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1. 发明申请

WO2009115486A1 TRIAZOLE AMIDE DERIVATIVES FOR USE IN THERAPY 审中-公开
标题翻译：三唑胺衍生物用于治疗
公开(公告)号：WO2009115486A1
公开(公告)日：2009-09-24
申请号：PCT/EP2009/053070
申请日：2009-03-16
申请人： GLAXO GROUP LIMITED , GARZYA, Vincenzo , WATSON, Stephen, Paul
发明人： GARZYA, Vincenzo , WATSON, Stephen, Paul
IPC分类号： C07D249/06 , C07D401/04 , C07D401/12 , C07D403/12 , A61K31/4192 , A61P3/00 , A61P25/00
CPC分类号： C07D249/06 , C07D401/04 , C07D401/12 , C07D403/12
摘要： The invention relates to triazole amide derivatives of formula (I) for use in therapy, in particular for treating diseases and conditions mediated by antagonism of the mGluR 5 receptor, in particular substance related disorders. The invention also relates to certain novel derivatives. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明涉及式（I）的三唑酰胺衍生物，其用于治疗，特别是用于治疗由mGluR5受体的拮抗作用介导的疾病和病症，特别是与物质有关的疾病。本发明还涉及某些新型衍生物。此外，本发明涉及含有衍生物的组合物及其制备方法。

2. 发明申请

WO2009087220A1 USE OF THIAZOLOIMIDAZOLES, THIAZOLOTETRAZOLES AND THIAZOLOTRIAZOLES AS MGLUR5 ANTAGONISTS 审中-公开
标题翻译：三唑来膦酸作为MGLUR5拮抗剂使用噻唑酮和噻唑烷
公开(公告)号：WO2009087220A1
公开(公告)日：2009-07-16
申请号：PCT/EP2009/050217
申请日：2009-01-09
申请人： GLAXO GROUP LIMITED , D'ALESSANDRO, Pier , LORTHIOIR, Olivier, Eric , WATSON, Stephen, Paul
发明人： D'ALESSANDRO, Pier , LORTHIOIR, Olivier, Eric , WATSON, Stephen, Paul
IPC分类号： A61K31/429 , C07D513/00 , A61P25/00
CPC分类号： A61K31/429 , C07D513/04
摘要： The invention relates to the use of thiazolotriazole, thiazoloimidazole and thiazolotetrazole derivatives of formula (I) in treating diseases and conditions for which antagonism of the mGluR 5 receptor is beneficial, in particular substance related disorders. The invention also relates to certain novel derivatives. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明涉及式（I）的噻唑并三唑，噻唑并咪唑和噻唑四唑衍生物在治疗mGluR5受体拮抗作用有益的疾病和病症中的用途，特别是与物质有关的疾病。本发明还涉及某些新型衍生物。此外，本发明涉及含有衍生物的组合物及其制备方法。

