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1. 发明申请

WO2007007069A1 AZACYCLIC COMPOUNDS AS INHIBITORS OF SENSORY NEURONE SPECIFIC SODIUM CHANNELS 审中-公开
标题翻译：作为感觉神经元特异性钠通道的抑制剂的AZACYCLIC化合物
公开(公告)号：WO2007007069A1
公开(公告)日：2007-01-18
申请号：PCT/GB2006/002539
申请日：2006-07-07
申请人： VERNALIS (R & D) LIMITED , HAMLYN, Richard , ADDISON, Glyn , EARNSHAW, Christopher, Geoffrey , FINCH, Harry , HUCKSTEP, Mike , LYNCH, Rosemary , MELLOR, Sarah
发明人： HAMLYN, Richard , ADDISON, Glyn , EARNSHAW, Christopher, Geoffrey , FINCH, Harry , HUCKSTEP, Mike , LYNCH, Rosemary , MELLOR, Sarah
IPC分类号： C07D487/08 , C07D487/04 , C07D487/10 , A61K31/407
CPC分类号： C07D487/04 , C07D487/08 , C07D487/10
摘要： Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents; wherein (1) represents (A), (B) or (C); R 1 represents: (a)-L-A or L’-A’ wherein L represents a bond or a C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl moiety, A represents a phenyl, 5-to 10-membered heteroaryl, C 3 -C 6 carbocyclyl or 5-to 10 membered heterocyclyl group, L’ represents a C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl moiety, and A’ represents -Het-A or-X-A wherein Het represents -O-, -S- or NR’, and X represents -CO-, -SO-, SO 2 -, -CO-O-, CO-S, CONR’, -O-CO-, -S-CO-or NR’-CO-, wherein R’ represents hydrogen or C 1 -C 6 alkyl; (b)-L-A-A’ or -L-A-L-A wherein A’ is as defined above , each A is the same or different and is as defined above and each L is the same or different and is as defined above; (c) -A-Z-A wherein Z is -Het-L’, -X-L’, -L’-Het-or L’-X, wherein Het, L’ and X are as defined above and each A is the same or different and is as defined above; (d) -A-Het-Y or -A-X-Y wherein is [L’-Het] n -L’, [L’-Het] n -L’, -[L’-Het] n -A, -L’-B-L’, -L’-B-A or -A-L-A wherein n is from 1 to 4 and B is -X-, -NR’-CO-NR’, -O-CO-NR’- or -NR’-CO-O, and wherein X and L are as defined above, each A is the same or different and is as defined above, each L’ is the same or different and is as defined above, each R’ is the same or different and is as defined above and each Het is the same or different and is as defined above; or (e) -L-CR(A)(A’) or L-CR(A)(L-A) wherein R is hydrogen or C 1 -C 4 alkyl, A’ is as defined above, each L is the same or different and is as defined above and each A is the same or different and is as defined above; R 2 represents -L-A-, L’-A’, -L-A-A’ or L-A-L-A wherein L’ and A’ are as defined above, each L is the same or different and is as defined above and each A is the same or different and is as defined above J represents -NR 3 -, -O- or a direct bond wherein R 3 represent s hydrogen C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; p is an integer from 1 to 3; q is 1 or 2; and one of E and E’ is -CH 2 - and the other is a direct bond.
摘要翻译：发现式（I）化合物及其药学上可接受的盐是SNS钠通道的拮抗剂。因此它们可用作镇痛和神经保护剂; 其中（1）代表（A），（B）或（C）; R 1表示：（a）-LA或L'-A'，其中L表示键或C 1 -C 6烷基， C 2 -C 6亚烷基或C 2 -C 6炔基部分，A代表苯基，5- 至10元杂芳基，C 3 -C 6碳环基或5至10元杂环基，L'表示C 1 -C 3 C 6 -C 6烷基，C 2 -C 6亚烯基或C 2 -C 6亚烷基，C 2 -C 6亚烷基或C 2 -C 6亚烷基，炔基部分，A'表示-Het-A或-XA，其中Het表示-O-，-S-或NR'，X表示-CO-，-SO-，SO 2 - ， -CO-O-，CO-S，CONR'，-O-CO-，-S-CO-或NR'-CO-，其中R'表示氢或C 1 -C > 6个烷基; （b）-L-A-A'或-L-A-L-A其中A'如上所定义，每个A相同或不同，如上所定义，并且每个L相同或不同，如上所定义; （c）-AZA其中Z是-Het-L'，-X-L'，-L'-Het-或L'-X，其中Het，L'和X如上所定义，并且每个A相同或不同，如上所述; （d）-A-Het-Y或-AXY，其中是[L-Het] n -L'，[L'-Het] n -L-， - 其中n为1至4，B为-X-， - - - - NR'-CO-NR'，-O-CO-NR'-或-NR'-CO-O，其中X和L如上所定义，每个A相同或不同，如上所定义，每个L “相同或不同，如上所定义，每个R'相同或不同，如上所定义，并且每个Het相同或不同，如上所定义; 或（e）-L-CR（A）（A'）或L-CR（A）（LA）其中R是氢或C 1 -C 4烷基 A'如上所定义，每个L相同或不同，如上所定义，并且每个A相同或不同，如上所定义; R 2表示-LA-，L'-A'，-LAA'或LALA，其中L'和A'如上所定义，每个L相同或不同，如上所定义，并且每个 A相同或不同，如上所定义。J代表-NR 3 - ，-O-或直接键，其中R 3表示氢C 1 C 6 -C 6烷基，C 2 -C 6亚烯基或C 2 -C 6亚烷基或C 2 -C 6亚烷基 > 6炔基; p是1至3的整数; q为1或2; E和E'之一是-CH 2 - ，另一个是直接键。

