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1. 发明授权

US06369096B1 Benzyloxy prodigiosine compounds 失效
标题翻译：苄氧基孕激素化合物
公开(公告)号：US06369096B1
公开(公告)日：2002-04-09
申请号：US09402455
申请日：1999-10-07
申请人： Roberto D'Alessio , Ermes Vanotti , Alberto Bargiotti , Marcellino Tibolla , Mario Ferrari , Anna Maria Isetta , Francesco Colotta
发明人： Roberto D'Alessio , Ermes Vanotti , Alberto Bargiotti , Marcellino Tibolla , Mario Ferrari , Anna Maria Isetta , Francesco Colotta
IPC分类号： A61K314025
CPC分类号： C07D207/44
摘要： A compound, having utility as an immunomodulating agent, which is a prodigiosine of formula (I): wherein R1 is hydrogen or C1-C5 alkyl; and R2 is a C1-C5 alkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：具有作为免疫调节剂的作用的化合物，其是式（I）的产物：其中R 1是氢或C 1 -C 5烷基; 并且R 2是C 1 -C 5烷基;或其药学上可接受的盐。

2. 发明授权

US6071947A Indolyl-pyrrolydenemethylpyrrole derivatives and process for their preparation 失效
标题翻译：吲哚基 - 吡咯烷酮甲基吡咯衍生物及其制备方法
公开(公告)号：US6071947A
公开(公告)日：2000-06-06
申请号：US147249
申请日：1998-11-12
申请人： Roberto D'Alessio , Marcellino Tibolla , Alberto Bargiotti , Anna Maria Isetta , Mario Ferrari , Francesco Colotta
发明人： Roberto D'Alessio , Marcellino Tibolla , Alberto Bargiotti , Anna Maria Isetta , Mario Ferrari , Francesco Colotta
IPC分类号： A61K31/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61P35/00 , A61P37/00 , A61P37/06 , C07D403/14 , A61K31/4025 , A61K31/405 , C07D207/333 , C07D209/12
CPC分类号： C07D403/14
摘要： The present invention relates to substituted (1H-indol-2-yl)-5[(2H-pyrrol-2-ylidene) methyl]-1H-pyrrole compounds and their use as immunomodulating agents, to the preparation of the compounds and to pharmaceutical compositions comprising them.
摘要翻译： PCT No.PCT / EP98 / 01285 Sec。 371日期：1998年11月12日 102（e）1998年11月12日日期PCT提交1998年2月27日PCT公布。公开号WO98 / 40380 PCT 日期：1998年9月17日本发明涉及取代的（1H-吲哚-2-基）-5 [（2H-吡咯-2-亚基）甲基] -1H-吡咯化合物及其作为免疫调节剂的用途，所述化合物和包含它们的药物组合物。