3. 发明申请

WO2004110974A1 MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：WO2004110974A1
公开(公告)日：2004-12-23
申请号：PCT/EP2004/005966
申请日：2004-06-01
申请人： GLAXO GROUP LIMITED , GAINES, Simon , HOLMES, Ian, Peter , WATSON, Stephen, Paul
发明人： GAINES, Simon , HOLMES, Ian, Peter , WATSON, Stephen, Paul
IPC分类号： C07C59/48
CPC分类号： C07D307/91 , C07C17/16 , C07C59/48 , C07C59/54 , C07C59/56 , C07C59/68 , C07C59/90 , C07C205/56 , C07C233/54 , C07C255/57 , C07C323/62 , C07C2603/18 , C07D277/04 , C07C22/04
摘要： Compounds of formula (1): Wherein: Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents 0, S, NR 5 or CR 6 R 7 ; Y represents CHOH, CHSH, NOR 8 , CNR 8 or CNOR 8 ; Z represents a bond, CR 10 R 11 , 0,S,S0,S0 2 , NR 10 , OCR 10 R 11 , CR 10 R 11 O or Z, R 4 and Q together form an optionally substituted fused tricyclic group; R 1 , R 1’ , R 3 and R 3 each independently represents H, C 1-6 alkyl or C 1-4 alkylaryl; R 2 represents C0 2 R 8 , CONR 5 OR 9 or NR 5 COR 9 ; R 4 represents optionally substituted 5- or 6-membered aryl or heteroaryl; R 5 represents H or C 1-3 alkyl; R 6 and R 7 each independently represents H, C 1-3 alkyl or halo; R 8 represents H or C 1-2 alkyl; R 9 represents H or C 1-3 alkyl; R 10 and R 11 each independently represents H, C 1-6 alkyl or C 1-4 alkylaryl; and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metal loproteinase enzymes (MMPs) are described.
摘要翻译：式（1）的化合物：其中：Q表示任选取代的5或6元芳基或杂芳基环; X表示0，S，NR 5或CR 6 R 7; Y代表CHOH，CHSH，NOR 8，CNR 8或CNOR 8; Z表示键，CR 10 R 11，O，S，SO，SO 2，NR 10，OCR 10 R 11，CR 10 R 11或Z， 4>和Q一起形成任选取代的稠合三环基团; R 1，R 1，R 3和R 3各自独立地表示H，C 1-6烷基或C 1-4烷基芳基; R 2表示CO 2 R 8，CONR 5 OR 9或NR 5 COR 9; R 4表示任选取代的5或6元芳基或杂芳基; R 5表示H或C 1-3烷基; R 6和R 7各自独立地表示H，C 1-3烷基或卤素; R 8表示H或C 1-2烷基; R 9表示H或C 1-3烷基; R 10和R 11各自独立地表示H，C 1-6烷基或C 1-4烷基芳基; 及其生理功能衍生物，其制备方法，含有它们的药物制剂及其作为基质金属蛋白酶（MMP）抑制剂的用途。

4. 发明申请

WO0020112A2 CHEMICAL CONSTRUCTS AND THEIR USES 审中-公开
标题翻译：化学结构及其用途
公开(公告)号：WO0020112A2
公开(公告)日：2000-04-13
申请号：PCT/GB9903284
申请日：1999-10-05
申请人： GLAXO GROUP LTD , MCKEOWN STEPHEN CARL , WATSON STEPHEN PAUL
发明人： MCKEOWN STEPHEN CARL , WATSON STEPHEN PAUL
IPC分类号： G01N27/62 , C07B61/00 , C07D239/38 , C07K1/04 , C07K1/107 , C07K5/083 , C40B40/10 , C40B70/00 , G01N37/00 , B01J19/00
CPC分类号： C07K1/1077 , B01J2219/00572 , B01J2219/00596 , B01J2219/00702 , B01J2219/0072 , B01J2219/00725 , C07B2200/11 , C07D239/38 , C07K1/042 , C40B40/10 , C40B70/00
摘要： The invention provides a chemical construct for use in solid phase synthesis comprising a solid support Q having linked thereto groups Y R and Y R; wherein R is a substrate or a coding tag and the groups Y and Y are connecting groups each having a first cleavage site, at least one of Y and Y having a second cleavage site located between the first cleavage site and group R, the first cleavage site being orthogonally and selectively cleavable with respect to the second cleavage site, and, when both groups Y and Y contain a second cleavage site, the second cleavage site in Y being selectively and orthogonally cleavable with respect to the second cleavage site in Y ; the second cleavage site being cleavable to release the substrate; and the first cleavage site being selectively cleavable to release a fragment Fr comprising the substrate R and at least a portion of the connecting group Y; and wherein: (i) the chemical fragment Fr contains a sensitising group G which sensitises the chemical fragment Fr to instrumental, e.g. mass spectroscopic analysis; and/or (ii) the fragment Fr contains a means for imparting a characteristic signature to the mass spectrum of the fragment.
摘要翻译：本发明提供用于固相合成的化学构建体，其包含与Y 1 R和Y 2 R基团连接的固体载体Q; 其中R是底物或编码标签，基团Y 1和Y 2分别是具有第一切割位点的连接基团，Y 1和Y 2中的至少一个具有位于第二切割位点在第一切割位点和基团R之间，第一切割位点相对于第二切割位点是正交且可选择性切割的，并且当两个基团Y 1和Y 2都含有第二切割位点时，第二切割位点 Y 1相对于Y 2中的第二切割位点是选择性和正交可切割的; 第二切割位点可裂解以释放底物; 并且第一切割位点可选择性地切割以释放包含基底R和连接基团Y的至少一部分的碎片Fr; 并且其中：（i）化学片段Fr含有致敏基团G，其使化学片段Fr致敏，例如。质谱分析; 和/或（ii）片段Fr含有赋予片段质谱特性的方法。

