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1. 发明专利

AU2002217070B2 Method for the production of fatty acid esters 未知
公开(公告)号：AU2002217070B2
公开(公告)日：2005-10-13
申请号：AU2002217070
申请日：2001-11-29
申请人： WESTFALIA SEPARATOR AG
发明人： FRISCHE RAINER , BRUNNER KARLHEINZ , RICKER RAINER
IPC分类号： B01D17/02 , C11B3/00 , C11B3/04 , C11B3/06 , C11C3/00 , C11C3/04 , C11C003/00 , C11C003/04 , C10L001/18
摘要： A method for the production of fatty acid esters of primary and/or secondary alcohols from raw, unpurified oils or fats containing free fatty acids and slimy substances or from waste oils loaded with free fatty acids from the food industry. Acidic catalytic esterification is performed on the free fatty acids along with extensive deactivation of the slimy substances present with respect to the disadvantageous emulsion-forming property thereof, whereby a water-free primary and/or secondary alcohol and a highly acidic hygroscopic catalyst are added to the starting substance in the form of crude oil or fat or waste oil, the reaction product is rinsed with glycol from a prior alkaline transesterification, whereupon alkaline transesterification occurs for the unmodified remaining glyceridically bound fatty acids in the reaction product of the acidic-catalytic esterification process.

2. 发明申请

US20020103192A1 Inhibitors of histone deacetylase 审中-公开
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US20020103192A1
公开(公告)日：2002-08-01
申请号：US09808389
申请日：2001-03-14
发明人： Michael L. Curtin , Steven K. Davidsen , Robin R. Frey , Howard R. Heyman , Michael R. Michaelides , Anil Vasudevan , Carol K. Wada
IPC分类号： C11C003/00 , A61K031/54 , A61K031/541 , A61K031/5375 , A61K031/5377 , A61K031/495 , A61K031/496 , A61K031/421 , A61K031/426 , A61K031/277 , A61K031/16
CPC分类号： C07D213/30 , C07C45/29 , C07C45/30 , C07C45/45 , C07C45/515 , C07C45/673 , C07C47/277 , C07C49/255 , C07C59/90 , C07C69/716 , C07C235/14 , C07C235/16 , C07C235/20 , C07C235/74 , C07C235/80 , C07C243/38 , C07C255/54 , C07C255/60 , C07C311/19 , C07C317/32 , C07C317/44 , C07C323/41 , C07C323/60 , C07C2601/14 , C07C2603/18 , C07C2603/74 , C07D209/08 , C07D209/42 , C07D213/40 , C07D213/75 , C07D215/38 , C07D231/40 , C07D235/06 , C07D257/04 , C07D263/14 , C07D263/32 , C07D263/58 , C07D271/10 , C07D277/46 , C07D277/56 , C07D277/74 , C07D277/82 , C07D285/08 , C07D295/112 , C07D307/68 , C07D307/85 , C07D317/58 , C07D317/66 , C07D317/68 , C07D413/04 , C07D413/12 , C07D417/04 , C07D491/10
摘要： Substituted trifluoromethyl ketones, ketooxazoles, ketoamides, ketoesters, and diketones having the formula 1 or therapeutically acceptable salts thereof, are histone deacetylase (HDAC) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed.
摘要翻译：组氨酸脱乙酰酶（HDAC）抑制剂是取代的三氟甲基酮，酮唑酮，酮酰胺，酮酯和具有下式的治疗上可接受的盐的二酮。公开了化合物的制备，含有该化合物的组合物以及使用该化合物治疗疾病。

3. 发明申请

US20040044050A1 Analogues of lipid mediators derived from omega-3 PUFAs and methods of use 有权
标题翻译：衍生自ω-3 PUFA的脂质介体的类似物和使用方法
公开(公告)号：US20040044050A1
公开(公告)日：2004-03-04
申请号：US10460913
申请日：2003-06-13
发明人： Daniel W. Goodman , Michael R. Hanley , Stuart L. Bursten
IPC分类号： C11C003/00 , C11D001/28 , A61K031/44 , A61K031/40
CPC分类号： C07C59/68 , C07C59/42 , C07C59/48 , C07C59/64 , C07C69/732 , C07C69/736 , C07C235/28 , C07C235/34
摘要： The present invention is directed to compounds that are analogues of lipid mediators derived from a fish oil-derived fatty acid, eicosapentaenoic acid nullC20:5 null-3; EPAnull, but with a longer tissue half-life and enhanced bioactivity. These analogues may be used to treat inflammatory, angioproliferative, cardiovascular, thrombophlebotic, vascular, ocular, dermatologic, neurodegenerative, pulmonary, endocrine, reproductive, rheumatologic and gastrointestinal diseases.
摘要翻译：本发明涉及衍生自鱼油衍生的脂肪酸，二十碳五烯酸[C20：5ω-3; EPA]，但具有更长的组织半衰期和增强的生物活性。这些类似物可用于治疗炎症，血管增生，心血管，血栓形成，血管，眼，皮肤病，神经变性，肺，内分泌，生殖，风湿病和胃肠道疾病。

