-
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。
-
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.
-
公开(公告)号:US20050203079A1
公开(公告)日:2005-09-15
申请号:US10511769
申请日:2003-04-17
申请人: Federica Damiani , Dieter Hamprecht , Albert Jaxa-Chamiec , Fabrizio Micheli , Alessandro Pasquarello , Giovanna Tedesco
发明人: Federica Damiani , Dieter Hamprecht , Albert Jaxa-Chamiec , Fabrizio Micheli , Alessandro Pasquarello , Giovanna Tedesco
IPC分类号: A61K31/4015 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61P1/00 , A61P9/08 , A61P15/12 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/36 , A61P43/00 , C07D207/26 , C07D207/27 , C07D207/273 , C07D207/38 , C07D211/76 , C07D211/88 , C07D401/12 , A61K31/55 , A61K31/4025 , A61K31/4439 , C07D43/02
CPC分类号: C07D207/26 , C07D207/273 , C07D207/38 , C07D211/76 , C07D211/88 , C07D401/12
摘要: Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: wherein R1 is hydrogen, hydroxy, fluoro, chloro, 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 an optionally substituted C-linked 4 to 7 membered heterocyclic group containing at least one nitrogen, an optionally substituted N-linked 4 to 7 membered heterocyclic group, or Z is —NR11R12 where R11 and R12 are independently hydrogen or C1-6alkyl. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression and anxiety, are also disclosed.
-
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。
-
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
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
-
-
-
-