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1. 发明授权

US07202221B2 Macrolides 失效
标题翻译：大环内酯类
公开(公告)号：US07202221B2
公开(公告)日：2007-04-10
申请号：US10495413
申请日：2002-11-13
申请人： Suleman Alihodzic , Daniele Andreotti , Andrea Berdik , Ilaria Bientinesi , Stefano Biondi , Manuela Ciraco , Federica Damiani , Marko Djerek , Miljenko Dumic , Vesna Erakovic , Antun Hutinec , Gorjana Lazarevski , Sergio Lociuro , Natasa Marsic , Zorica Marusic-Istuk , Stjepan Mutak , Alfredo Paio , Drazen Pavlovic , Anna Quaglia , Wolfgang Schoenfeld , Vlado Stimac , Jessica Tibasco
发明人： Suleman Alihodzic , Daniele Andreotti , Andrea Berdik , Ilaria Bientinesi , Stefano Biondi , Manuela Ciraco , Federica Damiani , Marko Djerek , Miljenko Dumic , Vesna Erakovic , Antun Hutinec , Gorjana Lazarevski , Sergio Lociuro , Natasa Marsic , Zorica Marusic-Istuk , Stjepan Mutak , Alfredo Paio , Drazen Pavlovic , Anna Quaglia , Wolfgang Schoenfeld , Vlado Stimac , Jessica Tibasco
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to 14 or 15 membered macrolides substituted at the 4′ position of formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body
摘要翻译：本发明涉及在式（I）的4'位取代的14或15元大环内酯及其药学上可接受的盐和溶剂化物，其制备方法及其在治疗或预防人体全身或局部细菌感染中的用途或动物体

2. 发明申请

US20050080025A1 Macrolides 失效
标题翻译：大环内酯类
公开(公告)号：US20050080025A1
公开(公告)日：2005-04-14
申请号：US10495413
申请日：2002-11-13
申请人： Suleman Alihodzic , Daniele Andretoh , Andrea Berdik , Ilaria Bientinesi , Stefano Biondi , Manuela Ciraco , Federica Damiani , Marko Djerek , Miljenko Dumic , Vesna Erakovic , Antun Hutinec , Gorjana Lazarevski , Sergio Lociuro , Natasa Marsic , Zorica Marusic-Istuk , Stjepan Mutak , Alfred Paio , Drazen Pavlovic , Anna Quaglia , Wolfgang Schoenfeld , Vlado Stimac , Jessica Tibasco
发明人： Suleman Alihodzic , Daniele Andretoh , Andrea Berdik , Ilaria Bientinesi , Stefano Biondi , Manuela Ciraco , Federica Damiani , Marko Djerek , Miljenko Dumic , Vesna Erakovic , Antun Hutinec , Gorjana Lazarevski , Sergio Lociuro , Natasa Marsic , Zorica Marusic-Istuk , Stjepan Mutak , Alfred Paio , Drazen Pavlovic , Anna Quaglia , Wolfgang Schoenfeld , Vlado Stimac , Jessica Tibasco
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08 , A61K31/7052
CPC分类号： C07H17/08
摘要： The present invention relates to 14 or 15 membered macrolides substituted at the 4th position of formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
摘要翻译：本发明涉及在式（I）的第4位取代的14或15元大环内酯类及其药学上可接受的盐和溶剂化物，其制备方法及其在治疗或预防全身或局部细菌感染中的用途一个人或动物的身体。

