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    Recombinant KAT enzyme and process for its preparation
    1.
    发明授权
    Recombinant KAT enzyme and process for its preparation 失效
    重组KAT酶及其制备方法

    公开(公告)号：US6136572A

    公开(公告)日：2000-10-24

    申请号：US765889

    申请日：1997-04-01

    申请人： Luca Benatti ,  Jerome Breton ,  Carmela Speciale ,  Etsuo Okuno ,  Robert Schwarcz ,  Monica Mosca

    发明人： Luca Benatti ,  Jerome Breton ,  Carmela Speciale ,  Etsuo Okuno ,  Robert Schwarcz ,  Monica Mosca

    IPC分类号： C12N15/09 ,  A61K31/47 ,  A61K35/76 ,  A61K38/45 ,  A61K48/00 ,  A61P25/28 ,  C07D215/48 ,  C12N5/10 ,  C12N9/10 ,  C12N15/54 ,  C12Q1/68 ,  C12R1/91 ,  C12P17/00 ,  C07H21/04

    CPC分类号： C12N9/1096 ,  A61K48/00

    摘要： Disclosed are isolated DNAs encoding a kynurenine aminotransferase selected from the group consisting of:(a) isolated DNA sequences which encode rat KAT;(b) an isolated DNA sequence which hybridizes to isolated DNA sequences of (a) above and which encodes a mammalian KAT enzyme; and(c) an isolated DNA sequence differing from the isolated DNA sequences of (a) and (b) above in codon sequence due to the degeneracy of the genetic code, and which encodes a KAT enzyme.Vectors and host cells containing the same, oligonucleotide probes for identifying kynurenine aminotransferase, and isolated and purified kynurenine aminotransferase are also disclosed.

    摘要翻译： PCT No.PCT / US95 / 07855 Sec。 371日期1997年04月1日 102（e）日期1997年4月1日PCT提交1995年6月23日PCT公布。 公开号WO96 / 01893 日期1996年1月25日公开是编码选自以下的犬尿氨酸氨基转移酶的分离的DNA：（a）编码大鼠KAT的分离的DNA序列; （b）分离的DNA序列，其与上述（a）的分离的DNA序列杂交并编码哺乳动物KAT酶; 和（c）由于遗传密码的简并性而编码KAT酶，密码子序列中与（a）和（b）分离的DNA序列不同的分离的DNA序列。 还公开了含有相同载体和宿主细胞，用于鉴定犬尿氨酸氨基转移酶的寡核苷酸探针和分离纯化的犬尿氨酸转氨酶。

    Recombinant kat enzyme from rat
    2.
    发明授权
    Recombinant kat enzyme from rat 失效
    来自大鼠的重组kat酶

    公开(公告)号：US5817496A

    公开(公告)日：1998-10-06

    申请号：US271667

    申请日：1994-07-07

    申请人： Luca Benatti ,  Jerome Breton ,  Carmela Speciale ,  Etsuo Okuno ,  Robert Schwarcz ,  Monica Mosca

    发明人： Luca Benatti ,  Jerome Breton ,  Carmela Speciale ,  Etsuo Okuno ,  Robert Schwarcz ,  Monica Mosca

    IPC分类号： C12N15/09 ,  A61K31/47 ,  A61K35/76 ,  A61K38/45 ,  A61K48/00 ,  A61P25/28 ,  C07D215/48 ,  C12N5/10 ,  C12N9/10 ,  C12N15/54 ,  C12Q1/68 ,  C12R1/91

    CPC分类号： C12N9/1096 ,  A61K48/00

    摘要： Disclosed are isolated DNAs encoding a kynurenine aminotransferase selected from the group consisting of: (a) an isolated DNA sequence which encodes rat KAT; (b) an isolated DNA sequence which hybridizes to the isolated DNA sequence of (a) above and which encodes a KAT enzyme; and (c) an isolated DNA sequence differing from the isolated DNA sequences of (a) and (b) above in codon sequence due to the degeneracy of the genetic code, and which encodes a KAT enzyme. Also disclosed are vectors and host cells containing the same; oligonucleotide probes for identifying kynurenine aminotransferase; and isolated and purified kynurenine aminotransferase.

    摘要翻译： 公开了编码选自以下的犬尿氨酸转氨酶的分离的DNA：（a）编码大鼠KAT的分离的DNA序列; （b）分离的DNA序列，其与上述（a）的分离的DNA序列杂交并编码KAT酶; 和（c）由于遗传密码的简并性而编码KAT酶，密码子序列中与（a）和（b）分离的DNA序列不同的分离的DNA序列。 还公开了载体和含有其的宿主细胞; 用于鉴定犬尿氨酸转氨酶的寡核苷酸探针; 和纯化的犬尿氨酸氨基转移酶。

    Substituted kynurenines and process for their preparation
    3.
    发明授权
    Substituted kynurenines and process for their preparation 失效
    替代的犬尿苷及其制备方法

