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1. 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。

2. 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）。

3. 发明申请

WO2004094420A1 CONDENSED N-HETEROCYCLIC COMPOUNDS AND THEIR USE AS CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译：简便的N-杂环化合物及其作为CRF受体拮抗剂的用途
公开(公告)号：WO2004094420A1
公开(公告)日：2004-11-04
申请号：PCT/IB2004/001350
申请日：2004-04-07
申请人： SB PHARMCO PUERTO RICO INC , NEUROCRINE BIOSCIENCES INC , ANDREOTTI, Daniele , BERNASCONI, Giovanni , CASTIGLIONI, Emiliano , CONTINI, Stefania , DI FABIO, Romano , FAZZOLARI, Elettra , FERIANI, Aldo , GENTILE, Gabriella , MATTIOLI, Mario , MINGARDI, Anna , SABBATINI, Fabio , ST-DENIS, Yves
发明人： ANDREOTTI, Daniele , BERNASCONI, Giovanni , CASTIGLIONI, Emiliano , CONTINI, Stefania , DI FABIO, Romano , FAZZOLARI, Elettra , FERIANI, Aldo , GENTILE, Gabriella , MATTIOLI, Mario , MINGARDI, Anna , SABBATINI, Fabio , ST-DENIS, Yves
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof (Formula (I)) wherein the dashed line may represent a double bond; R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 lkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -C(O)R 2 , nitro, hydroxy, -NR 3 R 4 , cyano and or a group Z; R 1 is hydrogen, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo Cl-C6 alkoxy, halogen, NR 3 R 4 or cyano; D, G is . -C- optionally substituted; X is carbon or nitrogen; Y is nitrogen or -C- optionally substituted; W is a 4-8 membered ring, which may be saturated or may contain one to three double bonds, and in which: - one carbon atom is replaced by a carbonyl or S(O) m ; and - one to four carbon atoms may optionally be replaced by oxygen, nitrogen or NR 12 , S(O) m , carbonyl, and such ring may be further substituted by 1 to 8 substituents; Z is a 5-6 membered heterocycle, which may be substituted by 1 to 8 R 5 groups or a phenyl ring, which may be substituted by 1 to 4 substituents; m is an integer from 0 to 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：本发明提供了包括立体异构体，前体药物和药学上可接受的盐或溶剂合物（式（I））的式（I）化合物，其中虚线可以表示双键; 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，卤素 C 1 -C 6烷氧基，-C（O）R 2，硝基，羟基，-NR 3 R 4，氰基和/或Z; R 1是氢，C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6硫代烷基，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; D，G为-C-任选取代的; X是碳或氮; Y是氮或-C-任选取代的; W是4-8元环，其可以是饱和的或可以含有一至三个双键，其中： - 一个碳原子被羰基或S（O）m取代; 和 - 1-4个碳原子可以任选被氧，氮或NR 12，S（O）m，羰基取代，并且这样的环可进一步被1至8个取代基取代; Z是5-6元杂环，其可以被1至8个R5基团取代或可被1至4个取代基取代的苯基环; m为0至2的整数。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。

4. 发明申请

WO2002094826A1 TRI-AND TETRAAZA-ACENAPHTHYLEN DERIVATIVES AS CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为CRF受体拮抗剂的三硝基苯并噻吩衍生物
公开(公告)号：WO2002094826A1
公开(公告)日：2002-11-28
申请号：PCT/GB2002/002377
申请日：2002-05-21
申请人： NEUROCRINE INC. , SB PHARMCO PUERTO RICO INC. , DI FABIO, Romano , GENTILE, Gabriella , HADDACH, Mustapha , ST-DENIS, Yves , WILLIAMS, John, Patrick
发明人： DI FABIO, Romano , GENTILE, Gabriella , HADDACH, Mustapha , ST-DENIS, Yves , WILLIAMS, John, Patrick
IPC分类号： C07D471/16
CPC分类号： C07D471/16
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure of formula (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, R1, R2, R4, R5, R6, A, X, and Y are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
摘要翻译：公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。本发明的CRF受体拮抗剂具有以下结构式（I）：其包括立体异构体，其前药和药学上可接受的盐，R 1，R 2，R 4，R 5，R 6，A，X和Y如本文所定义。还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

5. 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。

6. 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）。

7. 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。

8. 发明授权

EP1583531B1 HETEROARYL-SUBSTITUTED PYRROLO[2, 3- B]PYRIDINE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS 有权
标题翻译：杂芳基取代吡咯并[2,3-b]吡啶衍生物作为CRF受体拮抗剂
公开(公告)号：EP1583531B1
公开(公告)日：2007-04-18
申请号：EP04701955.9
申请日：2004-01-14
申请人： SB Pharmco Puerto Rico Inc , NEUROCRINE BIOSCIENCES, INC.
发明人： CASTIGLIONI, Emiliano , DI FABIO, Romano , FERIANI, Aldo , MICHELI, Fabrizio , SABBATINI, Fabio , ST-DENIS, Yves
IPC分类号： A61K31/437 , A61P1/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P29/00 , C07D471/04
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).

9. 发明公开

EP1583531A1 HETEROARYL- SUBSTITUTED PYRROLO' 2, 3- B! PYRIDINE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS 有权
标题翻译：杂芳基取代吡咯并[2,3-b]吡啶衍生物作为CRF受体拮抗剂
公开(公告)号：EP1583531A1
公开(公告)日：2005-10-12
申请号：EP04701955.9
申请日：2004-01-14
申请人： SB Pharmco Puerto Rico Inc , NEUROCRINE BIOSCIENCES, INC.
发明人： CASTIGLIONI, Emiliano , DI FABIO, Romano , FERIANI, Aldo , MICHELI, Fabrizio , SABBATINI, Fabio , ST-DENIS, Yves
IPC分类号： A61K31/437 , A61P1/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P29/00 , C07D471/04
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).

10. 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。

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