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1. 发明授权

US06794408B2 Drechsleranol derivatives, processes for their preparation and their use 失效
标题翻译：德舒辛醇衍生物，其制备方法及其用途
公开(公告)号：US06794408B2
公开(公告)日：2004-09-21
申请号：US10351773
申请日：2003-01-27
申请人： Claudia Eder , Michael Kurz , Luigi Toti
发明人： Claudia Eder , Michael Kurz , Luigi Toti
IPC分类号： A61K3134
CPC分类号： C07D307/77 , C12P17/04 , C12R1/645
摘要： The present invention provides novel drechsleranol compounds of formula (I) which are formed by the microorganism Drechslera australlensis, ST 003360, DSM 14093, or a fungus ST 004112, DSM 14524, during fermentation. A process for their preparation, pharmaceutical compositions containing said drechsleranols their use for the treatment and/or prophylaxis of degenerative neuropathies, such as, Alzheimeu's disease, or psychiatric disorders, such as depression, sleep disturbance or seasonal affective disorder, and their use as chelating agents or antioxidants are also disclosed and claimed.
摘要翻译：本发明提供了在发酵期间由微生物Drechslera australlensis，ST 003360，DSM14093或真菌ST 004112，DSM14524形成的式（I）的新颖的德劳克醇化合物。它们的制备方法，含有所述的drechsleranols的药物组合物，它们用于治疗和/或预防退行性神经病，例如阿尔茨海默病，或精神疾病如抑郁症，睡眠障碍或季节性情感障碍，以及它们作为螯合剂的用途还公开并要求保护剂或抗氧化剂。

2. 发明授权

US06723736B2 Tricyclic compounds and uses thereof 失效
标题翻译：三环化合物及其用途
公开(公告)号：US06723736B2
公开(公告)日：2004-04-20
申请号：US09973190
申请日：2001-10-10
申请人： Debendranath Dey , Partha Neogi , Ananda Sen , Somesh D. Sharma , Bishwajit Nag
发明人： Debendranath Dey , Partha Neogi , Ananda Sen , Somesh D. Sharma , Bishwajit Nag
IPC分类号： A61K3134
CPC分类号： C07D335/06 , C07D217/16 , C07D217/24 , C07D311/76
摘要： Substituted isoquinolines, isochromanones and isothiochromanones that inhibit the pro-inflammatory cytokines tumor necrosis factor-alpha (TNF-alpha) and/or interleukin-6 (IL-6) and/or the enzyme cyclooxygenase-2 (COX-2) and/or interleukin-10 (IL-10). Compositions containing such compounds and methods of using such compounds for treatment and/or prevention of inflammation, inflammatory diseases, immunologic diseases and other diseases mediated by TNF-alpha, IL-6, COX-2 and/or IL-10 are also disclosed.
摘要翻译：抑制促炎细胞因子肿瘤坏死因子-α（TNF-α）和/或白细胞介素-6（IL-6）和/或酶环加氧酶-2（COX-2）和/或其他细胞因子的替代异喹啉，异色满酮和异硫代色酮白细胞介素-10（IL-10）。还公开了含有这些化合物的组合物和使用这些化合物治疗和/或预防炎症，炎性疾病，免疫疾病和由TNF-α，IL-6，COX-2和/或IL-10介导的其它疾病的方法。

3. 发明授权

US06703419B1 Chemical composition for aiding the absorption, binding and elimination of undigested fat 失效
标题翻译：帮助吸收，结合和消除未消化脂肪的化学成分
公开(公告)号：US06703419B1
公开(公告)日：2004-03-09
申请号：US10237546
申请日：2002-09-09
申请人： Jose A. Diaz , Eduardo M. Naranjo
发明人： Jose A. Diaz , Eduardo M. Naranjo
IPC分类号： A61K3134
CPC分类号： A61K36/48 , A23L19/115 , A23L29/231 , A23L29/238 , A23L29/244 , A23L29/275 , A23L33/10 , A23L33/21 , A23V2002/00 , A61K36/68 , A61K2300/00 , A23V2250/5074 , A23V2250/511 , A23V2250/5058 , A23V2250/5072 , A23V2250/1886 , A23V2200/224 , A23V2250/2042
摘要： A composition and method for facilitating weight loss and aiding in the maintenance of a stable weight in humans, wherein a preferred embodiment of the chemical composition comprises a mixture of psyllium husks generally in an amount of between 72% and 88% by weight of the total chemical composition, natural marine shellfish extract generally in an amount of between 9% and 11% by weight, acacia generally in an amount of between 4.5% and 5.5% by weight, an amount of apple pectin generally in an amount of between 1.4% and 2.2% by weight of the total chemical composition, ascorbic acid (Vitamin C) generally in an amount of between 1.8% and 2.2% by weight. Magnesium stearate may also be included generally in an amount of about 1% by weight of the total chemical composition.
摘要翻译：一种用于促进体重减轻并有助于维持人体稳定体重的组合物和方法，其中化学组合物的优选实施方案包含欧车前体的混合物，通常其总量为72％至88％化学成分，天然海洋贝类提取物的量通常为9重量％至11重量％，阿拉伯胶通常为4.5重量％至5.5重量％，苹果果胶的用量通常为1.4％至化学成分总量的2.2重量％，抗坏血酸（维生素C）的含量通常为1.8〜2.2重量％。硬脂酸镁通常也可以包括总化学成分的约1重量％的量。

