UK-373911 | 291305-06-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: UK-373911
• 英文别名: cis-(1S)-N-methyl-7-sulphonamido-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine；(5S,8S)-5-(3,4-dichlorophenyl)-8-(methylamino)-5,6,7,8-tetrahydronaphthalene-2-sulfonamide
• CAS: 291305-06-1
• 化学式: C₁₇H₁₈Cl₂N₂O₂S
• 分子量: 385.314
• InChiKey: HGBGXSPIBLZGHS-SJCJKPOMSA-N

物化性质

• 沸点：
  544.6±60.0 °C(Predicted)
• 密度：
  1.44±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  80.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  盐酸舍曲林 在 氯磺酸 、 氯化亚砜 、 氨 、 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 16.5h， 以58%的产率得到UK-373911
  参考文献：
  名称：

  1,2,3,4-TETRAHYDRO-1-NAPHTHALENAMINE COMPOUNDS USEFUL IN THERAPY

  摘要：

  公开号：

  EP1157002B1

文献信息

• COMPOSITIONS AND METHODS FOR TREATMENT OF VIRAL DISEASES
  申请人：Johansen Lisa M.

  公开号：US20100009970A1

  公开（公告）日：2010-01-14

  The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.

  本发明涉及用于治疗病毒性疾病的组合物、方法和试剂盒。在某些实施方式中，病毒性疾病是由单链RNA病毒、黄病毒科病毒或肝病毒引起的。在特定实施方式中，病毒性疾病是病毒性肝炎（例如甲型肝炎、乙型肝炎、丙型肝炎、丁型肝炎、戊型肝炎），药剂或药剂组合包括舍曲林、舍曲林类似物、UK-416244或UK-416244类似物。还包括用于鉴定可用于治疗病毒性疾病的新化合物的筛选方法。
• [EN] 1,2,3,4-TETRAHYDRO-1-NAPHTHALENAMINE COMPOUNDS USEFUL IN THERAPY<br/>[FR] COMPOSES 1,2,3,4-TETRAHYDRO-1-NAPHTHALENAMINES UTILES EN THERAPIE
  申请人：PFIZER LTD

  公开号：WO2000051972A1

  公开（公告）日：2000-09-08

  The invention provides compounds of formula (I), wherein R?1 and R2¿ independently represent H or C¿1-6? alkyl; R?3¿ represents phenyl substituted by at least one group selected form halo, CF¿3?, OCF3, CN, OH, C1-6 alkyl and C1-6 alkoxy; and R?4, R5 and R11¿ independently represent H or -(CH¿2?)n-A, wherein n represents 0, 1 or 2, provided that at least one of R?4, R5 and R11¿ is other than H; A represents CONR6R7 or SO¿2NR?6R7, wherein R?6 and R7¿ independently represent H, C¿3-6? cycloalkyl or C1-6 alkyl, the C?1-6¿ alkyl group being optionally substituted, in addition, R?6 and R7¿ may, together with the N atom to which they are attached, represent a ring which is optionally substituted; CO¿2R?8, wherein R8 represents H or C¿1-6? alkyl; NR?9R10¿, wherein R?9 and R10¿ independently represent H, C¿1-6? alkyl (optionally substituted), (C1-6 alkyl)SO2-, (C1-6 alkyl)CO-, H2NSO2- or H2NCO-; a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, which is optionally substituted; S(O)x(C1-6 alkyl), wherein x represents 0, 1 or 2; OH; CN, NO2; or C1-6 alkoxy which is optionally substituted; provided that when NR?1R2¿ represents N(H) methyl, R4 represents H and R3 represents 4- chlorophenyl, then R5 does not represent methoxy; and pharmaceutically acceptable salts thereof. The compounds of the invention are useful in the treatment or prevention of a variety of disorders, including those in which the regulation of monoamine transporter function is implicated.

  本发明提供了式（I）的化合物，其中R?1和R2¿独立表示H或C¿1-6?烷基; R?3¿表示苯基，其被至少一个从卤，CF¿3？，OCF3，CN，OH，C1-6烷基和C1-6烷氧基中选择的基团取代; R?4，R5和R11¿独立表示H或-（CH¿2？）n-A，其中n表示0，1或2，前提是至少有一个R?4，R5和R11¿不是H; A表示CONR6R7或SO¿2NR?6R7，其中R?6和R7¿独立表示H，C¿3-6?环烷基或C1-6烷基，C?1-6?烷基可以选择性地取代，此外，R?6和R7¿可以与它们所连接的N原子一起表示可选择取代的环; CO¿2R?8，其中R8表示H或C¿1-6?烷基; NR?9R10¿，其中R?9和R10¿独立表示H，C¿1-6?烷基（可选择性取代），（C1-6烷基）SO2-，（C1-6烷基）CO-，H2NSO2-或H2NCO-; 包含1、2或3个从N、S和O中选择的杂原子的5-或6元杂环，可选择性取代; S（O）x（C1-6烷基），其中x表示0，1或2; OH; CN，NO2;或可选择性取代的C1-6烷氧基; 前提是当NR?1R2¿表示N（H）甲基，R4表示H且R3表示4-氯苯基时，R5不表示甲氧基;以及其药学上可接受的盐。本发明的化合物在治疗或预防各种疾病方面有用，包括那些涉及单胺转运体功能调节的疾病。
• Compositions and methods for treating medical conditions
  申请人：Lessem Jan N.

  公开号：US20080287406A1

  公开（公告）日：2008-11-20

  The invention features methods, compositions, and kits for the treatment of pain, pruritus, immunoinflammatory disorders, musculoskeletal disorders, and the reduction of serum C reactive protein (CRP) in a patient having a disease or conditions associated with an increased CRP level. The methods, compositions, and kits of the invention provide for a combination therapy including an SSRI and a corticosteroid.
• COMPOSITIONS AND METHODS FOR TREATING VIRAL INFECTIONS
  申请人：Sharma Geeta

  公开号：US20100081713A1

  公开（公告）日：2010-04-01

  The present invention provides compositions, methods, and kits for treating or preventing a viral infection (e.g., an infection caused by an influenza virus).
• Compositions and methods for selective delivery of oligonucleotide molecules to specific neuron types
  申请人：Montefeltro Andres Pablo

  公开号：US20120322991A1

  公开（公告）日：2012-12-20

  The invention provides a conjugate comprising (i) a nucleic acid which is complementary to a target nucleic acid sequence and which expression prevents or reduces expression of the target nucleic acid and (ii) a selectivity agent which is capable of binding with high affinity to a neurotransmitter transporter. The conjugates of the present invention are useful for the delivery of the nucleic acid to a cell of interests and thus, for the treatment of diseases which require a down-regulation of the protein encoded by the target nucleic acid as well as for the delivery of imaging agents to the cells for diagnostic purposes.