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1. 发明公开

EP1369422A1 PROCESS FOR PREPARATION OF ALKENYLPHOSPHINE OXIDES OR ALKENYLPHOSPHINIC ACID ESTERS 有权
标题翻译：制备烷基氧膦氧化物或烷基膦酸酯的方法
公开(公告)号：EP1369422A1
公开(公告)日：2003-12-10
申请号：EP02711453.7
申请日：2002-02-12
申请人： JAPAN SCIENCE AND TECHNOLOGY CORPORATION , National Institute of Advanced Industrial Science and Technology
发明人： HAN, Li-Biao , ZHAO, Chang-Qiu , TANAKA, Masato
IPC分类号： C07F9/32 , C07F9/6553
CPC分类号： C07F9/655345 , C07F9/3217 , C07F9/3223 , C07F9/3235 , C07F9/5316 , C07F9/532 , C07F9/5329
摘要： A novel process for preparation of alkenylphosphine oxides or alkenylphosphinic acid esters provided by which the objective compounds can be easily, safely and efficiently synthesized and easily separated and purified with little formation of by-products . Specifically, a process of conducting the addition reaction of an easily available secondary phosphine oxide or hydrogen phosphinic acid ester with an acetylene compound with a catalyst containing a Group 9 or 10 metal of the periodic table to thereby obtain the corresponding alkenylphosphine oxide or alkenylphosphinic acid ester.
摘要翻译：一种制备链烯基膦氧化物或链烯基次膦酸酯的新方法，通过该方法，目标化合物可以容易，安全和有效地合成，并且容易分离和纯化，少量副产物形成。具体而言，使用容易获得的仲膦氧化物或次膦酸氢酯与乙炔化合物与含有周期表第9或10族金属的催化剂进行加成反应，从而获得相应的烯基氧化膦或烯基次膦酸酯。

2. 发明公开

EP0209897A2 Peptide enzyme inhibitors 失效
标题翻译： Peptid-Enzymhemmende Stoffe。
公开(公告)号：EP0209897A2
公开(公告)日：1987-01-28
申请号：EP86110125.1
申请日：1986-07-23
申请人： Merck & Co., Inc.
发明人： Boger, Joshua S. , Bock, Mark G. , Freidinger, Roger , Veber, Daniel F. , Patchett, Arthur A. , Greenlee, William J. , Parsons, William H.
IPC分类号： C07K5/00 , C07K7/00 , C07C103/50 , C07D233/64 , C07F9/65 , A61K37/64 , A61K31/195 , A61K31/66
CPC分类号： C07D233/64 , A61K38/00 , C07F9/301 , C07F9/303 , C07F9/3211 , C07F9/3217 , C07F9/3223 , C07F9/4006 , C07F9/4816 , C07F9/4833 , C07F9/65067 , C07K5/0227 , C07K5/06078 , C07K7/02
摘要： Enzyme peptides of the formula
and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
摘要翻译：式的酶肽及其类似物，其抑制肾素，并且可用于治疗各种形式的肾素相关性高血压和醛固酮增多症。

3. 发明公开

EP1694623A2 PRACTICAL, COST-EFFECTIVE SYNTHESIS OF UBIQUINONES 审中-公开
标题翻译：泛醌的实用，经济综合
公开(公告)号：EP1694623A2
公开(公告)日：2006-08-30
申请号：EP04812975.3
申请日：2004-12-03
申请人： Zymes, Inc.
发明人： LIPSHUTZ, Bruce H. , BERL, Volker , SCHEIN, Karin , WETTERICH, Frank
IPC分类号： C07C50/28 , A61K31/122
CPC分类号： C07F9/094 , B01J31/2404 , B01J2231/4205 , B01J2531/847 , C07C17/16 , C07C39/10 , C07C46/00 , C07C46/06 , C07C46/10 , C07C50/28 , C07C50/38 , C07F9/117 , C07F9/3223 , C07F9/3241 , C07F9/4446 , C07F9/4453 , C07C21/04
摘要： The present invention provides a convergent method for the synthesis of ubiquinones and ubiquinones analogues. Also provided are precursors of ubiquinones and their analogues that are useful in the methods of the invention, The invention further provides an improved method for the carboalumination of alkyne substrates.

