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    • 8. 发明申请
    • PEPTIDE BEADS
    • 肽珠
    • WO2013004716A9
    • 2013-04-11
    • PCT/EP2012062963
    • 2012-07-04
    • UNIV BASELDE BRUYN OUBOTER DIRKSCHUSTER THOMASSHANKER VIJAYMEIER WOLFGANG
    • DE BRUYN OUBOTER DIRKSCHUSTER THOMASSHANKER VIJAYMEIER WOLFGANG
    • A61K9/51A61K47/48C12N15/88
    • A61K9/0019A61K9/5169A61K47/645A61K47/6455B82Y5/00C12N15/88
    • The invention relates to peptide beads comprising amphiphilic bead-forming peptides of the formula R1 (A1)k (A2 D-A3)m (A2)n (A1)l R2, wherein R1 is an amino acid, biotin, an acyl group or hydrogen, R2 is NH2, OH, alkoxy, hydroxyethylamide or an optionally amidated amino acid, or biotin; A1 is a hydrophilic L-amino acid; A2 is an aromatic L-amino acid; A3 is an aliphatic D-amino acid; k and l are, independently of each other, between 0 and 12; m is between 2 and 8; and n is 0 or 1; a mediator peptide of the formula R1 (A1)k (A2 D-A3)m (A2)n (A1)l R2, wherein at least one of the substituents R1, R2 and/or at least one of the amino acids A1 is different from the corresponding substituents R1, R2 and/or amino acids A1 in the peptide forming the peptide beads; and a payload, such as RNA, DNA or hydrophilic drug, furthermore to the use of such peptide beads for the delivery of an active pharmaceutical ingredient into tissue and cells, and the release of the active pharmaceutical ingredient in the tissue or cell causing the desired therapeutic effect.
    • 本发明涉及包含式R1(A1)k(A2D-A3)m(A2)n(A1)l R2的两亲珠形成肽的肽珠,其中R1是氨基酸,生物素,酰基或 氢,R2是NH2,OH,烷氧基,羟乙基酰胺或任选酰胺化的氨基酸,或生物素; A1是亲水性L-氨基酸; A2是芳族L-氨基酸; A3是脂肪族D-氨基酸; k和l彼此独立地在0和12之间; m在2和8之间; n为0或1; 式(A1)k(A2D-A3)m(A2)n(A1)l R2的介体肽,其中至少一个取代基R1,R2和/或至少一个氨基酸A1为 不同于形成肽珠的肽中相应的取代基R1,R2和/或氨基酸A1; 和有效载荷,例如RNA,DNA或亲水药物,此外使用这样的肽珠将活性药物成分递送到组织和细胞中,以及活性药物成分在组织或细胞中的释放,导致所需的 治疗效果。
    • 10. 发明申请
    • IMPROVED MICROEMULSION HAVING WIDE APPLICATION RANGE
    • 改进MICROEMULSION范围广
    • WO2009133166A3
    • 2010-05-14
    • PCT/EP2009055249
    • 2009-04-30
    • BASF SETARANTA CLAUDEMEIER WOLFGANGBORK THOMASSTRAUSS KARLLEVY TATJANAMONTAG JURITH
    • TARANTA CLAUDEMEIER WOLFGANGBORK THOMASSTRAUSS KARLLEVY TATJANAMONTAG JURITH
    • A01N25/04
    • A01N25/04A01N43/653A01N47/02A01N2300/00
    • The present invention relates to a microemulsion, comprising (A) 0.1 to 50 wt.% of at least one active agent as component A, (B) 0.5 to 40 wt.% of at least one solvent that can be completely mixed with water and selected from the group consisting of esters from acetic acid, lactic acid, benzoic acid, dicarboxylic acids, cyclic esters, cyclic amides, carbonates, sulfurous solvents, phosphates, ethers and mixtures thereof, as component B, (C) 10 to 40 wt.% of at least one non-ionic surfactant as component C, (D) 0 to 10 wt.% further additives as component D, (E) 10 to 90 wt.% water as component E, and (F) 0.1 to 60 wt.% of at least one solvent that can be partially mixed with water as component F, each in relation to the entire microemulsion, wherein the sum of the amounts of components, A, B, C, D, E, and F is 100 wt.%, and the microemulsion does not comprise any anionic surfactants. The invention further relates to a method for the production of said microemulsion and to the use of said microemulsion for treating plants.
    • 本发明涉及包含0.1微乳液(A)至50重量%的活性剂作为组分A,(B)0.5〜40重量的组中选择的至少一个完全与水混溶的溶剂中的至少一个的% 自由乙酸,乳酸,苯甲酸,二羧酸的酯,环状酯,环状酰胺,碳酸酯,含硫溶剂,磷酸盐,醚和它们的混合物的酯的酯,作为组分B,(C)10〜40重量%的至少一种非离子型的% 表面活性剂作为组分C,(D)0至10重量%的其它添加剂作为组分D,(E)为10至90重量的水作为组分e%,和(F)0.1〜60重量%的至少一种% 部分地包含水可混溶的溶剂作为组分F,在基于总微滴乳状液每一种情况下,其中组分A的量的总和,B,C,D,E和F是100重量%,和微乳液没有阴离子表面活性剂,和 用于制备这些Mik的一个方法 roemulsion和用于治疗植物中的用途,这些微乳化的。