3. 发明申请

US20050215495A1 Macrolide antibiotics 审中-公开
标题翻译：大环内酯抗生素
公开(公告)号：US20050215495A1
公开(公告)日：2005-09-29
申请号：US11127701
申请日：2005-05-12
申请人： Sulejman Alihodzic , Daniele Andreotti , Luca Arista , Stefano Biondi , Francesca Cardullo , Manuela Ciraco , Federica Damiani , Sergio Lociuro , Carla Marchioro , Giancarlo Merlo , Anna Mingardi , Daniela Niccolai , Alfredo Paio , Elisabetta Piga , Alfonso Pozzan , Catia Seri , Luca Tarsi , Silvia Terreni , Jessica Tibasco
发明人： Sulejman Alihodzic , Daniele Andreotti , Luca Arista , Stefano Biondi , Francesca Cardullo , Manuela Ciraco , Federica Damiani , Sergio Lociuro , Carla Marchioro , Giancarlo Merlo , Anna Mingardi , Daniela Niccolai , Alfredo Paio , Elisabetta Piga , Alfonso Pozzan , Catia Seri , Luca Tarsi , Silvia Terreni , Jessica Tibasco
IPC分类号： A61K31/7048 , A61P31/10 , C07H17/08 , A61K31/7052
CPC分类号： C07H17/08 , A61K9/0019 , A61K9/2018 , Y02P20/55
摘要： The present invention relates to 11,12 γ lactone ketolides of formula (I) wherein R, R1, R2, R3 are as defined herein and pharmaceutically acceptable salts and solvates thereof, to process for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
摘要翻译：本发明涉及式（I）的11,12个γ-内酯酮内酯，其中R 1，R 1，R 2，R 3，3，本文定义其药学上可接受的盐和溶剂化物，以处理其制备及其在治疗或预防人或动物体内的全身或局部细菌感染中的用途。

4. 发明申请

US20060211636A1 Macrolide Antibiotics 审中-公开
标题翻译：大环内酯抗生素
公开(公告)号：US20060211636A1
公开(公告)日：2006-09-21
申请号：US11422122
申请日：2006-06-05
申请人： Sulejman ALIHODZIC , Daniele Andreotti , Luca Arista , Stefano Biondi , Francesca Cardullo , Manuela Ciraco , Federica Damiani , Sergio Lociuro , Carla Marchioro , Giancarlo Merlo , Anna Mingardi , Daniela Niccolai , Alfredo Paio , Elisabetta Piga , Alfonso Pozzman , Catai Seri , Luca Tarsi , Silvia Terreni , Jessica Tibasco
发明人： Sulejman ALIHODZIC , Daniele Andreotti , Luca Arista , Stefano Biondi , Francesca Cardullo , Manuela Ciraco , Federica Damiani , Sergio Lociuro , Carla Marchioro , Giancarlo Merlo , Anna Mingardi , Daniela Niccolai , Alfredo Paio , Elisabetta Piga , Alfonso Pozzman , Catai Seri , Luca Tarsi , Silvia Terreni , Jessica Tibasco
IPC分类号： C07H17/08 , A61K31/7048
CPC分类号： C07H17/08 , A61K9/0019 , A61K9/2018 , Y02P20/55
摘要： The present invention relates to 11,12 γ lactone ketolides of formula (I) wherein R, R1, R2, R3 are as defined herein and pharmaceutically acceptable salts and solvates thereof, to process for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
摘要翻译：本发明涉及式（I）的11,12个γ-内酯酮内酯，其中R 1，R 1，R 2，R 3，3，本文定义其药学上可接受的盐和溶剂化物，以处理其制备及其在治疗或预防人或动物体内的全身或局部细菌感染中的用途。

5. 发明申请

US20080139532A1 Tetrahydrobenzazepine Derivatives as Modulators of Dopamine D3 Receptors (Antipsychotic Agents) 审中-公开
标题翻译：四氢苯并吖庚因衍生物作为多巴胺D3受体的调节剂（抗精神病药）
公开(公告)号：US20080139532A1
公开(公告)日：2008-06-12
申请号：US10591782
申请日：2005-03-04
申请人： Luca Arista , Giorgio Bonanomi , Federica Damiani , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco
发明人： Luca Arista , Giorgio Bonanomi , Federica Damiani , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco
IPC分类号： C07D403/12 , A61K31/55 , A61P25/30
CPC分类号： C07D403/14 , C07D401/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, 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. as agents to treat various aspects 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，其制备方法，用于这些方法的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D 3的调节剂， / SUB>受体，例如作为治疗各方面药物依赖的药剂或作为抗精神病药。

