8-bromo-2-chloroquinoline-3-carbaldehyde | 1018050-36-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 8-bromo-2-chloroquinoline-3-carbaldehyde
• CAS: 1018050-36-6
• 化学式: C₁₀H₅BrClNO
• 分子量: 270.513
• InChiKey: ARFJBUGMPWRAJF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  30
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  、 8-bromo-2-chloroquinoline-3-carbaldehyde 、 (R)-(+)-叔丁基亚磺酰胺 在 titanium(IV) isopropylate 作用下， 以afforded the title compound (335 mg, 87%) as a yellow solid的产率得到(R,E)-N-[(8-bromo-2-chloroquinolin-3-yl)methylidene]-2-methylpropane-2-sulfinamide
  参考文献：
  名称：

  Triazine derivatives as kinase inhibitors

  摘要：

  一系列取代的[1,3,5]三嗪-2-基衍生物，具有选择性地抑制PI3激酶酶，因此在医学上具有益处，例如在治疗炎症、自身免疫、心血管、神经退行性、代谢、肿瘤、疼痛或眼科疾病方面。

  公开号：

  US08785628B2

文献信息

• [EN] TRIAZINE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] DÉRIVÉS DE TRIAZINE EN TANT QU'INHIBITEURS DE KINASES
  申请人：UCB PHARMA SA

  公开号：WO2010100405A1

  公开（公告）日：2010-09-10

  A series of substituted [1,3,5]triazin-2-yl derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

  一系列取代的[1,3,5]三嗪-2-基衍生物，作为选择性PI3激酶酶抑制剂，在医学上具有益处，例如在治疗炎症性、自身免疫性、心血管、神经退行性、代谢性、肿瘤学、疼痛或眼科疾病方面。
• HETEROCYCLIC COMPOUNDS AND USES THEREOF
  申请人：Ruan Fuqiang

  公开号：US20190308963A1

  公开（公告）日：2019-10-10

  In recognition of the unmet need to develop novel therapeutic agents, the present invention discloses a novel class of heterocycles as dual inhibitors of BRD4 and class I PI3Ks. The compounds claimed herein could be used alone or in combination therapies for the effective treatment of a wide range of age-related diseases, including cancer. The present invention also provides methods for preparing compounds of the invention thereto.

  为了开发新型治疗药物的未满足需求，本发明公开了一类新型杂环化合物，作为BRD4和I类PI3Ks的双重抑制剂。本文所述的化合物可单独使用或与其他药物联合治疗，有效治疗包括癌症在内的广泛的年龄相关疾病。本发明还提供了制备这些化合物的方法。
• Triazine Derivatives as Kinase Inhibitors
  申请人：Allen Daniel Rees

  公开号：US20120053167A1

  公开（公告）日：2012-03-01

  A series of substituted [1,3,5]triazin-2-yl derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

  一系列取代的[1,3,5]三嗪-2-基衍生物是选择性PI3激酶抑制剂，因此在医学上具有益处，例如在治疗炎症、自身免疫、心血管、神经退行性、代谢、肿瘤、疼痛或眼科疾病方面。
• HETEROCYCLIC COMPOUNDS AND THEIR USES
  申请人：Chen Yi

  公开号：US20120220586A1

  公开（公告）日：2012-08-30

  Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

  含有代替的双环杂环芳基和组合物，用于治疗一般炎症、关节炎、风湿性疾病、骨关节炎、炎症性肠病、炎症性眼疾、炎症性或不稳定膀胱疾病、牛皮癣、具有炎症成分的皮肤疾病、慢性炎症病症，包括但不限于自身免疫性疾病，如系统性红斑狼疮（SLE）、重症肌无力、类风湿性关节炎、急性播散性脑脊髓炎、特发性血小板减少性紫癜、多发性硬化症、Sjogren综合征和自身免疫性溶血性贫血，过敏反应包括所有形式的过敏反应。本发明还提供了治疗通过、依赖或与p110δ活性相关的癌症的方法，包括但不限于白血病，如急性髓细胞白血病（AML）、骨髓增生异常综合征（MDS）、骨髓增生性疾病（MPD）、慢性髓细胞白血病（CML）、T细胞急性淋巴细胞白血病（T-ALL）、B细胞急性淋巴细胞白血病（B-ALL）、非霍奇金淋巴瘤（NHL）、B细胞淋巴瘤和实体瘤，如乳腺癌。
• Heterocyclic compounds and their uses
  申请人：Chen Yi

  公开号：US20090137581A1

  公开（公告）日：2009-05-28

  Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

  含有取代的双环杂芳基和组合物，用于治疗一般炎症、关节炎、风湿性疾病、骨关节炎、炎症性肠病、炎症性眼病、炎症性或不稳定的膀胱疾病、牛皮癣、带有炎症成分的皮肤疾病、慢性炎症性疾病，包括但不限于自身免疫性疾病，如系统性红斑狼疮（SLE）、重症肌无力、类风湿性关节炎、急性播散性脑脊髓炎、特发性血小板减少性紫癜、多发性硬化症、干燥综合症和自身免疫性溶血性贫血，过敏症包括所有形式的过敏反应。本发明还能够治疗介导、依赖或与p110δ活性相关的癌症的方法，包括但不限于白血病，如急性髓性白血病（AML）、骨髓增生异常综合症（MDS）、骨髓增生性疾病（MPD）、慢性髓性白血病（CML）、T细胞急性淋巴细胞白血病（T-ALL）、B细胞急性淋巴细胞白血病（B-ALL）、非霍奇金淋巴瘤（NHL）、B细胞淋巴瘤和实体肿瘤，如乳腺癌。