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1.发明申请Compounds Having Aryl-Sulphonamidic Structure Useful As Metalloproteases Inhibitors 失效具有芳基磺酰胺结构的化合物可用作金属蛋白酶抑制剂公开(公告)号：US20100087505A1
公开(公告)日：2010-04-08
申请号：US12531119
申请日：2008-03-14
IPC分类号： A61K31/404 , C07C313/06 , C07D209/36 , A61K31/18 , A61P35/00
CPC分类号： C07C311/48 , C07D295/08 , C07D295/088
摘要： The invention relates to aryl-sulphonamido compounds endowed with inhibitory activity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, R4, R5, n and m have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.
摘要翻译： 本发明涉及赋予对金属蛋白酶MMP的抑制活性的芳基磺酰胺化合物，其具有式（I），其中R，R 1，R 2，R 3，R 4，R 5，n和m具有本说明书中报道的含义; 本发明还涉及其制备方法，包含它们的药物组合物及其作为治疗剂的用途，特别是治疗退行性疾病。
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2.发明授权Compounds having aryl-sulphonamidic structure useful as metalloproteases inhibitors 失效具有芳基 - 磺酰胺结构的化合物可用作金属蛋白酶抑制剂公开(公告)号：US08329751B2
公开(公告)日：2012-12-11
申请号：US12531119
申请日：2008-03-14
IPC分类号： A61K31/495 , A61K31/4035 , A61K31/18 , C07D295/088 , C07D209/48 , C07D311/48
CPC分类号： C07C311/48 , C07D295/08 , C07D295/088
摘要： The invention relates to aryl-sulphonamido compounds endowed with inhibitory activity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, R4, R5, n and m have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.
摘要翻译： 本发明涉及赋予对金属蛋白酶MMP的抑制活性的芳基磺酰胺化合物，其具有式（I），其中R，R 1，R 2，R 3，R 4，R 5，n和m具有本说明书中报道的含义; 本发明还涉及其制备方法，包含它们的药物组合物及其作为治疗剂的用途，特别是治疗退行性疾病。
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公开(公告)号：US08093386B2
公开(公告)日：2012-01-10
申请号：US12309701
申请日：2007-07-25
IPC分类号： C07D207/40 , C07D209/48 , C07D211/40 , C07D211/54 , C07D239/02 , C07C57/13 , C07C259/04 , C07C311/10 , A61K31/18 , A61K31/19 , A61K31/40 , A61K31/445 , A61K31/515
CPC分类号： C07C317/44 , C07C317/14 , C07C317/22 , C07C323/62 , C07D207/46 , C07D209/48 , C07D211/76 , C07D239/60 , C07F9/3882
摘要： There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc metalloproteinases.
摘要翻译： 描述了具有下面通式（I）的化合物及其药学上可接受的盐，其中E，X，m，q，R 1，R 2，n和ZBG具有在本说明书中报道的含义，在治疗中作为抑制剂 锌金属蛋白酶。
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公开(公告)号：US20090239829A1
公开(公告)日：2009-09-24
申请号：US12309701
申请日：2007-07-25
IPC分类号： A61K31/662 , C07C233/64 , A61K31/165 , C07D333/06 , A61K31/381 , C07F9/38 , C07D207/00 , A61K31/40 , C07D239/02 , A61K31/515 , C07D211/40 , A61K31/445 , A61P35/00
CPC分类号： C07C317/44 , C07C317/14 , C07C317/22 , C07C323/62 , C07D207/46 , C07D209/48 , C07D211/76 , C07D239/60 , C07F9/3882
摘要： There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc metalloproteinases.
摘要翻译： 描述了具有下面通式（I）的化合物及其药学上可接受的盐，其中E，X，m，q，R 1，R 2，n和ZBG具有在本说明书中报道的含义，在治疗中作为抑制剂 锌金属蛋白酶。
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5.发明申请1-PHENYLALCOXY-2-BETA-PHENYLETHYL DERIVATIVES AS P-GLYCOPROTEIN (P-GP) INHIBITORS USEFUL IN DRUG RESISTANCE EVENTS 审中-公开作为P-GLYCOPROTEIN（P-GP）抑制剂用于药物耐药活动的1-苯基氧基-2-戊基衍生物公开(公告)号：US20090093493A1
公开(公告)日：2009-04-09
申请号：US11869136
申请日：2007-10-09
申请人： Francesco Berardi , Nicola Antonio Colabufo , Roberto Perrone , Aldo Balsamo , Simona Rapposelli , Maria Digiacomo
发明人： Francesco Berardi , Nicola Antonio Colabufo , Roberto Perrone , Aldo Balsamo , Simona Rapposelli , Maria Digiacomo
IPC分类号： A61K31/497 , C07D217/00 , C07D211/04 , C07D401/04 , C07D241/04 , A61K31/47 , A61K31/445 , A61P35/00
CPC分类号： C07D211/22 , C07D213/30 , C07D213/74 , C07D217/04 , C07D239/42 , C07D295/088 , C07D295/096 , C07D303/23
摘要： The invention relates to a new class of compounds, which are 1-phenylalcoxy-2-β-phenylethyl derivatives, as P-glycoprotein (P-GP) inhibitors. These compounds are useful in drug resistance events. They have been shown able to inhibit in a dose-dependent manner Glycoprotein-P (P-gp) activity in cell lines in which the expression of said glycoprotein is very high, like Caco-2 (human colon cancer) cells and MCF7/Adr (adriamycin-resistant human breast carcinoma) cells. The invention also relates to methods of production and the utilization of such compounds as medicaments useful in the treatment of states linked to the difficulty for some drugs to cross the blood-brain barrier (BBB) and generally within the context of the problems of drug resistance induced by chemotherapy agents.
