7-Ethylpurin | 6625-65-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: 7-Ethylpurin
• 英文别名: 8-ethyl-7(9)H-purine；8-Ethyl-9H-purine；8-ethyl-7H-purine
• CAS: 6625-65-6
• 化学式: C₇H₈N₄
• 分子量: 148.167
• InChiKey: ZMHKYXRDQNTJNL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  54.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] HINDERED DISULFIDE DRUG CONJUGATES<br/>[FR] CONJUGUÉS MÉDICAMENTEUX À PONT DISULFURE ENCOMBRÉ
  申请人：GENENTECH INC

  公开号：WO2017064675A1

  公开（公告）日：2017-04-20

  The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.

  该发明一般涉及二硫键药物偶联物，其中含有至少一个被至少一个碳氢化合物或取代碳氢化合物所取代的含硫碳原子的连接剂通过二硫键与靶向载体的半胱氨酸硫原子偶联，并且连接剂进一步与药物部分偶联。该发明进一步涉及适合通过二硫键与靶向载体偶联的活化连接剂-药物偶联物。该发明还进一步涉及制备受阻二硫键药物偶联物的方法。
• 21-Heterocyclic-4-azasteroid derivatives as androgen receptor modulators
  申请人：Dankulich P. William

  公开号：US20070088047A1

  公开（公告）日：2007-04-19

  Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive impairment, decreased libido, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

  结构式（I）的化合物以组织选择性方式调节雄激素受体（AR）。它们可作为雄激素受体在骨骼和/或肌肉组织中的激动剂，同时在男性患者的前列腺或女性患者的子宫中对抗雄激素受体。因此，这些化合物在增强肌肉张力和治疗由雄激素缺乏引起或可以通过雄激素治疗改善的疾病方面具有用途，包括骨质疏松症、骨质疏松症、糖皮质激素诱导的骨质疏松症、牙周病、骨折、骨重建手术后的骨损伤、肌肉减少症、虚弱、老化皮肤、男性睾丸功能减退、女性绝经后症状、动脉粥样硬化、高胆固醇血症、高脂血症、肥胖、再生障碍性贫血和其他造血系统疾病、炎症性关节炎和关节修复、艾滋病消耗综合征、前列腺癌、癌症消耗综合征、阿尔茨海默病、肌肉萎缩症、认知障碍、性欲减退、卵巢早衰和自身免疫疾病等疾病的治疗，可单独使用或与其他活性药物联合使用。
• 2-Substituted-6-trifluoromethyl purine derivatives with adenosine-A3 antagonistic activity
  申请人：Koch Melle

  公开号：US20060052331A1

  公开（公告）日：2006-03-09

  The present invention relates to 2-substituted-6-trifluoromethyl purine derivatives as selective adenosine antagonists, in particular adenosine-A 3 receptor antagonists, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said purine derivatives. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

  本发明涉及作为选择性腺苷拮抗剂的2-取代-6-三氟甲基嘌呤衍生物，特别是腺苷A3受体拮抗剂，以及用于制备这些化合物的方法和用于合成所述嘌呤衍生物的新型中间体。这些化合物具有一般式（1），其中符号具有规范中给定的含义。
• PROCESS FOR PREPARING [(3-HYDROXYPYRIDINE-2-CARBONYL)AMINO]ALKANOIC ACIDS, ESTERS AND AMIDES
  申请人：Akebia Therapeutics, Inc.

  公开号：US20150361043A1

  公开（公告）日：2015-12-17

  Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and [3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.

  本发明涉及制备[(3-羟基吡啶-2-羧基)氨基]-烷基酸，其衍生物，包括5-芳基取代和5-杂环芳基取代的[(3-羟基吡啶-2-羧基)氨基]乙酸。此外，还公开了制备[(3-羟基吡啶-2-羧基)氨基]乙酸的前药的方法，例如[(3-羟基吡啶-2-羧基)氨基]乙酸酯和[3-羟基吡啶-2-羧基]氨基}乙酸酰胺。所公开的化合物可用作脯氨酸羟化酶抑制剂或用于治疗需要脯氨酸羟化酶抑制的疾病。
• Shape memory polymers
  申请人：Anthamatten Mitchell L.

  公开号：US20080177303A1

  公开（公告）日：2008-07-24

  The present disclosure relates to Shape Memory Polymers (SMP's) comprising function groups that allow the polymers to be elastically deformed, utilized in the elastically deformed state, and subsequently returned to the original polymorphic shape.

  本公开涉及形状记忆聚合物（SMP），其中包含允许聚合物弹性变形的功能基团，可在弹性变形状态下使用，并随后返回到原始的多态形状。