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公开(公告)号：US08999960B2
公开(公告)日：2015-04-07
申请号：US13122766
申请日：2009-10-01
申请人： Eyal Breitbart , Eti Kovalevski-Ishai , Erez Feige , Itzhak Mendel , Zeev Ziniuk , Gideon Halperin
发明人： Eyal Breitbart , Eti Kovalevski-Ishai , Erez Feige , Itzhak Mendel , Zeev Ziniuk , Gideon Halperin
IPC分类号： C07F9/10 , C07F9/165 , A61K31/661 , A61P37/06
CPC分类号： C07F9/10
摘要： Novel oxidized thiophospholipids are provided herein, as well as methods for producing same, and uses thereof in treating or preventing an inflammation associated with endogenous oxidized lipids and related conditions. Exemplary oxidized thiophospholipid according to embodiments described herein have the formula: wherein X1, X2, A1, A2, B′, B″, D′ and D″ are as described herein.
摘要翻译： 本文提供了新的氧化型硫代磷脂，以及其生产方法及其用于治疗或预防与内源性氧化脂质和相关病症相关的炎症的用途。 根据本文所述实施方案的示例性氧化硫磷脂具有下式：其中X1，X2，A1，A2，B'，B“，D'和D”如本文所述。
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公开(公告)号：US20110195937A1
公开(公告)日：2011-08-11
申请号：US13122766
申请日：2009-10-01
申请人： Eyal Breitbar , Eti Kovalevski-Ishai , Erez Feige , Itzhak Mendel , Zeev Ziniuk , Gideon Halperin
发明人： Eyal Breitbar , Eti Kovalevski-Ishai , Erez Feige , Itzhak Mendel , Zeev Ziniuk , Gideon Halperin
IPC分类号： A61K31/661 , C07F9/165 , A61P37/06
CPC分类号： C07F9/10
摘要： Novel oxidized thiophospholipids are provided herein, as well as methods for producing same, and uses thereof in treating or preventing an inflammation associated with endogenous oxidized lipids and related conditions. Exemplary oxidized thiophospholipid according to embodiments described herein have the formula: wherein X1, X2, A1, A2, B′, B″, D′ and D″ are as described herein.
摘要翻译： 本文提供了新的氧化型硫代磷脂，以及其生产方法及其用于治疗或预防与内源性氧化脂质和相关病症相关的炎症的用途。 根据本文所述实施方案的示例性氧化硫磷脂具有下式：其中X1，X2，A1，A2，B'，B“，D'和D”如本文所述。
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3.发明授权Oxidized lipids and uses thereof in the treatment of inflammatory diseases and disorders 有权氧化脂质及其在治疗炎性疾病和病症中的用途公开(公告)号：US07973023B2
公开(公告)日：2011-07-05
申请号：US12588371
申请日：2009-10-14
申请人： Dror Harats , Jacob George , Gideon Halperin , Itzhak Mendel , Niva Yacov , Eti Kovalevski-Ishai
发明人： Dror Harats , Jacob George , Gideon Halperin , Itzhak Mendel , Niva Yacov , Eti Kovalevski-Ishai
IPC分类号： A61K31/66
CPC分类号： C07F9/106 , A61K31/075 , A61K31/08 , A61K31/11 , A61K31/19 , A61K31/20 , A61K31/215 , A61K31/225 , A61K31/24 , A61K31/685 , C07C43/13 , C07C43/1785 , C07C43/1787 , C07F9/10 , Y02A50/411 , Y02A50/414
摘要： Novel synthetic oxidized lipids and methods utilizing oxidized lipids for treating and preventing an inflammation associated with an endogenous oxidized lipid are provided.
摘要翻译： 提供新型合成氧化脂质和利用氧化脂质治疗和预防与内源性氧化脂质相关的炎症的方法。
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4.发明申请METHODS EMPLOYING AND COMPOSITIONS CONTAINING DEFINED OXIDIZED PHOSPHOLIPIDS FOR PREVENTION AND TREATMENT OF ATHEROSCLEROSIS 有权含有定义氧化磷脂的方法和组合物用于预防和治疗甲状腺功能亢进公开(公告)号：US20110097350A1
公开(公告)日：2011-04-28
申请号：US12985365
申请日：2011-01-06
申请人： Dror HARATS , Jacob George , Gideon Halperin , Niva Yacov , Eti Kovalevski-Ishai
发明人： Dror HARATS , Jacob George , Gideon Halperin , Niva Yacov , Eti Kovalevski-Ishai
CPC分类号： C07F9/106 , A61K31/075 , A61K31/08 , A61K31/11 , A61K31/19 , A61K31/20 , A61K31/215 , A61K31/225 , A61K31/24 , A61K31/685 , C07C43/13 , C07C43/1785 , C07C43/1787 , C07F9/10 , Y02A50/411 , Y02A50/414
摘要： Novel synthetic forms of etherified oxidized phospholipids and methods of utilizing same for preventing and treating atherosclerosis and other related disorders, as well as inflammatory disorders, immune mediated diseases, autoimmune diseases and proliferative disorders, are provided. In addition, methods of synthesizing etherified and esterified oxidized phospholipids and of using same for preventing and treating atherosclerosis and other related disorders are also provided.
