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1. 发明申请

WO2006119168A2 USE OF CAROTENOIDS AND/OR CAROTENOID DERIVATIVES/ANALOGS FOR REDUCTION/INHIBITION OF CERTAIN NEGATIVE EFFECTS OF COX INHIBITORS 审中-公开
标题翻译：用于减少/抑制COX抑制剂某些负面影响的CAROTENOIDS和/或CAROTENOID衍生物/模拟物
公开(公告)号：WO2006119168A2
公开(公告)日：2006-11-09
申请号：PCT/US2006016590
申请日：2006-05-02
申请人： HAWAII BIOTECH INC , LOCKWOOD SAMUEL F , MASON R PRESTON
发明人： LOCKWOOD SAMUEL F , MASON R PRESTON
CPC分类号： A61K31/415 , A61K31/015 , A61K31/196 , A61K31/522 , A61K45/06 , A61K2300/00
摘要： Administering carotenoids, and in particular xanthophyll carotenoids, or analogs or derivatives of astaxanthin, lutein, zeaxanthin, lycoxanthin, lycophyll, or lycopene to a subject undergoing treatment with COX-2 inhibitor drugs may reduce at least a portion of the adverse side effects associated with administration of COX-2 selective inhibitor drugs. The carotenoids, or analogs or derivatives thereof may be administered to a subject prior to, at the same time as, or after the commencement of COX-2 selective inhibitor drug therapy. The carotenoids, or analogs or derivatives thereof may be administered to a subject concurrently with COX-2 selective inhibitor drugs therapy. The carotenoids, or analogs or derivatives thereof may be incorporated into pharmaceutical preparation in combination with the COX-2 selective inhibitor drug or may be administered separately. Administration of the analogs or derivatives described herein may reduce peroxidation of LDL and other lipids in the serum and plasma cell membranes of subjects undergoing COX-2 selective inhibitor drug therapy. Administration of the analogs or derivatives described herein may reduce the incidence of deleterious clinical cardiovascular events undergoing COX-2 selective inhibitor drug therapy.
摘要翻译：将类胡萝卜素，特别是叶黄素类胡萝卜素或虾青素，叶黄素，玉米黄质，lycoxanthin，番茄红素或番茄红素的类似物或衍生物施用于用COX-2抑制剂药物治疗的受试者可以减少至少一部分与给予COX-2选择性抑制药物。类胡萝卜素或其类似物或衍生物可以在COX-2选择性抑制剂药物治疗开始之前，同时或之后施用于受试者。类胡萝卜素或其类似物或衍生物可以与COX-2选择性抑制剂药物治疗同时给予受试者。类胡萝卜素或其类似物或衍生物可以与COX-2选择性抑制剂药物组合引入药物制剂中，或者可以分开施用。本文所述的类似物或衍生物的施用可以减少经历COX-2选择性抑制剂药物治疗的受试者的血清和浆细胞膜中LDL和其它脂质的过氧化。本文所述的类似物或衍生物的给药可以降低经历COX-2选择性抑制剂药物治疗的有害临床心血管事件的发生率。