4. 发明申请

US20020120159A1 Process for the preparation of a monoglyceride 有权
公开(公告)号：US20020120159A1
公开(公告)日：2002-08-29
申请号：US09796083
申请日：2001-02-28
申请人： CONCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
发明人： Narayana Balagopala Kaimal Thengumpillil , Vijayalakshmi Penumarthy , Ananta Laxmi Ayyagari
IPC分类号： C11C003/00
CPC分类号： C11C3/02 , C07C67/08 , C07C69/30
摘要： An improved process for the preparation of a monoglyceride by reacting a fatty acid and glycerol in the presence of a food grade polar solvent and avoiding the use of catalysts is provided.

5. 发明申请

US20010056116A1 Dopamine analog amide 失效
标题翻译：多巴胺类似物酰胺
公开(公告)号：US20010056116A1
公开(公告)日：2001-12-27
申请号：US09901209
申请日：2001-07-09
发明人： Victor Shashoua
IPC分类号： A61K038/00 , C11C003/00 , C07K005/00 , A61K031/5513 , A61K031/16
CPC分类号： A61K31/165 , A61K31/135 , A61K38/00 , A61K47/54 , A61K47/542 , C11C3/003 , C11C3/04
摘要： The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.
摘要翻译：本发明涉及从脂肪酸载体和神经活性药物形成前体药物。前药在胃和血液两者的环境中是稳定的，并且可以通过摄入来递送。前药容易通过血脑屏障。一旦在中枢神经系统中，前药被水解成脂肪酸载体和药物以释放药物。在优选的实施方案中，载体是4,7,10,13,16,19，二十二碳六烯酸，并且该药物是多巴胺。两者都是中枢神经系统的正常组成部分。药物和载体之间的共价键优选是酰胺键，其键可以在胃中的条件下存活。因此，前药可以被摄入并且不会完全水解成胃中的载体分子和药物分子。

6. 发明申请

US20010018533A1 Process for producing 13-cis retinoic acid 审中-公开
标题翻译：生产13-顺式视黄酸的方法
公开(公告)号：US20010018533A1
公开(公告)日：2001-08-30
申请号：US09484675
申请日：2000-01-18
发明人： Xiu C. Wang , Ashok V. Bhatia , Azad Hossain , Timothy B. Towne
IPC分类号： C11C003/00
CPC分类号： C07C403/20 , C07B2200/09 , C07C2601/16
摘要： The process of the present invention relates to a process for producing 1 3-cis retinoic acid. The process of the present invention involves reacting a Wittig salt in a solvent with a butenolide in the presence of a weak base and optionally, a Lewis acid.
摘要翻译：本发明的方法涉及一种生产13-顺式视黄酸的方法。本发明的方法包括在弱碱和任选的路易斯酸的存在下使Wittig盐在溶剂中与丁烯内酯反应。

