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381 条记录 (耗时 0.018 秒)

    Pyridyl substituted cyclopentadienes for the treatment of inflamation
    91.
    发明授权
    Pyridyl substituted cyclopentadienes for the treatment of inflamation 失效
    吡啶基取代环戊二烯用于治疗炎症

    公开(公告)号：US5576339A

    公开(公告)日：1996-11-19

    申请号：US417341

    申请日：1995-04-05

    申请人： Horng-Chih Huang ,  David R. Reitz

    发明人： Horng-Chih Huang ,  David R. Reitz

    IPC分类号： C07C311/16 ,  C07C317/14 ,  A61K31/44

    CPC分类号： C07C317/14 ,  C07C311/16 ,  C07C2101/10

    摘要： A class of 2,3-substituted cyclopenta-2,4-dienyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, lower alkyl, lower hydroxyalkyl, halo, lower haloalkyl, lower alkoxycarbonyl and carboxyl; and wherein each of R.sup.3 through R.sup.12 is independently selected from hydrido, halo, lower alkyl, lower alkylthio, cyano, hydroxyl, mercapto, lower haloalkyl, lower haloalkoxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl, lower alkylsulfonyl, lower haloalkylsulfonyl and sulfamyl; provided R.sup.5 and R.sup.10 are not both hydrido or methoxy; or a pharmaceutically suitable salt or prodrug thereof.

    摘要翻译： 描述了一类2,3-取代的环戊二烯-2,4-二烯基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II定义：倾向选自氢化，低级烷基，低级羟烷基，卤素，低级卤代烷基，低级烷氧基羰基和羧基; R 3至R 12各自独立地选自氢，卤素，低级烷基，低级烷硫基，氰基，羟基，巯基，低级卤代烷基，低级卤代烷氧基，低级烷氧基，低级羟烷基，低级烷氧基烷基，低级烷基磺酰基，低级卤代烷基磺酰基和氨磺酰基。 条件是R 5和R 10不同时为氢或甲氧基; 或其药学上合适的盐或前药。

    Halogenated phenylacetonitrile alkylaminoalkylphenyl compounds as immunosuppressives
    97.
    发明授权
    Halogenated phenylacetonitrile alkylaminoalkylphenyl compounds as immunosuppressives 失效
    卤代苯乙腈烷基氨基烷基苯基化合物作为免疫抑制剂

    公开(公告)号：US5451604A

    公开(公告)日：1995-09-19

    申请号：US97809

    申请日：1993-07-26

    申请人： Richard A. Mueller ,  Thomas E. Barta ,  John P. McKearn ,  Susan A. Gregory ,  Richard A. Partis ,  Francis J. Koszyk

    发明人： Richard A. Mueller ,  Thomas E. Barta ,  John P. McKearn ,  Susan A. Gregory ,  Richard A. Partis ,  Francis J. Koszyk

    IPC分类号： C07C255/42 ,  A61K31/275 ,  C07C247/06 ,  C07C255/35

    CPC分类号： C07C255/42 ,  C07C2101/10

    摘要： A class of halogenated phenylacetonitrile alkylaminoalkylphenyl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula ##STR1## wherein m is a number selected from three to five, inclusive; wherein n one or two; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein each of R.sup.3 through R.sup.7 is selected from hydrido, fluoro, chloro, bromo, azide, trifluoromethyl, difluorochloromethyl, 1,1-difluoroethyl, 2,2,2-trifluoroethyl, perfluoroethyl and 2,2,2,3-tetrafluoropropyl; with the proviso that at least one of R.sup.3 through R.sup.7 is selected from fluoro and trifluoromethyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类具有免疫抑制特性的卤代苯基乙腈烷基氨基烷基苯基化合物。 该类化合物可用于减少移植器官的受体排斥和治疗自身免疫性或炎性疾病。 特别感兴趣的化合物具有下式：其中m是选自三至五的数字，包括端值; 其中n个或两个; 其中R1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，叔丁基，异丁基，正戊基，异戊基，环丙基，环丁基，环戊基，环己基，环丙基甲基，环丁基甲基，环戊基甲基 ，环己基甲基，苄基和苯乙基; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，叔丁基，异丁基，正戊基，异戊基，环丙基，环丁基，环戊基，环己基，环丙基甲基，环丁基甲基，环戊基甲基 ，环己基甲基，苄基和苯乙基; 其中R3至R7各自选自氢，氟，氯，溴，叠氮化物，三氟甲基，二氟氯甲基，1,1-二氟乙基，2,2,2-三氟乙基，全氟乙基和2,2,2,3-四氟丙基; 条件是R3至R7中的至少一个选自氟和三氟甲基; 或其互变异构体或其药学上可接受的盐。

    Method for preparing cyclopentadienyl-type ligands and metallocene compounds
    99.
    发明授权
    Method for preparing cyclopentadienyl-type ligands and metallocene compounds 失效
    制备环戊二烯基型配体和金属茂化合物的方法

