4-iodo-6-(pyridin-3-yl)pyrimidine | 1279017-18-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 4-iodo-6-(pyridin-3-yl)pyrimidine
• 英文别名: 4-iodo-6-pyridin-3-ylpyrimidine
• CAS: 1279017-18-3
• 化学式: C₉H₆IN₃
• 分子量: 283.071
• InChiKey: KKGZFIFRYLJNRY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  38.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  3-吡啶硼酸 、 4,6-二氯嘧啶 、 、 氢碘酸 生成 4-iodo-6-(pyridin-3-yl)pyrimidine
  参考文献：
  名称：

  NOVEL IODO PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)-IMPLICATED DISEASES AND CONDITIONS

  摘要：

  本文提供了用于抑制巨噬细胞迁移抑制因子（MIF）的化合物，其化学式为（I）：其中A选自芳香环、非芳香环、双环、多环、烯烃或炔烃；B为H、OH、OR、SR、NH2、NHR或烷基；R为H或烷基，X和Y独立地为N或CH，但其中一个必须为N。此外，还提供了包含I式化合物的药物组合物和治疗MIF相关疾病或病情的方法，包括给予I式化合物的安全有效剂量。

  公开号：

  US20130079361A1

文献信息

• [EN] ENPP1 INHIBITORS AND THEIR USE FOR THE TREATMENT OF CANCER<br/>[FR] INHIBITEURS D'ENPP1 ET LEUR UTILISATION POUR LE TRAITEMENT DU CANCER
  申请人：UNIV LELAND STANFORD JUNIOR

  公开号：WO2019051269A1

  公开（公告）日：2019-03-14

  Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with a ENPP1 inhibitor to inhibit cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor is cell impermeable. Also provided are compositions and methods for treating cancer. Aspects of the methods include administering to a subject a therapeutically effective amount of a ENPP1 inhibitor to treat the subject for cancer. In certain cases, the cancer is a solid tumor cancer. Also provided are methods of administering radiation therapy to a subject either before or after administering an ENPP1 inhibitor. The radiation therapy can be administered at a dosage and/or frequency effective to reduce radiation damage to the subject. In certain cases, the method is performed in combination with a chemotherapeutic agent, or a checkpoint inhibitor, or both.

  提供了用于抑制ENPP1的化合物、组合物和方法。所述方法的方面包括将样品与ENPP1抑制剂接触以抑制ENPP1的cGAMP水解活性。在某些情况下，ENPP1抑制剂是细胞不透过的。还提供了用于治疗癌症的组合物和方法。方法的方面包括向受试者施用治疗有效量的ENPP1抑制剂以治疗受试者的癌症。在某些情况下，癌症是实体肿瘤癌。还提供了在向受试者施用ENPP1抑制剂之前或之后进行放射治疗的方法。放射治疗可以以有效剂量和/或频率对受试者减少放射损伤。在某些情况下，该方法与化疗药物、或检查点抑制剂、或两者结合使用。
• [EN] ENPP1 INHIBITORS AND METHODS OF MODULATING IMMUNE RESPONSE<br/>[FR] INHIBITEURS D'ENPP1 ET MÉTHODES DE MODULATION DE RÉPONSE IMMUNITAIRE
  申请人：ANGARUS THERAPEUTICS INC

  公开号：WO2021226136A1

  公开（公告）日：2021-11-11

  Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with a cell impermeable ENPP1 inhibitor to inhibit cGAMP hydrolysis activity of ENPP 1. Also provided are vaccine compositions and methods relate thereto. Aspects of the methods include administering to a subject an effective amount of a cell impermeable ENPP1 inhibitor to inhibit the hydrolysis of cGAMP in combination with a vaccine.

  本发明提供了用于抑制ENPP1的化合物、组合物和方法。该方法的一些方面包括使用细胞不透性的ENPP1抑制剂与样品接触，以抑制ENPP1的cGAMP水解活性。还提供了疫苗组合物和相关方法。该方法的一些方面包括向受体施用细胞不透性的ENPP1抑制剂的有效量，以结合疫苗抑制cGAMP的水解。
• Iodo pyrimidine derivatives useful for the treatment of macrophage migration inhibitory factor (MIF)-implicated diseases and conditions
  申请人：Mitchell Robert A.

  公开号：US09162987B2

  公开（公告）日：2015-10-20

  Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula (I): wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH2, NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions comprising a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions, comprising administering a safe and effective amount of a Formula I compound.

  本文提供了用于抑制巨噬细胞迁移抑制因子（MIF）的化合物，其具有以下式子（I）：其中A选自芳香环、非芳香环、双环、多环、烯烃或炔烃组成的群体；B为H、OH、OR、SR、NH2、NHR或烷基；R为H或烷基，X和Y独立地为N或CH，但其中一个必须为N。还提供了包含式I化合物的制药组合物和治疗MIF相关疾病或病症的方法，包括给予安全有效的式I化合物量。
• METHOD FOR TREATING MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)-IMPLICATED DISEASES AND CONDITIONS WITH IODO PYRIMIDINE DERIVATIVES
  申请人：UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.

  公开号：US20150368207A1

  公开（公告）日：2015-12-24

  Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula I: wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH 2 , NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions that contain a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions that include administering a safe and effective amount of a Formula I compound.

  本文提供了用于抑制巨噬细胞迁移抑制因子（MIF）的化合物，其具有公式I：其中A选择自芳香环或非芳香环、双环环、多环环、烯烃或炔烃的群体；B是H、OH、OR、SR、NH2、NHR或烷基；R是H或烷基，而X和Y独立地是N或CH，但其中一个必须是N。还提供了含有公式I化合物的药物组合物，以及治疗涉及MIF的疾病或病状的方法，包括给予安全有效量的公式I化合物。
• METHODS AND COMPOSITIONS FOR MODULATING OCULAR DAMAGE
  申请人：Tezel Tongalp H.

  公开号：US20130177552A1

  公开（公告）日：2013-07-11

  Methods for modulating eye damage associated with a disease or disorder, and/or damage incident to trauma including but not limited to trauma associated with ocular surgery are provided. In some embodiments, the methods include administering an effective amount of a modulator of a migration inhibitory factor (MIF) polypeptide biological activity to a subject. Also provided are methods for modulating the severity of delaying the onset of and/or inhibiting and/or preventing the development of an ocular disease, and methods for modulating the severity of delaying the onset of and/or inhibiting and/or preventing the development of scarring and/or other consequence of wound healing incident to ocular surgery, as well as modulating the survival, function, and/or differentiation of engrafted cells that can be employed as part of tissue engineering procedures to correct structural, functional, and/or cellular defects of the eye.