5-Pentyl-1,3-oxazole | 84027-84-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-Pentyl-1,3-oxazole
• CAS: 84027-84-9
• 化学式: C₈H₁₃NO
• 分子量: 139.19
• InChiKey: RZCKQDLMEGXPFA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  10
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  26
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• 5-HT2B receptor antagonists
  申请人：Oxford William Alexander

  公开号：US20050176791A1

  公开（公告）日：2005-08-11

  The present invention relates to compounds which include compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein one of R 1 and R 4 is selected from the group consisting of H, and optionally substituted C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl-C 1-4 alkyl, and phenyl-C 1-4 alkyl; and the other of R 1 and R 4 is an optionally substituted C 9-14 aryl group; R 2 and R 3 are either: (i) independently selected from H, R, R′, SO 2 R, C(═O)R, (CH 2 ) n NR 5 R 6 , where n is from 1 to 4 and R 5 and R 6 are independently selected from H and R, where R is optionally substituted C 1-4 alkyl, and R′ is optionally substituted phenyl-C 1-4 alkyl, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C 5-7 heterocyclic group. The compounds are useful in the treatment of conditions including conditions which can be alleviated by antagonism of a 5-HT 2B receptor such as GI disorders and congestive heart failure.

  本发明涉及包括公式I化合物的化合物：或其药用可接受的盐，其中R1和R4之一选自由H、以及可选地取代的C1-6烷基、C3-7环烷基、C3-7环烷基-C1-4烷基和苯基-C1-4烷基组成的组；而R1和R4中的另一个是可选地取代的C9-14芳基基团；R2和R3是：(i)独立地选自H、R、R′、SO2R、C(═O)R、(CH2)nNR5R6，其中n是从1到4，而R5和R6独立地选自H和R，其中R是可选地取代的C1-4烷基，而R′是可选地取代的苯基-C1-4烷基，或(ii)与它们所连接的氮原子一起，形成一个可选地取代的C5-7杂环基团。这些化合物可用于治疗包括可以通过对抗5-HT2B受体而缓解的条件，如胃肠道疾病和充血性心力衰竭。
• ARYLOXAZOLE, ARYLOXADIAZOLE AND BENZIMIDAZOLE DERIVATIVES
  申请人：Christ Andreas D.

  公开号：US20080306116A1

  公开（公告）日：2008-12-11

  This invention relates to compounds of the formula wherein X is O or NR 8 , Y is CR 7 or N, and R 1 to R 8 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

  这项发明涉及以下式的化合物 其中X为O或NR 8 ，Y为CR 7 或N，R 1 至R 8 如规范中所定义，并且其药学上可接受的盐。该发明还涉及含有这种化合物的药物组合物，以及用于制备它们的过程以及它们用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。
• [EN] 2-AMINOARYL-5-ARYLOXAZOLE ANALOGS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES<br/>[FR] ANALOGUES DE 2-AMINOARYL-5-ARYLOXAZOLE DESTINÉS AU TRAITEMENT DE MALADIES NEURODÉGÉNÉRATIVES
  申请人：SOUTHERN RES INST

  公开号：WO2019164996A1

  公开（公告）日：2019-08-29

  The present disclosure is concerned with 2-aminoaryl-5-aryloxazole compounds that are capable of activating NF-κΒ signaling. The present disclosure is also concerned with methods of using these compounds for the treatment of neurological disorders such as, for example, amyotrophic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, spinal muscular atrophy, traumatic brain injury, vascular dementia, Huntington's disease, mental retardation, and attention deficit and hyperactivity disorder (ADHD), and neuromuscular disorders such as, for example, Duchenne muscular dystrophy (DMD). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

