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1. 发明申请

WO2005000309A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2005000309A2
公开(公告)日：2005-01-06
申请号：PCT/GB2004/002697
申请日：2004-06-24
申请人： IONIX PHARMACEUTICALS LIMITED , JENNINGS, Neil, Stuart , STOKES, Stephen , HAMLYN, Richard, John , TICKLE, David, Christopher , HUCKSTEP, Michael, Richard , LYNCH, Rosemary , KNUTSEN, Lars, Jacob, Stray
发明人： JENNINGS, Neil, Stuart , STOKES, Stephen , HAMLYN, Richard, John , TICKLE, David, Christopher , HUCKSTEP, Michael, Richard , LYNCH, Rosemary , KNUTSEN, Lars, Jacob, Stray
IPC分类号： A61K31/4439
CPC分类号： C07D277/28 , A61K31/4439 , C07C311/29 , C07D207/335 , C07D211/96 , C07D231/12 , C07D233/64 , C07D249/04 , C07D249/14 , C07D263/10 , C07D263/32 , C07D277/52 , C07D285/06 , C07D285/135 , C07D295/13 , C07D333/20 , C07D417/12
摘要： Compounds of the formulae (I) and (II), and pharmaceutically acceptable salts thereof, are found to be inhibitors of sensory neurone specific (SNS) sodium channels. They are therefore useful as analgesic and neuroprotective agents. Formula (I) & Formula (II) wherein, in the formula (I), R 1 is an organic substituent, X 1 and X 2 are direct bonds or spacer moieties, Ar is aryl or heteroaryl and Y is a substituted aminoalkyl group or a heteroaryl-, heterocyclyl- or phenyl-containing moiety and, in the formula(II), R 1 , R 2 , R 3 , Ar and R 4 are organic substituents, X is a spacer moiety and Het is a 5-membered heteroaryl or heterocyclyl group.
摘要翻译：发现式（I）和（II）的化合物及其药学上可接受的盐是感觉神经元特异性（SNS）钠通道的抑制剂。因此它们可用作镇痛剂和神经保护剂。式（I）＆amp; 式（II）其中在式（I）中，R 1是有机取代基，X 1和X 2是直接键或间隔基部分，Ar为芳基或杂芳基，并且Y为取代的氨基烷基或含杂芳基 - ，杂环基或苯基的部分，并且在式（II）中，R 1，R 2， 2R 3，Ar和R 4是有机取代基，X是间隔基部分，Het是5元杂芳基或杂环基基团。 p>

2. 发明申请

WO2005000309A3 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2005000309A3
公开(公告)日：2005-03-03
申请号：PCT/GB2004002697
申请日：2004-06-24
申请人： IONIX PHARMACEUTICALS LTD , JENNINGS NEIL STUART , STOKES STEPHEN , HAMLYN RICHARD JOHN , TICKLE DAVID CHRISTOPHER , HUCKSTEP MICHAEL RICHARD , LYNCH ROSEMARY , KNUTSEN LARS JACOB STRAY
发明人： JENNINGS NEIL STUART , STOKES STEPHEN , HAMLYN RICHARD JOHN , TICKLE DAVID CHRISTOPHER , HUCKSTEP MICHAEL RICHARD , LYNCH ROSEMARY , KNUTSEN LARS JACOB STRAY
IPC分类号： A61K31/4439 , C07C311/29 , C07D207/32 , C07D207/335 , C07D211/96 , C07D231/12 , C07D233/54 , C07D249/04 , C07D249/14 , C07D263/10 , C07D263/32 , C07D277/28 , C07D277/52 , C07D285/06 , C07D285/12 , C07D285/135 , C07D295/13 , C07D333/20 , C07D417/12
CPC分类号： C07D277/28 , A61K31/4439 , C07C311/29 , C07D207/335 , C07D211/96 , C07D231/12 , C07D233/64 , C07D249/04 , C07D249/14 , C07D263/10 , C07D263/32 , C07D277/52 , C07D285/06 , C07D285/135 , C07D295/13 , C07D333/20 , C07D417/12
摘要： Compounds of the formulae (I) and (II), and pharmaceutically acceptable salts thereof, are found to be inhibitors of sensory neurone specific (SNS) sodium channels. They are therefore useful as analgesic and neuroprotective agents. Formula (I) & Formula (II) wherein, in the formula (I), R1 is an organic substituent, X1 and X2 are direct bonds or spacer moieties, Ar is aryl or heteroaryl and Y is a substituted aminoalkyl group or a heteroaryl-, heterocyclyl- or phenyl-containing moiety and, in the formula(II), R1, R2, R3, Ar and R4 are organic substituents, X is a spacer moiety and Het is a 5-membered heteroaryl or heterocyclyl group.
摘要翻译：发现式（I）和（II）的化合物及其药学上可接受的盐是感觉神经元特异性（SNS）钠通道的抑制剂。因此它们可用作止痛剂和神经保护剂。式（I）和式（II）其中，在式（I）中，R 1是有机取代基，X 1和X 2是直接键或间隔部分，Ar是芳基或杂芳基，Y是取代的氨基烷基或杂芳基 - （II）中，R 1，R 2，R 3，Ar和R 4为有机取代基，X为间隔基，Het为5元杂芳基或杂环基。

