2-pentyloxyacetamide | 90048-38-7

• 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-pentyloxyacetamide
• 英文别名: Pentyloxy-acetamid；2-Pentoxyacetamide
• CAS: 90048-38-7
• 化学式: C₇H₁₅NO₂
• 分子量: 145.202
• InChiKey: JRLSJIFCUQOCMQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  10
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  52.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  Pentyloxy-essigsaeure-aethylester 在 ammonium hydroxide 作用下， 以 乙醇 为溶剂， 生成 2-pentyloxyacetamide
  参考文献：
  名称：

  Mueller,E.; Huber-Emden,H., Justus Liebigs Annalen der Chemie, 1961, vol. 649, p. 70 - 87

  摘要：

  DOI：

文献信息

• COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ENHANCER OF ZESTE HOMOLOG 2 POLYPEPTIDE
  申请人：Arvinas, Inc.

  公开号：US20180177750A1

  公开（公告）日：2018-06-28

  The present disclosure relates to bifunctional compounds, which find utility as modulators of enhancer of zeste homolog 2 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

  本公开涉及双功能化合物，其作为增强子锁定同源2的调节剂而发挥作用。具体而言，本公开涉及包含一端为Von Hippel-Lindau、cereblon、凋亡抑制蛋白或鼠双分子同源2配体的双功能化合物，该配体与相应的E3泛素连接酶结合，另一端含有结合目标蛋白的基团，使目标蛋白靠近泛素连接酶以实现目标蛋白的降解（和抑制）。本公开展示了与目标蛋白的降解/抑制相关的广泛药理活性范围。本公开的化合物和组合物用于治疗或预防由目标蛋白聚集或积累导致的疾病或紊乱。
• [EN] NEW ARYLOXY ACETIC ACID AMIDE DERIVATIVES<br/>[FR] NOUVEAUX DÉRIVÉS D'AMIDE D'ACIDE ARYLOXY-ACÉTIQUE
  申请人：RICHTER GEDEON VEGYESZET

  公开号：WO2006010968A1

  公开（公告）日：2006-02-02

  The new aryloxy acetic acid amide derivatives of formula (I) where R1 and R2 are the same or different and can be hydrogen atom or C1-4 alkanoylamido group optionally substituted by halogen atom or C1-4 alkyl-sulfonylamido group or N'-( C1-4 alkyl)-ureido group C1-6 alkoxy-carbonyl-amido or di-( C1-4 alkyl)-amino group with the proviso that only one of them can be hydrogen atom, or R1 and R2 form together a -NH-CO-NH-, -NH-N=CH- or -NH-CO-O- chain attached to two neighbouring carbon atoms of the benzyl group, R3 and R4 mean the same or different C1-4 alkyl groups which are substituted by phenyl group, or R3 and R4 mean together a C4-6 alkylene chain which can be interrupted optionally by a nitrogen atom and which can contain a C-C double bound and which C4-6 alkylene chain can substituted by one or two substituents from the following hydroxy group, phenyl or phenoxy group optionally substituted by a C1-4 alkyl or trifluoro methyl group, =CH-phenyl group which can be substituted by halogen atom or C1-4 alkyl group, C1-4 alkyl group optionally substituted by hydroxy groµp and one or two phenyl groups which can be substituted by halogen atom or C1-4 alkyl group, C1-4 alkyl amino group which is substituted by a phenyl or naphtyl group which can be substituted optionally by a halogen atom or a C1-4 alkyl group, as well as their salts formed with organic or inorganic acids or bases and solvates of these compounds are functional antagonists of NMDA receptors, which target the NMDA receptors primarily via binding to the ifenprodil binding site. Furthermore objects of the present invention are the pharmaceutical compositions containing new aryloxy acetic acid amide derivatives of formula (I) or optical antipodes or racemates or the salts thereof as active ingredients and processes for producing these compounds and pharmaceutical compositions.

  公式（I）的新的芳氧乙酸酰胺衍生物，其中R1和R2相同或不同，可以是氢原子或C1-4烷酰胺基团，可选择地被卤素原子或C1-4烷基磺酰胺基团或N'-(C1-4烷基)-脲基团C1-6烷氧基羰基胺或二-(C1-4烷基)-氨基团取代，但其中只有一个可以是氢原子，或者R1和R2共同形成一个-NH-CO-NH-，-NH-N=CH-或-NH-CO-O-链，附加在苯甲基的两个相邻碳原子上，R3和R4表示相同或不同的C1-4烷基，它们被苯基取代，或者R3和R4共同表示一个C4-6烷基链，可以被氮原子随意中断，并且可以包含一个C-C双键，这个C4-6烷基链可以被以下羟基，苯基或苯氧基取代，可选择地被C1-4烷基或三氟甲基基团取代，=CH-苯基团，可被卤素原子或C1-4烷基团取代，可选择地被羟基团取代的C1-4烷基基团以及一个或两个苯基团，这些苯基团可以被卤素原子或C1-4烷基团取代，被苯基或萘基团取代的C1-4烷基氨基团，这些基团可选择地被卤素原子或C1-4烷基团取代，以及它们与有机或无机酸或碱形成的盐和这些化合物的溶剂化合物，是NMDA受体的功能性拮抗剂，其通过主要结合ifenprodil结合位点来靶向NMDA受体。此外，本发明的目标是含有公式（I）的新的芳氧乙酸酰胺衍生物或其光学异构体或外消旋体或其盐作为活性成分的制药组合物以及制备这些化合物和制药组合物的过程。
• 2-(ARYLOXY) ACETAMIDE FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
  申请人：Nirschl Alexandra A.

