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1. 发明授权

US06784302B2 Method of producing optically active lactone compound and complex used in the method 失效
标题翻译：在该方法中使用的光学活性内酯化合物和络合物的制造方法
公开(公告)号：US06784302B2
公开(公告)日：2004-08-31
申请号：US10405603
申请日：2003-04-03
申请人： Tsutomu Katsuki , Akira Watanabe , Tatsuya Uchida
发明人： Tsutomu Katsuki , Akira Watanabe , Tatsuya Uchida
IPC分类号： C07D30793
CPC分类号： C07D315/00 , C07F7/003
摘要： An optically active lactone compound is produced by using a Zr(salen) complex of the following formula (I) or its enantiomer as a catalyst and subjecting a cyclic ketone compound to a Baeyer-Villiger reaction with at least one oxidizer selected from hydrogen peroxide, aqueous hydrogen peroxide and urea-hydrogen peroxide adduct in a solvent: wherein Ar1 is an aryl group having a carbon number of 10 to 16 and Y is a phenoxy group or an alkoxy group having a carbon number of 1 to 10.
摘要翻译：通过使用下述式（I）的Zr（salen）配合物或其对映异构体作为催化剂并使环酮化合物与Baeyer-Villiger反应与至少一种选自过氧化氢的氧化剂反应来制备光学活性的内酯化合物，过氧化氢水溶液和脲 - 过氧化氢加合物，其中Ar 1是碳原子数为10〜16的芳基，Y为苯氧基或碳数为1〜10的烷氧基。

2. 发明授权

US06462077B1 Thromboxane ligands without blood clotting side effects 失效
标题翻译：血凝素配体无凝血副作用
公开(公告)号：US06462077B1
公开(公告)日：2002-10-08
申请号：US09899713
申请日：2001-07-05
申请人： Robert M. Burk , Achim H-P Krauss , David F. Woodward
发明人： Robert M. Burk , Achim H-P Krauss , David F. Woodward
IPC分类号： C07D30793
CPC分类号： C07D307/00 , A61K31/558 , C07D319/08 , C07D493/08
摘要： A method of treating ocular hypotension, hypertension, hemorrhage, myocardial ischemia, angina pectoris, coronary contraction, cerebrovascular contraction after subarachnoidal hemorrhage, cerebral hemorrhage and asthma which comprises administering to a mammal suffering therefrom a therapeutically effective amount of a thromboxane ligand which is a compound formula I, wherein Y is (CH2)x; Z is selected from the group consisting of O, OCH2, and (CR2)x, x is an integer of 1 or 2; n is 0 or 1; R2 is hydrogen or an alkyl radical of from 1 to 4 carbons; A is an alkylene or alkenylene radical having from two to seven carbon atoms, which radical may be substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups or said alkylene or alkenylene may have one or more enchained oxa or imino radicals; B is a methyl radical or a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroaryl radicals wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms, or substituted derivatives of said methyl, cycloalkyl or aryl radicals wherein said substituent is selected from the group consisting of halo, nitro, amino, thiol, hydroxy, alkyloxy and alkylcarboxy; and X is selected from the group consisting of nitro, cyano, —COOR, —CH2OR1, —C(O)N(R1)2, —CH2N(R1)2 —CH═N—OH and —CH2SR1 radicals wherein R is a C1 to C10 alkyl, phenyl or benzyl and R1 is R or hydrogen; or a pharmaceutically acceptable salt thereof
摘要翻译：一种治疗眼低血压，高血压，出血，心肌缺血，心绞痛，冠状动脉收缩，蛛网膜下腔出血后脑血管收缩，脑出血和哮喘的方法，其包括向患有其的哺乳动物施用治疗有效量的作为化合物的血栓烷配体式I，其中Y是（CH 2）x; Z选自O，OCH 2和（CR 2）x，x为1或2的整数; n为0或1; R2是氢或1至4个碳的烷基; A是具有2-7个碳原子的亚烷基或亚烯基，该基团可以被一个或多个羟基，氧代，烷氧基或烷基羧基取代，或者所述亚烷基或亚烯基可以具有一个或多个链烯氧基或亚氨基; B是具有3至7个碳原子的甲基或环烷基，或选自烃基芳基和杂芳基的芳基，其中杂原子选自氮，氧和硫原子，或所述甲基，环烷基或芳基的取代衍生物，其中所述取代基选自卤素，硝基，氨基，硫醇，羟基，烷氧基和烷基羧基; 并且X选自硝基，氰基，-COOR，-CH 2 OR 1，-C（O）N（R 1）2，-CH 2 N（R 1）2 -CH = N-OH和-CH 2 S R 1基团，其中R为 C1至C10烷基，苯基或苄基，R1为R或氢; 或其药学上可接受的盐

