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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

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。

3. 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。

4. 发明授权

US5420296A Ureido derivatives of poly-4-amino-2-carboxy-1-methyl compounds 失效
标题翻译：聚-4-氨基-2-羧基-1-甲基化合物的脲基衍生物
公开(公告)号：US5420296A
公开(公告)日：1995-05-30
申请号：US66583
申请日：1993-05-25
申请人： Nicola Mongelli , Giovanni Biasoli , Alfredo Paio , Maria Grandi , Marina Ciomei
发明人： Nicola Mongelli , Giovanni Biasoli , Alfredo Paio , Maria Grandi , Marina Ciomei
IPC分类号： A61K31/40 , A61K31/7056 , A61P3/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D207/325 , C07D207/335 , C07D207/34 , C07D403/02 , C07D403/14
CPC分类号： C07D207/34
摘要： The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;each of the B groups, which are the same, isa) a saturated or unsaturated, carbocyclic or condensed carbocyclic ring substituted by one or more acid groups;b) a saturated or unsaturated, heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen, oxygen and sulphur, substituted by one or more acid groups;c) a pyranyl or furanyl sugar residue substituted by one or more acid groups; ord) a --CH.sub.2 (CHA).sub.r CH.sub.2 A group, wherein each A group, being the same or different, is an acid group and r is 0, 1 or 2; and the pharmaceutically acceptable salts thereof, which are useful as angiogenesis inhibitors.
摘要翻译：本发明涉及式（I）的取代吡咯的脲基衍生物，其中m和n各自相同，为1〜3的整数; W是硫的氧; 每个B基团相同，是a）被一个或多个酸基团取代的饱和或不饱和的碳环或稠合的碳环; b）饱和或不饱和的异单环或杂双环，其含有一个或多个选自氮，氧和硫的杂原子，被一个或多个酸基取代; c）被一个或多个酸基取代的吡喃基或呋喃基糖残基; 或d）-CH 2（CHA）r CH 2 A基团，其中每个A基团相同或不同，为酸基团，r为0,1或2; 及其药学上可接受的盐，其可用作血管生成抑制剂。

5. 发明授权

US5260329A Ureido derivatives of poly-4-amino-2-carboxy-1-methyl compounds 失效
标题翻译：聚-4-氨基-2-羧基-1-甲基化合物的脲基衍生物
公开(公告)号：US5260329A
公开(公告)日：1993-11-09
申请号：US752577
申请日：1991-09-09
申请人： Nicola Mongelli , Giovanni Biasoli , Alfredo Paio , Maria Grandi , Marina Ciomei
发明人： Nicola Mongelli , Giovanni Biasoli , Alfredo Paio , Maria Grandi , Marina Ciomei
IPC分类号： A61K31/40 , A61K31/7056 , A61P3/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D207/325 , C07D207/335 , C07D207/34 , C07D403/02 , C07D403/14
CPC分类号： C07D207/34
摘要： The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;each of the B groups, which are the same, isa) a saturated or unsaturated, carbocyclic or condensed carbocyclic ring substituted by one or more acid groups;b) a saturated or unsaturated, heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen, oxygen and sulphur, substituted by one or more acid groups;c) a pyranyl or furanyl sugar residue substituted by one or more acid groups; ord) a --CH.sub.2 (CHA).sub.r CH.sub.2 A group, wherein each A group, being the same or different, is an acid group and r is 0, 1 or 2; and the pharmaceutically acceptable salts thereof, which areuseful as angiogenesis inhibitors.
摘要翻译： PCT No.PCT / EP91 / 00014 Sec。 371日期1991年9月9日 102（e）1991年9月9日PCT PCT 1991年1月7日PCT公布。出版物WO91 / 10649 日期：1991年7月25日本发明涉及式（I）的取代吡咯的脲基衍生物，其中m和n相同，为1〜3的整数; W是硫的氧; 每个B基团相同，是a）被一个或多个酸基团取代的饱和或不饱和的碳环或稠合的碳环; b）饱和或不饱和的异单环或杂双环，其含有一个或多个选自氮，氧和硫的杂原子，被一个或多个酸基取代; c）被一个或多个酸基取代的吡喃基或呋喃基糖残基; 或d）-CH 2（CHA）r CH 2 A基团，其中每个A基团相同或不同，为酸基团，r为0,1或2; 及其药学上可接受的盐，其可用作血管生成抑制剂。

