A PEPTIDE FOR THE DELIVERY OF ANIONIC MATERIALS

    公开(公告)号:WO2020182728A1

    公开(公告)日:2020-09-17

    申请号:PCT/EP2020/056216

    申请日:2020-03-09

    Abstract: The present invention is directed to a peptide for the delivery of anionic materials, such as anionic therapeutic agents, across a biological barrier, and methods of use thereof. The invention relates to a peptide comprising, or consisting of: X-(Xaa1)a-(Xaa2)b-Y-(Xaa3)c-(Xaa4)d-Z, in which each of X and Z is independently selected from Asn, Cys, Gln, Gly, Ser, Thr and Tyr; in which one of Xaa1 and Xaa2 is His and the other of Xaa1 and Xaa2 is Arg; in which one of Xaa3 and Xaa4 is His and the other of Xaa3 and Xaa4 is Arg; in which the amino functional group of X is, optionally, acylated; in which the carboxylate functional group of Z is, optionally, amidated; in which Y is selected from Ala and Trp; in which each of a and d is independently 2 to 4; and each of b and c is independently 2 to 4, or a salt or amide thereof. The invention also relates to a peptide for use in inducing an immune response in a subject in need thereof or a method for inducing an immune response in a subject comprising the administration of the peptide to a subject in need thereof. The invention also relates to a peptide for use in the treatment and/or prophylaxis of an infection, cancer, wounds in a subject in need thereof or a method for the treatment and/or prophylaxis of an infection, cancer, wounds comprising the administration of the peptide of the first aspect of the invention to a subject in need thereof.

    METHOD AND APPARATUS FOR ALKANE OXIDATION
    43.
    发明申请

    公开(公告)号:WO2020173885A1

    公开(公告)日:2020-09-03

    申请号:PCT/EP2020/054794

    申请日:2020-02-24

    Abstract: The present invention provides a method for catalytic oxidation of alkanes, where the catalyst comprises a photoactive material that is activated when the catalyst is irradiated with UV light. In particular, the method is for the catalytic oxidation of a C1-C5 alkane using an oxidation catalyst comprising a photoactive material, said method comprising the steps of a) activating the photoactive material by irradiating the catalyst with UV light and b) contacting the activated catalyst with a gaseous feedstream comprising an amount of C1-C5 alkane at a temperature of from 150 °C to 600 °C.

    A MODEL OF LOW- AND HIGH- GRADE CANCER
    44.
    发明申请

    公开(公告)号:WO2019149706A1

    公开(公告)日:2019-08-08

    申请号:PCT/EP2019/052149

    申请日:2019-01-29

    Abstract: The present invention relates to the field of cancer research and in particular provides novel tools for cancer research and drug and biomarker discovery. Specifically, the present invention relates to models of low- and high- grade cancer, specifically adenocarcinoma. In particular, the present invention concerns Caco-2 cells, which have been modified to reproduce the events and cellular morphology associated with low- or high-grade colorectal adenocarcinoma in a controllable manner. In particular, the present invention concerns modified Caco-2 cells, which have been engineered to be defective in centrosome anchoring to the cell cortex, clustering of interphase centrosomes and having supernumerary centrosomes. The invention concerns modified Caco-2 cells, cancer model systems comprising modified Caco-2 cells and polynucleotides, expression vectors comprising said polynucleotides and methods of producing the cells and cancer model systems.

    POROUS LIQUIDS
    45.
    发明申请
    POROUS LIQUIDS 审中-公开

    公开(公告)号:WO2018206977A1

    公开(公告)日:2018-11-15

    申请号:PCT/GB2018/051279

    申请日:2018-05-11

    Abstract: The invention relates to dispersions of porous solids in liquids selected from deep eutectic solvents, liquid oligomers, bulky liquids, liquid polymers, silicone oils, halogenated oils, paraffin oils or triglyceride oils, as well as to their methods of preparation. In embodiments of the invention, the porous solids are metal organic framework materials (MOFs), zeolites, covalent organic frameworks (COFs), porous inorganic materials, Mobil Compositions of Matter (MCMs) or a porous carbon. The invention also relates to the use of porous materials to form dispersions, and to assemblages of such dispersions with a gas or gases. The dispersions can exhibit high gas capacities and selectivities.

