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31. 发明授权

US07419961B2 9a-azalides with anti-inflammatory activity 失效
标题翻译：具有消炎活性的9-氮杂
公开(公告)号：US07419961B2
公开(公告)日：2008-09-02
申请号：US10531462
申请日：2003-10-28
申请人： Mauro Napoletano , Andrea Mereu , Ermanno Moriggi , Fernando Ornaghi , Gabriele Morazzoni , Franco Pellacini
发明人： Mauro Napoletano , Andrea Mereu , Ermanno Moriggi , Fernando Ornaghi , Gabriele Morazzoni , Franco Pellacini
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： C07H17/00
摘要： Macrolides with anti-inflammatory activity are described. Particularly described are 9a-azalides and their anti-inflammatory activity without cladinose in position 3, the pharmaceutically acceptable salts thereof and the pharmaceutical composition that contain them as active principle.
摘要翻译：描述了具有抗炎活性的大环内酯类。具体描述的是9-氮杂ides啶及其在3位上没有分裂蛋白的抗炎活性，其药学上可接受的盐和含有它们作为活性成分的药物组合物。

32. 发明申请

US20080108679A1 Isoxazolic Derivative to Relieve Neuropathic Pain 失效
标题翻译：异恶唑衍生物减轻神经性疼痛
公开(公告)号：US20080108679A1
公开(公告)日：2008-05-08
申请号：US11718935
申请日：2005-11-14
申请人： Mauro Napoletano , Ermanno Moriggi
发明人： Mauro Napoletano , Ermanno Moriggi
IPC分类号： A61K31/42 , C07D261/08 , A61P25/02
CPC分类号： C07D261/18
摘要： The present invention relates to new pharmaceutical uses of an isoxazolic derivative or a pharmaceutically acceptable salt thereof in the preparation of a medicament useful for treating the neuropathic pain.
摘要翻译：本发明涉及异恶唑衍生物或其药学上可接受的盐在制备用于治疗神经性疼痛的药物中的新药用途。

33. 发明申请

US20070167381A1 Macrolides with antiinflammatory activity 失效
标题翻译：具有抗炎活性的大环内酯类
公开(公告)号：US20070167381A1
公开(公告)日：2007-07-19
申请号：US10587623
申请日：2005-01-25
申请人： Andrea Mereu , Mauro Napoletano , Fernando Ornaghi , Ermanno Moriggi , Franco Pellacini
发明人： Andrea Mereu , Mauro Napoletano , Fernando Ornaghi , Ermanno Moriggi , Franco Pellacini
IPC分类号： A61K31/7048 , C07H17/08
CPC分类号： C07H17/08
摘要： Macrolide compounds of formula (I) wherein X, R, R1, R2, R3 and R4, have the meanings as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and the use thereof in the treatment and prophylaxis of inflammatory diseases, are described.
摘要翻译：式（I）的大环内酯化合物，其中X，R，R 1，R 2，R 3和R 4 ，具有本说明书中定义的含义，其药学上可接受的盐，含有它们作为活性成分的药物组合物及其在治疗和预防炎性疾病中的用途。

34. 发明申请

US20060166904A1 9a-azalides with anti-inflammatory activity 失效
标题翻译：具有消炎活性的9-氮杂
公开(公告)号：US20060166904A1
公开(公告)日：2006-07-27
申请号：US10531462
申请日：2003-10-28
申请人： Mauro Napoletano , Andrea Mereu , Ermanno Moriggi , Fernando Ornaghi , Gabriele Morazzoni , Franco Pellacini
发明人： Mauro Napoletano , Andrea Mereu , Ermanno Moriggi , Fernando Ornaghi , Gabriele Morazzoni , Franco Pellacini
IPC分类号： A61K31/7052 , C07H17/08
CPC分类号： C07H17/00
摘要： Macrolides with anti-inflammatory activity are described, and more particularly, 9a-azalides without cladinose in position 3 with anti-inflammatory activity, their pharmaceutically acceptable salts and pharmaceutical compositions that contain them as active principle.
摘要翻译：描述了具有抗炎活性的大环内酯，更具体地说，具有抗炎活性的位置3中没有分裂蛋白的9a-氮杂，其药学上可接受的盐和药物组合物含有它们作为活性成分。

