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353 条记录 (耗时 0.018 秒)

    Phosphorus-containing cyclic nitroxide free radicals
    91.
    发明授权
    Phosphorus-containing cyclic nitroxide free radicals 失效
    含磷环状氮氧自由基

    公开(公告)号：US5006663A

    公开(公告)日：1991-04-09

    申请号：US433597

    申请日：1989-11-08

    申请人： Yves Berchadsky ,  Nelly Kernevez ,  Francois Le Moigne ,  Anne Mercier ,  Liliane Secourgeon ,  Paul Tordo

    发明人： Yves Berchadsky ,  Nelly Kernevez ,  Francois Le Moigne ,  Anne Mercier ,  Liliane Secourgeon ,  Paul Tordo

    IPC分类号： A61K49/20 ,  C07F9/572 ,  C07F9/59 ,  C07F9/6506 ,  C07F9/653 ,  C07F9/6533

    CPC分类号： A61K49/20 ,  C07F9/5726 ,  C07F9/597 ,  C07F9/65066 ,  C07F9/653 ,  C07F9/6533

    摘要： A nitroxide radical of the formula (I) or (II): ##STR1## in which R.sub.1 and R.sub.2 are independently chosen from among the optionally deuterated alkyl, alkoxyl, dialkylaminyl and phenyl radicals, H, D or Cl; R.sub.3, R.sub.8 and R.sub.9 are independently chosen from among the optionally deuterated alkyl, alkoxyl and phenyl radicals; R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are independently chosen from among the optionally deuterated alkyl, alkoxyl, dialkylaminyl and phenyl radicals, COOH, OH, OD, H, D, a halogen, COOR (in which R is an alkyl radical); R.sub.10 and R.sub.11 are independently chosen from among optionally deuterated alkyl, alkoxyl, dialkylaminyl and phenyl radicals, COOH, OH, OD, H, D, a halogen, COOR (in which R is an alkyl radical) or represent an oxygen atom linked with the cycle of the radical by a double bond is described.

    摘要翻译： 式（I）或（II）的氮氧自由基：其中R 1和R 2独立地选自任选的氘代烷基，烷氧基，二烷基氨基和苯基，H， D或Cl; R3，R8和R9独立地选自任选的氘代烷基，烷氧基和苯基; R 4，R 5，R 6和R 7独立地选自任选的氘代烷基，烷氧基，二烷基氨基和苯基，COOH，OH，OD，H，D，卤素，COOR（其中R是烷基） R 10和R 11独立地选自氘代烷基，烷氧基，二烷基氨基和苯基，COOH，OH，OD，H，D，卤素，COOR（其中R是烷基）或代表与 描述了基团的双键循环。

    2-oxy-4H-3,1-benzoxazin-4-ones and related compounds and pharmaceutical use
    93.
    发明授权
    2-oxy-4H-3,1-benzoxazin-4-ones and related compounds and pharmaceutical use 失效
    2-氧-4H-3,1-苯并恶嗪-4-酮及相关化合物及药物用途