    BINDING COMPOUND AND USES THEREOF
    46.
    发明申请
    BINDING COMPOUND AND USES THEREOF 审中-公开
    结合化合物及其用途

    公开(公告)号:WO2018078351A1

    公开(公告)日:2018-05-03

    申请号:PCT/GB2017/053205

    申请日:2017-10-24

    Abstract: Described are compounds for targeting proteases, e.g. serine proteases and their use in the diagnostic methods and methods for treatment of respiratory diseases such as cystic fibrosis. The compounds have the structure [H]-[B]-[A]; wherein [H] is a hydrophilic group, [B] is a subsite recognition group and [A] is a binding group; wherein A has the formula: -C(0)-CH 2 -NR 1 -COOR 2 and wherein [B] has the structure :(i)-[CO-CH 2 - NR 3 ]m-, or (ii)-[AA1-AA2]- or (iii) -(AA1-C0-CH 2 NR 3 )- or (iv) -(CO-CH 2 -NR 3 - AA1)- or (v) -(C0-CH 2 -NR 4 -AA1-AA3)-.

    Abstract translation: 描述了用于靶向蛋白酶的化合物,例如, 丝氨酸蛋白酶及其在治疗呼吸系统疾病例如囊性纤维化的诊断方法和方法中的用途。 该化合物具有结构[H] - [B] - [A]; 其中[H]为亲水性基团,[B]为亚位点识别基团,[A]为结合基团; 其中A具有式-C(O)-CH 2 -NR 1 -COOR 2和其中[B]具有以下结构: (ii) - [AA 1 -AA 2] - 或(iii) - (AA 1 -C 0) - [AA 1 -CO 2 -CH 2 -NR 3) - 或(iv) - (CO-CH 2 -NR 3 3 -AA 1) ) - 或(v) - (C 0 -CH 2 -NR 4 -AA 1 -AA 3) - 。

    OCULAR COMPOSITIONS
    47.
    发明申请
    OCULAR COMPOSITIONS 审中-公开
    眼部组合物

    公开(公告)号:WO2017081154A1

    公开(公告)日:2017-05-18

    申请号:PCT/EP2016/077269

    申请日:2016-11-10

    Abstract: The invention provides an ocular composition comprising: 99to 60 % (w/w) of a photopolymerizable composition selected from the group of fragments or monomers consisting of polyalkylene glycol diacrylate and polyalkylene glycol dimethacrylate, wherein the photopolymerizable composition has a molecular weight in the range of 100 to 20,000 Dalton; a biodegradable polymer selected from the group consisting of aliphatic polyester-based polyurethanes, polylactides, polycaprolactones, polyorthoesters and mixtures, copolymers, and block copolymers thereof; a photoinitiator; and a therapeutic agent. The composition can be used to form an ocular implant and an in situ ocular implant.

    Abstract translation: 本发明提供一种眼用组合物,其包含:99-60%(w / w)的选自由聚亚烷基二醇二丙烯酸酯和聚亚烷基二醇二甲基丙烯酸酯组成的片段或单体的可光聚合组合物,其中所述可光聚合组合物 具有100至20,000道尔顿范围内的分子量; 选自脂族聚酯基聚氨酯,聚丙交酯,聚己内酯,聚原酸酯及其混合物,共聚物和嵌段共聚物的生物可降解聚合物; 光引发剂; 和治疗剂。 该组合物可用于形成眼部植入物和原位眼部植入物。

    METHODS OF PREPARING NICOTINAMIDE RIBOSIDE AND DERIVATIVES THEREOF
    48.
    发明申请
    METHODS OF PREPARING NICOTINAMIDE RIBOSIDE AND DERIVATIVES THEREOF 审中-公开
    制备尼古丁酰胺及其衍生物的方法

    公开(公告)号:WO2015014722A1

    公开(公告)日:2015-02-05

    申请号:PCT/EP2014/065971

    申请日:2014-07-24

    CPC classification number: C07H19/048 C07H1/00 C07H1/06 C07H19/04 Y02P20/582

    Abstract: The invention relates to methods of preparing nicotinamide riboside and derivatives thereof. In an aspect, the invention relates to a method of preparing a compound of formula (I), wherein n is 0 or 1; m is 0 or 1; Y is O or S; R 1 is selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted primary or secondary amino, and substituted or unsubstituted azido; R 2 - R 5 , which may be the same or different, are each independently selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, and substituted or unsubstituted aryl; and X - is an anion, selected from an anion of a substituted or unsubstituted carboxylic acid, a halide, a substituted or unsubstituted sulfonate, a substituted or unsubstituted phosphate, a substituted or unsubstituted sulfate, a substituted or unsubstituted carbonate, and a substituted or unsubstituted carbamate.

