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    ENZYMATIC RESOLUTION OF RACEMIC (2R,S)-2-(ACETYLAMINO)-3-METHOXY-N-(PHENYLMETHYL)PROPANAMIDE
    2.
    发明申请
    ENZYMATIC RESOLUTION OF RACEMIC (2R,S)-2-(ACETYLAMINO)-3-METHOXY-N-(PHENYLMETHYL)PROPANAMIDE 审中-公开
    （2R，S）-2-（乙酰氨基）-3-甲氧基-N-（苯基甲基）丙酰胺的酶解

    公开(公告)号：WO2011158194A1

    公开(公告)日：2011-12-22

    申请号：PCT/IB2011/052607

    申请日：2011-06-15

    Applicant: MEDICHEM, S.A. ,  BOSCH I LLADO, Jordi ,  DURAN LOPEZ, Ernesto

    Inventor： BOSCH I LLADO, Jordi ,  DURAN LOPEZ, Ernesto

    IPC: C12P13/02

    CPC classification number: C12P41/006 ,  C12P13/02 ,  C12P41/007 ,  C12Y301/01003

    Abstract: The present invention is concerned with a process of preparing (R)-lacosamide. The process comprises providing an (R,S)-lacosamide precursor and contacting the same with at least an enzyme in the presence of a solvent. The enzyme either stereoselectively hydrolyzes or acetylates an (R)- or (S)-enantiomer of the (R,S)-lacosamide precursor. The process further comprises where appropriate also concurrently, or successively, employing one or more reagents capable of converting the hydrolysed or acetylated (R)- or (S)-enantiomer to (R)- lacosamide.

    Abstract translation: 本发明涉及制备（R） - 肉豆蔻酰胺的方法。 该方法包括提供（R，S） - 可可酰胺前体，并在溶剂存在下使其与至少一种酶接触。 该酶可立即选择性地水解或乙酰化（R，S） - 酰胺前体的（R） - （S） - 对映异构体。 该方法还在适当的情况下还同时或相继地使用一种或多种能够将水解或乙酰化的（R） - 或（S） - 对映异构体转化为（R） - 拉诺卡胺的试剂。

    PROCESS FOR THE PREPARATIN OF ALKYNOLS
    5.
    发明申请
    PROCESS FOR THE PREPARATIN OF ALKYNOLS 审中-公开
    阿尔茨海默氏菌的制备方法

    公开(公告)号：WO2005040076A1

    公开(公告)日：2005-05-06

    申请号：PCT/EP2004/011614

    申请日：2004-10-14

    Applicant: DSM IP ASSETS B.V. ,  BOXTEL VAN, Danniël, Adrianus, Franciscus, Jacobus ,  VERZIJL, Gerardus, Karel, Maria

    Inventor： BOXTEL VAN, Danniël, Adrianus, Franciscus, Jacobus ,  VERZIJL, Gerardus, Karel, Maria

    IPC: C07C29/00

    CPC classification number: C12P7/04 ,  C07C29/00 ,  C07C29/095 ,  C12P9/00 ,  C12P41/007 ,  C07C33/042

    Abstract: Process for the preparation of an alkynol with formula HC=C-C(OH)-R 2 (formula 2) wherein R 2 represents methyl, halomethyl or ethyl, wherein the corresponding silyl-protected alkynol ester with formula 1 (1) wherein R 1 represents H, or an optionally substituted alkyl, an optionally substituted alkenyl or an optionally substituted (hetero)aryl group, R 2 is as defined above and A 3 Si represents a trisubstituted silyl group wherein each A independently represents anoptionally substituted alkyl or an optionally substituted (hetero)aryl group, in the presence of water and at least an equivalent amount of amine functionalities is converted into the alkynol with formula 2. Preferably, the amount of water is between 0.5 and 3 equivalents calculated with respect to the amount of silyl-protected alkynol ester with formula (1).

