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11. 发明申请

WO2007130823A3 POLYCYCLIC HETEROCYCLIC COMPOUNDS AND THEIR USE AS MODULATORS OF THE METABOTROPIC GLUTAMATE 5 RECEPTOR 审中-公开
标题翻译：多环杂环化合物及其作为代谢谷氨酸盐5受体的调节剂
公开(公告)号：WO2007130823A3
公开(公告)日：2008-01-24
申请号：PCT/US2007067370
申请日：2007-04-25
申请人： ASTRAZENECA AB , NPS PHARMA INC , ISAAC METHVIN , SLASSI ABDELMALIK , EDWARDS LOUISE , XIN TAO , WAALLBERG ANDREAS , STEFANAC TOMISLAV
发明人： ISAAC METHVIN , SLASSI ABDELMALIK , EDWARDS LOUISE , XIN TAO , WAALLBERG ANDREAS , STEFANAC TOMISLAV
IPC分类号： C07D413/14 , A61K31/4439 , A61P1/00 , A61P25/02 , A61P25/22
CPC分类号： C07D207/16 , C07D207/08 , C07D207/09 , C07D213/78 , C07D213/79 , C07D413/04 , C07D413/14
摘要： The present invention is directed to novel compounds of Formula (I) for modulation of metabotropic glutamate receptors (mGluRs), to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
摘要翻译：本发明涉及用于调节代谢型谷氨酸受体（mGluR）的新型式（I）化合物，其制备方法及其在治疗中的应用以及包含新化合物的药物组合物。

12. 发明申请

WO2007130824A3 FUSED HETEROCYLIC COMPOUNDS AND THEIR USE AS MGLUR5 MODULATORS 审中-公开
标题翻译：熔化的杂环化合物及其作为MGLUR5调制剂的用途
公开(公告)号：WO2007130824A3
公开(公告)日：2008-05-22
申请号：PCT/US2007067371
申请日：2007-04-25
申请人： ASTRAZENECA AB , WAALLBERG ANDREAS , NILSSON KAROLINA , GRANBERG KENNETH , GHOSAL SASWATI , SLASSI ABDELMALIK , EDWARDS LOUISE , ISAAC METHVIN , XIN TAO , STEFANAC TOMISLAV , DOVE PETER
发明人： WAALLBERG ANDREAS , NILSSON KAROLINA , GRANBERG KENNETH , GHOSAL SASWATI , SLASSI ABDELMALIK , EDWARDS LOUISE , ISAAC METHVIN , XIN TAO , STEFANAC TOMISLAV , DOVE PETER
IPC分类号： C07D487/04 , A61K31/4196 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
摘要翻译：本发明涉及新化合物，其制备方法，其在治疗中的应用和包含新化合物的药物组合物。

13. 发明申请

WO2007130825A3 FUSED HETEROCYCLIC COMPOUNDS AND THEIR USE AS MGLUR5 MODULATORS 审中-公开
标题翻译：熔融杂环化合物及其作为MGLUR5调制剂的用途
公开(公告)号：WO2007130825A3
公开(公告)日：2008-05-15
申请号：PCT/US2007067372
申请日：2007-04-25
申请人： ASTRAZENECA AB , ISAAC METHVIN , SLASSI ABDELMALIK , EDWARDS LOUISE , XIN TAO , STEFANAC TOMISLAV , DOVE PETER , NAAGAARD MATS
发明人： ISAAC METHVIN , SLASSI ABDELMALIK , EDWARDS LOUISE , XIN TAO , STEFANAC TOMISLAV , DOVE PETER , NAAGAARD MATS
IPC分类号： C07D487/04 , A61K31/4196 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
摘要翻译：本发明涉及新化合物，其制备方法，其在治疗中的应用和包含新化合物的药物组合物。

14. 发明申请

WO2007021575A3 ACETYLENIC PIPERAZINES AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：乙酰胆碱作为代谢谷氨酸受体拮抗剂
公开(公告)号：WO2007021575A3
公开(公告)日：2007-04-05
申请号：PCT/US2006030394
申请日：2006-08-04
申请人： ASTRAZENECA AB , NPS PHARMA INC , EDWARDS LOUISE , ISAAC METHVIN , SLASSI ABDELMALIK , SUN GUANG-RI , DOVE PETER , ARZEL ERWAN
发明人： EDWARDS LOUISE , ISAAC METHVIN , SLASSI ABDELMALIK , SUN GUANG-RI , DOVE PETER , ARZEL ERWAN
IPC分类号： C07D487/04 , A61K31/4985 , A61P1/00 , A61P25/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar 1 , A, B, R 1 , m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR 5 mediated disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐或溶剂化物：其中Ar 1，A，B，R 1，m和n如说明书中所定义。本发明还包括药物组合物及其制备方法及其制备方法以及治疗mGluR5介导的病症的方法。

