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    NOVEL INHIBITORS OF CELLULAR SIGNALLING
    2.
    发明申请
    NOVEL INHIBITORS OF CELLULAR SIGNALLING 审中-公开

    公开(公告)号：WO2018146641A1

    公开(公告)日：2018-08-16

    申请号：PCT/IB2018/050839

    申请日：2018-02-12

    Applicant: INVICTUS ONCOLOGY PVT. LTD.

    Inventor： ROY, Monideepa ,  BISWAS, Goutam ,  SURYAVANSHI, Hemant ,  MUKHERJEE, Anubhab

    IPC: C07D417/12 ,  C07J9/00 ,  A61K47/28

    CPC classification number: C07J43/003 ,  A61K9/1075 ,  A61K9/1271 ,  A61K47/554 ,  A61K47/6909 ,  A61K47/6911

    Abstract: The present disclosure relates generally to Cellular Signalling inhibitors of compound of Formula I, compositions and formulations comprising the same, methods, processes, and uses thereof. In particular, the present disclosure provides CSF-1R inhibitors of BLZ-945-lipids conjugates, GW2580-lipid conjugates and PLX-3397-lipid conjugates demonstrating sustained inhibition of CSF/CSF1R signalling pathway with decreased toxicity. The present disclosure also provides supramolecular combinatorial therapeutics, wherein a CSF-1R inhibitor is combined with one or more of a chemotherapeutic agent, a kinase inhibitor, and an immunoregulator, each of which is optionally conjugated with a lipid. The present disclosure also provides a method for treating cancer, allergy, Systemic lupus erythematosus, nephritis, Chronic Obstructive Pulmonary Disease, and abnormal macrophage functions or any combinations thereof.

    CONJUGATED ANTI-PROLIFERATIVE DRUG NANO-PARTICLES AND PROCESS FOR PREPARATION THEREOF
    3.
    发明申请
    CONJUGATED ANTI-PROLIFERATIVE DRUG NANO-PARTICLES AND PROCESS FOR PREPARATION THEREOF 审中-公开
    共轭抗增殖药物纳米颗粒及其制备方法

    公开(公告)号：WO2017221270A1

    公开(公告)日：2017-12-28

    申请号：PCT/IN2017/050253

    申请日：2017-06-21

    Applicant: REGIONAL CENTRE FOR BIOTECHNOLOGY

    Inventor： BAJAJ, Avinash ,  SENGUPTA, Sagar ,  SREEKANTH, Vedagopuram ,  KUMAR, Sandeep

    IPC: A61K47/60 ,  A61K47/61 ,  A61K47/56 ,  A61K47/64 ,  A61K47/66 ,  A61K31/138 ,  A61K31/337 ,  A61P35/00 ,  A61P31/04 ,  A61P31/10 ,  A61P3/10 ,  A61P29/00

    CPC classification number: A61P3/10 ,  A61K47/544 ,  A61K47/554 ,  A61K47/60 ,  A61K47/6911 ,  A61K49/0052 ,  A61K49/0084 ,  A61P29/00 ,  A61P31/04 ,  A61P31/10 ,  A61P35/00

    Abstract: A modified bile acid-drug conjugate nanoparticle of formula R-L1-BA-L2-D or pharmaceutically acceptable salts thereof; wherein R is natural, synthetic or modified phospholipid head group,polyethylene glycol or poloxamer class of polyols, or other compatible pharmaceutically acceptable head group; BA is sterol structural class compound, natural and synthetic bile acids and bile salts; D is drug molecules, enzyme/protein inhibitor molecules, imaging ligands, dyes, fluorophores and near-infrared dyes; L1 and L2 represent linkers or spacers and are independently selected from covalent bond, carbon-carbon bond, aromatic, aliphatic, alicyclic, small polymeric linkers including functional groups that covalently conjugate the bile acid moiety and drug or polyethylene glycol moiety or another group.