    Abstract translation: 本发明涉及制备烟酰胺核苷及其衍生物的方法。 一方面,本发明涉及制备式(I)化合物的方法,其中n为0或1; m为0或1; Y为O或S; R 1选自H,取代或未取代的烷基,取代或未取代的烯基,取代或未取代的炔基,取代或未取代的芳基,取代或未取代的伯或仲氨基,以及取代或未取代的叠氮基; R 2 -R 5可以相同或不同,各自独立地选自H,取代或未取代的烷基,取代或未取代的烯基,取代或未取代的炔基和取代或未取代的芳基; 并且X是阴离子,其选自取代或未取代的羧酸的阴离子,卤化物,取代或未取代的磺酸酯,取代或未取代的磷酸酯,取代或未取代的硫酸酯,取代或未取代的碳酸酯, 未取代的氨基甲酸酯。

    PROCESS FOR THE PREPARATION OF A METAL-ORGANIC COMPOUND
    49.
    发明申请
    PROCESS FOR THE PREPARATION OF A METAL-ORGANIC COMPOUND 审中-公开
    制备金属有机化合物的方法

    公开(公告)号:WO2014191725A1

    公开(公告)日:2014-12-04

    申请号:PCT/GB2014/051605

    申请日:2014-05-27

    Abstract: A process for the preparation of a metal-organic compound, said metal- organic compound comprising at least one metal ion and at least one organic ligand, wherein said organic ligand is capable of associating with said metal ion, comprising at least the steps of; providing a first reactant comprising at least one metal in ionic form; providing a second reactant comprising at least one organic ligand capable of associating with said metal in ionic form; and admixing said first and second reactants under conditions of prolonged and sustained pressure and shear sufficient to synthesise said metal-organic compound.

    Abstract translation: 一种制备金属 - 有机化合物的方法,所述金属有机化合物包含至少一种金属离子和至少一种有机配体,其中所述有机配体能够与所述金属离子缔合,至少包括以下步骤: 提供包含至少一种离子形式的金属的第一反应物; 提供第二反应物,其包含至少一种能够以离子形式与所述金属缔合的有机配体; 并在足以合成所述金属 - 有机化合物的持续压力和剪切力的条件下混合所述第一和第二反应物。

    AN AMPHIPATHIC PEPTIDE
    50.
    发明申请
    AN AMPHIPATHIC PEPTIDE 审中-公开
    AMPPIPIPIC PEPTIDE

    公开(公告)号:WO2014087023A1

    公开(公告)日:2014-06-12

    申请号:PCT/EP2013/075985

    申请日:2013-12-09

    Abstract: The present invention is directed to an amphipathic peptide and methods of using the amphipathic peptide for delivering small molecule agents to a cell. Ideally, the amphipathic cell penetrating peptide comprises less than approximately 50 amino acid residues with at least 6 arginine residues, at least 12 Alanine Residues, at least 6 leucine resiues, optionally at least one cysteine residue, and at least two but no greater than three glutamic acids wherein the arginine residues are evenly distributed along the length of the peptide; and the peptide has a defined ratio of arginine to negatively charged amino acid residues and a defined ratio of hydrophilic amino acid residues to hydrophobic amino acid residues. The present invention is also directed to a nanoparticle and cell del ivery system comprising the amph ipathic cell penetrating peptide of the invention. The peptide, nanoparticle or cell delivery system of the invention may be used in therapy. For example, the peptide may be used as a therapeutic agent delivery system, in which the therapeutic agent may include nucleic acids or other small molecules.

    Abstract translation: 本发明涉及两亲肽和使用两亲肽将小分子试剂递送至细胞的方法。 理想情况下,两亲性细胞穿透肽包含少于约50个氨基酸残基,至少6个精氨酸残基,至少12个丙氨酸残基,至少6个亮氨酸残基,任选至少一个半胱氨酸残基,以及至少两个但不大于三个 其中精氨酸残基沿肽长度均匀分布的谷氨酸; 并且肽具有限定的精氨酸与带负电荷的氨基酸残基的比例和亲水性氨基酸残基与疏水性氨基酸残基的确定比例。 本发明还涉及一种包含本发明的amph ipathic细胞穿透肽的纳米颗粒和细胞定型系统。 本发明的肽,纳米颗粒或细胞递送系统可用于治疗。 例如,肽可以用作治疗剂递送系统,其中治疗剂可以包括核酸或其他小分子。

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