(9ci)-1H-咪唑并[4,5-f]喹噁啉 | 233-90-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: (9ci)-1H-咪唑并[4,5-f]喹噁啉
• 英文名称: 1H-imidazo<4,5-f>quinoxaline
• 英文别名: 3H-imidazo[4,5-f]quinoxaline
• CAS: 233-90-9
• 化学式: C₉H₆N₄
• mdl: MFCD18808180
• 分子量: 170.173
• InChiKey: YELMWJNXDALKFE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.59
• 重原子数：
  13.0
• 可旋转键数：
  0.0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  54.46
• 氢给体数：
  1.0
• 氢受体数：
  3.0

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  4-Chloro-7,8-dimethoxyimidazo[1,5-a]quinoxaline 、 (9ci)-1H-咪唑并[4,5-f]喹噁啉 、 L-酪氨酸 、 potassium carbonate 、 2-氯-6-甲酚 以 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 以to give 9.0 mg of the title compound as a tan solid的产率得到4-(2-Chloro-6-methylphenoxy)-7,8-dimethoxyimidazo[1,5-a]quinoxaline
  参考文献：
  名称：

  Imidazoquinoxaline protein tyrosine kinase inhibitors

  摘要：

  新型咪唑喹噁啉及其盐类，含有这些化合物的药物组合物，以及使用这些化合物治疗蛋白酪氨酸激酶相关疾病，如免疫系统疾病的方法。

  公开号：

  US06635626B1
• 作为产物：
  描述：

  甲酸 、 5,6-喹喔啉二胺 反应 3.0h， 以30%的产率得到(9ci)-1H-咪唑并[4,5-f]喹噁啉
  参考文献：
  名称：

  Kishan Rao, S.; Pandu Ranga Reddy, A.; Veerangaiah, V., Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1988, vol. 27, # 1-12, p. 960 - 961

  摘要：

  DOI：

文献信息

• [EN] 2-AMINO-4-HYDROXY-5-PYRIMIDINECARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF T CELL ACTIVATION FOR THE TREATMENT OF INFLAMMATORY DISEASES<br/>[FR] DERIVES DE 2-AMINO-4-HYDROXY-5-PYRIMIDINOCARBOXAMIDE ET COMPOSES ASSOCIES SERVANT D'INHIBITEURS DE L'ACTIVATION DES LYMPHOCYTES T POUR LE TRAITEMENT DE MALADIES INFLAMMATOIRES
  申请人：AMGEN INC

  公开号：WO2005009443A1

  公开（公告）日：2005-02-03

  The present invention relates to pyrimidine or pyridine carboxamides or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell activation and proliferation, arthritis, rheumatoid arthritis, psoriatic arthritis, osteoarthritis, organ transplant, acute transplant or heterograft or homograft rejection, transplantation tolerance induction, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn's disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis, colon carcinoma or thymoma in a mammal comprising administering a therapeutically-effective amount a compound as described above.

  本发明涉及嘧啶或吡啶甲酰胺或其药用可接受的盐。还包括一种治疗炎症、抑制T细胞激活和增殖、关节炎、类风湿性关节炎、银屑病关节炎、骨关节炎、器官移植、急性移植或异体移植或同种异体移植排斥、移植耐受性诱导、缺血或再灌注损伤、心肌梗死、中风、多发性硬化症、炎症性肠病，包括溃疡性结肠炎、克罗恩病、狼疮、接触超敏反应、迟发型超敏反应和谷蛋白敏感性肠病、1型糖尿病、银屑病、接触性皮炎、桥本甲状腺炎、舍格伦综合征、自身免疫性甲状腺功能亢进、阿狄森病、自身免疫多腺体病、自身免疫性脱发、恶性贫血、白癜风、自身免疫性垂体功能减退、吉兰-巴雷综合征、肾小球肾炎、血清病、荨麻疹、过敏性疾病、哮喘、花粉症、过敏性鼻炎、硬皮病、真菌病、皮肌炎、斑秃、慢性日光性皮炎、湿疹、贝赫切特病、掌跖脓疱病、脓皮病、塞扎里综合征、特应性皮炎、系统性硬化病、硬皮病、特应性皮炎、结肠癌或胸腺瘤的方法，包括施用如上所述的化合物的治疗有效量。
• CHELATE NANOEMULSION FOR MRI
  申请人：Port Marc

  公开号：US20130309176A1

  公开（公告）日：2013-11-21

  The present invention relates to an oil-in-water nanoemulsion composition for MRI, comprising: an aqueous phase, representing 70% to 90% by weight of the composition, advantageously 75% to 85% and more advantageously from 78% to 82% a lipid phase comprising an oil, representing 9.5% to 29.5% by weight of the composition, advantageously 14% to 25% and more advantageously 17% to 21%, a surfactant at the interface between the aqueous and lipid phases, the surfactant comprising at least one amphiphilic paramagnetic metal chelate and optionally an amphiphilic lipid; the total content of surfactant by weight relative to the oil being between 4% and 10% and advantageously between 5% and 8%; the total content of surfactant by weight relative to the composition being between 0.35% and 2.95% and advantageously between 0.5% and 2%; the oil comprising at least 70%, advantageously at least 80%, advantageously at least 95% by weight and especially at least 97% of saturated C6-C18, advantageously C6-C14 and more advantageously C6-C10 fatty acids.

