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1. 发明申请

WO2004062665A1 HETEROARYL- SUBSTITUTED PYRROLO` 2, 3- B! PYRIDINE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译： HETEROARYL-替代PYRROLO` 2，3-B！吡啶衍生物作为CRF受体拮抗剂
公开(公告)号：WO2004062665A1
公开(公告)日：2004-07-29
申请号：PCT/EP2004/000409
申请日：2004-01-14
申请人： SB PHARMCO PUERTO RICO INC , NEUROCRINE BIOSCIENCES INC , GLAXO GROUP LIMITED , CASTIGLIONI, Emiliano , DI FABIO, Romano , FERIANI, Aldo , MICHELI, Fabrizio , SABBATINI, Fabio , ST-DENIS, Yves
发明人： CASTIGLIONI, Emiliano , DI FABIO, Romano , FERIANI, Aldo , MICHELI, Fabrizio , SABBATINI, Fabio , ST-DENIS, Yves
IPC分类号： A61K31/437
CPC分类号： C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供了包括其立体异构体，前体药物和药学上可接受的盐或溶剂合物的式（I）化合物，其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症）。

2. 发明申请

WO2002100863A1 CORTICOTROPIN RELEASING FACTOR ANTAGONISTS 审中-公开
标题翻译： CORTICOTROPIN释放因子拮抗剂
公开(公告)号：WO2002100863A1
公开(公告)日：2002-12-19
申请号：PCT/GB2002/002656
申请日：2002-06-11
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
发明人： DI FABIO, Romano , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K51/0459 , C07B2200/05 , C07D239/70 , C07D239/94 , C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, wherein R is aryl or heteroaryl and each of the above groups R may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -COR 4 , nitro, -NR 3 R 4 cyano, or a group R 5 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR 3 R 4 or cyano; R 2 corresponds to a group CHR 6 R 7 ; R 3 is hydrogen, C1-C6 alkyl; R 4 independently from R 3 , has the same meanings; R 5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle; wherein each of the above groups R 5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 dialkylamino, nitro or cyano; R 6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R 6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R 7 independently from R 6 , has the same meanings; X is carbon or nitrogen; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供式（I）化合物，其包括立体异构体，其前药和药学上可接受的盐或溶剂化物，其中R是芳基或杂芳基，并且上述基团中的每一个R可以被1至4个选自以下的基团取代：卤素， C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-COR 4，硝基，-NR 3 R 4氰基或基团R 5; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; R2对应于CHR6R7基团; R3是氢，C1-C6烷基; R4独立于R3，具有相同的含义; R5是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中上述基团R 5可以被一个或多个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6 烷氧基，C1-C6二烷基氨基，硝基或氰基; R 6是氢，C 2 -C 6烯基或C 1 -C 6烷基，其中上述基团R 6可以被一个或多个选自：C 1 -C 6烷氧基和羟基的基团取代; R7独立于R6，具有相同的含义; X是碳或氮; 其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