5. 发明申请

WO2005040128A1 HETEROCYCLYL COMPOUNDS 审中-公开
标题翻译：杂环化合物
公开(公告)号：WO2005040128A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011964
申请日：2004-10-21
申请人： GLAXO GROUP LIMITED , GIBLIN, Gerard, Martin, Paul , HALL, Adrian , HURST, David, Nigel , LEWELL, Xiao, Qing , LORTHIOIR, Olivier, Eric , MCKEOWN, Stephen, Carl , SCOCCITTI, Tiziana , WATSON, Stephen, Paul
发明人： GIBLIN, Gerard, Martin, Paul , HALL, Adrian , HURST, David, Nigel , LEWELL, Xiao, Qing , LORTHIOIR, Olivier, Eric , MCKEOWN, Stephen, Carl , SCOCCITTI, Tiziana , WATSON, Stephen, Paul
IPC分类号： C07D231/14
CPC分类号： C04B35/632 , C07D207/34 , C07D231/14 , C07D401/12 , C07D409/04
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein W, X, Y, Z, R 1 , R 2a , R 2b , and R x , R 8 , and R 9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其药学上可接受的衍生物：其中W，X，Y，Z，R 1，R 2a，R 2b和R x，R 8和R 本说明书中定义，制备这些化合物的方法，包含这些化合物的药物组合物和这些化合物在医药中的用途。