3. 发明授权

US06291509B1 Synergistic immunosuppressant composition containing a 2,2'-bi-1H-pyrrole compound 失效
标题翻译：含有2,2'-双-1H-吡咯化合物的协同免疫抑制剂组合物
公开(公告)号：US06291509B1
公开(公告)日：2001-09-18
申请号：US09068555
申请日：1998-05-19
申请人： Mario Ferrari , Paola Gnocchi , Maria Chiara Fornasiero , Francesco Colotta , Roberto D′Alessio , Anna Maria Isetta
发明人： Mario Ferrari , Paola Gnocchi , Maria Chiara Fornasiero , Francesco Colotta , Roberto D′Alessio , Anna Maria Isetta
IPC分类号： A61K3140
CPC分类号： A61K45/06 , A61K38/13 , A61K31/40 , A61K2300/00
摘要： A product containing: (a) an immunosuppressant agent (A) and (b) at least one immunosuppressant 2,2′-bi-1H-pyrrole compound (B) having formula (I) wherein R1 is hydrogen, phenyl, C1-C20 alkyl or C2-C20 alkenyl, wherein the alkyl and alkenyl groups are unsubstituted or substituted by 1 to 3 substituents, which are the same or different, chosen independently from halogen, C1-C6 alkoxy, hydroxy, aryl and aryloxy; R2 is hydrogen, C1-C6 alkyl, cyano, carboxy or (C1-C6 alkoxy)carbonyl; R3 is halogen, hydroxy or C1-C11 alkoxy unsubstitued or substituted by phenyl; R4 is hydrogen, C1-C6 alkyl or phenyl; each of R5 and R6, which are the same or different, is independently hydrogen, C2-C20 alkanoyl, C3-C20 alkenoyl, phenyl, C1-C20 alkyl or C2-C20 alkenyl; or two of R4, R5 and R6, taken together, form a C4-C12 polymethylene chain, which is unsubstituted or substituted by a C1-C12 alkyl, by a C2-C12 alkenyl or by a C1-C12 alkylidene group; or a pharmaceutically acceptable salt thereof; as a combined preparation for simultaneous, separate or sequential use in immunosuppressant therapy, said preparation having a potentiated immunosuppressive activity with respect to products containing either the immunosuppressive agent (A) or the 2,2′-bi-1H-pyrrole immunosuppressive compound (B).
摘要翻译：一种产品，其包含：（a）免疫抑制剂（A）和（b）至少一种具有式（I）的至少一种免疫抑制剂2,2'-双-1H-吡咯化合物（B），其中R 1是氢，苯基，C 1 -C 20 烷基或C 2 -C 20烯基，其中烷基和烯基是未取代的或被1至3个取代基取代，所述取代基相同或不同，独立地选自卤素，C 1 -C 6烷氧基，羟基，芳基和芳氧基; R2是氢，C1-C6烷基，氰基，羧基或（C1-C6烷氧基）羰基; R3是卤素，羟基或未取代或被苯基取代的C1-C11烷氧基; R4是氢，C1-C6烷基或苯基; R 5和R 6各自相同或不同，独立地为氢，C 2 -C 20烷酰基，C 3 -C 20链烯酰基，苯基，C 1 -C 20烷基或C 2 -C 20烯基; 一起形成C4-C12聚亚甲基链，其未被取代或被C 1 -C 12烷基取代，被C 2 -C 12烯基或C 1 -C 12亚烷基组成; 或其药学上可接受的盐; 作为用于免疫抑制剂治疗的同时，单独或顺序使用的组合制剂，所述制剂对于含有免疫抑制剂（A）或2,2'-双-1H-吡咯免疫抑制化合物（B）的产品具有增强的免疫抑制活性）。

4. 发明授权

US07776909B2 2-aryl-acetic acids, their derivatives and pharmaceutical compositions containing them 有权
标题翻译： 2-芳基乙酸，它们的衍生物和含有它们的药物组合物
公开(公告)号：US07776909B2
公开(公告)日：2010-08-17
申请号：US10541429
申请日：2004-02-04
申请人： Alessio Moriconi , Marcello Allegretti , Riccardo Bertini , Cinzia Bizzarri , Maria Candida Cesta , Francesco Colotta
发明人： Alessio Moriconi , Marcello Allegretti , Riccardo Bertini , Cinzia Bizzarri , Maria Candida Cesta , Francesco Colotta
IPC分类号： A61K31/40 , A61K31/18 , C07D207/333 , C07D207/325 , C07C311/51 , C07C311/32
CPC分类号： C07D207/337 , C07C57/30 , C07C57/58 , C07C311/09 , C07C311/21 , C07C311/51 , C07D209/26 , C07D209/42 , C07D295/13 , C07D471/04
摘要： Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2-membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
摘要翻译：选择的2-芳基乙酸，它们的衍生物和含有这些化合物的药物组合物可用于抑制由白细胞介素-8（IL-8）与CXCR1和CXCR2-膜受体相互作用诱导的嗜中性粒细胞（PMN白细胞）的趋化活化。所述化合物用于预防和治疗由所述活化引起的病理学。特别地，2（邻位）取代的芳基乙酸或其衍生物如酰胺和磺酰胺缺乏环加氧酶抑制活性，特别可用于治疗嗜中性粒细胞依赖性病理学如牛皮癣，溃疡性结肠炎，黑素瘤，慢性阻塞性肺疾病（COPD），大疱性类天疱疮，类风湿性关节炎，特发性纤维化，肾小球性肾炎，以及预防和治疗由缺血和再灌注引起的损伤。