2. 发明申请

WO2006030211A3 ACYCLIC SULPHONAMIDES 审中-公开
公开(公告)号：WO2006030211A3
公开(公告)日：2006-03-23
申请号：PCT/GB2005/003551
申请日：2005-09-14
申请人： VERNALIS (R & D) LIMITED , HOBBS, Christopher, John , LYNCH, Rosemary , MELLOR, Sarah, Louise , RADFORD, Fleur , GILBERT, Jenny, Christine , STOKES, Stephen , GLEN, Angela , FUIMANA, Andrea , EARNSHAW, Christopher, Geoffrey , KNUTSEN, Lars, Jacob, Stray , DEAN, Kathryn, Elizabeth, Sorrel
发明人： HOBBS, Christopher, John , LYNCH, Rosemary , MELLOR, Sarah, Louise , RADFORD, Fleur , GILBERT, Jenny, Christine , STOKES, Stephen , GLEN, Angela , FUIMANA, Andrea , EARNSHAW, Christopher, Geoffrey , KNUTSEN, Lars, Jacob, Stray , DEAN, Kathryn, Elizabeth, Sorrel
IPC分类号： C07D271/10 , C07D498/04 , C07D213/40 , C07D231/12 , C07D285/12 , C07D271/06 , C07D263/32 , C07D263/10 , C07D263/56 , C07D261/08 , C07D277/28 , C07D239/26 , A61K31/415 , A61K31/4164 , A61K31/421
摘要： Compounds of formula: (I) are found to antagonise N-type calcium channels wherein: - A is a 5- to 10-membered heteroaryl or heterocyclyl moiety, said moiety being optionally fused to a phenyl, 5- to 6-membered heteroaryl, C 3 -C 6 carbocyclyl or 5- to 6- membered heterocyclyl group; - B is a bond or a C 1 -C 6 alkyl or C 2 -C 6 alkenyl moiety; - either (a) R 1 is hydrogen or C 1 -C 6 alkyl and R 2 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, halogen, hydroxy, thio, amino, -Het-L or -L-Het-L', wherein L and L' are the same or different and represent C 1 -C 6 alkyl or C 2 -C 6 alkenyl and Het is O, S or NR, wherein R is hydrogen or C 1 -C 6 alkyl or (b) R 1 and R 2 form, together with the carbon to which they are attached, a 5- to 10-membered heterocyclyl or a C 3 -C 8 carbocyclyl moiety; R 3 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or -L-Het-L', wherein L, L' and Het are as defined above; and - R 4 , R 5 and R 6 are the same or different and represent hydrogen, halogen, hydroxy, amino, thio, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 1 -C 6 alkoxy, C 1 -C 6 alkylthio, mono(C 1 -C 6 alkyl)amino or di(C 1 -C 6 alkyl)amino.