6. 发明授权

US08263782B2 Azabicyclo (3.1.0) hexane derivatives useful as modulators of dopamine D3 receptors 有权
公开(公告)号：US08263782B2
公开(公告)日：2012-09-11
申请号：US12639129
申请日：2009-12-16
申请人： Luca Arista , Giorgio Bonanomi , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
发明人： Luca Arista , Giorgio Bonanomi , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： C07D215/38
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; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; 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, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, 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 D3 receptors, e.g. to treat drug dependency or as antipsychotic agents.

7. 发明申请

US20100152195A1 Azabicyclo (3.1.0) Hexane Derivatives Useful As Modulators Of Dopamine D3 Receptors 有权
公开(公告)号：US20100152195A1
公开(公告)日：2010-06-17
申请号：US12639129
申请日：2009-12-16
申请人： Luca Arista , Giorgio Bonanomi , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
发明人： Luca Arista , Giorgio Bonanomi , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61K31/501 , C07D403/12 , C07D417/14 , A61K31/428 , A61K31/4196 , A61K31/4439 , C07D401/14 , A61K31/4965
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; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; 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, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, 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 D3 receptors, e.g. to treat drug dependency or as antipsychotic agents.

8. 发明申请

US20070142438A1 Azabicyclo (3.1.0.) hexane derivatives useful as modulators of dopamine d3 receptors 有权
公开(公告)号：US20070142438A1
公开(公告)日：2007-06-21
申请号：US10598200
申请日：2005-02-21
申请人： Luca Arista , Giorgio Bonanomi , Anna Capelli , Federica Damiani , Romano Di Fabio , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
发明人： Luca Arista , Giorgio Bonanomi , Anna Capelli , Federica Damiani , Romano Di Fabio , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61K31/4439 , A61K31/4196 , A61K31/428 , C07D417/14 , C07D403/14
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: 1. wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, halo1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; 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, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—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, C1-4alkyl, halo1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; or a salt thereof which are useful as modulators of dopamine D3 receptors, e.g. to treat drug dependency or as antipsychotic agents.

9. 发明授权

US07989444B2 Compounds having affinity for dopamine D3 receptor and uses thereof 失效
标题翻译：对多巴胺D3受体具有亲和性的化合物及其用途
公开(公告)号：US07989444B2
公开(公告)日：2011-08-02
申请号：US11569880
申请日：2005-05-31
申请人： Giorgio Bonanomi , Federica Damiani , Gabriella Gentile , Dieter Wolfgang Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
发明人： Giorgio Bonanomi , Federica Damiani , Gabriella Gentile , Dieter Wolfgang Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61P25/18 , A61K31/55 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D513/04 , C07D487/04
摘要： Compounds of formula (I) wherein A is a 5 or 6 membered heteroaromatic ring or a 5 or 6 membered heterocyclic ring, and which are useful for treating mental disorders such as schizophrenia are set out herein.
摘要翻译：本文列出了其中A为5或6元杂芳环或5或6元杂环，可用于治疗精神障碍如精神分裂症的式（I）化合物。

10. 发明授权

US07855298B2 Azabicyclo (3.1.0.) hexane derivatives useful as modulators of dopamine D3 receptors 有权
标题翻译：可用作多巴胺D3受体调节剂的氮杂双环（3.1.0。）己烷衍生物
公开(公告)号：US07855298B2
公开(公告)日：2010-12-21
申请号：US10598200
申请日：2005-02-21
申请人： Luca Arista , Giorgio Bonanomi , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
发明人： Luca Arista , Giorgio Bonanomi , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： C07D215/38
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: 1. wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; 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, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; or a salt thereof which are useful as modulators of dopamine D3 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：1.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; 或其盐，其可用作多巴胺D3受体的调节剂，例如，治疗药物依赖或作为抗精神病药。

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