3. 发明授权

US06376684B1 Stereoselective process for alkyl phenylglycolic acids 有权
标题翻译：烷基苯基乙醇酸的立体选择性方法
公开(公告)号：US06376684B1
公开(公告)日：2002-04-23
申请号：US09711776
申请日：2000-11-13
申请人： Chris Hugh Senanayake , Paul T. Grover
发明人： Chris Hugh Senanayake , Paul T. Grover
IPC分类号： C07D30793
CPC分类号： C07D317/34 , C07C51/353 , C07C59/54
摘要： A process for preparing an alkyl phenylglycolic acid is disclosed. It follows the sequence of condensing a substituted acetaldehyde with mandelic acid to provide a 5-phenyl-1,3-dioxolan-4-one, which is condensed with an alkyl ketone or aldehyde to provide a 5-(1-hydroxyalkyl)-5-phenyl-1,3-dioxolan-4-one, which is dehydrated to a 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one. The 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one may be hydrolyzed and reduced to an &agr;-alkylphenylglycolic acid or the hydrolysis and reduction steps may be reversed. The process enables the production of single enantiomers of cyclohexylphenylglycolic acid (CHPGA). An analogous process for racemic CHPGA is disclosed employing racemic mandelic acid and acetone. Novel intermediates in the process are also disclosed.
摘要翻译：公开了一种制备烷基苯基乙醇酸的方法。它遵循将取代的乙醛与扁桃酸缩合的顺序，得到5-烷基酮或醛缩合的5-苯基-1,3-二氧戊环-4-酮，得到5-（1-羟基烷基）-5 - 苯基-1,3-二氧戊环-4-酮，将其脱水至5-（1-烯基）-5-苯基-1,3-二氧戊环-4-酮。可以将5-（1-烯基）-5-苯基-1,3-二氧戊环-4-酮水解并还原成α-烷基苯基乙醇酸，或者可以逆转水解和还原步骤。该方法能够生产环己基苯基乙醇酸（CHPGA）的单一对映异构体。公开了外消旋CHPGA的类似方法，其使用外消旋扁桃酸和丙酮。还公开了该方法中的新型中间体。

4. 发明授权

US06660872B1 Method of producing methoxyimino acetic amide 失效
标题翻译：制备甲氧基亚氨基乙酰胺的方法
公开(公告)号：US06660872B1
公开(公告)日：2003-12-09
申请号：US09979213
申请日：2001-11-21
申请人： Herbert Gayer , Bernd Gallenkamp , Peter Gerdes , Ulrich Heinemann , Walter Hübsch , Bernd-Wieland Krüger , Fritz Maurer , Holger Weintritt
发明人： Herbert Gayer , Bernd Gallenkamp , Peter Gerdes , Ulrich Heinemann , Walter Hübsch , Bernd-Wieland Krüger , Fritz Maurer , Holger Weintritt
IPC分类号： C07D30793
CPC分类号： C07D239/56 , C07C67/20 , C07C69/738 , C07C249/04 , C07C249/08 , C07C251/48 , C07D239/52
摘要： The present invention relates to novel processes for preparing methoxyimino-acetamides.
摘要翻译：本发明涉及制备甲氧基亚氨基 - 乙酰胺的新方法。

5. 发明授权

US06197979B1 Method for producing polytetrahydrofuran with low color index 失效
标题翻译：低颜色指数聚四氢呋喃的制备方法
公开(公告)号：US06197979B1
公开(公告)日：2001-03-06
申请号：US09485459
申请日：2000-02-10
申请人： Rainer Becker , Karsten Eller , Heinz Rütter , Michael Hesse
发明人： Rainer Becker , Karsten Eller , Heinz Rütter , Michael Hesse
IPC分类号： C07D30793
CPC分类号： C08G65/20 , B01J23/24
摘要： In a process for preparing polytetrahydrofuran, tetrahydrofuran copolymers, diesters or monoesters of these polymers having a low color number by polymerization of tetrahydrofuran in the presence of at least one telogen and/or comonomer over a heterogeneous catalyst, the polymerization is carried out in the presence of hydrogen.
摘要翻译：在通过在非均相催化剂的存在下，在至少一种环糊精和/或共聚单体的存在下通过四氢呋喃聚合而制备聚四氢呋喃的这些聚合物的四氢呋喃共聚物，二酯或单酯具有低色数的聚合反应在存在下进行的氢。

