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1. 发明授权

US08759320B2 Process for the preparation of trivalent iron complexes with mono-, di- and polysaccharide sugars 有权
标题翻译：用单糖，二糖和多糖制备三价铁络合物的方法
公开(公告)号：US08759320B2
公开(公告)日：2014-06-24
申请号：US11908575
申请日：2006-03-14
申请人： Stefania Sacchi , Mauro Montorsi , Egidio Marchi
发明人： Stefania Sacchi , Mauro Montorsi , Egidio Marchi
IPC分类号： C07H1/00 , C08B30/18 , C08B31/00 , C08B37/02
CPC分类号： C07H23/00 , C07H1/00 , C08B30/18 , C08B31/00 , C08B37/0021
摘要： Process for the preparation of trivalent iron complexes with mono-, di- and polysaccharide sugars, consisting of the activation of the sugar by oxidation with nascent bromine generated in situ by reaction between an alkaline or alkaline earth bromine and an alkaline hypochlorite, the complexation of the activated sugar in solution with a ferric salt dissolved in an aqueous solution, the purification of the resulting solution through ultrafiltration and finally the stabilization of the trivalent iron-sugar complex by heating at a temperature between 60° C. and 100° C. for a period between 1 and 4 hours at a pH between 9.0 and 11.0.
摘要翻译：用单糖，二糖和多糖制备三价铁络合物的方法，其由通过碱性或碱性碱性溴和碱性次氯酸盐之间的反应原位产生的用新生溴氧化而激活糖组成，其络合在溶液中的活性糖与溶解在水溶液中的铁盐，通过超滤纯化所得溶液，最后通过在60℃和100℃之间的温度加热来稳定三价铁 - 糖络合物，以获得在9.0和11.0之间的pH为1至4小时之间。

2. 发明授权

US5639744A Bile acids derivatives useful in the therapy of the biliary calculosis from cholesterol and of the pathologies caused by cholestasis 失效
标题翻译：胆汁酸衍生物可用于治疗由胆固醇引起的胆汁淤积症和胆汁淤积引起的病理学
公开(公告)号：US5639744A
公开(公告)日：1997-06-17
申请号：US416155
申请日：1995-04-04
申请人： Egidio Marchi , Maria Rita Milani , Silvano Piani , Aldo Roda , Gianfranco Cainelli
发明人： Egidio Marchi , Maria Rita Milani , Silvano Piani , Aldo Roda , Gianfranco Cainelli
IPC分类号： C07J43/00 , A61K31/58
CPC分类号： C07J43/003
摘要： An amide of formula ##STR1## and its pharmacologically acceptable organic or inorganic salt shows a metabolic stability, both enteric and hepatic, greater than that of the corresponding bile acids conjugated with glycine or taurine physiologically present in the enterohepatic circulation. The pharmacological activity of the compounds of formula I or their pharmacologically acceptable organic or inorganic salt makes the use effective for the therapy of biliary calculosis from cholesterol and in every pathology caused by cholestasis like chronic hepatitis from cholestasis, primitive biliary cirrhosis and juvenile hepatopathy associated with cystic fibrosis.
摘要翻译：式Ⅰ的酰胺及其药理学上可接受的有机或无机盐显示出与肠肝循环中生理上存在的甘氨酸或牛磺酸结合的相应胆汁酸的代谢稳定性，包括肠和肝的代谢稳定性。式I化合物或其药理学上可接受的有机或无机盐的药理活性使其有效用于治疗胆固醇和胆汁淤积引起的每一种胆汁淤积症，如胆汁淤积症，慢性肝炎，原始胆汁性肝硬化和与青少年肝病有关的少年肝病囊性纤维化。

