利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

54 条记录 (耗时 0.038 秒)

    24-homo vitamin D derivatives, process for their production and pharmaceutical preparations obtained therefrom
    34.
    发明授权
    24-homo vitamin D derivatives, process for their production and pharmaceutical preparations obtained therefrom 失效
    24-homo维生素D衍生物，其制备方法和由其获得的药物制剂

    公开(公告)号：US5665716A

    公开(公告)日：1997-09-09

    申请号：US592017

    申请日：1990-10-02

    申请人： Gerald Kirsch ,  Gunter Neef ,  Katicia Schwarz ,  Matthias Brautigam ,  Ruth Thieroff-Ekerdt ,  Petra Rach

    发明人： Gerald Kirsch ,  Gunter Neef ,  Katicia Schwarz ,  Matthias Brautigam ,  Ruth Thieroff-Ekerdt ,  Petra Rach

    IPC分类号： A61K31/59 ,  A61P3/02 ,  A61P35/00 ,  A61P43/00 ,  C07C401/00

    CPC分类号： C07C401/00

    摘要： New 24-homo vitamin D derivatives of formula I ##STR1## are described, in which R.sup.1 means a hydrogen atom, a hydroxy, an alkanoyloxy group with 1 to 8 carbon atoms or an aralkanoyloxy group with up to 8 carbon atoms,R.sup.2 and R.sup.3, independently of one another, mean a linear or branched alkyl group with 1 to 4 carbon atoms, a trifluoromethyl group or together mean a saturated carbocyclic ring with 3 to 9 carbon atoms formed with carbon atom 25,R.sup.4 and R.sup.5, independently of one another, mean a hydrogen atom, an alkanoyl group with 1 to 8 carbon atoms or an aralkanoyl group with up to 8 carbon atoms, andA and B each mean a hydrogen or together a second bond, andn stands for 1, 2, 3,4 or 5.

    摘要翻译： 描述了式I（I）1的新的24-高维生素D衍生物，其中R 1表示氢原子，羟基，具有1至8个碳原子的烷酰氧基或具有至多8个碳原子的芳烷酰氧基 R2和R3彼此独立地表示具有1至4个碳原子的直链或支链烷基，三氟甲基或一起表示与碳原子25，R4和R5形成的具有3至9个碳原子的饱和碳环， 彼此独立地表示氢原子，具有1至8个碳原子的烷酰基或具有至多8个碳原子的芳烷酰基，A和B各自表示氢或一起形成第二键，n表示1， 2,3,4或5。

    10.beta.,11.beta.-bridged steroids
    37.
    发明授权
    10.beta.,11.beta.-bridged steroids 失效
    10（BETA），11（BETA）-BRIDGED STEROIDS

    公开(公告)号：US5093507A

    公开(公告)日：1992-03-03

    申请号：US367165

    申请日：1989-06-16

    申请人： Cornelius Scheidges ,  Eckhard Ottow ,  Gunter Neef ,  Sybille Beier ,  Walter Elger

    发明人： Cornelius Scheidges ,  Eckhard Ottow ,  Gunter Neef ,  Sybille Beier ,  Walter Elger

    IPC分类号： A61K31/58 ,  A61P3/06 ,  A61P3/08 ,  A61P5/38 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P27/02 ,  A61P35/00 ,  A61P43/00 ,  C07B61/00 ,  C07J31/00 ,  C07J41/00 ,  C07J63/00 ,  C07J71/00

    CPC分类号： C07J31/003 ,  C07J41/0044 ,  C07J71/0078

    摘要： 10.beta.,11.beta.-bridged steroids of Formula I ##STR1## wherein R.sup.1 is H or methyl;R.sup.2 is H, a cyanide residue, a heteroaryl residue, a straight-chain or branched aliphatic, e.g., alkyl group of up to 20 carbon atoms, optionally exhibiting double or triple bonds and, if desired, being substituted by one or several oxo groups, a C.sub.4-7 cycloalkyl or C.sub.4-7 cycloalkenyl group, an OR.sup.3 --, SR.sup.3 --, --OSO.sub.2 --R.sup.11 -- group wherein R.sup.11 means a perfluroinated C.sub.1 -C.sub.4 -alkyl group or an NR.sup.3 R.sup.4 -group wherein R.sup.3 means an H atom or C.sub.1 -C.sub.8 -alkyl residue, R.sup.4 means R.sup.3, a cyanide or a C.sub.1 -C.sub.10 -acyl residue, or R.sup.3 and R.sup.4 jointly with the inclusion of N means of 5- or 6-membered heterocyclic ring wherein the ring can additionally contain a further hetero atom N, O, or S, or a 4-cyano-, 4-methoxy- or 4-dimethylamino-substituted phenyl group,A and B either mean jointly a further bond between C4 and C5, or A is an .alpha.-hydroxy group and B is H,X is a keto or oxime group, andZ is a pentagonal or hexagonal ring residue which is optionally substituted and optionally unsaturated,or pharmaceutically compatible acid additional salts thereof which possess antigestagen and antiglucocorticoid properties.