6. 发明申请

WO2005026120A1 MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：WO2005026120A1
公开(公告)日：2005-03-24
申请号：PCT/EP2004/010319
申请日：2004-09-10
申请人： GLAXO GROUP LIMITED , GAINES, Simon , HOLMES, Ian, Peter , MARTIN, Stephen, Lewis , WATSON, Stephen, Paul
发明人： GAINES, Simon , HOLMES, Ian, Peter , MARTIN, Stephen, Lewis , WATSON, Stephen, Paul
IPC分类号： C07D209/48
CPC分类号： C07D209/48 , C07D239/54 , C07D403/10 , C07D405/10
摘要： Compounds of Formula (I): Wherein: A represents bond, C1-6alkyl or CH=CH-C1-4alkyl; B represents bond, O, S, SO, SO2, CO, CR7R8, CO2R14, CONR14R15, N(COR14)(COR15), N(SO2R14)(COR15) or NR14R15; D represents bond, or C1-6alkyl; E represents substituted aryl or substituted or unsubstituted heteroaryl; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, SO, SO2, CO, CNR5, CNOR5, CNNR5R6, NR11 or CR7R8; Y represents CR5OR11, CR5SR11, NOR5, CR5NR6R11, SO, SO2, CO, CNR5, CNOR5 or CS; R1 and R1' each independently represents H, C1-6alkyl or C1-4alkylaryl; R2 represents CO2R12, CH2OR12 or CONR12R13, CONR12OR13, NR12COR13, SR12, PO(OH)2, PONHR12 or SONHR12; R3 represents H, C1-6alkyl or C1-4alkylaryl; R4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR5, OCR5R6, CR9R10O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R5 and R6 each independently represent H, C1-6 alkyl or C1-4 alkylaryl; R7 and R8 each independently represent H, halo, C1-6 alkyl or C1-4 alkylaryl; R9 and R10 each independently represents H, C1-6 alkyl optionally substituted by halo, cyano, OR11 or NR6R11 , C1-4 alkylaryl optionally substituted by halo, cyano, OR11 or NR6R11, OR11 or, together with the N to which they are attached, R9 and R10 form a heterocyclic group: R11 represents H, C1-6 alkyl, C1-4 alkylaryl or COR5; R12 and R13 each independently represent H, C1-3 alkyl, C1-3 alkylaryl or C1-3 alkylheteroaryl or, together with the functionality to which they are attached, R12 and R13 form a heterocyclic group: R14 and R15 each independently represent H, C1-6 alkyl, C1-4 alkylaryl or C1-4 alkylheteroaryl or together with the functionality to which they are attached R14 and R15 form a heterocyclic or fused heterocyclic group: and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metallproteinase enzymes (MMPs) are described.
摘要翻译：式（I）化合物：其中：A表示键，C 1-6烷基或CH = CH-C 1-4烷基; B代表键，O，S，SO，SO2，CO，CR7R8，CO2R14，CONR14R15，N（COR14）（COR15），N（SO2R14）（COR15）或NR14R15; D表示键或C 1-6烷基; E表示取代的芳基或取代或未取代的杂芳基; Q表示任选取代的5或6元芳基或杂芳基环; X表示O，S，SO，SO 2，CO，CNR 5，CNOR 5，CNNR 5 R 6，NR 11或CR 7 R 8; Y代表CR5OR11，CR5SR11，NOR5，CR5NR6R11，SO，SO2，CO，CNR5，CNOR5或CS; R 1和R 1'各自独立地表示H，C 1-6烷基或C 1-4烷基芳基; R2代表CO 2 R 12，CH 2 OR 12或CONR 12 R 13，CONR 12 OR 13，NR 12 COR 13，SR 12，PO（OH）2，PONHR 12或SONHR 12; R3表示H，C1-6烷基或C1-4烷基芳基; R 4表示任选取代的芳基或杂芳基; Z表示键，CH2，O，S，SO，SO2，NR5，OCR5R6，CR9R10O或Z，R4和Q一起形成任选取代的稠合三环基团; R5和R6各自独立地表示H，C1-6烷基或C1-4烷基芳基; R 7和R 8各自独立地表示H，卤素，C 1-6烷基或C 1-4烷基芳基; R 9和R 10各自独立地表示H，任选被卤素，氰基，OR 11或NR 6 R 11取代的C 1-6烷基，任选被卤素，氰基，OR 11或NR 6 R 11，OR 11取代的C 1-4烷基芳基或与它们相连的N R 9和R 10形成杂环基：R 11表示H，C 1-6烷基，C 1-4烷基芳基或COR 5; R 12和R 13各自独立地表示H，C 1-3烷基，C 1-3烷基芳基或C 1-3烷基杂芳基，或者与它们所连接的官能团一起，R 12和R 13形成杂环基：R 14和R 15各自独立地表示H， C 1-6烷基，C 1-4烷基芳基或C 1-4烷基杂芳基或与它们所连接的官能团一起R14和R15形成杂环或稠合杂环基团及其生理功能衍生物，其制备方法，含有它们的药物制剂并且其用作基质金属蛋白酶（MMP）的抑制剂。