  本发明涉及一种用于磁共振成像的油包水纳米乳液组合物，包括： 水相，表示组合物重量的70%至90%，优选75%至85%，更优选78%至82%； 脂相包括一种油，表示组合物重量的9.5%至29.5%，优选14%至25%，更优选17%至21%； 表面活性剂位于水相和脂相之间的界面上，表面活性剂包括至少一种两性磁性金属螯合物和可选的两性脂质； 相对于油的重量，表面活性剂的总含量在4%至10%之间，优选在5%至8%之间； 相对于组合物的重量，表面活性剂的总含量在0.35%至2.95%之间，优选在0.5%至2%之间； 油包括至少70%，优选至少80%，优选至少95%的饱和C6-C18，优选C6-C14，更优选C6-C10脂肪酸。
• [EN] SUBSTITUTED TRIAZOLOPYRIDINES<br/>[FR] TRIAZOLOPYRIDINES SUBSTITUÉES
  申请人：BAYER PHARMA AG

  公开号：WO2011157688A1

  公开（公告）日：2011-12-22

  The present invention relates to substituted triazolopyridine compounds of general formula (I) : in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.

  本发明涉及通式（I）的取代三唑吡啶化合物，其中R1、R2、R3、R4和R5如描述和索赔中所述，以及制备所述化合物的方法，包括所述化合物的药物组合物和组合物，用于制造用于治疗或预防细��生长、增殖和/或存活失控疾病的药物组合物以及用于制备所述化合物的中间化合物的用途。
• [EN] COMPOUNDS FOR THE TREATMENT OF CANCER<br/>[FR] COMPOSÉS POUR LE TRAITEMENT D'UN CANCER
  申请人：BAYER PHARMA AG

  公开号：WO2016091825A1

  公开（公告）日：2016-06-16

  The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, and their use for the treatment and/or prophylaxis of diseases.

  本发明涉及Mps-1激酶抑制剂的前药衍生物，以及它们在治疗和/或预防疾病中的应用。
• [EN] PROGNOSTIC BIOMARKERS FOR TTK INHIBITOR CHEMOTHERAPY<br/>[FR] BIOMARQUEURS PRONOSTIQUES POUR CHIMIOTHÉRAPIE BASÉE SUR UN INHIBITEUR DE TTK
  申请人：NETHERLANDS TRANSLATIONAL RES CENTER B V

  公开号：WO2016166255A1

  公开（公告）日：2016-10-20

  The present invention provides a method for identifying a tumor - in a human individual or in an animal - that is susceptible to treatment with a TTK inhibitor, said method comprising: a] providing a sample of a tumor; b] determining the presence of a mutated CTNNB1 gene in said tumor sample, wherein said mutation is located in exon 3 of CTNNB1 and whereby the presence of a mutated CTNNB1 gene indicates that the tumor is susceptible to treatment with a TTK inhibitor. In an alternative aspect, step b] of the above defined method is replaced by the step of determining the presence of a mutated CTNNB1 protein in said tumor sample, wherein said mutation is located in exon 3 of CTNNB1 and whereby the presence of a mutated CTNNB1 protein indicates that the tumor is susceptible to treatment with a TTK inhibitor. In a further alternative, step b] comprises determining an altered expression of a CTNNB1 regulated gene, whereby an altered expression of a CTNNB1 regulated gene indicates that the tumor is susceptible to treatment with a TTK inhibitor.

  本发明提供了一种用于识别易受TTK抑制剂治疗的人体或动物肿瘤的方法，所述方法包括：a] 提供肿瘤样本；b] 确定肿瘤样本中是否存在突变的CTNNB1基因，其中所述突变位于CTNNB1的第3外显子中，并且存在突变的CTNNB1基因表明肿瘤易受TTK抑制剂治疗。在另一种方面，上述定义方法的步骤b] 被替换为确定肿瘤样本中是否存在突变的CTNNB1蛋白，其中所述突变位于CTNNB1的第3外显子中，并且存在突变的CTNNB1蛋白表明肿瘤易受TTK抑制剂治疗。在进一步的替代方案中，步骤b] 包括确定CTNNB1调控基因的表达改变，其中CTNNB1调控基因的表达改变表明肿瘤易受TTK抑制剂治疗。