3. 发明申请

WO2005005392A1 AZACYCLIC COMPOUNDS AS INHIBITORS OF SENSORY NEURONE SPECIFIC CHANNELS 审中-公开
标题翻译：作为感觉神经元特异性通道的抑制剂的AZACYCLIC化合物
公开(公告)号：WO2005005392A1
公开(公告)日：2005-01-20
申请号：PCT/GB2004/002945
申请日：2004-07-07
申请人： IONIX PHARMACEUTICALS LIMITED , HAMLYN, Richard, John , HUCKSTEP, Michael, Richard , LYNCH, Rosemary , STOKES, Stephen , TICKLE, David, Christopher , PATIENT, Lee
发明人： HAMLYN, Richard, John , HUCKSTEP, Michael, Richard , LYNCH, Rosemary , STOKES, Stephen , TICKLE, David, Christopher , PATIENT, Lee
IPC分类号： C07D217/04
CPC分类号： C07D223/16 , C07D209/44 , C07D209/86 , C07D217/02 , C07D217/10 , C07D217/14 , C07D217/22 , C07D401/06 , C07D401/12 , C07D403/06 , C07D409/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D487/04
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: X is -N- or -CH-; n is from 0 to 3.
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剂和神经保护剂，其中：X为-N-或-CH-; n为0〜3。

