2',4'-difluoro-[1,1'-biphenyl]-4-sulfonic acid | 1218794-17-2

• 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',4'-difluoro-[1,1'-biphenyl]-4-sulfonic acid
• 英文别名: 2',4'-difluorobiphen-4-yl sulfonic acid；2',4'-difluorobiphenyl-4-sulfonic acid；2',4'-Difluorobiphenyl-4-sulfonic acid；4-(2,4-difluorophenyl)benzenesulfonic acid
• CAS: 1218794-17-2
• 化学式: C₁₂H₈F₂O₃S
• 分子量: 270.257
• InChiKey: PBRRGRQTSBNNJY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  62.8
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2',4'-difluoro-[1,1'-biphenyl]-4-sulfonic acid 在 N,N-二甲基甲酰胺 氯化亚砜 作用下， 反应 4.5h， 生成 2′,4′-difluoro-biphenyl-4-sulfonylchloride
  参考文献：
  名称：

  [EN] ARYL-PHENYL-SULFONAMIDO-CYCLOALKYL COMPOUNDS AND THEIR USE
  [FR] COMPOSÉS ARYL-PHÉNYL-SULFONAMINO-CYCLOALKYLE ET LEURS UTILISATIONS

  摘要：

  本发明一般涉及治疗化合物领域，更具体地涉及以下化学式的某些芳基-苯基-磺酰胺基-环烷基化合物（以下统称为“APSAC化合物”）。本发明还涉及包含这种化合物的药物组合物，以及这种化合物和组合物的使用，无论是在体外还是体内，用于治疗炎症和/或关节破坏和/或骨质流失等疾病，过度和/或不适当和/或持续激活免疫系统介导的疾病，例如炎症性和自身免疫性疾病，如类风湿关节炎、银屑病、银屑病性关节炎、慢性阻塞性肺病（COPD）、动脉粥样硬化、炎症性肠病、强直性脊柱炎等；与骨质流失相关的疾病，例如类风湿性关节炎中由过度破骨细胞活动引起的骨质流失、骨质疏松症、癌症相关的骨病、帕金森病等等；以及癌症，如血液恶性肿瘤、实体肿瘤等。化学式（I）。

  公开号：

  WO2010032009A1
• 作为产物：
  描述：

  2,4-二氟联苯 在 氯磺酸 作用下， 以 氯仿 为溶剂， 生成 2',4'-difluoro-[1,1'-biphenyl]-4-sulfonic acid
  参考文献：
  名称：

  [EN] ARYL-PHENYL-SULFONAMIDO-CYCLOALKYL COMPOUNDS AND THEIR USE
  [FR] COMPOSÉS ARYL-PHÉNYL-SULFONAMINO-CYCLOALKYLE ET LEURS UTILISATIONS

  摘要：

  本发明一般涉及治疗化合物领域，更具体地涉及以下化学式的某些芳基-苯基-磺酰胺基-环烷基化合物（以下统称为“APSAC化合物”）。本发明还涉及包含这种化合物的药物组合物，以及这种化合物和组合物的使用，无论是在体外还是体内，用于治疗炎症和/或关节破坏和/或骨质流失等疾病，过度和/或不适当和/或持续激活免疫系统介导的疾病，例如炎症性和自身免疫性疾病，如类风湿关节炎、银屑病、银屑病性关节炎、慢性阻塞性肺病（COPD）、动脉粥样硬化、炎症性肠病、强直性脊柱炎等；与骨质流失相关的疾病，例如类风湿性关节炎中由过度破骨细胞活动引起的骨质流失、骨质疏松症、癌症相关的骨病、帕金森病等等；以及癌症，如血液恶性肿瘤、实体肿瘤等。化学式（I）。

  公开号：

  WO2010032009A1

文献信息

• [EN] N-ACYL-{4-[(4-ARYL-PHENYL)SULFONYLMETHYL]PIPERIDINE} COMPOUNDS AND THEIR THERAPEUTIC USE<br/>[FR] COMPOSÉS N-ACYL-{4-[(4-ARYL-PHÉNYL)SULFONYLMÉTHYL]PIPÉRIDINE} ET LEUR UTILISATION THÉRAPEUTIQUE
  申请人：MODERN BIOSCIENCES LTD

  公开号：WO2020212581A1

  公开（公告）日：2020-10-22

  The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain N-acyl-4-[(4-aryl- phenyl)sulfonylmethyl]piperidine} compounds of the following formula (collectively referred to herein as NASMP compounds) that are useful, for example, in the treatment of disorders (e.g., diseases) including, e.g., multiple myeloma, diffuse large B-cell lymphoma, acute myeloid leukemia, eosinophilic leukemia, glioblastoma, melanoma, ovarian cancer, chemotherapy resistant cancer, radiation resistant cancer, inflammatory arthritis, rheumatoid arthritis, psoriatic arthritis, psoriasis, ulcerative colitis, Crohn's disease, systemic lupus erythematosus (SLE), lupus nephritis, asthma, chronic obstructive pulmonary disease (COPD), Hidradenitis suppurativa, autoimmune hepatitis, etc. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, for example, in therapy.