6. 发明授权

US06590109B2 Method for isolating terpene trilactones (ginkgolides, bilobalide) from leaves and pharmaceutical powders of ginkgo biloba 失效
标题翻译：从叶片和银杏叶药物粉末中分离萜内三聚物（银杏内酯，银杏内酯）的方法
公开(公告)号：US06590109B2
公开(公告)日：2003-07-08
申请号：US10194089
申请日：2002-07-11
申请人： Dirk Lichtblau , Nina Berova , John Berger , Koji Nakanishi
发明人： Dirk Lichtblau , Nina Berova , John Berger , Koji Nakanishi
IPC分类号： C07D30793
CPC分类号： C07D307/77 , A61K31/365 , A61K36/16
摘要： A method of isolating terpene trilactones from Ginkgo biloba plant material or extract comprising the steps of suspending the plant material or extract in either water or an aqueous solution of an oxidation reagent; extracting the terpene trilactones using an acceptable extraction agent; separating the organic layer from the aqueous layer; washing the organic layer with an acceptable aqueous salt or hydroxide solution, which may be an alkaline solution; and drying the organic layer to form a dried extract containing terpene trilactones. Further purification by treatment with or filtration over activated charcoal, by treatment with or filtration over alumina and by recrystallization with an acceptable solvent or solvent mixture leads to extracts with a content of terpene trilactones higher than 50%. Unwanted levels of ginkgolic acids are reduced to acceptable levels by reversed phase chromatography.
摘要翻译：从银杏植物材料或提取物中分离萜品三内酯的方法，包括将植物材料或提取物悬浮在水或氧化试剂的水溶液中的步骤; 使用可接受的提取剂萃取萜烯三内酯; 从水层分离有机层; 用可接受的盐或氢氧化物溶液洗涤有机层，其可以是碱性溶液; 并干燥有机层以形成含有萜烯三内酯的干燥提取物。通过用活性炭处理或过滤进一步纯化，通过在氧化铝上处理或过滤，并用可接受的溶剂或溶剂混合物重结晶，得到萜烯三内酯的含量高于50％的提取物。不需要的银杏酸水平通过反相色谱法降至可接受的水平。

7. 发明授权

US06303797B1 Sesterterpene derivatives exhibiting antifungal activities 失效
标题翻译：表现出抗真菌活性的西萜烯衍生物
公开(公告)号：US06303797B1
公开(公告)日：2001-10-16
申请号：US09744765
申请日：2001-01-30
申请人： Atsushi Hirano , Eiji Sugiyama , Hisao Kondo , Hiroyuki Suda , Hidenori Ogawa , Katsuhisa Kojiri
发明人： Atsushi Hirano , Eiji Sugiyama , Hisao Kondo , Hiroyuki Suda , Hidenori Ogawa , Katsuhisa Kojiri
IPC分类号： C07D30793
CPC分类号： C07D311/94
摘要： A compound represented by the formula [I] wherein Y1 represents an oxygen atom, or a group represented by NH, O—CO, O—SO2, O—CO—NH, O—CS—NH, NH—CO, NH—SO2, NH—CO—NH or NH—CS—NH, R1 represents an alkyl group, an alkenyl group, an alkynyl group, an aryl group, an aralkyl group, an arylalkenyl group, an arylalkynyl group, a cycloalkyl group, a cycloalkylalkyl group, an alkylcarbonyl group, an alkoxycarbonyl group, an arylcarbonyl group or a heterocyclic group, each optionally having a substituent, or a pharmacologically acceptable salt or ester thereof. The compound shows an excellent antifungal activity on fungi on which existing antifungal agents cannot sufficiently display their effects, and thus is useful as an antifungal agent.
摘要翻译：由式[I]表示的化合物，其中Y 1表示氧原子，或由NH，O-CO，O-SO 2，O-CO-NH，O-CS-NH，NH-CO，NH-SO 2表示的基团， NH-CO-NH或NH-CS-NH，R1表示烷基，烯基，炔基，芳基，芳烷基，芳基烯基，芳基炔基，环烷基，环烷基烷基，任选具有取代基的烷基羰基，烷氧基羰基，芳基羰基或杂环基，或其药理学上可接受的盐或酯。该化合物对现有的抗真菌剂不能充分显示其效果的真菌显示出优异的抗真菌活性，因此可用作抗真菌剂。