    公开(公告)号：US4745116A

    公开(公告)日：1988-05-17

    申请号：US945751

    申请日：1986-12-23

    申请人： Alexander Krantz ,  Robin Spencer ,  Tim Tam ,  Teng J. Liak

    发明人： Alexander Krantz ,  Robin Spencer ,  Tim Tam ,  Teng J. Liak

    IPC分类号： C07D265/26 ,  C07F9/6533 ,  A61K31/535 ,  C07D265/36

    CPC分类号： C07D265/26 ,  C07F9/65335

    摘要： 2-Oxy-4H-3,1-benzoxazin-4-ones, useful as serine protease inhibitors, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein:a is an integer of 1 to 4;A is a bond, or alkylene having one to eight carbon atoms;R is hydrogen, phenyl, imidazolyl or cycloalkyl having three to six carbon atoms, wherein the phenyl, imidazolyl or cycloalkyl ring is optionally substituted with 1 to 3 substituents independently selected from the group consisting of lower alkyl having one to four carbon atoms, lower alkoxy having one to four carbon atoms, --N(R.sup.1).sub.2, --NO.sub.2, halo or lower alkylthio having one to four carbon atoms, and,each R' is independently selected from the group consisting of hydroxy, benzyloxy, lower alkyl having one to six atoms, lower alkenyl having two to six carbon atoms, lower alkoxy having one to six carbon atoms, lower alkylthio or halo-lower alkyl having one to six carbon atoms, halo, --NO.sub.2, --N(R.sup.1).sub.2, --NR.sup.1 CO.sub.2 R.sup.2, --NR.sup.1 COR.sup.2, and --NR.sup.1 C(O)N(R.sup.1).sub.2,in whicheach R.sup.1 is independently hydrogen or lower alkyl having one to four carbon atoms, or together form a piperidine or a piperazine ring optionally substituted at the ring nitrogen by lower alkyl having one to four carbon atoms or --CH.sub.2 CH.sub.2 OH;each R.sup.2 is independently lower alkyl having one to four carbon atoms,A is an alkylene group if R is hydrogen,or a pharmaceutically acceptable acid addition salt thereof.

    摘要翻译： 2-氧代-4H-3,1-苯并恶嗪-4-酮，其可用作丝氨酸蛋白酶抑制剂，由下式表示：其中：a为1的整数 到4; A是键或具有1-8个碳原子的亚烷基; R是氢，苯基，咪唑基或具有3至6个碳原子的环烷基，其中苯基，咪唑基或环烷基环任选地被1至3个独立地选自具有1至4个碳原子的低级烷基，低级烷氧基 具有1-4个碳原子的-N（R 1）2，-NO 2，卤素或具有1至4个碳原子的低级烷硫基，并且每个R'独立地选自羟基，苄氧基，具有一个至 六个原子，具有2-6个碳原子的低级烯基，具有1-6个碳原子的低级烷氧基，具有1-6个碳原子的低级烷硫基或卤代低级烷基，卤素，-NO 2，-N（R 1）2，-NR 1 CO 2 R 2， -NR1COR2和-NR1C（O）N（R1）2，其中每个R1独立地是氢或具有1-4个碳原子的低级烷基，或者一起形成在环氮上被低级烷基任意取代的哌啶或哌嗪环 具有1-4个碳原子或-CH 2 CH 2 OH; 每个R 2独立地是具有1-4个碳原子的低级烷基，如果R是氢，则A是亚烷基，或其药学上可接受的酸加成盐。

    Phosphates of resorufin derivatives and compositions thereof for the determination of the activity of phosphatases
    94.
    发明授权
    Phosphates of resorufin derivatives and compositions thereof for the determination of the activity of phosphatases 失效
    用于测定磷酸酶活性的雷蛇烯衍生物的磷酸盐及其组合物

    公开(公告)号：US4719097A

    公开(公告)日：1988-01-12

    申请号：US912395

    申请日：1986-09-26

    申请人： Klaus Muhlegger ,  Herbert von der Eltz

    发明人： Klaus Muhlegger ,  Herbert von der Eltz

    IPC分类号： C07F9/6533 ,  C12Q1/42 ,  A61K31/675 ,  C07F9/65

    CPC分类号： C07F9/65335 ,  C12Q1/42 ,  C12Q2334/00

    摘要： The present invention provides phosphates of resorufin derivatives of the general formulae: ##STR1## wherein R.sup.2 and R.sup.5, which can be the same or different, are hydrogen or halogen atoms or lower alkyl radicals, R.sup.1, R.sup.3, R.sup.4 and R.sup.6, which can be the same or different, are hydrogen or halogen atoms, cyano or carboxy groups or lower alkyl, lower alkoxy, lower alkoxycarbonyl, carboxy lower alkyl or lower alkoxycarbonyl lower alkyl radicals or carboxamide groups which are optionally mono- or disubstituted or radicals of the general formula --COO--(CH.sub.2 CH.sub.2 O).sub.n --R.sup.7, R.sup.7 being a hydrogen atom or a lower alkyl radical and n being a whole number of from 1 to 4, and wherein R.sup.6 can additionally also be a sulphonyl or nitro group, Y is a nitrogen atom or an N.fwdarw.O group and M and M', which can be the same or different, are hydrogen atoms or alkali metal, alkaline earth metal or ammonium ions.The present invention also provides processes for the preparation of these compounds and diagnostic agents containing them for the detection of phosphatases.

