(2S)-5-(diaminomethylideneamino)-2-[[2-(2,2-diphenylethoxy)acetyl]amino]pentanoic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (2S)-5-(diaminomethylideneamino)-2-[[2-(2,2-diphenylethoxy)acetyl]amino]pentanoic acid
• 化学式: C₂₂H₂₈N₄O₄
• 分子量: 412.5
• InChiKey: RRKKJYBCPXAJAO-IBGZPJMESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  30
• 可旋转键数：
  12
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  140
• 氢给体数：
  4
• 氢受体数：
  5

文献信息

• Low molecular weight immune-modulators as adjuvants for specific immunotherapy
  申请人：PLS-Design GmbH

  公开号：EP2813242A1

  公开（公告）日：2014-12-17

  The invention relates to a pharmaceutical composition for local modulation of T cell and B cell responses at the site of allergen or antigen presentation, made of one or more preparations comprising one or more antigens or allergens, and a therapeutically effective dose of two or more low molecular weight immune modulators selected from four groups of tolerance-inducing therapeutics comprising inhibitors of complement-mediated functions, inhibitors of tumor necrosis factor receptor 1 (TNFR1)-mediated functions, inhibitors of interleukin 4- and interleukin 13-mediated functions', and therapeutic agents suitable for vitamin D3 supplementation wherein preferably two or more low molecular weight immune modulators and one or more antigens or allergens are coated or adsorbed on or embedded in a matrix, wherein the matrix is selected as to enable sustained release of one or more antigens or allergens and two or more immune modulators for the treatment of T cell-mediated diseases, including allergy, allergic asthma, and autoimmune disease such as type 1 diabetes, rheumatoid arthritis, multiple sclerosis.

  本发明涉及一种用于在过敏原或抗原呈递部位局部调节T细胞和B细胞反应的药物组合物，由一种或多种制剂制成，这些制剂包括一种或多种抗原或过敏原，以及治疗有效剂量的两种或多种低分子量免疫调节剂，这些免疫调节剂选自四组耐受诱导治疗剂，包括补体介导的功能抑制剂、肿瘤坏死因子受体1（TNFR1）介导的功能抑制剂、白细胞介素4和白细胞介素13介导的功能抑制剂'、和适用于补充维生素 D3 的治疗剂，其中优选将两种或两种以上低分子量免疫调节剂和一种或多种抗原或过敏原涂布或吸附在基质上或嵌入基质中，选择基质的目的是使一种或多种抗原或过敏原和两种或多种免疫调节剂持续释放，用于治疗 T 细胞介导的疾病，包括过敏、过敏性哮喘和自身免疫性疾病，如 1 型糖尿病、类风湿性关节炎、多发性硬化症。
• ANTIGEN-SPECIFIC IMMUNOTHERAPY USING TOLERIZING LIPOSOMES
  申请人：PLS-Design GmbH

  公开号：EP3095440A1

  公开（公告）日：2016-11-23

  The invention relates to a pharmaceutical composition for the treatment of allergic and autoimmune diseases by in vivo generation of tolerogenic dendritic cells (DCs) and macrophages using tolerizing liposomes loaded with at least one maturation inhibitor of DCs and at least one antigen or allergen or peptide derived thereof, made of at least one preparation, and comprising a matrix suitable for locally restricted sustained release of therapeutically effective doses of therapeutics including tolerogenic liposomestailored for effective phagocytosis, at least one immune modulator of phagocytosis, and optionally at least one immune modulator suitable for enhancing the suppressive function of regulatory T cells and/or inhibiting the production of pro-inflammatory cytokines,and/or inhibiting the biological activity of secreted pro-inflammatory cytokinesat the site of antigen or allergen presentation.

  本发明涉及一种用于治疗过敏性和自身免疫性疾病的药物组合物，该组合物是由至少一种制剂制成的，通过使用负载有至少一种DCs成熟抑制剂和至少一种抗原或过敏原或其衍生肽的耐受性脂质体在体内生成耐受性树突状细胞（DCs）和巨噬细胞、并包含适合局部限制性持续释放治疗有效剂量的基质，包括适合有效吞噬的耐受性脂质体、至少一种吞噬免疫调节剂，以及可选的至少一种适合增强调节性 T 细胞的抑制功能和/或抑制促炎细胞因子的产生，和/或抑制抗原或过敏原呈现部位分泌的促炎细胞因子的生物活性的免疫调节剂。
• MATRIX-EMBEDDED TOLERANCE-PROMOTION ADJUVANTS FOR SUBCUTANEOUS IMMUNOTHERAPY
  申请人：Tolerogenics S.à.r.l.

  公开号：EP3251662A1

  公开（公告）日：2017-12-06

  The present invention relates to compositions and methods for the application of tolerance-promoting adjuvants embedded in alum-, microcrystalline tyrosine-, or hydrogel-based formulations for allergen- or autoantigen-specific immunotherapy.

  本发明涉及将耐受性促进佐剂嵌入明矾、微晶酪氨酸或水凝胶制剂中，用于过敏原或自身抗原特异性免疫疗法的组合物和方法。
• Controlled-release otic structure modulating and innate immune system modulating compositions and methods for the treatment of otic disorders
  申请人：Lichter Jay

  公开号：US10092580B2

  公开（公告）日：2018-10-09

  Disclosed herein are compositions and methods for the treatment of otic disorders with otic structure modulating compositions administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and compositions onto or via perfusion into the targeted auris structure(s).

  本文公开了用于治疗耳部疾病的组合物和方法，通过将这些组合物和成分直接施用到或通过灌注到目标虹膜结构，对患有耳部疾病的人局部施用调节耳部结构的组合物。
• Mobilizing agents and uses therefor
  申请人：The University of Queensland

  公开号：US10933049B2

  公开（公告）日：2021-03-02

  The present invention discloses the use of a complement 3a receptor (C3aR) antagonist and a mobilizer of hematopoietic stem cells and/or progenitor cells in methods and compositions for stimulating or enhancing the development, mobilization, proliferation and/or differentiation of a neutrophil-containing leukocyte population that inhibits growth and/or spread of a tumor and for treating or preventing a hyperproliferative cell disorder.

  本发明公开了补体3a受体（C3aR）拮抗剂和造血干细胞和/或祖细胞动员剂在刺激或增强含中性粒细胞的白细胞群的发育、动员、增殖和/或分化的方法和组合物中的应用，该方法和组合物能抑制肿瘤的生长和/或扩散，并能治疗或预防细胞过度增殖症。