6. 发明授权

US07482365B2 Piperidylcarboxamide derivatives and their use in the treatment of tachykinin-mediated diseases 失效
标题翻译：哌啶甲酰胺衍生物及其用于治疗速激肽介导的疾病
公开(公告)号：US07482365B2
公开(公告)日：2009-01-27
申请号：US10502266
申请日：2003-02-05
申请人： Giuseppe Alvaro , Alfredo Paio , Alessandro Pontiroli , Simone Spada , Maria Elvira Tranquillini
发明人： Giuseppe Alvaro , Alfredo Paio , Alessandro Pontiroli , Simone Spada , Maria Elvira Tranquillini
IPC分类号： A61K31/445 , C07D211/60
CPC分类号： C07D401/04 , C07D211/58 , C07D405/12
摘要： The present invention relates to piperidine derivatives of formula (I): wherein R, R1, R2, R3, R4, R5, R6, X, Y, m and n are as defined herein; and pharmaceutically acceptable salts and solvates thereof; the process for their preparation and their use in the treatment of conditions mediated by tachykinins.
摘要翻译：本发明涉及式（I）的哌啶衍生物：其中R，R 1，R 2，R 3，R 4，R 5，R 6，X，Y，m和n如本文所定义; 及其药学上可接受的盐和溶剂合物; 其制备方法及其用于治疗由速激肽介导的病症。

7. 发明申请

US20080262041A1 Beta-Lactams for Treatment of Cns Disorders 审中-公开
标题翻译：用于治疗Cns病的β-内酰胺类
公开(公告)号：US20080262041A1
公开(公告)日：2008-10-23
申请号：US10595662
申请日：2004-11-10
申请人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Alfredo Paio , Maria Elvira Tranquillini , Lucia Mattioli
发明人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Alfredo Paio , Maria Elvira Tranquillini , Lucia Mattioli
IPC分类号： A61K31/4439 , A61K31/4025 , C07D401/04 , A61P25/18 , A61P25/24 , A61P19/02 , C07D403/04
CPC分类号： C07D401/04
摘要： The present invention relates to novel compounds of formula (I): wherein — represents a single or a double bond; R is a radical selected from: in which R1 is halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy and p is zero or an integer from 1 to 3; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen, hydroxy or C1-4 alkyl; R4 is hydrogen or R4 together with R3 represents ═O or ═CH2; R5 is phenyl, naphthyl, a 9 to 10 membered fused bicyclic heterocyclic group or a 5 or 6 membered heteroaryl group, wherein said groups are optionally substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, hydroxy, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or S(O)qC1-4 alkyl; R6 and R7 independently are hydrogen, cyano, C1-4 alkyl; R8 is (CH2)rR10; R9 is hydrogen, halogen, C3-7 cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by one or two groups selected from halogen, cyano, hydroxy or C1-4 alkoxy; R10 is hydrogen or C3-7 cycloalkyl; n is 1 or 2; q is 0, 1 or 2; r is 0 or an integer from 1 to 4; or a pharmaceutically acceptable salt or a solvate thereof, process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of the serotonin reuptake transporter protein
摘要翻译：本发明涉及新的式（I）化合物：其中 - 表示单键或双键; R是选自以下的基团：其中R 1是卤素，氰基，C 1-4烷基，C 1-4烷氧基，三氟甲基或三氟甲氧基，p为0或1至3的整数; R 2是氢或C 1-4烷基; R 3是氢，羟基或C 1-4烷基; R 4是氢或R 4与R 3一起代表-O或-CH 2; R 5是苯基，萘基，9至10元稠合双环杂环基或5或6元杂芳基，其中所述基团任选被1至3个独立地选自三氟甲基，烷基，羟基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或S（O）q C 1-4烷基; R 6和R 7独立地是氢，氰基，C 1-4烷基; R 8是（CH 2 2）r R 10; R 9是氢，卤素，C 3-7环烷基，羟基，硝基，氰基或C 1-4烷基，任选被一个或多个两个选自卤素，氰基，羟基或C 1-4烷氧基的基团; R 10是氢或C 3-7环烷基; n为1或2; q是0,1或2; r为0或1至4的整数; 或其药学上可接受的盐或溶剂合物，其制备方法及其用于治疗由粘蛋白介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白

