4-(4-氯苯氧基)-苯磺酰氯 | 191327-30-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 4-(4-氯苯氧基)-苯磺酰氯
• 中文别名: 4-(4-氯苯氧基)苯-1-磺酰氯
• 英文名称: 4-(4'-chlorophenoxy)phenylsulfonyl chloride
• 英文别名: 4-(4-chlorophenoxy)-benzenesulfonyl chloride；4-(4-chlorophenyloxy)benzene-sulfonyl chloride；4''-chloro-4'-phenoxybenzenesulfonyl chloride；4-(4-chloro-phenoxy)-benzenesulphonyl chloride；4-(4-chlorophenoxy)benzenesulfonyl Chloride
• CAS: 191327-30-7
• 化学式: C₁₂H₈Cl₂O₃S
• mdl: MFCD01631865
• 分子量: 303.166
• InChiKey: XOXRXINFTQAJBW-UHFFFAOYSA-N

物化性质

• 沸点：
  396.3±22.0 °C(Predicted)
• 密度：
  1.453±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  51.8
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 危险品标志：
  Xi
• 储存条件：
  2-8°C

反应信息

• 作为反应物：
  描述：

  4-(4-氯苯氧基)-苯磺酰氯 生成 1-氯-4-[4-(甲硫基)苯氧基]苯
  参考文献：
  名称：

  Processes for preparing 3-Arylsulfur hydroxamic acids

  摘要：

  该发明提供了制备公式I化合物的过程：Y-C(═O-C(R1)(R2)-CH2-S(O)nR3其中：Y为羟基或XONX，其中每个X独立地为氢、低碳基或低酰基；R1为氢或低碳基；R2为氢、低碳基、芳基、芳基烷基、环烷基、环烷基烷基，或R1和R2与它们所连接的碳原子形成环烷基或杂环烷基；R3为芳基；n为0、1或2。该发明还提供了新颖的芳基卤代烷基硫醚中间体，用于制备公式I化合物，以及制备芳基烷基硫醚的新方法。

  公开号：

  US06342639B1
• 作为产物：
  描述：

  二苯醚 在 氯磺酸 、 磺酰氯 作用下， 以60%的产率得到4-(4-氯苯氧基)-苯磺酰氯
  参考文献：
  名称：

  Processes for preparing 3-Arylsulfur hydroxamic acids

  摘要：

  这项发明提供了一种制备化合物I的方法：Y—C(═O—C(R1)(R2)—CH2—S(O)nR3其中：Y是羟基或XONX，其中每个X独立地是氢、低烷基或低酰基；R1是氢或低烷基；R2是氢、低烷基、芳基、芳基烷基、环烷基、环烷基烷基，或者R1和R2与它们附着的碳原子一起形成环烷基或杂环基；R3是芳基；n为0、1或2。该发明还提供了用于制备化合物I的新型芳基卤代烷基硫代中间体以及制备芳基烷基硫代化合物的新方法。

  公开号：

  US06342639B1

文献信息

• (4-arylsulfonylamino)-tetrahydropyran-4-carboxylic acid hydroxamides
  申请人：Pfizer Inc.

  公开号：US06087392A1

  公开（公告）日：2000-07-11

  A compound of the formula ##STR1## wherein Q is as defined above, are useful in the treatment of a condition selected from the group consisting of arthritis (including osteoarthritis and rheumatoid arthritis), inflammatory bowel disease, Crohn's disease, emphysema, chronic obstructive pulmonary disease, Alzheimer's disease, organ transplant toxicity, cachexia, allergic reactions, allergic contact hypersensitivity, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, osteoporosis, loosening of artificial joint implants, atherosclerosis (including atherosclerotic plaque rupture), aortic aneurysm (including abdominal aortic aneurysm and brain aortic aneurysm), congestive heart failure, myocardial infarction, stroke, cerebral ischemia, head trauma, spinal cord injury, neuro-degenerative disorders (acute and chronic), autoimmune disorders, Huntington's disease, Parkinson's disease, migraine, depression, peripheral neuropathy, pain, cerebral amyloid angiopathy, nootropic or cognition enhancement, amyotrophic lateral sclerosis, multiple sclerosis, ocular angiogenesis, corneal injury, macular degeneration, abnormal wound healing, burns, diabetes, tumor invasion, tumor growth, tumor metastasis, corneal scarring, scleritis, AIDS, sepsis and septic shock. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.

  公式为##STR1##的化合物，在治疗以下疾病方面是有用的：关节炎（包括骨关节炎和类风湿关节炎）、炎症性肠病、克罗恩病、肺气肿、慢性阻塞性肺病、阿尔茨海默病、器官移植毒性、虚弱症、过敏反应、过敏性接触性过敏症、癌症、组织溃疡、再狭窄、牙周病、表皮溃疡性水疱病、骨质疏松症、人工关节植入物松动、动脉粥样硬化（包括动脉粥样硬化斑块破裂）、主动脉瘤（包括腹主动脉瘤和脑主动脉瘤）、充血性心力衰竭、心肌梗死、中风、脑缺血、头部创伤、脊髓损伤、神经退行性疾病（急性和慢性）、自身免疫性疾病、亨廷顿病、帕金森病、偏头痛、抑郁症、周围神经病、疼痛、脑淀粉样血管病、脑力增强剂或认知增强剂、肌萎缩侧索硬化、多发性硬化、眼部血管生成、角膜损伤、黄斑变性、异常伤口愈合、烧伤、糖尿病、肿瘤浸润、肿瘤生长、肿瘤转移、角膜瘢痕、巩膜炎、艾滋病、败血症和脓毒性休克。此外，本发明的化合物可与标准非甾体类抗炎药（NSAID'S）和镇痛药联合治疗，也可与阿霉素、多柔比星、顺铂、依托泊苷、紫杉醇、多西他赛和其他生物碱（如长春碱）等细胞毒药物联合治疗癌症。
• 3-(arylsulfonylamino)-tetrahydropyran-3-carboxylic acid hydroxamides
  申请人：Pfizer Inc