4. 发明公开

EP0209897A3 Peptide enzyme inhibitors 失效
标题翻译：肽类酶抑制剂
公开(公告)号：EP0209897A3
公开(公告)日：1989-08-16
申请号：EP86110125.1
申请日：1986-07-23
申请人： Merck & Co., Inc.
发明人： Boger, Joshua S. , Bock, Mark G. , Freidinger, Roger , Veber, Daniel F. , Patchett, Arthur A. , Greenlee, William J. , Parsons, William H.
IPC分类号： C07K5/00 , C07K7/00 , C07C103/50 , C07D233/64 , C07F9/65 , A61K37/64 , A61K31/195 , A61K31/66
CPC分类号： C07D233/64 , A61K38/00 , C07F9/301 , C07F9/303 , C07F9/3211 , C07F9/3217 , C07F9/3223 , C07F9/4006 , C07F9/4816 , C07F9/4833 , C07F9/65067 , C07K5/0227 , C07K5/06078 , C07K7/02
摘要： Enzyme peptides of the formula
and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.

5. 发明授权

EP1369422B1 PROCESS FOR PREPARATION OF ALKENYLPHOSPHINE OXIDES OR ALKENYLPHOSPHINIC ACID ESTERS 有权
标题翻译：制备烷基氧膦氧化物或烷基膦酸酯的方法
公开(公告)号：EP1369422B1
公开(公告)日：2008-07-23
申请号：EP02711453.7
申请日：2002-02-12
申请人： Japan Science and Technology Agency , National Institute of Advanced Industrial Science and Technology
发明人： HAN, Li-Biao , ZHAO, Chang-Qiu , TANAKA, Masato
IPC分类号： C07F9/32 , C07F9/6553
CPC分类号： C07F9/655345 , C07F9/3217 , C07F9/3223 , C07F9/3235 , C07F9/5316 , C07F9/532 , C07F9/5329
摘要： A novel process for preparation of alkenylphosphine oxides or alkenylphosphinic esters is provided by which the objective compounds can be easily, safely and efficiently synthesized and easily separated and purified with little formation of by-products. Specifically, a process of conducting the addition reaction of an easily available secondary phosphine oxide or hydrogenated phosphinic ester with an acetylene compound with a catalyst containing a Group 9 or 10 metal of the periodic table to thereby obtain the corresponding alkenylphosphine oxide or alkenylphosphinic ester.
摘要翻译：提供了制备链烯基膦氧化物或链烯基亚膦酸酯的新方法，通过该方法，目标化合物可以容易，安全和有效地合成，并且容易分离和纯化，少量副产物形成。具体而言，是使易于获得的仲膦氧化物或氢化次膦酸酯与乙炔化合物与含有周期表第9族或第10族金属的催化剂进行加成反应，从而获得相应的烯基氧化膦或链烯基次膦酸酯的方法。

6. 发明公开

EP0347840A2 Phosphinic acid derivates 失效
标题翻译： Phosphinsäure衍。
公开(公告)号：EP0347840A2
公开(公告)日：1989-12-27
申请号：EP89111208.8
申请日：1989-06-20
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： Ishikawa, Kiyofumi , Fukami, Takehiro , Takezawa, Hiroshi , Nakamichi, Kyoko
IPC分类号： C07F9/30 , C07F9/32 , A61K31/66
CPC分类号： C07F9/65182 , C07F9/302 , C07F9/303 , C07F9/3217 , C07F9/3223 , C07F9/582 , C07F9/65062
摘要： A phosphinic acid derivative represented by the general formula [I], or a pharmaceutically acceptable salt thereof,
wherein R¹ represents an alkyl, cycloalkyl or aralkyl group which may be substituted; R² and R⁵ may be identical or different, and each represents a hydrogen atom, or an ester residue capable of forming a non-toxic ester hydrolyzable in vivo ; and A represents a group of the formula
wherein R³ represents an alkyl group, a group of the formula
wherein R³⁰ represents a halogen atom, a carboxyl group, a hydroxyl group, a cycloalkyl group which may be substituted, an aryl group which may be substituted, an arylthio group, a heteroarylthio group which may be substituted, an alkylthio group which may be substituted, an amino group which may be substituted, or a lower alkoxycarbonyl group; R³¹ represents a hydrogen atom or a lower alkyl group; and n represents an integer of 0 to 6,
a cycloalkyl group which may be substituted or an aryl group which may be substituted; and the double bond at A has a Z-configuration,
or a group of the formula
wherein R⁴ represents a cycloalkyl group which may be substituted.
Said phosphinic acid derivative is useful for reducing renal toxicity induced by a carbapenem or penem antibiotic and for inhibiting dipeptidase.
摘要翻译：由通式[I]表示的次膦酸衍生物或其药学上可接受的盐，其中R 1表示可被取代的烷基，环烷基或芳烷基; R 2和R 5可以相同或不同，各自表示氢原子或能够形成体内可水解的无毒酯的酯残基; A表示式CH 2的基团，其中R 3表示烷基，式的基团，其中R 3表示卤原子，羧基，羟基，可被取代的环烷基，可被取代的芳基，芳硫基，可被取代的杂芳基硫基，可被取代的烷硫基，可被取代的氨基或低级烷氧基羰基; R 3表示氢原子或低级烷基; n表示0〜6的整数，可被取代的环烷基或可被取代的芳基; 并且A处的双键具有Z构型，或式CHEM的基团，其中R 4表示可被取代的环烷基。所述次膦酸衍生物可用于降低由碳青霉烯或青霉烯抗生素诱导的肾毒性，并用于抑制二肽酶。