3. 发明申请

WO2002087573A1 CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译： CRF受体拮抗剂
公开(公告)号：WO2002087573A1
公开(公告)日：2002-11-07
申请号：PCT/GB2002/001981
申请日：2002-04-30
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MICHELI, Fabrizio , PASQUARELLO, Alessandra , ST-DENIS, Yves
发明人： DI FABIO, Romano , MICHELI, Fabrizio , PASQUARELLO, Alessandra , ST-DENIS, Yves
IPC分类号： A61K31/4353
CPC分类号： C07D471/06 , C07D487/06
摘要： The present invention relates to tricyclic pyrimidines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereofwherein R is aryl or heteroaryl, wherein each of the above groups R may be substituted by 1 to 4 substituents indendently selected from the group consisting of:halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 mono or dialkylamino, nitro, cyano and a group R 4 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, NH 2 , halogen or cyano; R 2 is hydrogen or C(H) n (R 5 ) q (CH 2 ) p ZR 6 ; R 3 is hydrogen, C2-C6 alkenyl, C2-C6 alkynyl or [CH(R 5 )(CH 2 ) p ] m ZR 6 ; R 4 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle; wherein each of the above groups R 4 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 mon a or dialkylamino, nitro, and cyano; R 5 is hydrogen, C2-C6 alkenyl, C2-C6 alkynyl or (CH 2 ) p ZR 6 ; R 6 is C1-C6 alkyl, which may be substituted by one or more groups selected from halogen, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 alkoxy, C1-C6 mono or dialkylamino, nitro, cyano and a group R 4 ; Y and X are independently carbon or nitrogen; m and n are independently 0 or 1; p is 0 or an integer from 1 to 4;q is 1 or 2;Z is a bond, O, NH or S;to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明涉及式（I）的三环嘧啶化合物，包括立体异构体，其前药和药学上可接受的盐或溶剂化物，其中R是芳基或杂芳基，其中上述基团R中的每一个可以被1至4个取代基所取代，由以下组成：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，C 1 -C 6单或二烷基氨基，硝基，氰基和 R4; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，NH 2，卤素或氰基; R2是氢或C（H）n（R5）q（CH2）pZR6; R3是氢，C2-C6烯基，C2-C6炔基或[CH（R5）（CH2）p] mZR6; R4是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中每个上述基团R 4可以被一个或多个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6 烷氧基，C 1 -C 6单烷基或二烷基氨基，硝基和氰基; R5是氢，C2-C6烯基，C2-C6炔基或（CH2）pZR6; R6是C1-C6烷基，其可以被一个或多个选自卤素，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，C 1 -C 6烷氧基，C 1 -C 6 单或二烷基氨基，硝基，氰基和基团R 4; Y和X独立地为碳或氮; m和n独立地为0或1; p为0或1至4的整数; q为1或2; Z为O，NH或S键;其制备方法为含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）。

4. 发明申请

WO2003008412A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2003008412A2
公开(公告)日：2003-01-30
申请号：PCT/EP2002/007865
申请日：2002-07-15
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MICHELI, Fabrizio , ST-DENIS, Yves
发明人： DI FABIO, Romano , MICHELI, Fabrizio , ST-DENIS, Yves
IPC分类号： C07D471/00
CPC分类号： C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, wherein R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -C(O)R 5 , nitro, -NR 6 R 7 , cyano, and a group R 8 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR 6 R 7 or cyano; R 2 is hydrogen, C3-C7 cycloalkyl, or a group R 9 ; R 3 is C3-C7 cycloalkyl, or a group R 9 ; or R 2 and R 3 together with N form a 5-14 membered heterocycle, which may be substituted 1 to 3 R 10 groups; R 4 is hydrogen, C1-C6 alkyl, halogen or halo C1-C6 alkyl; R 5 is a C1-C4 alkyl, -OR 6 or NR 6 R 7 ; R 6 is hydrogen or C1-C6 alkyl; R 7 is hydrogen or C1-C6 alkyl; R 8 is a 5-6 membered heterocycle, which may be saturated or may contain one to three double bonds, and which may be substituted by 1 or more R 11 groups; R 9 is a C1-C6 alkyl that may be substituted by one or more groups selected from: C3-C7 cycloalkyl, C1-C6 alkoxy, halo C1-C6 alkoxy, hydroxy, halo C1-C6 alkyl; R 10 is a group R 8 , C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, C(O)NR 6 R 7 , phenyl which may be substituted by 1 to 4 R 11 groups; R 11 is C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, or C(O)NR 6 R 7 ; X is carbon or nitrogen; n is 1 or 2; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供式（I）化合物，其包括其立体异构体，前药和药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基，其各自可以被1-4个选自以下的基团取代：卤素，C 1 -C 6烷基， C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-C（O）R 5，硝基，-NR 6 R 7，氰基和基团R 8; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 6 R 7或氰基; R2是氢，C3-C7环烷基或基团R9; R 3为C 3 -C 7环烷基或基团R 9; 或R 2和R 3与N一起形成5-14元杂环，其可以被取代1至3个R 10基团; R4是氢，C1-C6烷基，卤素或卤素C1-C6烷基; R5是C1-C4烷基，-OR6或NR6R7; R6是氢或C1-C6烷基; R7是氢或C1-C6烷基; R8是5-6元杂环，其可以是饱和的或可以含有一至三个双键，并且其可以被1个或多个R 11基团取代; R9是可以被一个或多个选自以下的基团取代的C 1 -C 6烷基：C 3 -C 7环烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷氧基，羟基，卤代C 1 -C 6烷基; R 10是基团R 8，C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，羟基，卤素，硝基，氰基，C（O）NR 6 R 7，可被1至4个R 11基团取代的苯基; R 11是C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，羟基，卤素，硝基，氰基或C（ O）NR6R7; X是碳或氮; n为1或2; 其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

