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1. 发明申请

US20110130555A1 LIPID-POLYMER CONJUGATES, THEIR PREPARATION AND USES THEREOF 审中-公开
标题翻译：脂质聚合物共混物，其制备及其用途
公开(公告)号：US20110130555A1
公开(公告)日：2011-06-02
申请号：US12997014
申请日：2010-05-11
申请人： Saul Yedgar , Yuval Cohen , Joseph V. Bondi
发明人： Saul Yedgar , Yuval Cohen , Joseph V. Bondi
IPC分类号： C08B37/10 , C08B37/08 , C08B37/00
CPC分类号： A61K47/544 , A61K31/727 , A61K31/728 , A61K47/61
摘要： This invention provides low molecular weight lipid-GAG and phospholipids-GAG conjugates and methods of use thereof in suppressing, inhibiting, preventing, or treating a pathogenic effect on a cell, including, inter alia, infection with intracellular pathogens.
摘要翻译：本发明提供低分子量脂质GAG和磷脂-GAG缀合物及其在抑制，抑制，预防或治疗对细胞的致病作用的用途的方法，包括特别是细胞内病原体的感染。

2. 发明申请

US20080113935A1 Use of lipid conjugates in the treatment of diseases or disorders of the eye 有权
标题翻译：使用脂质偶联物治疗眼睛疾病或病症
公开(公告)号：US20080113935A1
公开(公告)日：2008-05-15
申请号：US11984223
申请日：2007-11-14
申请人： Saul Yedgar , Yuval Cohen
发明人： Saul Yedgar , Yuval Cohen
IPC分类号： A61K31/727 , A61K31/685 , A61K31/715 , A61K31/717 , A61P27/02 , A61K31/718 , A61K31/726
CPC分类号： A61K31/661 , A61K9/0048 , A61K31/685 , A61K31/715 , A61K31/717 , A61K31/718 , A61K31/726 , A61K31/727 , A61K47/544 , A61K47/56 , A61K47/61 , Y02A50/401
摘要： In one embodiment, the invention provides a method of treating, reducing the incidence, reducing the severity or pathogenesis of an eye disease or disorder in a subject, including, inter alia, retinal detachment, macular degeneration, glaucoma or retinopathy, comprising the step of administering an effective amount of a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof. This invention also provides a contact lens solution comprising a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.
摘要翻译：在一个实施方案中，本发明提供了治疗，降低发病率，降低受试者眼睛疾病或病症的严重性或发病机理的方法，包括尤其是视网膜脱离，黄斑变性，青光眼或视网膜病变，包括以下步骤：通过酯或酰胺键将有效量的任选地通过间隔基连接到生理上可接受的单体，二聚体，低聚物或聚合物的脂质或磷脂部分，和/或其药学上可接受的盐或药物产品。本发明还提供一种隐形眼镜溶液，其包含通过间隔基任选地通过酯或酰胺键与生理学上可接受的单体，二聚体，低聚物或聚合物结合的脂质或磷脂部分和/或其药学上可接受的盐或其药物产物。