3. 发明授权

US5430133A Semi-synthetic glycosaminoglycans with heparin or heparan structure of .alpha.-L-iduronic-2-O-sulfate acid modified in position 2 失效
标题翻译：具有肝素或乙酰肝素结构的半合成糖胺聚糖在位置2修饰的α--L-艾杜糖醛酸-2-硫酸酯酸
公开(公告)号：US5430133A
公开(公告)日：1995-07-04
申请号：US46248
申请日：1993-04-13
申请人： Silvano Piani , Egidio Marchi , Gianfranco Tamagnone , Fabrizio Ungarelli
发明人： Silvano Piani , Egidio Marchi , Gianfranco Tamagnone , Fabrizio Ungarelli
IPC分类号： C08B37/10 , C08B37/00 , A61K31/725
CPC分类号： C08B37/0075
摘要： New heparin and heparan sulfate derivatives having antithrombotic activity, also endowed with reduced haemorrhagic and anticoagulant activity, are obtained by nucleophilic addition to heparin and heparan sulfate derivatives containing 2,3-anhydrogulonic acid residues. The compounds have the formula IV ##STR1## The glycosaminoglycan derivatives obtained through this treatment show a structural modification in the unit of .alpha.-L-iduronic acid 2-O-sulfate with the partial or total selective substitution of the O-sulfate group in position 2 with a nucleophilic residue. The structural modifications produce an improvement of the biological properties of the heparin and heparan sulfate, substantially keeping the antithrombotic activity while diminishing the haemorragic effect in vivo and the anticoagulant activity in vitro.
摘要翻译：具有抗血栓形成活性的新型肝素和硫酸乙酰肝素衍生物，具有减少的出血和抗凝血活性，通过亲和加入含有2,3-脱水瓜来酸残留物的肝素和硫酸乙酰肝素衍生物获得。该化合物具有式IV通过该处理获得的糖胺聚糖衍生物以α-L-异杜酸2-氧硫酸盐为单位的结构改性，部分或全部选择性用亲核残基取代位置2的硫酸盐基团。结构修饰产生了肝素和硫酸乙酰肝素的生物学性质的改善，基本上保持了抗血栓形成活性，同时降低了体内的血液效应和抗凝血活性。

4. 发明申请

US20080207558A1 Process for the Preparation of Trivalent Iron Complexes with Mono-, Di- and Polysaccharide Sugars 有权
标题翻译：用单糖，二糖和多糖糖制备三价铁配合物的方法
公开(公告)号：US20080207558A1
公开(公告)日：2008-08-28
申请号：US11908575
申请日：2006-03-14
申请人： Stefania Sacchi , Mauro Montorsi , Egidio Marchi
发明人： Stefania Sacchi , Mauro Montorsi , Egidio Marchi
IPC分类号： A61K31/7016 , C08B37/00 , C08B37/02 , C07H23/00 , C13K7/00 , A61K31/721 , C13K5/00
CPC分类号： C07H23/00 , C07H1/00 , C08B30/18 , C08B31/00 , C08B37/0021
摘要： Process for the preparation of trivalent iron complexes with mono-, di- and polysaccharide sugars, consisting of the activation of the sugar by oxidation with nascent bromine generated in situ by reaction between an alkaline or alkaline earth bromine and an alkaline hypochlorite, the complexation of the activated sugar in solution with a ferric salt dissolved in an aqueous solution, the purification of the resulting solution through ultrafiltration and finally the stabilization of the trivalent iron-sugar complex by heating at a temperature between 60° C. and 100° C. for a period between 1 and 4 hours at a pH between 9.0 and 11.0.
摘要翻译：用单糖，二糖和多糖制备三价铁络合物的方法，其由通过碱性或碱性碱性溴和碱性次氯酸盐之间的反应原位产生的用新生溴氧化而激活糖组成，其络合在溶液中的活性糖与溶解在水溶液中的铁盐，通过超滤纯化所得溶液，最后通过在60℃和100℃之间的温度加热来稳定三价铁 - 糖络合物，以获得在9.0和11.0之间的pH为1至4小时之间。

5. 发明授权

US5686432A Use of some glycosaminoglycans in the peritoneal dialysis 失效
标题翻译：在腹膜透析中使用一些糖胺聚糖
公开(公告)号：US5686432A
公开(公告)日：1997-11-11
申请号：US530597
申请日：1995-09-19
申请人： Bruno Baggio , Giorgio Bazzato , Agostino Fracasso , Giovanni Gambaro , Egidio Marchi , Gianfranco Tamagnone
发明人： Bruno Baggio , Giorgio Bazzato , Agostino Fracasso , Giovanni Gambaro , Egidio Marchi , Gianfranco Tamagnone
IPC分类号： A61K31/726 , A61K31/727 , A61K31/737 , A61K31/73 , A61K31/725
CPC分类号： A61K35/38 , A61K31/726 , A61K31/727 , A61K31/737
摘要： The use of some glycosaminoglycans like sulodexide, low molecular weight heparin and low molecular weight dermatan sulfate and of the medicines by parenteral use that contain them in the treatment of patients suffering from chronic renal insufficiency subjected to peritoneal dialysis is described. The effectiveness of this use has been shown both by pharmacological studies carried out in nephrectomized rats to whom a peritoneal damage has been caused and by clinical studies carried out in patients suffering from chronic renal insufficiency subjected to CAPD and treated by intraperitoneal route (i.p.) with 2 ml vials of VESSEL DUE F.RTM. containing 50 mg of sulodexide. A significant increase of the peritoneal transports of urea and of creatinine joined to a significant decrease of the protein-loss in the peritoneal effluent has been observed. Significant changes of the ultrafiltration capacity and of haemorrhagic-coagulative complications have not been observed during the study.
摘要翻译：描述了一些糖胺聚糖如顺铂，低分子量肝素和低分子量硫酸皮肤素以及通过肠胃外使用的药物，用于治疗患有腹膜透析的慢性肾功能不全的患者。已经通过在已经引起腹膜损伤的肾切除大鼠中进行的药理学研究和通过腹膜内途径（ip）治疗的患有慢性肾功能不全的患者进行临床研究，并通过腹膜内途径（ip）治疗， 2毫升含有50毫克sulodexide的VESSEL DUE F TM小瓶。已经观察到尿素和肌酸酐的腹膜转运的显着增加与腹膜流出物中蛋白质损失的显着降低相关。研究期间没有观察到超滤能力和出血性凝血并发症的显着变化。

