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1. 发明申请

WO2007090095A3 SYNTHESIS OF CAROTENOID ANALOGS OR DERIVATIVES WITH IMPROVED ANTIOXIDANT CHARACTERISTICS 审中-公开
公开(公告)号：WO2007090095A3
公开(公告)日：2007-08-09
申请号：PCT/US2007/061241
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 , C07C39/23 , C07C43/205 , A61K31/05 , A61K31/085 , A61P35/00 , A61P9/06 , A61P9/04
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.

2. 发明申请

WO2007147163A2 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：WO2007147163A2
公开(公告)日：2007-12-21
申请号：PCT/US2007/071482
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.
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。

3. 发明申请

WO2006102576A1 WATER-DISPERSIBLE CAROTENOIDS, INCLUDING ANALOGS AND DERIVATIVES 审中-公开
标题翻译：含水不溶性毛细血管细胞，包括模拟物和衍生物
公开(公告)号：WO2006102576A1
公开(公告)日：2006-09-28
申请号：PCT/US2006/010726
申请日：2006-03-23
申请人： HAWAII BIOTECH, INC. , LOCKWOOD, Samuel, F , NADOLSKI, Geoff
发明人： LOCKWOOD, Samuel, F , NADOLSKI, Geoff
IPC分类号： C07C403/24 , C07F9/117 , C07F9/655 , A61K31/225 , A61K31/665 , A61K31/6615 , A61P27/02
CPC分类号： C07D295/205 , A61K31/07 , A61K31/12 , A61K31/225 , A61K31/6615 , A61K31/665 , C07C403/24 , C07D307/62 , C07F9/117 , C07F9/65515
摘要： A chemical composition; comprising one or more carotenoid analogs or derivatives having a structure (I), (II) and (III) where each R 3 is independently hydrogen or methyl, and where each R 1 and R 2 are independently wherein each R 5 is independently hydrogen, -OH, or -OR 6 , wherein at least one R 5 group is -OR 6 ; wherein each R 6 is independently: alkyl; aryl; -alkyl-N(R 7 ) 2 ; -aryl-N(R 7 ) 2 ; -alkyl-N + (R 7 ) 3 ; -aryl-N + (R 7 ) 3 ; -alkyl-CO 2 R 7 ; -aryl-CO 2 R 7 ; -alkyl-CO 2 ; -aryl-CO 2 ; -CO 2 R 8 ; -P(O)(OR 8 ) 2 ; -S(O)(OR 8 ) 2 ; an amino acid; a peptide, a carbohydrate; -C(O)- (CH 2 ) 0 -CO 2 R 9 ; a nucleoside residue, or a co-antioxidant; wherein R 7 is hydrogen, alkyl, or aryl; wherein R 8 is hydrogen, alkyl, aryl, benzyl or a co-antioxidant; wherein R 9 is hydrogen; alkyl; aryl; -P(0)(OR 8 ) 2 ; -S(0)(OR 8 ) 2 ; an amino acid; a peptide, a carbohydrate; a nucleoside, or a co-antioxidant; and wherein n is 1 to 9. The compounds are useful for the inhibition and amelioration of diseases resulting in change and/or loss of vision.
摘要翻译：化学成分; 包含一种或多种具有结构（I），（II）和（III）的类胡萝卜素类似物或衍生物，其中每个R 3独立地为氢或甲基，并且其中每个R 1〜 >和R 2独立地是其中每个R 5独立地是氢，-OH或-OR 6，其中至少一个R 0 > 5 组为-OR 6; 其中每个R 6独立地为：烷基; 芳基; - 烷基-N（R ^{7 ）_{2 ; 芳基 - N（R ^{7 ）_{2 ; - 烷基-N +（R 7）3 - ; 芳基-N ^{+ （R ^{7 ）_{3 ; - 烷基CO _{2 - [R ^{7 ; - 芳基 - CO _{2 - [R ^{7 ; - 烷基CO _{2 ; - 芳基 - CO _{2 ; -CO _{2 - [R ^{8 ; -P（O）（OR ^{8 ）_{2 ; -S（O）（OR ^{8 ）_{2 ; 氨基酸; 肽，碳水化合物; -C（O） - （CH 2 CH 2）2 -CO 2 R 9; 核苷残基或共抗氧化剂; 其中R 7为氢，烷基或芳基; 其中R 8为氢，烷基，芳基，苄基或共抗氧化剂; 其中R 9是氢; 烷基; 芳基; -P（O）（OR ^{8 ）_{2 ; -S（O）（OR ^{8 ）_{2 ; 氨基酸; 肽，碳水化合物; 核苷或共抗氧化剂; 并且其中n为1至9.所述化合物可用于抑制和改善导致变化和/或视力丧失的疾病。}}}}}}}}}}}}}}}}}}}}}}}

4. 发明申请

WO2006099015A2 CAROTENOIDS, CAROTENOID ANALOGS, OR CAROTENOID DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开
标题翻译：类胡萝卜素，类胡萝卜素类似物或类胡萝卜素衍生物用于治疗增殖性疾病
公开(公告)号：WO2006099015A2
公开(公告)日：2006-09-21
申请号：PCT/US2006/008363
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 , A61K31/6615 , A61K31/215 , A61K31/01 , 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：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。该方法和系统可以诱导靶细胞，组织和/或器官的凋亡。类似物，衍生物或中间体可以施用于细胞，一组细胞，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。

5. 发明申请

WO2008106606A2 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：WO2008106606A2
公开(公告)日：2008-09-04
申请号：PCT/US2008/055334
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.
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-κB 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。

6. 发明申请

WO2008118862A1 CAROTENOID ANALOGS AND DERIVATIVES FOR THE PREVENTION OF PLATELET AGGREGATION 审中-公开
标题翻译：用于防止血小板聚集的CAROTENOID类似物和衍生物
公开(公告)号：WO2008118862A1
公开(公告)日：2008-10-02
申请号：PCT/US2008/058029
申请日：2008-03-24
申请人： CARDAX PHARMACEUTICALS, INC. , LOCKWOOD, Samuel, F , MASON, R. Preston
发明人： LOCKWOOD, Samuel, F , MASON, R. Preston
IPC分类号： A61K31/01 , A61P9/00
CPC分类号： A61K31/01
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 a disorder associated with platelet aggregation. 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 a disorder associated with platelet aggregation. Yet further embodiments provide for methods of treating a disorder associated with platelet aggregation that include administering to a subject who would benefit from such treatment pharmaceutical compositions suitable for inhibiting platelet aggregation in a subject undergoing said treatments, and that include carotenoid analogs or derivatives, optionally in combination with one or more additional antiplatelet agents.
摘要翻译：目前描述的实施方案涉及包含用于治疗与血小板聚集相关的病症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用于治疗与血小板聚集有关的病症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与血小板聚集相关的病症的方法，其包括向受试者受益，所述受试者适合于在经历所述治疗的受试者中抑制血小板聚集的药物组合物，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另外的抗血小板药物组合。

7. 发明申请

WO2006119168A3 USE OF CAROTENOIDS AND/OR CAROTENOID DERIVATIVES/ANALOGS FOR REDUCTION/INHIBITION OF CERTAIN NEGATIVE EFFECTS OF COX INHIBITORS 审中-公开
公开(公告)号：WO2006119168A3
公开(公告)日：2006-11-09
申请号：PCT/US2006/016590
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
IPC分类号： A61K45/06 , A61K31/522 , A61K31/415 , A61K31/196 , A61P29/00 , A61P43/00
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.

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