    Abstract translation: 制备具有式HC = CC（OH）-R 2（式2）的炔醇的方法，其中R 2表示甲基，卤代甲基或乙基，其中相应的具有式1（1）的甲硅烷基保护的炔醇酯 其中R 1表示H或任选取代的烷基，任选取代的烯基或任选取代的（杂）芳基，R 2如上所定义，并且A3Si表示三取代甲硅烷基，其中每个A独立地表示取代的 烷基或任选取代的（杂）芳基在水的存在下和至少等量的胺官能团转化为具有式2的炔醇。优选地，水的量相对于 具有式（1）的甲硅烷基保护的炔醇酯的量。

    METHOD OF SEPARATING OPTICAL ISOMERS OF A PROTECTED AMINOACID
    6.
    发明申请
    METHOD OF SEPARATING OPTICAL ISOMERS OF A PROTECTED AMINOACID 审中-公开
    分离保护氨基酸的光学异构体的方法

    公开(公告)号：WO2005001107A1

    公开(公告)日：2005-01-06

    申请号：PCT/RU2004/000244

    申请日：2004-06-25

    Applicant: CLEA TECHNOLOGIES BV ,  BIOTIR LTD ,  YOUSHKO, Maxim Ilich ,  SVEDAS, Vytautas-Juozapas Kajetono ,  SHELDON, Roger, Arthur ,  VAN LANGEN, Lukas, Michael

    Inventor： YOUSHKO, Maxim Ilich ,  SVEDAS, Vytautas-Juozapas Kajetono ,  SHELDON, Roger, Arthur ,  VAN LANGEN, Lukas, Michael

    IPC: C12P41/00

    CPC classification number: C07K14/38 ,  C12P13/04 ,  C12P41/005 ,  C12P41/007 ,  Y02P20/55

    Abstract: The invention relates to a method Method of enzy­matically separating optical isomers of a protected amino­ acid. According to the invention, a (non-sidechain-carboxyl)­ protected aminoacid is used having the general formula (I) HR 1 N-CR 2 - (CH) n -C (0) ZR 3 wherein R 1 is an amino-protective group or hydrogen; - R 2 is a side chain; n is a number chosen from 0, 1, and 2; ZR 3 is a carboxy-protective group where Z is chosen from 0 or NH; and R 1 and R 3 may be integrated, forming a heterocy­clic (non-sidechain-carboxyl)-protected ring, the ring backbone comprising 5 to 8 atoms; the (non-sidechain-carboxyl)-protected aminoacid having a mo­lecular weight of less than 1000 Dalton, said method comprising the steps of - contacting the (non-sidechain-carboxyl) -protected aminoacid (I) in the presence of water with an optionally partially pu­rified cell-free extract of a fungus containing an enzyme having at least one of an esterase and amidase activity yielding a mixture of (non-sidechain carboxyl) deprotected product and starting material; and - optionally separating the (non-sidechain carboxyl) depro­tected product and starting material.

    Abstract translation: 本发明涉及一种酶法分离被保护氨基酸的光学异构体的方法。 根据本发明，使用具有通式（I）HR 1 N-CR 2 - （CH）n C（O）Z R 3的（非侧链羧基）保护的氨基酸，其中R 1 >是氨基保护基或氢; -R 2是侧链; n是选自0,1和2的数字; ZR 3是羧基保护基，其中Z选自0或NH; 并且R 1和R 3可以整合，形成杂环（非侧链羧基）保护的环，所述环骨架包含5-8个原子; 分子量小于1000道尔顿的（非侧链羧基）保护的氨基酸，所述方法包括以下步骤：在水存在下使（非侧链羧基）保护的氨基酸（I）与 任选地部分纯化的无细胞提取物，其含有具有酯酶和酰胺酶活性中至少一种的酶，产生（非侧链羧基）脱保护产物和起始材料的混合物; 和 - 任选分离（非侧链羧基）脱保护产物和起始原料。

    A METHOD OF SELECTIVELY PRODUCING MALE OR FEMALE STERILE PLANTS
    8.
    发明申请
    A METHOD OF SELECTIVELY PRODUCING MALE OR FEMALE STERILE PLANTS 审中-公开
    选择生产男性或女性纯天然植物的方法

    公开(公告)号：WO2003072792A2

    公开(公告)日：2003-09-04

    申请号：PCT/GB2003/000683

    申请日：2003-02-14

    Applicant: SYNGENTA LIMITED ,  HAWKES, Timothy, Robert ,  MITCHELL, Glynn ,  HADFIELD, Stephen, Thomas ,  THOMPSON, Paul, Anthony ,  VINER, Russell ,  ZHANG, Yan

