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1. 发明申请

WO2003097626A1 MANUFACTURE OF ASCORBIC ACID ESTERS 审中-公开
标题翻译：抗坏血酸酯的制备
公开(公告)号：WO2003097626A1
公开(公告)日：2003-11-27
申请号：PCT/EP2003/004907
申请日：2003-05-12
申请人： ROCHE VITAMINS AG , STAMM, Thomas
发明人： STAMM, Thomas
IPC分类号： C07D307/62
CPC分类号： C07D307/62
摘要： A process for the isolation of substantially pure ascorbyl-6-fatty acid ester from the products obtained by the sulphuric acid-catalyzed esterification of ascorbic acid with fatty acids comprises extracting with diethyl ketone such reaction products from the mixture remaining after the esterification reaction, hydrolysing the sulphate ester by-products in the diethyl ketone extract, removing the generated sulphuric acid from the product of this hydrolysis, isomerizing the ascorbyl-5-fatty acid ester by-product to the desired ascorbyl-6-fatty acid ester by acid catalysis in a non-polar aprotic organic solvent, and recovering the accumulated ascorbyl-6-fatty acid ester. As another aspect, the present invention provides a process for the manufacture of fatty acid esters of ascorbic acid, said process comprising the initial step of reacting ascorbic acid or an alkali metal or alkaline earth metal salt thereof with a fatty acid or with a lower alkyl ester or an alkali metal salt or alkaline earth metal thereof in concentrated sulphuric acid, and subsequent steps based on the above-described isolation process.
摘要翻译：从由抗坏血酸与脂肪酸的硫酸催化酯化获得的产物中分离基本上纯的抗坏血酸-6-脂肪酸酯的方法包括用二乙基酮萃取来自在酯化反应后残留的混合物的反应产物，水解二乙基酮提取物中的硫酸酯副产物，从该水解产物中除去产生的硫酸，通过酸催化将抗坏血酸-5-脂肪酸酯副产物异构化成所需的抗坏血酸-6-脂肪酸酯非极性非质子有机溶剂，并回收积累的抗坏血酸-6-脂肪酸酯。另一方面，本发明提供了制备抗坏血酸的脂肪酸酯的方法，所述方法包括将抗坏血酸或其碱金属或碱土金属盐与脂肪酸或低级烷基反应的初始步骤酯或其在浓硫酸中的碱金属盐或碱土金属，以及基于上述分离方法的后续步骤。

2. 发明申请

WO2003078399A1 PROCESS FOR ASYMMETRIC HYDROGENATION OF HEXAHYDROQUINOLINE SALTS 审中-公开
标题翻译：六氢喹啉盐不对称加氢方法
公开(公告)号：WO2003078399A1
公开(公告)日：2003-09-25
申请号：PCT/EP2003/002610
申请日：2003-03-13
申请人： ROCHE VITAMINS AG , PUENTENER, Kurt , SCALONE, Michelangelo , WANG, Shaoning
发明人： PUENTENER, Kurt , SCALONE, Michelangelo , WANG, Shaoning
IPC分类号： C07D217/20
CPC分类号： C07D217/20
摘要： The asymmetrical hydrogenation of 1-(4-methoxybenzyl)-3,4,5,6,7,8-hexahydroisoquinolinium salts to yield (S) or (R)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-hexahydroisoquinolinium salts can be effected with superior optical yield by the use of an iridium or rhodium complex catalyst comprising a chiral dipohsphine ligand of the general formula (I) or (II), (S)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-hexahydroisoquinoline and salts thereof are intermediate products in the manufacture of dextromethorphan, a known antitussive agent.
摘要翻译： 1-（4-甲氧基苄基）-3,4,5,6,7,8-六氢异喹啉鎓盐的不对称氢化反应得到（S）或（R）-1-（4-甲氧基苄基）-1,2,3， 4,5,6,7,8-六氢异喹啉鎓盐可以通过使用包含通式（I）或（II），（S） - （II）的手性二硫代吗啡配体的铱或铑配合物催化剂， 1-（4-甲氧基苄基）-1,2,3,4,5,6,7,8-六氢异喹啉及其盐是制备右美沙芬的中间产物，右美沙芬是已知的止咳剂。

