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1. 发明授权

US5264425A Glycosaminoglycan salts and pharmaceutical compositions containing them 失效
标题翻译：糖胺聚糖盐和含有它们的药物组合物
公开(公告)号：US5264425A
公开(公告)日：1993-11-23
申请号：US623378
申请日：1990-11-15
申请人： Alma Dal Pozzo , Maurizio Acquasaliente , Giancarlo Sportoletti , Monique Sarret , Paolo Ferruti , Francesco De Santis
发明人： Alma Dal Pozzo , Maurizio Acquasaliente , Giancarlo Sportoletti , Monique Sarret , Paolo Ferruti , Francesco De Santis
IPC分类号： C07C233/36 , A61K20060101 , A61K31/715 , A61P3/06 , A61P7/02 , C07C20060101 , C07C211/63 , C07C219/02 , C07C229/06 , C07C237/00 , C07C237/04 , C07C237/10 , C07C271/06 , C07C271/20 , C07C275/04 , C07C275/14 , C08B20060101 , C08B37/00 , C08B37/10 , A61K31/725 , A61K31/73 , C07C69/96
CPC分类号： C08B37/0075 , C08B37/0069
摘要： Salts of glycosaminoglycans (heparin, its fractions or fragments which are supersulfated, dermatan sulfate, heparan sulfate, and modified heparins) with bases of formula (I), ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 represent H, alkyl, or cycloalkyl; R.sub.5 and R.sub.6 represent H, or alkyl; R.sub.7 and R.sub.8 represent H or alkyl; n and m are integers from 1-4 and X is --O--CO--O--, which salts have the pharmacological properties of the glycosaminoglycans themselves, and are orally and rectally administrable.
摘要翻译： PCT No.PCT / EP89 / 00605 Sec。 371日期1990年11月15日 102（e）1990年11月15日日期PCT提交1989年5月30日PCT公布。公开号WO90 / 12589 1990年11月1日。具有式（I）的碱的糖胺聚糖（肝素，其过硫酸盐，硫酸皮肤素，硫酸乙酰肝素和修饰的肝素）的片段，其中R1，R2， R3和R4代表H，烷基或环烷基; R5和R6代表H或烷基; R 7和R 8表示H或烷基; n和m是1-4的整数，X是-O-CO-O-，这些盐具有糖胺聚糖本身的药理学性质，并且是口服和直肠给药的。

2. 发明授权

US4405643A Treatment of acute pulmonary edema with arginine esters 失效
标题翻译：用精氨酸酯治疗急性肺水肿
公开(公告)号：US4405643A
公开(公告)日：1983-09-20
申请号：US296830
申请日：1981-08-27
申请人： Giancarlo Sportoletti , Alessandro Baglioni
发明人： Giancarlo Sportoletti , Alessandro Baglioni
IPC分类号： A61K31/22 , A61P3/00 , A61P7/02 , A61P7/10 , A61P9/00 , A61P11/00 , A61P37/08
CPC分类号： A61K31/22 , Y10S514/87
摘要： Pharmaceutical compositions for use in the relief of acute pulmonary edema, different types of shock including anaphylactic shock, shock induced by bacterial endotoxins, and hyperfibrinolysis induced by substances which activate plasminogen, consist of solutions of an ester of L-arginine with an aliphatic alcohol in water at a pH between 5.5 and 8.5. The compositions may be provided in unit dosage form containing 0.25-100 mg of active substance per kilogram of body weight of the subject in need of treatment and are administered through the parenteral route. The esters may be provided in the form of a salt with a pharmaceutically acceptable organic or inorganic acid. The esters may be with methyl or ethyl alcohol. The compositions are more effective than aspirin and aprotinin.
摘要翻译：用于缓解急性肺水肿的药物组合物，不同类型的休克，包括过敏性休克，由细菌内毒素引起的休克，以及激活纤溶酶原的物质引起的超纤维蛋白溶解，由L-精氨酸与脂肪醇的酯溶液组成 pH在5.5和8.5之间的水。组合物可以以每公斤体重需要治疗的受试者含有0.25-100mg活性物质的单位剂型提供，并且通过肠胃外途径施用。酯可以以药学上可接受的有机酸或无机酸的形式提供。酯可以与甲基或乙醇一起使用。组合物比阿司匹林和抑肽酶更有效。