    Abstract translation: 式R-L1-BA-L2-D的修饰的胆汁酸 - 药物缀合物纳米颗粒或其药学上可接受的盐; 其中R是天然的，合成的或改性的磷脂头基，聚乙二醇或泊洛沙姆类的多元醇，或其它相容的药学上可接受的头基; BA是固醇结构类化合物，天然和合成胆汁酸和胆汁盐; D是药物分子，酶/蛋白质抑制剂分子，成像配体，染料，荧光团和近红外染料; L1和L2代表连接子或间隔子，并且独立地选自共价键，碳 - 碳键，芳族，脂族，脂环族，小聚合物连接子，包括共价缀合胆汁酸部分和药物或聚乙二醇部分或另一基团的官能团。 / p>

    P-ETHOXY NUCLEIC ACIDS FOR LIPOSOMAL FORMULATION
    6.
    发明申请
    P-ETHOXY NUCLEIC ACIDS FOR LIPOSOMAL FORMULATION 审中-公开
    用于脂质体制剂的对乙氧基核酸

    公开(公告)号：WO2017066643A1

    公开(公告)日：2017-04-20

    申请号：PCT/US2016/057148

    申请日：2016-10-14

    Applicant: BIO-PATH HOLDING, INC.

    Inventor： NIELSEN, Peter

    IPC: C12N15/113

    CPC classification number: A61K31/7125 ,  A61K47/544 ,  A61K47/548 ,  A61K47/6911 ,  C12N15/111 ,  C12N15/113 ,  C12N2310/11 ,  C12N2310/113 ,  C12N2310/31 ,  C12N2320/32

    Abstract: Provided herein are therapeutic oligonucleotides that comprise at least one p-ethoxy backbone linkage but no more than 80% p-ethoxy backbone linkages. Provided herein are improved delivery systems for therapeutic oligonucleotides comprising a liposome that comprises neutral phospholipids and a p-ethoxy oligonucleotide that is entrapped in the liposome.

    Abstract translation: 本文提供了包含至少一个对乙氧基骨架键但不超过80％对乙氧基骨架键的治疗性寡核苷酸。 本文提供了用于治疗性寡核苷酸的改进的递送系统，其包含脂质体，所述脂质体包含中性磷脂和截留在脂质体中的对乙氧基寡核苷酸。

    GUANIDINOGLYCOSIDE-MEDIATED LIPOSOME-BASED DELIVERY OF THERAPEUTICS
    10.
    发明申请
    GUANIDINOGLYCOSIDE-MEDIATED LIPOSOME-BASED DELIVERY OF THERAPEUTICS 审中-公开
    基于脂多糖介导的基于脂质体的治疗药物的输送

    公开(公告)号：WO2016161377A1

    公开(公告)日：2016-10-06

    申请号：PCT/US2016/025730

    申请日：2016-04-01

    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

    Inventor： ESKO, Jeffrey, D. ,  TOR, Yitzhak

    IPC: A61K31/7036 ,  C07H15/228 ,  C07H15/232

    CPC classification number: C07H15/232 ,  A61K9/127 ,  A61K47/544 ,  A61K47/6911

    Abstract: This disclosure relates to the incorporation of amphiphilic guanidinylated aminoglycosides (e.g., neomycin) into liposomal assemblies, which contain entrapped therapeutics. The lysosome is responsible for enzymatically breaking down and recycling large biomolecules and aged organelles. While malfunctioned lysosomal enzymes have been established in Lysosomal Storage Disorders (LSDs), recent reports have suggested that defects in lysosomal enzymes (e.g., glucocerebrosidase) are also linked to other chronic ailments, including neurological disorders such as Parkinson's Disease and related disorders.

    Abstract translation: 本公开涉及将两亲胍基化的氨基糖苷（例如新霉素）掺入脂质体组合物，其含有截留的治疗剂。 溶酶体负责酶促分解和回收大的生物分子和老化的细胞器。 尽管已经在溶酶体贮积障碍（LSD）中建立了故障的溶酶体酶，但是最近的报道已经表明，溶酶体酶（例如，葡糖脑苷脂酶）中的缺陷也与其它慢性疾病有关，包括神经系统疾病如帕金森病和相关疾病。

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