    公开(公告)号：US5786508A

    公开(公告)日：1998-07-28

    申请号：US411656

    申请日：1995-04-06

    申请人： Robert Schwarcz ,  Mario Varasi ,  Arturo Della Torre ,  Carmela Speciale ,  Alberto Bianchetti

    发明人： Robert Schwarcz ,  Mario Varasi ,  Arturo Della Torre ,  Carmela Speciale ,  Alberto Bianchetti

    IPC分类号： C07C229/36 ,  A61K31/195 ,  C07C239/36

    CPC分类号： C07C229/36 ,  C07C2101/14

    摘要： The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT). The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, and R.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, mono-C.sub.1 -C.sub.6 alkylamino, di-C.sub.1 -C.sub.6 alkylamino, hydroxylamino, C.sub.1 -C.sub.4 alkoxyamino or benzyloxyamino, with the provisos that: (i) when R.sub.1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and (ii) when R.sub.1 is hydroxy and, at the same time, R is C.sub.1 -C.sub.6 alkyl, then this C.sub.1 -C.sub.6 alkyl is not methyl, either as a single isomer or as a mixture of isomers, and the pharmaceutically acceptable salts thereof.

    摘要翻译： PCT No.PCT / US94 / 07804 Sec。 371日期：1995年4月6日 102（e）日期1995年4月6日PCT 1994年7月15日PCT公布。 公开号WO95 / 04714 日期1995年2月16日本发明涉及用作治疗与作为犬尿氨酸转氨酶（KAT）酶抑制剂的化合物的脑老化过程和围产期脑疾病相关的认知障碍的用途。 本发明还提供作为新化合物的选择类别的作为式（IA）化合物的KAT抑制剂，其中R是卤素，C 1 -C 6烷基，C 5 -C 7环烷基，苯基-C 1 -C 4烷基， C 1 -C 6烷氧基，C 6 -C 10芳氧基，苯基-C 1 -C 4烷氧基或三氟甲基，R 1是羟基，C 1 -C 6烷氧基，氨基，单-C 1 -C 6烷基氨基，二-C 1 -C 6烷基氨基，羟基氨基，C 1 -C 4 烷氧基氨基或苄氧基氨基，条件是：（ⅰ）当R 1为羟基，同时R为卤素时，该卤素不为氟; 和（ii）当R 1是羟基，并且同时R是C 1 -C 6烷基时，则该C 1 -C 6烷基不是甲基，作为单一异构体或作为异构体的混合物，以及其药学上可接受的盐 。

    Substituted kynurenines and process for their preparation
    5.
    发明授权
    Substituted kynurenines and process for their preparation 失效
    替代的犬尿苷及其制备方法

    公开(公告)号：US5519055A

    公开(公告)日：1996-05-21

    申请号：US102843

    申请日：1993-08-06

    申请人： Robert Schwarcz ,  Mario Varasi ,  Arturo Della Torre ,  Carmela Speciale ,  Alberto Bianchetti

    发明人： Robert Schwarcz ,  Mario Varasi ,  Arturo Della Torre ,  Carmela Speciale ,  Alberto Bianchetti

    IPC分类号： A61K31/00 ,  A61K31/165 ,  A61K31/195 ,  A61K31/198 ,  A61K31/215 ,  A61K31/216 ,  C07C229/36 ,  C07C233/43 ,  C07C233/44 ,  C07C235/10 ,  A61K31/24 ,  C07C229/00

    CPC分类号： C07C229/36 ,  A61K31/00 ,  A61K31/165 ,  A61K31/195 ,  A61K31/198 ,  A61K31/215 ,  A61K31/216 ,  C07C2101/08

    摘要： The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, andR.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, mono-C.sub.1 -C.sub.6 alkylamino, di-C.sub.1 -C.sub.6 alkylamino, hydroxylamino, C.sub.1 -C.sub.4 alkoxyamino or benzyloxyamino; with the provisos that(i) when R.sub.1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and(ii) when R.sub.1 is hydroxy and, at the same time, R is C.sub.1 -C.sub.6 alkyl, then this C.sub.1 -C.sub.6 alkyl is not methyl, and the pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及用于治疗与脑衰老过程相关的认知障碍和围产期脑疾病的化合物的用途，所述化合物作为犬尿氨酸转氨酶（KAT）酶的抑制剂。 本发明还提供作为新化合物的选定类别的KAT抑制剂，其是式（IA）化合物其中R是卤素，C 1 -C 6烷基，C 5 -C 7环烷基，苯基-C 1 -C 6烷基， C4烷基，C1-C6烷氧基，C6-C10芳氧基，苯基-C1-C4烷氧基或三氟甲基，R1为羟基，C1-C6烷氧基，氨基，单C1-C6烷基氨基，二C1-C6烷基氨基， C1-C4烷氧基氨基或苄氧基氨基; 条件是（i）当R 1是羟基，同时R是卤素时，该卤素不是氟; 和（ii）当R 1是羟基，并且同时R是C 1 -C 6烷基时，则该C 1 -C 6烷基不是甲基，及其药学上可接受的盐。