    摘要翻译： 本发明提供了以下通式的聚砜衍生物的磷酸盐：其中R 2和R 5可以相同或不同，为氢或卤素原子或低级烷基，R 1，R 2， 可以相同或不同的R 3，R 4和R 6是氢或卤素原子，氰基或羧基或低级烷基，低级烷氧基，低级烷氧基羰基，羧基低级烷基或低级烷氧基羰基低级烷基或羧酰胺基， - 或二取代的或通式-COO-（CH 2 CH 2 O）n -R 7，R 7为氢原子或低级烷基的基团，n为1至4的整数，并且其中R 6还可以为磺酰基 或硝基，Y是氮原子或N-> O基，M和M'可以相同或不同，是氢原子或碱金属，碱土金属或铵离子。 本发明还提供了制备这些化合物的方法和含有它们用于检测磷酸酶的诊断剂。

    2-oxy-4H-3,1-benzoxazin-4-ones and pharmaceutical use
    95.
    发明授权
    2-oxy-4H-3,1-benzoxazin-4-ones and pharmaceutical use 失效
    2-氧基-4H-3,1-苯并恶嗪-4-酮和药物用途

    公开(公告)号：US4665070A

    公开(公告)日：1987-05-12

    申请号：US748631

    申请日：1985-06-25

    申请人： Alexander Krantz ,  Robin Spencer ,  Tim Tam ,  Teng J. Liak

    发明人： Alexander Krantz ,  Robin Spencer ,  Tim Tam ,  Teng J. Liak

    IPC分类号： C07D265/24 ,  A61K31/535 ,  A61K31/536 ,  A61P43/00 ,  C07D265/18 ,  C07D265/26 ,  C07F9/6533 ,  C07D265/36

    CPC分类号： C07D265/26 ,  C07F9/65335

    摘要： 2-Oxy-4H-3,1-benzoxazin-4-ones represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-4;A is a bond, or alkylene having one to eight carbon atoms;R is hydrogen, phenyl, imidazolyl or cycloalkyl having three to six carbon atoms, wherein the phenyl, imidazolyl or cycloalkyl ring is optionally substituted with 1-3 substituents independently selected from the group consisting of lower alkyl having one to four carbon atoms, lower alkoxy having one to four carbon atoms, --N(R.sup.1).sub.2, --NO.sub.2, halo or lower alkylthio having one to four carbon atoms, and,each R' is independently selected from the group consisting of lower alkyl having one to six atoms, lower alkenyl having two to six carbon atoms, lower alkoxy having one to six carbon atoms,lower alkylthio or halo-lower alkyl having one to four carbon atoms, halo, --NO.sub.2, --N(R.sup.1).sub.2, ##STR2## --NR.sup.1 COR.sup.2, and ##STR3## in which each R.sup.1 is independently hydrogen or lower alkyl having one to four carbon atoms, or together form a piperidine or a piperazine ring optionally substituted at the ring nitrogen by lower alkyl having one to four carbon atoms or --CH.sub.2 CH.sub.2 OH,each R.sup.2 is independently lower alkyl having one to four carbon atoms,A is an alkylene group if R is hydrogen,and the pharmaceutically acceptable acid addition salts thereof are useful as serine protease inhibitors in humans and animals.

    摘要翻译： 由式（I）表示的2-氧代-4H-3,1-苯并恶嗪-4-酮及其药学上可接受的酸加成盐，其中：a为0-4的整数; A是键或具有1-8个碳原子的亚烷基; R是氢，苯基，咪唑基或具有3至6个碳原子的环烷基，其中苯基，咪唑基或环烷基环任选地被1-3个独立地选自具有1-4个碳原子的低级烷基，低级烷氧基 具有1-4个碳原子的-N（R 1）2，-NO 2，卤代或低级烷硫基，每个R'独立地选自具有1-6个原子的低级烷基，低级烷基 具有2-6个碳原子的烯基，具有1-6个碳原子的低级烷氧基，具有1-4个碳原子的低级烷硫基或卤代低级烷基，卤素，-NO 2，-N（R 1）2，-NR 1 COR 2和 其中每个R 1独立地为氢或具有1-4个碳原子的低级烷基，或者一起形成哌啶或哌嗪环，其任选在环氮上被具有1-4个碳原子的低级烷基或-CH 2 CH 2 OH取代，每个R 2 独立地是低级烷基 g为1-4个碳原子，如果R为氢，则A为亚烷基，其药学上可接受的酸加成盐可用作人和动物中的丝氨酸蛋白酶抑制剂。

