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1. 发明申请

WO2007118323B1 ISOXAZOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译： ISOXAZOLE衍生物作为钙通道阻断剂
公开(公告)号：WO2007118323B1
公开(公告)日：2007-12-21
申请号：PCT/CA2007000632
申请日：2007-04-17
申请人： NEUROMED PHARMACEUTICALS LTD , PAJOUHESH HASSAN , HOLLAND RICHARD , PAJOUHESH HOSSEIN
发明人： PAJOUHESH HASSAN , HOLLAND RICHARD , PAJOUHESH HOSSEIN
IPC分类号： C07D413/06 , A61K31/42 , A61K31/496 , C07D261/08 , C07D261/18
CPC分类号： C07D261/08 , A61K31/42 , A61K31/496 , C07D261/18 , C07D295/03 , C07D413/06
摘要： Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type or T-type calcium channel activity are disclosed. Specifically, a series of isoxazole containing compounds are disclosed of the general formula (1) where Z is N or CHNR 3 and (Ar 1 ) 2 CR 4 is optionally substituted benzhydryl.
摘要翻译：公开了有效改善由不需要的钙通道活性，特别是不需要的N型或T型钙通道活性表征的病症的方法和化合物。具体地说，通式（1）中公开了一系列含异唑的化合物，其中Z是N或CHNR 3，和（Ar 1）2 CR 4是任选取代的二苯甲基。

2. 发明申请

WO2007071035A1 HETEROCYCLIC AMIDE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译：杂环酰胺衍生物作为钙通道阻断剂
公开(公告)号：WO2007071035A1
公开(公告)日：2007-06-28
申请号：PCT/CA2006/002070
申请日：2006-12-19
申请人： NEUROMED PHARMACEUTICALS LTD. , PAJOUHESH, Hassan , KAUL, Ramesh , DING, Yanbing , HUM, Gabriel , PAJOUHESH, Hossein
发明人： PAJOUHESH, Hassan , KAUL, Ramesh , DING, Yanbing , HUM, Gabriel , PAJOUHESH, Hossein
IPC分类号： C07D295/185 , A61K31/495 , A61K31/496 , C07D401/06 , C07D405/06
CPC分类号： C07D211/26 , A61K31/495 , A61K31/496 , C07D211/62 , C07D211/64 , C07D213/74 , C07D241/04 , C07D295/185 , C07D309/04
摘要： Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type or T-type calcium channel activity are disclosed. Specifically, a series of heterocyclic amides are disclosed of the general formula (I) where Z is N or CHNR 2 and X is NR 2 , O, S, S=O or SO 2 . Among other definitions for R, R 1 , W and Y, the compounds of formula (1) are further characterized by at least one of W or Y being CR 3 Ar 2 where Ar is an aromatic or heteroaromatic ring (for example, where W or Y is a benzhydryl moiety).
摘要翻译：公开了有效改善由不需要的钙通道活性，特别是不想要的N型或T型钙通道活性表征的病症的方法和化合物。具体地，公开了通式（I）的一系列杂环酰胺，其中Z是N或CHNR 2，X是NR 2，O，S，S = O 或SO 2 2。对于R，R 1，W和Y的其它定义中，式（1）的化合物的进一步特征在于W或Y中的至少一个是CR 3 Ar 其中Ar是芳族或杂芳族环（例如，其中W或Y是二苯甲基部分）。

3. 发明申请

WO2005070919A1 N-TYPE CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译： N型钙通道阻塞器
公开(公告)号：WO2005070919A1
公开(公告)日：2005-08-04
申请号：PCT/CA2005/000073
申请日：2005-01-21
申请人： NEUROMED TECHNOLOGIES, INC. , PAJOUHESH, Hassan , PAJOUHESH, Hossein , DING, Yanbing , SNUTCH, Terrance, P.
发明人： PAJOUHESH, Hassan , PAJOUHESH, Hossein , DING, Yanbing , SNUTCH, Terrance, P.
IPC分类号： C07D401/06
CPC分类号： C07D207/273 , C07D207/14 , C07D207/16
摘要： The present invention relates to 3-amino pyrrolidine derivatives of Formula (1) or (2) Where : X is CR 3 or N; W is L 2 -A 3 or X'(A 1 )(A 2 ); A 1 , A 2 , and A 3 are 5- or 6- membered aliphatic or aromatic rings optionally containing one heteroatom selected from 0, N, and S, and optionally fused to an additional ring; L' and L 2 are C 1-10 alkyl or C 2-10 alkenyl, wherein C is optionally replaced by a heteroatom selected from N, 0, or S, and/or further substituted with =0; R', R 2 , and R 3 vary amongst several possible substituents; and n is 0 to 7.The present invention further relates to methods for modulating calcium channel activity. Compounds of formula (1) and (2) are useful in treating conditions associated which benefit from blocking calcium ion channels.
摘要翻译：（1）或（2）的3-氨基吡咯烷衍生物其中：X是CR 3或N; W是L 2 -A 3或X'（A 1）（A 2）。 A 1，A 2和A 3是任选含有一个选自O，N的杂原子的5或6元脂族或芳族环和S，并且任选地与另外的环稠合; L'和L 2是C 1-10烷基或C 2-10烯基，其中C任选被选自N ，0或S，和/或进一步被= 0取代; R'，R'2和R 3在几种可能的取代基之间变化; 并且n是0至7.本发明进一步涉及调节钙通道活性的方法。式（1）和（2）的化合物可用于治疗因阻断钙离子通道而受益的相关疾病。

