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1. 发明授权

US5587368A Administration of a 27-hydroxycholesterol or related compound or sterol-27-hydroxylase stimulant to prevent restenosis following vascular endothelial injury 失效
标题翻译：施用27-羟基胆固醇或相关化合物或甾醇-27-羟化酶刺激剂以防止血管内皮损伤后的再狭窄
公开(公告)号：US5587368A
公开(公告)日：1996-12-24
申请号：US319225
申请日：1994-10-06
申请人： Norman B. Javitt
发明人： Norman B. Javitt
IPC分类号： A61K31/575 , A61K47/48 , A61P7/00 , C07J9/00 , A61K31/56
CPC分类号： A61K31/7072 , A61K31/575 , A61K47/48969 , B82Y5/00
摘要： A method for preventing or reducing restenosis wherein a 27-hydroxycholesterol or a 25,26 and/or 27-aminocholesterol, or a sterol 27-hydroxylase stimulant, is administered in a restenosis preventing and/or reducing amount. The invention also includes a method for treating cancer using 27-hydroxycholesterol.
摘要翻译：一种预防或减少再狭窄的方法，其中27-羟基胆固醇或25,26和/或27-氨基胆固醇或固醇27-羟化酶兴奋剂以预防和/或减少再狭窄的量施用。本发明还包括使用27-羟基胆固醇治疗癌症的方法。

2. 发明授权

US5494901A Topical compositions for the eye comprising a .beta.-cyclodextrin derivative and a therapeutic agent 失效
公开(公告)号：US5494901A
公开(公告)日：1996-02-27
申请号：US935
申请日：1993-01-05
申请人： Jonathan C. Javitt , Norman B. Javitt , Peter McDonnell
发明人： Jonathan C. Javitt , Norman B. Javitt , Peter McDonnell
IPC分类号： A61K9/08 , A61K9/00 , A61K31/41 , A61K31/42 , A61K31/425 , A61K47/40 , A61P27/02 , A61P27/06 , A61K31/715 , A61K31/70
CPC分类号： A61K9/0048 , A61K31/42 , A61K31/425 , A61K47/40 , Y10S514/912 , Y10S514/913 , Y10S514/914 , Y10S514/915
摘要： A topical composition comprising an amount of a carbonic anhydrase inhibitor and an amount of .beta.-cyclodextrin derivative effective in increasing the bioavailability of the carbonic anhydrase inhibitor when coadministered topically to the eye.

3. 发明授权

US5773431A Administration of a 27-hydroxycholesterol or prodrug thereof as an anti-cancer agent 失效
标题翻译：施用27-羟基胆固醇或其前药作为抗癌剂
公开(公告)号：US5773431A
公开(公告)日：1998-06-30
申请号：US809435
申请日：1997-04-04
申请人： Norman B. Javitt
发明人： Norman B. Javitt
IPC分类号： A61K31/575 , A61K47/48 , C07H19/06 , A61K31/56
CPC分类号： A61K31/7072 , A61K31/575 , A61K47/48969 , B82Y5/00 , C07H19/06
摘要： A method for preventing or reducing restenosis wherein a 27-hydroxycholesterol or a 25,26 and/or 27-aminocholesterol, or a sterol 27-hydroxylase stimulant, is administered in a restenosis preventing and/or reducing amount. The invention also includes a method for treating cancer using 27-hydroxycholesterol.
摘要翻译：一种预防或减少再狭窄的方法，其中27-羟基胆固醇或25,26和/或27-氨基胆固醇或固醇27-羟化酶兴奋剂以预防和/或减少再狭窄的量施用。本发明还包括使用27-羟基胆固醇治疗癌症的方法。

4. 发明授权

US5376652A Administration of a 27-hydroxycholesterol or related compound or sterol-27-hydroxylase stimulant to prevent restenosis following vascular endothelial injury 失效
标题翻译：施用27-羟基胆固醇或相关化合物或甾醇-27-羟化酶刺激剂以防止血管内皮损伤后的再狭窄
公开(公告)号：US5376652A
公开(公告)日：1994-12-27
申请号：US159226
申请日：1993-11-30
申请人： Norman B. Javitt
发明人： Norman B. Javitt
IPC分类号： A61K31/575 , A61K47/48
CPC分类号： A61K31/7072 , A61K31/575 , A61K47/48969 , B82Y5/00
摘要： A method for preventing or reducing restenosis wherein a 27-hydroxycholesterol or a 25,26 and/or 27-aminocholesterol, or a sterol 27-hydroxylase stimulant is administered in a restenosis preventing and/or reducing amount.
摘要翻译：一种预防或减少再狭窄的方法，其中以预防和/或减少再狭窄的量施用27-羟基胆固醇或25,26和/或27-氨基胆固醇或甾醇27-羟化酶兴奋剂。