    摘要翻译： 10β，11β-桥连类固醇，其中R1是H或甲基; R2是H，氰化物残基，杂芳基残基，直链或支链脂族，例如至多20个碳原子的烷基，任选地表现出双键或三键，并且如果需要，被一个或几个氧代基团 ，C4-7环烷基或C4-7环烯基，OR3-，SR3-，-OSO2-R11-基，其中R11表示全氟化C1-C4-烷基或NR3R4-基团，其中R3表示H原子或C1 -C 8 - 烷基残基，R4表示R3，氰化物或C1-C10酰基残基，或R3和R4与N或5元或6元杂环的N基相结合，其中环可以另外含有另外的杂原子 原子N，O或S或4-氰基 - ，4-甲氧基 - 或4-二甲基氨基取代的苯基，A和B可以共同意指C4和C5之间的另一个键，或A是α-羟基 并且B是H，X是酮基或肟基，Z是任选被取代且任选不饱和的五
    角或六方晶的残基，或药学上相容性 其酸性附加盐，其具有抗老化和抗糖皮质激素特性。

    Antigestagenically active steroids with a fluorinated 17alpha-alkyl chain
    38.
    发明申请
    Antigestagenically active steroids with a fluorinated 17alpha-alkyl chain 失效
    具有氟化17α-烷基链的抗发生活性类固醇

    公开(公告)号：US20050080060A1

    公开(公告)日：2005-04-14

    申请号：US10948652

    申请日：2004-09-24

    申请人： Wolfgang Schwede ,  Arwed Cleve ,  Ulrich Klar ,  Gunter Neef ,  Kristof Chwalisz ,  Martin Schneider ,  Ulrike Fuhrmann ,  Holger Heb-Stumpp

    发明人： Wolfgang Schwede ,  Arwed Cleve ,  Ulrich Klar ,  Gunter Neef ,  Kristof Chwalisz ,  Martin Schneider ,  Ulrike Fuhrmann ,  Holger Heb-Stumpp

    IPC分类号： A61K31/56 ,  A61P5/36 ,  C07J1/00 ,  C07J41/00 ,  C07J43/00 ,  C07J53/00

    CPC分类号： C07J1/0033 ,  C07J41/0083 ,  C07J41/0094 ,  C07J43/003 ,  C07J53/002

    摘要： This invention describes the new 17α-fluoroalkyl steroids of general formula I in which R1 stands for a methyl or ethyl group, R2 stands for a radical of formula CnFmHo, whereby n is 2, 3, 4, 5 or 6, m>1 and m+o=2n+1, R3 stands for a free, etherified or esterified hydroxy group, R4 and R5 each stand for a hydrogen atom, or together for an additional bond or a methylene group, St stands for a steroidal ABC-ring system of partial formula A, B or C in which R6 means a hydrogen atom, a straight-chain C1-C4 alkyl group or branched C3-C4 alkyl group or a halogen atom, R7 means a hydrogen atom, a straight-chain C1-C4 alkyl group or a branched C3-C4 alkyl group, or if St stands for a steroidal ABC-ring system A or B, in addition R6 and R7 together can mean an additional bond, X means an oxygen atom, a hydroxyimino grouping ═N—OH or two hydrogen atoms, R8 means a radical Y or an aryl radical that is optionally substituted in several places with a group Y, whereby Y is a hydrogen atom, a halogen atom, an —OH, —NO2, —N3, —CN, —NR9aR9b, —NHSO2R9, —CO2R9, C1-C10 alkoxy, C1-C10 alkanoyloxy, benzoyloxy, C1-C10 alkanoyl, C1-C10 hydroxyalkyl or benzoyl group, and R9a and R9b are the same or different and in the same way as R9 represent a hydrogen atom or a C1-C10 alkyl group, and for —NR9aR9b radicals, as well as their physiologically compatible salts with acids and for —CO2R9 radicals with R9 meaning hydrogen, as well as their physiologically compatible salts with bases. The new compounds have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.

    摘要翻译： 本发明描述了通式I的新型17α-氟烷基类固醇，其中R 1代表甲基或乙基，R 2代表式C n F m H o基团，其中n为2,3,4,5或 6，m> 1和m + o = 2n + 1，R 3表示游离的醚化或酯化的羟基，R 4和R 5各自代表氢原子，或一起代表另外的 键或亚甲基，St代表部分式A，B或C的甾族ABC-环体系，其中R 6表示氢原子，直链C 1 -C 4烷基或支链C 3 -C 4烷基 或卤素原子，R 7表示氢原子，直链C 1 -C 4烷基或支链C 3 -C 4烷基，或者如果St代表甾族ABC环系统A或B，另外R R 6和R 7一起可以表示另外的键，X表示氧原子，羟基亚氨基= N-OH或两个氢原子，R 8表示任意取代的基团Y或芳基 几个地方有一个Y组，Y是一个 氢原子，卤素原子，-OH，-NO 2，-N 3，-CN，-NR 9a R 9b，-NHSO 2 R 9，-CO 2 R 9，C 1 -C 10烷氧基，C 1 -C 10 烷酰氧基，苯甲酰氧基，C 1 -C 10烷酰基，C 1 -C 10羟烷基或苯甲酰基，R 9a和R 9b相同或不同，并且R 9表示氢原子或C1- C10烷基，对于-NR 9a R 9b基团，以及它们与酸的生理上相容的盐以及具有R 9表示氢的-CO 2 R 9基团，以及它们与 基地 新化合物具有非常强的抗前体作用，适用于制备药物制剂。