  公开号：US06197810B1

  公开（公告）日：2001-03-06

  A compound of the formula wherein R1, R2, R3, R4 and Q are as defined above, are useful in the treatment of arthritis (including osteoarthritis and rheumatoid arthritis), cancer and other diseases. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID's), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.

  其中R1、R2、R3、R4和Q如上定义，可用于治疗关节炎（包括骨关节炎和类风湿性关节炎）、癌症和其他疾病。此外，本发明的化合物可与标准非甾体抗炎药（NSAID's）、COX-2抑制剂和止痛药联合使用，也可与细胞毒性药物如阿霉素、道诺霉素、顺铂、依托泊苷、紫杉醇、多西他赛和其他生物碱如长春新碱联合用于治疗癌症。
• Metalloproteinase inhibitors-compositions, uses preparation and intermediates thereof
  申请人：Agouron Pharmaceuticals, Inc.

  公开号：US06500948B1

  公开（公告）日：2002-12-31

  The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder are carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt of solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates. The invention still further relates to methods and intermediates useful for preparing these compounds, prodrugs, salts, and solvates.

  这项发明涉及以下式子的化合物： 其中：Z为O或S；V为二价基团，与C*和N一起形成具有六个环原子的环，其中除C*和N之外的每个环原子独立地未取代或被适当取代基取代，且其中至少一个其他环原子为从O、N和S中选择的杂原子，其余为碳原子；Ar为芳基或杂芳基；以及其药学上可接受的前药、盐和溶剂化合物。 该发明还涉及这些化合物的药学上可接受的前药、盐和溶剂。该发明还涉及通过给予式I的化合物或其前药、盐或溶剂来抑制金属蛋白酶活性的方法。该发明还涉及包含这些化合物、前药、盐和溶剂的有效量的药物组合物。该发明还涉及用于制备这些化合物、前药、盐和溶剂的方法和中间体。
• Metalloproteinase inhibitors and intermediates useful for their
  申请人：Agouron Pharmaceuticals, Inc.

  公开号：US06153757A1

  公开（公告）日：2000-11-28

  The invention relates to compounds of formula (1) ##STR1## wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder is carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of formula (1) or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates. The invention still further relates to methods and intermediates useful for preparing these compounds, prodrugs, salts, and solvates.

  该发明涉及式（1）的化合物##STR1##其中：Z为O或S；V为与C*和N一起形成具有六个环原子的环的二价基团，其中除C*和N之外的每个环原子独立地未取代或被适当取代基取代，且所述其他环原子中至少有一个是从O、N和S中选择的杂原子，其余为碳原子；Ar为芳基或杂芳基团；以及其药学上可接受的前药、盐和溶剂化合物。该发明还涉及这些化合物的药学上可接受的前药、盐和溶剂。该发明还涉及通过给予式（1）的化合物或其前药、盐或溶剂来抑制金属蛋白酶活性的方法。该发明还涉及包含这些化合物、前药、盐和溶剂的有效量的药物组合物。该发明还涉及用于制备这些化合物、前药、盐和溶剂的方法和中间体。
• Metalloproteinase inhibitors, pharmaceutical compositions containing
  申请人：Agouron Pharmaceuticals, Inc.

  公开号：US05753653A1

  公开（公告）日：1998-05-19

  The invention relates to compounds of the formula I ##STR1## in which Q is a divalent radical having four ring atoms which together with C* and N form a six-membered ring, each of these four ring atoms being unsubstituted or substituted by a suitable substituent and at least one being a heteroatom selected from O, N and S, with the remainder being carbon atoms; and Ar is an aryl or heteroaryl group. The invention further relates to pharmaceutically acceptable prodrugs and pharmaceutically acceptable salts of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases, especially MMPs or TNF-.alpha., by administering a compound of the formula I or a salt or prodrug thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, salts, and prodrugs.

  该发明涉及公式I的化合物，其中Q是一个二价基团，具有四个环原子，这四个环原子与C*和N一起形成一个六元环，这四个环原子中的每一个未被取代或被适当取代，至少有一个是从O、N和S中选择的杂原子，其余为碳原子；Ar是芳基或杂芳基基团。该发明还涉及这些化合物的药学上可接受的前药和药学上可接受的盐。该发明还涉及通过给予公式I的化合物或其盐或前药来抑制金属蛋白酶活性的方法，特别是MMPs或TNF-α。该发明还涉及包含这些化合物、盐和前药的有效量的药物组合物。