(2-Amino-4-bromophenyl)carbamic acid

• 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: (2-Amino-4-bromophenyl)carbamic acid
• 英文别名: (2-amino-4-bromophenyl)carbamic acid
• 化学式: C₇H₇BrN₂O₂
• 分子量: 231.05
• InChiKey: LOLVIEKEJOVUBV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  75.4
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• [EN] METABOTROPIC GLUTAMATE RECEPTOR NEGATIVE ALLOSTERIC MODULATORS (NAMS) AND USES THEREOF<br/>[FR] MODULATEURS ALLOSTÉRIQUES NÉGATIFS (NAM) DU RÉCEPTEUR MÉTABOTROPIQUE DU GLUTAMATE ET UTILISATIONS DE CEUX-CI
  申请人：SANFORD BURNHAM MED RES INST

  公开号：WO2015191630A1

  公开（公告）日：2015-12-17

  Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.

  本文提供了小分子活性代谢型谷氨酸亚型-2和-3受体负向变构调节剂（NAMs），包括这些化合物的组合物，以及使用这些化合物和组合物的方法。
• [EN] PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS<br/>[FR] ACIDES PHÉNYLSULFAMOYLBENZOÏQUES EN TANT QUE MODULATEURS D'ERAP1
  申请人：GREY WOLF THERAPEUTICS LTD

  公开号：WO2020225569A1

  公开（公告）日：2020-11-12

  The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X-Y is -NHSO2- or -SO2NH-; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one ormore substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, C land alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl,Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl andhaloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl,SO2NR12R13, heteroaryl, CONR10R11 and alkyl, wherein said heteroaryl group is optionallysubstituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; and R9 is H, alkyl or halo; R10 and R11 are each independently H or alkyl; and R12 and R13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno- oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).

  本发明涉及一种具有式(I)的化合物，或其药学上可接受的盐或水合物，其中：基团X-Y为-NHSO2-或-SO2NH-；Z为单环芳基或杂环芳基，每个基团可选择地由一种或多种从烷基、环烷基、卤素、烷氧基、CN、卤代烷基和羟基中选择的取代基取代；R1为H或烷基；R2从COOH和四唑基团中选择；R3从H、C和烷基中选择；R4从H和卤素中选择；R5从H、烷基、卤代烷基、SO2-烷基、Cl、烷氧基、OH、CN、羟基烷基、烷基硫、杂环芳基、环烷基、杂环烷基和卤代烷氧基中选择；R6为H；R7从H、CN、卤代烷基、卤素、SO2-烷基、SO2NR12R13、杂环芳基、CONR10R11和烷基中选择，其中所述的杂环芳基可选择地由一种或多种从烷基、卤素、烷氧基、CN、卤代烷基和羟基中选择的取代基取代；R8从H、烷基、卤代烷基和卤素中选择；R9为H、烷基或卤素；R10和R11各自独立地为H或烷基；R12和R13各自独立地为H或烷基。本发明的进一步方面涉及这些化合物在免疫肿瘤学领域及相关应用中的用途。本发明的另一个方面涉及式(la)和(lb)的化合物。
• [EN] INHIBITORS OF HISTONE DEACETYLASE<br/>[FR] INHIBITEURS D'HISTONE-DÉSACÉTYLASES
  申请人：BROAD INST INC

  公开号：WO2014018979A1

  公开（公告）日：2014-01-30

  The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein X1, X2, X3, X4, X5, W1, W2, W3, and W4 are as described. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. In one aspect, the invention relates to selective HDAC3 inhibitors useful for protecting β-cells and improving insulin resistence. The selective HDAC3 inhibitors are also useful for promoting cognitive function and enhancing learning and memory formation. Compounds of the invention are useful for treating, alleviating, and/or preventing various conditions, including for example, a metabolic disorder such as type 1 or type 2 diabetes, dyslipidemias, lipodystrophies, liver disease associated with metabolic syndrome, polycystic ovarian syndrome, or obesity; inflammatory disease; neurological disorder; a memory or cognitive function disorder/impairment; an extinction learning disorder; fungal disease or infection; viral disease or infection such as HIV; hematological disease; liver disease; lysosomal storage disease; or neoplastic disease in humans or animals.

  本发明涉及式(I)的化合物或其药学上可接受的盐、水合物、溶剂合物或前药，其中X1、X2、X3、X4、X5、W1、W2、W3和W4如所述。本发明一般涉及组织脱乙酰化酶抑制剂以及制备和使用它们的方法。在一个方面，该发明涉及选择性HDAC3抑制剂，可用于保护β细胞并改善胰岛素抵抗。选择性HDAC3抑制剂还可用于促进认知功能，增强学习和记忆形成。本发明的化合物可用于治疗、缓解和/或预防各种疾病，例如代谢紊乱，如1型或2型糖尿病、血脂异常、脂肪萎缩、与代谢综合征相关的肝病、多囊卵巢综合征或肥胖症；炎症性疾病；神经系统疾病；记忆或认知功能障碍；消除学习障碍；真菌疾病或感染；病毒性疾病或感染，如艾滋病病毒；血液病；肝病；溶酶体贮积病；或人类或动物的肿瘤性疾病。
• INHIBITORS OF HISTONE DEACETYLASE
  申请人：The General Hospital Corporation d/b/a Massachusetts General Hospital

  公开号：US20150191427A1

  公开（公告）日：2015-07-09

  The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein X 1 , X 2 , X 3 , X 4 , X 5 , W 1 , W 2 , W 3 , and W 4 are as described. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. In one aspect, the invention relates to selective HDAC3 inhibitors useful for protecting β-cells and improving insulin resistance. The selective HDAC3 inhibitors are also useful for promoting cognitive function and enhancing learning and memory formation. Compounds of the invention are useful for treating, alleviating, and/or preventing various conditions, including for example, a metabolic disorder such as type 1 or type 2 diabetes, dyslipidemias, lipodystrophies, liver disease associated with metabolic syndrome, polycystic ovarian syndrome, or obesity; inflammatory disease; neurological disorder; a memory or cognitive function disorder/impairment; an extinction learning disorder; fungal disease or infection; viral disease or infection such as HIV; hematological disease; liver disease; lysosomal storage disease; or neoplastic disease in humans or animals.

  本发明涉及公式(I)的化合物或其药学上可接受的盐、水合物、溶剂物或前药，其中X1、X2、X3、X4、X5、W1、W2、W3和W4如所述。本发明通常涉及组织脱乙酰化酶抑制剂及其制备和使用方法。在一个方面，本发明涉及选择性HDAC3抑制剂，用于保护β细胞和改善胰岛素抵抗力。选择性HDAC3抑制剂还有助于促进认知功能和增强学习和记忆形成。本发明的化合物可用于治疗、缓解和/或预防各种疾病，包括代谢紊乱，例如1型或2型糖尿病、脂质代谢异常、脂肪萎缩症、代谢综合征相关的肝病、多囊卵巢综合征或肥胖症；炎症性疾病；神经系统疾病；记忆或认知功能障碍；灭绝学习障碍；真菌疾病或感染；病毒性疾病或感染，如HIV；血液学疾病；肝脏疾病；溶酶体贮积病；或动物中的肿瘤性疾病。
• Metabotropic glutamate receptor negative allosteric modulators (NAMs) and uses thereof
  申请人：Sanford Burnham Prebys Medical Discovery Institute

  公开号：US10597367B2

  公开（公告）日：2020-03-24

  Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.

  本文提供了小分子活性代谢型谷氨酸亚型-2 和-3 受体负异调节剂（NAMs）、包含这些化合物的组合物以及使用这些化合物和组合物的方法。