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    PROCESS FOR THE PREPARATION 2-SUBSTITUTED DERIVATIVES OF ESTRONE AND ESTRADIOL
    5.
    发明申请
    PROCESS FOR THE PREPARATION 2-SUBSTITUTED DERIVATIVES OF ESTRONE AND ESTRADIOL 审中-公开
    制备ESTRONE和ESTRADIOL的2替代衍生物的方法

    公开(公告)号：US20110152544A1

    公开(公告)日：2011-06-23

    申请号：US13031975

    申请日：2011-02-22

    申请人： Johannes STOELWINDER ,  Nicolaas Elisabeth Cornelis MOERS

    发明人： Johannes STOELWINDER ,  Nicolaas Elisabeth Cornelis MOERS

    IPC分类号： C07D319/06 ,  C07J1/00 ,  C07C49/603

    CPC分类号： C07J75/005

    摘要： The invention provides a process for the preparation of 2-substituted-derivatives of estrone and estradiol comprising i) the preparation of a compound of general formula (II) by reacting a compound of general formula (I) in one or more steps to a compound of general formula II wherein R1 is a C1-C10 alkyl, alkenyl or aryl group; —Cl, —Br, —I, —F; —CN; —OH; or a —OR2, —O(CO)R2 or —R2-OH group, wherein R2 is an alkyl or alkylene group having 1-6 C atoms; and the bonding between atoms 9 and 10 is a single or a double bond. ii) aromatization of the compound of general formula II to a compound of general formula III wherein R1 and R2 have the above defined meanings; and iii) optionally, reduction of the compound of general formula III to a compound of general formula IV wherein R1 and R2 have the above defined meanings.Furthermore the invention provides several novel compounds, which can be intermediates in the above process, and processes to prepare these novel compounds.The invention also provides 2-alkoxy-estrone, 2-alkoxy-estradiol or mixtures thereof essentially free from other estrogenic intermediates.

    摘要翻译： 本发明提供了一种制备雌酮和雌二醇的2-取代衍生物的方法，其包括：i）通过一种或多种步骤将通式（I）的化合物与一种或多种步骤反应制备通式（II）的化合物， 其中R 1是C 1 -C 10烷基，烯基或芳基; -Cl，-Br，-I，-F; -CN; -哦; 或-OR 2，-O（CO）R 2或-R 2 -OH基团，其中R 2是具有1-6个C原子的烷基或亚烷基; 并且原子9和10之间的键合是单键或双键。 ii）通式II化合物与通式Ⅲ化合物的芳构化，其中R1和R2具有上述定义; 和iii）任选地将通式III的化合物还原成通式IV的化合物，其中R 1和R 2具有上述定义。 此外，本发明提供了几种新颖的化合物，其可以是上述方法中的中间体，以及制备这些新化合物的方法。 本发明还提供基本上不含其它雌激素中间体的2-烷氧基 - 雌酮，2-烷氧基 - 雌二醇或其混合物。

    1-(BIPHENYL-4-YLMETHYL)IMIDAZOLIDINE-2,4-DIONE
    6.
    发明申请
    1-(BIPHENYL-4-YLMETHYL)IMIDAZOLIDINE-2,4-DIONE 失效
    1-（联苯-4-基甲基）咪唑烷-2,4-二酮

    公开(公告)号：US20100144723A1

    公开(公告)日：2010-06-10

    申请号：US12628523

    申请日：2009-12-01

    申请人： Marcelis van der Stelt ,  Joseph Maria Gerardus Barbara Cals

    发明人： Marcelis van der Stelt ,  Joseph Maria Gerardus Barbara Cals

    IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/4178 ,  C07D417/10 ,  C07D413/10 ,  C07D401/10 ,  C07D405/10 ,  A61P29/02 ,  A61P25/02

    CPC分类号： C07D233/74 ,  C07D401/10

    摘要： The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2′ are independently H or (C1-3)alkyl; or R2 and R2′ form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.

    摘要翻译： 本发明涉及具有通式I的1-（联苯-4-基甲基）咪唑烷-2,4-二酮衍生物，其中R 1是H，（C 1-6）烷基（任选被氧代取代，OR 4，COOR 5，卤素或 CN），（C2-6）烯基，（C2-6）炔基，（C3-6）环烷基或（C3-6）环烷基（C1-3）烷基; R2和R2'独立地为H或（C1-3）烷基; 或R 2和R 2'与它们所连接的碳原子一起形成（C 3-5）环烷基; R 3表示H或1至4个F取代基; Y表示或NR8R9; X表示CHR6，CF2，O，S，SO或SO2; R4和R5是（C1-6）烷基; R6是H，OR7或CN; R7是（C1-3）烷基; R8是包含选自O，S，SO和SO 2的杂原子的（C5-7）环烷基; R 9为H或（C 1-4）烷基; o和m表示取代基Y-CH 2的邻位或间位; 或其药学上可接受的盐; 以及所述1-（联苯-4-基甲基）咪唑烷-2,4-二酮衍生物在治疗疼痛中的用途，例如手术前疼痛，慢性疼痛，神经性疼痛，癌症疼痛和疼痛，以及 与多发性硬化有关的痉挛症。