3. 发明授权

US4507205A Process for the purification of glucosaminoglucans 失效
标题翻译：葡聚糖葡聚糖纯化方法
公开(公告)号：US4507205A
公开(公告)日：1985-03-26
申请号：US237880
申请日：1981-02-25
申请人： Pietro Cremonesi , Giancarlo Sportoletti
发明人： Pietro Cremonesi , Giancarlo Sportoletti
IPC分类号： C08B37/10 , B01D13/00
CPC分类号： C08B37/0075
摘要： A process for the removal of components having low or no anticoagulant activity from a glucosaminoglucan is described which comprises subjecting said glucosaminoglucan in the form of a salt in an aqueous solution to flow across a membrane suitable for ultrafiltration, hyperfiltration (inverse osmosis) or dialysis with partial passage through said membrane, whereby fractions of low activity go through the membrane and fractions of higher activity do not go through the membrane and are concentrated. The membrane suitable for ultrafiltration may have a nominal molecular cut-off between 1000 and 15,000. The membrane suitable for dialysis may have a nominal molecular cut-off at less than 30,000. The glucosaminoglucan may be heparin in the form of the sodium or calcuium salt.
摘要翻译：描述了从葡糖淀粉葡聚糖中除去具有低或不具有抗凝血活性的成分的方法，其包括使所述水溶液中盐形式的葡糖胺葡聚糖流过适于超滤，超滤（反渗透）或透析的膜部分通过所述膜，其中低活性部分通过膜，较高活性的级分不通过膜并且被浓缩。适用于超滤的膜可能具有1000至15,000之间的标称分子截止值。适用于透析的膜可能具有小于30,000的标称分子截止值。葡糖胺葡聚糖可以是钠或钙盐形式的肝素。

4. 发明授权

US4282217A Pharmaceutical compositions containing a corticosteroid substance 失效
标题翻译：含有皮质类固醇物质的药物组合物
公开(公告)号：US4282217A
公开(公告)日：1981-08-04
申请号：US162686
申请日：1980-06-25
申请人： Alessandro Baglioni , Giancarlo Sportoletti
发明人： Alessandro Baglioni , Giancarlo Sportoletti
IPC分类号： A61K31/22 , A61K31/57 , A61P9/00 , A61P43/00 , C07J5/00 , A61K31/56
CPC分类号： A61K31/57 , Y10S514/921
摘要： Pharmaceutical compositions containing a corticosteroid and an ester of L-arginine with an aliphatic alcohol exhibit a synergistic effect in the protection against shock. The corticosteroid may be 6-.alpha.-methylprednisolone-21-hemisuccinate sodium salt and the L-arginine ester may be the methyl ester in the form of the hydrochloride salt.
摘要翻译：含有皮质类固醇和L-精氨酸与脂肪醇的酯的药物组合物在防止休克中具有协同效应。皮质类固醇可以是6-甲基强的松龙-21-半琥珀酸钠盐，L-精氨酸酯可以是盐酸盐形式的甲酯。

5. 发明授权

US4717719A Modified glucosaminoglucans having antithrombotic activity 失效
标题翻译：具有抗血栓活性的改性葡糖胺葡萄糖
公开(公告)号：US4717719A
公开(公告)日：1988-01-05
申请号：US572448
申请日：1984-01-20
申请人： Giancarlo Sportoletti , Piergiuseppe Pagella , Pietro Cremonesi
发明人： Giancarlo Sportoletti , Piergiuseppe Pagella , Pietro Cremonesi
IPC分类号： C08B37/10 , A61K20060101 , A61K31/715 , A61P7/02 , C08B20060101 , A61K31/725
CPC分类号： A61K31/715 , Y10S514/822 , Y10S514/824
摘要： Pharmaceutical compositions are described which have antithrombotic activity suitable for the prevention and for the therapy of cardiac infarcts, cerebral infarcts and venous thrombosis. They contain as the active component a fraction of heparin which has been modified by nitrogen desulfatation and succinylation, which fraction contains less than 10% of the N-sulfate groups of the heparin starting material and more than 0.6 succinyl radicals per disaccharide unit. The method of treatment is described.
摘要翻译：描述了具有适合于预防和治疗心肌梗死，脑梗死和静脉血栓形成的抗血栓形成活性的药物组合物。它们作为活性成分含有已被氮脱硫和琥珀酰化修饰的肝素的一部分，该级分含有少于10％的肝素起始物质的N-硫酸盐基团，每个二糖单元含有多于0.6个琥珀酰基。描述了治疗方法。

