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174 条记录 (耗时 0.079 秒)

    Process for making optically active alpha-amino ketones and selected novel optically active alpha-amino ketones
    102.
    发明授权
    Process for making optically active alpha-amino ketones and selected novel optically active alpha-amino ketones 失效
    制备光学活性α-氨基酮和选择的新型光学活性α-氨基酮的方法

    公开(公告)号：US06316656B1

    公开(公告)日：2001-11-13

    申请号：US09611334

    申请日：2000-07-05

    申请人： John J. Talley

    发明人： John J. Talley

    IPC分类号： C07C22900

    CPC分类号： B01J31/2409 ,  B01J31/24 ,  B01J2231/645 ,  B01J2531/822 ,  C07C231/12 ,  C07C233/47

    摘要： The invention includes selected novel optically active &agr;-ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.

    摘要翻译： 本发明包括选择性的新型光学活性α-酮，其本身可用或用作制备用作抗生素，抗生素增强剂或酶抑制剂的已知酮亚甲基伪肽的中间体。 此外，本发明提供了一种脱氢/不对称氢化的方法，以获得具有两个手性中心的基本上纯的对映体。

    Benz �G! indazolyl derivatives for the treatment of inflammation
    103.
    发明授权
    Benz �G! indazolyl derivatives for the treatment of inflammation 失效
    Benz [G]吲唑基衍生物用于治疗炎症

    公开(公告)号：US5696143A

    公开(公告)日：1997-12-09

    申请号：US309294

    申请日：1994-09-20

    申请人： John J. Talley ,  Stephen R. Bertenshaw ,  Roland S. Rogers

    发明人： John J. Talley ,  Stephen R. Bertenshaw ,  Roland S. Rogers

    IPC分类号： C07D231/54 ,  A61K31/415

    CPC分类号： C07D231/54

    摘要： A class of benz�g!indazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --CH.dbd.CH--; wherein R.sup.1 is selected from lower haloalkyl, cyano, lower alkoxycarbonyl, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.3 is one or more radicals selected from halo, lower alkylthio, lower alkylsulfinyl, lower alkyl, cyano, lower alkoxycarbonyl, aminocarbonyl, lower N-alkylaminocarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, lower hydroxyalkyl, lower haloalkoxy, amino, lower N,N-dialkylamino and nitro; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类苯并[g]吲唑基衍生物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式I（I）定义，其中A为-CH = CH-; 其中R 1选自低级卤代烷基，氰基，低级烷氧基羰基，低级N-烷基氨基羰基，N-苯基氨基羰基，低级N，N-二烷基氨基羰基和低级N-烷基-N-苯基氨基羰基。 其中R2是在可取代的位置被选自低级烷基磺酰基和氨磺酰基的基团取代的苯基; 并且其中R 3是一个或多个选自卤素，低级烷硫基，低级烷基亚磺酰基，低级烷基，氰基，低级烷氧基羰基，氨基羰基，低级N-烷基氨基羰基，低级卤代烷基，羟基，低级烷氧基，低级羟烷基，低级卤代烷氧基，氨基，低级 N，N-二烷基氨基和硝基; 或其药学上可接受的盐。

    Pyrazolyl derivatives for the treatment of inflammation
    104.
    发明授权
    Pyrazolyl derivatives for the treatment of inflammation 失效
    吡唑基衍生物用于治疗炎症

    公开(公告)号：US5670532A

    公开(公告)日：1997-09-23

    申请号：US719501

    申请日：1996-09-25

    申请人： John J. Talley ,  Stephen R. Bertenshaw ,  Matthew J. Graneto ,  Donald J. Rogier

    发明人： John J. Talley ,  Stephen R. Bertenshaw ,  Matthew J. Graneto ,  Donald J. Rogier

    IPC分类号： C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  A61K31/415 ,  A61K31/435 ,  C07D487/04

    CPC分类号： C07D491/04 ,  C07D495/04

    摘要： A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --; wherein X is S(O).sub.p or O; wherein m is 0 or 1; wherein n is 0 or 1; wherein p is 0 or 1; wherein B is selected from phenyl and five and six membered heteroaryl; wherein R.sup.1 is selected from lower haloalkyl, cyano, formyl, lower alkoxycarbonyl, lower alkoxy, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.4 is one or more radicals selected from hydrido, halo, lower alkylthio, lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, aminocarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, amino, lower N-alkylamino, lower N,N-dialkylamino, lower hydroxyalkyl and lower haloalkoxy; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类苯并吡喃并吡唑基衍生物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式I（I）定义，其中A是 - （CH 2）m -X-（CH 2）n - ; 其中X是S（O）p或O; 其中m为0或1; 其中n为0或1; 其中p为0或1; 其中B选自苯基和五元和六元杂芳基; 其中R 1选自低级卤代烷基，氰基，甲酰基，低级烷氧基羰基，低级烷氧基，低级N-烷基氨基羰基，N-苯基氨基羰基，低级N，N-二烷基氨基羰基和低级N-烷基-N-苯基氨基羰基。 其中R2是在可取代的位置被选自低级烷基磺酰基和氨磺酰基的基团取代的苯基; 氰基，羧基，低级烷氧基羰基，氨基羰基，低级卤代烷基，羟基，低级烷氧基，氨基，低级N-烷基氨基，低级N，低级烷基氨基，低级烷基氨基，低级烷基氨基， N-二烷基氨基，低级羟烷基和低级卤代烷氧基; 或其药学上可接受的盐。

