2-Acetamido-3-[3-hydroxy-2-(3-hydroxy-2-methylpropyl)-4-methyl-5-oxopyrrolidine-2-carbonyl]sulfanylpropanoic acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-Acetamido-3-[3-hydroxy-2-(3-hydroxy-2-methylpropyl)-4-methyl-5-oxopyrrolidine-2-carbonyl]sulfanylpropanoic acid
• 英文别名: 2-acetamido-3-[3-hydroxy-2-(3-hydroxy-2-methylpropyl)-4-methyl-5-oxopyrrolidine-2-carbonyl]sulfanylpropanoic acid
• 化学式: C₁₅H₂₄N₂O₇S
• 分子量: 376.4
• InChiKey: NDCRQFJMCRZFMQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  25
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.73
• 拓扑面积：
  178
• 氢给体数：
  5
• 氢受体数：
  8

文献信息

• TARGET PEPTIDES FOR IMMUNOTHERAPY AND DIAGNOSTICS
  申请人：University Of Virginia Patent Foundation

  公开号：EP2897631A2

  公开（公告）日：2015-07-29
• [EN] TARGET PEPTIDES FOR IMMUNOTHERAPY AND DIAGNOSTICS<br/>[FR] PEPTIDES CIBLES POUR L'IMMUNOTHÉRAPIE ET LE DIAGNOSTIC
  申请人：UNIV VIRGINIA PATENT FOUND

  公开号：WO2014036562A2

  公开（公告）日：2014-03-06

  A set of target peptides are presented by HLA A*0101, A*0201, A*0301, B*4402, B*2705, B*1402, and B*0702 on the surface of disease cells. They are envisioned to among other things (a) stimulate an immune response to the proliferative disease, e.g., cancer, (b) to function as immunotherapeutics in adoptive T cell therapy or as a vaccine, (c) facilitate antibody recognition of tumor boundaries in surgical pathology samples, (d) act as biomarkers for early detection and/or diagnosis of the disease, and (e) act as targets in the generation antibody-like molecules which recognize the target-peptide/MHC complex.
• [EN] COMBINATION THERAPIES<br/>[FR] POLYTHÉRAPIES
  申请人：INFINITY PHARMACEUTICALS INC

  公开号：WO2015160986A2

  公开（公告）日：2015-10-22

  Provided herein are pharmaceutical compositions comprising a phosphatidylinositol 3-kinase inhibitor, or pharmaceutically acceptable form thereof, in combination with a second agent, or a pharmaceutically acceptable form thereof, wherein the second agent is chosen from one or more of 1) a CDK4/6 inhibitor, 2) an HDAC inhibitor, 3) a MEK inhibitor, 4) a mTOR inhibitor, 5) an AKT inhibitor, 6) a proteasome inhibitor, 7) an immunomodulator, 8) a glucocorticosteroid, 9) a BET inhibitor, 10) an epigenetic inhibitor, 11) a PI3K alpha inhibitor, 12) a topoisomerase inhibitor, or 13) an ERK inhibitor. Also provided herein are methods of treatment comprising administration of the compositions, and uses of the compositions, e.g., for treatment of cancer.
• [EN] TARGETING CASEIN KINASE-1 AND PI3K/AKT/mTOR PATHWAYS FOR TREATMENT OF C-MYC-OVEREXPRESSING CANCERS, ORGAN TRANSPLANT ASSOCIATED COMPLICATIONS AND AUTOIMMUNE DISEASES<br/>[FR] VOIES CIBLANT LA CASÉINE KINASE-1 ET PI3K/AKT/MTOR POUR LE TRAITEMENT DE CANCERS SUREXPRIMANT C-MYC, DE COMPLICATIONS ASSOCIÉES À DES GREFFES D'ORGANE ET DE MALADIES AUTO-IMMUNES
  申请人：UNIV COLUMBIA

  公开号：WO2017079558A1

  公开（公告）日：2017-05-11

  The invention relates to the co-administration of select proteasome and PI3K inhibitors is useful for treating c-Myc-overexpressing cancers, particularly hematological cancers such as aggressive B- and T-cell lymphomas. In exemplified embodiments, coadministration of a dual PI3K/CK-1 inhibitor with a proteasome inhibitor synergistically increases cell death of aggressive B- and T-cell lymphomas as well as multiple myeloma over the individual or additive effect of either or both agents. This synergistic effect is associated with the previously unknown inhibition of the kinase casein kinase 1 epsilon (CK-1ε) by a PI3K inhibitor, such as TGR-1202. Accordingly, use of PI3K inhibitors that possess CK-1ε inhibition in combination with proteasome inhibitors provides a new therapy regime for treating c-Myc-overexpressing cancers, and particularly hematological cancers.
• [EN] COMPOUNDS FOR REDUCING C-MYC IN C-MYC OVEREXPRESSING CANCERS<br/>[FR] COMPOSÉS POUR FAIRE DIMINUER C-MYC DANS LES CANCERS SUREXPRIMANT C-MYC
  申请人：UNIV COLUMBIA

  公开号：WO2018013213A1

  公开（公告）日：2018-01-18

  The invention relates to new compounds that reduce c-Myc expression and useful for cancer treatment, particularly hematological cancers such as aggressive B- and T-cell lymphomas. The new compounds may be combined with adjunct c-Myc inhibor agents such as a PI3K inhibitor, CK-1 inhibitor, Akt-inhibitor, proteasome inhibitor and/or mTor inhibitor. The c-Myc reducing agent may be provided as a lead-in treatment to reduce or initiate reduction of c-Myc prior to adminstration of the adjunct cancer therapeutic agent. Treatment with a c-Myc reducing agent modulates the disease state of the c-Myc overexpressing cancer making it less malignant and more susceptible to adjunctive cancer therapies.