6. 发明授权

US5110918A Process for preparing EDTA-free heparins, heparin fractions and fragments 失效
$Process for preparing EDTA-free heparins, heparin fractions and fragments$
标题翻译：制备不含EDTA的肝素，肝素级分和片段的方法
公开(公告)号：US5110918A
公开(公告)日：1992-05-05
申请号：US587605
申请日：1990-09-24
申请人： Benito Casu , Annamaria Naggi , Pasqua Oreste , Giangiacomo Torri , Giorgio Zoppetti , Giancarlo Sportoletti , Francesco De Santis
发明人： Benito Casu , Annamaria Naggi , Pasqua Oreste , Giangiacomo Torri , Giorgio Zoppetti , Giancarlo Sportoletti , Francesco De Santis
IPC分类号： C08B37/10 , A61K31/715 , A61P7/02 , C08B37/00
CPC分类号： C08B37/0075
摘要： Heparins, heparin fractions or fragments, optionally salified with pharmaceutically acceptable cations, having molecular weight ranging from 1.000 to 30.000 D, characterized by an EDTA content lower than 0.1%, by the absence, in the .sup.1 H--NMR spectra, of the signals due to EDTA between 2.50 and 4.00 p.p.m. and substantially free from bleeding effect and optionally free from signals, in the .sup.13 C--NMR spectrum, from 80 to 86 ppm.
摘要翻译：盐酸，肝素级分或片段，任选地与药学上可接受的阳离子盐化，其分子量范围为1.000至30.000D，其特征在于EDTA含量低于0.1％，在1H-NMR谱中不存在由于 EDTA在2.50和4.00 ppm之间并且在13 C-NMR光谱中基本上没有出血作用并且任选地没有信号，从80至86ppm。

7. 发明授权

US4789681A Cytoprotective guanidine derivatives useful in ischemic diseases 失效
标题翻译：用于缺血性疾病的细胞保护胍衍生物
公开(公告)号：US4789681A
公开(公告)日：1988-12-06
申请号：US944949
申请日：1986-12-22
申请人： Giancarlo Sportoletti , Pietro Cremonesi , Moniquet Sarret
发明人： Giancarlo Sportoletti , Pietro Cremonesi , Moniquet Sarret
IPC分类号： A61K31/195 , A61K31/215 , A61K31/22 , A61K31/33 , A61K31/415 , A61P9/00 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , C07C67/00 , C07C239/00 , C07C279/14 , C07D233/44 , C07D233/52 , C07D233/88
CPC分类号： C07D233/88
摘要： Compounds of the general formula I ##STR1## wherein R.sub.1 is hydrogen or methyl;R.sub.2 and R.sub.3, which are the same or different, represent hydrogen or methyl, or taken together, form the amidine system to which an imidazole or imidazoline ring is bound;R.sub.4 is a linear or branched C.sub.1 -C.sub.10 alkyl group; cycloalkyl, aryl, aralkyl or hetaryl group;R.sub.5 is hydrogen or methyl;A is a propylene chain optionally substituted by one or two methyl groups in one or more of the positions thereof; a chain of formula --HN--CH.sub.2 --CH.sub.2 -- or of formula --N.dbd.CH--CH.sub.2 --; a 1,4-cyclohexylene group optionally substituted by one or more methyl groups; a 1,4- phenylene group optionally substituted by one or more halogen atoms, alkyl groups or C.sub.1 -C.sub.4 alkoxy group with the proviso that, when R.sub.4 is methyl or ethyl and R.sub.1 =R.sub.2 =R.sub.3 =R.sub.5 are hydrogen, A is different from an unsubstituted propylene chain, are therapeutically useful as antilischemic, cytoprotective and cardioprotective agents.
摘要翻译：通式I的化合物（Ⅰ）其中R1是氢或甲基; R2和R3相同或不同，表示氢或甲基，或一起形成咪唑或咪唑啉环结合的脒体系; R4是直链或支链C1-C10烷基; 环烷基，芳基，芳烷基或杂芳基; R5是氢或甲基; A是在其一个或多个位置中任选被一个或两个甲基取代的丙烯链; 式-HN-CH2-CH2-或式-N = CH-CH2-的链; 任选被一个或多个甲基取代的1,4-亚环己基; 任选被一个或多个卤素原子，烷基或C 1 -C 4烷氧基取代的1,4-亚苯基，条件是当R 4为甲基或乙基且R 1 = R 2 = R 3 = R 5为氢时，A不同于未取代的丙烯链可用作抗缺血，细胞保护和心脏保护剂。

