[1-(4,4'-dimethoxytrityl)]-2-succinyl-3-hexadecylglycerol | 260430-24-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: [1-(4,4'-dimethoxytrityl)]-2-succinyl-3-hexadecylglycerol
• 英文别名: 1-(4,4'-dimethoxytrityl)-2-succinyl-3-hexadecylglycerol；4-[1-[Bis(4-methoxyphenyl)-phenylmethoxy]-3-hexadecoxypropan-2-yl]oxy-4-oxobutanoic acid
• CAS: 260430-24-8
• 化学式: C₄₄H₆₂O₈
• 分子量: 718.971
• InChiKey: CYAJOUOHBRBLCH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  11.7
• 重原子数：
  52
• 可旋转键数：
  30
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  101
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  1-O-hexadecyl isopropylideneglycerol 在 吡啶 、 4-二甲氨基吡啶 、 溶剂黄146 作用下， 以 吡啶 为溶剂， 反应 84.0h， 生成 [1-(4,4'-dimethoxytrityl)]-2-succinyl-3-hexadecylglycerol
  参考文献：
  名称：

  NUCLEIC ACID OF FORMULA (I): GlXmGn, OR (II): ClXmCn, IN PARTICULAR AS AN IMMUNE-STIMULATING AGENT/ADJUVANT

  摘要：

  本发明涉及一般式(I)：G l X m G n 或(II)：C l X m C n的核酸，该核酸可以通过脂质进行修饰。本发明的核酸作为免疫刺激剂，诱导先天免疫应答。本发明还涉及一种药物组合物（在第一实施例中），每种组合物包含本发明的免疫刺激剂与药用活性载体/载体（以及可选的进一步辅助物质、添加剂和/或进一步佐剂）的组合。在另一实施例中，创新的核酸与至少一种药用活性成分、药用可接受的载体/载体（以及可选的进一步辅助物质、添加剂和/或进一步佐剂）结合。因此，本发明涉及一种疫苗，该疫苗对应于本发明的药物组合物（第二实施例），其中药用活性成分诱导特异免疫应答（例如抗原）。本发明同样涉及利用本发明的核酸或药物组合物治疗传染病、自身免疫疾病、过敏或癌症疾病。

  公开号：

  US20200016264A1

文献信息

• ADJUVANT IN THE FORM OF A LIPID-MODIFIED NUCLEIC ACID
  申请人：Hoerr Ingmar

  公开号：US20070280929A1

  公开（公告）日：2007-12-06

  The present invention relates to an immune-stimulating adjuvant in the form of a lipid-modified nucleic acid, optionally in combination with further adjuvants. The invention relates further to a pharmaceutical composition and to a vaccine, each containing an immune-stimulating adjuvant according to the invention, at least one active ingredient and optionally a pharmaceutically acceptable carrier and/or further auxiliary substances and additives and/or further adjuvants. The present invention relates likewise to the use of the pharmaceutical composition according to the invention and of the vaccine according to the invention for the treatment of infectious diseases or cancer diseases. Likewise, the present invention includes the use of the immune-stimulating adjuvant according to the invention in the preparation of a pharmaceutical composition for the treatment of cancer diseases or infectious diseases.

  本发明涉及一种免疫刺激佐剂，其形式为脂质修饰的核酸，可选地与其他佐剂结合。该发明还涉及一种含有根据本发明的免疫刺激佐剂、至少一种活性成分以及可选的药用载体和/或其他辅助物质和添加剂和/或其他佐剂的药物组合物和疫苗。本发明还涉及根据本发明的药物组合物和疫苗用于治疗传染病或癌症的用途。同样，本发明包括根据本发明的免疫刺激佐剂用于制备用于治疗癌症或传染病的药物组合物的用途。
• AZIRIDINYL-EPOTHILONE COMPOUNDS
  申请人：Vite D. Gregory

  公开号：US20070276018A1

  公开（公告）日：2007-11-29

  The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: wherein K is —O—, —S—, or —NR 7 —; A is —(CR 8 R 9 )—(CH 2 ) m -Z- wherein Z is —(CHR 10 )—, —C(═O)—, —C(═O)—C(═O)—, —OC(═O)—, —N(R 11 )C(═O)—, —SO 2 —, or —N(R 11 )SO 2 —; B 1 is hydroxyl or cyano and R 1 is hydrogen or B 1 and R 1 are taken together to form a double bond; R 2 , R 3 , and R 5 are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R 2 and R 3 may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R 4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R 6 is hydrogen, alkyl or substituted alkyl; R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substituted heteroaryl; and R 13 is aryl, substituted aryl, heteroaryl or substituted heteroaryl.