2. 发明申请

WO2006039685A3 METHODS FOR SYNTHESIS OF CHIRAL INTERMEDIATES OF CAROTENOIDS, CAROTENOID ANALOGS, AND CAROTENOID DERIVATIVES 审中-公开
标题翻译：合成CAROTENOIDS，CAROTENOID ANALOGS和CAROTENOID DERIVATIVES的CHIRAL中间体的方法
公开(公告)号：WO2006039685A3
公开(公告)日：2007-01-04
申请号：PCT/US2005035599
申请日：2005-10-03
申请人： HAWAII BIOTECH INC , LOCKWOOD SAMUEL F , TANG PENG CHO , NADOLSKI GEOFF , FANG ZHIQIANG , DU YISHU , GEISS WILLIAM , WILLIAMS RICHARD , BURDICK WILLIAM , YANG MIN
发明人： LOCKWOOD SAMUEL F , TANG PENG CHO , NADOLSKI GEOFF , FANG ZHIQIANG , DU YISHU , GEISS WILLIAM , WILLIAMS RICHARD , BURDICK WILLIAM , YANG MIN
IPC分类号： C07C29/145 , C07C33/14 , C07C45/29 , C07C45/61 , C07C45/64 , C07C45/65 , C07C45/67 , C07C45/71 , C07C45/74 , C07C47/21 , C07C49/713 , C07C49/753 , C07C401/00 , C07F7/04 , C07F7/18
CPC分类号： C07C403/24 , C07B2200/07 , C07B2200/09 , C07C29/143 , C07C45/298 , C07C45/511 , C07C45/61 , C07C45/64 , C07C45/673 , C07C45/70 , C07C45/71 , C07C47/21 , C07C49/713 , C07C49/753 , C07C403/08 , C07C2601/16 , C07D319/06 , C07F7/188 , C07F7/1892 , C07F9/113 , C07F9/5442 , C12P23/00 , C07C49/603 , C07C33/02 , C07C35/08 , C07C35/21
摘要： A method used for synthesizing intermediates for use in the synthesis of carotenoids and carotenoid analogs, and/or carotenoid derivatives. In some embodiments, the invention includes methods for synthesizing optically active intermediates useful for the synthesis of optically active carotenoids.
摘要翻译：用于合成用于合成类胡萝卜素和类胡萝卜素类似物的中间体和/或类胡萝卜素衍生物的方法。在一些实施方案中，本发明包括用于合成可用于合成光学活性类胡萝卜素的光学活性中间体的方法。

3. 发明申请

WO2006105214A2 REDUCTION IN COMPLEMENT ACTIVATION AND INFLAMMATION DURING TISSUE INJURY BY CAROTENOIDS, CAROTENOID ANALOGS, OR DERIVATIVES THEREOF 审中-公开
标题翻译：减轻激素和引起的损伤，由卡培他酮，卡那霉素类似物或其衍生物组织损伤
公开(公告)号：WO2006105214A2
公开(公告)日：2006-10-05
申请号：PCT/US2006011496
申请日：2006-03-29
申请人： HAWAII BIOTECH INC , NADOLSKI GEOFF , LOCKWOOD SAMUEL F
发明人： NADOLSKI GEOFF , LOCKWOOD SAMUEL F
CPC分类号： A61K31/225 , A61K31/192 , A61K31/195 , A61K31/341 , A61K31/573 , A61K31/6615 , A61K31/7034 , A61K38/16 , A61K45/06
摘要： Administering water-soluble or dispersible synthetic analogs or derivatives of astaxanthin, lutein, zeaxanthin, or lycophyll and/or other carotenoids to a subject may reduce some of the adverse effects of inflammation in a body organ or tissue. The analogs or derivatives may be incorporated into pharmaceutical, over-the-counter, or nutraceutical preparations. Administration of the analogs or derivatives described herein may reduce deposition of inflammatory mediators such as C-reactive protein, complement system proteins or the membrane attack complex (MAC) in tissues. Reduced deposition of these molecules in tissues may reduce cell damage and/or lysis in the tissues.
摘要翻译：向受试者施用虾青素，叶黄素，玉米黄质或者叶绿素和/或其他类胡萝卜素的水溶性或可分散的合成类似物或衍生物可以减少身体器官或组织中炎症的一些不利影响。类似物或衍生物可以并入药物，非处方药或营养制剂中。本文所述的类似物或衍生物的施用可以减少炎症介质如C反应蛋白，补体系统蛋白或膜攻击复合物（MAC）在组织中的沉积。这些分子在组织中的沉淀减少可以减少组织中的细胞损伤和/或裂解。