3. 发明申请

WO03070959A2 PROCESS FOR PRODUCING LEVODIONE 审中-公开
标题翻译：生产LEVODIONE的工艺
公开(公告)号：WO03070959A2
公开(公告)日：2003-08-28
申请号：PCT/EP0301537
申请日：2003-02-15
申请人： ROCHE VITAMINS AG , SHIMIZU SAKAYU , WADA MASARU
发明人： SHIMIZU SAKAYU , WADA MASARU
IPC分类号： C12N15/09 , C12N9/02 , C12N15/53 , C12P7/26 , C12P
CPC分类号： C12P7/26
摘要： An enone reductase characterized by a molecular mass of 61,300 5,000 Da NADPH and NADH as co-factor a temperature optimum of 55-60 C at pH 7.4 a pH optimum of 4.5-8.5 and a substrate specificity on alpha,beta-unsaturated ketones, especially derived from a yeast and a process for the preparation of levodione from ketoisophorane.
摘要翻译：一种烯酮还原酶，其分子质量为61,300 5,000Da NADPH和NADH作为辅助因子，pH 7.4时的最适温度为55-60℃，pH最佳值为4.5-8.5，对α，β-不饱和酮特别是底物特异性衍生自酵母和由酮异佛烷制备左旋二酮的方法。

4. 发明申请

WO2003070924A1 ENONE REDUCTASE 审中-公开
标题翻译：降低成本
公开(公告)号：WO2003070924A1
公开(公告)日：2003-08-28
申请号：PCT/EP2003/001473
申请日：2003-02-14
申请人： ROCHE VITAMINS AG , KATAOKA, Michihiko , SHIMIZU, Sakayu
发明人： KATAOKA, Michihiko , SHIMIZU, Sakayu
IPC分类号： C12N9/02
CPC分类号： C12N9/001 , C12P7/26
摘要： An isolated enone reductase characterized by a molecular mass of 61300 +/- 5000 Da; NADPH and NADH as co-factor; a temperature optimum of 55-60 °C at pH 7.4 ; a pH optimum of 4.5-8.5 and substrate specificity on ∝,β-unsatured ketones; a process for producing it from a microorganism and a process for producing levodione from ketoisophorone using such reductase.
摘要翻译：分离的烯酮还原酶的特征在于分子量为61300 +/- 5000Da NADPH和NADH作为辅因子，pH 7.4时的最适温度为55-60℃，pH最佳为4.5-8.5，底物特异性为prop，未成熟的酮是由微生物生产的方法，以及使用这种还原酶从酮异二酮生产左旋二酮的方法。

