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    Microbial asymmetric reduction of 2-chloro-1-[-6-(2,5-dimethyl-pyrrol-1-yl)-pyridin-3-yl]-ethanone
    2.
    发明授权
    Microbial asymmetric reduction of 2-chloro-1-[-6-(2,5-dimethyl-pyrrol-1-yl)-pyridin-3-yl]-ethanone 失效
    2-氯-1- [ - 6-（2,5-二甲基 - 吡咯-1-基） - 吡啶-3-基] - 乙酮的微生物不对称还原

    公开(公告)号：US06451587B1

    公开(公告)日：2002-09-17

    申请号：US09587032

    申请日：2000-06-02

    Applicant: Michael P. Burns ,  John W. Wong

    Inventor： Michael P. Burns ,  John W. Wong

    IPC: C12P1712

    CPC classification number: C12P7/02 ,  C12P17/12

    Abstract: The present invention relates to microbial processes for carrying out the asymmetric reduction of a ketone to an alcohol, which comprises: contacting the ketone with a microorganism, or an enzyme reduction system capable of accomplishing the subject reduction comprising an enzyme derived from said microorganism and a co-factor for said enzyme, and incubating the resulting mixture under conditions sufficient to yield more of the desired (R)-enantiomer of the corresponding alcohol than the undesired (S)-enantiomer. The chiral (R)-enantiomer can be used in the synthesis of certain &bgr;-adrenergic receptor agonists.

    Abstract translation: 本发明涉及用于进行酮向醇的不对称还原的微生物方法，其包括：将酮与微生物或能够完成受试者还原的酶还原体系接触，所述还原系统包含源自所述微生物的酶和 所述酶的辅因子，并将所得混合物在足以产生比不需要的（S） - 对映体更多的相应醇的所需（R） - 对映异构体的条件下孵育。 手性（R） - 对映体可用于合成某些β-肾上腺素能受体激动剂。

    Method of producing dihydroxypyrimidine derivatives
    3.
    发明授权
    Method of producing dihydroxypyrimidine derivatives 失效
    二羟基嘧啶衍生物的制备方法

    公开(公告)号：US06248571B1

    公开(公告)日：2001-06-19

    申请号：US09029230

    申请日：1998-02-25

    Applicant: Beat Schmidt ,  Andreas Kiener ,  John McGarrity

    Inventor： Beat Schmidt ,  Andreas Kiener ,  John McGarrity

    IPC: C12P1712

    CPC classification number: C07D239/54 ,  C12P13/02

    Abstract: A process for the preparation of dihydroxypyrimidine derivatives of the general formula: in which R1 and R2 are identical or different and are a hydrogen atom, aryl group, or a C1-C4-alkyl group or an aryl group, starting from a compound of the general formula: in which R2 has the meaning mentioned above and R3 is —CN or COOR4, in which R4 is a C1-C4-alkyl group.

    Abstract translation: 制备以下通式的二羟基嘧啶衍生物的方法：其中R 1和R 2相同或不同，为氢原子，芳基或C 1 -C 4烷基或芳基，以 通式：其中R 2具有上述含义，R 3是-CN或COOR 4，其中R 4是C 1 -C 4 - 烷基。

    Microbes and methods for remediation
    5.
    发明授权
    Microbes and methods for remediation 有权
    微生物和修复方法

    公开(公告)号：US06673582B2

    公开(公告)日：2004-01-06

    申请号：US09769719

    申请日：2001-01-25

    Applicant: Hugh McTavish

    Inventor： Hugh McTavish

    IPC: C12P1712

    CPC classification number: B09C1/10 ,  C12N9/14 ,  C12N11/16

    Abstract: The present invention provides methods of using a microbe containing a polypeptide that degrades, preferably detoxifies, a compound that is present in the environment. Preferably, the polypeptide is a hydrolase and the compound is at least one s-triazine. The present invention also provides a microbe containing a polypeptide that degrades, preferably detoxifies, a compound that is present in the environment.

    Abstract translation: 本发明提供使用含有多肽的微生物的方法，所述多肽降解，优选地使存在于环境中的化合物解毒。 优选地，多肽是水解酶，并且化合物是至少一种s-三嗪。 本发明还提供一种含有多肽的微生物，其降解，优选地使存在于环境中的化合物解毒。

    Enzymatic process of making alpha 1a adrenergic receptor antagonists using protease
    6.
    发明授权
    Enzymatic process of making alpha 1a adrenergic receptor antagonists using protease 失效
    使用蛋白酶制备α1a肾上腺素能受体拮抗剂的酶学方法

    公开(公告)号：US06207444B1

    公开(公告)日：2001-03-27

    申请号：US09122301

    申请日：1998-07-24

    Applicant: Daniel R. Sidler ,  Michel Chartrain ,  Norihiro Ikemoto ,  Gerald F. Bills ,  Christopher Roberge ,  Colleen S. Taylor

    Inventor： Daniel R. Sidler ,  Michel Chartrain ,  Norihiro Ikemoto ,  Gerald F. Bills ,  Christopher Roberge ,  Colleen S. Taylor

    IPC: C12P1712

    CPC classification number: C07D239/22 ,  C07D401/04 ,  C07D401/14

    Abstract: This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.