摘要翻译： 本发明涉及作为P-糖蛋白（P-GP）抑制剂的新类化合物，其是1-苯基乙氧基-2-β-苯乙基衍生物。 这些化合物可用于耐药事件。 已经显示能够以剂量依赖性方式抑制糖蛋白-P（P-gp）活性，其中所述糖蛋白的表达非常高，如Caco-2（人结肠癌）细胞和MCF7 / Adr （阿霉素抗性人乳腺癌）细胞。 本发明还涉及生产和利用这些化合物的方法，所述化合物可用于治疗与某些药物跨越血脑屏障（BBB）的困难有关的状态，并且通常在耐药性问题的背景下 由化疗药物引起。
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6.发明授权Ceramide analogs, process for their preparation and their use as antitumor agents 失效神经酰胺类似物，其制备方法及其作为抗肿瘤剂的用途公开(公告)号：US06956109B1
公开(公告)日：2005-10-18
申请号：US10031692
申请日：2000-07-21
申请人： Bruno Macchia , Aldo Balsamo , Marco Macchia , Mario Del Tacca , Romano Danesi
发明人： Bruno Macchia , Aldo Balsamo , Marco Macchia , Mario Del Tacca , Romano Danesi
IPC分类号： A61K31/513 , A61K31/7068 , A61P35/00 , C07D239/54 , C07D239/56 , C07H15/26 , C07G11/00 , C07G3/00 , C07H15/00 , C07H17/00
CPC分类号： C07D239/54 , C07D239/56 , C07H15/26
摘要： The present invention is directed to ceramide analog compounds of general formula (I) the process for their preparation and use for the preparation of pharmaceutical formulations for the treatment of tumors.
摘要翻译： 本发明涉及通式（I）的神经酰胺类似物化合物，其用于制备和用于制备用于治疗肿瘤的药物制剂的方法。
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7.发明授权Ceramide analogs, process for their preparation and their use as antitumor agents 失效神经酰胺类似物，其制备方法及其作为抗肿瘤剂的用途公开(公告)号：US07214794B2
公开(公告)日：2007-05-08
申请号：US10919867
申请日：2004-08-17
申请人： Bruno Macchia , Aldo Balsamo , Marco Macchia , Mario Del Tacca , Romano Danesi
发明人： Bruno Macchia , Aldo Balsamo , Marco Macchia , Mario Del Tacca , Romano Danesi
IPC分类号： C07D293/10 , A01N43/04 , A61K31/70
CPC分类号： C07D239/54 , C07D239/56 , C07H15/26
摘要： The present invention is directed to ceramide analog compounds of general formula (I) the process for their preparation and use for the preparation of pharmaceutical formulations for the treatment of tumors
摘要翻译： 本发明涉及通式（I）的神经酰胺类似物化合物，其用于制备和用于制备用于治疗肿瘤的药物制剂的方法
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公开(公告)号：US20050020533A1
公开(公告)日：2005-01-27
申请号：US10919867
申请日：2004-08-17
申请人： Bruno Macchia , Aldo Balsamo , Marco Macchia , Mario Del Tacca , Romano Danesi
发明人： Bruno Macchia , Aldo Balsamo , Marco Macchia , Mario Del Tacca , Romano Danesi
IPC分类号： A61K31/513 , A61K31/7068 , A61P35/00 , C07D239/54 , C07D239/56 , C07H15/26 , C07H19/048 , A61K31/7072
CPC分类号： C07D239/54 , C07D239/56 , C07H15/26
摘要： The present invention is directed to ceramide analog compounds of general formula (I) the process for their preparation and use for the preparation of pharmaceutical formulations for the treatment of tumors.
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9.发明授权Geranylgeranyl-derivatives, process for the preparation thereof and related pharmaceutical compositions 失效香叶基香叶基香叶基衍生物，其制备方法和相关的药物组合物公开(公告)号：US06242433B1
公开(公告)日：2001-06-05
申请号：US09077196
申请日：1998-09-15
申请人： Aldo Balsamo , Bruno Macchia , Marco Macchia , Massimo Baldacci , Romano Danesi , Mario Del Tacca
发明人： Aldo Balsamo , Bruno Macchia , Marco Macchia , Massimo Baldacci , Romano Danesi , Mario Del Tacca
IPC分类号： A61K31664
CPC分类号： C07F9/3808 , C07C307/04 , C07C307/06 , C07F9/3821 , C07F9/3826 , C07F9/4006
摘要： The present invention relates to novel geranylgeranyl derivatives and the pharmaceutically acceptable salts thereof having antiproliferative activity in eukaryotic cells with respect to the inhibition of protein geranygeranylation. The invention also relates to the pharmaceutical compositions containing the novel derivatives and to the process of preparation thereof.
摘要翻译： 本发明涉及新颖的香叶基香叶基香叶基衍生物及其在真核细胞中具有抗增殖活性的药学上可接受的盐，涉及抑制蛋白质龙胆神经酰化。 本发明还涉及含有新衍生物的药物组合物及其制备方法。
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