35. 发明授权

US06894164B2 Process for the preparation of (pyridinylidene)-phthalides 失效
标题翻译：制备（亚吡啶基） - 酞菁的方法
公开(公告)号：US06894164B2
公开(公告)日：2005-05-17
申请号：US10671525
申请日：2003-09-29
申请人： Mauro Napoletano
发明人： Mauro Napoletano
IPC分类号： C07B61/00 , C07D401/06 , C07D405/06
CPC分类号： C07D405/06
摘要： A process for the preparation of phthalazines by preparing intermediate (pyridinylidene)-phthalides starting from 3-oxo-1,3-dihydro-isobenzofuran-1-carboxylic acids and pyridinecarbaldehydes, is described.
摘要翻译：描述了从3-氧代-1,3-二氢 - 异苯并呋喃-1-羧酸和吡啶甲醛开始制备中间体（亚吡啶基） - 酞菁的制备酞嗪的方法。

36. 发明授权

US06525055B1 Tricyclic phthalazine derivatives as phosphodiesterase 4 inhibitors 失效
标题翻译：三环酞嗪衍生物作为磷酸二酯酶4抑制剂
公开(公告)号：US06525055B1
公开(公告)日：2003-02-25
申请号：US09830679
申请日：2001-04-30
申请人： Mauro Napoletano , Gabriele Norcini , Franco Pellacini , Gabriele Morazzoni
发明人： Mauro Napoletano , Gabriele Norcini , Franco Pellacini , Gabriele Morazzoni
IPC分类号： A61K315025
CPC分类号： C07D487/04
摘要： Tricyclic phthalazine compounds of formula (I) wherein A is a 5-7 membered heterocycle containing from 1 to 4 nitrogen atoms, optionally partially or totally unsaturated, and optionally substituted by a (C1-4)alkyl group in turn optionally substituted; Z is NH, methylene, a C2-6 alkylene chain optionally branched and/or unsaturated and/or interrupted by a C5-7 cycloalkyl residue; Cy is phenyl or heterocycle optionally substituted by one or more substituents, or a COR4 group wherein R4 is hydroxy, alkoxy, amino optionally substituted by one or two (C1-6)alkyl groups or by hydroxy; R is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; R1 is hydrogen; a (C1-8)-alkyl, (C2-8)-alkenyl or (C2-8)-alkynyl group optionally substituted by hydroxy, oxo, aryl or heterocycle, and optionally interrupted by one or more heteroatoms or heterogroups; a (C1-4)alkoxy group or a (C4-7)cycloalkoxy group optionally containing an oxygen atom and optionally substituted by a polar substituent in the cyclic moiety, aryloxy aryl-(C1-10)-alkoxy; the N—O derivatives and the pharmaceutically acceptable salts thereof are described. The compounds of formula (I) are PDE 4 inhibitors.
摘要翻译：式（I）的三环酞嗪化合物，其中A是含有1至4个氮原子的5-7元杂环，任选地部分或完全不饱和，并且任选地被（C 1-4）烷基取代， Z是NH，亚甲基，任选支链和/或不饱和的和/或被C5-7环烷基残基中断的C2-6亚烷基链; Cy是任选被一个或多个取代基取代的苯基或杂环，或其中R4是羟基，烷氧基，任选被一个或两个（C 1-6）烷基或羟基取代的氨基的COR 4基团; R为（C 1-6）烷基或多氟（C 1-6）烷基; R1是氢; 任选被羟基，氧代，芳基或杂环取代的（C 1-8） - 烷基，（C 2-8） - 烯基或（C 2-8） - 炔基，并且任选被一个或多个杂原子或杂团中断; 芳氧基芳基 - （C 1-10） - 烷氧基，（C 1-4）烷氧基或任选含有氧原子且任选被环状部分中的极性取代基取代的（C 4-7）环烷氧基; 描述了N-O衍生物及其药学上可接受的盐。式（I）化合物是PDE 4抑制剂。

37. 发明授权

US06498160B2 Phthalazine derivatives as phosphodiesterase 4 inhibitors 失效
标题翻译：酞嗪衍生物作为磷酸二酯酶4抑制剂
公开(公告)号：US06498160B2
公开(公告)日：2002-12-24
申请号：US09987266
申请日：2001-11-14
申请人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gabriele Morazzoni
发明人： Mauro Napoletano , Gabriele Norcini , Giancarlo Grancini , Franco Pellacini , Gabriele Morazzoni
IPC分类号： A61K31502
CPC分类号： C07D401/06 , C07D237/30 , C07D237/32 , C07D237/34 , C07D405/06
摘要： Phthalazine compounds having formula I wherein , A, B, R, R1, R2 and R3 are as defined herein, useful as phosphodiesterase 4 inhibitors.
摘要翻译： “CUSTOM-CHARACTER FILE =”US06498160-20021224-P00900.TIF“中的具有式I的酞嗪化合物”ALT =“自定义字符”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00001”/> B，R，R 1，R 2和R 3如本文所定义，可用作磷酸二酯酶4抑制剂。