3. 发明授权

US08865681B2 Use of lipid conjugates in the treatment of diseases or disorders of the eye 有权
标题翻译：使用脂质偶联物治疗眼睛疾病或病症
公开(公告)号：US08865681B2
公开(公告)日：2014-10-21
申请号：US11984223
申请日：2007-11-14
申请人： Saul Yedgar , Yuval Cohen
发明人： Saul Yedgar , Yuval Cohen
IPC分类号： A61K31/715 , A61K31/727 , A61K31/717 , A61K31/726 , A61K31/718 , A61K47/48 , A61K9/00 , A61K31/685
CPC分类号： A61K31/661 , A61K9/0048 , A61K31/685 , A61K31/715 , A61K31/717 , A61K31/718 , A61K31/726 , A61K31/727 , A61K47/544 , A61K47/56 , A61K47/61 , Y02A50/401
摘要： In one embodiment, the invention provides a method of treating, reducing the incidence, reducing the severity or pathogenesis of an eye disease or disorder in a subject, including, inter alia, retinal detachment, macular degeneration, glaucoma or retinopathy, comprising the step of administering an effective amount of a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof. This invention also provides a contact lens solution comprising a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.
摘要翻译：在一个实施方案中，本发明提供了治疗，降低发病率，降低受试者眼睛疾病或病症的严重性或发病机理的方法，包括尤其是视网膜脱离，黄斑变性，青光眼或视网膜病变，包括以下步骤：通过酯或酰胺键将有效量的任选地通过间隔基连接到生理上可接受的单体，二聚体，低聚物或聚合物的脂质或磷脂部分，和/或其药学上可接受的盐或药物产品。本发明还提供一种隐形眼镜溶液，其包含通过间隔基任选地通过酯或酰胺键与生理学上可接受的单体，二聚体，低聚物或聚合物结合的脂质或磷脂部分和/或其药学上可接受的盐或其药物产物。

4. 发明申请

US20080113002A1 Contact lens compositions 审中-公开
标题翻译：隐形眼镜组合物
公开(公告)号：US20080113002A1
公开(公告)日：2008-05-15
申请号：US11984224
申请日：2007-11-14
申请人： Saul Yedgar , Yuval Cohen
发明人： Saul Yedgar , Yuval Cohen
IPC分类号： A61K9/00 , A61P27/00
CPC分类号： A61K9/0048 , A61K9/0051 , A61K31/685 , A61K31/715 , A61K31/717 , A61K31/718 , A61K31/726 , A61K31/727 , A61K47/544 , A61K47/61 , G02B1/043
摘要： In one embodiment, the invention provides a contact lens comprising a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.
摘要翻译：在一个实施方案中，本发明提供了一种隐形眼镜，其包含通过间隔基任选地通过酯或酰胺键与生理学上可接受的单体，二聚体，低聚物或聚合物结合的脂质或磷脂部分和/或其药学上可接受的盐或药物其产品。

5. 发明授权

US08383787B2 Use of lipid conjugates in the treatment of diseases 有权
标题翻译：使用脂质偶联物治疗疾病
公开(公告)号：US08383787B2
公开(公告)日：2013-02-26
申请号：US13031990
申请日：2011-02-22
申请人： Saul Yedgar
发明人： Saul Yedgar
IPC分类号： C07H5/04
CPC分类号： C08B37/0069 , A61K31/728 , A61K31/737 , A61K47/544 , A61K47/61 , C08B37/0072
摘要： This invention provides compounds represented by the structure of the general formula (A): wherein L is a lipid or a phospholipid, Z is either nothing, ethanolamine, serine, inositol, choline, or glycerol, Y is either nothing or a spacer group ranging in length from 2 to 30 atoms, X is a physiologically acceptable monomer, dimer, oligomer, or polymer, wherein X is a glycosaminoglycan; and n is a number from 1 to 1000, wherein any bond between L, Z, Y and X is either an amide or an esteric bond.
摘要翻译：本发明提供由通式（A）的结构表示的化合物：其中L为脂质或磷脂，Z为无，乙醇胺，丝氨酸，肌醇，胆碱或甘油，Y为无或间隔基范围长度为2至30个原子，X为生理上可接受的单体，二聚体，低聚物或聚合物，其中X为糖胺聚糖; n为1〜1000的数，L，Z，Y和X之间的任意键为酰胺键或酯键。

