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    Self-assembled ionophores
    1.
    发明授权
    Self-assembled ionophores 失效
    自组装离子载体

    公开(公告)号：US06448400B1

    公开(公告)日：2002-09-10

    申请号：US09380585

    申请日：1999-11-24

    申请人： Jeffrey T. Davis ,  Sampath K. Tirumala ,  Allison L. Marlow

    发明人： Jeffrey T. Davis ,  Sampath K. Tirumala ,  Allison L. Marlow

    IPC分类号： C07D47334

    CPC分类号： C07D473/00

    摘要： Ionophores having the capacity spontaneously assemble in solution and composed of hydrogen bonded monomers of 5′-(t-butyl-dimethylsilyl)-2′,3′-O-isopropylidene-isoguanosine, 5′-(t-butyl-dimethylsilyl)-2′,3′-O-isopropylidene-thio-isoguanosine or 2′,3′-Di-O-acetyl-5′-(t-butyl-dimethylsilyl)-isoguanosine are used to remove 137-cesium ions (137Cs+) from nuclear waste.

    摘要翻译： 具有在溶液中自发组装的5'-（叔丁基 - 二甲基甲硅烷基）-2'，3'-O-异亚丙基 - 异鸟嘌呤，5' - （叔丁基 - 二甲基甲硅烷基）-2 '，3'-O-异亚丙基 - 硫代 - 异鸟嘌呤或2'，3'-二-O-乙酰基-5' - （叔丁基 - 二甲基甲硅烷基） - 异胍苷用于从核中除去137-铯离子（137Cs +） 浪费。

    Purine derivatives having phosphodiesterase IV inhibition activity
    2.
    发明授权
    Purine derivatives having phosphodiesterase IV inhibition activity 失效
    具有磷酸二酯酶IV抑制活性的嘌呤衍生物

    公开(公告)号：US06228859B1

    公开(公告)日：2001-05-08

    申请号：US09210556

    申请日：1998-12-11

    申请人： David J. Cavalla ,  Mark Chasin ,  Peter Hofer ,  Andre Gehrig ,  Peter Wintergerst

    发明人： David J. Cavalla ,  Mark Chasin ,  Peter Hofer ,  Andre Gehrig ,  Peter Wintergerst

    IPC分类号： C07D47334

    CPC分类号： C07D473/30 ,  C07D473/34

    摘要： Disclosed are compounds of the formula (I): wherein R3 is selected from the group consisting of C1-10 alkyl, C1-10 alkenyl, C3-10 cycloalkyl, C4-10 cycloalkylalkyl or C3-10 cycloalkenyl, wherein said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or cycloalkenyl is optionally substituted in one position with hydroxy; or benzyl, wherein said benzyl is optionally substituted in one or two positions with halogen, alkoxy, cycloalkoxy or polycycloalkyl, and wherein said alkyl moiety of said alkoxy or cycloalkoxy substituent is optionally substituted in one position with hydroxy; R8 is selected from the group consisting of hydrogen, C1-10 alkyl, C1-10 alkenyl, C3-10 cycloalkyl, C4-10 cycloalkylalkyl or C3-10 cycloalkenyl, wherein said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or cycloalkenyl is optionally substituted in one position with hydroxy; or benzyl, wherein said benzyl is optionally substituted in one or two positions with halogen, alkoxy, cycloalkoxy or polycycloalkyl, and wherein said alkyl moiety of said alkoxy or cycloalkoxy is optionally substituted in one position with hydroxy; R6a and R6b are independently selected from the group consisting of hydrogen, C1-10 alkyl, C1-10 alkenyl, C3-10 cycloalkyl, C4-10 cycloalkylalkyl, or C3-10 cycloalkenyl, wherein said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or cycloalkenyl is optionally substituted in one position with hydroxy; and pharmaceutically acceptable salts thereof.