5. 发明申请

WO03022071A3 COLORANT FOR FOOD AND PHARMACEUTICALS 审中-公开
标题翻译：着色剂用于食品和药物
公开(公告)号：WO03022071A3
公开(公告)日：2003-08-28
申请号：PCT/EP0209913
申请日：2002-09-04
申请人： ROCHE VITAMINS AG , BECK MARKUS IVO , BERNHARD KURT , GIGER ALFRED , LEUENBERGER BRUNO
发明人： BECK MARKUS IVO , BERNHARD KURT , GIGER ALFRED , LEUENBERGER BRUNO
IPC分类号： A23L1/00 , A23L1/275 , A61K9/08 , A61K9/10 , A61K9/107 , A61K9/20 , A61K9/48 , A61K36/00 , A61K36/185 , A61K36/286 , A61K36/31 , A61K36/48 , A61K36/889 , A61K36/899 , A61K47/04 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/20 , A61K47/22 , A61K47/26 , A61K47/36 , A61K47/42 , C07C403/24 , C09B61/00 , C09B67/02 , C09B67/46 , A61K35/78 , C07C175/00
CPC分类号： C09B61/00 , A23L5/44 , A61K36/185 , A61K36/286 , A61K36/31 , A61K36/48 , A61K36/889 , A61K36/899 , A61K2300/00
摘要： The use of alpha -zeacarotene, beta -zeacarotene or a mixture of both as a colouring agent for food or pharmaceutical compositions. For addition to the food or pharmaceutical composition or otherwise incorporation therein during its preparation the zeacarotene (mixture) is generally first formulated to a solid or liquid colorant composition in the form of a stable water-soluble or -dispersible powder, an aqueous colloidal solution or oil-in-water dispersion of such a powder, an oil-in-water dispersion of the zeacarotene (mixture), or an oil-soluble dispersion of the zeacarotene (mixture) in a triglyceride. In a solid colorant composition the the zeacarotene (mixture) is generally finely dispersed in a matrix or carrier. Such colorant compositions may be prepared by homogenizing, in an aqueous or colloidal solution of a carrier and optionally one or more water-soluble excipients and/or adjuvants, a solution or dispersion of the zeacarotene (mixture) and optionally one or more fat-soluble excipients and/or adjuvants in a triglyceride or an organic solvent, or in a mixture of both triglyceride and organic solvent, and, if required, converting the so obtained dispersion into a solid composition. The colorant compositions, their processes of preparation and the food or pharmaceutical compositions which comprise the zeacarotene (mixture) as the colouring agent are further aspects of this invention.
摘要翻译： α-泽卡萨汀，β-泽可罗汀或两者的混合物作为食品或药物组合物的着色剂的用途。为了在食品或药物组合物中加入或以其它方式掺入其中，通常首先将zeacarotene（混合物）配制成固体或液体着色剂组合物，其形式为稳定的水溶性或分散性粉末，胶体水溶液或这种粉末的水包油分散体，玉米赤霉烯酮（混合物）的水包油分散体或玉米赤铜
矿（混合物）在甘油三酯中的油溶性分散体。在固体着色剂组合物中，该zeacarotene（混合物）通常很好地分散在基质或载体中。这样的着色剂组合物可以通过在载体和任选的一种或多种水溶性赋形剂和/或佐剂的水性或胶体溶液中匀化玉米黄质（混合物）的溶液或分散体和任选的一种或多种脂溶性赋形剂和/或佐剂在甘油三酯或有机溶剂中，或在甘油三酸酯和有机溶剂的混合物中，并且如果需要，将如此获得的分散体转化成固体组合物。着色剂组合物，它们的制备方法以及包含玉米赤道酮（混合物）作为着色剂的食物或药物组合物是本发明的另一方面。