7. 发明申请

WO2009087218A1 THIAZOLTRIAZOLES AND THIAZOLIMIDAZOLES AS ANTAGONISTS OF THE MGLUR5 RECEPTOR 审中-公开
标题翻译：作为MGLUR5受体拮抗剂的噻唑啉和噻唑烷
公开(公告)号：WO2009087218A1
公开(公告)日：2009-07-16
申请号：PCT/EP2009/050215
申请日：2009-01-09
申请人： GLAXO GROUP LIMITED , D'ALESSANDRO, Pier, Luca , LORTHIOIR, Olivier, Eric , WATSON, Stephen, Paul
发明人： D'ALESSANDRO, Pier, Luca , LORTHIOIR, Olivier, Eric , WATSON, Stephen, Paul
IPC分类号： C07D513/04 , A61K31/429 , A61P25/00
CPC分类号： C07D513/04
摘要： This invention relates to novel thiazolotriazole and thiazoloimidazole derivatives of formula (I). The invention also relates to the use of the derivatives in treating diseases and conditions wherein antagonism of the mGluR5 receptor is beneficial, in particular substance related disorders. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明涉及式（I）的新型噻唑并三唑和噻唑并咪唑衍生物。本发明还涉及该衍生物在治疗其中mGluR5受体的拮抗作用有益的疾病和病症中的用途，特别是与物质相关的疾病。此外，本发明涉及含有衍生物的组合物及其制备方法。

8. 发明申请

WO2007014054A3 BENZENESULFONAMIDE INHIBITOR OF CCR2 CHEMOKINE RECEPTOR 审中-公开
公开(公告)号：WO2007014054A3
公开(公告)日：2007-02-01
申请号：PCT/US2006/028419
申请日：2006-07-21
申请人： GLAXO GROUP LIMTED , BROOKS, Carl , CLEARY, Pamela, A. , GOODMAN, Krista, B. , PEACE, Simon , PHILP, Joanne , SEHON, Clark, A. , SMETHURST, Christian , WATSON, Stephen, Paul
发明人： BROOKS, Carl , CLEARY, Pamela, A. , GOODMAN, Krista, B. , PEACE, Simon , PHILP, Joanne , SEHON, Clark, A. , SMETHURST, Christian , WATSON, Stephen, Paul
IPC分类号： A01N41/06 , A61K31/18
摘要： Disclosed are compounds of formula (I): or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a combination thereof, as well as compositions of methods of use of the compound, wherein R 1 , R 2 , R 3 , and m are described herein.

9. 发明申请

WO2007014008A2 BENZENESULFONAMIDE INHIBITOR OF CCR2 CHEMOKINE RECEPTOR 审中-公开
标题翻译： CCR2 CHEMOKINE受体的苯并呋喃半导体抑制剂
公开(公告)号：WO2007014008A2
公开(公告)日：2007-02-01
申请号：PCT/US2006028321
申请日：2006-07-21
申请人： GLAXO GROUP LIMTED , BROOKS CARL , PEACE SIMON , SMETHURST CHRISTIAN , WATSON STEPHEN PAUL
发明人： BROOKS CARL , PEACE SIMON , SMETHURST CHRISTIAN , WATSON STEPHEN PAUL
IPC分类号： A61K31/18
CPC分类号： C07D401/06 , C07D409/14
摘要： The present invention is related to a compound of formula (I) or a salt thereof, or a solvate thereof, or a combination thereof. The present invention also includes a compositions including the compound of Formula I as well as a method of treating disorders mediated by the CCR2 receptor with the compound of Formula I.
摘要翻译：本发明涉及式（I）化合物或其盐或其溶剂化物或其组合。本发明还包括包含式I化合物的组合物以及用式I化合物治疗由CCR2受体介导的病症的方法。

