公开(公告)号：US5138048A

公开(公告)日：1992-08-11

申请号：US578949

申请日：1990-09-07

申请人： Bruno Tamburini ,  Alcide Perboni ,  Tino Rossi ,  Daniele Donati ,  Daniele Andreotti ,  Giovanni Gaviraghi ,  Stefano Biondi ,  Claudio Bismara

发明人： Bruno Tamburini ,  Alcide Perboni ,  Tino Rossi ,  Daniele Donati ,  Daniele Andreotti ,  Giovanni Gaviraghi ,  Stefano Biondi ,  Claudio Bismara

IPC分类号： C07D487/04 ,  A61K31/395 ,  A61K31/397 ,  A61K31/40 ,  A61K31/407 ,  A61P31/04 ,  C07C45/71 ,  C07C49/753 ,  C07D205/08 ,  C07D477/00 ,  C07D487/00 ,  C07F7/18

CPC分类号： C07D477/00 ,  C07C45/71 ,  C07C49/753 ,  C07D205/08 ,  C07F7/186 ,  Y02P20/55

摘要： Compounds of the general formula (I) ##STR1## in which: R.sub.1 represents a hydroxyl protecting group; andR.sub.2 represents a hydrogen or halogen atom, an azido group, a C.sub.1-3 alkyl group, a group (CH.sub.2).sub.m OR.sub.3 wherein m is zero or one and R.sub.3 represents a hydrogen atom or a hydroxyl protecting group, an azidoethoxy group, a protected hydroxyethoxy group or a group XR.sub.4 in which X is an oxygen atom or the group S(O).sub.n in which n is zero, 1 or 2 and R.sub.4 represents a C.sub.1-5 alkyl, C.sub.3-7 cycloalkyl or phenyl group or when X is oxygen or sulphur then R.sub.4 may also represent the group AlkNR.sub.5 R.sub.6 in which Alk represents a C.sub.2-6 straight or branched alkylene chain and R.sub.5 and R.sub.6 independently represent a hydrogen atom or C.sub.1-4 alkyl group or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached form a pyrrolidino or piperidino ring or the group NR.sub.5 R.sub.6 represents a protected amino group, or R.sub.2 represents the group (CH.sub.2).sub.m NR.sub.7 R.sub.8 in which m is zero or 1 and R.sub.7 and R.sub.8 independently represent a hydrogen atom or a C.sub.1-4 alkyl group or NR.sub.7 R.sub.8 represents a protected amino group, or R.sub.2 and the carbon atom to which it is attached represent a keto group or a ketal derivative thereof; and acid addition salts of such compounds containing basic centers.

公开(公告)号：US06531466B2

公开(公告)日：2003-03-11

申请号：US09781292

申请日：2001-02-13

申请人： Tino Rossi ,  Daniele Andreotti ,  Giovanna Tedesco ,  Luca Tarsi ,  Emiliangelo Ratti ,  Aldo Feriani ,  Domenica Antonia Pizzi ,  Giovanni Gaviraghi ,  Stefano Biondi ,  Gabriella Finizia

发明人： Tino Rossi ,  Daniele Andreotti ,  Giovanna Tedesco ,  Luca Tarsi ,  Emiliangelo Ratti ,  Aldo Feriani ,  Domenica Antonia Pizzi ,  Giovanni Gaviraghi ,  Stefano Biondi ,  Gabriella Finizia

IPC分类号： C07D47714

CPC分类号： C07D477/00

摘要： A compound of formula (I), salts and metabolically labile esters thereof, wherein R represents optionally substituted aryl or heteroaryl group; A represents a propylene chain or A is a chain of 3 members one of which is selected from an oxygen or sulphur atom or the group NH or a substituted derivative thereof and the other two members are methylene groups, having antibacterial activity, processes for their preparation and to their use in medicine.

摘要翻译： 式（I）的化合物，其盐和代谢不稳定的酯，其中R表示任选取代的芳基或杂芳基; A表示丙烯链或A是3个成员的链，其中一个选自氧或硫原子，或NH基或其取代衍生物，另外两个成员是具有抗菌活性的亚甲基，其制备方法 并用于医学。

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

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：US06900183B2

公开(公告)日：2005-05-31

申请号：US10450886

申请日：2001-12-20

申请人： Daniele Andreotti ,  Stefano Biondi ,  Sergio Lociuro

发明人： Daniele Andreotti ,  Stefano Biondi ,  Sergio Lociuro

IPC分类号： A01N25/34 ,  A01N43/22 ,  A01N63/02 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  A61K31/70

CPC分类号： C07H17/08 ,  A61K9/0019 ,  A61K9/2018

摘要： 11,12 γ lactone ketolides of the following formula: and pharmaceutically acceptable salts and solvates thereof, wherein R, R1, R2, and R3 are as described herein. The disclosure also relates to processes for the preparation of such compounds, to compositions containing them, and to their use in the therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.