5. 发明授权

US4743597A Composition comprising an oxygenated cholesterol and use thereof for topical treatment of diseases 失效
标题翻译：包含氧合胆固醇的组合物及其用于局部治疗疾病的用途
公开(公告)号：US4743597A
公开(公告)日：1988-05-10
申请号：US822878
申请日：1986-01-27
申请人： Norman B. Javitt , Richard B. Stoughton
发明人： Norman B. Javitt , Richard B. Stoughton
IPC分类号： A61K31/56 , A61K31/575 , A61K47/22
CPC分类号： A61K9/0014 , A61K31/575 , A61K47/22 , Y10S514/863
摘要： The invention is directed to a pharmaceutical composition comprising an oxygenated cholesterol and a penetration-enhancing agent which is useful for topical application to the skin of a patient suffering from a proliferative skin disease characterized by geminative cells having a rapid rate of replication, e.g. psoriasis. The composition comprises an effective amount for the inhibition of germinative cell mitosis of an oxygenated cholesterol, e.g. 26-hydroxycholesterol, or a pharmaceutically effective derivative thereof e.g. an ester or ether. The invention is further directed to a method of treating a patient suffering from said skin disease comprising applying to the effected skin said therapeutic composition. The invention is also directed to the topical application of these compositions to the skin to decrease inflammation.
摘要翻译：本发明涉及包含含氧胆固醇和渗透增强剂的药物组合物，其可用于局部施用于患有以具有快速复制速率的联合细胞为特征的增殖性皮肤疾病的患者的皮肤，例如，银屑病。组合物包含用于抑制氧合胆固醇的发芽细胞有丝分裂的有效量，例如。 26-羟基胆固醇，或其药学上有效的衍生物，例如。酯或醚。本发明还涉及一种治疗患有所述皮肤疾病的患者的方法，其包括将所述治疗组合物施用于受影响的皮肤。本发明还涉及将这些组合物局部施用于皮肤以减少炎症。

6. 发明授权

US08741812B2 Class of sterol ligands and their uses in regulation of cholesterol and gene expression 有权
标题翻译：甾醇配体类及其在调节胆固醇和基因表达中的用途
公开(公告)号：US08741812B2
公开(公告)日：2014-06-03
申请号：US11212031
申请日：2005-08-25
申请人： Norman B. Javitt
发明人： Norman B. Javitt
IPC分类号： C40B30/04 , A61K49/00
CPC分类号： A61K49/00 , A61K31/56
摘要： This invention relates to novel physiological oxysteroids and oxysteroid hormones which are C27 modified sterols, particularly derivatives of intermediates in cholesterol synthesis, including lanosterol, zymosterol and desmosterol, including C27 diol and C27 acid derivatives, as well as related compounds and analogs thereof. The invention relates to treatment of cholesterol-related conditions by modulating the rate of cholesterol synthesis or cholesterol metabolism by administration of the oxysteroids, analogs or antagonists thereof. Methods are provided for ameliorating, treating or preventing macular degeneration by administering an agent which stimulates the expression or activity of steroid sulphotransferase (SLUT2), particularly SLUT2B1b, or which stimulates the expression or activity of CYP27A1 or sterol 27-hydroxylase. Assays for identification of analogs, antagonists or modulators of the oxysteroids or of sterol 27-hydroxylase are provided.
摘要翻译：本发明涉及新兴的生理甾类固醇激素和固醇类激素，它们是C27修饰的甾醇，特别是胆固醇合成中的中间体衍生物，包括羊毛甾醇，止痛精和止痛药，包括C27二醇和C27酸衍生物，以及相关化合物及其类似物。本发明涉及通过施用氧固醇类，类似物或拮抗剂调节胆固醇合成或胆固醇代谢的速率来治疗胆固醇相关病症。提供了通过施用刺激类固醇sulphotransferase（SLUT2）的表达或活性（SLUT2），特别是SLUT2B1b或刺激CYP27A1或甾醇27-羟化酶的表达或活性的药剂来改善，治疗或预防黄斑变性的方法。提供了用于鉴定类固醇，拮抗剂或氧化物固醇或甾醇27-羟化酶的调节剂的分析。

