Teall
发明人： Frank Burkamp , Graham David Checksfield , Stephen Robert Fletcher , Stephen John Lewis , Edward Giles Mciver , Paul Joseph Oakley , Martin Richard Teall
IPC分类号： C07D209/02 , C07D209/52
CPC分类号： C07D209/30 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/42 , C07D209/86 , C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译：公开了式（I）的四氢吲哚衍生物：这些化合物调节γ-分泌酶的活性，因此可用于治疗或预防阿尔茨海默氏病。

2. 发明申请

US20100016308A1 Tetrahydroindole Derivatives for Treatment of Alzheimer's Disease 失效
标题翻译：用于治疗阿尔茨海默病的四氢吲哚衍生物
公开(公告)号：US20100016308A1
公开(公告)日：2010-01-21
申请号：US12084814
申请日：2006-11-03
申请人： Frank Burkamp , Graham David Checksfield , Stephen Robert Fletcher , Stephen John Lewis , Edward Giles Meiver , Paul Joseph Oakley , Martin Richard Teall
发明人： Frank Burkamp , Graham David Checksfield , Stephen Robert Fletcher , Stephen John Lewis , Edward Giles Meiver , Paul Joseph Oakley , Martin Richard Teall
IPC分类号： A61K31/5377 , C07D209/52 , A61K31/403 , C07D401/04 , A61K31/4439 , C07D413/02
CPC分类号： C07D209/30 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/42 , C07D209/86 , C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译：公开了式（I）的四氢吲哚衍生物：这些化合物调节γ-分泌酶的活性，因此可用于治疗或预防阿尔茨海默氏病。

3. 发明授权

US07365196B2 Sulphonamido-substituted bridged bicycloalkyl derivatives 有权
标题翻译：磺酰氨基取代的桥连双环烷基衍生物
公开(公告)号：US07365196B2
公开(公告)日：2008-04-29
申请号：US10239233
申请日：2001-03-15
申请人： Patrice Charles Belanger , Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Edward Giles McIver , Alan John Nadin , Joseph George Neduvelil , Mark Steven Shearman , Adrian Leonard Smith , Timothy Jason Sparey , Graeme Irvine Stevenson , Martin Richard Teall
发明人： Patrice Charles Belanger , Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Edward Giles McIver , Alan John Nadin , Joseph George Neduvelil , Mark Steven Shearman , Adrian Leonard Smith , Timothy Jason Sparey , Graeme Irvine Stevenson , Martin Richard Teall
IPC分类号： C07D413/14 , C07D413/12 , C07D213/71 , C07D213/52 , C07D333/34 , C07D409/14 , C07D409/12 , C07D249/12 , C07D233/84 , C07D207/48 , C07D277/16 , C07D307/64 , A61P25/28
CPC分类号： C07D213/30 , A61K31/18 , A61K31/40 , C07C311/07 , C07C311/09 , C07C311/11 , C07C311/14 , C07C311/20 , C07C311/24 , C07C323/67 , C07C2601/08 , C07C2601/14 , C07C2602/44 , C07C2602/46 , C07C2603/72 , C07C2603/78 , C07D207/36 , C07D211/14 , C07D211/18 , C07D213/71 , C07D213/81 , C07D215/12 , C07D223/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D271/107 , C07D277/36 , C07D285/14 , C07D285/16 , C07D295/088 , C07D295/135 , C07D295/26 , C07D307/64 , C07D307/81 , C07D319/18 , C07D333/34 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10 , C07D513/10
摘要： A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
摘要翻译：公开了一类化合物，其包含磺酰氨基取代的桥连双环烷基结构。这些化合物是γ-分泌酶的抑制剂，因此可用于治疗和/或预防阿尔茨海默氏病。

4. 发明申请

US20100056524A1 Compound 审中-公开
标题翻译：复合
公开(公告)号：US20100056524A1
公开(公告)日：2010-03-04
申请号：US12384477
申请日：2009-04-02
申请人： Edward Giles Mciver , Justin Stephen Bryans , Ela Smiljanic , Stephen John Lewis , Joanne Hough , Thomas Drake
发明人： Edward Giles Mciver , Justin Stephen Bryans , Ela Smiljanic , Stephen John Lewis , Joanne Hough , Thomas Drake
IPC分类号： A61K31/5377 , C07D239/02 , C07D403/12 , C07D413/12 , A61K31/505 , A61K31/506
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D407/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/04
摘要： A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is C3-8-cycloalkyl; X is O, NR7 or C3-6-heterocycloalkyl; R2 is aryl, heteroaryl, fused or unfused aryl-C3-6-heterocycloalkyl or fused or unfused heteroaryl-C3-6-heterocycloalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C1-6-alkyl, C3-7-cycloalkyl and a group A, wherein said C1-6-alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R10 and a group A, said heteroaryl group is optionally substituted by one or more R10 groups; and wherein said C3-6-heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R3 is C1-6-alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, —NR4R5, —OR6, —NR7(CO)R6, —NR7(CO)NR4R5, —NR7SO2R6, —NR7COOR7, —CONR4R5, C3-6-heterocycloalkyl and wherein R4-7 and A are as defined in the claims.Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of one or more kinases.
摘要翻译：本发明的第一方面涉及式（I）化合物或其药学上可接受的盐或酯，其中：R 1为C 3-8 - 环烷基; X是O，NR 7或C 3-6 - 杂环烷基; R 2是芳基，杂芳基，稠合或未稠合的芳基-C 3-6 - 杂环烷基或稠合或未稠合的杂芳基-C 3-6 - 杂环烷基，其各自任选被一个或多个选自芳基，杂芳基，C 1-6 - 烷基 C 3-7 - 环烷基和基团A，其中所述C 1-6 - 烷基任选被一个或多个选自芳基，杂芳基，R 10和A基团的取代基取代，所述杂芳基任选地被一个或多个R 10 团体并且其中所述C 3-6杂环烷基任选地含有一个或多个选自氧，硫，氮和CO的基团; R 3是任选被一个或多个选自芳基，杂芳基，-NR 4 R 5，-OR 6，-NR 7（CO）R 6，-NR 7（CO）NR 4 R 5，-NR 7 SO 2 R 6，-NR 7 COOR 7，-CONR 4 R 5，C 3 -6-杂环烷基，其中R 4-7和A如权利要求中所定义。其它方面涉及所述化合物在治疗各种治疗性疾病中的用途，更具体地涉及一种或多种激酶的抑制剂。