5. 发明申请

WO2003008414A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2003008414A1
公开(公告)日：2003-01-30
申请号：PCT/US2002/022394
申请日：2002-07-15
申请人： SB PHARMCO PUERTO RICO INC. , NEUROCRINE BIOSCIENCES INC. , DI FABIO, Romano , MICHELI, Fabrizio , REGAN, Collin, F. , SCHWAEBE, Michael, K. , ST-DENIS, Yves
发明人： DI FABIO, Romano , MICHELI, Fabrizio , REGAN, Collin, F. , SCHWAEBE, Michael, K. , ST-DENIS, Yves
IPC分类号： C07D471/16
CPC分类号： C07D471/16
摘要： The present invention relates to tricyclic pyridines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof Please insert formula (I) here: to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明涉及包括立体异构体，前体药物和药学上可接受的盐或溶剂化物的式（I）的三环吡啶化合物。请在此处插入式（I）：其制备方法，含有它们的药物组合物及其在治疗中的用途的促肾上腺皮质激素释放因子（CRF）介导的病症。

6. 发明申请

WO2008148853A1 N-PHENYL HYDRAZIDES AS MODULATORS OF THE GHRELIN RECEPTOR 审中-公开
标题翻译：作为GHRELIN受体的调节剂的N-苯基水杨酸
公开(公告)号：WO2008148853A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/057018
申请日：2008-06-05
申请人： GLAXO GROUP LIMITED , BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
发明人： BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
IPC分类号： C07D213/54 , C07D239/26 , C07D307/79 , C07D307/85 , C07D307/91 , C07D317/46 , C07D317/60 , C07D319/18 , C07D333/72 , C07D333/76 , C07D405/06 , C07D471/04 , C07D487/04 , C07D295/15 , A61K31/498
CPC分类号： C07D333/76 , C07D211/34 , C07D213/56 , C07D213/61 , C07D239/26 , C07D295/15 , C07D307/81 , C07D307/85 , C07D307/91 , C07D317/46 , C07D317/60 , C07D319/18 , C07D333/60 , C07D405/06 , C07D471/04 , C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: each R 1 is independently selected from the group consisting of Cl, Br, CH 3 and CF 3 ; X is carbon or nitrogen; R 1a is H or a straight C 1-3 alkyl group; R 2a is H or a methyl group R 2 is selected from the group consisting of C 1-3 alkyl, H and -(CH 2 ) n -, wherein n is 3 or 4 and the terminal carbon of the chain is bonded to the carbon atom adjacent to the nitrogen bearing the R 2 group, such that a fused 6,5 or 6,6-bicyclic ring is formed. Y is selected from the group consisting of: phenyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of C 1-3 alkyl, C 1-3 alkoxy, halogen, C 1-3 alkyl substituted by 1 to 7 fluoro atoms and C 1-3 alkoxy substituted by 1 to 7 fluoro atoms; pyridyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of