6. 发明申请

WO2003022071A2 COLORANT FOR FOOD AND PHARMACEUTICALS 审中-公开
标题翻译：食品和药物的着色剂
公开(公告)号：WO2003022071A2
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009913
申请日：2002-09-04
申请人： ROCHE VITAMINS AG , BECK, Markus, Ivo , BERNHARD, Kurt , GIGER, Alfred , LEUENBERGER, Bruno
发明人： BECK, Markus, Ivo , BERNHARD, Kurt , GIGER, Alfred , LEUENBERGER, Bruno
IPC分类号： A23L
CPC分类号： C09B61/00 , A23L5/44 , A61K36/185 , A61K36/286 , A61K36/31 , A61K36/48 , A61K36/889 , A61K36/899 , A61K2300/00
摘要： The use of α-zeacarotene, β-zeacarotene or a mixture of both as a colouring agent for food or pharmaceutical compositions. For addition to the food or pharmaceutical composition or otherwise incorporation therein during its preparation the zeacarotene (mixture) is generally first formulated to a solid or liquid colorant composition in the form of a stable water-soluble or -dispersible powder, an aqueous colloidal solution or oil-in-water dispersion of such a powder, an oil-in-water dispersion of the zeacarotene (mixture), or an oil-soluble dispersion of the zeacarotene (mixture) in a triglyceride. In a solid colorant composition the the zeacarotene (mixture) is generally finely dispersed in a matrix or carrier. Such colorant compositions may be prepared by homogenizing, in an aqueous or colloidal solution of a carrier and optionally one or more water-soluble excipients and/or adjuvants, a solution or dispersion of the zeacarotene (mixture) and optionally one or more fat-soluble excipients and/or adjuvants in a triglyceride or an organic solvent, or in a mixture of both triglyceride and organic solvent, and, if required, converting the so obtained dispersion into a solid composition. The colorant compositions, their processes of preparation and the food or pharmaceutical compositions which comprise the zeacarotene (mixture) as the colouring agent are further aspects of this invention.
摘要翻译： β-胡萝卜素，β-卡必妥因或二者的混合物作为食品或药物组合物的着色剂的用途。为了加入食品或药物组合物或在其制备过程中以其它方式并入其中，将玉米角胡萝卜素（混合物）通常首先以稳定的水溶性或可分散粉末，水性胶体溶液或水溶性溶液形式配制成固体或液体着色剂组合物这种粉末的水包油分散体，玉米黄素（混合物）的水包油分散体，或马来酸罗丹汀（混合物）的油溶性分散体在甘油三酯中。在固体着色剂组合物中，玉米角质素（混合物）通常细分散在基质或载体中。这样的着色剂组合物可以通过在载体和任选的一种或多种水溶性赋形剂和/或佐剂的水溶液或胶体溶液中均匀化，将玉米胡萝卜素（混合物）的溶液或分散体和任选的一种或多种脂溶性甘油三酯或有机溶剂中的赋形剂和/或佐剂，或甘油三酯和有机溶剂的混合物，如果需要，将所得分散体转化成固体组合物。着色剂组合物，其制备方法以及包含作为着色剂的zeahrotrot（混合物）的食品或药物组合物是本发明的另外的方面。

7. 发明申请

WO2002102298A3 PROCESS FOR THE PREPARATION OF DISPERSIONS 审中-公开
公开(公告)号：WO2002102298A3
公开(公告)日：2002-12-27
申请号：PCT/EP2002/006328
申请日：2002-06-10
申请人： ROCHE VITAMINS AG , SCHAFFNER, David
发明人： SCHAFFNER, David
IPC分类号： A61K31/07
摘要： The present invention relates to a process of a dispersion of an active substance or composition in an aqueous phase which comprises dispersing in an aqueous phase a solution of such substance or composition in dimethylether or in a C4-hydrocarbon or mixtures thereof in super-or nearcritical state, decompressing the mixture and separating the dispersion from the gaseous solvent.

8. 发明申请

WO2002089756A1 DENTRIFICE 审中-公开
标题翻译：洁牙
公开(公告)号：WO2002089756A1
公开(公告)日：2002-11-14
申请号：PCT/EP2002/004898
申请日：2002-05-04
申请人： ROCHE VITAMINS AG , WESTENFELDER, Horst
发明人： WESTENFELDER, Horst
IPC分类号： A61K7/22
CPC分类号： A61Q11/00 , A61K8/44 , A61K8/676 , A61K2800/59
摘要： A dentifrice containing an ascorbic acid derivative and ethylenediaminetetraacetic acid or a salt thereof.
摘要翻译：含有抗坏血酸衍生物和乙二胺四乙酸的洁齿剂或其盐。