3. 发明申请

WO2006030211A2 ACYCLIC SULPHONAMIDES 审中-公开
公开(公告)号：WO2006030211A2
公开(公告)日：2006-03-23
申请号：PCT/GB2005003551
申请日：2005-09-14
申请人： VERNALIS R & D LTD , HOBBS CHRISTOPHER JOHN , LYNCH ROSEMARY , MELLOR SARAH LOUISE , RADFORD FLEUR , GILBERT JENNY CHRISTINE , STOKES STEPHEN , GLEN ANGELA , FUIMANA ANDREA , EARNSHAW CHRISTOPHER GEOFFREY , KNUTSEN LARS JACOB STRAY , DEAN KATHRYN ELIZABETH SORREL
发明人： HOBBS CHRISTOPHER JOHN , LYNCH ROSEMARY , MELLOR SARAH LOUISE , RADFORD FLEUR , GILBERT JENNY CHRISTINE , STOKES STEPHEN , GLEN ANGELA , FUIMANA ANDREA , EARNSHAW CHRISTOPHER GEOFFREY , KNUTSEN LARS JACOB STRAY , DEAN KATHRYN ELIZABETH SORREL
IPC分类号： C07D213/40 , C07D231/12 , C07D239/26 , C07D261/08 , C07D263/10 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/28 , C07D285/12 , C07D498/04
CPC分类号： C07D213/40 , C07D231/12 , C07D239/26 , C07D261/08 , C07D263/10 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/28 , C07D285/12
摘要： Compounds of formula: (I) are found to antagonise N-type calcium channels wherein: - A is a 5- to 10-membered heteroaryl or heterocyclyl moiety, said moiety being optionally fused to a phenyl, 5- to 6-membered heteroaryl, C
摘要翻译：发现式（I）化合物拮抗N-型钙通道，其中：A为5-至10-元杂芳基或杂环基部分，所述部分任选地与苯基，5-至6-元杂芳基， ç<子

4. 发明申请

WO2005068448A1 SULFONAMIDES ANTAGONISING N-TYPE CALCIUM CHANNELS 审中-公开
标题翻译：拮抗N型钙通道的磺酰胺
公开(公告)号：WO2005068448A1
公开(公告)日：2005-07-28
申请号：PCT/GB2004/003705
申请日：2004-08-31
申请人： IONIX PHARMACEUTICALS LIMITED , RADFORD, Fleur , LYNCH, Rosemary , MELLOR, Sarah, Louise , HOBBS, Christopher, John , GILBERT, Jenny, Christine , STOKES, Stephen , GLEN, Angela , FIUMANA, Andrea , SMITH, Nichola, Jane , EARNSHAW, Christopher, Geoffrey , KNUTSEN, Lars, Jacob, Stray
发明人： RADFORD, Fleur , LYNCH, Rosemary , MELLOR, Sarah, Louise , HOBBS, Christopher, John , GILBERT, Jenny, Christine , STOKES, Stephen , GLEN, Angela , FIUMANA, Andrea , SMITH, Nichola, Jane , EARNSHAW, Christopher, Geoffrey , KNUTSEN, Lars, Jacob, Stray
IPC分类号： C07D295/22
CPC分类号： C07D211/96 , C07D401/04 , C07D401/06 , C07D405/12 , C07D409/12 , C07D413/04 , C07D417/04
摘要： Compounds of the general formula (I), tautomers thereof and pharmaceutically acceptable salts thereof, are found to antagonise N-type calcium channels. The compounds are used for the treatment or prevention of a condition mediated by N-Type calcium channels, such as pain.
摘要翻译：发现通式（I）的化合物，其互变异构体和其药学上可接受的盐拮抗N型钙通道。该化合物用于治疗或预防N型钙通道介导的病症，如疼痛。

