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31. 发明申请

US20090221618A1 AZABICYCLO (3, 1, 0) HEXAN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 失效
标题翻译： AZ Y Y O 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
公开(公告)号：US20090221618A1
公开(公告)日：2009-09-03
申请号：US12064123
申请日：2006-08-18
申请人： Luca Arista , Anna Checchia , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli
发明人： Luca Arista , Anna Checchia , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli
IPC分类号： A61K31/506 , C07D403/06
CPC分类号： C07D403/06 , C07D403/12
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is ; and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中：p为0,1,2,3,4或5; 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烷酰基和SF 5; n为3或4; R2是氢或C1-4烷基; n为2或3; X是-CH 2 - ， - O-或-S-; Z可以是-CH-或N; A是P或P1组，其中P和P1是; 并且Y是氢，-OH，C 1-4烷基，卤代C 1-4烷基，苯基或杂芳基，其中苯基和杂芳基任选被一个或两个选自C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基和卤代C 1-4烷氧基; 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。治疗物质相关疾病，作为抗精神病药物早泄或认知障碍。

32. 发明授权

US07253284B2 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US07253284B2
公开(公告)日：2007-08-07
申请号：US10483792
申请日：2002-07-15
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： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： Compounds of the formula I, Wherein X is N, n is 1 and R2and R3 together form a ring, R, R1 and R4 are as defined in the specifications.
摘要翻译：式I化合物，其中X为N，n为1，R 2和R 3一起形成环，R，R 1和R 4如说明书中所定义。

33. 发明申请

US20070066640A1 Heteroaryl-substituted pyrrolo'2,3-b1 pyridine derivatives as crf receptor antagonists 审中-公开
标题翻译：杂芳基取代的吡咯并[2,3-b]吡啶衍生物作为受体拮抗剂
公开(公告)号：US20070066640A1
公开(公告)日：2007-03-22
申请号：US10542196
申请日：2004-01-14
申请人： Emiliano Castiglioni , Romano Di Fabio , Aldo Feriani , Fabrizio Micheli , Fabio Sabbatini , Yves St-Denis
发明人： Emiliano Castiglioni , Romano Di Fabio , Aldo Feriani , Fabrizio Micheli , Fabio Sabbatini , Yves St-Denis
IPC分类号： A61K31/4745 , C07D471/02
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）。

34. 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：

35. 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).

36. 发明申请

US20060205788A1 Compounds having activity at 5ht2c receptor and uses thereof 审中-公开
公开(公告)号：US20060205788A1
公开(公告)日：2006-09-14
申请号：US10548118
申请日：2004-02-24
申请人： Federica Damiani , Dieter Hamprecht , Fabrizio Micheli , Alessandra Pasquarello , Giovanna Tedesco
发明人： Federica Damiani , Dieter Hamprecht , Fabrizio Micheli , Alessandra Pasquarello , Giovanna Tedesco
IPC分类号： A61K31/454 , C07D403/02
CPC分类号： C07D207/26 , C07D207/273 , C07D207/38
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 is hydrogen, fluoro, chloro, hydroxy, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy or haloC1-6alkoxy; m is 0 when ═ is a double bond and m is 1 when ═ is a single bond; R2 is hydrogen, halogen, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is —(CH2—CH2)—, —(CH═CH)—, —(CH2)3—, —C(CH3)2—, —(CH═CH—CH2)—, —(CH2-CH═CH)— or a group —(CHR5)— wherein R5 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1-6alkylthio; R3 is halogen, cyano, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy, C1-6alkylthio, hydroxy, amino, mono- or di-C1-6alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC1-6alkyl, haloC1-6alkoxy, aryl, arylC1-6alkyl, arylC1-6alkyloxy, arylC1-6alkylthio or COOR6, CONR7R8 or COR9 wherein R6, R7, R8 and R9 are independently hydrogen or C1-6alkyl; p is 0, 1 or 2 or 3; R4 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C1-6alkanoyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; Y is oxygen, sulfur, —CH2— or NR10 wherein R10 is hydrogen or C1-6alkyl; D is a single bond, —CH2—, —(CH2)2— or —CH═CH—; and Z is —NR11R12 where R11 and R12 are independently hydrogen or C1-6alkyl, or an optionally substituted N-linked or C-linked 4 to 7 membered heterocyclic group. Method of preparation and uses of the compounds in therapy, for example depression and anxiety, are also disclosed.