5. 发明授权

US07560487B2 Use of (R)—ibuprofen methanesulfonamide and salts thereof in the treatment and prevention of rejection reactions of transplanted organs 有权
标题翻译：（R） - 布洛芬甲磺酰胺及其盐在治疗和预防移植器官排斥反应中的应用
公开(公告)号：US07560487B2
公开(公告)日：2009-07-14
申请号：US10250465
申请日：2003-01-30
申请人： Riccardo Bertini , Francesco Colotta , Roberto Novellini
发明人： Riccardo Bertini , Francesco Colotta , Roberto Novellini
IPC分类号： A61K31/195 , A61K31/16
CPC分类号： A61K31/216
摘要： The use of (R)-ibuprofen methanesulfonamide is described for the preparation of medicaments for the treatment and prevention of functional injury resulting from rejection reactions of transplanted organs.In particular, the use of non-toxic salts of (R)-ibuprofen methanesulfonamide, such as the (L)-lysine salt, is described for the prevention and the treatment of rejection reactions of transplanted kidneys.
摘要翻译：描述了（R） - 布洛芬甲磺酰胺的用途，用于制备用于治疗和预防由移植器官排斥反应引起的功能性损伤的药物。特别地，描述了（R） - 布洛芬甲磺酰胺（例如（L） - 赖氨酸盐）的无毒盐的用途，用于预防和治疗移植肾的排斥反应。

6. 发明申请

US20080045522A1 OMEGA-AMINOALKYLAMIDES OF R-2-ARYL-PROPIONIC ACIDS AS INHIBITORS OF THE CHEMOTAXIS OF POLYMORPHONUCLEATE AND MONONUCLEATE CELLS 审中-公开
标题翻译：作为聚马来酸酐和单核细胞化合物的化学抑制剂的R-2-ARYL-PROPIONIC的OMEGA-氨基甲酰胺
公开(公告)号：US20080045522A1
公开(公告)日：2008-02-21
申请号：US11838180
申请日：2007-08-13
申请人： Marcello ALLEGRETTI , Riccardo Bertini , Valerio Berdini , Cinzia Bizzarri , Maria Cesta , Vito Di Cioccio , Gianfranco Caselli , Francesco Colotta , Carmelo Gandolfi , Janete Gandolfi , Giulio Gandolfi , Maria Gandolfi , Arrigo Gandolfi
发明人： Marcello ALLEGRETTI , Riccardo Bertini , Valerio Berdini , Cinzia Bizzarri , Maria Cesta , Vito Di Cioccio , Gianfranco Caselli , Francesco Colotta , Carmelo Gandolfi , Janete Gandolfi , Giulio Gandolfi , Maria Gandolfi , Arrigo Gandolfi
IPC分类号： A61K31/165 , A61K31/192 , A61K31/435 , A61K31/445 , A61K31/4468 , A61K31/5375 , A61P17/06 , A61P9/00 , A61P9/10
CPC分类号： C07C233/51 , A61K31/165 , A61K31/198 , A61K31/445 , A61K31/4453 , A61K31/5375 , C07B2200/07 , C07C231/02 , C07C231/16 , C07C233/40 , C07C233/44 , C07C235/34 , C07C235/70 , C07C235/78 , C07C237/20 , C07C237/22 , C07C279/12 , C07C281/16 , C07D211/04 , C07D211/58 , C07D233/24 , C07D233/46 , C07D295/13 , C07D451/04
摘要： (R)-2-Arylpropionamide compounds of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear leukocytes (leukocytes PMN) and of monocytes at the inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use in the inhibition of the chemotaxis of neutrophils and monocytes induced by the C5a fraction of the complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of PMN leukocytes. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, rheumatoid arthritis and in the prevention and the treatment of injury caused by ischemia and reperfusion.
摘要翻译：描述了式（I）的（R）-2-芳基丙酰胺化合物。还描述了其制备方法及其制备药物。本发明的2-芳基丙酰胺可用于预防和治疗由于多发性白细胞（白细胞PMN）和单核细胞在炎症部位的加剧性募集引起的组织损伤。特别地，本发明涉及式（I）的2-芳基丙酸的ω-氨基烷基酰胺的R对映异构体，其用于抑制由补体的C5a部分诱导的嗜中性粒细胞和单核细胞的趋化性和其它其生物活性与7-TD受体激活相关的趋化蛋白。选择的式（I）化合物是C5a诱导的嗜中性粒细胞和单核细胞的趋化性和IL-8诱导的PMN白细胞趋化性的双重抑制剂。本发明的化合物用于治疗牛皮癣，溃疡性胆囊炎，肾小球肾炎，急性呼吸功能不全，特发性纤维化，类风湿性关节炎，以及预防和治疗由缺血和再灌注引起的损伤。