8. 发明申请

US20050171153A1 Piperidylcarboxamide derivatives and their use in the treatment of tachykinin-mediated diseases 失效
标题翻译：哌啶甲酰胺衍生物及其用于治疗速激肽介导的疾病
公开(公告)号：US20050171153A1
公开(公告)日：2005-08-04
申请号：US10502266
申请日：2003-02-05
申请人： Giuseppe Alvaro , Alfredo Paio , Alessandro Pontiroli , Simone Spada , Maria Tranquillini
发明人： Giuseppe Alvaro , Alfredo Paio , Alessandro Pontiroli , Simone Spada , Maria Tranquillini
IPC分类号： A61K31/451 , A61K31/4525 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P1/08 , A61P1/10 , A61P9/10 , A61P11/02 , A61P11/06 , A61P11/14 , A61P17/00 , A61P17/04 , A61P17/06 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P29/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D211/58 , C07D211/60 , C07D401/04 , C07D405/12 , C07D41/02 , A61K31/445
CPC分类号： C07D401/04 , C07D211/58 , C07D405/12
摘要： The present invention relates to piperidine derivatives of formula (I): wherein R, R1, R2, R3, R4, R5, R6, X, Y, m and n are as defined herein; and pharmaceutically acceptable salts and solvates thereof; the process for their preparation and their use in the treatment of conditions mediated by tachykinins.
摘要翻译：本发明涉及式（I）的哌啶衍生物：其中R 1，R 2，R 2，R 3，R 3， R 5，R 5，R 6，X，Y，m和n如本文所定义; 及其药学上可接受的盐和溶剂合物; 其制备方法及其用于治疗由速激肽介导的病症。

9. 发明授权

US5593976A New ureido derivatives of poly-4-amino-2-carboxy-1-methyl compounds 失效
标题翻译：聚-4-氨基-2-羧基-1-甲基化合物的新脲基衍生物
公开(公告)号：US5593976A
公开(公告)日：1997-01-14
申请号：US426130
申请日：1995-04-21
申请人： Nicola Mongelli , Giovanni Biasoli , Alfredo Paio , Maria Grandi , Marina Ciomei
发明人： Nicola Mongelli , Giovanni Biasoli , Alfredo Paio , Maria Grandi , Marina Ciomei
IPC分类号： A61K31/40 , A61K31/7056 , A61P3/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D207/325 , C07D207/335 , C07D207/34 , C07D403/02 , C07D403/14
CPC分类号： C07D207/34
摘要： The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;each of the B groups, which are the same, isa) a saturated or unsaturated, carbocyclic or condensed carbocyclic ring substituted by one or more acid groups;b) a saturated or unsaturated, heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen, oxygen and sulphur, substituted by one or more acid groups;c) a pyranyl or furanyl sugar residue substituted by one or more acid groups; ord) a --CH.sub.2 (CHA).sub.8 CH.sub.2 A group, wherein each A group, being the same or different, is an acid group and r is 0, 1 or 2;and the pharmaceutically acceptable salts thereof, which are useful as angiogenesis inhibitors.
摘要翻译：本发明涉及式（I）的取代吡咯的脲基衍生物，其中m和n各自相同，为1〜3的整数; W是硫的氧; 每个B基团相同，是a）被一个或多个酸基团取代的饱和或不饱和的碳环或稠合的碳环; b）饱和或不饱和的异单环或杂双环，其含有一个或多个选自氮，氧和硫的杂原子，被一个或多个酸基取代; c）被一个或多个酸基取代的吡喃基或呋喃基糖残基; 或d）-CH 2（CHA）8 CH 2 A基团，其中每个A基团相同或不同，为酸基团，r为0,1或2; 及其药学上可接受的盐，其可用作血管生成抑制剂。

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