C 1-3 alkyl, OCH 3 , CF 3 , CN, and halogen; naphthyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of F and OCH 3 ; pyrimidinyl; imidazo[1,2-a]pyridine-6-yl; benzothiophen-2-yl; benzothiophen-5-yl; benzofuran-2-yl; dibenzo[b,d]furan-3-yl; dibenzo[b,d]thiophen-2-yl; dibenzo[b,d]thiophen-4-yl; 1,3- benzodioxol-5-yl; 2,3-dihydro-1,4-benzodioxin-5-yl; 2,3-dihydro-1,4-benzodioxin-6-yl; 2,3- dihydro-1-benzofuran-4-yl; 2,2-difluoro-1,3-benzodiox-4-yl; pyridazinyl; imidazolyl; oxazolyl; pyrazolyl; thiazolyl; and triazolyl; with the proviso that when Y is 2,3-dihydro-1,4-benzodioxin-6-yl, R 1 is not Cl; processes for their preparation, intermediates useble in these processes, pharmaceutical compositions containing them and their use in therapy, for example as modulators of of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂化物，其中：每个R 1独立地选自Cl，Br，CH 3和CF 3; X是碳或氮; R 1a是H或直链C 1-3烷基; R2a是H或甲基R2选自C1-3烷基，H和 - （CH2）n-，其中n是3或4，并且该链的末端碳键合到邻近的碳原子上含有R2基团的氮，使得形成稠合的6,5或6,6-双环。 Y选自：可以是未取代的或被一个或多个独立地选自C 1-3烷基，C 1-3烷氧基，卤素，被1至7个氟原子取代的C 1-3烷基和C 1 由1-7个氟原子取代的3-烷氧基; 吡啶基，其可以是未取代的或被一个或多个独立地选自C 1-3烷基，OCH 3，CF 3，CN和卤素的取代基取代; 萘基，其可以是未取代的或被一个或多个独立地选自F和OCH 3的取代基取代; 嘧啶; 咪唑并[1,2-a]吡啶-6-基; 苯并噻吩-2-基; 苯并噻吩-5-基; 苯并呋喃-2-基; 二苯并[b，d]呋喃-3-基; 二苯并[b，D]噻吩-2-基; 二苯并[b，D]噻吩-4-基; 1,3-苯并间二氧杂环戊烯-5-基; 2,3-二氢-1,4-苯并二恶英-5-基; 2,3-二氢-1,4-苯并二恶英-6-基; 2,3-二氢-1-苯并呋喃-4-基; 2,2-二氟-1,3- benzodiox -4-基; 哒嗪; 咪唑; 恶唑; 吡唑; 噻唑基; 和三唑基; 条件是当Y是2,3-二氢-1,4-苯并二恶英-6-基时，R 1不是Cl; 其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，例如作为生长激素促分泌素受体（也称为生长素释放肽受体或GHSR1a受体）的调节剂和/或用于治疗和/或预防由生长素释放肽受体介导的病症。

7. 发明申请

WO2008148854A1 GHRELIN MODULATORS 审中-公开
标题翻译： GHRELIN调制器
公开(公告)号：WO2008148854A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/057019
申请日：2008-06-05
申请人： GLAXO GROUP LIMITED , BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
发明人： BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
IPC分类号： C07D401/06
CPC分类号： C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes for their preparation, intermediates useble in these processes, pharmaceutical compositions containing them and their use in therapy, for example as modulators of of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂化物，其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，例如作为生长调节剂激素促分泌素受体（也称为生长素释放肽受体或GHSR1a受体）和/或用于治疗和/或预防由生长素释放肽受体介导的病症。