37. 发明授权

US07863299B2 Triazolyl derivatives of azabicyclo [3.1.0] hexane as dopamine D3 receptor modulators 失效
标题翻译：氮杂双环[3.1.0]己烷的三唑基衍生物作为多巴胺D3受体调节剂
公开(公告)号：US07863299B2
公开(公告)日：2011-01-04
申请号：US12064118
申请日：2006-08-18
申请人： Anna Maria Capelli , Elettra Fazzolari , Fabrizio Micheli , Giovanna Tedesco , Silvia Terreni
发明人： Anna Maria Capelli , Elettra Fazzolari , Fabrizio Micheli , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61K31/428 , A61K31/4196 , A61K31/4439 , C07D403/14 , C07D417/14
CPC分类号： C07D413/14
摘要： The present invention relates to novel compounds of formula (IC) or a salt thereof: wherein: p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; m1, m2, m3, and m4 are 0; m5, m6 and m7 are each independently 0, 1 or 2 wherein the sum of m5, m6 and m7 is 1 or 2; R6 is C1-6alkyl; R7 is halogen, C1-6alkyl or haloC1-6alkyl; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; R3 is C1-4alkyl; R4 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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl, wherein each group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; with the proviso that when m5=m6=1, R7 is not chlorine; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents, premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新型式（IC）化合物或其盐：其中：p为0至4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SF 5; 或对应于R5组; m1，m2，m3，m4为0; m5，m6和m7各自独立地为0,1或2，其中m5，m6和m7的和为1或2; R6是C1-6烷基; R7是卤素，C1-6烷基或卤代C 1-6烷基; R2是氢或C1-4烷基; n为2或3; X是S或-CH 2 - ; 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烷氧基和C 1-4烷酰基; R5是异恶唑基，-CH2-N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基或2-吡咯烷基，其中每个基团任选被一个或两个选自以下的取代基取代：卤素，氰基，C1 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基和C 1-4烷酰基; 条件是当m5 = m6 = 1时，R7不是氯; 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。治疗与物质相关的疾病，作为抗精神病药，早泄或认知障碍。

38. 发明申请

US20070191457A1 Compounds having activity at 5ht2c receptor and uses thereof 审中-公开
公开(公告)号：US20070191457A1
公开(公告)日：2007-08-16
申请号：US10551904
申请日：2004-04-05
申请人： Giorgio Bonanomi , Dieter Hamprecht , Fabrizio Micheli , Silvia Terreni
发明人： Giorgio Bonanomi , Dieter Hamprecht , Fabrizio Micheli , Silvia Terreni
IPC分类号： A61K31/454 , C07D401/02
CPC分类号： C07D209/46
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 is halogen, cyano, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy, C1-6alkylthio, hydroxy, amino, mono- or di-C1-6alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC1-6alkyl, haloC1-6alkoxy, aryl, —COOR3, —COR4, wherein R3 and R4 are independently hydrogen or C1-6alkyl, or —COR5, wherein R5 is amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; p is 0, 1, 2 or 3; Q is a 6-membered aromatic group or a 6-membered heteroaromatic group; A is —(CH2—CH2)—, —(CH═CH)—, or a group —(CHR7)— wherein R7 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1-6alkylthio; R2 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C1-6alkanoyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is oxygen, sulfur, —CH2— or NR8 wherein R8 is hydrogen or C1-6alkyl; Y is a single bond, —CH2—, —(CH2)2— or —CH═CH—; and Z is an optionally substituted N-linked heterocyclic group or a C-linked 4 to 7 membered heterocyclic group containing at least one nitrogen, or Z is —NR9R10 where R9 and R10 are independently hydrogen or C1-6alkyl. Methods of preparation and uses thereof in therapy, such as for depression or anxiety, are also disclosed.