    摘要翻译： 公开了式（I）的化合物：其中R 3选自C 1-10烷基，C 1-10烯基，C 3-10环烷基，C 4-10环烷基烷基或C 3-10环烯基，其中所述烷基，烯基，环烷基 环烷基烷基或环烯基任选在一个位置被羟基取代; 或苄基，其中所述苄基在一个或两个位置任选被卤素，烷氧基，环烷氧基或多环烷基取代，并且其中所述烷氧基或环烷氧基取代基的所述烷基部分任选在一个位置被羟基取代; R 8选自 的氢，C 1-10烷基，C 1-10烯基，C 3-10环烷基，C 4-10环烷基烷基或C 3-10环烯基，其中所述烷基，烯基，环烷基，环烷基烷基或环烯基任选在一个位置被羟基取代; 或苄基，其中所述苄基在一个或两个位置任选被卤素，烷氧基，环烷氧基或多环烷基取代，并且其中所述烷氧基或环烷氧基的所述烷基部分任选在一个位置被羟基取代; R 6a和R 6b独立地选自 由氢，C 1-10烷基，C 1-10烯基，C 3-10环烷基，C 4-10环烷基烷基或C 3-10环烯基组成的基团，其中所述烷基，链烯基，环烷基，环烷基烷基或环烯基任选在一个位置被羟基取代 ;及其药学上可接受的盐。

    Carbamoyl tetrahydropyridine derivatives
    3.
    发明授权
    Carbamoyl tetrahydropyridine derivatives 失效
    氨基甲酰四氢吡啶衍生物

    公开(公告)号：US06600038B1

    公开(公告)日：2003-07-29

    申请号：US09914534

    申请日：2001-08-30

    申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshihito Kumagai ,  Kazuyuki Tomisawa

    发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshihito Kumagai ,  Kazuyuki Tomisawa

    IPC分类号： C07D47334

    CPC分类号： A61K31/519 ,  C07D473/00 ,  C07D487/04

    摘要： Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1-Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7)N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.

    摘要翻译： 由下式表示的氨基甲酰基四氢吡啶衍生物：[式中，R 1和R 2相同或不同，各自表示氢原子，C 1 -C 5烷基等; Y1-Y2表示（R4）C = C（R5），（R6）C = N，N = N，（R7）N-CO或N = C（R8） X1，X2和X3相同或不同，各自表示氢原子，卤素原子等; R3，R4，R5和R6相同或不同，各自表示氢原子或烷基; R7表示氢原子，C1-C5烷基等; 并且R8表示氢原子或氨基甲酰基]或其药学上可接受的盐，并且提供其制备的中间体。上述衍生物对于被认为涉及CRF的疾病是有效的。

    Carbocyclic nucleoside agents useful as selective inhibitors of proinflammatory cytokines
    4.
    发明授权
    Carbocyclic nucleoside agents useful as selective inhibitors of proinflammatory cytokines 失效
    可用作促炎细胞因子选择性抑制剂的碳环核苷

    公开(公告)号：US06541482B2

    公开(公告)日：2003-04-01

    申请号：US08383339

    申请日：1995-02-03

    申请人： Carl K. Edwards, III ,  David R Borcherding

    发明人： Carl K. Edwards, III ,  David R Borcherding

    IPC分类号： C07D47334

    CPC分类号： C07D473/00 ,  C07D471/04

    摘要： The present invention relates to compounds of the formula wherein X is N3, NH2, NHR, N(R)2, CN, SH, SR, or OR1; R is C1-C4 alkyl or (CH2)n—&phgr;; n is an integer 0, 1, 2, 3 or 4; &phgr; is a phenyl group unsubstituted or substituted with from 1 to 3 substituents, each substituent is independently selected from the group consisting of C1-C4 alkyl, C1-C4 alkoxy, halogen, CF3, OCF3, OH, CN, NO2 or NH2; R1 is C1-C4 alkyl or (CH2)m—NR2R3; m is an integer 1, 2, 3 or 4; R2 and R3 are each independently C1-C4 fluorinated akyl or cycloalkyl; The X substituent on the cyclopentanyl ring is in the TRANS configuration relative to the bicyclic substituent; Y is nitrogen; Z1 and Z2 are each independently hydrogen, halogen or NH2; and ---- represents a singe or double bond; or pharmaceutically acceptable salts thereof, compositions comprising such compounds, and methods of treatment comprising administering of such compounds.

