pteroylamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 蝶啶及其衍生物
• 英文名称: pteroylamide
• 英文别名: 4-[(2-amino-4-oxo-3H-pteridin-6-yl)methylamino]benzamide
• 化学式: C₁₄H₁₃N₇O₂
• 分子量: 311.303
• InChiKey: HIAQREOAYKIZHG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  148
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  pteroylamide 在 potassium thioacyanate 、 三氟乙酸 、 肼 、 四甲基胍 作用下， 以 二甲基亚砜 为溶剂， 反应 24.0h， 生成 N2-(4-(((2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl)amino)benzoyl)-N6-(tert-butoxycarbonyl)-L-lysine
  参考文献：
  名称：

  The synthesis of pteroyl-lys conjugates and its application as Technetium-99m labeled radiotracer for folate receptor-positive tumor targeting

  摘要：

  Aiming to develop a new Tc-99m-labeled folate derivative for FR-positive tumor imaging, a simpler method has been established to synthesize the folate-drug conjugates with free alpha-carboxyl group. In this study, the conjugate pteroyl-lys-HYNIC was synthesized and labeled with Tc-99m using tricine and TPPTS as co-ligands. The radiochemical purity of the final complex Tc-99m(HYNIC-lys-pteroyl)(tricine/TPPTS), 5 was high (>98%), and it remained stable in saline and plasma over 6 h after preparation. The biologic evaluation results showed that the Tc-99m labeled pteroyl-lys conjugate was able to specifically target the FR-positive tumor cells and tissues both in vitro and in vivo, highlighting its potential as an effective folate receptor targeted agent for tumor imaging. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.02.014
• 作为产物：
  描述：

  folate 以 四氢呋喃 为溶剂， 反应 15.0h， 生成 pteroylamide
  参考文献：
  名称：

  The synthesis of pteroyl-lys conjugates and its application as Technetium-99m labeled radiotracer for folate receptor-positive tumor targeting

  摘要：

  Aiming to develop a new Tc-99m-labeled folate derivative for FR-positive tumor imaging, a simpler method has been established to synthesize the folate-drug conjugates with free alpha-carboxyl group. In this study, the conjugate pteroyl-lys-HYNIC was synthesized and labeled with Tc-99m using tricine and TPPTS as co-ligands. The radiochemical purity of the final complex Tc-99m(HYNIC-lys-pteroyl)(tricine/TPPTS), 5 was high (>98%), and it remained stable in saline and plasma over 6 h after preparation. The biologic evaluation results showed that the Tc-99m labeled pteroyl-lys conjugate was able to specifically target the FR-positive tumor cells and tissues both in vitro and in vivo, highlighting its potential as an effective folate receptor targeted agent for tumor imaging. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.02.014

文献信息

• [EN] PBD CONJUGATES FOR TREATING DISEASES<br/>[FR] CONJUGUÉS DE PBD POUR LE TRAITEMENT DE MALADIES
  申请人：ENDOCYTE INC

  公开号：WO2017172930A1

  公开（公告）日：2017-10-05

  The present disclosure relates to pyrrolobenzodiazepine (PBD) prodrugs and conjugates thereof. The present disclosure also relates to pharmaceutical compositions of the conjugates described herein, methods of making and methods of using the same.

  本公开涉及吡咯并苯二氮卓（PBD）前药及其共轭物。本公开还涉及所述共轭物的药物组合物，以及制造和使用它们的方法。
• [EN] METHODS OF MANUFACTURE AND SYNTHESIS OF AMINO ACID LINKING GROUPS CONJUGATED TO COMPOUNDS USED FOR TARGETED IMAGING OF TUMORS<br/>[FR] PROCÉDÉS DE FABRICATION ET DE SYNTHÈSE DE GROUPES DE LIAISON D'ACIDE AMINÉ CONJUGUÉS À DES COMPOSÉS UTILISÉS POUR L'IMAGERIE CIBLÉE DE TUMEURS
  申请人：ON TARGET LAB LLC

  公开号：WO2014149073A1

  公开（公告）日：2014-09-25

  Methods of synthesis and compositions of use for compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a pteroyi ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid or derivative thereof.