4. 发明申请

WO2004089922A2 CALCIUM CHANNEL INHIBITORS COMPRISING BENZHYDRIL SPACED FROM PIPERAZINE 审中-公开
标题翻译：钙通道抑制剂包含苯哌嗪分离的苯甲酸
公开(公告)号：WO2004089922A2
公开(公告)日：2004-10-21
申请号：PCT/CA2004/000539
申请日：2004-04-08
申请人： NEUROMED TECHNOLOGIES, INC. , BELARDETTI, Francesco , PAJOUHESH, Hassan , PAJOUHESH, Hossein , SNUTCH, Terrance, P. , ZAMPONI, Gerald, W.
发明人： BELARDETTI, Francesco , PAJOUHESH, Hassan , PAJOUHESH, Hossein , SNUTCH, Terrance, P. , ZAMPONI, Gerald, W.
IPC分类号： C07D295/08
CPC分类号： C07D295/185 , A61K31/4468 , A61K31/451 , A61K31/4515 , A61K31/454 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/5375 , A61K31/538 , A61K31/5415 , C07D211/14 , C07D211/16 , C07D211/46 , C07D211/58 , C07D213/38 , C07D277/74 , C07D277/82 , C07D295/03 , C07D317/60 , C07D401/04 , C07D401/14
摘要： Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.
摘要翻译：描述了可用于改变钙通道活性的某些哌嗪取代的化合物。

5. 发明申请

WO2009132453A8 CYCLYLAMINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译：环丙基胺衍生物作为钙通道阻断剂
公开(公告)号：WO2009132453A8
公开(公告)日：2010-01-14
申请号：PCT/CA2009000579
申请日：2009-04-28
申请人： NEUROMED PHARMACEUTICALS LTD , GALEMMO JR ROBERT , HOLLAND RICHARD , HUM GABRIEL , PAJOUHESH HOSSEIN , CHAHAL NAVJOT , SEID-BAGHERZADEH MEHRAN , GIRARD AMY
发明人： GALEMMO JR ROBERT , HOLLAND RICHARD , HUM GABRIEL , PAJOUHESH HOSSEIN , CHAHAL NAVJOT , SEID-BAGHERZADEH MEHRAN , GIRARD AMY
IPC分类号： C07C233/00 , A61K31/165 , A61K31/277 , A61K31/395 , A61P29/00 , C07C255/00 , C07C317/32 , C07D207/00 , C07D213/00 , C07D231/00 , C07D241/00 , C07D261/00 , C07D277/00 , C07D295/192 , C07D309/00 , C07D401/12 , C07D405/12 , C07D413/12 , C07D413/14
CPC分类号： C07D277/28 , C07C233/81 , C07C237/24 , C07C255/41 , C07C311/08 , C07C317/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/40 , C07D213/75 , C07D213/81 , C07D231/12 , C07D241/12 , C07D261/08 , C07D295/067 , C07D295/185 , C07D309/08 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12
摘要： Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds of substituted or unsubstituted cyclylamine derivatives as shown in formulas (1).
摘要翻译：公开了有效改善特征在于不需要的钙通道活性，特别是不需要的N型和/或T型钙通道活性的病症的方法和化合物。具体而言，是式（1）所示的一系列取代或未取代的环基胺衍生物的化合物。