5. 发明申请

WO2004017966A1 FIVE-MEMBERED HETEROCYCLIC COMPOUNDS IN THE TREATMENT OF CHRONIC AND ACUTE PAIN 审中-公开
标题翻译：治疗慢性疼痛的五种成分化合物
公开(公告)号：WO2004017966A1
公开(公告)日：2004-03-04
申请号：PCT/GB2003/003674
申请日：2003-08-22
申请人： IONIX PHARMACEUTICALS LIMITED , KNUTSEN, Lars, Jacob, Stray , HOBBS, Christopher, John , RADFORD, Fleur , FIUMANA, Andrea , EARNSHAW, Christopher, Geoffrey , MELLOR, Sarah, Louise , SMITH, Nichola, Jane
发明人： KNUTSEN, Lars, Jacob, Stray , HOBBS, Christopher, John , RADFORD, Fleur , FIUMANA, Andrea , EARNSHAW, Christopher, Geoffrey , MELLOR, Sarah, Louise , SMITH, Nichola, Jane
IPC分类号： A61K31/427
CPC分类号： C07D417/04 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/381 , A61K31/4025 , A61K31/4184 , A61K31/427 , A61K31/44 , A61K31/4425 , A61K31/4436 , A61K31/4439 , A61K31/4709 , A61K31/496 , C07D277/14 , C07D417/06
摘要： Compounds of formula (I) are found to antagonise N-type calcium channels F(I) wherein R 1 , R 2 and R 4 are organic residues, Y is a linker and R 3 is aryl, heteroaryl, carbocyclyl a heterocyclyl are N-type calcium channel antagonists and are therefore useful in the treatment of both chronic and acute pain.
摘要翻译：发现式（I）化合物可拮抗其中R 1，R 2和R 4为有机残基的N型钙通道F（I），Y为连接基，R 3为芳基，杂环基，碳环基a杂环基是N型钙通道拮抗剂，因此可用于治疗慢性和急性疼痛。