8. 发明申请

WO2008031772A1 AZABICYCLIC COMPOUNDS AS INHIBITORS OF MONOAMINES REUPTAKE 审中-公开
标题翻译：单一化合物作为单体反应的抑制剂
公开(公告)号：WO2008031772A1
公开(公告)日：2008-03-20
申请号：PCT/EP2007/059381
申请日：2007-09-07
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D221/04 , A61K31/435 , A61P25/00
CPC分类号： C07D221/04
摘要： The present invention relates to novel compounds of formula (I)´, pharmaceutically acceptable salts, prodrugs or solvates thereof: wherein R 1 is hydrogen or C 1-4 alkyl; R 2 is a group A, K or W wherein A is (II) K is an α or β naphthyl group, optionally substituted by 1 or 2 groups R 18 , each of them being the same or different; and W is (III) and wherein G is a 5,6-membered monocyclic heteroaryl, or a 8- to 11-membered heteroaryl bicyclic group; such G may be substituted by (R 15 ) p , which can be the same or different; p is an integer from 0 to 5; R 3 is selected in the group consisting of: hydrogen, fluorine, and C 1-4 alkyl; or corresponds to a group X or X 1 ; R 4 is selected in the group consisting of: hydrogen, fluorine, and C 1-4 alkyl; or corresponds to a group X or X 1 ; R 5 is hydrogen or C 1-4 alkyl; R 7 is hydrogen or C 1-4 alkyl; or is a group X, X 1 , X 2 or X 3 ; wherein X is (IV) X 1 is (V) X 2 is (VI) and X 3 is (VII) R 6 is hydrogen or C 1-4 alkyl; or is a group X or X 1 ; R 9 is C 1-4 alkyl; R 10 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 8 is a 5-6 membered heterocycle group, which may be substituted by one or two substituents selected from a group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy and C 1-4 alkanoyl; R 11 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 12 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 13 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 14 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 15 is selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 16 is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl or C 3-6 cycloalkylC 1-3 alkyl; R 17 is hydrogen or C 1-4 alkyl; R 18 is selected from a group consisting of: halog
摘要翻译：本发明涉及新的式（I）化合物，其药学上可接受的盐，前药或溶剂合物：其中R 1是氢或C 1-4烷基; R 2是基团A，K或W，其中A是（II）K是任选被1或2个基团R 18取代的a或β萘基，每个他们是相同或不同的; 并且W是（III），并且其中G是5,6-元单环杂芳基或8至11元杂芳基双环基团; 这样的G可以被相同或不同的（R 15） p是0至5的整数; R 3 3选自：氢，氟和C 1-4烷基; 或对应于组X或X 1 1; R 4选自：氢，氟和C 1-4烷基; 或对应于组X或X 1 1; R 5是氢或C 1-4烷基; R 7是氢或C 1-4烷基; 或者为X，X 1，X 2或X 3; 其中X是（Ⅳ）ⅩⅢ是（Ⅴ）ⅩⅥ是（Ⅵ），ⅩⅢ是（Ⅶ） 6是氢或C 1-4烷基; 或者是X或X 1族; R 9是C 1-4烷基; R 10选自：氢，卤素，羟基，氰基，C 1-4 - 烷基，卤代C 1-4 - 烷基 C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; 或对应于基团R 8; R 8是5-6元杂环基团，其可以被一个或两个选自以下的取代基取代：卤素，氰基，C 1-4烷基卤代C 1-4烷基，C 1-4烷氧基和C 1-4烷酰基; R 11选自：氢，卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5。或对应于基团R 8; R 12选自：氢，卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5。或对应于基团R 8; R 13选自：氢，卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基 C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; 或对应于基团R 8; R 14选自：氢，卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5。或对应于基团R 8; R 15选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4个碳原子的烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5。或对应于基团R 8; R 16是氢，C 1-4烷基，C 3-6环烷基或C 3-6环烷基C _{1-3 烷基; R 17是氢或C 1-4烷基; R 18选自：卤素}