7. 发明申请

US20060247297A1 Chiral arylketones in the treatment of neutrophil-dependent inflammatory diseases 审中-公开
标题翻译：手性芳基酮治疗嗜中性粒细胞依赖性炎性疾病
公开(公告)号：US20060247297A1
公开(公告)日：2006-11-02
申请号：US10537824
申请日：2003-12-09
申请人： Marcello Allegretti , Riccardo Bertini , Cinzia Bizzarri , Maria Cesta , Francesco Colotta
发明人： Marcello Allegretti , Riccardo Bertini , Cinzia Bizzarri , Maria Cesta , Francesco Colotta
IPC分类号： A61K31/4035 , A61K31/381 , A61K31/366
CPC分类号： C07C69/738 , C07B2200/07 , C07C45/562 , C07C45/673 , C07C45/676 , C07C49/213 , C07C49/215 , C07C49/782 , C07C271/18 , C07C309/65 , C07C311/21 , C07C317/24 , C07D209/46 , C07D213/50 , C07D319/06 , C07F9/4059
摘要： The compounds of formula (I): where Ar is an aromatic ring and Ra, Rb, are as defined in the description, are useful in therapy as drugs for the treatment of diseases mediated by infiltrations of neutrophils induced by IL-8, such as psoriasis, rheumatoid arthritis, ulcerative cholitis and for the treatment of damages caused by ischemia and reperfusion.
摘要翻译：式（I）化合物：其中Ar是芳环，Ra，Rb如说明书中所定义，可用于治疗由IL-8诱导的嗜中性粒细胞浸润介导的疾病的药物，例如牛皮癣，类风湿性关节炎，溃疡性胆囊炎和治疗由缺血和再灌注引起的损伤。

8. 发明申请

US20050038119A1 2-Aryl-propionic acids and pharmaceutical compositions containing them 有权
标题翻译： 2-芳基 - 丙酸和含有它们的药物组合物
公开(公告)号：US20050038119A1
公开(公告)日：2005-02-17
申请号：US10495365
申请日：2002-11-19
申请人： Marcello Allegretti , Riccardo Bertini , Cinzia Bizzarri , Maria Cesta , Francesco Colotta
发明人： Marcello Allegretti , Riccardo Bertini , Cinzia Bizzarri , Maria Cesta , Francesco Colotta
IPC分类号： A61P1/04 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/255 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C20060101 , C07C57/30 , C07C57/32 , C07C57/38 , C07C57/42 , C07C57/46 , C07C57/50 , C07C57/58 , C07C59/135 , C07C59/48 , C07C59/68 , C07C211/56 , C07C229/42 , C07C307/02 , C07C307/10 , C07C309/00 , C07C309/65 , C07C309/67 , C07C309/73 , C07C311/00 , C07C311/08 , C07C311/09 , C07C311/21 , C07C317/44 , C07C311/42 , A61K31/34 , C07D307/02
CPC分类号： A61K31/192 , A61K31/196 , C07C57/30 , C07C57/38 , C07C57/42 , C07C57/46 , C07C57/58 , C07C59/135 , C07C59/48 , C07C229/42 , C07C307/02 , C07C307/10 , C07C309/65 , C07C309/67 , C07C309/73 , C07C311/08 , C07C311/09 , C07C311/21 , C07C317/44
摘要： (R) and (S) 2-Aryl-propionic acids, and pharmaceutical compositions that contain them, are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The acids are used for the prevention and treatment of pathologies deriving from said activation. In particular, the (R) enantiomers of said acids are lacking cyclo-oxygenase inhibition activity and are particularly useful in the tratment of neutrofil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bollous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
摘要翻译：（S）2-芳基 - 丙酸和含有它们的药物组合物可用于抑制白细胞介素-8（IL-8）与CXCR1和CXCR2的相互作用诱导的嗜中性粒细胞（PMN白细胞）的趋化活化膜受体。酸用于预防和治疗由所述活化引起的病理学。特别地，所述酸的（R）对映异构体缺乏环加氧酶抑制活性，并且特别可用于中和细胞依赖性病理学的研究，例如牛皮癣，溃疡性结肠炎，黑素瘤，慢性阻塞性肺病（COPD），浮肿性呼吸系统，类风湿关节炎，特发性纤维化，肾小球性肾炎，以及预防和治疗由缺血和再灌注引起的损伤。