6. 发明授权

US4341785A Imidazo-rifamycin derivatives with antibacterial utility 失效
标题翻译：咪唑利利霉素衍生物具有抗菌效用
公开(公告)号：US4341785A
公开(公告)日：1982-07-27
申请号：US262123
申请日：1981-05-11
申请人： Egidio Marchi , Lauretta Montecchi
发明人： Egidio Marchi , Lauretta Montecchi
IPC分类号： A61K31/435 , A61P31/04 , C07D498/22 , A61K31/44 , C07D491/22
CPC分类号： C07D498/22
摘要： New rifamicyn derivatives of the following general formula ##STR1## wherein: A may be the structure ##STR2## --x-- is a chemical bond or nil; R is hydrogen or acetylR.sub.1 and R.sub.2 independently represent hydrogen, (C.sub.1-4) alkyl, benzyloxy, mono- and di-(C.sub.1-3)alkylamino- (C.sub.1-4)alkyl, (C.sub.1-3)alkoxy- (C.sub.1-4)alkyl, hydroxymethyl, hydroxy-(C.sub.2-4)-alkyl, nitro or R.sub.1 and R.sub.2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two methyl or ethyl groups; R.sub.3 is a hydrogen atom or nil;with the proviso that, when A is A.sub.1, --x-- is nil and R.sub.3 is a hydrogen atom; with the further proviso that, when A is A.sub.2, --x-- is a chemical bond and R.sub.3 is nil.The compounds possess antibacterial utility.
摘要翻译：下列通式的新的rifamicyn衍生物 I其中：A可以是化学键或nil的结构。 R为氢或乙酰基，R 1和R 2独立地表示氢，（C 1-4）烷基，苄氧基，单 - 和二 - （C 1-3）烷基氨基 - （C 1-4）烷基，（C 1-3）烷氧基 - （C1- 4）烷基，羟甲基，羟基 - （C 2-4） - 烷基，硝基或R 1和R 2与吡啶核的两个连续碳原子一起形成任选被一个或两个甲基或乙基取代的苯环; R3是氢原子或无; 条件是当A为A1时，-x-为无，R3为氢原子; 进一步的条件是当A为A2时，-x-为化学键，R3为零。该化合物具有抗菌效用。

7. 发明授权

US4200573A Derivatives of 3-carboxyrifamycin S and SV and process for their preparation 失效
标题翻译： 3-羧基化霉素S和SV的衍生物及其制备方法
公开(公告)号：US4200573A
公开(公告)日：1980-04-29
申请号：US968409
申请日：1978-12-11
申请人： Mario Brufani , Egidio Marchi , Pierfranco Bellomo , Giuseppe Mascellani
发明人： Mario Brufani , Egidio Marchi , Pierfranco Bellomo , Giuseppe Mascellani
IPC分类号： A61K31/395 , A61P31/04 , C07D498/08 , C07D491/08 , A61K31/33
CPC分类号： C07D498/08
摘要： New compounds being derivatives of 3-carboxyrifamycin S and SV are prepared by oxidation of cyanohydrin of 3-formylrifamycin S to 3-(cyanocarbonyl)rifamycin S, condensation with a compound of formula HR (an alcohol, an amine or an substituted hydrazine) and, optionally, reduction of the derivative of 3-carboxyrifamycin S so obtained to the corresponding SV form. Alternatively 3-(cyanocarbonyl)rifamycin S may be converted to the SV form before condensing with the compound HR.
摘要翻译：通过将3-甲酰基叶绿素S的氰醇氧化成3-（氰基羰基）利福霉素S，与式HR化合物（醇，胺或取代的肼）缩合制备3-氧化碳霉素S和SV的衍生物的新化合物和任选地，将如此获得的3-羧基化霉素S的衍生物还原成相应的SV形式。或者，3-（氰基羰基）利福霉素S可以在与化合物HR冷凝之前转化成SV形式。