9. 发明申请

WO2002062771A1 NOVEL 2-BENZOXAZOLYL BENZENE DERIVATIVES AND THEIR USE AS UV SCREENING AGENTS 审中-公开
标题翻译：新型2-苯并恶唑苯并噻吩衍生物及其作为紫外线杀菌剂的用途
公开(公告)号：WO2002062771A1
公开(公告)日：2002-08-15
申请号：PCT/EP2002/000847
申请日：2002-01-28
申请人： ROCHE VITAMINS AG , HUBER, Ulrich
发明人： HUBER, Ulrich
IPC分类号： C07D263/62
CPC分类号： A61K8/49 , A61Q17/04 , C07C233/75 , C07D263/64 , C07F7/0854
摘要： Novel benzoxazolyl benzene derivatives of formula (I) wherein R 1 is hydrogen, C 1-20 -alkyl or C 2-20 -alkenyl; R 2 and R 3 are independently a group -C(R 4 , R 5 )C(R 6 )=C(R 7 , R 8 ) (a) or a group -C(R 4' ,R 5' )CH(R 6' )CH(R 7' ,R 8' ) (b), wherein R 4 , R 5 , R 6 , R 7 , R 8 , R 4' , R 6' , R 7' and R 8' are independently, hydrogen, C 1-10 -alkyl or C 2-10 -alkenyl, or C 2-10 -alkyl or C 3-10 -alkenyl containing at least one oxygen atom interrupting the hydrocarbon chain; or wherein R 4 , R 5 , R 6 , R 4' , R 5' and R 6' are hydrogen, C 1-10 -alkyl or C 2-10 alkyl containing at least one oxygen atom interrupting the hydrocarbon chain, or alkyl substituted by a silane or oligosiloxane moiety, and one of R 7 and R 8 or R 7' and R 8' is a silane or oligosiloxane moiety and the other one of R 7 and R 8 or R 7' and R 8' is hydrogen; and X is phenylene or naphthylene, or substituted phenylene or naphthylene for use as UV screening agents for protecting human skin or hair against UV radiation, and in UV screening compositions, particularly topical compositions for cosmetic or dermatological use.
摘要翻译：式（I）的新型苯并恶唑基苯衍生物，其中R 1是氢，C 1-20 - 烷基或C 2-20 - 烯基; R 2和R 3独立地是基团-C（R 4，R 5）C（R 6）= C（R 7，R 8）（a）或基团-C（R 4'，R 5'）CH（R 6'）CH（R 7'，R 8'）（b），其中R 4，R R 5，R 7，R 8，R 4'，R 6'，R 7'和R 8'独立地是氢，C 1-10 或含有至少一个中断烃链的氧原子的C 2-10 - 烷基或C 2-10 - 烯基; 或其中R 4，R 5，R 6，R 4'，R 5'和R 6'是氢，至少含有C 1-10 - 烷基或C 2-10烷基一个中断烃链的氧原子或被硅烷或低聚硅氧烷部分取代的烷基，R 7和R 8或R 7'和R 8'之一是硅烷或低聚硅氧烷部分， R 7和R 8或R 7'和R 8'中的另一个是氢; 并且X是亚苯基或亚萘基，或取代的亚苯基或亚萘基，用作用于保护人类皮肤或头发免受紫外线辐射的UV屏蔽剂，以及UV屏蔽组合物，特别是用于化妆品或皮肤病学用途的局部组合物。

10. 发明申请

WO2003086340A1 ORGANOSILICONE DERIVATIVES OF AMINO HYDROXYBENZOPHENONES AND THEIR USE AS UV-A FILTERS IN COSMETIC PREPARATIONS 审中-公开
标题翻译：氨基羟基苯并噻唑的有机硅酮衍生物及其作为化妆品制剂中的UV-A过滤剂使用
公开(公告)号：WO2003086340A1
公开(公告)日：2003-10-23
申请号：PCT/EP2003/003095
申请日：2003-03-25
申请人： ROCHE VITAMINS AG , BERG-SCHULTZ, Katja , HUBER, Ulrich
发明人： BERG-SCHULTZ, Katja , HUBER, Ulrich
IPC分类号： A61K7/42
CPC分类号： A61K8/898 , A61K8/585 , A61K8/8152 , A61K2800/57 , A61Q17/04 , C07F7/0818 , C08G77/388
摘要： The present invention relates to organosilicone derivatives of amino hydroxybenzophenones, a process for their preparation thereof, a cosmetic compositions comprising the organosilicone derivative and the use thereof for protecting hair and/or skin from damage caused by UV-A irradiation.
摘要翻译：本发明涉及氨基羟基二苯甲酮的有机硅氧烷衍生物，其制备方法，包含有机硅酮衍生物的化妆品组合物及其用于保护毛发和/或皮肤免受UV-A照射引起的损伤的用途。

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