    Substituted pyrazolyl benzenesulfonamides
    107.
    发明授权
    Substituted pyrazolyl benzenesulfonamides 失效
    取代的吡唑基苯磺酰胺

    公开(公告)号：US5510496A

    公开(公告)日：1996-04-23

    申请号：US456441

    申请日：1995-06-01

    申请人： John J. Talley ,  Thomas D. Penning ,  Paul W. Collins ,  James W. Malecha ,  Stephen R. Bertenshaw ,  Matthew J. Graneto

    发明人： John J. Talley ,  Thomas D. Penning ,  Paul W. Collins ,  James W. Malecha ,  Stephen R. Bertenshaw ,  Matthew J. Graneto

    IPC分类号： A61K31/415 ,  A61P11/06 ,  A61P17/06 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D495/04

    CPC分类号： C07D405/04 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D495/04

    摘要： A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R.sup.1 is selected from sulfamyl, fluoro, chloro, methyl, hydroxyl, methoxy and trifluoromethyl: wherein R.sup.2 is selected from hydrido, difiuoromethyl, trifluoromethyl, amido, dichloromethyl, trichloromethyl, pentafluoroethyl, cyano, heptatluoropropyl, difluorochloromethyl, methoxycarbonyl, dichlorofluoromethyl, N-phenylamido, N-3-fluorophenyl) amido, 2-pyridylamido, N-(4-methylphenyl)amido, hydroxypropyl, N-(3-chlorophenyl)amido, N-(4-methoxyphenyl)amido, hydroxymethyl, hydroxyethyl, carboxylpropyl, carboxymethyl and carboxyethyl; wherein R.sup.3 is selected from hydrido, methyl, triflouromethyl, fluoro, chloro and bromo; wherein R.sup.4 is selected from phenyl, biphenyl, pyrazinyl, cyclohexyl, cyclohexenyl and thienyl; and wherein R.sup.4 is optionally substituted at a substitutable position with one or more radicals selected from chloro, bromo, fluoro, methylthio, methylsulfonyl, morpholinyl, amino, methyl, ethyl, propyl, isopropyl, butyl, ethoxy, nitro, chloromethyl, trifluoromethoxy, trifluoroenhoxy, fluoromethyl, methoxy, difluoromethyl, trifluoromethyl, dichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, and difluoropropyl; or wherein R.sup.3 and R.sup.4 together form ##STR2## provided R.sup.2 and R.sup.3 are not both hydrido; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式I定义：其中R 1选自氨磺酰基，氟，氯，甲基，羟基，甲氧基和三氟甲基：其中R 2选自氢，二氟甲基，三氟甲基，酰氨基，二氯甲基， 三氯甲基，五氟乙基，氰基，七氟丙基，二氟氯甲基，甲氧基羰基，二氯氟甲基，N-苯基酰氨基，N-3-氟苯基）酰氨基，2-吡啶基酰氨基，N-（4-甲基苯基）酰氨基，羟丙基，N-（3-氯苯基） N-（4-甲氧基苯基）酰氨基，羟甲基，羟乙基，羧基丙基，羧甲基和羧乙基; 其中R 3选自氢，甲基，三氟甲基，氟，氯和溴; 其中R 4选自苯基，联苯基，吡嗪基，环己基，环己烯基和噻吩基; 并且其中R 4在可取代位置任选被一个或多个选自氯，溴，氟，甲硫基，甲基磺酰基，吗啉基，氨基，甲基，乙基，丙基，异丙基，丁基，乙氧基，硝基，氯甲基，三氟甲氧基，三氟甲氧基 氟甲基，甲氧基，二氟甲基，三氟甲基，二氯甲基，五氟乙基，七氟丙基，二氟氯甲基，二氯氟甲基，二氟乙基和二氟丙基; 或者其中R3和R4一起形成“IMAGE”，其中R2和R3不都是氢的; 或其药学上可接受的盐。

    Process for making optically active alpha-amino ketones and selected novel optically active alpha-amino ketones
    110.
    发明授权
    Process for making optically active alpha-amino ketones and selected novel optically active alpha-amino ketones 失效
    制备光学活性α-氨基酮和选择的新型光学活性α-氨基酮的方法

    公开(公告)号：US5488132A

    公开(公告)日：1996-01-30

    申请号：US232786

    申请日：1994-04-22

    申请人： John J. Talley

    发明人： John J. Talley

    IPC分类号： B01J31/24 ,  C07C231/12 ,  C07C233/47 ,  C07C229/00

    CPC分类号： B01J31/2409 ,  C07C231/12 ,  C07C233/47 ,  B01J2231/645 ,  B01J2531/822 ,  B01J31/24

    摘要： The invention includes selected novel optically active .alpha.-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.

    摘要翻译： 本发明包括选择性的新型光学活性α-氨基酮，其本身可用或用作制备用作抗生素，抗生素增强剂或酶抑制剂的已知酮亚甲基伪肽的中间体。 此外，本发明提供了一种脱氢/不对称氢化的方法，以获得具有两个手性中心的基本上纯的对映体。