6. 发明申请

WO2008138126A1 BICYCLIC PYRIMIDINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译：双相吡啶衍生物作为钙通道阻断剂
公开(公告)号：WO2008138126A1
公开(公告)日：2008-11-20
申请号：PCT/CA2008/000904
申请日：2008-05-08
申请人： NEUROMED PHARMACEUTICALS LTD. , PAJOUHESH, Hassan , PAJOUHESH, Hossein , DING, Yanbing , TAN,Jason , GRIMWOOD, Mike , BELARDETTI, Francesco , KAUL, Ramesh
发明人： PAJOUHESH, Hassan , PAJOUHESH, Hossein , DING, Yanbing , TAN,Jason , GRIMWOOD, Mike , BELARDETTI, Francesco , KAUL, Ramesh
IPC分类号： A61K31/519 , A61K31/517 , A61K31/5377
CPC分类号： A61K31/496 , A61K31/5377
摘要： Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6).
摘要翻译：公开了有助于改善由不希望的钙通道活性，特别是不希望的T型钙通道活性表征的病症的方法和化合物。具体地说，通式（1）或式（2）公开了一系列含有噻吩并嘧啶或氧代喹唑啉衍生物的化合物，其中X为连接基，Y为芳族部分或N（R5）（R6）。

7. 发明申请

WO2006024160A1 UREA DERIVATIVES AS CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译：尿素衍生物作为钙通道阻断剂
公开(公告)号：WO2006024160A1
公开(公告)日：2006-03-09
申请号：PCT/CA2005/001324
申请日：2005-08-30
申请人： NEUROMED TECHNOLOGIES INC. , PAJOUHESH, Hassan , PAJOUHESH, Hossein , DING, Yanbing , SNUTCH, Terrance, P.
发明人： PAJOUHESH, Hassan , PAJOUHESH, Hossein , DING, Yanbing , SNUTCH, Terrance, P.
IPC分类号： C07D413/06
CPC分类号： C07D295/215 , C07D211/26 , C07D211/58 , C07D213/38 , C07D241/04 , C07D295/20 , C07D401/06 , C07D403/06 , C07D405/06
摘要： Urea derivatives of formula (1) which comprise piperidine or piperazine ring. Each of A and B is independently hydrogen; alkyl; a 6membered aromatic or nonaromatic, carbocyclic or heterocyclic moiety; an aminoalkyl or an aminoalkenyl; wherein only one of A and B may be hydrogen or alkyl. RI is H, alkyl, alkenyl or alkynyl. Z is N or CHNR2. Each of R3 may be a variety of substituents. Each of R4 may be H or alkyl. Each Ar is a 6-membered or fused aromatic system optionally containing nitrogen atoms; m is 0-3 and n is 0-2. These compounds are effective in ameliorating conditions characterized by unwanted calcium channel activity.
摘要翻译：包含哌啶或哌嗪环的式（1）的脲衍生物。 A和B各自独立地为氢; 烷基; 6个芳族或非芳族，碳环或杂环部分; 氨基烷基或氨基烯基; 其中A和B中只有一个可以是氢或烷基。 R 1是H，烷基，烯基或炔基。 Z是N或CHNR2。 R3中的每一个可以是各种取代基。 R 4可以是H或烷基。每个Ar是任选含有氮原子的6元或稠合芳族体系; m为0-3，n为0-2。这些化合物有效地改善以不希望的钙通道活性为特征的病症。

8. 发明申请

WO2005097779A1 DIARYLAMINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译：二胺衍生物作为钙通道阻断剂
公开(公告)号：WO2005097779A1
公开(公告)日：2005-10-20
申请号：PCT/CA2005/000544
申请日：2005-04-08
申请人： NEUROMED TECHNOLOGIES INC. , PAJOUHESH, Hassan , PAJOUHESH, Hossein , DING, Yanbing , SNUTCH, Terrance, P.
发明人： PAJOUHESH, Hassan , PAJOUHESH, Hossein , DING, Yanbing , SNUTCH, Terrance, P.
IPC分类号： C07D405/06
CPC分类号： C07D295/13 , C07D211/26 , C07D211/58 , C07D213/38 , C07D241/04 , C07D241/08 , C07D295/15 , C07D295/185 , C07D317/58 , C07D401/06
摘要： N-diarylaminoalkyl-substituted piperazine/4-aminopiperidine compounds of formula (1) are disclosed, wherein each of A and B is independently a 6-membered aromatic or nonaromatic, carbocyclic or heterocyclic moiety or is an aminoalkyl and wherein one and only one of A and B may be H or alkyl (1-8C) or wherein A and B together form an optionally substituted 6-membered aromatic of nonaromatic, carbocyclic or heterocyclic moiety; R 1 is H or alkyl (1-8C), Z is N or CHNR 2 wherein R 2 is H or alkyl (1-8C), X is straight chain alkylene (1-4C) wherein optionally at least one carbon adjacent to a nitrogen is in the form of C=0; each R 3 is an independent substituent; n=0-2; Ar is a six-membered aromatic or heteroaromatic ring; wherein each cyclic moiety included in A or B each Ar moiety in formula (1) may be substituted by one or more substituents. These compounds and salts or conjugated thereof are able to block N-type and T-type calcium channels and are useful for treating conditions mediated by calcium ion channel activity such as chronic pain.
摘要翻译：公开了式（1）的N-二芳基氨基烷基取代的哌嗪/ 4-氨基哌啶化合物，其中A和B各自独立地是6元芳族或非芳族，碳环或杂环部分或者是氨基烷基，并且其中， A和B可以是H或烷基（1-8C）或其中A和B一起形成非芳族，碳环或杂环部分的任选取代的6元芳族; R 1是H或烷基（1-8C），Z是N或CHNR 2，其中R 2是H或烷基（1-8C），X是直链亚烷基（1-4C），其中任选地与氮相邻的至少一个碳为C = 0的形式; 每个R 3是独立的取代基; N = 0-2; Ar是六元芳族或杂芳族环; 其中包含在A或B中的每个环状部分，式（1）中的每个Ar部分可以被一个或多个取代基取代。这些化合物和其盐或缀合物能够阻断N-型和T型钙通道，并且可用于治疗由钙离子通道活性（如慢性疼痛）介导的病症。