4. 发明申请

WO2006119125A3 METHODS FOR SYNTHESIS OF CAROTENOIDS, INCLUDING ANALOGS, DERIVATIVES, AND SYNTHETIC AND BIOLOGICAL INTERMEDIATES 审中-公开
标题翻译：用于合成碳酸的方法，包括模拟物，衍生物，合成和生物中间体
公开(公告)号：WO2006119125A3
公开(公告)日：2007-01-11
申请号：PCT/US2006016487
申请日：2006-05-01
申请人： HAWAII BIOTECH INC , LOCKWOOD SAMUEL F , NADOLSKI GEOFF , BURDICK DAVID , TANG PENG CHO , JACKSON HENRY L , FANG ZHIQIANG , DU YISHU , YANG MIN , GEISS WILLIAM , WILLIAMS RICHARD
发明人： LOCKWOOD SAMUEL F , NADOLSKI GEOFF , BURDICK DAVID , TANG PENG CHO , JACKSON HENRY L , FANG ZHIQIANG , DU YISHU , YANG MIN , GEISS WILLIAM , WILLIAMS RICHARD
IPC分类号： C07F9/113 , C07C69/40
CPC分类号： C07C29/147 , C07C11/21 , C07C33/02 , C07C45/298 , C07C47/21 , C07C49/743 , C07C67/08 , C07C67/30 , C07C67/343 , C07C67/39 , C07C69/40 , C07C69/602 , C07C403/24 , C07C2601/16 , C07F9/113 , C07F9/65515 , C07C69/73 , C07C35/21
摘要： A method for synthesizing intermediates for use in the synthesis of carotenoid synthetic intermediates, carotenoid analogs, and/or carotenoid derivatives. The carotenoid analog, derivative, or intermediate may be administered to a subject for the inhibition and/or amelioration of any disease that involves production of reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals. In some embodiments, the invention may include methods for synthesizing chemical compounds including an analog or derivative of a carotenoid. Carotenoid analogs or derivatives may include acyclic end groups. In some embodiments, a carotenoid analog or derivative may include at least one substituent. The substituent may enhance the solubility of the carotenoid analog or derivative such that the carotenoid analog or derivative at least partially dissolves in water. Each R 3 ma be independently hydrogen or methyl. Each R 1 and R 2 may be independently:
摘要翻译：用于合成用于合成类胡萝卜素合成中间体，类胡萝卜素类似物和/或类胡萝卜素衍生物的中间体的方法。类胡萝卜素类似物，衍生物或中间体可以施用于受试者以抑制和/或改善涉及产生活性氧，活性氮物质，自由基和/或非自由基的任何疾病。在一些实施方案中，本发明可以包括合成包括类胡萝卜素类似物或衍生物的化合物的方法。类胡萝卜素类似物或衍生物可包括无环端基。在一些实施方案中，类胡萝卜素类似物或衍生物可包括至少一个取代基。取代基可以增强类胡萝卜素类似物或衍生物的溶解度，使得类胡萝卜素类似物或衍生物至少部分地溶解在水中。每个R 3独立地是氢或甲基。每个R 1和R 2可以独立地是：

5. 发明申请

WO2006099015A3 CAROTENOIDS, CAROTENOID ANALOGS, OR CAROTENOID DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开
标题翻译： CAROTENOIDS，CAROTENOID ANALOGS，或用于治疗增殖性疾病的CAROTENOID衍生物
公开(公告)号：WO2006099015A3
公开(公告)日：2006-12-21
申请号：PCT/US2006008363
申请日：2006-03-09
申请人： HAWAII BIOTECH INC , LOCKWOOD SAMUEL F , NADOLSKI GEOFF , FREY DEAN ALLEN , MCLAWS MARK , BURDICK DAVID
发明人： LOCKWOOD SAMUEL F , NADOLSKI GEOFF , FREY DEAN ALLEN , MCLAWS MARK , BURDICK DAVID
IPC分类号： A61K31/7024 , A61K31/01 , A61K31/215 , A61K31/6615 , A61P35/00
CPC分类号： A61K31/01 , A61K31/12 , A61K31/13 , A61K31/185 , A61K31/192 , A61K31/195 , A61K31/215 , A61K31/6615 , A61K31/7024 , A61K38/16
摘要： A method and system used for treating proliferative disorders using carotenoids, carotenoid analogs, and/or carotenoid derivatives. The method and system may be used for chemoprevention and/or chemotherapy. The method and system may induce apoptosis in target cells, tissues, and/or organs. The analog, derivative, or intermediate may be administered to a cell, a group of cells, a tissue, an organ or a subject, such that at least a portion of the undesirable consequences of the proliferative disorder are thereby reduced.
摘要翻译：用于使用类胡萝卜素，类胡萝卜素类似物和/或类胡萝卜素衍生物治疗增殖性疾病的方法和系统。该方法和系统可用于化学预防和/或化疗。该方法和系统可诱导靶细胞，组织和/或器官中的细胞凋亡。可以将类似物，衍生物或中间体施用于细胞，细胞组织，组织，器官或受试者，从而减少增殖性疾病的不良后果的至少一部分。