    摘要翻译： 本发明涉及式X的化合物是N 3，NH 2，NHR，N（R）2，CN，SH，SR或OR 1; R是C 1 -C 4烷基或（CH 2）n-phi; n是整数0,1,2,3或4; phi是未取代或被1至3个取代基取代的苯基，每个取代基独立地选自C 1 -C 4烷基，C 1 -C 4烷氧基，卤素，CF 3，OCF 3，OH，CN，NO 2或NH 2; R1是C1-C4烷基或（CH2）m-NR2R3; m是整数1,2,3或4; R2和R3各自独立地为C1-C4氟化烷基或环烷基;环戊基环上的X取代基相对于双环取代基为TRANS构型; Y为氮; Z 1和Z 2各自独立地为氢，卤素或NH 2; 和 - 表示单键或双键;或其药学上可接受的盐，包含这些化合物的组合物，以及包括施用这些化合物的治疗方法。

    Methods of Synthesing Purine Compounds Having PDE Iv Inhibitory Activity
    7.
    发明授权
    Methods of Synthesing Purine Compounds Having PDE Iv Inhibitory Activity 有权
    合成具有PDE Iv抑制活性的嘌呤化合物的方法

    公开(公告)号：US06211367B1

    公开(公告)日：2001-04-03

    申请号：US09210557

    申请日：1998-12-11

    申请人： David J. Cavalla ,  Mark Chasin ,  Peter Hofer

    发明人： David J. Cavalla ,  Mark Chasin ,  Peter Hofer

    IPC分类号： C07D47334

    CPC分类号： C07D473/30 ,  C07D473/34

    摘要： The present invention comprises compounds having the general formula I: wherein: Y, is N or CH Z is selected from the group consisting of alkyl groups such as alkylene groups such as CH2, CH2CH2, CH(CH3); alkenyl groups such as CH═CH; alkynyl groups such as C≡C; and NH, N(C1-C3 alkyl), O, S, C(O)CH2 and OCH2; R1 and R2 are selected from the group consisting of hydrogen and a C1-C8 straight or branched alkyl or a C3-C8 cycloalkyl; R3 is a C3-C12 straight or branched alkyl; R4 is a C3-C10 cycloalkyl optionally substituted with OH or C3-C10 cycloalkenyl optionally substituted with OH; and R8 is a C1-C8 straight or branched alkyl or a C3-C8 cycloalkyl, optionally substituted with OH; and methods of synthesis.

    摘要翻译： 本发明包括具有通式I的化合物：其中：Y是N或CHZ选自烷基如亚烷基如CH 2，CH 2 CH 2，CH（CH 3）; 烯基如CH = CH; 炔基如C = C; 和NH，N（C 1 -C 3烷基），O，S，C（O）CH 2和OCH 2; R 1和R 2选自氢和C 1 -C 8直链或支链烷基或C 3 -C 8环烷基; R3是C3-C12直链或支链烷基; R4是任选被OH或任选被OH取代的C 3 -C 10环烯基取代的C 3 -C 10环烷基; 和R 8是任选被OH取代的C1-C8直链或支链烷基或C3-C8环烷基;以及合成方法。

    Substituted purine derivatives as inhibitors of cell adhesion
    8.
    发明授权
    Substituted purine derivatives as inhibitors of cell adhesion 失效
    取代嘌呤衍生物作为细胞粘附的抑制剂

    公开(公告)号：US06747016B1

    公开(公告)日：2004-06-08

    申请号：US10030290

    申请日：2002-03-06

    申请人： Anuschirwan Peyman ,  Jochen Knolle ,  Thomas R Gadek ,  Jean-Francois Gourvest ,  Jean-Marie Ruxer

    发明人： Anuschirwan Peyman ,  Jochen Knolle ,  Thomas R Gadek ,  Jean-Francois Gourvest ,  Jean-Marie Ruxer

    IPC分类号： C07D47334

    CPC分类号： C07D473/34

    摘要： The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R1, R2 and s have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonist and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or prolifertion of cells of the vascular smooth musculature. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中B，D，E，G，X，Y，Z，R 1，R 2和s具有权利要求书中所示的含义， 盐及其前药。 式（I）化合物是有价值的药理活性化合物。 它们是玻连蛋白受体拮抗剂和细胞粘附抑制剂，并且适用于治疗和预防基于玻连蛋白受体及其配体在细胞 - 细胞或细胞 - 基质相互作用过程中的相互作用的疾病，或可被预防，缓解或 通过影响这种相互作用来治愈。 例如，它们可以用于抑制破骨细胞的骨吸收，从而用于治疗和预防骨质疏松症，或用于抑制血管平滑肌肉细胞的不期望的血管生成或增殖。 本发明还涉及制备式（I）化合物，其用途，特别是作为药物中的活性成分的方法，以及包含它们的药物组合物。