6. 发明申请

WO2007007057A1 ANTAGONISTS OF SNS SODIUM CHANNELS 审中-公开
标题翻译： SNS钠通道的拮抗剂
公开(公告)号：WO2007007057A1
公开(公告)日：2007-01-18
申请号：PCT/GB2006/002523
申请日：2006-07-07
申请人： VERNALIS (R & D) LIMITED , HAMLYN, Richard , CALLIS, David , EARNSHAW, Christopher, Geoffrey , FINCH, Harry , HUCKSTEP, Mike , LYNCH, Rosemary , MELLOR, Sarah
发明人： HAMLYN, Richard , CALLIS, David , EARNSHAW, Christopher, Geoffrey , FINCH, Harry , HUCKSTEP, Mike , LYNCH, Rosemary , MELLOR, Sarah
IPC分类号： A61K31/397 , A61P23/00
CPC分类号： A61K31/397
摘要： Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents, formula (I): R 1 represents: (a) -L-A or -L' -A' wherein L represents a bond or a C 1- C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl moiety, A represents a phenyl, 5- to 10-membered heteroaryl, C 3 -C 6 carbocyclyl or 5- to 10-membered heterocyclyl group, L' represents a C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl moiety, and A' represents -Het-A or -X-A wherein Het represents -O-, -S- or -NR'-, and X represents -CO-, -SO-, -SO 2 -, -CO-O-, -CO-S-, -CONR'-, -O-CO-, -S-CO- or -NR'-CO-, wherein R' represents hydrogen or C 1 -C 6 alkyl; (b) -L-CR(A)(A') or -L-CR(A)(L-A) wherein R is hydrogen or C 1 1-C 4 alkyl, A' is as defined above, each L is the same or different and is as defined above and each A' is the same or different and is as defined above; (c) -L-A-A' or -L-A-L-A wherein A' and L are as defined above and each A is the same or different and is as defined above; or (d) -A-Z-A wherein Z is -Het-L'-, -X-L'-, -L'-Het- or -L'-X-, wherein Het, L' and X are as defined above and each A is the same or different and is as defined above; J represents -NR 5 -, -O- or a direct bond; R 5 represents hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; R 4 is represents hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; and either R 2 represents -L-A, -L-A’, -L-A-A’, -L-A-L-A, -L-CR(A)(L-A), -L- CR(A)(A’) or -L-CR(A)(L") wherein L" is -Het-L', -X-L', -CONH 2 or -CO 2 H, and wherein A', Het, X and R are as defined above, each L is the same or different and is as defined above, each A is the same or different and is as defined above and R 3 represents hydrogen, C 1 -C 6 alkyl C 2 -C 6 alkynyl or (CO)-L', wherein L is as defined above or R 2 and R 3 form, together with the nitrogen to which they are attached, a 5-to 10-membered heteroaryl or 5-to 10-membered heterocyclyl ring.
摘要翻译：发现式（I）化合物及其药学上可接受的盐是SNS钠通道的拮抗剂。因此，它们可用作止痛和神经保护剂，式（I）：R 1表示：（a）-LA或-L'-A'，其中L表示键或C 1 C 6 -C 6烷基，C 2 -C 6亚烯基或C 2 -C 6亚烷基或C 2 -C 6亚烷基 C 6炔基部分，A表示苯基，5至10元杂芳基，C 3 -C 6碳环基或5至10元杂环基基团，L'表示C 1 -C 6烷基，C 2 -C 6亚烷基或C 1 -C 6烷基， A'表示-Het-A或-XA，其中Het表示-O - ， - S-或-NR'-，X表示 -CO - ， - SO - ， - SO 2 - ， - CO-O-，-CO-S-，-CONR'-，-O-CO-，-S-CO-或 - NR'-CO-，其中R'表示氢或C 1 -C 6烷基; （b）-L-CR（A）（A'）或-L-CR（A）（LA）其中R是氢或C 1〜烷基，A'如上所定义，每个L相同或不同，如上所定义，每个A'相同或不同，如上所定义; （c）-L-A-A'或-L-A-L-A其中A'和L如上所定义，并且每个A相同或不同，如上所定义; 或（d）-AZA，其中Z是-Het-L'-，-X-L' - ，-L'-Het-或-L'-X-，其中Het，L'和X如上所定义， A相同或不同，如上所述; J表示-NR 5 - ，-O-或直接键; R 5表示氢，C 1 -C 6烷基，C 2 -C 6烷基，C 1 -C 6烷基，链烯基或C 2 -C 6 -C 6炔基; R 4表示氢，C 1 -C 6烷基，C 2 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， / SUB链烯基或C 2 -C 6炔基; 并且R 2表示-LA，-L-A'，-LA-A'，-LALA，-L-CR（A）（LA），-L-CR（A）（A '）或-L-CR（A）（L“）其中L”是-Het-L'，-X-L'，-CONH 2或-CO 2 H，其中A'，Het，X和R如上所定义，每个L相同或不同，如上所定义，每个A相同或不同，如上所定义，R 3， / SO 2表示氢，C 1 -C 6烷基C 2 -C 6炔基或（CO） -L'，其中L如上定义或R 2和R 3形式与它们所连接的氮一起形成5至10元杂芳基或5至10元杂环基环。

7. 发明专利

GB9621335D0 Honcho poncho 未知
公开(公告)号：GB9621335D0
公开(公告)日：1996-12-04
申请号：GB9621335
申请日：1996-10-12
申请人： MELLOR SARAH A M

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