  本发明涉及如下所述的吲哚环毒毒素化合物，以及/或其在下式中具有以下结构的药学上可接受的盐和/或溶剂：其中K为—O—、—S—或—NR7—；A为—(CR8R9)—(CH2)m-Z-，其中Z为—(CHR10)—、—C(═O)—、—C(═O)—C(═O)—、—OC(═O)—、—N(R11)C(═O)—、—SO2—或—N(R11)SO2—；B1为羟基或氰基，R1为氢或B1和R1一起形成双键；R2、R3和R5独立地为氢、烷基、取代烷基、芳基或取代芳基；或R2和R3可以与它们连接的碳一起形成可选择取代的环烷基；R4为氢、烷基、烯烃基、取代烷基、取代烯烃基、芳基或取代芳基；R6为氢、烷基或取代烷基；R7、R8、R9、R10、R11和R12独立地为氢、烷基、取代烷基、环烷基、取代环烷基、芳基、取代芳基、杂环烷基、取代杂环烷基、杂芳基或取代杂芳基；而R13为芳基、取代芳基、杂芳基或取代杂芳基。
• Nucleic Acid of Formula (I): GIXmGn, or (II): CIXmCn, in Particular as an Immune-Stimulating Agent/Adjuvant
  申请人：Hoerr Ingmar

  公开号：US20090324584A1

  公开（公告）日：2009-12-31

  The present invention relates to a nucleic acid of the general formula (I): G l X m G n , or (II): C l X m C n , which may be modified by a lipid. The nucleic acid of the invention acts as an immune-stimulating agent inducing the innate immune response. The invention relates further to a pharmaceutical composition (in a first embodiment), each containing an immune-stimulating agent according to the invention in combination with a pharmaceutically active carrier/vehicle (and, optionally, further auxiliary substances, additives and/or further adjuvants). In another embodiment, the inventive nucleic acid is combined with at least one pharmaceutically active component, a pharmaceutically acceptable carrier/vehicle (and, optionally, further auxiliary substances, additives and/or further adjuvants). Accordingly, the present invention is directed to a vaccine, which corresponds to a pharmaceutical composition of the invention (second embodiment), wherein the pharmaceutically active component induces a specific immune response (e.g. an antigen). The present invention relates likewise to the use of a nucleic acid of the invention or a pharmaceutical composition according to the invention for the treatment of infectious diseases, autoimmune diseases, allergies or cancer diseases.

  本发明涉及一般式(I)：GlXmGn或(II)：ClXmCn的核酸，该核酸可以通过脂质进行修饰。本发明的核酸作为一种免疫刺激剂，诱导先天免疫应答。本发明进一步涉及一种药物组合物（在第一实施例中），每种组合物包含根据本发明的免疫刺激剂与药学活性载体/载体（以及可选的进一步辅助物质、添加剂和/或进一步佐剂）的组合。在另一实施例中，创新的核酸与至少一种药学活性成分、药学可接受的载体/载体（以及可选的进一步辅助物质、添加剂和/或进一步佐剂）结合。因此，本发明涉及一种疫苗，该疫苗对应于本发明的药物组合物（第二实施例），其中药学活性成分诱导特异免疫应答（例如抗原）。本发明同样涉及利用本发明的核酸或药物组合物用于治疗传染病、自身免疫疾病、过敏或癌症疾病。
• Nucleic acid comprising GlXmGn as an immune-stimulating agent/adjuvant
  申请人：Hoerr Ingmar

  公开号：US10441653B2

  公开（公告）日：2019-10-15

  The present invention relates to a nucleic acid of the general formula (I): GIXmGn, which may be modified by a lipid. The invention relates further to a pharmaceutical composition containing an immune-stimulating agent according to the invention in combination with a pharmaceutically active carrier/vehicle (and, optionally, further auxiliary substances, additives and/or further adjuvants). The present invention can relate to a vaccine, which corresponds to a pharmaceutical composition of the invention, wherein the pharmaceutically active component induces a specific immune response (e.g. an antigen). The present invention can relate to the use of a nucleic acid of the invention or a pharmaceutical composition according to the invention for the treatment of infectious diseases, autoimmune disease, allergies or cancer diseases.

  本发明涉及通式 (I) 的核酸：GIXmGn 的核酸，该核酸可被脂质修饰。本发明还涉及一种药物组合物，该组合物含有根据本发明的免疫刺激剂与药用活性载体/载体（以及可选的进一步辅助物质、添加剂和/或进一步佐剂）。本发明可涉及一种疫苗，它与本发明的药物组合物相对应，其中的药物活性成分可诱导特异性免疫反应（如抗原）。本发明可涉及将本发明的核酸或根据本发明的药物组合物用于治疗传染性疾病、自身免疫性疾病、过敏或癌症疾病。
• Nucleic Acid of Formula (I): GlXmGn, or (II): ClXmCn, in Particular as an Immune-Stimulating Agent/Adjuvant
  申请人：Hoerr Ingmar

  公开号：US20130121988A1

  公开（公告）日：2013-05-16

  The present invention relates to a nucleic acid of the general formula (I): G l X m G n , which may be modified by a lipid. The invention relates further to a pharmaceutical composition containing an immune-stimulating agent according to the invention in combination with a pharmaceutically active carrier/vehicle (and, optionally, further auxiliary substances, additives and/or further adjuvants). The present invention can relate to a vaccine, which corresponds to a pharmaceutical composition of the invention, wherein the pharmaceutically active component induces a specific immune response (e.g. an antigen). The present invention can relate to the use of a nucleic acid of the invention or a pharmaceutical composition according to the invention for the treatment of infectious diseases, autoimmune disease, allergies or cancer diseases.