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21. 发明授权

US07462622B2 Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists 失效
标题翻译：吡咯并[2,3-d]嘧啶衍生物作为促肾上腺皮质激素释放因子拮抗剂
公开(公告)号：US07462622B2
公开(公告)日：2008-12-09
申请号：US10480958
申请日：2002-06-11
申请人： Romano Di Fabio , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Bendetta Perini , Yves St-Denis
发明人： Romano Di Fabio , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Bendetta Perini , Yves St-Denis
IPC分类号： A61K31/519 , C07D487/04 , A61P25/24 , A61P25/22
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, —COR4, nitro, —NR3R4 cyano, or a group R5; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; R2 corresponds to a group CHR6R7; R3 is hydrogen, C1-C6 alkyl; R4 independently from R3, has the same meanings; R5 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 R5 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; R6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R7 independently from R6, 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，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，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; 其中每个上述基团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以下的基团取代：C 1 -C 6烷氧基和羟基; 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。

22. 发明授权

US07279474B2 Substituted pyrrolo[2,3-d]pyrimidines as antagonists of the corticotropin releasing factor (CRF) 失效
标题翻译：取代的吡咯并[2,3-d]嘧啶作为促肾上腺皮质激素释放因子（CRF）的拮抗剂
公开(公告)号：US07279474B2
公开(公告)日：2007-10-09
申请号：US10476368
申请日：2002-04-30
申请人： Anna Maria Capelli , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Benedetta Perini , Yves St-Denis , Romano Di Fabio
发明人： Anna Maria Capelli , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Benedetta Perini , Yves St-Denis , Romano Di Fabio
IPC分类号： A61K31/5355 , A61K31/519 , C07D487/04 , C07D413/14 , A61P25/24 , A61P25/22
CPC分类号： C07D487/04 , A61K51/0459 , A61K51/0463 , A61K51/0465 , 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 the variables are as defined in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF)
摘要翻译：本发明提供了式（I）化合物，其包括立体异构体，前药和药学上可接受的盐或溶剂合物，其中变量如本说明书所定义，其制备方法，含有它们的药物组合物及其在治疗由促肾上腺皮质激素释放因子（CRF）

23. 发明授权

US07273871B2 Phenyl-5,6,6A,7,8,9-hexahydro-4H-1,4,9-triaza-phenalene derivatives as CRF antagonists 失效
标题翻译：作为CRF拮抗剂的苯基-5,6,6A，7,8,9-六氢-4H-1,4,9-三氮杂 - 非那烯衍生物
公开(公告)号：US07273871B2
公开(公告)日：2007-09-25
申请号：US10483872
申请日：2002-07-15
申请人： Romano Di Fabio , Collin F Regan , Yves St-Denis , Fabrizio Micheli , Michael K Schwaebe
发明人： Romano Di Fabio , Collin F Regan , Yves St-Denis , Fabrizio Micheli , Michael K Schwaebe
IPC分类号： A61K31/505 , C07D471/04 , C07D239/00
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:
摘要翻译：本发明涉及式（I）的三环吡啶化合物，其包括立体异构体，其前药和药学上可接受的盐或溶剂合物：

24. 发明申请

US20070219232A1 Chemical Compounds 审中-公开
公开(公告)号：US20070219232A1
公开(公告)日：2007-09-20
申请号：US11749433
申请日：2007-05-16
申请人： Romano Di Fabio , Fabrizio Micheli , Yves St-Denis
发明人： Romano Di Fabio , Fabrizio Micheli , Yves St-Denis
IPC分类号： A61K31/44 , C07D211/00 , 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)R5, nitro, —NR6R7, cyano, and a group R8; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR6R7 or cyano; R2 is hydrogen, C3-C7 cycloalkyl, or a group R9; R3 is C3-C7 cycloalkyl, or a group R9; or R2 and R3 together with N form a 5-14 membered heterocycle, which may be substituted by 1 to 3 R10 groups; R4 is hydrogen, C1-C6 alkyl, halogen or halo C1-C6 alkyl; R5 is a C1-C4 alkyl, —OR6 or —NR6R7; R6 is hydrogen or C1-C6 alkyl; R7 is hydrogen or C1-C6 alkyl; R8 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 R11 groups; R9 is a C1-C6 alkyl that may be substituted by one or more groups selected from: C3-C7 cycloalkyl, C1-C6 alkoxy, haloC1-C6 alkoxy, hydroxy, haloC1-C6 alkyl; R10 is a group R8, 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)NR6R7, phenyl which may be substituted by 1 to 4 R11 groups; R11 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)NR6R7; 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).