9. 发明申请

WO2007113232A1 AZABICYCLO [3. 1. 0] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZABICYCLO [3。作为DOPAMINE D3受体的调节剂的HEXYL衍生物
公开(公告)号：WO2007113232A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053074
申请日：2007-03-30
申请人： Glaxo Group Limited , BERTANI, Barbara , BONANOMI, Giorgio , CAPELLI, Anna Maria , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BERTANI, Barbara , BONANOMI, Giorgio , CAPELLI, Anna Maria , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , A61K31/513 , A61P25/00
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I)' or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11 -membered heteroaryl bicyclic group; A is a group P1 or a group P2 Wherein p is an integer ranging from 0 to 5; R 1 is halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1- 4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 6 ; and when p is an integer ranging from 2 to 5, each R 1 may be the same or different; R 2 is hydrogen or C 1-4 alkyl; n is 3, 4, 5 or 6; R 6 is a moiety selected from the group consisting of: isoxazolyl, -CH 2 -N-pyrrolyl, 1,1 -dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such R 6 group is optionally substituted by one or two substituents selected from: halogen, cyano, C 1- 4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; R 4 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C 1- 4 alkyl, C 3-7 cycloalkyl, haloC 1-4 alkyl, C 1-4- alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and NR'R"; or R 4 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl, haloC 1-4 alkoxy and SF 5 ; R 5 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, C 3-7 cycloalkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and NR'R"; or R 5 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; R 7 is hydrogen or C 1-2 alkyl; R' is H, C 1-4 alkyl or C 1-4 alkanoyl; R" is defined as R'; R' and R" taken together with the interconnecting nitrogen atom may form a 5-, 6- membered saturated or unsaturated heterocyclic ring; wherein at least one of R 4 and R 5 is hydrogen; and wherein only one R 2 group may be different from hydrogen; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中G选自：苯基，5-或6-元单环杂芳基或8-至11元杂芳基双环基团 A是基团P1或基团P2，其中p是0至5的整数; R 1是卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷基，烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; 或对应于基团R 6; 并且当p是2至5的整数时，每个R 1可以相同或不同; R 2是氢或C 1-4烷基; n为3,4,5或6; R 6是选自以下的部分：异恶唑基，-CH 2 - N-吡咯基，1,1-二氧代-2-异噻唑烷基，噻吩基，噻唑基，吡啶基，2-吡咯烷酮基和这样的R 6 C 6基团任选地被一个或两个选自以下的取代基取代：卤素，氰基，C 1-4 - >一

10. 发明申请

WO2005080382A1 AZABICYCLO (3.1.0) HEXANE DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZ Y Y O O O O S S S S S S S S S S S S S S S S S S S S S S S S S S
公开(公告)号：WO2005080382A1
公开(公告)日：2005-09-01
申请号：PCT/EP2005/001940
申请日：2005-02-21
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , BONANOMI, Giorgio , CAPELLI, Anna Maria , DAMIANI, Federica , DI FABIO, Romano , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
发明人： ARISTA, Luca , BONANOMI, Giorgio , CAPELLI, Anna Maria , DAMIANI, Federica , DI FABIO, Romano , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D403/12
CPC分类号： C07D495/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/08
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl; or corresponds to a group R 5 ; R 2 is hydrogen or C 1-4 alkyl; R 3 is C 1-4 alkyl; R 4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; R 5 is a moiety selected from the group consisting of: isoxazolyl, -CH 2 -N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; and when R 1 is chlorine and p is 1, such R 1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R 1 corresponds to R 5 , p is 1; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency or as antipsychotic agents.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐，其中G选自：苯基，吡啶基，苯并噻唑基，吲唑基; p为0〜5的整数; R 1独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基; 或对应于R5组; R2是氢或C1-4烷基; R3是C1-4烷基; R 4是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被1,2,3或4个取代基取代选自：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基; R5是选自以下的部分：异恶唑基，-CH 2 -N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基，2-吡咯烷酮基，任选地被一个或多个选自以下的两个取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基; 当R1为氯且p为1时，该R1不存在于与分子的其余部分的连接键的邻位; 当R1对应于R5时，p为1; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体的调节剂。治疗药物依赖或作为抗精神病药。

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