7. 发明申请

US20040028638A1 Carboxylic acid-type lipid 失效
标题翻译：羧酸型脂质
公开(公告)号：US20040028638A1
公开(公告)日：2004-02-12
申请号：US10416275
申请日：2003-07-02
发明人： Eishun Tsuchida , Shinji Takeoka , Keitaro Sou , Haruki Ohkawa , Katsura Mori
IPC分类号： A61K007/075 , A61K007/08 , C11C003/00
CPC分类号： A61K9/1272 , C07C69/44 , C07C69/704 , C07C233/47 , C07C237/22 , C07C323/52 , C07C323/60 , C07H13/04 , C07H15/04
摘要： As a negatively charged lipid that can stably add negative charges to the surface of vesicles without side effects, the carboxyl acid-type lipid of the following general formula null1null 1 nullwherein R1, R2 and R3 represent substituents of which one is represented by the following general formula nullXnull: 2 (wherein M is a hydrogen atom or monovalent cation, and m is an integer of 1 to 5 that represents the methylene chain length), and the other two are chained hydrocarbon groups; A1, A2 and A3 are the same or different substituents selected from the group consisting of C(O)O, CONH or NHCO; and n is an integer of 1 to 3 that represents the methylene chain length) is provided.
摘要翻译：作为能够在没有副作用的情况下能够稳定地向囊泡表面添加负电荷的带负电荷的脂质，以下通式[1]的羧酸型脂质[其中，R1，R2和R3表示取代基，以下通式[X]：（其中M为氢原子或一价阳离子，m为代表亚甲基链长度的1〜5的整数），另外两个为链状烃基; A1，A2和A3是相同或不同的选自C（O）O，CONH或NHCO的取代基; 并且n是表示亚甲基链长度的1〜3的整数）。

8. 发明申请

US20040019229A1 Process for preparing acyloxybenzenesulfonates 失效
标题翻译：酰氧基苯磺酸盐的制备方法
公开(公告)号：US20040019229A1
公开(公告)日：2004-01-29
申请号：US10431951
申请日：2003-05-08
申请人： Clariant GmbH
发明人： Gerd Reinhardt , Peter Naumann , Alexander Lerch , Wolf-Dieter Mueller , Narayan D. Sadanani
IPC分类号： C11C003/00 , C07C39/42
CPC分类号： C07C303/32 , C07C303/22 , C07C309/42
摘要： A process for preparing acyloxybenzenesulfonates by reacting anhydrous phenolsulfonates with carboxylic acid derivatives comprises conducting the reaction with a salt of a phenolsulfonic acid which has a water content of less than 0.5% by weight and has been contacted with a substance having basic properties.
摘要翻译：通过使无水苯磺酸盐与羧酸衍生物反应制备酰氧基苯磺酸盐的方法包括与水含量小于0.5重量％的苯酚磺酸盐进行反应，并与具有碱性的物质接触。

9. 发明申请

US20030078417A1 Cytoprotective compounds 失效
公开(公告)号：US20030078417A1
公开(公告)日：2003-04-24
申请号：US10043641
申请日：2002-01-10
发明人： Richard C. Franson , Raphael M. Ottenbrite
IPC分类号： C11C003/00 , C07H013/06 , C07F009/02
CPC分类号： C07C309/15 , C07C69/732 , C07C219/08 , C07C229/16 , C07C233/38 , C07C235/28 , C07C309/14
摘要： The present invention provides compositions and methods for protecting cells from injury due to intrinsic membrane lysis, oxidation and/or invasion by destructive agents. Even more particularly, the present invention provides compositions and methods for treating or prophylactically inhibiting phospholipase mediated injury, injury due to oxidation, and inflammation. In a very specific sense, this invention provides compositions and methods of making these compositions that are inhibitors of phospholipase.

10. 发明申请

US20020143196A1 Histone deacetylase inhibitors 有权
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US20020143196A1
公开(公告)日：2002-10-03
申请号：US09812944
申请日：2001-03-27
发明人： Hsuan-Yin Lan-Hargest , Robert J. Kaufman , Norbert L. Wiech
IPC分类号： C07D307/02 , C11C003/00 , C07C233/01
CPC分类号： C07C57/42 , A61K31/16 , C07C57/60 , C07C259/06 , C07D307/54
摘要： Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Inhibition of histone deacetylase can lead to the histone deacetylase-mediated transcriptional repression of tumor suppressor genes. For example, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, such as hematopoiesis, and genetic related metabolic disorders, such as, cystic fibrosis and adrenoleukodystrophy.
摘要翻译：具有锌结合部分的化合物，例如异羟肟酸基团，可以抑制组蛋白脱乙酰酶。组蛋白脱乙酰酶抑制可抑制基因表达，包括与肿瘤抑制相关的基因的表达。组蛋白脱乙酰酶的抑制可导致组蛋白去乙酰酶介导的抑制肿瘤基因的转录抑制。例如，组蛋白脱乙酰酶的抑制可以提供用于治疗癌症，血液学疾病例如造血作用和遗传相关代谢紊乱（例如囊性纤维化和肾上腺脑白质营养不良）的替代途径。

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