4. 发明申请

WO2004087125A1 AMINO ACID DERIVATIVES AS INHIBITORS OF MAMMALIAN SODIUM CHANNELS 审中-公开
标题翻译：氨基酸衍生物作为MAMMALIAN SODIUM通道的抑制剂
公开(公告)号：WO2004087125A1
公开(公告)日：2004-10-14
申请号：PCT/GB2004/001474
申请日：2004-04-02
申请人： IONIX PHARMACEUTICALS LIMITED , HAMLYN, Richard, John , TICKLE, David, Christopher , HUCKSTEP, Michael, Richard , LYNCH, Rosemary
发明人： HAMLYN, Richard, John , TICKLE, David, Christopher , HUCKSTEP, Michael, Richard , LYNCH, Rosemary
IPC分类号： A61K31/18
CPC分类号： C07K14/705
摘要： Use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in the treatment or prevention of a condition selected from chronic and acute pain, tinnitus, bowel disorders, bladder dysfunctions and demyelinating diseases, Formula (I) wherein: - R 1 is C l -C 6 alkyl, C 6 -C 10 aryl, a 5- to 10- membered heteroaryl group, a 5- to 10- membered heterocyclyl group or a C 3 -C 6 carbocyclyl group; each R 2 is the same or different and represents C l -C 6 alkyl, halogen, C l -C 6 alkoxy, C l -C 6 alkythio, hydroxy, nitro, cyano, amino, (C l -C 6 alkyl)amino or di-( C l -C 6 alkyl)amino; - R 3 represents hydrogen, C l -C 6 alkyl, or together with R 4 represents a C 2 -C 4 alkylene group; - R 4 is hydrogen, C l -C 6 alkyl, C 6 -C 10 aryl, C 3 -C 6 carbocyclyl, a 5- to 10membered heteroaryl group, a 5- to 10- membered heterocyclyl group, -( C l -C 6 alkyl)-(C 6 -C 10 aryl), -(C 1 -C 6 alkyl)-(C 3 -C 6 carbocyclyl), -(C 1 -C 6 alkyl)-(5-to 10- membered heteroaryl), - ( C l -C 6 alkyl)-(5- to 10- membered heterocyclyl) or, together with R 3 represents a C 2 -C 4 alkylene group; - R 5 and R 6 are the same or different and each represent hydrogen or a C l -C 6 alkyl group; - n is 0,1, 2, 3 or 4; X 1 represents a direct bond or a methylene group; and X 2 represents a -CH 2 -, -CO-, -SO- or -S(O)2- group, wherein: the alkyl and alkylene groups and moieties in the substituents R 1 to R 6 and X, are unsubstituted or are substituted by 1, 2 or 3 substituents which are the same or different and are selected from hydroxy, amino, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylamino and di(C 1 -C 4 alkyl)amino substituents; and the aryl, heteroaryl, heterocyclyl and carbocyclyl groups and moieties in the substituents R 1 and R 4 are unsubstituted or are substituted by 1, 2 or 3 substituents which are the same or different and are selected from halogen, C l -C 6 alkyl, C l -C 6 alkoxy, C l -C 6 alkylthio, hydroxy, amino, C l -C 6 alkylamino, di-( C l -C 6 alkyl)amino, C l -C 6 haloalkyl, C l -C 6 haloalkoxy and C l -C 6 haloalkylthio substituents. provided that, when n is 1, 2, 3 or 4, R 4 is other than hydrogen and when n is 0, X 2 is -CH 2 - and R 1 is an aryl or heteroaryl group, then either: (a) R, is a phenyl group which carries at least one -SCF 3 substituent or is a thienyl group which carries at least one chloro substituent; (d) R 1 is a phenyl group which carries at least one -CF 3 substituent or at least two halogen substituents; or (e) R 4 is benzyl or hydroxybenzyl and R 1 is a phenyl group which carries a fluorine or -OCH 3 substituent.
摘要翻译：式（I）化合物或其药学上可接受的盐在制备用于治疗或预防选自慢性和急性疼痛，耳鸣，肠病，膀胱功能障碍和脱髓鞘疾病中的病症的药物中的用途式（I）其中：-R 1是C 1 -C 6烷基，C 6 -C 10芳基，5-至10-元杂芳基，5-至10-元杂环基或C 3 -C 6碳环基; 每个R 2相同或不同，表示C 1 -C 6烷基，卤素，C 1 -C 6烷氧基，C 1 -C 6连接基，羟基，硝基，氰基，氨基，（C 1 -C 6烷基）氨基或二 - （C 1 -C 6烷基）氨基; -R 3表示氢，C 1 -C 6烷基或与R 4一起代表C 2 -C 4亚烷基; R 4是氢，C 1 -C 6烷基，C 6 -C 10芳基，C 3 -C 6碳环基，5-至10元杂芳基，5-至10-元杂环基， - （C 1 -C 6烷基） - （C 6 -C 10）（C 1 -C 6烷基） - （C 3 -C 6碳环基）， - （C 1 -C 6烷基） - （5-至10-元杂芳基）， - （C 1 -C 6烷基） - （5-至10 元环杂环基）或与R 3一起代表C 2 -C 4亚烷基; -R 5和R 6相同或不同，各自表示氢或C 1 -C 6烷基; - n为0,1,2,3或4; X1表示直接键或亚甲基; 并且X 2表示-CH 2 - ， - CO - ， - SO-或-S（O）2 - 基团，其中：取代基R 1至R 6和X中的烷基和亚烷基和部分未被取代或被1 2或3个相同或不同并且选自羟基，氨基，C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4烷基氨基和二（C 1 -C 4烷基）氨基取代基的取代基; 并且取代基R 1和R 4中的芳基，杂芳基，杂环基和碳环基团和部分是未取代的或被1,2或3个相同或不同并且选自卤素，C 1 -C 6烷基，C 1 -C 6 烷氧基，C1-C6烷硫基，羟基，氨基，C1-C6烷基氨基，二（C1-C6烷基）氨基，C1-C6卤代烷基，C1-C6卤代烷氧基和C1-C6卤代烷硫基取代基。条件是当n为1,2,3或4时，R4不为氢，当n为0时，X2为-CH2-，R1为芳基或杂芳基，则：（a）R为苯基携带至少一个-SCF 3取代基的基团，或是携带至少一个氯取代基的噻吩基; （d）R 1是携带至少一个-CF 3取代基或至少两个卤素取代基的苯基; 或（e）R 4为苄基或羟基

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