    Abstract translation: 本发明涉及可用于治疗良性前列腺增生的α1α肾上腺素能受体拮抗剂，化合物A的结晶药学上可接受的盐。 还公开了使用结晶盐的药物组合物，以及制备和使用化合物A的结晶盐和药物组合物的方法。 本发明还涉及用于获得可用于合成终产物α1α肾上腺素能受体拮抗剂的对映体纯中间体的方法。 最终产品化合物可用于治疗良性前列腺增生和放松下尿路组织。 本发明还涉及一种制备其中化合物A为成员的一类二氢嘧啶酮化合物的方法，其中该方法包括使二氢嘧啶酮化合物去质子化，然后将去质子化衍生物与伯胺偶联。

    5-substituted picolinic acid compounds production by Marasmiellus sp
    8.
    发明授权
    5-substituted picolinic acid compounds production by Marasmiellus sp 失效
    由马拉斯马司属（Malasmiellus sp。）生产的5-取代吡啶甲酸化合物

    公开(公告)号：US06416979B1

    公开(公告)日：2002-07-09

    申请号：US09657730

    申请日：2000-09-08

    Applicant: Hideo Hirai ,  Katsuomi Ichikawa ,  Nakao Kojima ,  Hiroyuki Nishida ,  Kunio Satake ,  Nobuji Yoshikawa

    Inventor： Hideo Hirai ,  Katsuomi Ichikawa ,  Nakao Kojima ,  Hiroyuki Nishida ,  Kunio Satake ,  Nobuji Yoshikawa

    IPC: C12P1712

    CPC classification number: A61K31/44

    Abstract: The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are independently H, C2-C6 acyl or halo-substituted benzoyl; and R3 is —C(O)O—C1-C6 alkyl, C(O)OH, CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R2 is acetyl and R3 is methoxycarbonyl, R1 is not H; and that when R3 is CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, R1 and R2 are H. The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like. The present invention further relates to a process for producing the compounds of the formula (I).

    Abstract translation: 本发明提供式（I）的新的5-取代的吡啶甲酸化合物或其药学上可接受的盐：其中R 1和R 2独立地为H，C 2 -C 6酰基或卤素取代的苯甲酰基; 并且R 3是-C（O）O-C 1 -C 6烷基，C（O）OH，CN，CONH 2，CONHCH 3，CON（CH 3）2,1-甲基四唑或2-甲基四唑，条件是当R 2是乙酰基和 R3是甲氧基羰基，R1不是H; 当R3为CN，CONH2，CONHCH3，CON（CH3）2,1-甲基四唑或2-甲基四唑时，R 1和R 2为H.本发明还涉及含有本发明化合物的药物组合物，其有用 在治疗IL-1和TNF介导的疾病等中。本发明还涉及制备式（I）化合物的方法。

    Process for producing cytidine diphosphate choline
    9.
    发明授权
    Process for producing cytidine diphosphate choline 失效
    胞苷二磷酸胆碱生产方法

    公开(公告)号：US06387667B1

    公开(公告)日：2002-05-14

    申请号：US08014012

    申请日：1993-01-28

    Applicant: Akihiko Maruyama ,  Tatsuro Fujio ,  Sadao Teshiba

    Inventor： Akihiko Maruyama ,  Tatsuro Fujio ,  Sadao Teshiba

    IPC: C12P1712

    CPC classification number: C12N9/93 ,  C12N9/12 ,  C12N15/52 ,  C12P19/32

    Abstract: A process for producing cytidine diphosphate choline is provided. The process comprises carrying out an enzymatic reaction using microorganisms having the enzyme activities of cytidine-5′-triphosphate synthetase (pyrG), cholinephosphate cytidylyltransferase (CCT) and choline kinase (CKI) and a microorganism capable of producing uridine-5′-triphosphate from orotic acid as the enzyme sources, and orotic acid and choline and/or phosphorylcholine as the substrates; allowing cytidine diphosphate choline to accumulate in the reaction mixture; and recovering cytidine diphosphate choline from said reaction mixture.

    Abstract translation: 提供了制备胞苷二磷酸胆碱的方法。 该方法包括使用具有胞苷-5'-三磷酸合成酶（pyrG），胆碱磷酸胞苷酰转移酶（CCT）和胆碱激酶（CKI）的酶活性的微生物进行酶反应，以及能够从尿嘧啶-5'-三磷酸合成酶 乳清酸作为酶源，乳清酸和胆碱和/或磷酸胆碱作为底物; 使胞苷二磷酸胆碱积累在反应混合物中; 并从所述反应混合物中回收胞苷二磷酸胆碱。

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