8. 发明授权

US06818781B2 Simultaneous reaction and separation process for the manufacture of dianhydro sugar alcohols 失效
标题翻译：用于制备二氢糖醇的同时反应和分离过程
公开(公告)号：US06818781B2
公开(公告)日：2004-11-16
申请号：US10414611
申请日：2003-04-16
申请人： Kamlesh Kumar Bhatia
发明人： Kamlesh Kumar Bhatia
IPC分类号： C07D30793
CPC分类号： C07D493/04
摘要： A continuous process for the manufacture of dianhydro sugar alcohols by dehydration of the corresponding sugar alcohols or monoanhydro sugar alcohols in the presence of a dehydration catalyst, using evolved water vapor as a carrier for continuous separation of the product from the reaction mass.
摘要翻译：一种通过在脱水催化剂存在下使相应的糖醇或单氢糖醇脱水而制备二氢糖醇的连续方法，该方法使用放出的水蒸气作为将产物从反应物料中连续分离的载体。

9. 发明授权

US06797832B1 Process for the production of 5-oxy-7-oxabicyclo [4.1.0] hept-3-ene-3-carboxylic acid esters 失效
标题翻译：制备5-氧代-7-氧杂双环[4.1.0]庚-3-烯-3-羧酸酯的方法
公开(公告)号：US06797832B1
公开(公告)日：2004-09-28
申请号：US10168388
申请日：2002-06-21
申请人： Shiro Terashima , Katsuji Ujita , Tomoya Kuwayama , Takashi Sugioka , Kazuya Shimizu , Koichi Kanehira
发明人： Shiro Terashima , Katsuji Ujita , Tomoya Kuwayama , Takashi Sugioka , Kazuya Shimizu , Koichi Kanehira
IPC分类号： C07D30793
CPC分类号： C07D303/40 , C07C67/31 , C07C69/757 , C07C2601/14 , C07C2601/16 , C07D493/18 , Y02P20/55
摘要： The present invention provides a method of producing 5-oxy-7-oxabicyclo[4.1.0]hept-3-ene-3-carboxylic acid ester economically, industrially advantageously and efficiently in a large amount. The present invention is a method of producing 5-oxy-7-oxabicyclo[4.1.0]hept-3-ene-3-carboxylic acid ester (X), which is shown in the following scheme. wherein each symbol is as defined in the specification.
摘要翻译：本发明提供了在工业上有效且高效率地经济地生产5-氧基-7-氧杂二环[4.1.0]庚-3-烯-3-羧酸酯的方法。本发明是一种生产5-氧基-7-氧杂二环[4.1.0]庚-3-烯-3-羧酸酯（X）的方法，如下列方案所示。其中每个符号如规格。

10. 发明授权

US06323348B1 Process for producing cycloalkyl [b]benzofurans 失效
标题翻译：制备环烷基[b]苯并呋喃的方法
公开(公告)号：US06323348B1
公开(公告)日：2001-11-27
申请号：US09423827
申请日：2000-02-14
申请人： Hisao Nishiyama , Hisanori Wakita , Hiroshi Nagase
发明人： Hisao Nishiyama , Hisanori Wakita , Hiroshi Nagase
IPC分类号： C07D30793
CPC分类号： C07D307/79 , C07C43/247 , C07C43/253 , C07C69/013 , C07C2601/10 , C07D307/93
摘要： The present invention provides a process for producing an optically active compound of cycloalkyl[b]benzofuran using a readily available optically active compound as a starting material by a reaction using a transition metal or the Mitsunobu reaction, or a combination thereof, followed by a cyclization reaction using a metal or an organometallic reagent. The process can exclude the needs of complicated optical resolution steps as well as enzyme reactions that requires a large amount of solvent and long reaction time besides repeatability is hardly obtained, providing a very useful production process that can apply for not only laboratory preparation but also for industrial scale productions.
摘要翻译：本发明提供了使用容易获得的光学活性化合物作为原料的通过使用过渡金属或Mitsunobu反应或其组合的反应或其组合制备环烷基[b]苯并呋喃的旋光活性化合物的方法，然后进行环化使用金属或有机金属试剂进行反应。该方法可以排除复杂的光学拆分步骤的需要以及需要大量溶剂的酶反应以及除了重复性之外的长反应时间，几乎不可获得，提供非常有用的生产方法，不仅适用于实验室准备，还适用于工业规模生产。

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