  本公开涉及能够激活NF-κΒ信号通路的2-氨基芳基-5-芳氧唑化合物。本公开还涉及使用这些化合物治疗神经系统疾病的方法，例如肌萎缩侧索硬化症（ALS）、阿尔茨海默病、帕金森病、脊髓性肌萎缩、创伤性脑损伤、血管性痴呆、亨廷顿病、智力障碍以及注意力缺陷和多动症（ADHD），以及神经肌肉疾病，例如杜兴氏肌营养不良（DMD）。本摘要旨在作为在特定领域中搜索的扫描工具，并不意味着对本发明的限制。
• [EN] NOVEL SUBSTITUTED ARYL DERIVATIVES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES AS ANTI-HIV AGENTS<br/>[FR] NOUVEAUX DÉRIVÉS ARYLES SUBSTITUÉS, LEUR PROCÉDÉ DE PRÉPARATION ET LEURS UTILISATIONS THÉRAPEUTIQUES EN TANT QU'AGENTS ANTI-VIH
  申请人：CELLVIR

  公开号：WO2010066847A1

  公开（公告）日：2010-06-17

  The present invention concerns novel substituted aryl derivatives, their process of preparation and their use for inhibiting virus replication and for treating viral diseases or disorders such as HIV and/or HCV infection.

  本发明涉及新型取代芳基衍生物，其制备方法以及用于抑制病毒复制和治疗病毒性疾病或障碍，如HIV和/或HCV感染的用途。
• [EN] SUBSTITUTED BIPHENYL ISOXAZOLE SULFONAMIDES<br/>[FR] BIPHENYL ISOXAZOLYL SULFONAMIDES, SUBSTITUES
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：WO1997029748A1

  公开（公告）日：1997-08-21

  (EN) Compounds of formula (I) inhibit the activity of endothelin. The symbols are defined as follows: R1, R2, R3 and R4 are each directly bonded to a ring carbon and are each independently (a) hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z1, Z2 and Z3; (c) halo; (d) hydroxyl; (e) cyano; (f) nitro; (g) -C(O)H or -C(O)R5; (h) -CO2H or -CO2R5; (i) -Z4-NR6R7; (j) -Z4-N(R10)-Z5-NR8R9; or (k) R3 and R4 together may also be alkylene or alkenylene, either of which may be substituted with Z1, Z2 and Z3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached; and the remaining symbols are as defined in the specification.(FR) Les composés de la formule (I) inhibent l'activité de l'endothéline. Dans cette formule, chaque groupe R1, R2, R3 et R4 est lié directement à un carbone de cycle et représente, d'une manière indépendante : (a) un hydrogène; (b) un alkyle, alcényle, alcynyle, alcoxy, cycloalkyle, cycloalkyl-alkyle, cycloalcényle, cycloalcényl-alkyle, aryle, aryloxy, aralkyle ou aralcoxy, qui peuvent tous être substitués par Z1, Z2 et Z3: (c) halo; (d) hydroxyle; (e) cyano; (f) nitro; (g) -C(O)H ou -C(O)R5; (h) -CO2H ou -CO2R5; (i) -Z4-NR6R7; (j) -Z4-N(R10)-Z5-NR8R9; ou (k) R3 et R4 peuvent former ensemble un alkylène ou un alcénylène (éventuellement substitués par Z1, Z2 et Z3) formant avec les atomes de carbone auxquels il est fixé, un cycle à 4 - 8 éléments, saturé, insaturé ou aromatique. La signification des autres symboles est donnée dans la description.

  化合物式（I）的化合物能够抑制内皮素的活性。符号定义如下：R1、R2、R3和R4都直接结合在环碳上，且分别独立地表示：（a）氢；（b）烷基，烯基，炔基，氧烷基，环烷基，环烷基烷基，环烯基，环烯基烷基，芳基，芳氧基，芳基烷基或芳氧基烷基，其中任何一种都可以用Z1、Z2和Z3取代；（c）卤素；（d）羟基；（e）氰基；（f）硝基；（g）-C（O）H或-C（O）R5；（h）-CO2H或-CO2R5；（i）-Z4-NR6R7；（j）-Z4-N（R10）-Z5-NR8R9；或（k）R3和R4也可以相互结合成为烷基或烯基，其中任何一种都可以用Z1、Z2和Z3取代，与它们附着的碳原子一起形成4-8元饱和、不饱和或芳香环；其余符号如说明书所定义。