Pyrazole compounds having therapeutic effect on multiple myeloma
    32.
    发明授权
    Pyrazole compounds having therapeutic effect on multiple myeloma 有权
    对多发性骨髓瘤具有治疗作用的吡唑类化合物

    公开(公告)号:US08658686B2

    公开(公告)日:2014-02-25

    申请号:US13991024

    申请日:2011-12-01

    IPC分类号: A61K31/415 C07D231/10

    摘要: Novel therapeutic agents for myeloma are provided.A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.

    摘要翻译: 提供了新型骨髓瘤治疗剂。 一种含有由式(1)表示的吡唑化合物的多发性骨髓瘤治疗剂:其中R1是C1-C6烷基,被R17取代的C1-C6烷基,C1-C6卤代烷基,苯基,被R11等取代的苯基, R 2是氢原子,C 1 -C 6烷基,苯基或任选被e R 21等取代的苯基,R 3是氢原子等,X是单键或 - (CR 6 R 7)n - 各自为R 4和R 5 独立地为C 1 -C 6烷基等,R 6和R 7为氢原子或C 1 -C 6烷基,R 8为苯基,任选被k R 81等取代的苯基,化合物的互变异构体或其药学上可接受的盐或溶剂合物, 作为活性成分。

    Preparation of cis—olefins
    33.
    发明授权
    Preparation of cis—olefins 失效
    顺式烯烃的制备

    公开(公告)号:US06333441B1

    公开(公告)日:2001-12-25

    申请号:US08026681

    申请日:1993-03-04

    IPC分类号: C07C505

    摘要: A cis-olefin of the formula: R1—CH═CH—R2 is prepared by reducing an alkyne of the formula: R1—C≡C—R2 with formic acid in the presence of a palladium catalyst. R1 and R2 are independently selected from the group consisting of a hydrogen atom, ester group, substituted silyl group, carboxyl group, cyano group, aliphatic C1-C20 hydrocarbon group, and phenyl group. The cis-olefin which is a useful intermediate for the synthesis of fine chemicals is selectively produced in high yields.

    摘要翻译: 通过在钯催化剂存在下用甲酸还原具有下式的R 1 -C = C-R 2的炔来制备下式的顺式烯烃:R1-CH = CH-R2。 R1和R2独立地选自氢原子,酯基,取代的甲硅烷基,羧基,氰基,脂族C1-C20烃基和苯基。 作为合成精细化学品的有用中间体的顺式烯烃以高产率选择性地生产。

    Organic bismuth derivatives for X-ray imaging
    34.
    发明授权
    Organic bismuth derivatives for X-ray imaging 失效
    有机铋衍生物用于X射线成像

    公开(公告)号:US5939045A

    公开(公告)日:1999-08-17

    申请号:US860320

    申请日:1997-07-18

    IPC分类号: A61K49/04 C07F9/94

    CPC分类号: C07F9/94 A61K49/04 Y10S424/90

    摘要: An organic bismuth derivative represented by formula (I) or its salt: �wherein X.sup.1 is YNR.sup.1 R.sup.2 (wherein Y is --SO.sub.2 -- or --C(O)--, R.sup.1 is a C.sub.3-6 alkyl group which have from 2 to 5 hydroxyl groups which may be protected, and R.sup.2 is a hydrogen atom, a C.sub.1-6 alkyl group or a C.sub.1-5 acyl group which may have from 1 to 5 hydroxyl groups which may be protected, or R.sup.1 and R.sup.2, together with each other, represent a C.sub.2-6 cyclic alkylene which may have from 1 to 4 hydroxyl groups which may be protected), and each of X.sup.2 and X.sup.3 is, independently of each other, a hydrogen atom, a C.sub.1-4 alkyl group, a C.sub.1-4 alkoxy group, a C.sub.1-4 alkylsulfonyl group, a C.sub.1-4 alkylcarbonyl group, a nitro group, a cyano group or the same as defined for X.sup.1 !.

    摘要翻译: PCT No.PCT / JP95 / 02551 Sec。 371日期1997年7月18日 102(e)1997年7月18日PCT 1995年12月13日PCT PCT。 WO96 / 19487 PCT出版物 日期:1996年6月27日由式(I)表示的有机铋衍生物或其盐:[其中X1为YNR1R2(其中Y为-SO2-或-C(O) - ,R1为C3-6烷基, 2〜5个可被保护的羟基,R2是氢原子,可以具有1〜5个可被保护的羟基的C1-6烷基或C1-5酰基,或者R1和R2一起 彼此表示可以具有1〜4个可被保护的羟基的C 2-6环状亚烷基,X2和X3各自独立地为氢原子,C1-4烷基, C 1-4烷氧基,C 1-4烷基磺酰基,C 1-4烷基羰基,硝基,氰基或与X 1所定义的相同]。

    .alpha.-methylenecyclopentanone derivative and process for producing the
same
    38.
    发明授权
    .alpha.-methylenecyclopentanone derivative and process for producing the same 失效
    α-亚甲基环戊酮衍生物及其制备方法

    公开(公告)号:US5380900A

    公开(公告)日:1995-01-10

    申请号:US834348

    申请日:1992-02-12

    摘要: Disclosed herein is an .alpha.-methylene-cyclopentanone derivative represented by the formula [I] below which is useful as an intermediate for pharmaceuticals and insecticides, especially prostaglandins. Also disclosed herein is a process for producing the derivative advantageously on an industrial scale. ##STR1## where X denotes (.alpha.-OZ, .beta.-H) or (.alpha.-H, .beta.-OZ), with Z representing a protecting group for the hydroxyl group; U denotes (.alpha.-H, .beta.-R.sup.1) or (.beta.-R.sup.1, .alpha.-H); R.sup.1 denotes ##STR2## where R.sup.2 denotes a protected hydroxyl group, a substituted or unsubstituted C.sub.1-15 alkyl group, a substituted or unsubstituted C.sub.2-15 alkenyl group, a substituted or unsubstituted C.sub.2-15 alkynyl group, or a substituted or unsubstituted C.sub.6-15 aryl group; Z' denotes a protecting group for the hydroxyl group; and k is 0 or 1).

    摘要翻译: 本文公开了下式[I]表示的α-亚甲基 - 环戊酮衍生物,其可用作药物和杀虫剂,特别是前列腺素的中间体。 本文还公开了有利于工业规模生产衍生物的方法。 其中X表示(α-OZ,β-H)或(α-H,β-OZ),其中Z表示羟基的保护基; U表示(α-H,β-R1)或(β-R1,α-H); R1表示,其中R2表示被保护的羟基,取代或未取代的C1-15烷基,取代或未取代的C2-15烯基,取代或未取代的C2-15炔基,或取代或未取代的C6- 15芳基; Z'表示羟基的保护基; k为0或1)。