(5-Methyl-3-(trifluoromethyl)pyridin-2-yl)methanamine | 1211534-22-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: (5-Methyl-3-(trifluoromethyl)pyridin-2-yl)methanamine
• 英文别名: [5-methyl-3-(trifluoromethyl)pyridin-2-yl]methanamine
• CAS: 1211534-22-3
• 化学式: C₈H₉F₃N₂
• 分子量: 190.17
• InChiKey: FVWCMBDLVCBIEE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  6-chloro-5-methyl-3-trifluoromethyl-pyridine-2-carbonitrile 、 氨 在 镍 氢气 、 silica gel 、 Dichloromethane methanol ammonium hydroxide 作用下， 以 甲醇 为溶剂， 反应 2.0h， 以affording C-(5-methyl-3-trifluoromethyl-pyridin-2-yl)-methylamine as a colorless oil (0.113 g, 44%)的产率得到(5-Methyl-3-(trifluoromethyl)pyridin-2-yl)methanamine
  参考文献：
  名称：

  CXCR4 chemokine receptor binding compounds

  摘要：

  本发明涉及结合趋化因子受体的化合物，其具有以下式子： 其中每个A、X、Y、R1、R2和R3均为取代基。本发明还涉及使用这种化合物的方法，例如用于治疗HIV感染和炎症性疾病，如类风湿性关节炎。此外，本发明还涉及使用这种化合物提高祖细胞和干细胞计数的方法，以及提高白细胞计数的方法。

  公开号：

  US07291631B2

文献信息

• CXCR4 chemokine receptor binding comounds
  申请人：——

  公开号：US20040209921A1

  公开（公告）日：2004-10-21

  The present invention relates to compounds that bind to chemokine receptors, and having the formula 1 wherein each A, X, Y, R 1 , R 2 and R 3 are substituents. The present invention also relates to methods of using such compounds, such as in treating HIV infection and inflammatory conditions such as rheumatoid arthritis. Furthermore, the present invention relates to methods to elevate progenitor and stem cell counts, as well as methods to elevate white blood cell counts, using such compounds.

  本发明涉及与趋化因子受体结合的化合物，其具有式1的结构，其中A、X、Y、R1、R2和R3均为取代基。本发明还涉及使用这类化合物的方法，例如在治疗HIV感染和炎症性疾病如类风湿性关节炎中的应用。此外，本发明还涉及使用这类化合物来提高祖细胞和干细胞计数的方法，以及提高白细胞计数的方法。
• [EN] SPIROINDOLINE DERIVATIVES FOR USE AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS DE SPIROINDOLINE POUR UNE UTILISATION EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE L'HORMONE DE LIBÉRATION DES GONADOTROPHINES
  申请人：BAYER PHARMA AG

  公开号：WO2014166958A1

  公开（公告）日：2014-10-16

  Spiroindoline derivatives, processes for their preparation and pharmaceutical compositions thereof, their use for the treatment of diseases, and their use for the manufacture of medicaments for the treatment of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine leiomyoma (fibroids), polycystic ovarian disease, menorrhagia, dysmenorrhea, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception, infertility and assisted reproductive therapy such as in vitro fertilization. The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.

  螺环吲哚衍生物，其制备方法及药用组合物，用于治疗疾病，并用于制造治疗疾病的药物，特别是用于治疗男性和女性的性激素相关疾病，特别是从子宫内膜异位症、子宫平滑肌瘤（纤维瘤）、多囊卵巢综合征、月经过多、经痛、多毛症、早熟、依赖性性腺类固醇的肿瘤如前列腺、乳腺和卵巢癌、促性腺激素垂体瘤、睡眠呼吸暂停、肠易激综合征、经前综合征、良性前列腺增生、避孕、不孕症和辅助生殖疗法如体外受精等疾病组中选择的疾病。本申请特别涉及螺环吲哚衍生物作为促性腺释放激素（GnRH）受体拮抗剂。
• CXCR4 CHEMOKINE RECEPTOR BINDING COMPOUNDS
  申请人：BRIDGER Gary J.

  公开号：US20080255197A1

  公开（公告）日：2008-10-16

  The present invention relates to compounds that bind to chemokine receptors, and having the formula wherein each A, X, Y, R 1 , R 2 and R 3 are substituents. The present invention also relates to methods of using such compounds, such as in treating HIV infection and inflammatory conditions such as rheumatoid arthritis. Furthermore, the present invention relates to methods to elevate progenitor and stem cell counts, as well as methods to elevate white blood cell counts, using such compounds.

  本发明涉及与趋化因子受体结合的化合物，其具有以下式子： 其中每个A、X、Y、R1、R2和R3均为取代基。本发明还涉及使用这种化合物的方法，例如用于治疗HIV感染和炎症性疾病，如类风湿性关节炎。此外，本发明还涉及使用这种化合物提高祖细胞和干细胞数量的方法，以及提高白细胞计数的方法。
• SPIROINDOLINE DERIVATIVES FOR USE AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20160052936A1

  公开（公告）日：2016-02-25

  Spiroindoline derivatives, processes for their preparation and pharmaceutical compositions thereof, their use for the treatment of diseases, and their use for the manufacture of medicaments for the treatment of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine leiomyoma (fibroids), polycystic ovarian disease, menorrhagia, dysmenorrhea, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception, infertility and assisted reproductive therapy such as in vitro fertilization. The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.

  螺内酰吲哚衍生物，其制备方法和制药组合物，用于治疗疾病，以及用于制造治疗疾病的药物，特别是针对男女性激素相关疾病，尤其是在内膜异位症、子宫肌瘤（纤维瘤）、多囊卵巢综合症、月经过多、痛经、多毛症、性早熟、性腺激素依赖性肿瘤（如前列腺癌、乳腺癌和卵巢癌）、促性腺激素垂体腺瘤、睡眠呼吸暂停、肠易激综合症、经前综合症、良性前列腺增生、避孕、不孕和辅助生殖治疗（如体外受精）。本申请特别涉及作为促性腺激素释放激素（GnRH）受体拮抗剂的螺内酰吲哚衍生物。
• US7291631B2
  申请人：——

  公开号：US7291631B2

  公开（公告）日：2007-11-06