8. 发明授权

US4493829A Bio-available succinylated protein-iron derivatives which do not cause gastric lesions, method of preparation and related pharmaceutical compounds 失效
标题翻译：生物可利用的不引起胃损伤的琥珀酰化蛋白 - 铁衍生物，制备方法和相关药物化合物
公开(公告)号：US4493829A
公开(公告)日：1985-01-15
申请号：US469282
申请日：1983-02-24
申请人： Giancarlo Sportoletti , Piergiuseppe Pagella , Pietro Cremonesi
发明人： Giancarlo Sportoletti , Piergiuseppe Pagella , Pietro Cremonesi
IPC分类号： C07K1/02 , A61K35/14 , A61K35/20 , A61K35/407 , A61K35/54 , A61K36/00 , A61K36/48 , A61K36/896 , A61K38/00 , A61K38/16 , A61P7/06 , C07F15/02 , C07K1/107 , C07K1/113 , C07K1/30 , C07K14/00 , C07K14/415 , C07K14/47 , C07K14/76 , C07K14/77 , C07G7/04
CPC分类号： C07K14/415 , C07K1/1077 , C07K14/47 , C07K14/77 , A61K38/00 , Y10S530/832 , Y10S530/846
摘要： The invention relates to succinylated proteins, with a degree of succinylation of between 20 to 100%, containing from 0.1 to 20% by weight of iron, obtained by treating succinylated proteins with iron salts in suitable pH ranges. The compounds in question, which are completely tolerated, are characterized by an optimum bioavailability of iron.
摘要翻译：本发明涉及琥珀酰化的蛋白质，其琥珀酰化程度为20至100％，含有0.1至20重量％的铁，其通过在合适的pH范围内用铁盐处理琥珀酰化的蛋白质而获得。所述化合物是完全耐受的，其特征在于铁的最佳生物利用度。

9. 发明授权

US06734298B1 Cross-linking process of carboxylated polysaccharides 有权
标题翻译：羧化多糖的交联过程
公开(公告)号：US06734298B1
公开(公告)日：2004-05-11
申请号：US09830744
申请日：2001-06-18
申请人： Rolando Barbucci , Giancarlo Sportoletti
发明人： Rolando Barbucci , Giancarlo Sportoletti
IPC分类号： C08B3700
CPC分类号： A61K8/731 , A61Q19/00 , C08B15/005 , C08B31/006 , C08B37/0072 , C08B37/0084
摘要： A process for the preparation of cross-linked polysaccharides containg carboxy groups. The process comprises a first step of activating the carboxy groups in an anhydrous aprotic solvent and then reacting with a polyamine. The cross-linked polysaccharide may be subjected to sulfonation of the five hydroxy groups.
摘要翻译：一种制备包含羧基的交联多糖的方法。该方法包括在无水非质子溶剂中活化羧基然后与多胺反应的第一步骤。交联的多糖可以进行五个羟基的磺化。

10. 发明授权

US4409103A Method for the preparation of calcium heparinate 失效
标题翻译：方法制备肝素钙
公开(公告)号：US4409103A
公开(公告)日：1983-10-11
申请号：US176861
申请日：1980-08-11
申请人： Pietro Cremonesi , Giancarlo Sportoletti
发明人： Pietro Cremonesi , Giancarlo Sportoletti
IPC分类号： C08B37/10 , B01D13/00
CPC分类号： C08B37/0075
摘要： A process for the preparation of the calcium salt of heparin containing an amount of sodium by weight not in excess of 0.1% and containing an amount of calcium by weight not less than 9.5% is described, which comprises subjecting a solution of sodium heparinate to dialysis, hyperfiltration (inverse osmosis) or ultrafiltration by means of a semi-permeable membrane and isolating the calcium heparinate with anticoagulant activity essentially equal to the anticoagulant activity of the sodium heparinate. For the ultrafiltration, a membrane may be used in the form of a planar sheet or a membrane in the form of a spiral or "needle" having a molecular nominal cut-off at 20,000 Dalton. For the hyperfiltration (inverse osmosis), a membrane may be used having a rejection of sodium ion between 0 and 75%. For the dialysis, a membrane may be used in the form of multiple sheets or a coiled tube or hollow fibers. A plurality of dialyzers in series or in parallel is used. The process may be carried out continuously or discontinuously.
摘要翻译：描述了一种制备含有不超过0.1％重量的钠含量不超过9.5％的肝素钙盐的方法，其包括使肝素钠溶液透析，通过半透膜超滤（反渗透）或超滤，并分离具有基本上等于肝素钠的抗凝血活性的抗凝血活性的肝素钙。对于超滤，膜可以以螺旋形式的平面片或膜的形式使用，或者具有20,000道尔顿的分子标称截止值的“针”形式。对于超滤（反渗透），可以使用具有0至75％的钠离子排斥的膜。对于透析，膜可以以多张片或螺旋管或中空纤维的形式使用。使用多个串联或并联的透析器。该过程可以连续地或不连续地进行。

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