  公开号：US20090131473A1

  公开（公告）日：2009-05-21

  The present invention relates generally to novel 2-(aryloxy)acetamides of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables W, Y, Z, R 7 , R 8 , and R 9 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.

  本发明涉及一般而言公式（I）的新型2-(芳氧基)乙酰胺或其立体异构体、互变异构体、药学上可接受的盐、溶剂化物或前药，其中变量W、Y、Z、R7、R8和R9如本文所定义。这些化合物是选择性抑制丝氨酸蛋白酶凝血因子VIIa的药物。
• Phenyl alpha-acyloxyacetamide derivates and their therapeutic use
  申请人：Yu, Ruey J., Dr.

  公开号：EP0098743A1

  公开（公告）日：1984-01-18

  Therapeutic as well as preventive measures to alleviate the symptoms of dermatologic and other conditions and disorders with phenyl alpha-acyloxyacetamide derivatives is disclosed. Dermatologic and other conditions and disorders in humans in which the compounds may be useful include pruritus, atopic dermatitis, eczema, psoriasis, acne, dry skin, dandruff, malodors of integumental areas; and various aches, pains and discomforts of skin, joints and other body parts. The phenyl alpha-acyloxyacetamide derivatives include, for example, N-ethyl phenyl alpha-acetoxyacetamide, N-benzyl phenyl-alpha-acetoxyacetamide, N-phenethyl phenyl-alpha--acetoxyacetamide, N-benzyl diphenyl-alpha-acetoxyacetamide and N-phenethyl diphenyl-alpha-acetoxyacetamide. The compositions containing the active ingredients are also useful for treatment of skin conditions or disorders, and musculoskeletal disorders, of domestic animals, for example dogs, such as dry skin, scurf, eczema, mange, prurigo, malodors, arthritis or myositis. Some phenyl-alpha-acyloxy- acetamide derivatives may have a tranquilizing effect.

  本发明公开了利用苯基α-乙酰氧基乙酰胺衍生物减轻皮肤病和其他疾病症状的治疗和预防措施。本发明化合物可用于治疗的人类皮肤病和其他病症包括瘙痒症、特应性皮炎、湿疹、牛皮癣、痤疮、皮肤干燥、头皮屑、皮肤周围异味，以及皮肤、关节和身体其他部位的各种疼痛和不适。苯基 alpha-乙酰氧基乙酰胺衍生物包括 N-乙基苯基 alpha-乙酰氧基乙酰胺、N-苄基苯基 alpha-乙酰氧基乙酰胺、N-苯乙基苯基 alpha-乙酰氧基乙酰胺、N-苄基二苯基 alpha-乙酰氧基乙酰胺和 N-苯乙基二苯基 alpha-乙酰氧基乙酰胺等。含有这些活性成分的组合物还可用于治疗家养动物（如狗）的皮肤状况或疾病以及肌肉骨骼疾病，如皮肤干燥、鳞屑、湿疹、疥疮、瘙痒症、恶臭、关节炎或肌炎。某些苯基-α-乙酰氧基-乙酰胺衍生物可能具有镇静作用。
• Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
  申请人：Arvinas, Inc.

  公开号：US10723717B2

  公开（公告）日：2020-07-28

  The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.

  本公开涉及双功能化合物，它们可用作快速加速纤维肉瘤（RAF，如c-RAF、A-RAF和/或B-RAF；靶蛋白）的调节剂。特别是，本公开内容涉及双功能化合物，其一端含有与相应 E3 泛素连接酶结合的 Von Hippel-Lindau、cereblon、抑制细胞凋亡蛋白或小鼠双敏同源物 2 配体，另一端含有与靶蛋白 RAF 结合的分子，从而将靶蛋白置于泛素连接酶附近，以实现对靶蛋白的降解（和抑制）。本公开物具有与降解/抑制靶蛋白相关的广泛药理活性。本公开的化合物和组合物可以治疗或预防由于靶蛋白的聚集或积聚或靶蛋白的组成性激活而导致的疾病或失调。