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    • 3. 发明申请
    • Topical agent containing phytanic acid or a derivative thereof
    • 含有植酸酐或其衍生物的局部药剂
    • US20060165637A1
    • 2006-07-27
    • US10559625
    • 2004-06-17
    • Jurgen VollhardtRaphael Beumer
    • Jurgen VollhardtRaphael Beumer
    • A61K8/64A61K8/40
    • A61K8/361A61K8/33A61K8/37A61K8/42A61Q5/00A61Q19/06
    • The invention relates to agents for topical administration of a compound of formula (I): (CH3)2CH—(CH2)3—CH(CH3)—(CH2)3—CH(CH3)—(CH2)3—C(A)(CH3)—C(B)2—C(O)—R, wherein R represents hydrogen, OR1, N(OH)R1 or NR2R3; R1, R2 and R3 independently represent hydrogen C1-C22-alkyl, C1-C22-alkenyl, C7-C12-arylalkyl (particularly benzyl, phenethyl and phenylpropyl), retinyl, tocopheryl, ascorbyl or a radical stemming from an amino acid or a peptide and A and B represent hydrogen atoms or A and a radical B form a double bond and the other radical B represents a hydrogen atom or radical A represents a hydrogen atom and the radicals B together form an oxygen atom or one of the radicals B represents a hydroxyl group and the other radical B and radical A represent hydrogen atoms. Said agents contain a compound of formula (I) and a pharmaceutically and/or cosmetically acceptable carrier provided that the agent does not contain any retinoids.
    • 本发明涉及用于局部施用式(I)化合物的试剂:(CH 3)2 CH-(CH 2) CH 3(CH 3) - (CH 2)3 - (CH 3) (CH 3)3 -C(A)(CH 3) - C(B)2 (O)-R,其中R表示氢,OR 1,N(OH)R 1或NR 2 R SUP> 3 ; R 1,R 2和R 3独立地表示氢C 1 -C 22 烷基,C 1 -C 22 - 烯基,C 7 -C 12 - 芳基烷基(特别是苄基 ,苯乙基和苯基丙基),视黄酯,生育酚,抗坏血酸或源自氨基酸或肽的基团,A和B表示氢原子或A,自由基B形成双键,另一个基团B表示氢原子或基团 A表示氢原子,基团B一起形成氧原子或基团B中的一个表示羟基,另一个基团B和基团A表示氢原子。 所述试剂含有式(I)化合物和药学上和/或化妆品上可接受的载体,条件是该试剂不含任何类维生素A。
    • 4. 发明授权
    • Process for the production of 1-functional allylalcohol carboxylic esters
    • 用于制备1-官能烯丙醇羧酸酯的方法
    • US5981792A
    • 1999-11-09
    • US31131
    • 1998-02-26
    • Jurgen Vollhardt
    • Jurgen Vollhardt
    • C07C67/08C07C67/293C07C69/025C07C69/145C07C67/00C07C67/02C07C69/76
    • C07C67/08C07C67/293
    • The process for preparing 1-functional allyl alcohol carboxylic esters comprises reacting a 3-functional allyl alcohol with the anhydride of the carboxylic acid at temperatures above 100.degree. C. in the presence of metal compounds of transition groups V to VII, namely at temperatures of 100-200.degree. C., preferably 130-150.degree. C. As metal compounds, it is possible to use oxidic metal compounds in the highest or at least second highest oxidation state of the transition metals, for example tungstic acid or its salts and/or tungsten(VI) oxide and/or molybdenum(V) oxide and/or molybdenum(VI) oxide and/or rhenium(VII) oxide. The 3-functional allyl alcohol and the carboxylic anhydride are advantageously used in equimolar amounts, if desired with a slight excess of anhydride, and an alkali metal salt of a weak acid, for example sodium carbonate or sodium acetate, can be added to the reaction mixture in an amount sufficient to trap free protons.
    • 制备1-官能烯丙醇羧酸酯的方法包括在过渡基团V至VII的金属化合物存在下,在高于100℃的温度下,即3-乙烯基醇与羧酸酐反应,即在 100-200℃,优选130-150℃。作为金属化合物,可以使用过渡金属的最高或至少第二高氧化态的氧化金属化合物,例如钨酸或其盐和/ 或氧化物(V)氧化物和/或氧化钼(V)和/或氧化钼(VI)和/或氧化铼(VII)。 如果需要,3-官能的烯丙醇和羧酸酐有利地以等摩尔量的使用,稍微过量的酸酐,并且可以向反应中加入弱酸的碱金属盐,例如碳酸钠或乙酸钠 混合物的量足以捕获游离质子。