10. 发明申请

WO2005016868A2 MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：WO2005016868A2
公开(公告)日：2005-02-24
申请号：PCT/EP2004/009087
申请日：2004-08-12
申请人： GLAXO GROUP LIMITED , HOLMES, Ian , WATSON, Stephen, Paul
发明人： HOLMES, Ian , WATSON, Stephen, Paul
IPC分类号： C07C235/00
CPC分类号： C07C235/78 , C07C233/51 , C07C235/34 , C07C255/57 , C07C2601/14 , C07D209/08 , C07D333/24
摘要： Compounds of Formula (I), wherein R 1 represents optionally substituted -C 4-12 alkyl, -C 2-10 alkylcycloalkyl, -C 2-6 alkyl heterocycloalkyl, -C 2-6 alkylaryl, optionally substituted 5- or 6- membered aryl or heteroaryl, except pyridinyl. Z represents a bond, CH 2 , O, S, SO, SO 2 , NR 4 , OCR 4 R 5 , CR 4 R 5 O, or Z, R 1 and Q together form an optionally substituted fused tricyclic group; Q represents an optionally substituted 5- or 6- membered aryl or heteroaryl ring; X represents COR 3 ; R 2 represents CONH 2 , CO 2 H, CO 2 R 7 , SO 2 R 7 or SO 2 NR 8 R 9 , except that R 2 ; may not represent CO 2 R 7 when X is CONH 2 ; R 3 represents OR 6 , or NR 8 R 9 ; R 4 and R 5 each independently represents H, C 1-6 alkyl or C 1-4 alkylaryl; R 6 represents H or C 1-6 alkyl; R 7 represents C 1-6 alkyl; R 8 and R 9 each independently represents H or C 1-6 alkyl or R 8 and R 9 together with the nitrogen atom to which they are attached form a 5- or 6- membered ring which may optionally include 1 or more further heteroatoms selected from O, S and N; and physiologically functional derivatives thereof with the exception of [3-(acetylamino)-4-cyclohexylphenyl]-butanedioic acid and 3-(acetylamino)-4-cyclohexylphenyl]-butanedioic acid diethyl ether; butanedioic acid [3-methoxy-4-(phenylmethoxy)phenyl]; butanedioic acid [4-(phenylmethoxy)phenyl]; with the proviso that when R 1 represents C 4-12 alkyl, Z is other than a bond, O or CH 2 ; and physiologically functional derivatives thereof , processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metallproteinase enzymes (MMPs) are described.
摘要翻译：式（I）的化合物，其中R 1表示任选取代的-C 4-12烷基，-C 2-10烷基环烷基，-C 2-6烷基杂环烷基，-C 2-6烷基芳基，任选取代的5-或6-元芳基或杂芳基，除吡啶基外。 Z表示键，CH 2，O，S，SO，SO 2，NR 4，OCR 4 R 5，CR 4 R 5 O或Z，R 1和Q一起形成任选取代的稠合三环基团; Q表示任选取代的5或6元芳基或杂芳基环; X表示COR 3; R 2表示CONH 2，CO 2 H，CO 2 R 7，SO 2 R 7或SO 2 NR 8 R 9，除了R 2; 当X为CONH2时，可能不表示CO 2 R 7; R 3表示OR 6，或NR 8 R 9; R 4和R 5各自独立地表示H，C 1-6烷基或C 1-4烷基芳基; R 6表示H或C 1-6烷基; R 7表示C 1-6烷基; R 8和R 9各自独立地表示H或C 1-6烷基或R 8和R 9与它们所连接的氮原子一起形成5-或6-元环，其可任选地包括1个或更多个选自O，S和N的杂原子; 和其生理功能衍生物，但[3-（乙酰氨基）-4-环己基苯基]丁二酸和3-（乙酰基氨基）-4-环己基苯基]丁二酸二乙醚除外。丁二酸[3-甲氧基-4-（苯基甲氧基）苯基]; 丁二酸[4-（苯基甲氧基）苯基]; 条件是当R 1表示C 4-12烷基时，Z不是键O或CH 2; 和其生理功能衍生物，其制备方法，含有它们的药物制剂及其作为基质金属蛋白酶（MMP）抑制剂的用途。

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