6. 发明申请

WO2007147163A3 COMPOSITIONS COMPRISING CAROTENOID ANALOGS OR DERIVATIVES AND METHODS FOR SYNTHESIS 审中-公开
标题翻译：含有卡诺霉素类似物或衍生物的组合物和合成方法
公开(公告)号：WO2007147163A3
公开(公告)日：2008-03-20
申请号：PCT/US2007071482
申请日：2007-06-18
申请人： CARDAX PHARMACEUTICALS INC , LOCKWOOD SAMUEL F , TANG PENG CHO , NADOLSKI GEOFF , JACKSON HENRY L , FANG ZHIQIANG , DU YISHU , YANG MIN , GEISS WILLIAM , WILLIAMS RICHARD , BURDICK DAVID , BRAUN CHRISTI L
发明人： LOCKWOOD SAMUEL F , TANG PENG CHO , NADOLSKI GEOFF , JACKSON HENRY L , FANG ZHIQIANG , DU YISHU , YANG MIN , GEISS WILLIAM , WILLIAMS RICHARD , BURDICK DAVID , BRAUN CHRISTI L
IPC分类号： C07C33/02 , A61K31/22 , A61K31/223 , A61P9/04 , A61P9/06 , A61P35/00 , C07C69/40 , C07C229/12 , C07C229/26 , C07C229/30 , C07C271/22 , C07D207/10 , C07D295/185 , C07F9/113
CPC分类号： C07F9/113 , C07C33/02 , C07C45/298 , C07C47/21 , C07C67/343 , C07C69/40 , C07C229/12 , C07C229/26 , C07C271/22 , C07D207/16 , C07D295/205 , C07C69/602
摘要： A method for synthesizing intermediates for use in the synthesis of carotenoid synthetic intermediates, carotenoid analogs, and/or carotenoid derivatives. The carotenoid analog, derivative, or intermediate may be administered to a subject for the inhibition and/or amelioration of any disease that involves production of reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals. In some embodiments, the invention may include methods for synthesizing chemical compounds including an analog or derivative of a carotenoid. Carotenoid analogs or derivatives may include acyclic end groups. In some embodiments, a carotenoid analog or derivative may include at least one substituent. The substituent may enhance the solubility of the carotenoid analog or derivative such that the carotenoid analog or derivative at least partially dissolves in water.
摘要翻译：用于合成用于合成类胡萝卜素合成中间体，类胡萝卜素类似物和/或类胡萝卜素衍生物的中间体的方法。类胡萝卜素类似物，衍生物或中间体可以施用于受试者以抑制和/或改善涉及产生活性氧，活性氮物质，自由基和/或非自由基的任何疾病。在一些实施方案中，本发明可以包括合成包括类胡萝卜素类似物或衍生物的化合物的方法。类胡萝卜素类似物或衍生物可包括无环端基。在一些实施方案中，类胡萝卜素类似物或衍生物可包括至少一个取代基。取代基可以增强类胡萝卜素类似物或衍生物的溶解度，使得类胡萝卜素类似物或衍生物至少部分地溶解在水中。

