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1. 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。

2. 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。

3. 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

4. 发明授权

US06531466B2 Tricyclic carbapenem compounds 失效
标题翻译：三环碳青霉烯化合物
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。

5. 发明申请

US20080167351A1 Compounds Which Potentiate Glutamate Receptor and Uses Thereof in Medicine 失效
标题翻译：增加谷氨酸受体的化合物及其在医学中的应用
公开(公告)号：US20080167351A1
公开(公告)日：2008-07-10
申请号：US11816284
申请日：2006-02-13
申请人： Daniele Andreotti , Luca Arista , Francesca Cardullo , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
发明人： Daniele Andreotti , Luca Arista , Francesca Cardullo , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
IPC分类号： A61K31/44 , C07D213/02 , C07C311/01 , A61K31/18 , C07D333/02 , A61K31/381 , A61P25/18
CPC分类号： C07D277/64 , C07D213/42 , C07D213/61 , C07D213/65 , C07D317/58 , C07D333/20
摘要： This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明涉及通过新的式（I）化合物增强谷氨酸受体：本发明还涉及该衍生物在治疗由谷氨酸受体增强介导的疾病和病症中的用途，含有衍生物的组合物及其制备方法。

6. 发明授权

US06900183B2 Macrolide antibiotics 失效
标题翻译：大环内酯抗生素
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。

7. 发明授权

US07790758B2 Compounds which potentiate glutamate receptor and uses thereof in medicine 失效
标题翻译：增强谷氨酸受体的药物及其在药物中的应用
公开(公告)号：US07790758B2
公开(公告)日：2010-09-07
申请号：US11816284
申请日：2006-02-13
申请人： Daniele Andreotti , Luca Arista , Francesca Cardullo , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
发明人： Daniele Andreotti , Luca Arista , Francesca Cardullo , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
IPC分类号： C07D333/20 , C07D317/58 , C07D277/64 , C07D213/61 , C07D213/42 , C07D213/647 , C07D213/64 , C07D213/65 , C07C311/08 , A61K31/4418 , A61K31/428 , A61K31/381 , A61K31/36 , A61K31/277 , A61K31/18
CPC分类号： C07D277/64 , C07D213/42 , C07D213/61 , C07D213/65 , C07D317/58 , C07D333/20
摘要： This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明涉及通过新的式（I）化合物增强谷氨酸受体：本发明还涉及该衍生物在治疗由谷氨酸受体增强介导的疾病和病症中的用途，含有衍生物的组合物及其制备方法。

8. 发明申请

US20110172255A1 Condensed N-Heterocyclic Compounds and their Use as CRF Receptor Antagonists 审中-公开
标题翻译：浓缩N-杂环化合物及其作为CRF受体拮抗剂的用途
公开(公告)号：US20110172255A1
公开(公告)日：2011-07-14
申请号：US11931313
申请日：2007-10-31
申请人： Daniele Andreotti , Giovanni Bernasconi , Emiliano Castiglioni , Stefania Anne Contini , Romano Di Fabio , Elettra Fazzolari , Aldo Feriani , Gabriella Gentile , Mario Mattioli , Anna Mingardi , Fabio Maria Sabbatini , Yves St-Denis
发明人： Daniele Andreotti , Giovanni Bernasconi , Emiliano Castiglioni , Stefania Anne Contini , Romano Di Fabio , Elettra Fazzolari , Aldo Feriani , Gabriella Gentile , Mario Mattioli , Anna Mingardi , Fabio Maria Sabbatini , Yves St-Denis
IPC分类号： A61K31/519 , C07D487/04 , C07D471/04 , A61K31/437 , A61P25/24 , A61P25/22
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula (I), 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：本发明提供式（I）化合物，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）介导的病症中的用途。

9. 发明申请

US20070004708A1 Condensed n-heterocyclic compounds and their use as crf receptor antagonists 有权
标题翻译：缩合的N-杂环化合物及其作为crf受体拮抗剂的用途
公开(公告)号：US20070004708A1
公开(公告)日：2007-01-04
申请号：US10552493
申请日：2004-04-07
申请人： Daniele Andreotti , Giovannie Bernasconi , Emiliano Castiglioni , Stefania Contini , Romano Di Fabio , Elettra Fazzolari , Aldo Feriani , Gabriella Gentile , Mario Mattioli , Anna Mingardi , Fabio Sabbatini , Yves St-Denis
发明人： Daniele Andreotti , Giovannie Bernasconi , Emiliano Castiglioni , Stefania Contini , Romano Di Fabio , Elettra Fazzolari , Aldo Feriani , Gabriella Gentile , Mario Mattioli , Anna Mingardi , Fabio Sabbatini , Yves St-Denis
IPC分类号： A61K31/549 , A61K31/519 , A61K31/496 , A61K31/501 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof (Formula (I)) wherein the dashed line may represent a double bond; R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 lkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R2, nitro, hydroxy, —NR3R4, cyano and or a group Z; R1 is hydrogen, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; D, G is —C— optionally substituted; X is carbon or nitrogen; Y is nitrogen or —C— optionally substituted; W is a 4-8 membered ring, which may be saturated or may contain one to three double bonds, and in which:—one carbon atom is replaced by a carbonyl or S(O)m; and—one to four carbon atoms may optionally be replaced by oxygen, nitrogen or NR12, S(O)m, carbonyl, and such ring may be further substituted by 1 to 8 substituents; Z is a 5-6 membered heterocycle, which may be substituted by 1 to 8 R5 groups or a phenyl ring, which may be substituted by 1 to 4 substituents; m is an integer from 0 to 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).
摘要翻译：本发明提供了包含立体异构体，前体药物和药学上可接受的盐或溶剂合物（式（I））的式（I）化合物，其中虚线可以表示双键; R是芳基或杂芳基，其各自可以被1-4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，卤素 C 1 -C 6烷氧基，-C（O）R 2，硝基，羟基，-NR 3 R 4，氰基和/或Z ; R 1是氢，C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6硫代烷基，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; D，G是-C-任选取代的; X是碳或氮; Y是氮或-C-任选取代的; W是4-8元环，其可以是饱和的或可以含有一至三个双键，并且其中： - 一个碳原子被羰基或S（O）m取代; 一至四个碳原子可以任选地被氧，氮或NR 12，S（O）m H，羰基取代，并且这种环可进一步被1 至8个取代基; Z是5-6元杂环，其可被1至8个R 5取代基或可被1至4个取代基取代的苯环; m为0至2的整数。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。

10. 发明授权

US5138048A 4-(2-Oxo-cyclohexyl) azetidinones 失效
标题翻译： 4-（2-氧代 - 环己基）氨基甲酸酯
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.

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