6. 发明申请

US20100317591A1 USE OF LIPID CONJUGATES IN THE TREATMENT OF DISEASES 有权
标题翻译：在治疗疾病中使用脂质偶联物
公开(公告)号：US20100317591A1
公开(公告)日：2010-12-16
申请号：US12820161
申请日：2010-06-22
申请人： Saul Yedgar
发明人： Saul Yedgar
IPC分类号： A61K31/726 , A61K31/728 , A61K31/737 , A61K31/727 , A61P17/00 , A61P17/06 , A61P17/08 , A61P29/00
CPC分类号： A61K47/544
摘要： This invention provides a method of treating a subject suffering from a dermatologic condition, including, inter alia, psoriasis, contact dermatitis, and seboreic dermatitis, the method includes the step of administering to a subject a compound comprising a lipid or phospholipid moiety bound to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof, in an amount effective to treat the subject suffering from a dermatologic condition.
摘要翻译：本发明提供了一种治疗患有皮肤病症状的个体的方法，其中包括尤其是牛皮癣，接触性皮炎和皮脂炎性皮炎，所述方法包括向受试者施用包含与生理上可接受的单体，二聚体，低聚物或聚合物，和/或其药学上可接受的盐或其药物产品，其量有效地治疗患有皮肤病学病症的受试者。

7. 发明授权

US07034006B2 Use of lipid conjugates in the treatment of disease 有权
公开(公告)号：US07034006B2
公开(公告)日：2006-04-25
申请号：US09756765
申请日：2001-01-10
申请人： Saul Yedgar , David Shuseyov , Gershon Golomb , Reuven Reich , Isaac Ginsburg , Abd-al-Roof Higazi , Moshe Ligumski , Miron Krimsky , David Ojcius , Benito Antonio Yard , Fokko Johannes van der Woude , Edit Schnitzer
发明人： Saul Yedgar , David Shuseyov , Gershon Golomb , Reuven Reich , Isaac Ginsburg , Abd-al-Roof Higazi , Moshe Ligumski , Miron Krimsky , David Ojcius , Benito Antonio Yard , Fokko Johannes van der Woude , Edit Schnitzer
IPC分类号： A61K31/70 , A61K31/715 , C08B37/08 , C08B37/10 , C07H5/06
CPC分类号： A61K47/544
摘要： The invention provides novel methods for treating disease based upon the medicinal use of lipids and phospholipids covalently bound to physiologically acceptable monomers or polymers. Phosphatidylethanolamine moieties conjugated to physiologically acceptable monomers and polymers (PE conjugates) manifest an unexpectedly wide range of pharmacological effects, including stabilizing cell membranes; limiting oxidative damage to cell and blood components; limiting cell proliferation, cell extravasation and (tumor) cell migratory behavior; suppressing immune responses; and attenuating physiological reactions to stress, as expressed in elevated chemokine levels. The surprisingly manifold pharmacological properties of the PL-conjugates allow for the invention, disclosed herein, of novel methods for the treatment of a diverse range of disease states, including obstructive respiratory disease, including asthma; colitis and Crohn's disease; central nervous system insult, including blood brain barrier compromise, ischemic stroke, and multiple sclerosis; contact dermatitis; psoriasis; cardiovascular disease, including ischemic conditions and prophylaxis for invasive vascular procedures; cellular proliferative disorders, including anti-tumor vasculogenesis, invasiveness, and metastases; anti-oxidant therapy; hemolytic syndromes; sepsis; acute respiratory distress syndrome; tissue transplant rejection syndromes; autoimmune disease; viral infection; and hypersensitivity conjunctivitis. The therapeutic methods of the invention include administration of phosphatidylethanolamine bound to carboxymethylcellulose, heparin, hyaluronic acid, polyethylene glycol, and hemaccel. Disclosed herein are also new compounds comprised of phospholipid moieties bound to low molecular weight monomers and dimers, including mono- and disaccharides, carboxylated disaccharides, mono- and dicarboxylic acids, salicylates, bile acids, and fatty acids.