7. 发明授权

US4939134A 26-aminocholesterol and derivatives and analogs thereof in the regulation of cholesterol accumulation in body tissue 失效
标题翻译： 26-氨基胆固醇及其衍生物和类似物在体内组织中胆固醇积累的调节
公开(公告)号：US4939134A
公开(公告)日：1990-07-03
申请号：US246444
申请日：1988-09-19
申请人： Norman B. Javitt , Stephen R. Wilson
发明人： Norman B. Javitt , Stephen R. Wilson
IPC分类号： A61K31/575 , C07J9/00
CPC分类号： A61K31/575
摘要： This invention relates to cholesterol synthesis and to the accumulation and regulation of cholesterol levels in body tissue. More specifically, the invention provides that the compound 26-aminocholesterol, ##STR1## and analogs and derivatives thereof, exhibit biological activity as a potent inhibitor of cholesterol synthesis and/or cholesterol accumulation in body tissue. The compounds strongly inhibit of the enzyme HMGCoA reductase and low density lipoprotein accumulation by non-hepatic cells. Surprisingly, it has been discovered that 26-aminocholesterol is selective for fibroblast (plasma) cells, and has little or no effect on hepato (liver) cells. Therapeutic compounds according to the invention include substituted or unsubstituted sterols of the formula: ##STR2## wherein the carbon atoms at positions 5 and 6 of the sterol are one of saturated and unsaturated, R.sub.1 is one of a 3-hydroxyl group and a 3-keto group, R.sub.2 is one of a hydroxyl group and a keto group, and wherein at least one of R.sub.3, R.sub.4 and R.sub.5 is an amino group and the others are each selected from the group consisting of hydrogen and an amino group.
摘要翻译：本发明涉及胆固醇合成和身体组织中胆固醇水平的积累和调节。更具体地说，本发明提供化合物26-氨基胆固醇及其类似物及其衍生物作为胆固醇合成和/或体内组织中胆固醇积聚的有效抑制剂具有生物活性。该化合物强烈地抑制HMGCoA还原酶和非肝细胞的低密度脂蛋白积累。令人吃惊的是，已经发现26-氨基胆固醇对成纤维细胞（血浆）细胞是选择性的，并且对肝细胞（肝）细胞几乎没有或没有影响。根据本发明的治疗化合物包括具有下式的取代或未取代的甾醇：其中固醇的5和6位的碳原子是饱和和不饱和的之一，R 1是3-羟基和3- 酮基，R2是羟基和酮基之一，其中R3，R4和R5中的至少一个是氨基，其它各自选自氢和氨基。

8. 发明授权

US4427668A 26-Hydroxycholesterol and derivatives and analogs thereof in regulation of cholesterol accumulation in body tissue 失效
标题翻译： 26-羟基胆固醇及其衍生物和类似物在体内组织中胆固醇积累的调节
公开(公告)号：US4427668A
公开(公告)日：1984-01-24
申请号：US364338
申请日：1982-04-01
申请人： Norman B. Javitt
发明人： Norman B. Javitt
IPC分类号： A61K31/575 , A61P3/06 , A61P25/02 , A61P43/00 , C07J9/00 , A61K31/56
CPC分类号： A61K31/575
摘要： Use of 26-hydroxycholesterol for reducing cholesterol synthesis and/or accumulation in body tissues.
摘要翻译：使用26-羟基胆固醇来减少身体组织中的胆固醇合成和/或积累。

9. 发明授权

US5418225A Topical compositions for the eye comprising a .beta.-cyclodextrin derivative and a therapeutic agent 失效
标题翻译：包含β-环糊精衍生物和治疗剂的用于眼睛的局部组合物
公开(公告)号：US5418225A
公开(公告)日：1995-05-23
申请号：US935
申请日：1993-01-05
申请人： Jonathan C. Javitt , Norman B. Javitt , Peter McDonnell
发明人： Jonathan C. Javitt , Norman B. Javitt , Peter McDonnell
IPC分类号： A61K9/08 , A61K9/00 , A61K31/41 , A61K31/42 , A61K31/425 , A61K47/40 , A61P27/02 , A61P27/06 , A61K31/715 , A61K31/70
CPC分类号： A61K9/0048 , A61K31/42 , A61K31/425 , A61K47/40 , Y10S514/912 , Y10S514/913 , Y10S514/914 , Y10S514/915
摘要： A topical composition comprising an amount of a carbonic anhydrase inhibitor and an amount of .beta.-cyclodextrin derivative effective in increasing the bioavailability of the carbonic anhydrase inhibitor when coadministered topically to the eye.
摘要翻译：一种局部组合物，其包含一定量的碳酸酐酶抑制剂和一定量的β-环糊精衍生物，当局部地局部施用于眼睛时，可有效增加碳酸酐酶抑制剂的生物利用度。

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