4. 发明授权

US06649649B1 Method of treating colonic adenomas 失效
公开(公告)号：US06649649B1
公开(公告)日：2003-11-18
申请号：US09261034
申请日：1999-03-02
申请人： Stacia Kargman , Thomas J. Simon , Jilly Evans
发明人： Stacia Kargman , Thomas J. Simon , Jilly Evans
IPC分类号： A61K3134
CPC分类号： A61K31/00 , A61K31/12 , A61K31/18 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/34 , A61K31/341 , A61K31/365 , A61K31/40 , A61K31/405 , A61K31/407 , A61K31/54 , A61K31/5415 , A61K31/603 , A61K31/616
摘要： This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.

5. 发明授权

US06552074B2 Arginine/ascorbic acid mixed powder as an oral supplement 失效
标题翻译：精氨酸/抗坏血酸混合粉末作为口服补充剂
公开(公告)号：US06552074B2
公开(公告)日：2003-04-22
申请号：US09987179
申请日：2001-11-13
申请人： Eiji Kimoto , Fukumi Morishige
发明人： Eiji Kimoto , Fukumi Morishige
IPC分类号： A61K3134
CPC分类号： A61K45/06 , A61K31/198 , A61K31/375 , A61K2300/00
摘要： A mixture obtained by mixing ascorbic acid powder with arginine powder in a weight ratio (ascorbic acid/arginine) of ⅕ to 20, especially ⅕ to ¼; and a supplement such as a nutrient preparation and a health-care food containing the mixture. Mixing of arginine powder and ascorbic acid powder in the weight ratios eliminates stringent taste specific to arginine and alleviates stringent feeling in the stomach (heartburn, nausea or vomiting) after oral intake thereof. The mixture prevents also peroxidative injuries of cells caused by an administration of a great amount of arginine alone. Further, mixing of arginine powder with ascorbic acid powder prevents browning of the mixture after long-term storage.
摘要翻译：将抗坏血酸粉末与精氨酸粉末（抗坏血酸/精氨酸）的重量比（1/5至20，特别是1/5至1/4）混合，以及补充剂，例如营养制剂和含有该混合物的保健食品。混合精氨酸粉末和抗坏血酸粉末的重量比消除了对精氨酸特异性的严格味道，并减轻了口服摄入后胃中的严重感觉（胃灼热，恶心或呕吐）。该混合物还防止单独施用大量精氨酸引起的细胞的过氧化损伤。此外，精氨酸粉末与抗坏血酸粉末的混合可以防止长期储存后混合物的褐变。

6. 发明授权

US06548539B1 Agents for regulation of colon cancer gene expression 失效
标题翻译：用于调节结肠癌基因表达的药剂
公开(公告)号：US06548539B1
公开(公告)日：2003-04-15
申请号：US10090866
申请日：2002-03-05
申请人： Stanislaw Pikul , Daniel R. Soppet , Paul E. Young
发明人： Stanislaw Pikul , Daniel R. Soppet , Paul E. Young
IPC分类号： A61K3134
CPC分类号： C07C323/42 , C07C323/40 , C07C323/41 , C07C323/44 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D307/22
摘要： Compounds of the general structure according to Formula (I) wherein R1 is selected from alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, and heterocycloalkyl; R2 is selected from alkyl, alkenyl, alkyny, heteroalkyl, haloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, and heterocycloalkylalkyl; R3 is selected from aryl, heteroaryl, cycloalkyl, and heterocycloalkyl; W is selected from Ch2, O and S; n is 0 to about 3: X is selected from S or O; Y, if present, is selected from a bond, aryl, NH, NR, O or S, where R3 is selected from hydrogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, and heterocycloalkylalkyl; and Z, if present, can represent a bond or is selected from lower alkyl, O or S are disclosed. Also disclosed are uses of such compounds for treating a variety of disease conditions, including cancer.
摘要翻译：其中R 1选自烷基，烯基，炔基，杂烷基，卤代烷基，芳基，芳烷基，杂芳基，杂芳基烷基，环烷基和杂环烷基中的根据式（I）的通式结构的化合物; R 2选自烷基，烯基，炔基，杂烷基，卤代烷基，芳基烷基，杂芳基烷基，环烷基烷基和杂环烷基烷基; R 3选自芳基，杂芳基，环烷基和杂环烷基; W选自Ch2，O和S; n为0至约3：X选自S或O; Y如果存在，选自键，芳基，NH，NR，O或S，其中R 3选自氢，烷基，烯基，炔基，杂烷基，卤代烷基，芳基烷基，杂芳基烷基，环烷基烷基和杂环烷基烷基; 和Z如果存在，可以表示键或选自低级烷基，O或S。还公开了这些化合物用于治疗各种疾病状况（包括癌症）的用途。