25. 发明授权

US5977136A Tetrahydroquinolines as NMDA antagonists 失效
标题翻译：四氢喹啉作为NMDA拮抗剂
公开(公告)号：US5977136A
公开(公告)日：1999-11-02
申请号：US29860
申请日：1998-03-17
申请人： Romano Di Fabio , Simone Giacobbe , Barbara Bertani , Fabrizio Micheli
发明人： Romano Di Fabio , Simone Giacobbe , Barbara Bertani , Fabrizio Micheli
IPC分类号： A61K20060101 , A61K31/47 , A61K31/4709 , C07D20060101 , C07D215/48
CPC分类号： C07D215/48
摘要： Compounds of formula (I) or a salt, or metabolically labile ester thereof, processes for the preparation thereof and their use as antagonists of excitatory amino acids. ##STR1##
摘要翻译： PCT No.PCT / EP96 / 04206 Sec。 371日期：1998年3月17日 102（e）1998年3月17日PCT 1996年9月26日PCT公布。公开号WO97 / 12870 日期1997年4月10日式（I）化合物或其盐或其代谢不稳定酯的方法用于制备它们及其作为兴奋性氨基酸拮抗剂的用途。

26. 发明申请

US20050054661A1 Corticotropin releasing factor antagonists 失效
标题翻译：促肾上腺皮质激素释放因子拮抗剂
公开(公告)号：US20050054661A1
公开(公告)日：2005-03-10
申请号：US10480958
申请日：2002-06-11
申请人： Romano Di Fabio , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Yves St-Denis
发明人： Romano Di Fabio , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Yves St-Denis
IPC分类号： A61K31/519 , A61K51/00 , A61K51/04 , A61P1/04 , A61P25/00 , A61P25/22 , A61P25/24 , A61P43/00 , C07D239/70 , C07D239/94 , C07D471/04 , C07D487/04 , C07D487/02
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, —COR4, nitro, —NR3R4 cyano, or a group R5; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; R2 corresponds to a group CHR6R7; R3 is hydrogen, C1-C6 alkyl; R4 independently from R3, has the same meanings; R5 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 R5 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; R6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R7 independently from R6, 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，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，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; 其中每个上述基团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以下的基团取代：C 1 -C 6烷氧基和羟基; 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。

27. 发明申请

US20120040991A1 3-AZABICYCLO [4.1.0] HEPTANES USED AS OREXIN ANTAGONISTS 审中-公开
标题翻译： 3-AZABICYCLO [4.1.0]用作OREXIN拮抗剂的HEPTANES
公开(公告)号：US20120040991A1
公开(公告)日：2012-02-16
申请号：US13265915
申请日：2010-04-23
申请人： David Amantini , Romano Di Fabio , Massimo Gianotti , Francesca Pavone , Francesco Ferroni
发明人： David Amantini , Romano Di Fabio , Massimo Gianotti , Francesca Pavone , Francesco Ferroni
IPC分类号： A61K31/444 , A61K31/506 , C07D413/14 , A61K31/497 , A61P25/24 , A61P25/00 , A61P9/00 , A61P11/00 , A61P25/22 , C07D401/14 , A61K31/501
CPC分类号： C07D401/12 , C07D403/14 , C07D413/14 , C07D417/14
摘要： Disclosed are 3-azabicyclo[4.1.0]heptane derivatives of formula (I) and their use as orexin receptor antagonists.
摘要翻译：公开了式（I）的3-氮杂双环[4.1.0]庚烷衍生物及其作为食欲素受体拮抗剂的用途。

