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    Lipid-derivatized bisphosphonic acid
    2.
    发明授权
    Lipid-derivatized bisphosphonic acid 有权
    脂质衍生的双膦酸

    公开(公告)号：US07455856B2

    公开(公告)日：2008-11-25

    申请号：US10597059

    申请日：2005-01-24

    申请人： Wolfgang Greb ,  Oleg Shyhskov ,  Gerd-Volker Röschenthaler ,  Verena Hengst

    发明人： Wolfgang Greb ,  Oleg Shyhskov ,  Gerd-Volker Röschenthaler ,  Verena Hengst

    IPC分类号： A61K9/127

    CPC分类号： C07J51/00 ,  A61K9/127 ,  A61K31/66 ,  C07F9/386 ,  C23F11/1676

    摘要： A bisphosphonic acid of the general formula (I) wherein R1 is H, OH, C1-C6 alkyl C1-C6 alkoxy, C1-C6 hydroxyalkyl, C1-C6 aminoalkyl, C1-C6 halogen alkyl X is a direct bond, alkylen group with 1 to 20 carbon atoms, (CH3)m—(OCR3HCH2)n—(O)o—, wherein R3 is H or CH3 and m is 0 or a number from 1 to 6, n is a number from 1 to 10, preferably 1 to 6, and o is 0 or 1, —(CR4HCH2O)p—, wherein R4 is H or CH3, p is a number from 1 to 10, preferably 1 to 6, (CH3)q—(OCR5HCH2)r—(O)s—(CH3)t—, wherein R5 is H or CH3 and q is 0 or a number from 1 to 6, r is a number from 1 to 10, preferably 1 to 6, and s is 0 or 1, and t is a number from 1 to 6, R2 is a group of the formula (II) as well as their physiologically compatible derivatives in particular salts and trimethyl silyl derivatives.

    摘要翻译： 通式（I）的二膦酸，其中R 1是H，OH，C 1 -C 6烷基C 1 C 6 -C 6烷氧基，C 1 -C 6羟烷基，C 1 -C 3 > 6个氨基烷基，C 1 -C 6卤代烷基X是直接键，具有1至20个碳原子的亚烷基（CH 3） （OCR 3）HCH 2 O 2 - （O）O 其中R 3为H或CH 3，m为0或1至6的数，n为1至10的数，优选为 1至6，且o为0或1， - （CR 4 HCH 2 O）p - ，其中R 4， / CH 2是H或CH 3，p是1至10，优选1至6的数，（CH 3 3）q - （OCR 5 HCH 2） - （O）S - （CH 3）3 其中R 5为H或CH 3，q为0或数1至6，r为数 1〜10，优选1〜6，s为0或1，t为数 m 1至6，R 2是式（II）的基团以及它们的生理上相容的衍生物，特别是盐和三甲基甲硅烷基衍生物。

    METHODS OF PREPARING FLUORINATED CARBOXYLIC ACIDS AND THEIR SALTS
    4.
    发明申请
    METHODS OF PREPARING FLUORINATED CARBOXYLIC ACIDS AND THEIR SALTS 有权
    制备氟化羧酸及其盐的方法

    公开(公告)号：US20120184770A1

    公开(公告)日：2012-07-19

    申请号：US13497173

    申请日：2010-10-21

    申请人： Klaus Hintzer ,  Dennis E. Vogel ,  Miguel A. Guerra ,  Jolanta Ignatowska ,  Gerd-Volker Röschenthaler ,  Oleg Shyshkov ,  Kim M Vogel ,  Tilman C. Zipplies

    发明人： Klaus Hintzer ,  Dennis E. Vogel ,  Miguel A. Guerra ,  Jolanta Ignatowska ,  Gerd-Volker Röschenthaler ,  Oleg Shyshkov ,  Kim M Vogel ,  Tilman C. Zipplies

    IPC分类号： C07C51/16 ,  C07C51/285 ,  C07C51/305 ,  C07C51/23 ,  C25B3/02 ,  C07C51/27 ,  C07C51/29

    CPC分类号： C07C51/27 ,  C07C53/21 ,  C07C59/135

    摘要： A method for preparing fluorinated carboxylic acids and theirs salts is described comprising subjecting a fluorinated alcohol of the general formula (A): A-CH2—OH to at least one first and at least one second oxidizing agent to produce a highly fluorinated carboxylic acid or their salts of the general formula (B): A-COO M+, wherein M+ represents a cation and wherein A in formulas (A) and (B) is the same and A represents the residue: Rf-[0]p-CX″Y″-[0]m-CX′Y′-[0]n-CXY— wherein Rf represents a fluorinated alkyl residue which may or may not contain one or more catenary oxygen atoms, p, m and n are independently from each other either 1 or O, X, X′, X″, Y, Y′ and Y″ are independently from each other H, F, CF3, or C2F5 with the proviso that not all of X, X′, X″, Y, Y′ and Y″ are H; or A represents the residue: R—CFX— wherein X and R are independently selected from a hydrogen, a halogen, or an alkyl, alkenyl, cycloalkyl, or aryl residue, which may or may not contain one or more fluorine atoms and which may or may not contain one or more catenary oxygen atoms; wherein said at least one first oxidizing agent is a compound that can be converted, by action of the second oxidizing agent, into a reactive species capable of oxidizing the fluorinated alcohol.

    摘要翻译： 描述了制备氟化羧酸及其盐的方法，其包括将通式（A）的氟化醇：A-CH 2 -OH置于至少一种第一和至少一种第二氧化剂中以产生高度氟化的羧酸或 其通式（B）的盐：A-COO M +，其中M +表示阳离子，式（A）和（B）中的A相同，A表示残基：Rf- [0] p-CX“ Y“ - [0] m-CX'Y' - [0] n-CXY-其中Rf表示可以或可以不含有一个或多个链状氧原子的氟化烷基残基，p，m和n彼此独立地 1或O，X，X'，X“，Y，Y'和Y”彼此独立地为H，F，CF 3或C 2 F 5，条件是不是全部X，X'，X“，Y， Y'和Y“为H; 或A表示残基：R-CFX-，其中X和R独立地选自氢，卤素或烷基，烯基，环烷基或芳基残基，其可以含有或不含有一个或多个氟原子， 或者可以不包含一个或多个链状氧原子; 其中所述至少一种第一氧化剂是可以通过第二氧化剂的作用转化成能够氧化氟化醇的反应性物质的化合物。