7. 发明授权

US06534540B2 Combination and method of treatment of cancer utilizing a COX-2 inhibitor and a 3-hydroxy-3-methylglutaryl-coenzyme-a (HMG-CoA) reductase inhibitor 失效
公开(公告)号：US06534540B2
公开(公告)日：2003-03-18
申请号：US09912703
申请日：2001-07-25
申请人： George Kindness , Brooke Schumm, III , F. Timothy Guilford
发明人： George Kindness , Brooke Schumm, III , F. Timothy Guilford
IPC分类号： A61K3134
CPC分类号： A61K45/06 , A61K31/195 , A61K31/198 , A61K31/22 , A61K31/225 , A61K31/34 , A61K31/35 , A61K31/355 , A61K31/365 , A61K31/366 , A61K31/385 , A61K31/415 , A61K33/04 , A61K33/38 , A61K2300/00
摘要： The inventors propose a combination of an HMG-CoA reductase inhibitor (also referred to as “HMG-CoA inhibitor(s)”), and COX-2 inhibitor for the treatment of cancer especially prostate cancer and a method of treatment of cancer by that combination, especially prostate cancer. The inventors propose a combination of an HMG-CoA reductase inhibitor, COX-2 inhibitor, and glutathione pathway enhancing and detoxifying compound, particularly cystine, for the treatment of cancer especially prostate cancer and a method of treatment of cancer by that combination, especially prostate cancer. Based on the clinical results of retardation, but not cure of cancer, the combination has the characteristic of sufficiently interfering with replication and apparently restoring the immune system capacity to manage cancer.

8. 发明授权

US06486202B1 Inhibitors of isoprenyl transferase 有权
标题翻译：异戊二烯转移酶抑制剂
公开(公告)号：US06486202B1
公开(公告)日：2002-11-26
申请号：US09835274
申请日：2001-04-13
申请人： Ana Maria Garcia , James Kowalczyk , Michael D. Lewis
发明人： Ana Maria Garcia , James Kowalczyk , Michael D. Lewis
IPC分类号： A61K3134
CPC分类号： C07D307/22 , C07C323/60
摘要： Provided are novel peptidomimetic isoprenyl transferase inhibitors, methods for synthesizing such inhibitors, and methods for the use of such inhibitors for the treatment of tumors.
摘要翻译：提供了新的拟肽异戊二烯转移酶抑制剂，合成这种抑制剂的方法，以及使用这种抑制剂治疗肿瘤的方法。

9. 发明授权

US06465510B2 Emulsion containing ascorbic acid and its uses in the cosmetics and dermatological fields 有权
标题翻译：含有抗坏血酸的乳液及其在化妆品和皮肤病领域的应用
公开(公告)号：US06465510B2
公开(公告)日：2002-10-15
申请号：US09801755
申请日：2001-03-09
申请人： Isabelle Afriat , Florence Chanvin
发明人： Isabelle Afriat , Florence Chanvin
IPC分类号： A61K3134
CPC分类号： A61Q17/00 , A61K8/06 , A61K8/064 , A61K8/676 , A61K8/894 , A61Q19/00 , A61Q19/08 , Y10S514/928
摘要： A water-in-oil emulsion containing ascorbic acid and, as an emulsifier, a dimethiconecopolyol or an alkyldimethiconecopolyol, where the aqueous phase having a pH ranging from 5.5 to 7.5. This emulsion allows ascorbic acid to be stabilized and can be used, in particular, in the cosmetics and/or dermatological fields. The invention also relates to a cosmetic process for treating the skin using the emulsion.
摘要翻译：含有抗坏血酸的油包水乳液，以及作为乳化剂的二甲基聚多元醇或烷基二甲基多羟基苯甲醇，其中水相的pH为5.5-7.5。该乳液使抗坏血酸稳定，特别可用于化妆品和/或皮肤病学领域。本发明还涉及使用乳液处理皮肤的美容方法。

10. 发明授权

US06417226B1 Skin whiteners containing hydroxytetronic acid 有权
标题翻译：皮肤增白剂含有羟基特膦酸
公开(公告)号：US06417226B1
公开(公告)日：2002-07-09
申请号：US09735144
申请日：2000-12-12
申请人： Nicholas V. Perricone
发明人： Nicholas V. Perricone
IPC分类号： A61K3134
CPC分类号： A61Q19/02 , A61K8/4973 , A61K31/365
摘要： Skin whitening compositions contain &agr;-hydroxytetronic acid or a &agr;-hydroxy tetronic derivative, and, in some cases, hydroquinone, an &agr;-hydroxy acid such as glycolic acid, and a fatty acid ester of ascorbic acid such as ascorbyl palmitate.
摘要翻译：皮肤美白组合物含有α-羟基特斯酸或α-羟基特龙衍生物，在某些情况下，有氢醌，α-羟基酸如乙醇酸，以及抗坏血酸的脂肪酸酯如抗坏血酸棕榈酸酯。

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