15. 发明专利

CA2287551C 3-(2-PYRROLIDINYLMETHYL)-INDOLE COMPOUNDS HAVING 5-HT6 AFFINITY 未知
公开(公告)号：CA2287551C
公开(公告)日：2009-06-02
申请号：CA2287551
申请日：1999-03-16
申请人： EDWARDS LOUISE , SLASSI ABDELMALIK , O'BRIEN ANNE , XIN TAO , TEHIM ASHOK
发明人： EDWARDS LOUISE , SLASSI ABDELMALIK , O'BRIEN ANNE , XIN TAO , TEHIM ASHOK
IPC分类号： C07D403/06 , A61K31/40 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Described herein are compounds with affinity for the 5-HT6 receptor, which have general formula (I) wherein: R1 is selected from the group consisting of H and C1-4alkyl; R2 is selected from the group consisting of H, C1-4alkyl and benzyl; R3 is selected from the group consisting of COR5, SO2R5, CONHC1-4alkyl and C(S)SR6; R4a is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R4b is selected from the group consisting of H, hydroxy, halo, C 3- 7cycloalkyloxy, C1-4alkoxy; C1-4alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl; R4c is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R4d is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R5 is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C1-4alkoxy, C1-4alkyl, halo, nitro, trifluoromethyl, trifluoromethoxy, 1,2-methylenedioxy, C1-4alkylcarbonyl, C1 - 4alkoxycarbonyl and C1-4alkylS-; and R6 is selected from C1-4alkyl, allyl, propargyl and optionally substituted benzyl wherein the benzyl group is optionally substituted with 1-4 substituents selected from cyano, C1-4alkyl and halo. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.

16. 发明专利

CA2287551A1 PYRROLIDINE-INDOLE COMPOUNDS HAVING 5-HT6 AFFINITY 未知
公开(公告)号：CA2287551A1
公开(公告)日：1999-09-23
申请号：CA2287551
申请日：1999-03-16
申请人： O'BRIEN ANNE , EDWARDS LOUISE , TEHIM ASHOK , XIN TAO , SLASSI ABDELMALIK
发明人： O'BRIEN ANNE , EDWARDS LOUISE , TEHIM ASHOK , XIN TAO , SLASSI ABDELMALIK
IPC分类号： C07D403/06 , C07D405/14 , C07D409/14 , C07D401/14 , A61K31/40
摘要： Described herein are compounds with affinity for the 5-HT6 receptor, which have general formula (I) wherein: R1 is selected from the group consisting of H and C1-4alkyl; R2 is selected from the group consisting of H, C1-4alkyl and benzyl; R3 is selected from the group consisting of COR5, SO2R5, CONHC1-4alkyl and C(S)SR6; R4a is selected from the group consisting of H, OH, halo, C14alkyl and C1-4alkoxy; R4b is selected from the group consisting of H, hydroxy, halo, C3-7cycloalkyloxy, C1-4alkoxy; C1-4alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl; R4c is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R4d is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R5 is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C14alkoxy, C1-4alkyl, halo, nitro, trifluoromethyl, trifluoromethoxy, 1,2methylenedioxy, C1-4alkylcarbonyl, C1-4alkoxycarbonyl and C1-4alkylS-; and R6 is selected from C1-4alkyl, allyl, propargyl and optionally substituted benzyl wherein the benzyl group is optionally substituted with 1-4 substituents selected from cyano, C1-4alkyl and halo. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5HT6 receptor is implicated, such as schizophrenia.