    Inventor： HAWKES, Timothy, Robert ,  MITCHELL, Glynn ,  HADFIELD, Stephen, Thomas ,  THOMPSON, Paul, Anthony ,  VINER, Russell ,  ZHANG, Yan

    IPC: C12N15/82

    CPC classification number: C12N9/0024 ,  C12N9/18 ,  C12N15/8287 ,  C12N15/8289 ,  C12N15/829 ,  C12P13/04 ,  C12P41/007

    Abstract: A method of producing male or female sterile plants comprising the steps of transforming plant material with a polynucleotide which encodes at least one enzyme which reacts with a non-phytotoxic substance to produce a phytotoxic one, and regenerating the thus transformed material into a plant, wherein the said non-phytotoxic substance is applied to the plant up to the time of male or female gamete formation and/ or maturation, so that the non- phytotoxic substance provides for the production of a phytotoxic one which selectively prevents the formation of or otherwise renders the said gametes non-functional, wherein the enzyme is expressed preferentially in either male or female reproductive structures, characterised in that (i) the non-phytotoxic substance is selected from the group consisting of ester derivatives of non-phosphonate herbicides which herbicides are directly phytotoxic to non-green tissue, D-alpha amino acids, peptide derivatives of non-protein D-alpha amino acids, S-enantiomers of aryloxyphenoxypropionates and S-enantiomers of ester derivatives of aryloxyphenoxypropionates and (ii) the enzyme is selected from the group consisting of carboxylesterases , D-amino acid oxidases, D-amino acid dehydrogenases, D-amino acid racemases, 2-arylpropionyl-CoA epimerases, alpha-methylacyl-CoA racemases, thioesterases and acyl-CoA synthetases.

    Abstract translation: 一种产生雄性或雌性不育植物的方法，包括以编码与非植物毒性物质反应产生植物毒性物质的至少一种酶的多核苷酸转化植物材料并将由此转化的材料再生成植物的步骤，其中 所述非植物毒性物质直到雄性或雌性配子形成和/或成熟时被施用于植物，使得非植物毒性物质提供用于选择性地防止形成或以其它方式形成的植物毒性物质 所述配子是非功能性的，其中所述酶优先在雄性或雌性生殖结构中表达，其特征在于，所述非植物毒性物质选自非膦酸酯除草剂的酯衍生物，所述除草剂直接植物毒性至 非绿色组织，D-α氨基酸，​​非蛋白D-α氨基酸的肽衍生物，S-enant 芳氧基苯氧基丙酸酯的酯衍生物的芳氧基苯氧基丙酸酯和S-对映异构体的末端异构体和ii酶选自羧酸酯酶，D-氨基酸氧化酶，D-氨基酸脱氢酶，D-氨基酸消旋酶，2-芳基丙酰-CoA差向异构酶， α-甲基酰基-CoA消旋酶，硫酯酶和酰基辅酶A合成酶。

    AMIDASES, NUCLEIC ACIDS ENCODING THEM AND METHODS FOR MAKING AND USING THEM
    9.
    发明申请
    AMIDASES, NUCLEIC ACIDS ENCODING THEM AND METHODS FOR MAKING AND USING THEM 审中-公开
    AMIDASES，核酸编码它们及其制备和使用它们的方法

    公开(公告)号：WO2003064613A2

    公开(公告)日：2003-08-07

    申请号：PCT/US2003/002694

    申请日：2003-01-28

    Applicant: DIVERSA CORPORATION ,  BARTON, Nelson, R. ,  WEINER, David, Paul ,  GREENBERG, William ,  LUU, Samantha ,  CHANG, Kristine ,  WATERS, Elizabeth

    Inventor： BARTON, Nelson, R. ,  WEINER, David, Paul ,  GREENBERG, William ,  LUU, Samantha ,  CHANG, Kristine ,  WATERS, Elizabeth

    IPC: C12N

    CPC classification number: C07D501/00 ,  A01K2217/05 ,  A61K38/00 ,  C12N9/78 ,  C12P35/00 ,  C12P35/02 ,  C12P41/007 ,  C12Q1/34