摘要翻译： 提供了醚化氧化磷脂的新型合成形式及其用于预防和治疗动脉粥样硬化和其它相关病症的方法，以及炎性疾病，免疫介导的疾病，自身免疫性疾病和增殖性疾病。 此外，还提供了合成醚化和酯化的氧化磷脂的方法以及用于预防和治疗动脉粥样硬化等相关疾病的方法。
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公开(公告)号：US09206206B2
公开(公告)日：2015-12-08
申请号：US13127717
申请日：2009-11-05
申请人： Eti Kovalevski-Ishai , Zeev Ziniuk , Gideon Halperin , Itzhak Mendel , Erez Feige , Niva Yacov , Eyal Breitbart
发明人： Eti Kovalevski-Ishai , Zeev Ziniuk , Gideon Halperin , Itzhak Mendel , Erez Feige , Niva Yacov , Eyal Breitbart
IPC分类号： C07C59/125 , C07C59/10 , A61K31/685 , A61K31/683 , A61K31/66 , C07F9/09 , C07F9/10
CPC分类号： C07F9/091 , C07C59/125 , C07F9/106
摘要： Novel oxidized lipids are provided herein, as well as methods for producing same, and uses thereof in treating or preventing an inflammation associated with endogenous oxidized lipids and related conditions.
摘要翻译： 本文提供了新的氧化脂质，以及其生产方法及其在治疗或预防与内源性氧化脂质和相关病症相关的炎症中的用途。
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公开(公告)号：US08563534B2
公开(公告)日：2013-10-22
申请号：US13431262
申请日：2012-03-27
申请人： Dror Harats , Jacob George , Gideon Halperin , Niva Yacov , Eti Kovalevski-Ishai
发明人： Dror Harats , Jacob George , Gideon Halperin , Niva Yacov , Eti Kovalevski-Ishai
IPC分类号： A61K31/66
CPC分类号： C07F9/106 , A61K31/075 , A61K31/08 , A61K31/11 , A61K31/19 , A61K31/20 , A61K31/215 , A61K31/225 , A61K31/24 , A61K31/685 , C07C43/13 , C07C43/1785 , C07C43/1787 , C07F9/10 , Y02A50/411 , Y02A50/414
摘要： Novel synthetic forms of etherified oxidized phospholipids and methods of utilizing same for preventing and treating atherosclerosis and other related disorders, as well as inflammatory disorders, immune mediated diseases, autoimmune diseases and proliferative disorders, are provided. In addition, methods of synthesizing etherified and esterified oxidized phospholipids and of using same for preventing and treating atherosclerosis and other related disorders are also provided.
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公开(公告)号：US20130079540A1
公开(公告)日：2013-03-28
申请号：US13672811
申请日：2012-11-09
IPC分类号： C07F9/09
摘要： Novel synthetic routes, which are highly applicable for industrial preparation of therapeutically beneficial oxidized phospholipids are disclosed. Particularly, novel methods for efficiently preparing compounds having a glycerolic backbone and one or more oxidized moieties attached to the glycerolic backbone, which are devoid of column chromatography are disclosed. Further disclosed are novel methods of introducing phosphorus-containing moieties such as phosphate moieties to compounds having glycerolic backbone and intermediates formed thereby. Further disclosed is substantially pure 1-hexadecyl-2-(4′-carboxy)butyl-sn-glycero-3-phosphocholine (CI-201).