9. 发明申请

WO2005070919A8 N-TYPE CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译： N型钙通道阻塞器
公开(公告)号：WO2005070919A8
公开(公告)日：2005-10-20
申请号：PCT/CA2005000073
申请日：2005-01-21
申请人： NEUROMED TECH INC , PAJOUHESH HASSAN , PAJOUHESH HOSSEIN , DING YANBING , SNUTCH TERRANCE P
发明人： PAJOUHESH HASSAN , PAJOUHESH HOSSEIN , DING YANBING , SNUTCH TERRANCE P
IPC分类号： A61K31/40 , A61K31/4439 , C07D207/14 , C07D207/16 , C07D207/26 , C07D207/273 , C07D207/30 , C07D401/06
CPC分类号： C07D207/273 , C07D207/14 , C07D207/16
摘要： The present invention relates to 3-amino pyrrolidine derivatives of Formula (1) or (2) Where : X is CR or N; W is L -A or X'(A )(A ); A , A , and A are 5- or 6- membered aliphatic or aromatic rings optionally containing one heteroatom selected from 0, N, and S, and optionally fused to an additional ring; L' and L are C1-10 alkyl or C2-10 alkenyl, wherein C is optionally replaced by a heteroatom selected from N, 0, or S, and/or further substituted with =0; R', R , and R vary amongst several possible substituents; and n is 0 to 7.The present invention further relates to methods for modulating calcium channel activity. Compounds of formula (1) and (2) are useful in treating conditions associated which benefit from blocking calcium ion channels.
摘要翻译：本发明涉及式（1）或（2）的3-氨基吡咯烷衍生物，其中：X为CR 3或N; W是L 2 -A 3或X'（A 1）（A 2）; A 1，A 2和A 3是任选地含有一个选自0，N和S的杂原子，并任选地与另外的环稠合的5-或6-元脂族或芳族环; L'和L 2是C 1-10烷基或C 2-10烯基，其中C任选被选自N，O或S的杂原子和/或进一步被= 0取代; R'，R 2和R 3在几个可能的取代基之间变化; n为0〜7。本发明还涉及钙通道活性的调节方法。式（1）和（2）的化合物可用于治疗受益于阻断钙离子通道的相关条件。

10. 发明申请

WO2004089377A1 CALCIUM CHANNEL BLOCKERS COMPRISING TWO BENZHYDRIL MOIETIES 审中-公开
标题翻译：包含两个BENZHYDRIL MOIETIES的CALCIUM通道阻塞器
公开(公告)号：WO2004089377A1
公开(公告)日：2004-10-21
申请号：PCT/CA2004/000535
申请日：2004-04-08
申请人： NEUROMED TECHNOLOGIES, INC. , BELARDETTI, Francesco , PAJOUHESH, Hassan , PAJOUHESH, Hossein , SNUTCH, Terrance, P. , ZAMPONI, Gerald, W.
发明人： BELARDETTI, Francesco , PAJOUHESH, Hassan , PAJOUHESH, Hossein , SNUTCH, Terrance, P. , ZAMPONI, Gerald, W.
IPC分类号： A61K31/495
CPC分类号： A61K31/4468 , A61K31/451 , A61K31/4515 , A61K31/454 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/5375 , A61K31/538 , A61K31/5415 , C07D211/14 , C07D211/16 , C07D211/46 , C07D211/58 , C07D213/38 , C07D277/74 , C07D277/82 , C07D295/03 , C07D295/185 , C07D317/60 , C07D401/04 , C07D401/14
摘要： Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.
摘要翻译：描述了可用于改变钙通道活性的某些哌嗪取代的化合物。

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