  本发明一般涉及治疗化合物领域。更具体地，本发明涉及以下公式的某些N-酰基-4-[(4-芳基苯基)磺酰甲基]哌啶}化合物（以下统称为NASMP化合物），这些化合物可用于治疗包括多发性骨髓瘤、弥漫性大B细胞淋巴瘤、急性髓细胞白血病、嗜酸性白血病、胶质母细胞瘤、黑色素瘤、卵巢癌、化疗耐药癌症、放射治疗耐药癌症、炎症性关节炎、类风湿关节炎、银屑病性关节炎、牛皮癣、溃疡性结肠炎、克罗恩病、系统性红斑狼疮（SLE）、狼疮性肾炎、哮喘、慢性阻塞性肺病（COPD）、汗腺脓肿、自身免疫性肝炎等疾病的治疗，本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在治疗中的使用。
• [EN] ARYL-PHENYL-SULFONAMIDE-PHENYLENE COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS ARYL-PHÉNYL-SULFONAMINO-PHÉNYLÈNE ET LEURS UTILISATIONS
  申请人：PIMCO 2664 LTD

  公开号：WO2010032010A1

  公开（公告）日：2010-03-25

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as "APSAP compounds"). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc.

  本发明通常涉及治疗化合物领域，更具体地涉及以下式(I)的某些芳基苯磺酰胺基苯基化合物（以下统称为“APSAP化合物”）。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体内外的使用，例如用于治疗炎症和/或关节破坏和/或骨质流失；过度和/或不适当和/或持续激活免疫系统的疾病；炎症性和自身免疫性疾病，例如类风湿关节炎、牛皮癣、银屑病性关节炎、慢性阻塞性肺病（COPD）、动脉粥样硬化、炎症性肠病、强直性脊柱炎等；与骨质流失相关的疾病，例如类风湿性关节炎中与过度破骨细胞活性相关的骨质流失、骨质疏松症、癌症相关骨病、帕吉特病等；以及癌症，如血液系统恶性肿瘤、实体肿瘤等。
• Aryl-Phenyl-Sulfonamido-Cycloalkyl Compounds and Their Use
  申请人：Greig Iain Robert

  公开号：US20110172189A1

  公开（公告）日：2011-07-14

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc. Formula (I).

  本发明涉及治疗化合物领域，更具体地涉及以下公式的某些芳基-苯基-磺酰胺基环烷化合物（统称为“APSAC化合物”）。本发明还涉及包含这种化合物的制药组合物以及在体内外使用这种化合物和组合物治疗炎症、关节破坏和/或骨质流失等问题，治疗由免疫系统过度和/或不适当和/或持久活化引起的疾病，如类风湿性关节炎、牛皮癣、银屑病性关节炎、慢性阻塞性肺疾病（COPD）、动脉粥样硬化、炎症性肠病、强直性脊柱炎等炎症和自身免疫性疾病，以及与骨质流失相关的疾病，如类风湿性关节炎、骨质疏松症、癌症相关骨病、帕吉特病等，以及癌症，如血液系统恶性肿瘤、实体瘤等。公式（I）。
• Aryl-Phenyl-Sulfonamide-Phenylene Compounds and Their Use
  申请人：Greig Iain Robert

  公开号：US20110190302A1

  公开（公告）日：2011-08-04

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as “APSAP compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc.

  本发明涉及治疗化合物领域，更具体地涉及以下公式（I）的某些芳基-苯基-磺酰胺基-苯基化合物（以下统称为“APSAP化合物”）。本发明还涉及包含这些化合物的制药组合物，以及这些化合物和组合物的使用，无论是在体外还是体内，用于治疗炎症和/或关节破坏和/或骨质流失；治疗由免疫系统过度和/或不适当和/或持续激活引起的疾病；治疗炎症和自身免疫性疾病，例如类风湿性关节炎、牛皮癣、银屑病性关节炎、慢性阻塞性肺疾病（COPD）、动脉粥样硬化、炎性肠病、强直性脊柱炎等；治疗与骨质流失有关的疾病，例如类风湿关节炎中过度破骨细胞活动引起的骨质流失、骨质疏松症、癌症相关骨病、帕吉特病等；以及治疗癌症，例如血液系统恶性肿瘤、实体瘤等。
• Aryl-phenyl-sulfonamide-phenylene compounds and their use
  申请人：PIMCO 2664 Limited

  公开号：US08207167B2

  公开（公告）日：2012-06-26

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as “APSAP compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumor, etc.

  本发明涉及治疗化合物领域，更具体地涉及以下公式（I）的某些芳基-苯基-磺酰胺基-苯基化合物（统称为“APSAP化合物”）。本发明还涉及包含这种化合物的制药组合物，以及这种化合物和组合物的使用，无论是体外还是体内，用于治疗炎症和/或关节破坏和/或骨质流失等疾病；过度和/或不适当和/或长时间激活免疫系统介导的疾病；炎症性和自身免疫性疾病，例如类风湿性关节炎、银屑病、银屑病性关节炎、慢性阻塞性肺疾病（COPD）、动脉硬化、炎症性肠病、强直性脊柱炎等；与骨质流失有关的疾病，例如类风湿性关节炎中过度破骨细胞活性、骨质疏松症、与癌症相关的骨病、帕吉特病等；以及癌症，例如血液系统恶性肿瘤、实体肿瘤等。