摘要翻译： 公开了高度适用于治疗有益的氧化磷脂的工业制备的新型合成路线。 特别地，公开了用于有效制备具有连接到甘油主链上的甘油主链和一个或多个氧化部分的化合物的新方法，其没有进行柱层析。 进一步公开的是将含磷部分如磷酸酯部分引入具有甘油主链的化合物和由此形成的中间体的新方法。 进一步公开的是基本上纯的1-十六烷基-2-（4'-羧基）丁基-sn-甘油基-3-磷酸胆碱（CI-201）。
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8.发明授权Methods employing and compositions containing defined oxidized phospholipids for prevention and treatment of atherosclerosis 有权使用含有限定氧化磷脂的组合物用于预防和治疗动脉粥样硬化公开(公告)号：US08158611B2
公开(公告)日：2012-04-17
申请号：US12985365
申请日：2011-01-06
申请人： Dror Harats , Jacob George , Gideon Halperin , Niva Yacov , Eti Kovalevski-Ishai
发明人： Dror Harats , Jacob George , Gideon Halperin , Niva Yacov , Eti Kovalevski-Ishai
IPC分类号： A61K31/66 , C07C229/00
CPC分类号： C07F9/106 , A61K31/075 , A61K31/08 , A61K31/11 , A61K31/19 , A61K31/20 , A61K31/215 , A61K31/225 , A61K31/24 , A61K31/685 , C07C43/13 , C07C43/1785 , C07C43/1787 , C07F9/10 , Y02A50/411 , Y02A50/414
摘要： Novel synthetic forms of etherified oxidized phospholipids and methods of utilizing same for preventing and treating atherosclerosis and other related disorders, as well as inflammatory disorders, immune mediated diseases, autoimmune diseases and proliferative disorders, are provided. In addition, methods of synthesizing etherified and esterified oxidized phospholipids and of using same for preventing and treating atherosclerosis and other related disorders are also provided.
摘要翻译： 提供了醚化氧化磷脂的新型合成形式及其用于预防和治疗动脉粥样硬化和其它相关病症的方法，以及炎性疾病，免疫介导的疾病，自身免疫性疾病和增殖性疾病。 此外，还提供了合成醚化和酯化的氧化磷脂的方法以及用于预防和治疗动脉粥样硬化等相关疾病的方法。
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9.发明授权CRYSTAL FORMS III, IV, V, AND NOVEL AMORPHOUS FORM OF CLOPIDOGREL HYDROGENSULFATE, PROCESSES FOR THEIR PREPARATION, PROCESSES FOR THE PREPARATION OF FORM I, COMPOSITIONS CONTAINING THE NEW FORMS AND METHODS OF ADMINISTERING THE NEW FORMS 失效晶状体III，IV，V和新型非晶形态非晶形态，其制备方法，制备形式I的方法，包含新形式的组合物和管理新形式的方法公开(公告)号：US06767913B2
公开(公告)日：2004-07-27
申请号：US10074409
申请日：2002-02-12
申请人： Revital Lifshitz , Eti Kovalevski-Ishai , Shlomit Wizel , Sharon Avhar Maydan , Rami Lidor-Hadas
发明人： Revital Lifshitz , Eti Kovalevski-Ishai , Shlomit Wizel , Sharon Avhar Maydan , Rami Lidor-Hadas
IPC分类号： A61K3144
CPC分类号： C07D495/04
摘要： The present invention provides new crystalline Forms III, IV and V of clopidogrel hydrogensulfate and the amorphous form of clopidogrel hydrogensulfate, as well as their pharmaceutical compositions, and method of treatments with such compositions. The present invention also provides novel processes for preparation of clopidogrel hydrogensulfate Form I, Form III, Form IV, Form V and the amorphous form. The present invention further provides a novel process where the amorphous form is converted to Form I by contacting Form I with an ether.
摘要翻译： 本发明提供氯吡格雷硫酸氢盐和无定形形式的氯吡格雷硫酸氢盐的新结晶形式III，IV和V，以及它们的药物组合物，以及用这种组合物处理的方法。 本发明还提供了制备氯吡格雷硫酸氢盐形式I，形式III，形式IV，形式V和无定形形式的新方法。 本发明还提供了一种新的方法，其中通过使形式I与醚接触将无定形形式转化成晶型I.
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公开(公告)号：US08124800B2
公开(公告)日：2012-02-28
申请号：US12861921
申请日：2010-08-24
IPC分类号： C07F9/02
CPC分类号： C07B41/00 , C07C29/48 , C07C41/26 , C07C45/27 , C07C45/29 , C07C51/16 , C07C51/29 , C07C67/08 , C07C67/28 , C07C67/39 , C07F9/091 , C07F9/10 , C07F9/106 , Y02P20/55
摘要： Novel synthetic routes, which are highly applicable for industrial preparation of therapeutically beneficial oxidized phospholipids are disclosed. Particularly, novel methods for efficiently preparing compounds having a glycerolic backbone and one or more oxidized moieties attached to the glycerolic backbone, which are devoid of column chromatography are disclosed. Further disclosed are novel methods of introducing phosphorous-containing moieties such as phosphate moieties to compounds having glycerolic backbone and intermediates formed thereby.
摘要翻译： 公开了高度适用于治疗有益的氧化磷脂的工业制备的新型合成路线。 特别地，公开了用于有效制备具有连接到甘油主链上的甘油主链和一个或多个氧化部分的化合物的新方法，其没有进行柱层析。 进一步公开的是将含有磷的部分例如磷酸酯部分引入具有甘油主链的化合物和由其形成的中间体的新方法。
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