    Abstract: This invention provides amidases, polynucleotides encoding the amidases, methods of making and using these polynucleotides and polypeptides. In one aspect, the invention provides enzymes having secondary amidase activity, e.g., having activity in the hydrolysis of amides, including enzymes having peptidase, protease and/or hydantoinase activity. In alternative aspects, the enzymes of the invention can be used to used to increase flavor in food (e.g., enzyme ripened cheese), promote bacterial and fungal killing, modify and de-protect fine chemical intermediates, synthesize peptide bonds, carry out chiral resolutions, hydrolyze Cephalosporin C. The enzymes of the invention can be used to generate 7-aminocephalosporanic acid (7-ACA) and semi-synthetic cephalosporin antibiotics, including caphalothin, cephaloridine and cefuroxime. The enzymes of the invention can be used as antimicrobial agents, e.g., as cell wall hydrolytic agents. The invention also provides a fluorescent amidase substrate comprising 7-(ε-D-2-aminoadipoyladipoylamido)-4-methylcoumarin.

    Abstract translation: 本发明提供酰胺酶，编码酰胺酶的多核苷酸，制备和使用这些多核苷酸和多肽的方法。 一方面，本发明提供了具有仲酰胺酶活性的酶，例如在酰胺水解中具有活性，包括具有肽酶，蛋白酶和/或乙内酰脲酶活性的酶。 在替代方面，本发明的酶可用于增加食物中的风味（例如酶熟干酪），促进细菌和真菌杀死，改善和去保护精细化学中间体，合成肽键，进行手性拆分 ，水解头孢菌素C.本发明的酶可用于产生7-氨基头孢烷酸（7-ACA）和半合成头孢菌素抗生素，包括沙司他啶，头孢菌啶和头孢呋辛。 本发明的酶可以用作抗微生物剂，例如细胞壁水解剂。 本发明还提供了包含7-（ε-D-2-氨基己二酰己二酰氨基）-4-甲基香豆素的荧光酰胺酶底物。

    PROCESS FOR RACEMIZATION OF N-ACETYL-D(L)-ALPHA-AMINOCARBOXYLIC ACIDS
    10.
    发明申请
    PROCESS FOR RACEMIZATION OF N-ACETYL-D(L)-ALPHA-AMINOCARBOXYLIC ACIDS 审中-公开
    过程对于N-乙酰基-D-（L）的外消旋 - α-氨基羧酸

    公开(公告)号：WO1997021650A1

    公开(公告)日：1997-06-19

    申请号：PCT/EP1996005438

    申请日：1996-12-05

    Applicant: DEGUSSA AKTIENGESELLSCHAFT ,  DRAUZ, Karlheinz ,  BOMMARIUS, Andreas ,  KARRENBAUER, Michael ,  KNAUP, Günter

    Inventor： DEGUSSA AKTIENGESELLSCHAFT

    IPC: C07B55/00

    CPC classification number: C12P41/007 ,  C07C231/16 ,  C07C323/59 ,  C12P13/12

    Abstract: With known methods of racemizing N-acetyl-D(L)- alpha -aminocarboxylic acids in the non-aqueous state by heating them to temperatures above room temperature, significant quantities of by-products are formed, especially acetyl dipeptides. By converting at least a proportion of the N-acetyl-D(L)- alpha -aminocarboxylic acids to corresponding N-acetyl-D(L)- alpha -aminocarboxylic acid salts before or during the heating, it is possible to increase the sojourn time of the educt which is to be racemized at higher temperatures without any evident increase in the quantity of by-product formed (in particular acetylated dipeptides). Also disclosed is the production of optically active amino acids by enzymatic splitting of racemic compounds.

    Abstract translation: 在用于N-乙酰基-D-（L）的外消旋化的已知方法 - 的α-氨基羧酸中通过加热到比室温高的温度下在非水状态，有一个显著副产物的形成，特别是Acetyldipeptiden。 之前或温度的作用期间在特征在于，至少所述N-乙酰基D（L）的一部分 - 的α-氨基羧酸为相应的N-乙酰基D（L） - 转移阿尔法-aminocarbonsäuresalze，所以能够消旋的更长的停留时间 以允许在升高的温度下反应物而不副产物组分的增加（特别是乙酰化的二肽）中观察到。 通过酶拆分获得的光学活性的氨基酸。

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