9. 发明授权

US5981713A Antibodies to intereleukin-1 antagonists 失效
标题翻译：抗白细胞介素-1拮抗剂的抗体
公开(公告)号：US5981713A
公开(公告)日：1999-11-09
申请号：US910884
申请日：1997-08-13
申请人： Francesco Colotta , Marta Muzio , Alberto Mantovani
发明人： Francesco Colotta , Marta Muzio , Alberto Mantovani
IPC分类号： A61K38/00 , C07K14/54 , C12N15/12 , C07K16/18
CPC分类号： C07K14/54 , A61K38/00
摘要： A novel interleukin-1 antagonist active against both IL-1.alpha. and IL-1.beta. and DNA encoding same/re described. Antibodies specific for the novel IL-1 antagonist and prophylatic, therapeutic and diagnostic uses of the IL-1 antagonist in pathologies associated with IL-1 production are also described.
摘要翻译：一种对IL-1α和IL-1β有活性的新型白细胞介素-1拮抗剂和编码相同/重述的DNA。还描述了特异于新型IL-1拮抗剂的抗体和IL-1拮抗剂在与IL-1生成相关的病理学中的预防，治疗和诊断用途。

10. 发明申请

US20120004264A1 2-PHENYLPROPIONIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权
标题翻译： 2-苯基丙酸衍生物和含有它们的药物组合物
公开(公告)号：US20120004264A1
公开(公告)日：2012-01-05
申请号：US13234125
申请日：2011-09-15
申请人： Marcello Allegretti , Marla Candida Cesta , Riccardo Bertini , Marco Mosca , Francesco Colotta
发明人： Marcello Allegretti , Marla Candida Cesta , Riccardo Bertini , Marco Mosca , Francesco Colotta
IPC分类号： A61K31/4453 , A61K31/18 , A61P13/12 , A61P11/00 , A61P19/02 , A61P17/06 , A61K31/165 , A61K31/40
CPC分类号： C07C309/65 , C07C2601/08 , C07D295/13
摘要： 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
摘要翻译： 4-（三氟甲磺酰氧基苯基）丙酸衍生物和含有这些化合物的药物组合物可用于抑制由白细胞介素-8（IL-8）与CXCR1和CXCR2膜受体相互作用诱导的嗜中性粒细胞（PMN白细胞）的趋化活化。所述化合物用于预防和治疗由所述活化引起的病理学。值得注意的是，这些代谢物没有环加氧酶抑制活性，并且特别可用于治疗嗜中性粒细胞依赖性病理学如牛皮癣，溃疡性结肠炎，黑素瘤，慢性阻塞性肺病（COPD），大疱性类天疱疮，类风湿性关节炎，特发性纤维化，在预防和治疗由缺血和再灌注引起的损伤中的肾小球肾炎。

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