    公开(公告)号：US5420320A

    公开(公告)日：1995-05-30

    申请号：US255591

    申请日：1994-06-08

    申请人： Roland Zenk ,  Helmut G. Alt ,  M. Bruce Welch ,  Syriac J. Palackal

    发明人： Roland Zenk ,  Helmut G. Alt ,  M. Bruce Welch ,  Syriac J. Palackal

    IPC分类号： C07C13/15 ,  C07C13/567 ,  C07F17/00 ,  C07C1/00 ,  C07F7/00

    CPC分类号： C07C13/567 ,  C07C13/15 ,  C07F17/00 ,  C07C2101/10 ,  C07C2103/18

    摘要： In accordance with the present invention there is provided a process for preparing a cyclopentadienyl-type ligand, the process comprises (1) reacting an alkali metal salt of a cyclopentadienyl-type compound and an aminofulvene compound to form a monoanion, (2) reacting the monoanion and a reducing agent to form a dianion, and (3) reacting the dianion and water to produce the cyclopentadienyl-type ligand. Another aspect of the present invention includes a process for preparing a metallocene compound comprising reacting the dianion of step (2) and a transition metal-containing compound to form the metallocene compound. Another aspect of the present invention includes a process for preparing a metallocene compound comprising reacting the ligand of step (3) and an alkali metal compound to form a dianion and then reacting the dianion with a transition metal-containing compound to form the metallocene compound.

    摘要翻译： 根据本发明，提供了一种制备环戊二烯基型配体的方法，该方法包括（1）使环戊二烯基型化合物的碱金属盐与氨基富烯化合物反应形成单阴离子，（2）使 单阴离子和还原剂形成二价阴离子，和（3）使二阴离子和水反应以产生环戊二烯基型配体。 本发明的另一方面包括一种制备茂金属化合物的方法，包括使步骤（2）的二价阴离子与含过渡金属的化合物反应形成茂金属化合物。 本发明的另一方面包括制备茂金属化合物的方法，包括使步骤（3）的配体与碱金属化合物反应形成二价阴离子，然后使二价阴离子与含过渡金属的化合物反应，形成茂金属化合物。

    Metallocenes and processes therefor and therewith
    100.
    发明授权
    Metallocenes and processes therefor and therewith 失效
    金属茂及其处理方法及其

    公开(公告)号：US5399636A

    公开(公告)日：1995-03-21

    申请号：US75712

    申请日：1993-06-11

    申请人： Helmut G. Alt ,  Konstantinos Patsidis ,  M. Bruce Welch ,  Rolf L. Geerts ,  Bernd Peifer ,  Syriac J. Palackal

    发明人： Helmut G. Alt ,  Konstantinos Patsidis ,  M. Bruce Welch ,  Rolf L. Geerts ,  Bernd Peifer ,  Syriac J. Palackal

    IPC分类号： B01J31/16 ,  B01J31/22 ,  C07C13/567 ,  C07F17/00 ,  C08F4/619 ,  C08F4/6192 ,  C08F10/00 ,  C08F4/648

    CPC分类号： B01J31/1633 ,  B01J31/2295 ,  C07C13/567 ,  C07F17/00 ,  C08F10/00 ,  B01J2531/36 ,  B01J2531/37 ,  B01J2531/46 ,  B01J2531/48 ,  B01J2531/49 ,  B01J2531/56 ,  C07B2200/11 ,  C07C2101/10 ,  C07C2103/18 ,  C08F4/61912 ,  C08F4/61916 ,  C08F4/61927

    摘要： A composition is provided comprising a metallocene having the formula of: ##STR1## wherein each Z can be the same or different hydrocarbyl radical selected from the group consisting of cyclopentadienyl, indenyl, tetrahydroindenyl, fluorenyl, and mixtures thereof; each X can be the same or different and is selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, R, OR, NR.sub.2, PR.sub.2, or OQ, or mixtures thereof wherein the R is a C.sub.1 -C.sub.20 hydrocarbyl radical and Q is an inorganic moiety selected from the group consisting of silica, alumina, clay, phosphated alumina, and mixtures thereof; each Y can be the same or different and is an alkyl group, hydrogen, fluorine, chlorine, bromine, iodine, or mixtures thereof; E is selected from C, Sn, Si, Ge, B, Al, N, or P; M is a metal selected from Ti, Zr, Hf, Sc, Y, V, or La; m is a number sufficient to fill out the valences of metal M; and n is 1 or 2. Also provided is a process for preparing the metallocene by contacting a hydrocarbon having an acidic, replaceable hydrogen with an organolithium and an organohalosilane to prepare a ligand which is then contacted with an organo alkali metal compound to form a bridged ligand followed by contacting the bridged ligand with an organolithium and a metal halide. The composition is useful for olefin polymerization, hydrogenation, alkene epoxidation, alkene isomerization, and ketone reduction.

    摘要翻译： 提供了一种组合物，其包含具有下式的茂金属：其中每个Z可以是相同或不同的选自环戊二烯基，茚基，四氢茚基，芴基及其混合物的烃基; 每个X可以相同或不同，并且选自氢，氟，氯，溴，碘，R，OR，NR2，PR2或OQ，或其混合物，其中R是C1-C20烃基 Q是选自二氧化硅，氧化铝，粘土，磷酸化氧化铝及其混合物的无机部分; 每个Y可以相同或不同，并且是烷基，氢，氟，氯，溴，碘或其混合物; E选自C，Sn，Si，Ge，B，Al，N或P; M是选自Ti，Zr，Hf，Sc，Y，V或La的金属; m是足以填充金属M的价数; 并且n为1或2.还提供了通过使具有酸性可置换氢的烃与有机锂和有机卤代硅烷接触来制备金属茂的方法，以制备配体，然后与有机碱金属化合物接触以形成桥连 配体，然后使桥连配体与有机锂和金属卤化物接触。 该组合物可用于烯烃聚合，氢化，烯烃环氧化，烯烃异构化和酮还原。