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1.发明授权
公开(公告)号：US5514659A
公开(公告)日：1996-05-07
申请号：US230921
申请日：1994-04-21
IPC分类号： C07H3/08 , A61K31/70 , A61K31/702 , A61K31/7028 , A61K31/726 , A61K31/737 , A61P7/02 , C07H3/04 , C07H3/06 , C07H3/10 , C07H11/00 , C07H13/04 , C07H13/08 , C07H15/04 , A61K31/725
摘要： The invention relates to 3-deoxy oligosaccharides of formula I: ##STR1## in which X represents an --OSO.sub.3.sup.- radical, a radical of formula R--O, a radical of formula: ##STR2## or a radical of formula: ##STR3## Y represents a radical of formula: ##STR4## R represents an alkyl radical, R.sub.1, R.sub.3, R.sub.5, R.sub.7, R.sub.8, R.sub.10, R.sub.12 and R.sub.13 represent a hydroxyl radical, an alkoxy radical or an --OSO.sub.3.sup.- radical,R.sub.2, R.sub.4, R.sub.6, R.sub.9 and R.sub.11 represent a hydrogen atom, a hydroxyl radical, an alkoxy radical or an --OSO.sub.3.sup.- radical, with the proviso that at least R.sub.2 or R.sub.4 or R.sub.6 or R.sub.9 or R.sub.11 represents a hydrogen atom,and their pharmaceutically acceptable salts with a base.
摘要翻译： 本发明涉及式I的3-脱氧低聚糖：其中X代表-OSO 3 - 基，式RO基团，式：基团或下式基团： > Y表示式的基团：R 1表示烷基，R 1，R 3，R 5，R 7，R 8，R 10，R 12和R 13表示羟基，烷氧基或-OSO 3 - 基，R 2，R 4 ，R 6，R 9和R 11表示氢原子，羟基，烷氧基或-OSO 3 - 基，条件是至少R 2或R 4或R 6或R 9或R 11表示氢原子，及其药学上可接受的盐 与一个基地。
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公开(公告)号：US4841041A
公开(公告)日：1989-06-20
申请号：US217997
申请日：1988-07-12
IPC分类号： C07H13/12 , A61K31/70 , A61K31/7024 , A61K31/7028 , A61P7/02 , C07H3/06 , C07H11/00 , C07H13/06 , C07H15/04 , C08B37/00
CPC分类号： C07H11/00 , C07H3/06 , C08B37/0078
摘要： The present invention is dealing with new pentasaccharides of the formula I: ##STR1## These pentasaccharides have anti-thrombotic activity and especially they possess potent anti-Xa activity, inactivate thrombin via HC-II, but do not inactivate thrombin via AT-III.The invention also refers to new tetrasaccharides which may be used as intermediates in the synthesis of the above pentasaccharides.
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公开(公告)号：US5705489A
公开(公告)日：1998-01-06
申请号：US690449
申请日：1996-08-05
IPC分类号： C07H7/033 , A61K20060101 , A61K31/70 , A61K31/7012 , A61K47/48 , A61P7/02 , A61P43/00 , C07H20060101 , C07H3/06 , C07H7/04 , C07H11/00 , C07H13/00 , C07H15/04 , C07H15/08 , C07H15/18 , C07H15/22 , C07H15/26 , C07K9/00 , C08B37/00 , C08B37/10 , C07H15/00
摘要： The invention relates to a tuneable bisconjugate comprising two saccharides and a spacer, each saccharide being the same or different and comprising two to six monosaccharide units, at least one unit being uronic acid, characterized in that at least one of the saccharides per se has anti-thrombotic activity, and that the spacer connects at least one saccharide to the other through its non-reducing end, the chain length of the spacer being 20-120 atoms.
摘要翻译： 本发明涉及包含两种糖类和间隔物的可调式双缀合物，每种糖相同或不同，并且包含两至六个单糖单元，至少一个单元是糖醛酸，其特征在于，至少一种糖本身具有抗 并且间隔物通过其非还原性末端将至少一个糖连接到另一个，间隔物的链长为20-120个原子。
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4.发明授权Sulfated glycosaminoglycanoid derivatives of the heparin and heparan sulfate type 失效硫酸盐型糖胺聚糖衍生物肝素和硫酸乙酰肝素型
公开(公告)号：US5543403A
公开(公告)日：1996-08-06
申请号：US325841
申请日：1994-10-19
IPC分类号： C07H11/00 , C07H15/04 , A61K31/715 , A61K31/725 , C07H5/10 , C08B37/10
摘要： The invention relates to sulfated glycosaminoglycanoid derivatives of the heparin and heparan sulfate type, of which N-sulfate, N-acetate, and hydroxy groups, are replaced by alkoxy, aryloxy, aralkoxy, or O-sulfate groups. The compounds have antithrombotic and smooth muscle cell proliferation inhibiting activities.
