1-(4-Hydroxyl-3-hydroxymethylphenyl)ethanol | 141024-79-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-(4-Hydroxyl-3-hydroxymethylphenyl)ethanol
• 英文别名: 4-(1-hydroxyethyl)-2-(hydroxymethyl)phenol
• CAS: 141024-79-5
• 化学式: C₉H₁₂O₃
• 分子量: 168.19
• InChiKey: GPDSMYDFAANBAN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  60.7
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• Pyrazolo[3,4-b]pyridine compounds, and their use as PDE4 inhibitors
  申请人：Allen George David

  公开号：US20080058369A1

  公开（公告）日：2008-03-06

  The invention provides N-[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-5-yl]methyl}-4-(8-[(2-hydroxyethyl)(methyl)amino]octanoyl}amino)benzamide, whose formula is , or a salt thereof, such as the monohydrochloride salt thereof. The invention also provides the use of the compound or salt as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, or rhinitis (e.g. allergic and/or non-allergic rhinitis).

  本发明提供一种N-[1,6-二乙基-4-(四氢-2H-吡喃-4-基氨基)-1H-吡唑并[3,4-b]吡啶-5-基]甲基}-4-(8-[(2-羟乙基)(甲基)氨基]辛酰}氨基)苯甲酰胺，其化学式为，或其盐，例如单盐酸盐。本发明还提供该化合物或盐作为磷酸二酯酶IV (PDE4) 的抑制剂以及/或用于治疗和/或预防炎症和/或过敏性疾病，如慢性阻塞性肺疾病 (COPD)，哮喘或鼻炎 (如过敏性和/或非过敏性鼻炎)。
• PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS
  申请人：Allen David George

  公开号：US20090318494A1

  公开（公告）日：2009-12-24

  The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (w), (y), (z1) or (z2): wherein the several groups are defined herein below, and the use of these compounds as inhibitors of phosphodiesterase type IV (PDE4).

  本发明提供了式(I)的化合物或其盐：其中Ar具有子式(w)，(y)，(z1)或(z2)：其中各个基团在下文中定义，并使用这些化合物作为磷酸二酯酶IV型（PDE4）的抑制剂。
• PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PDE4 INHIBITORS
  申请人：Allen David George

  公开号：US20090326003A1

  公开（公告）日：2009-12-31

  The present invention provides a compound of formula (I) or a salt thereof (in particular, a pharmaceutically acceptable salt thereof): The invention also provides the use of the compounds or salts as inhibitors of phosphodiesterase type IV (PDE4) for the treatment or prophylaxis of inflammatory or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis, atopic dermatitis or psoriasis, e.g. in a mammal such as a human.

  本发明提供了式（I）的化合物或其盐（特别是其药学上可接受的盐）：本发明还提供了将该化合物或盐用作磷酸二酯酶IV（PDE4）的抑制剂，用于治疗或预防炎症或过敏性疾病，如慢性阻塞性肺疾病（COPD），哮喘，鼻炎，特应性皮炎或银屑病，例如在哺乳动物，如人类中。
• PYRAZOLO [3,4-B] PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS
  申请人：Allen David George

  公开号：US20080132536A1

  公开（公告）日：2008-06-05

  The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (x) or (z): and wherein R 3 is optionally substituted C 3-8 cycloalkyl, optionally substituted C 5-7 cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc), or a bicyclic group (ee); and wherein R 4 is H, C 1-3 alkyl, C 1-2 fluoroalkyl, cyclopropyl, —CH 2 OR 4a , —CH(Me)OR 4a , or —CH 2 CH 2 OR 4a ; and R 5 is inter alia H, C 1-8 alkyl, C 1-3 fluoroalkyl, C 3-8 cycloalkyl, certain substituted alkyl groups, —(CH 2 ) n 13 -Het, or optionally substituted phenyl or —CH 2 -Ph; or R 4 and R 5 taken together are —(CH 2 ) p 1 — or —(CH 2 ) p 3 —X 5 —(CH 2 ) p 4 —; provided that at least one of R 4 and R 5 is not a hydrogen atom (H). The invention also provides the use of the compounds as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, allergic rhinitis or atopic dermatitis.

  该发明提供了式(I)的化合物或其盐： 其中Ar具有亚式(x)或(z)： 其中，R3是可选的取代C3-8环烷基，可选的取代C5-7环烯基，可选的取代的杂环基(aa)，(bb)或(cc)，或者是双环基(ee)； 其中，R4是氢，C1-3烷基，C1-2氟代烷基，环丙基，— OR4a，—CH(Me)OR4a或— OR4a； 而R5则是包括氢、C1-8烷基、C1-3氟代烷基、C3-8环烷基、某些取代烷基、—(CH2)n13-Het，或可选取代的苯基或—CH2-Ph等的基团； 或者，R4和R5在一起是—( )p1—或—( )p3—X5—( )p4—； 但是至少其中一个R4和R5不是氢原子（H）。 该发明还提供了将这些化合物用作磷酸二酯酶IV（PDE4）的抑制剂和/或用于治疗和/或预防炎症和/或过敏性疾病，如慢性阻塞性肺疾病（COPD）、哮喘、类风湿性关节炎、过敏性鼻炎或特应性皮炎的用途。
• Pyrazolo[3,4-b]Pyridine Compounds, and their Use as Phosphodiesterase Inhibitors
  申请人：ALLEN David George

  公开号：US20080175914A1

  公开（公告）日：2008-07-24

  The invention relates to a compound of formula (I) or a salt thereof: wherein: R 1 is C 1-4 alkyl, C 1-3 fluoroalkyl, —CH 2 CH 2 OH or —CH 2 CH 2 CO 2 C 1-2 alkyl; R 2 is a hydrogen atom (H), methyl or C 1 fluoroalkyl; R 3 is optionally substituted C 3-8 cycloalkyl or optionally substituted mono-unsaturated-C 5-7 cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n 1 and n 2 independently are 1 or 2; and in which Y is O, S, SO 2 , or NR 10 ; or R 3 is a bicyclic group (dd) or (ee): and wherein X is NR 4 R 5 or OR 5a . The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE 4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.

  本发明涉及公式（I）的化合物或其盐： 其中： R1是C1-4烷基，C1-3氟烷基，-CH2CH2OH或-CH2CH2CO2C1-2烷基; R2是氢原子（H），甲基或C1氟烷基; R3是可选取代的C3-8环烷基或可选取代的单不饱和C5-7环烯基或亚公式（aa），（bb）或（cc）的可选取代的杂环基; 其中n1和n2独立地为1或2; Y是O，S，SO2或NR10; 或R3是双环基（dd）或（ee）： 其中X是NR4R5或OR5a。 该化合物是磷酸二酯酶（PDE）抑制剂，特别是PDE4抑制剂。本发明还提供了公式（I）的化合物或其药学上可接受的盐的用途，用于制造治疗和/或预防哺乳动物，如人类的炎症性和/或过敏性疾病的药物，例如慢性阻塞性肺疾病（COPD），哮喘或过敏性鼻炎。