  合成方法和用于化合物的组合物，作为近红外荧光探针，其中化合物包括i）结合到目标受体蛋白质的叶酸配体，ii）染料分子和iii）包含氨基酸或其衍生物的连接分子。
• Vitamin receptor binding drug delivery conjugates
  申请人：Endocyte, Inc.

  公开号：EP2529758A2

  公开（公告）日：2012-12-05

  The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety is a vitamin, or a vitamin receptor binding analog or a derivative thereof, and the drug includes analogs or derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker, where the bivalent linker (L) comprises one or more spacer linkers, releasable linkers, and heteroatom linkers. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

  本发明描述了一种与维生素受体结合的给药共轭物及其制剂。该给药共轭物由维生素受体结合分子、二价连接体（L）和药物组成。维生素受体结合分子是维生素或维生素受体结合类似物或其衍生物，药物包括其类似物或衍生物。维生素受体结合分子与二价连接体共价连接，药物或其类似物或衍生物与二价连接体共价连接，其中二价连接体（L）包括一个或多个间隔连接体、可释放连接体和杂原子连接体。此外，还描述了使用该给药共轭物消除致病细胞群的方法和药物组合物。
• COMPOUNDS FOR POSITRON EMISSION TOMOGRAPHY
  申请人：Endocyte, Inc.

  公开号：EP3533473A2

  公开（公告）日：2019-09-04

  Described herein are compounds, compositions, and methods for diagnosing and/or monitoring pathogenic disease using positron emission tomography. Also described are conjugates of the formula B-L-P, wherein B is a radical of a targeting agent selected from vitamin receptor binding ligands (such as folate), PSMA binding ligands, or PSMA inhibitors; L is a divalent linker comprising aspartic acid, lysine, or arginine, and P is a radical of an imaging agent or radiotherapy agent, such as a radionuclide or radionuclide containing group, or a radical of a compound capable of binding a radionuclide, such as a metal chelating group.

  本文描述了利用正电子发射断层扫描诊断和/或监测致病性疾病的化合物、组合物和方法。还描述了式 B-L-P 的共轭物，其中 B 是选自维生素受体结合配体（如叶酸）、PSMA 结合配体或 PSMA 抑制剂的靶向药的基团；L 是由天冬氨酸、赖氨酸或精氨酸组成的二价连接体，P 是成像剂或放疗剂的基团，如放射性核素或含放射性核素的基团，或能结合放射性核素的化合物的基团，如金属螯合基团。
• Formulations useful in the treatment of proliferative diseases affecting the respiratory tract
  申请人：Université Libre de Bruxelles

  公开号：US10188738B2

  公开（公告）日：2019-01-29

  The present application provides a pharmaceutical formulation comprising a folate receptor (FR)-targeting antineoplastic substance or composition, wherein the pharmaceutical formulation is configured for administration by inhalation, wherein the FR-targeting antineoplastic substance or composition is comprised in a nanoparticle and wherein the nanoparticles are comprised in microparticles, and its use in the treatment of a proliferative disease affecting at least part of the respiratory tract. The present application further provides a pharmaceutical formulation comprising an antineoplastic agent and a FR-targeting excipient, for use in the treatment of a proliferative disease affecting at least part of the respiratory tract.

  本申请提供了一种药物制剂，其包含叶酸受体（FR）靶向抗肿瘤物质或组合物，其中所述药物制剂被配置为通过吸入给药，其中所述FR靶向抗肿瘤物质或组合物包含在纳米颗粒中，其中所述纳米颗粒包含在微粒中，及其在治疗影响至少部分呼吸道的增殖性疾病中的用途。本申请进一步提供了一种药物制剂，该制剂包含抗肿瘤剂和 FR 靶向赋形剂，用于治疗至少影响部分呼吸道的增殖性疾病。