    Coordination complexes of optically active phosphine compounds
    99.
    发明授权
    Coordination complexes of optically active phosphine compounds 失效
    光学活性膦化合物的配位络合物

    公开(公告)号：US4464306A

    公开(公告)日：1984-08-07

    申请号：US459275

    申请日：1983-01-19

    申请人： William C. Christopfel ,  William S. Knowles

    发明人： William C. Christopfel ,  William S. Knowles

    IPC分类号： C07F9/50 ,  C07F9/53 ,  C07F9/6533 ,  C07F15/00

    CPC分类号： C07F15/00 ,  C07F9/5004 ,  C07F9/5022 ,  C07F9/5304 ,  C07F9/5325 ,  C07F9/6533

    摘要： The invention is a new family of phosphine compounds which can be used to make optically active metal coordination complex catalysts which combine high efficiency with a capability of performing rapidly (high efficiency and rapidly being established from Tables I, II and III as being greater than 75% efficiency and in times of not more than a few hours, preferably less than one hour) in water and thus avoiding solvent recovery and loss problems. The catalysts can be used in some alcoholic mediums as well as in some aqueous mediums. These catalysts are useful in catalytic asymmetric hydrogenation of some olefinic compounds. The new phosphine compounds are made from novel phosphine oxides.

    摘要翻译： 本发明是一种新的膦化合物系列，其可用于制备光学活性金属配位络合物催化剂，其具有高效率和快速（快速地从表I，II和III中确定为高于75）的能力 ％的效率和不超过几个小时，优选少于1小时的时间），从而避免溶剂回收和损失问题。 催化剂可用于一些醇介质以及某些水性介质中。 这些催化剂可用于某些烯烃化合物的催化不对称氢化。 新的膦化合物由新的氧化膦制成。

    Optically active phosphine compounds
    100.
    发明授权
    Optically active phosphine compounds 失效
    光活性膦化合物

    公开(公告)号：US4376870A

    公开(公告)日：1983-03-15

    申请号：US213272

    申请日：1980-12-05

    申请人： William C. Christopfel ,  William S. Knowles

    发明人： William C. Christopfel ,  William S. Knowles

    IPC分类号： B01J31/24 ,  B01J25/00 ,  C07B53/00 ,  C07B61/00 ,  C07C231/00 ,  C07C231/18 ,  C07C233/65 ,  C07F9/50 ,  C07F9/53 ,  C07F9/6533 ,  C07F15/00

    CPC分类号： C07F15/008 ,  C07F9/5004 ,  C07F9/5022 ,  C07F9/5304 ,  C07F9/5325 ,  C07F9/6533

    摘要： The invention is a new family of phosphine compounds which can be used to make optically active metal coordination complex catalysts which combine high efficiency with a capability of performing rapidly (high efficiency and rapidly being established from Tables I, II and III as being greater than 75% efficiency and in times of not more than a few hours, preferably less than one hour) in water and thus avoiding solvent recovery and loss problems. The catalysts can be used in some alcoholic mediums as well as in some aqueous mediums. These catalysts are useful in catalytic asymmetric hydrogenation of some olefinic compounds. The new phosphine compounds are made from novel phosphine oxides.

    摘要翻译： 本发明是一种新的膦化合物系列，其可用于制备光学活性金属配位络合物催化剂，其具有高效率和快速（快速地从表I，II和III中确定为高于75）的能力 ％的效率和不超过几个小时，优选少于1小时的时间），从而避免溶剂回收和损失问题。 催化剂可用于一些醇介质以及某些水性介质中。 这些催化剂可用于某些烯烃化合物的催化不对称氢化。 新的膦化合物由新的氧化膦制成。