(1R,3S)-3-hydroxycyclopentanecarboxylic acid | 1443511-35-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (1R,3S)-3-hydroxycyclopentanecarboxylic acid
• 英文别名: (1R,3S)-3-Hydroxycyclopentane-1-carboxylic acid
• CAS: 1443511-35-0
• 化学式: C₆H₁₀O₃
• 分子量: 130.144
• InChiKey: XWWQLKYMTLWXKN-UHNVWZDZSA-N

物化性质

• 沸点：
  297.2±33.0 °C(Predicted)
• 密度：
  1.328±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  57.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (1R,3S)-3-hydroxycyclopentanecarboxylic acid 在 邻苯二甲酸二丁酯 作用下， 生成 2-氧杂双环[2.2.1]庚烷-3-酮
  参考文献：
  名称：

  Studies of Configuration. V. The Preparation and Configuration of cis-3-Methoxycyclopentanecarboxylic Acid

  摘要：

  DOI：

  10.1021/jo01087a616
• 作为产物：
  描述：

  3-氧代环戊羧酸甲酯 在 sodium hydroxide 、 乙醇 、 镍 作用下， 生成 (1R,3S)-3-hydroxycyclopentanecarboxylic acid
  参考文献：
  名称：

  Studies of Configuration. V. The Preparation and Configuration of cis-3-Methoxycyclopentanecarboxylic Acid

  摘要：

  DOI：

  10.1021/jo01087a616

文献信息

• Renin Inhibitors
  申请人：Baldwin John J.

  公开号：US20100168243A1

  公开（公告）日：2010-07-01

  The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

  本发明涉及天冬氨酸蛋白酶抑制剂。本发明还涉及包含所披露的天冬氨酸蛋白酶抑制剂的制药组合物。本发明进一步涉及在需要拮抗一个或多个天冬氨酸蛋白酶的患者中拮抗一个或多个天冬氨酸蛋白酶的方法，以及使用所披露的天冬氨酸蛋白酶抑制剂治疗天冬氨酸蛋白酶介导的疾病的方法。
• SELECTIVE KINASE INHIBITORS
  申请人：PORTOLA PHARMACEUTICALS, INC.

  公开号：US20140323418A1

  公开（公告）日：2014-10-30

  Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

  提供了用于抑制Syk激酶的嘧啶化合物，用于制备这种化合物的中间体，其制备方法，制备其制剂的制剂，抑制Syk激酶活性的方法，以及治疗至少部分由Syk激酶活性介导的病症的方法。
• [EN] N-(IMIDAZO[1,2-B]PYRIDAZIN-3-YL)-1-CYCLOHEXYL-2H-INDAZOLE-5-CARBOXAMIDE AND N-(PYRAZOLO[1,5-A]PYRIMIDIN-3-YL)-1-CYCLOHEXYL-2H-INDAZOLE-5-CARBOXAMIDE DERIVATIVES AS IRAK4 INHIBITORS FOR THE TREATMENT OF ASTHMA<br/>[FR] DÉRIVÉS DE N-(IMIDAZO[1,2-B]PYRIDAZIN-3-YL)-1-CYCLOHEXYL-2H-INDAZOLE-5-CARBOXAMIDE ET DE N-(PYRAZOLO[1,5-A]PYRIMIDIN-3-YL)-1-CYCLOHEXYL-2H-INDAZOLE-5-CARBOXAMIDE UTILISÉS EN TANT QU'INHIBITEURS D'IRAK4 POUR LE TRAITEMENT DE L'ASTHME
  申请人：ASTRAZENECA AB

  公开号：WO2022122876A1

  公开（公告）日：2022-06-16

  The present application relates to a compound of Formula (A),wherein R1 is selected from Formula (II) and Formula (III) and R2 is selected from Formula (IV), Formula (V) and Formula (VI) as IRAK4 inhibitors for use in methods of treatment of e.g. asthma and chronic obstructive pulmonary disease (COPD), cancer, inflammatory diseases, and autoinflammatory/autoimmune diseases such as e.g. systemic lupus erythematosus, rheumatoid arthritis, myositis, Sjogren's syndrome, systemic sclerosis, gout, endometriosis, atopic dermatitis and psoriasis. Preferred compounds of the present invention are e.g.: • N-(imidazo[1,2-b]pyridazin-3-yl)-1-cyclohexyl-2H-indazole-5- carboxamide, • N-(pyrazolo[1,5-a]pyrimidin-3-yl)-1-cyclohexyl-2H-indazole-5- carboxamide, • N-(imidazo[1,2-b]pyridazin-3-yl)-1-azaspiro[4.5]decan-8-yl-2H- indazole-5-carboxamide, and • N-(pyrazolo[1,5-a]pyrimidin-3-yl)-1-azaspiro[4.5]decan-8-yl-2H- indazole-5-carboxamide derivatives. An exemplary compound of the present invention is e.g. N- (imidazo[1,2-b]pyridazin-3-yl)-6-methoxy-2-((5r,8r)-1-methyl-2-oxo-1- azaspiro[4.5]decan-8-yl)-2H-indazole-5-carboxamide (Example 1): Formula (VII).

  本申请涉及一种化合物，其化学式为(A)，其中R1从化学式(II)和化学式(III)中选择，R2从化学式(IV)、化学式(V)和化学式(VI)中选择，作为IRAK4抑制剂用于治疗哮喘和慢性阻塞性肺疾病(COPD)、癌症、炎症性疾病以及自身免疫性疾病，如系统性红斑狼疮、类风湿性关节炎、肌炎、干燥综合症、系统性硬化症、痛风、子宫内膜异位症和银屑病等。本发明的优选化合物包括：•N-(咪唑并[1,2-b]吡嗪-3-基)-1-环己基-2H-吲唑-5-羧酰胺、•N-(吡唑并[1,5-a]嘧啶-3-基)-1-环己基-2H-吲唑-5-羧酰胺、•N-(咪唑并[1,2-b]吡嗪-3-基)-1-氮杂螺[4.5]癸烷-8-基-2H-吲唑-5-羧酰胺和•N-(吡唑并[1,5-a]嘧啶-3-基)-1-氮杂螺[4.5]癸烷-8-基-2H-吲唑-5-羧酰胺衍生物。本发明的一种示例化合物是N-(咪唑并[1,2-b]吡嗪-3-基)-6-甲氧基-2-((5r,8r)-1-甲基-2-氧代-1-氮杂螺[4.5]癸烷-8-基)-2H-吲唑-5-羧酰胺(实例1)：化学式(VII)。
• Inhibitors of Bruton's tyrosine kinase and methods of their use
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：US10689396B2

  公开（公告）日：2020-06-23

  The present disclosure is directed to compounds of formula I′ and methods of their use and preparation, as well as compositions comprising compounds of formula I′.

  本公开涉及式 I′化合物及其使用和制备方法，以及包含式 I′化合物的组合物。
• Inhibitors of Bruton's tyrosine kinase and method of their use
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：US10800792B2

  公开（公告）日：2020-10-13

  The present disclosure is directed to compounds of formula I′ and methods of their use and preparation, as well as compositions comprising compounds of formula I′.

  本公开涉及式 I′化合物及其使用和制备方法，以及包含式 I′化合物的组合物。