5. 发明授权

US06486153B1 Phenylindole derivatives as 5-HT2A receptor ligands 失效
标题翻译：苯基吲哚衍生物作为5-HT2A受体配体
公开(公告)号：US06486153B1
公开(公告)日：2002-11-26
申请号：US09508046
申请日：2000-03-03
申请人： Jose Luis Castro Pineiro , Steven Michael Hutchins , Stephen John Lewis , Michael Rowley , Adrian Leonard Smith , Graeme Irvine Stevenson
发明人： Jose Luis Castro Pineiro , Steven Michael Hutchins , Stephen John Lewis , Michael Rowley , Adrian Leonard Smith , Graeme Irvine Stevenson
IPC分类号： C07D20914
CPC分类号： C07D401/06 , C07D209/16 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D491/04
摘要： A class of tryptamine analogues bearing an optionally substituted phenyl nucleus at the 2-position are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse neurological conditions, including psychotic disorders such as schizophrenia.
摘要翻译：在2-位上带有任选取代的苯基核的一类色胺类似物是人5-HT 2A受体的选择性拮抗剂，因此可用作药物，特别是用于治疗和/或预防不良神经病症，包括精神病性疾病如精神分裂症。

6. 发明授权

US07359325B1 Method and apparatus for inserting empty memory cells into a data flow of network connections of a computer network 有权
标题翻译：将空的存储器单元插入到计算机网络的网络连接的数据流中的方法和装置
公开(公告)号：US07359325B1
公开(公告)日：2008-04-15
申请号：US10045290
申请日：2001-10-18
申请人： Stephen John Lewis , Nils Ramon Marchant , Mike Reynolds
发明人： Stephen John Lewis , Nils Ramon Marchant , Mike Reynolds
IPC分类号： H04L12/26
CPC分类号： H04L41/0896
摘要： A method and an apparatus are provided for inserting empty memory cells into a data flow of network connections of a computer network. In one example, the method includes receiving an insertion request for an empty memory cell to be inserted into the data flow. A base connection identification (CID) associated with the insertion request is also received. An appropriate insertion scheme for carrying out the insertion request is determined. Based on the appropriate insertion scheme, the insertion request is sent to an insertion device that is configured to insert the empty memory cell into the data flow. The memory cell is inserted prior to traffic shaping of the data flow.
摘要翻译：提供了一种用于将空的存储器单元插入到计算机网络的网络连接的数据流中的方法和装置。在一个示例中，该方法包括接收对要插入到数据流中的空的存储器单元的插入请求。还接收与插入请求相关联的基本连接标识（CID）。确定用于执行插入请求的适当插入方案。基于适当的插入方案，插入请求被发送到被配置为将空的存储器单元插入到数据流中的插入装置。在数据流的流量整形之前插入存储单元。

7. 发明授权

US07138400B2 Sulfamides as gamma-secretase inhibitors 有权
标题翻译：磺酰胺作为γ-分泌酶抑制剂
公开(公告)号：US07138400B2
公开(公告)日：2006-11-21
申请号：US10415751
申请日：2001-10-29
申请人： Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Timothy Jason Sparey , Brian John Williams
发明人： Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Timothy Jason Sparey , Brian John Williams
IPC分类号： C07D211/18 , C07D285/10 , A61K31/435 , A61K31/433
CPC分类号： C07D249/08 , A61K31/18 , A61K31/40 , C07C307/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07C2602/44 , C07C2602/46 , C07C2603/72 , C07C2603/78 , C07D207/36 , C07D211/14 , C07D211/18 , C07D213/30 , C07D213/71 , C07D213/81 , C07D215/12 , C07D223/32 , C07D231/12 , C07D233/56 , C07D271/107 , C07D277/36 , C07D285/14 , C07D285/16 , C07D295/088 , C07D295/135 , C07D295/26 , C07D307/64 , C07D307/81 , C07D319/18 , C07D333/34 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10 , C07D513/10
摘要： Novel sulfamides of formula (I) are disclosed. The compounds exert an inhibitory action on the processing of APP by gamma-secretase, and are therefore useful in the treatment or prevention of Alzheimer's disease.
摘要翻译：公开了式（I）的新型磺酰胺。该化合物通过γ-分泌酶对APP的加工发挥抑制作用，因此可用于治疗或预防阿尔茨海默氏病。

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