摘要翻译： 具有下式的11,12个γ-内酯酮内酯及其药学上可接受的盐和溶剂合物，其中R 1，R 2，R 2和R 3， SUB>如本文所述。 本公开还涉及制备这些化合物的方法，含有它们的组合物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：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。

公开(公告)号：US5705636A

公开(公告)日：1998-01-06

申请号：US570820

申请日：1995-12-12

申请人： Russell John Thomas ,  Stefano Biondi ,  Tino Rossi ,  Stefania Anna Contini

发明人： Russell John Thomas ,  Stefano Biondi ,  Tino Rossi ,  Stefania Anna Contini

IPC分类号： B01J31/02 ,  B01J31/12 ,  C07B61/00 ,  C07D205/04 ,  C07D205/08

CPC分类号： C07D205/08 ,  Y02P20/55

摘要： Compounds of the formula ##STR1## wherein R.sub.1 represents hydrogen or a nitrogen protecting group, useful as intermediates in the preparation of compounds having antibacterial activity.

摘要翻译： 式（I）的化合物，其中R 1表示氢或氮保护基，可用作制备具有抗菌活性的化合物的中间体。

公开(公告)号：US08367711B2

公开(公告)日：2013-02-05

申请号：US13483213

申请日：2012-05-30

申请人： Amjad Ali ,  Michael Man-Chu Lo ,  Christopher Franklin ,  Iyassu K. Sebhat ,  Nicoletta Almirante ,  Silvia Stefanini ,  Stefano Biondi ,  Ennio Ongini

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Christopher Franklin ,  Iyassu K. Sebhat ,  Nicoletta Almirante ,  Silvia Stefanini ,  Stefano Biondi ,  Ennio Ongini

IPC分类号： A61K31/41 ,  A61K31/405 ,  C07D209/00 ,  C07D257/04

CPC分类号： C07D403/10 ,  C07D235/20 ,  C07D257/04 ,  C07D409/06 ,  C07D493/04

摘要： A compound having the structure wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2) (C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is; Y1 is selected from the group consisting of C(O)—O— and P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.

摘要翻译： 具有其中R为例如Y的结构的化合物选自1）R5，2）-C（R1R2）（C（R3R4））0-1Y1R5和3）-C（R1R2） - O-Y1R5; R 1，R 2，R 3和R 4独立地选自氢和C 1-4烷基; R5是 Y1选自C（O）-O-和P（O）（OR 6）-O-; R6为氢或CH3，或其药学上可接受的盐，以及使用该化合物治疗高血压的方法。

公开(公告)号：US08252825B2

公开(公告)日：2012-08-28

申请号：US12743402

申请日：2008-11-21

申请人： Amjad Ali ,  Michael Man-Chu Lo ,  Christopher Franklin ,  Nicoletta Almirante ,  Silvia Stefanini ,  Laura Storoni ,  Stefano Biondi ,  Ennio Ongini

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Christopher Franklin ,  Nicoletta Almirante ,  Silvia Stefanini ,  Laura Storoni ,  Stefano Biondi ,  Ennio Ongini

IPC分类号： A61K31/4184 ,  A61K31/4178 ,  C07D403/10 ,  A61P9/12

CPC分类号： C07D403/10

摘要： A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is 1) —(CH2)3R5, 2) —C(O)(CH2)2R5, 3) —C(R1R2)OC(O)O(CH2)nR5, wherein n is 1 or 2, 4) —C(R1R2)OC(O)CH2CH2R5, 5) —C(R1R2)OC(O)OCH2CH2C(R3R4)R5, provided that when Y is —C(O)(CH2)2R5, then R is R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is —CH(ONO2)CH(ONO2)R6; R6 is selected from CH3, CH2CH3 and CH(CH3)2; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.

摘要翻译： 具有结构的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是1） - （CH 2）3 R 5，2）-C（O）（CH 2）2 R 5，3）-C（R 1 R 2）OC（O）O （CH 2）n R 5，其中n为1或2，4）-C（R 1 R 2）OC（O）CH 2 CH 2 R 5，5）-C（R 1 R 2）OC（O）OCH 2 CH 2 C（R 3 R 4） O）（CH 2）2 R 5，则R 1是R 1，R 2，R 3和R 4独立地选自氢和C 1-4烷基; R5是-CH（ONO2）CH（ONO2）R6; R 6选自CH 3，CH 2 CH 3和CH（CH 3）2; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

公开(公告)号：US07799784B2

公开(公告)日：2010-09-21

申请号：US12162529

申请日：2007-02-02

申请人： Francesca Benedini ,  Francesco Impagnatiello ,  Stefano Biondi ,  Ennio Ongini ,  Wesley Kwan Mung Chong

发明人： Francesca Benedini ,  Francesco Impagnatiello ,  Stefano Biondi ,  Ennio Ongini ,  Wesley Kwan Mung Chong

IPC分类号： A61K31/495

CPC分类号： C07D233/50 ,  C07D239/76

摘要： The present invention relates to alpha2-adrenergic receptor agonist nitrooxyderivatives, including the following structure, having improved pharmacological activity and enhanced tolerability. They can be employed for the treatment of ocular diseases, in particular high intraocular pressure and glaucoma.

摘要翻译： 本发明涉及具有改善的药理活性和增强的耐受性的α2-肾上腺素能受体激动剂硝基氧化酶，包括以下结构。 它们可用于治疗眼部疾病，特别是高眼内压和青光眼。