7. 发明公开

EP3356376A1 Verfahren zur Herstellung von Phosphinaten 有权转让
公开(公告)号：EP3356376A1
公开(公告)日：2018-08-08
申请号：EP16777612.9
申请日：2016-09-26
申请人： Bayer CropScience Aktiengesellschaft
发明人： RESSEL, Hans-Joachim
IPC分类号： C07F9/40
CPC分类号： C07F9/3211 , C07F9/3223 , C07F9/4075
摘要： The invention relates primarily to a method for the producing certain phosphinates (phosphoric acid mono esters) and to the use thereof for producing biologically active substances which can be used in the pharmaceutical or agrochemical field, preferably for producing phosphorous-containing amino acids.

8. 发明公开

EP1369422A4 PROCESS FOR PREPARATION OF ALKENYLPHOSPHINE OXIDES OR ALKENYLPHOSPHINIC ACID ESTERS 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON烷基磷酸氧化还原剂烷基磷酸烯醇酯
公开(公告)号：EP1369422A4
公开(公告)日：2004-09-08
申请号：EP02711453
申请日：2002-02-12
申请人： JAPAN SCIENCE & TECH AGENCY , NAT INST OF ADVANCED IND SCIEN
发明人： HAN LI-BIAO , ZHAO CHANG-QIU , TANAKA MASATO
IPC分类号： C07F9/32 , C07F9/53 , C07F9/6553
CPC分类号： C07F9/655345 , C07F9/3217 , C07F9/3223 , C07F9/3235 , C07F9/5316 , C07F9/532 , C07F9/5329
摘要： A novel process for preparation of alkenylphosphine oxides or alkenylphosphinic esters is provided by which the objective compounds can be easily, safely and efficiently synthesized and easily separated and purified with little formation of by-products. Specifically, a process of conducting the addition reaction of an easily available secondary phosphine oxide or hydrogenated phosphinic ester with an acetylene compound with a catalyst containing a Group 9 or 10 metal of the periodic table to thereby obtain the corresponding alkenylphosphine oxide or alkenylphosphinic ester.
摘要翻译：提供了制备链烯基膦氧化物或链烯基亚膦酸酯的新方法，通过该方法，目标化合物可以容易，安全和有效地合成，并且容易分离和纯化，少量副产物形成。具体而言，是使易于获得的仲膦氧化物或氢化次膦酸酯与乙炔化合物与含有周期表第9族或第10族金属的催化剂进行加成反应，从而获得相应的烯基氧化膦或链烯基次膦酸酯的方法。

9. 发明公开

EP1694623A4 PRACTICAL, COST-EFFECTIVE SYNTHESIS OF UBIQUINONES 审中-公开
标题翻译：泛醌的实用，经济综合
公开(公告)号：EP1694623A4
公开(公告)日：2007-01-17
申请号：EP04812975
申请日：2004-12-03
申请人： ZYMES INC
发明人： LIPSHUTZ BRUCE H , BERL VOLKER , SCHEIN KARIN , WETTERICH FRANK
IPC分类号： C07C50/28 , A61K31/12 , A61K31/122 , C07C17/16 , C07C39/10 , C07C43/23 , C07C46/00 , C07C46/06 , C07C46/10 , C07C50/26 , C07C50/38 , C07F5/06 , C07F9/09 , C07F9/117 , C07F9/32 , C07F9/44 , C12Q20060101
CPC分类号： C07F9/094 , B01J31/2404 , B01J2231/4205 , B01J2531/847 , C07C17/16 , C07C39/10 , C07C46/00 , C07C46/06 , C07C46/10 , C07C50/28 , C07C50/38 , C07F9/117 , C07F9/3223 , C07F9/3241 , C07F9/4446 , C07F9/4453 , C07C21/04
摘要： The present invention provides a convergent method for the synthesis of ubiquinones and ubiquinones analogues. Also provided are precursors of ubiquinones and their analogues that are useful in the methods of the invention, The invention further provides an improved method for the carboalumination of alkyne substrates.

