2-[7-(4-Bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino]-butan-1-ol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯
• 英文名称: 2-[7-(4-Bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino]-butan-1-ol
• 英文别名: 2-[[7-(4-Bromo-2,6-dimethylphenyl)-2,5-dimethylpyrrolo[2,3-d]pyrimidin-4-yl]amino]butan-1-ol
• 化学式: C₂₀H₂₅BrN₄O
• 分子量: 417.349
• InChiKey: MWCVMXXJBJFLBV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  63
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• New uses for corticotropin releasing factor (CRF) antagonists
  申请人：PFIZER INC.

  公开号：EP0773023A1

  公开（公告）日：1997-05-14

  A method of treating, preventing or inhibiting a disorder selected from the group consisting of cardiovascular or heart related diseases such as stroke, hypertension, tachycardia, and congestive heart failure, osteoporosis, premature birth, psychosocial dwarfism, stress-induced fever, ulcer, diarrhea, post-operative ileus, and colonic hypersensitivity associated with psychopathological disturbance and stress, comprising administering to a mammal, including a human, in need of such treatment a therapeutically effective amount of a compound of the formula    or a pharmaceutically acceptable salt thereof, wherein A, B, D, E, Y, Z, R3, R4, and R5 are as defined herein.

  一种治疗、预防或抑制心血管或心脏相关疾病（如中风、高血压、心动过速和充血性心力衰竭）、骨质疏松症、早产、心理社交侏儒症、压力诱发发热、溃疡、腹泻、术后肠梗阻和与心理病理障碍和压力相关的结肠过敏反应的方法，包括向需要此类治疗的哺乳动物（包括人类）中，给予化合物的治疗有效量，该化合物的结构式如下：其中A、B、D、E、Y、Z、R3、R4和R5的定义如本文所述，或其药学上可接受的盐。
• New uses for corticotropin releasing factor antagonists
  申请人：——

  公开号：US20010000340A1

  公开（公告）日：2001-04-19

  A method of treating, preventing or inhibiting a disorder selected from the group consisting of cardiovascular or heart related diseases such as stroke, hypertension, tachycardia, and congestive heart failure, osteoporosis, premature birth, psychosocial dwarfism, stress-induced fever, ulcer, diarrhea, post-operative ileus, and colonic hypersensitivity associated with psychopathological disturbance and stress, comprising administering to a mammal, including a human, in need of such treatment a therapeutically effective amount of a compound of the formula 1 or pharmaceutically acceptable salt thereof, wherein A, B, D, E, Y, Z, R 3 , R 4 , and R 5 are as defined herein.

  一种治疗、预防或抑制选自心血管或心脏相关疾病（如中风、高血压、心动过速和充血性心力衰竭）、骨质疏松症、早产、心理社交侏儒症、应激性发热、溃疡、腹泻、术后肠梗阻和与心理病理障碍和应激有关的结肠过敏反应的方法，包括向需要该治疗的哺乳动物，包括人类，投与化合物1或其药学上可接受的盐的治疗有效量，其中A、B、D、E、Y、Z、R3、R4和R5如本文所定义。
• Methods of administering CRF antagonists
  申请人：PFIZER INC.

  公开号：EP0691128A1

  公开（公告）日：1996-01-10

  Substituted pyrrazoles of the formula pyrazoles and pyzazolopyrimidines of the formula compounds of the formula and pyrrolopyzimidines of the formula have corticotropin-releasing factor antagonist activity and as such are of use in the treatment of a variety of stress-related disorders.

  式中的取代吡唑 式中的吡唑和哒唑嘧啶 式中的化合物 和式中的吡咯并嘧啶类化合物 具有促肾上腺皮质激素释放因子拮抗剂活性，因此可用于治疗各种与压力有关的疾病。
• Pyrazolopyrimidines and pyrrolopyrimidines for treatment of neuronal and other disorders
  申请人：PFIZER INC.

  公开号：EP0729758A2

  公开（公告）日：1996-09-04

  Pyrazolopyrimidines and pyrrolopyrimidines of the general formula wherein A, X, R3, R4 and R5 are defined in the application, and pharmaceutically acceptable salts of such compounds, are useful in the treatment or prevention of certain neuronal and other disorders.

  通式如下的吡唑并嘧啶和吡咯并嘧啶 其中 A、X、R3、R4 和 R5 的定义见本申请，此类化合物及其药学上可接受的盐类可用于治疗或预防某些神经元疾病和其他疾病。
• Basic drug compositions with enhanced bioavailability
  申请人：Pfizer Products Inc.

  公开号：EP1027885A2

  公开（公告）日：2000-08-16

  A composition comprising a basic drug, a drug which forms a zwitterion, or a salt of either entity, admixed with a polymer selected from hydroxypropylmethylcellulose acetate succinate (HPMCAS), cellulose acetate trimellitate (CAT), cellulose acetate phthalate (CAP), hydroxypropylcellulose acetate phthalate (HPCAP), hydroxypropylmethyl-cellulose acetate phthalate (HPMCAP), and methylcellulose acetate phthalate (MCAP). The compositions having improved solubility, hence bioavailability, in the small intestine; Processes for testing such compositions, and methods of using such compositions. The compositions comprise the basic drug, zwitterion, or salt and one or more of the aforementioned polymers. The invention further relates to a method for increasing the bioavailability of a basic or a zwitterionic drug comprising co-administering the basic drug, the zwitterionic drug, or the salt, with one or more of the aforementioned polymers.

  一种组合物，包括一种碱性药物、一种形成齐聚物的药物或其中一种的盐，与一种选自羟丙基甲基纤维素醋酸琥珀酸酯（HPMCAS）的聚合物混合、邻苯二甲酸醋酸纤维素（CAP）、邻苯二甲酸羟丙基纤维素（HPCAP）、邻苯二甲酸羟丙基甲基纤维素 （HPMCAP）和邻苯二甲酸甲基纤维素（MCAP）。这些组合物在小肠中的溶解度有所提高，因此生物利用率也有所提高；测试此类组合物的工艺以及使用此类组合物的方法。这些组合物包括基本药物、齐聚物或盐以及一种或多种上述聚合物。本发明还涉及一种提高碱性药物或齐聚物生物利用度的方法，包括将碱性药物、齐聚物或盐与一种或多种上述聚合物共同给药。