17. 发明申请

WO0105758A3 INDOLES AND INDAZOLES FOR THE TREATMENT OF MIGRAINE 审中-公开
标题翻译：用于治疗。。。。。。。。。。。
公开(公告)号：WO0105758A3
公开(公告)日：2001-07-19
申请号：PCT/CA0000831
申请日：2000-07-14
申请人： NPS ALLELIX CORP , EDWARDS LOUISE , ISAAC METHVIN , MADDAFORD SHAWN , SLASSI ABELMALIK , XIN TAO
发明人： EDWARDS LOUISE , ISAAC METHVIN , MADDAFORD SHAWN , SLASSI ABELMALIK , XIN TAO
IPC分类号： A61K31/351 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/416 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/551 , A61P25/06 , A61P43/00 , C07D209/08 , C07D231/56 , C07D309/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07F7/08
CPC分类号： C07F7/0814 , C07D209/08 , C07D231/56 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Described herein are compounds useful in the treatment of migraine, which have general formulae (I), (II), (III) and (IV), wherein : W is a CH group or an N atom ;Z is N or C-R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula (II), (III) or (IV), such that group A contains at least 1 N atom ; NR7 is either -NH- or -N= --- is a single or double bond ; X is an N atom, a CH group or a C(OH) group when --- is a single bond; or, when --- is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent an N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c and d is at least 2 and the sum of e and f is at least 2; R1 is selected from the group consisting of H, alkyl, alkyloxy, alkanoyl, aminoalkylenyl, alkylaminoalkylenyl, a hydroxyalkylenyl group, an alkyloxyalkylenyl group, a cycloalkyl group, a cycloalkylalkylenyl group, a heterocycloalkyl group, a heterocycloalkylalkylenyl group, an aryl group, a heterocycloaryl group, an amido group, a thioamido group, an arylcarbonyl group and an arylsulfonyl group; R2 and R3 are independently selected from the group consisting of H, alkyl, cycloalkyl, alkenyl and optionally-substituted benzyl; or R2 and R3, together with the nitrogen atom to which they are attached, may form a mono- or bi-cyclic group containing up to 10 carbon atoms and which, in addition, may contain a second heteroatom selected from the group consisting of N, S and O, and which may contain one or more substituents selected from the group consisting of alkyl, hydroxy, hydroxymethyl, alkyloxymethyl, amino and substituted amino; R4 is selected from the group consisting of H, alkyl and cycloalkyl; CR5 represents a group selected from -CH2-, CH(OH)-, -C(O)-, -CH(alkyl)- and -CH(alkyloxy)-; R6 is selected from the group consisting of H, alkyl, aryl, halogen, hydroxy, alkyloxy, amino, monoalkylamino and di-substituted alkylamino; and salts and solvates thereof.
摘要翻译：本文描述了可用于治疗偏头痛的化合物，其具有通式（I），（II），（III）和（IV），其中：W为CH基或N原子; Z为N或C-R4 ; B和D独立地选自CH和N，条件是B和D中的至少一个是CH，进一步的条件是仅当W和Z都不是N时，B和D中的一个可以表示N; A是式（II），（III）或（IV）的基团，使得A组含有至少1个N原子; NR 7是-NH-或-N = - 单键或双键; 当-O-单键时，X是N原子，CH基团或C（OH）基团; 或者当 - 是双键时，C原子; Y是NH，N-烷基，N-苄基或CH2基团; U和V各自表示N原子或CH基团，条件是两者不能为N; a和b独立地为0或1; c是0至3的整数; d为1〜3的整数; e为1〜2的整数; f为0〜3的整数; g为3〜6的整数，h为2〜3的整数，使得c和d的和为至少2，e和f的和为至少2; R 1选自H，烷基，烷氧基，烷酰基，氨基亚烷基，烷基氨基亚烷基，羟基烷基，烷氧基亚烷基，环烷基，环烷基亚烷基，杂环烷基，杂环烷基亚烷基，芳基，杂环基基团，酰胺基，硫代酰氨基，芳基羰基和芳基磺酰基; R2和R3独立地选自H，烷基，环烷基，烯基和任选取代的苄基; 或R 2和R 3与它们所连接的氮原子一起可以形成含有至多10个碳原子的单环或双环基团，并且另外可以含有选自N ，S和O，并且其可以含有一个或多个选自烷基，羟基，羟甲基，烷氧基甲基，氨基和取代的氨基的取代基; R 4选自H，烷基和环烷基; CR 5表示选自-CH 2 - ，CH（OH） - ， - C（O） - ， - CH（烷基） - 和-CH（烷氧基） - 的基团。 R 6选自H，烷基，芳基，卤素，羟基，烷氧基，氨基，单烷基氨基和二取代的烷基氨基; 及其盐和溶剂合物。

18. 发明专利

UY30309A1 MODULADORES DE MGLUR5 II 未知
公开(公告)号：UY30309A1
公开(公告)日：2007-11-30
申请号：UY30309
申请日：2007-04-25
申请人： ASTRAZENECA AB , NPS PHARMA INC
发明人： SLASSI ABDELMALIK , XIN TAO , EDWARDS LOUISE , METHVIN ISAAC
IPC分类号： C07D249/08 , A61K31/41 , A61K31/4196 , A61K31/435 , A61P1/00 , A61P25/00 , C07D211/06 , C07D213/02
摘要： Compuestos novedosos, un proceso para su preparacion, su utilizacion en terapia y composiciones farmacéuticas que los comprenden.

19. 发明专利

BRPI0417308A 未知
公开(公告)号：BRPI0417308A
公开(公告)日：2007-09-11
申请号：BRPI0417308
申请日：2004-12-13
申请人： ASTRAZENECA AB , NPS PHARMA INC
发明人： WENSBO DAVID , EDWARDS LOUISE , ISAAC METHVIN , MCLEOD DONALD A , SLASSI ABDELMALIK , XIN TAO , STORMANN THOMAS M
IPC分类号： C07D401/04 , A61K31/4439 , A61P25/04 , C07D213/84
摘要： The present invention relates to new compounds of formula I, wherein Z, Q, X1, X2, R1 and R2, are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.

20. 发明专利

BRPI0507481A 未知
公开(公告)号：BRPI0507481A
公开(公告)日：2007-07-17
申请号：BRPI0507481
申请日：2005-02-17
申请人： ASTRAZENECA AB , NPS PHARMA INC
发明人： ARORA JALAJ , EDWARDS LOUISE , ISAAC METHVIN , KERS ANNIKA , STAAF KARIN , SLASSI ABDELMALIK , STEFANAC TOMISLAV , WENSBO DAVID , XIN TAO , HOLM BJ RN
IPC分类号： C07D413/14 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61P25/00 , C07D401/14
摘要： The present invention relates to new compounds of formula (I), wherein P, Q, X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , R 1 , R 2 , R 3 , m, n, and p are as defined as in formula (I), or salts, or hydrates thereof, processes for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.

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