8. 发明授权

US08828967B2 Low molecular weight complexes between iron and maltobionic acid, use thereof for intramuscular or subcutaneous administration in the treatment of anemic states, and new pharmaceutical compositions adapted for these uses 有权
标题翻译：铁和麦芽糖二酸之间的低分子量配合物，其用于在治疗贫血状态下用于肌内或皮下施用，以及适用于这些用途的新药物组合物
公开(公告)号：US08828967B2
公开(公告)日：2014-09-09
申请号：US13703111
申请日：2011-06-08
申请人： Michele Autuori , Dario Bosi , Alessandro Lapini Sacchetti , Egidio Marchi
发明人： Michele Autuori , Dario Bosi , Alessandro Lapini Sacchetti , Egidio Marchi
IPC分类号： A01N43/04 , A61K31/715 , C07H15/04 , C07H23/00
CPC分类号： C07H23/00 , C07H15/04
摘要： New low molecular weight complexes between iron and maltobionic acid that can be administered parenterally, preferably intramuscularly or subcutaneously, in the treatment of anemic states, caused by iron deficiencies, and new pharmaceutical compositions adapted for this use. In particular, the invention provides a new complex between preferably trivalent iron and maltobionic acid that is characterized by a molecular weight Mw between 10,000 and 30,000 Da, by a polydispersity of 1.0-1.8 and by an iron content between 25% and 40% by weight.
摘要翻译：铁和麦芽二酸之间的新的低分子量复合物，其可以肠胃外，优选肌内或皮下施用于治疗由铁缺乏引起的贫血状态，以及适用于该用途的新药物组合物。特别地，本发明提供了优选三价铁和麦芽二酸之间的新配合物，其特征在于10,000至30,000Da的分子量Mw，多分散性为1.0-1.8，铁含量为25重量％至40重量％。

9. 发明授权

US5496807A Method of treatment of diabetic nephropathy by means of sulodexide of medicines containing it 失效
标题翻译：通过含有它的药物的sulodexide治疗糖尿病肾病的方法
公开(公告)号：US5496807A
公开(公告)日：1996-03-05
申请号：US227502
申请日：1994-04-14
申请人： Egidio Marchi , Gianfranco Tamagnone
发明人： Egidio Marchi , Gianfranco Tamagnone
IPC分类号： C08B37/00 , A61K20060101 , A61K31/69 , A61K31/70 , A61K31/715 , A61K31/726 , A61K35/38 , A61P3/08 , A61P3/10 , A61P13/02 , A61P15/00
CPC分类号： A61K31/726 , A61K31/727 , A61K31/737 , A61K35/38
摘要： The use of sulodexide, a glycosaminoglycan of natural origin extracted from mammalian intestinal mucosa, and of medicines containing it in the treatment of patients suffering from nephropathy of diabetic origin constitutes the object of the present invention. The effectiveness of sulodexide has been shown by the significative decrease of the albuminuria in microalbuminuric and macroalbuminuric diabetic patients treated with pharmaceutical compositions administered by oral or intramuscular route containing therapeutically effective amounts of drug.
摘要翻译：使用从哺乳动物肠粘膜提取的天然来源的糖胺聚糖和含有它的药物用于治疗患有糖尿病来源的患者的患者的用途构成了本发明的目的。通过含有治疗有效量的药物的口服或肌内途径给药的药物组合物治疗的微量白蛋白尿和大量白蛋白尿糖尿病患者中的白蛋白尿的显着降低已经证明了sulodexide的有效性。

10. 发明授权

US5446152A Heterocyclic compounds active in gastro-intestinal pathologies 失效
标题翻译：在胃肠道病理学中活跃的杂环化合物
公开(公告)号：US5446152A
公开(公告)日：1995-08-29
申请号：US223697
申请日：1994-04-06
申请人： Claudia Baldazzi , Silvano Piani , Maria Barbanti , Egidio Marchi
发明人： Claudia Baldazzi , Silvano Piani , Maria Barbanti , Egidio Marchi
IPC分类号： A61K31/505 , A61K31/517 , A61K31/535 , A61K31/536 , A61P1/08 , C07D239/88 , C07D239/90 , C07D243/14 , C07D265/22 , C07D413/06
CPC分类号： C07D239/90 , C07D265/22
摘要： This invention refers to heterocyclic compounds of general formula ##STR1## and their pharmacologically accepted salts. The derivatives described in this invention are active in the gastro-intestinal apparatus; in particular, they have prokinetic effects, in other words they create specific stimulation on gastro-intestinal motility, facilitating the passage of the contents of the alimentary tract, and possess anti-emetic qualities, without side effects involving the central nervous system.
摘要翻译：本发明涉及通式为Ⅰ的杂环化合物及其药理学上可接受的盐。本发明描述的衍生物在胃肠器具中是有活性的; 特别是具有促进作用，换句话说，它们对胃肠蠕动产生特异性刺激，促进消化道内容物通过，具有抗呕吐品质，而不会引起中枢神经系统的副作用。

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