1-(2-Methyl-1-oxo-2-propen-1-yl)-D-proline

• 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: 1-(2-Methyl-1-oxo-2-propen-1-yl)-D-proline
• 英文别名: 1-(2-methylprop-2-enoyl)pyrrolidine-2-carboxylic acid
• 化学式: C₉H₁₃NO₃
• 分子量: 183.2
• InChiKey: SJAYUJDJZUWFDO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  57.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• THERMO-RESPONSIVE HYDROGEL COMPOSITIONS
  申请人：KANG-MIELER Jennifer J.

  公开号：US20120231072A1

  公开（公告）日：2012-09-13

  A thermo-responsive hydrogel, including a biocompatible monomer and/or polymer having an amino acid side chain. The hydrogel is thermo-responsive at a physiological temperature, and can include, incorporate, or encapsulate a treatment agent, such as a drug composition, a biomolecule, and/or a nanoparticle. The hydrogel is useful in delivering the treatment agent. The hydrogel is in a first physicochemical state for administration to a mammal. The hydrogel is thermo-responsive at a physiological temperature of the mammal, and changes to a second physicochemical state that is more solid than the first physicochemical state. In the second physicochemical state the thermo-responsive hydrogel releases the treatment agent.

  一种热响应性水凝胶，包括具有氨基酸侧链的生物相容性单体和/或聚合物。该水凝胶在生理温度下具有热响应性，可以包含、结合或封装治疗剂，如药物组合物、生物分子和/或纳米颗粒。该水凝胶在传递治疗剂方面很有用。该水凝胶处于第一物理化学状态以用于哺乳动物。该水凝胶在哺乳动物的生理温度下具有热响应性，并转变为比第一物理化学状态更固体的第二物理化学状态。在第二物理化学状态下，热响应性水凝胶释放治疗剂。
• [EN] SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF<br/>[FR] LIGANDS DE SARD - COMPOSÉS DE DÉGRADATION SÉLECTIFS DE RÉCEPTEURS DES ANDROGÈNES - ET MÉTHODES D'UTILISATION
  申请人：UNIV TENNESSEE RES FOUND

  公开号：WO2017214634A1

  公开（公告）日：2017-12-14

  This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

  该发明涉及吡咯、吡唑、咪唑、三唑和吗啉基选择性雄激素受体降解剂（SARD）化合物，包括含有杂环苯胺环的合成前体、R-异构体以及非羟基化和/或非手性的丙酰胺，以及在治疗前列腺癌、晚期前列腺癌、去势耐药性前列腺癌、三阴性乳腺癌、其他表达雄激素受体的癌症、雄激素性脱发或其他高雄激素皮肤疾病、肯尼迪病、肌萎缩性侧索硬化（ALS）、腹主动脉瘤和子宫肌瘤等方面的制药组合物和用途，以及用于降低受试者中雄激素受体全长（AR-FL）的水平，包括致病性或耐药突变、AR-剪接变体（AR-SV）和AR的致病性多谷氨酸（polyQ）多态性的方法。
• [EN] PROPIONAMIDE DERIVATIVES USEFUL AS ANDROGEN RECEPTOR MODULATORS<br/>[FR] DERIVES DE PROPIONAMIDE UTILISES COMME MODULATEURS DU RECEPTEUR D'ANDROGENES
  申请人：ORION CORP

  公开号：WO2005000794A1

  公开（公告）日：2005-01-06

  Compounds of formula (I) wherein R1 to R4, X and A are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are useful in hormonal therapy, e.g. in the treatment or prevention of male hypogonadism and age-related conditions such as andropause.

  公式（I）中的化合物，其中R1至R4、X和A的定义如权利要求所述，并且其药用盐和酯已被披露。 公式（I）的化合物具有作为组织选择性雄激素受体调节剂（SARM）的效用，并且在激素疗法中有用，例如用于治疗或预防男性性腺功能减退和与年龄相关的病症，如男性更年期。
• Novel functionalized resin derived from polyallylamine
  申请人：NITTO BOSEKI CO., LTD.

  公开号：EP0154742A2

  公开（公告）日：1985-09-18

  A new functionalized resin represented by the general formula was derived from polyallylamine. [wherein; X represents the general formula (tis 0 or 1, l is an integer of 1 to 20), n ≧ 10, 0 < j < 1, u = 1 or 2, and m = 1 or 2, with the proviso that t and m are not simultaneously 0]. The functionalized resin is preferably used for recovering heavy metals in waste water and for optically dissolving amino acids.

  由聚烯丙基胺衍生出通式所示的新型功能化树脂。 [其中，X 代表通式 (t 为 0 或 1，l 为 1 至 20 的整数），n ≧ 10，0 < j < 1，u = 1 或 2，m = 1 或 2，但 t 和 m 不能同时为 0]。 功能化树脂最好用于回收废水中的重金属和光学溶解氨基酸。
• Selective androgen receptor degrader (SARD) ligands and methods of use thereof
  申请人：GTx, Inc.

  公开号：US10017471B2

  公开（公告）日：2018-07-10

  This invention provides novel indole, indazole, benzimidazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

  本发明提供了新型吲哚、吲唑、苯并咪唑、吲哚啉、喹诺酮、异喹啉和咔唑选择性雄激素受体降解剂（SARD）化合物、药物组合物及其在治疗前列腺癌、晚期前列腺癌、阉割耐药前列腺癌、其他表达AR的癌症、雄激素性脱发或其他高雄激素性皮肤病、肯尼迪病、肌萎缩性脊髓侧索硬化症（ALS）、腹主动脉瘤（AAA）和子宫肌瘤中的用途，以及降低其水平（通过降解）的方法、肌萎缩性脊髓侧索硬化症（ALS）、腹主动脉瘤（AAA）和子宫肌瘤，以及降低受试者体内任何雄激素受体的水平（通过降解）和/或活性（通过抑制）的方法，包括雄激素受体全长（AR-FL），包括致病性和/或抗性突变、AR-剪接变体（AR-SV）和致病性多谷氨酰胺（polyQ）多态性。