    Inhibitors of Kynurenine Aminotransferase and Uses Therefor
    8.
    发明申请
    Inhibitors of Kynurenine Aminotransferase and Uses Therefor 审中-公开
    犬尿氨酸转移酶抑制剂及其用途

    公开(公告)号：US20110144064A1

    公开(公告)日：2011-06-16

    申请号：US12085931

    申请日：2006-11-30

    申请人： Robert Schwarcz ,  Roberto Pellicciari ,  Timothy Gately

    发明人： Robert Schwarcz ,  Roberto Pellicciari ,  Timothy Gately

    IPC分类号： A61K31/662 ,  C12N5/071 ,  A61K31/197 ,  A61K31/19 ,  G01N33/50 ,  C07C53/08 ,  C07C55/02 ,  C07C309/63 ,  C07F9/38 ,  A61P25/00

    CPC分类号： A61K31/131 ,  A61K31/185 ,  Y10T436/163333 ,  Y10T436/173845 ,  Y10T436/182 ,  Y10T436/201666

    摘要： Provided herein are methods of decreasing a level of kynurenic acid in a cell and of treating a pathophysiological condition in a subject associated with an increase in kynurenic acid in a subject. In these methods the inhibitory action of dicarboxylic acids or derivatives or analogs thereof are effective to inhibit activity of kynurenine aminotransferase II. Also provided is a method of screening for potential inhibitory compounds for kynurenine aminotransferase II. The dicarboxylic acids or derivatives or analogs thereof may have the structural formula, where R1 is H, NH2 or NHCH3, R2 is H or CH3, n is 0 to 14, and X is —COOH, CH2OH, —PO3H2, —SO3H, or —SO3H; or a pharmacologically acceptable salt.

    摘要翻译： 本文提供了降低细胞中犬尿酸水平和治疗与受试者中犬尿酸增加相关的受试者的病理生理状况的方法。 在这些方法中，二羧酸或其衍生物或类似物的抑制作用对抑制犬尿氨酸氨基转移酶II的活性是有效的。 还提供了筛选针对犬尿氨酸氨基转移酶II的潜在抑制性化合物的方法。 二羧酸或其衍生物或类似物可具有结构式，其中R 1为H，NH 2或NHCH 3，R 2为H或CH 3，n为0至14，X为-COOH，CH 2 OH，-PO 3 H 2，-SO 3 H或 -SO 3 H; 或药理学上可接受的盐。

    Amino acid isomers, their production and their medicinal use
    10.
    发明授权
    Amino acid isomers, their production and their medicinal use 失效
    氨基酸异构体，其生产及其药用

    公开(公告)号：US4483853A

    公开(公告)日：1984-11-20

    申请号：US434361

    申请日：1982-10-14

    申请人： James F. Collins ,  Kenneth Curry ,  Robert Schwarcz

    发明人： James F. Collins ,  Kenneth Curry ,  Robert Schwarcz

    IPC分类号： C07F5/02 ,  A61K31/195 ,  A61K31/22 ,  A61K31/41 ,  A61P25/00 ,  A61P25/08 ,  C07C67/00 ,  C07C301/00 ,  C07C303/16 ,  C07C309/18 ,  C07D257/04 ,  C07F9/09 ,  C07F9/38 ,  C07F9/40 ,  A61K31/66 ,  A61K31/16 ,  A61K31/19

    CPC分类号： C07F9/3808 ,  C07F9/4006

    摘要： The (-)-D-isomers of compounds of the general formula ##STR1## in which X stands for an acidic radical, especially a radical of phosphonic acid, sulphonic acid, boronic acid or tetrazole,R stands for an alkylene, alkenylene or alkynylene radical with 3 or more carbon atoms, preferably 3 to 6 carbon atoms, or a C.sub.3 to C.sub.7 cycloalkyl radical, andA and B independently of each other stand for a hydrogen atom or a lipophilic radical, especially an ester radical,or salts thereof, or pharmaceutically acceptable bioprecursors thereof, especially (-)-D-aminophosphonopentanoic acid and (-)-D-aminophosphonoheptanoic acid, find use in the treatment of diseases of the central nervous system.The compound aminophosphonoheptanoic acid is also novel as a racemic mixture and the present invention also relates to that compound in racemic form which may be used in the same way as the said (-)-D-isomers.

    摘要翻译： 其中X代表酸性基团，特别是膦酸，磺酸，硼酸或四唑基团的通式为（IMA）的化合物的（ - ） - D-异构体，R代表亚烷基， 具有3个或更多个碳原子，优选3至6个碳原子或C3至C7环烷基的亚烯基或亚链炔基，A和B彼此独立地代表氢原子或亲油基团，特别是酯基，或 其盐或其药学上可接受的生物前体，特别是（ - ） - - - - - - - - - - - - - - - - - - - - 氨基膦酰基庚酸，（ - ） - D - 氨基膦酰庚酸可用于治疗中枢神经系统疾病。 化合物氨基膦酰庚酸也是新的外消旋混合物，本发明还涉及外消旋化合物，其可以以与所述（ - ） - D-异构体相同的方式使用。