7. 发明申请

WO2008106606A3 CAROTENOID ANALOGS AND DERIVATIVES IN THE TREATMENT OF PROSTATE CANCER 审中-公开
标题翻译： CAROTENOID ANALOGS AND DERIVATIVES IN THE ADVESTING OF PROSTATE CANCER
公开(公告)号：WO2008106606A3
公开(公告)日：2009-07-02
申请号：PCT/US2008055334
申请日：2008-02-28
申请人： CARDAX PHARMACEUTICALS INC , KING TIMOTHY J , LOCKWOOD SAMUEL F , HIEBER ANDREW DAVID , SHUBIN NICHOLAS J , JACKSON HENRY J , NADOLSKI GEOFFRY T
发明人： KING TIMOTHY J , LOCKWOOD SAMUEL F , HIEBER ANDREW DAVID , SHUBIN NICHOLAS J , JACKSON HENRY J , NADOLSKI GEOFFRY T
IPC分类号： A61K31/221 , A61K31/01 , A61K31/047 , A61K31/225 , A61K31/341 , A61P35/00
CPC分类号： A61K31/01 , A61K31/047 , A61K31/221 , A61K31/225 , A61K31/341
摘要： The presently described embodiments are directed to compositions that include one or more carotenoid analogs or derivatives for use in the treatment of prostate cancer, BPH or prostatitis. Certain embodiments provide for the use of said carotenoid analogs or derivatives in preparing compositions suitable for use in such treatments. Further embodiments provide for pharmaceutical compositions that include one or more carotenoid analogs or derivatives in combination with one or more additional compositions or medicaments suitable for the treatment of prostate cancer. Yet further embodiments provide for methods of treating prostate cancer that include administering to a subject who would benefit from such treatment pharmaceutical compositions suitable for inhibiting or reducing one or more components of NF-?B signaling in the subject undergoing said treatments, and that include carotenoid analogs or derivatives, optionally in combination with one or more additional compositions or medicaments suitable for the treatment of prostate cancer.
摘要翻译：目前描述的实施方案涉及包含用于治疗前列腺癌，BPH或前列腺炎的一种或多种类胡萝卜素类似物或衍生物的组合物。某些实施方案提供了使用所述类胡萝卜素类似物或衍生物制备适用于这种治疗的组合物。另外的实施方案提供包含一种或多种类胡萝卜素类似物或衍生物与一种或多种适合于治疗前列腺癌的其它组合物或药物组合的药物组合物。另外的实施方案提供了治疗前列腺癌的方法，其包括对受益于受治疗的受试者施用适合于抑制或减少经历所述治疗的受试者中NF-κB信号传导的一种或多种成分的药物组合物，并且包括类胡萝卜素类似物或衍生物，任选地与一种或多种适合于治疗前列腺癌的另外的组合物或药物组合。

8. 发明申请

WO2007090095A2 SYNTHESIS OF CAROTENOID ANALOGS OR DERIVATIVES WITH IMPROVED ANTIOXIDANT CHARACTERISTICS 审中-公开
标题翻译：具有改善的抗氧化特性的卡诺斯酸类似物或衍生物的合成
公开(公告)号：WO2007090095A2
公开(公告)日：2007-08-09
申请号：PCT/US2007061241
申请日：2007-01-29
申请人： CARDAX PHARMACEUTICALS INC , LOCKWOOD SAMUEL F , NADOLSKI GEOFF , FOSS BENTE J
发明人： LOCKWOOD SAMUEL F , NADOLSKI GEOFF , FOSS BENTE J
IPC分类号： C07C39/21 , A61K31/05 , A61K31/085 , A61P9/04 , A61P9/06 , A61P35/00 , C07C39/23 , C07C43/205
CPC分类号： C07C39/21 , C07C45/298 , C07C47/21
摘要： A method is described for synthesizing and adminisitering carotenoid compounds with improved antioxidant characteristics. In some embodiments, extension or improvement of conjugation may be employed in structural modification of carotenoids. In other embodiments, reduction of ring/chain steric hindrance may improve the lambda max, and hence, the overall antioxidant capability, of particular compounds. In other embodiments, introduction and/or increase in synthetic handles for conjugation may improve the stoichiometric ratios of conjugating moieties to the polyene backbone. The methods may be used to improve natural and/or synthetic compounds for medicinal application in the treatment of disease.
摘要翻译：描述了一种合成和管理具有改善的抗氧化特性的类胡萝卜素化合物的方法。在一些实施方案中，缀合的延伸或改进可用于类胡萝卜素的结构修饰。在其它实施方案中，环/链空间位阻的减少可以改善特定化合物的λmax，因此改善整体抗氧化能力。在其它实施方案中，用于缀合的合成手段的引入和/或增加可以改善缀合部分与多烯骨架的化学计量比。该方法可用于改善用于治疗疾病的药物应用的天然和/或合成化合物。

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