28. 发明授权

US07446108B2 Tri-and tetraaza-acenaphthylen derivatives as CRF receptor antagonists 失效
标题翻译：三 - 和四氮杂苊烯衍生物作为CRF受体拮抗剂
公开(公告)号：US07446108B2
公开(公告)日：2008-11-04
申请号：US10477886
申请日：2002-05-21
申请人： Romano Di Fabio , Gabriella Gentile , Yves St Denis
发明人： Romano Di Fabio , Gabriella Gentile , Yves St Denis
IPC分类号： A01N43/54 , C07D239/00
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: 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：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。

29. 发明申请

US20080262041A1 Beta-Lactams for Treatment of Cns Disorders 审中-公开
标题翻译：用于治疗Cns病的β-内酰胺类
公开(公告)号：US20080262041A1
公开(公告)日：2008-10-23
申请号：US10595662
申请日：2004-11-10
申请人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Alfredo Paio , Maria Elvira Tranquillini , Lucia Mattioli
发明人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Alfredo Paio , Maria Elvira Tranquillini , Lucia Mattioli
IPC分类号： A61K31/4439 , A61K31/4025 , C07D401/04 , A61P25/18 , A61P25/24 , A61P19/02 , C07D403/04
CPC分类号： C07D401/04
摘要： The present invention relates to novel compounds of formula (I): wherein — represents a single or a double bond; R is a radical selected from: in which R1 is halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy and p is zero or an integer from 1 to 3; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen, hydroxy or C1-4 alkyl; R4 is hydrogen or R4 together with R3 represents ═O or ═CH2; R5 is phenyl, naphthyl, a 9 to 10 membered fused bicyclic heterocyclic group or a 5 or 6 membered heteroaryl group, wherein said groups are optionally substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, hydroxy, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or S(O)qC1-4 alkyl; R6 and R7 independently are hydrogen, cyano, C1-4 alkyl; R8 is (CH2)rR10; R9 is hydrogen, halogen, C3-7 cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by one or two groups selected from halogen, cyano, hydroxy or C1-4 alkoxy; R10 is hydrogen or C3-7 cycloalkyl; n is 1 or 2; q is 0, 1 or 2; r is 0 or an integer from 1 to 4; or a pharmaceutically acceptable salt or a solvate thereof, process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of the serotonin reuptake transporter protein
摘要翻译：本发明涉及新的式（I）化合物：其中 - 表示单键或双键; R是选自以下的基团：其中R 1是卤素，氰基，C 1-4烷基，C 1-4烷氧基，三氟甲基或三氟甲氧基，p为0或1至3的整数; R 2是氢或C 1-4烷基; R 3是氢，羟基或C 1-4烷基; R 4是氢或R 4与R 3一起代表-O或-CH 2; R 5是苯基，萘基，9至10元稠合双环杂环基或5或6元杂芳基，其中所述基团任选被1至3个独立地选自三氟甲基，烷基，羟基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或S（O）q C 1-4烷基; R 6和R 7独立地是氢，氰基，C 1-4烷基; R 8是（CH 2 2）r R 10; R 9是氢，卤素，C 3-7环烷基，羟基，硝基，氰基或C 1-4烷基，任选被一个或多个两个选自卤素，氰基，羟基或C 1-4烷氧基的基团; R 10是氢或C 3-7环烷基; n为1或2; q是0,1或2; r为0或1至4的整数; 或其药学上可接受的盐或溶剂合物，其制备方法及其用于治疗由粘蛋白介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白

30. 发明授权

US07345041B2 Chemical compounds 有权
标题翻译：化合物
公开(公告)号：US07345041B2
公开(公告)日：2008-03-18
申请号：US11334267
申请日：2006-01-18
申请人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Giuseppe Guercio , Yves St-Denis , Antonella Ursini
发明人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Giuseppe Guercio , Yves St-Denis , Antonella Ursini
IPC分类号： A61K31/495 , A61K31/50
CPC分类号： C07D401/06 , A61K31/135 , A61K31/196 , A61K31/495 , A61K31/496 , C07D241/04 , C07D403/06 , A61K2300/00
摘要： The invention relates to methods for the treatment of a sleep disorder comprising administering a compound of formula (I): wherein all variables are as defined herein.
摘要翻译：本发明涉及治疗睡眠障碍的方法，包括给予式（I）化合物：其中所有变量如本文所定义。

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