摘要翻译： 本发明涉及肝素和硫酸乙酰肝素型的硫酸化糖胺聚糖衍生物，其中N-硫酸盐，N-乙酸酯和羟基被烷氧基，芳氧基，芳烷氧基或O-硫酸酯基取代。 该化合物具有抗血栓形成和平滑肌细胞增殖抑制活性。
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5.发明授权
公开(公告)号：US5529985A
公开(公告)日：1996-06-25
申请号：US333448
申请日：1994-11-02
CPC分类号： A61K31/715 , C08B37/0069
摘要： The invention relates to sulfated glycosaminoglycanoid derivatives of the dermatan sulfate and chondroitin sulfate type, of which N-sulfate, N-acetate, and hydroxy groups, are replaced by alkoxy, aryloxy, aralkoxy, or O-sulfate groups. The compounds have antithrombotic and smooth muscle cell proliferation inhibiting activities.
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6.发明授权Sulfated glycosaminoglycanoid derivatives of the dermatan sulfate and chondroitin sulfate type 失效硫酸皮肤素和硫酸软骨素类型的硫酸化糖胺聚糖衍生物
公开(公告)号：US5382570A
公开(公告)日：1995-01-17
申请号：US919683
申请日：1992-07-27
摘要： The invention relates to sulfated glycosaminoglycanoid derivatives of the dermatan sulfate and chondroitin sulfate type, of which N-sulfate, N-acetate, and hydroxy groups, are replaced by alkoxy, aryloxy, aralkoxy, or O-sulfate groups. The compounds have antithrombotic and smooth muscle cell proliferation inhibiting activities.
摘要翻译： 本发明涉及硫酸皮肤素和硫酸软骨素类型的硫酸化糖胺聚糖衍生物，其中N-硫酸盐，N-乙酸酯和羟基被烷氧基，芳氧基，芳烷氧基或O-硫酸酯基取代。 该化合物具有抗血栓形成和平滑肌细胞增殖抑制活性。
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7.发明授权Sulfated glycosaminoglycanoid derivatives of the heparin and heparan sulfate type 失效硫酸盐型糖胺聚糖衍生物肝素和硫酸乙酰肝素型
公开(公告)号：US5378829A
公开(公告)日：1995-01-03
申请号：US919684
申请日：1992-07-27
IPC分类号： C07H11/00 , C07H15/04 , A61K31/715
摘要： The invention relates to sulfated glycosaminoglycanoid derivatives of the heparin and heparin sulfate type, of which N-sulfate, N-acetate, and hydroxy groups, are replaced by alkoxy, aryloxy, aralkoxy, or O-sulfate groups. The compounds have antithrombotic and smooth muscle cell proliferation inhibiting activities.
摘要翻译： 本发明涉及肝素和硫酸肝素型的硫酸化糖胺聚糖衍生物，其中N-硫酸盐，N-乙酸酯和羟基被烷氧基，芳氧基，芳烷氧基或O-硫酸酯基取代。 该化合物具有抗血栓形成和平滑肌细胞增殖抑制活性。
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公开(公告)号：US09556215B2
公开(公告)日：2017-01-31
申请号：US14126776
申请日：2012-06-18
申请人： Ahmed El Hadri , Maurice Petitou
发明人： Ahmed El Hadri , Maurice Petitou
CPC分类号： C07H3/06 , A61K31/702 , A61K38/1709 , C07H5/04 , C07H11/00 , C07H15/26
摘要： The invention concerns a pentasaccharide compound of formula (I) and the salts thereof. The invention also concerns a pharmaceutical composition comprising the synthetic pentasaccharide compound of formula (I) and its salts. The invention further concerns these compounds for use as a medicament, and in particular intended to treat blood clotting disorders, to prevent ischaemia reperfusion injury associated with solid organ transplantation, or to reduce the risk of blood clotting in an extracorporeal blood circuit during cardiac surgery, extracorporeal membrane oxygenation, or during circulatory assistance such as artificial heart.
摘要翻译： 本发明还涉及包含式（I）的合成五糖化合物及其盐的药物组合物。 本发明还涉及用作药物的这些化合物，特别是旨在治疗血液凝固病症，防止与实体器官移植相关的局部缺血再灌注损伤或降低心脏手术期间体外血液循环中血液凝固的风险， 体外膜氧合，或循环辅助如人造心脏。
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公开(公告)号：US20100081708A1
公开(公告)日：2010-04-01
申请号：US12444198
申请日：2007-10-05
IPC分类号： A61K31/7088 , C07H21/04 , A61P7/02
摘要： The present invention is concerned with anticoagulants (i.e. substances that stop blood from clotting). More specifically, the present invention is concerned with orally available antithrombic oligosaccharides.
摘要翻译： 本发明涉及抗凝剂（即阻止血液凝固的物质）。 更具体地说，本发明涉及口服抗凝血寡糖。
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10.再颁专利
公开(公告)号：USRE35770E
公开(公告)日：1998-04-14
申请号：US574761
申请日：1995-12-19
IPC分类号： C08B37/00 , A61K31/725 , C08B37/10
CPC分类号： C08B37/0078 , G01N2333/8128 , G01N2400/40
摘要： Oligosaccharides obtainable from heparin including heparinic constituents of molecular weights ranging from 2000 to 50,000. Said fractions have a Yin-Wessler titer and a USP titer in a ratio of at least 30. They consist of chains constituted by no more than 8 saccharidic moities. They possess a strong antithrombotic activity and are then useful as antithrombotic drugs.
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