10. 发明公开

EP0772585A1 ARYLOXY AND ARYLTHIOPROPANOLAMINE DERIVATIVES USEFUL AS BETA 3-ADRENORECEPTOR AGONISTS AND ANTAGONISTS OF THE BETA 1 AND BETA 2-ADRENORECEPTORS AND PHARMACEUTICAL COMPOSITION THEREOF 失效
标题翻译：芳氧基和ARYLTHIOPROPANOLAMINDERIVATE ALSβ-3肾上腺素受体激动剂和β1和β2 ADRENORECEPTOREN的拮抗剂及其药物组合物
公开(公告)号：EP0772585A1
公开(公告)日：1997-05-14
申请号：EP95929029.0
申请日：1995-07-27
申请人： SMITHKLINE BEECHAM PLC
发明人： BEELEY, Lee J., SmithKline Beecham Pharmaceuticals , THOMPSON, Mervyn, SmithKline Beecham Pharmaceut. , DEAN, David K., SmithKline Beecham Pharmaceuticals , KOTECHA, Nikesh R., SmithKline Beecham Pharmaceut. , BERGE, John M., SmithKline Beecham Pharmaceuticals , WARD, Robert W., SmithKline Beecham Pharmaceut.
IPC分类号： C07D317 , A61K31 , A61P1 , A61P3 , A61P9 , A61P25 , A61P29 , A61P43 , C07C217 , C07C311 , C07C323 , C07F9
CPC分类号： C07F9/3211 , C07C217/34 , C07C2601/14 , C07D317/46 , C07F9/301 , C07F9/303 , C07F9/3223 , C07F9/4006
摘要： A compound formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein R0 represents an aryl group optionally substituted with one, two or three substituents selected from the list consisting of: hydroxy, hydroxymethyl, nitro, amino, alkylamino, dialkylamino, alkylsulphonamido, arylsulphonamido, formamido, halogen, alkoxy and allyl; X represents O or S; R?1 and R1a¿ each independently represents hydrogen or an alkyl group; R2 represents OCH¿2?CO2H, or an ester or amide thereof, or R?2¿ represents a moiety of formula (b), wherein R4 represents hydrogen, alkyl, hydroxyalkyl, arylalkyl, aryloxyalkyl, aralkyloxyalkyl or cycloalkyl and R5 represents hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, aryloxyalkyloxy, arylalkoxyalkyloxy or cycloalkyloxy or R5 represents hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, aryloxyalkyl, arylalkyloxyalkyl or R5 together with OR4 represents O(CH¿2?)nO, wherein n is 2, 3 or 4; and R?3¿ represents hydrogen, halogen, alkyl or alkoxy or R3 together with R2 represents a moiety of formula (c) or an ester or amide thereof; providing that 4-[2-[2-hydroxy-3-(4-hydroxyphenoxy)propylamino]propyl]phenoxyacetic acid and salts and esters thereof and the compounds of examples 1 to 36 disclosed in EP0328251 are excluded from the scope of formula (I); a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.
摘要翻译：羟基，羟甲基，硝基：的化合物，式（I）化合物或其药学上可接受的盐，或它们的药学上可接受的溶剂化物，worin - [R <0> darstellt芳基的任选地与从所述列表由...组成中选出的一个，两个或三个取代substituiertem 基，氨基，烷基氨基，二烷基氨基，alkylsulphonamido，芳基磺酰氨基，甲酰胺基，卤素，烷氧基和烯丙基; X darstellt O或S; [R <1>和R <1A>每个unabhängigdarstellt氢或烷基; [R <2> darstellt OCH2CO2H，或酯或酰胺，或R <2> darstellt式的部分（b）中，worinř<4> darstellt氢，烷基，羟烷基，芳基烷基，芳氧基烷基，芳烷氧基烷基或环烷基并且R < 5> darstellt羟基，烷氧基，芳基烷氧基，羟基烷，烷氧基烷氧基，aryloxyalkyloxy，arylalkoxyalkyloxy或环烷氧基或R <5> darstellt氢，烷基，取代烷基，环烷基，芳基，芳基烷基，芳氧基烷基，芳烷氧基烷基或R <5或<4>一起 > darstellt O（CH 2）N，worin n为2，3或4; 且R <3> darstellt氢，卤素，烷基或烷氧基或R <3>与R c一起<2> darstellt式（c）的基团或上的酯或酰胺; 提供了没有4- [2- [2-羟基-3-（4-羟基苯氧基）丙氨基]丙基]苯氧基乙酸和其盐和酯和实施例1至36在EP0328251中公开的化合物被排除在式（I范围）; 含寻求的化合物的药物组合物，制备的化合物的搜索和使用的过程中搜索药的化合物。

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