38. 发明授权

US06211387B1 Diol compounds as intermediates for preparing antimycotic compounds 失效
标题翻译：二醇化合物作为制备抗真菌化合物的中间体
公开(公告)号：US06211387B1
公开(公告)日：2001-04-03
申请号：US09555509
申请日：2000-06-05
申请人： Mauro Napoletano , Marco Villa , Aldo Belli , Giancarlo Grancini , Biase Continanza
发明人： Mauro Napoletano , Marco Villa , Aldo Belli , Giancarlo Grancini , Biase Continanza
IPC分类号： C07D31500
CPC分类号： C07C33/483 , Y02P20/55
摘要： A compound of formula (II), wherein R1 is chloro, fluoro or trifluoromethyl; R2 is hydrogen, chloro, fluoro or trifluoromethyl; and R is hydrogen or a protective group for the hydroxy moiety useful as an intermediate for the synthesis of antimycotic azole compounnds.
摘要翻译：式（II）的化合物，其中R 1是氯，氟或三氟甲基; R2是氢，氯，氟或三氟甲基; 并且R是氢或用作羟基部分的保护基团，其用作合成抗真菌唑化合物的中间体。

39. 发明授权

US6103909A Azole compounds endowed with antimycotic activity for human and veterinary use 失效
标题翻译：唑类化合物具有抗真菌活性，适用于人和兽用
公开(公告)号：US6103909A
公开(公告)日：2000-08-15
申请号：US138904
申请日：1998-08-24
申请人： Mauro Napoletano , Cristina Fraire , Enrico Albini , Giovanna Schioppacassi
发明人： Mauro Napoletano , Cristina Fraire , Enrico Albini , Giovanna Schioppacassi
IPC分类号： A61K31/00 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4196 , A61P31/00 , A61P31/10 , C07D233/60 , C07D249/08 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： Compounds of formula ##STR1## wherein R.sub.1 is chloro, fluoro, bromo or trifluoromethyl;R.sub.2 is hydrogen, chloro , fluoro, bromo or trifluoromethyl;Z is CH or N;R.sub.3, R.sub.4 and R.sub.5, which are the same or different, are hydrogen or C.sub.1 -C.sub.4 alkyl, with the proviso that R.sub.4 is different from R.sub.5 when R.sub.3 is hydrogen;X is O, S, SO or SO.sub.2 ;R.sub.6 is a C.sub.1 -C.sub.5 polyfluoroalkyl group containing at least two fluorine atoms and optionally other halogen atoms selected from the group consisting of chloro and bromo; processes for their preparation and pharmaceutical compositions containing them are described.The compounds of formula II-A are endowed with a marked wide range antimycotic acitivity.
摘要翻译：式的化合物其中R 1是氯，氟，溴或三氟甲基; R2是氢，氯，氟，溴或三氟甲基; Z是CH或N; R 3，R 4和R 5相同或不同，是氢或C 1 -C 4烷基，条件是当R3是氢时，R 4不同于R 5; X是O，S，SO或SO 2; R6是含有至少两个氟原子和任选地其它选自氯和溴的卤素原子的C1-C5多氟烷基; 描述了其制备方法和含有它们的药物组合物。式II-A的化合物具有显着的广泛的抗真菌活性。

40. 发明授权

US5142066A Stereoselective process for the preparation of 2-amino-ethanol derivatives having a central analgesic activity and intermidiates thereof 失效
标题翻译：制备具有中心活性的2-氨基 - 乙醇衍生物及其中间体的立体选择性方法
公开(公告)号：US5142066A
公开(公告)日：1992-08-25
申请号：US672685
申请日：1991-03-20
申请人： Mauro Napoletano , Gian C. Grancini , Carlo Veneziani , Dario Chiarino
发明人： Mauro Napoletano , Gian C. Grancini , Carlo Veneziani , Dario Chiarino
IPC分类号： C07B53/00 , C07D207/26 , C07D317/20 , C07D317/30
CPC分类号： C07D207/26
摘要： A stereoselective process for the preparation of the compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, a and b have the meanings reported in the specification, is described.The compounds of formula I have a remarkable central analgesic activity and they are useful in the pharmaceutical field.

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