8. 发明申请

US20050203054A1 Use of lipid conjugates in the treatment of diseases 失效
标题翻译：使用脂质偶联物治疗疾病
公开(公告)号：US20050203054A1
公开(公告)日：2005-09-15
申请号：US10952496
申请日：2004-09-29
申请人： Saul Yedgar
发明人： Saul Yedgar
IPC分类号： A61K31/685 , A61K31/715 , A61K31/727 , A61K31/737 , A61K31/739 , A61K38/16
CPC分类号： A61K47/61 , A61K47/544
摘要： This invention provides compounds represented by the structure of the general formula (A): wherein L is a lipid or a phospholipid, Z is either nothing, ethanolamine, serine, inositol, choline, or glycerol, Y is either nothing or a spacer group ranging in length from 2 to 30 atoms, X is a physiologically acceptable monomer, dimer, oligomer, or polymer, wherein X is a glycosaminoglycan; and n is a number from 1 to 1000, wherein any bond between L, Z, Y and X is either an amide or an esteric bond.
摘要翻译：本发明提供由通式（A）的结构表示的化合物：其中L为脂质或磷脂，Z为无，乙醇胺，丝氨酸，肌醇，胆碱或甘油，Y为无或间隔基范围长度为2至30个原子，X为生理上可接受的单体，二聚体，低聚物或聚合物，其中X为糖胺聚糖; n为1〜1000的数，L，Z，Y和X之间的任意键为酰胺键或酯键。

9. 发明授权

US10179106B2 Liposomes comprising polymer-conjugated lipids and related uses 有权
公开(公告)号：US10179106B2
公开(公告)日：2019-01-15
申请号：US14115869
申请日：2012-05-10
申请人： Saul Yedgar
发明人： Saul Yedgar
IPC分类号： A61K9/127 , A61K31/713 , A61K47/48
摘要： The present invention provides liposomes comprising a lipid bilayer and a polymer-conjugated lipid, wherein said polymer-conjugated lipid is incorporated into said lipid bilayer. The present invention also provides methods of producing the liposomes as well as a method of delivering a nucleic acid to a subject comprising the step of administering said nucleic acid encapsulated in a mixed liposome, a method for performing diagnostic imaging in a subject, comprising the step of administering a diagnostic agent encapsulated in a mixed liposome, and methods for treating, inhibiting, or suppressing a pathological condition in a subject comprising administering to said subject a mixed liposome.

10. 发明授权

US09040078B2 Use of lipid conjugates in the treatment of diseases of the nervous system 有权
标题翻译：使用脂质偶联物治疗神经系统疾病
公开(公告)号：US09040078B2
公开(公告)日：2015-05-26
申请号：US10919523
申请日：2004-08-17
申请人： Saul Yedgar
发明人： Saul Yedgar
IPC分类号： A61K47/48
CPC分类号： A61K47/48053 , A61K47/544
摘要： The invention provides a method for treating a subject suffering from a disease of the central nervous system which is associated with an inflammatory response, including, inter alia, multiple sclerosis, Amyotrophic Lateral Sclerosis (ALS), meningitis, Alzheimer's disease, pain, HIV-associated dementia, stroke, traumatic brain injury, encephalomyelitis, chronic inflammatory demyelinating polyneuropathy, cerebral ischemia-induced injury or any combination thereof. This invention further provides for the use of a conjugate, or composition comprising the same, for treating the subject, wherein the conjugate comprises a lipid or phospholipid moiety bonded to a physiologically acceptable monomer, dimer, oligomer, or polymer.
摘要翻译：本发明提供了一种治疗患有与炎性反应相关的中枢神经系统疾病的受试者的方法，其特别包括多发性硬化症，肌萎缩性侧索硬化症（ALS），脑膜炎，阿尔茨海默病，疼痛，HIV- 相关的痴呆，中风，创伤性脑损伤，脑脊髓炎，慢性炎症性脱髓鞘性多发性神经病，脑缺血诱发的损伤或其任何组合。本发明进一步提供了用于治疗受试者的缀合物或包含其的组合物的用途，其中所述缀合物包含与生理上可接受的单体，二聚体，低聚物或聚合物结合的脂质或磷脂部分。

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