39. 发明申请

US20080242715A1 Triazolyl Derivatives of Azabicyclo [3.1.0] Hexane as Dopamine D3 Receptor Modulators 失效
公开(公告)号：US20080242715A1
公开(公告)日：2008-10-02
申请号：US12064118
申请日：2006-08-18
申请人： Anna Marie Capelli , Elettra Fazzolari , Fabrizio Micheli , Giovanna Tedesco , Silvia Terreni
发明人： Anna Marie Capelli , Elettra Fazzolari , Fabrizio Micheli , Giovanna Tedesco , Silvia Terreni
IPC分类号： C07D413/14 , A61K31/422 , A61P25/18
CPC分类号： C07D413/14
摘要： The present invention relates to novel compounds of formula (IC) or a salt thereof: wherein: p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; m1, m2, m3, and m4 are 0; m5, m6 and m7 are each independently 0, 1 or 2 wherein the sum of m5, m6 and m7 is 1 or 2; R6 is C1-6alkyl; R7 is halogen, C1-6alkyl or haloC1-6alkyl; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; R3 is C1-4alkyl; R4 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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl, wherein each group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; with the proviso that when m5=m6=1, R7 is not chlorine; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents, premature ejaculation or cognition impairment.

40. 发明申请

US20100029740A1 AZABICYCLIC COMPOUNDS AS SEROTONIN, DOPAMINE AND NOREPINEPHRINE RE-UPTAKE INHIBITORS 审中-公开
标题翻译：作为丝氨酸，多巴胺和诺贝那韦再摄入抑制剂的化学式
公开(公告)号：US20100029740A1
公开(公告)日：2010-02-04
申请号：US12519438
申请日：2007-12-12
申请人： Giorgio Bonanomi , Fabrizio Micheli , Silvia Terreni
发明人： Giorgio Bonanomi , Fabrizio Micheli , Silvia Terreni
IPC分类号： A61K31/403 , C07D209/52 , A61P25/00
CPC分类号： C07D209/52
摘要： Novel compounds of formula (I)′ and pharmaceutically acceptable salts, solvates and prodrugs thereof: wherein A is: K is a mono or bicyclic aryl group; R1 is selected from halogen, C1-4alkyl and C1-4alkoxy (R1 may assume different meanings on the basis of p value); p is an integer from 0 to 5; R2 is a group P: R3 is hydrogen, C1-4alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-3alkyl, haloC1-2alkyl or an optionally substituted phenyl group; X is oxygen, —NR8— or sulphur; n is 0 or 1; R7 is hydrogen or methyl; R8 is hydrogen or C1-4alkyl; R4 is hydrogen or methyl; R5 is hydrogen or C1-4alkyl; and R6 is hydrogen or C1-4alkyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.
摘要翻译：新的式（I）化合物及其药学上可接受的盐，溶剂合物和前药：其中A是：K是单或双环芳基; R1选自卤素，C1-4烷基和C1-4烷氧基（R1可以基于p值取代不同的含义）; p是0至5的整数; R2是基团P：R3是氢，C1-4烷基，C3-6环烷基，C3-6环烷基C1-3烷基，卤代C1-2烷基或任选取代的苯基; X是氧，-NR8-或硫; n为0或1; R7是氢或甲基; R8是氢或C1-4烷基; R4是氢或甲基; R5是氢或C1-4烷基; R6为氢或C1-4烷基; 再摄入抑制剂，作为5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE），再摄取抑制剂，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应用。

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