阿查斯顿 | 13074-00-5

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 中文名称: 阿查斯顿
• 中文别名: 阿扎斯丁
• 英文名称: azastene
• 英文别名: 4,4,17-trimethyl-androst-5-eno[2,3-d]isoxazol-17β-ol；4,4,17-trimethylandrosta-2,5-dieno[2,3-d]isoxazol-17β-ol；17β-Hydroxy-4,4,17α-trimethyl-Δ⁵-androsteno<2.3-d>isoxazol；(1S,2R,13R,14S,17S,18S)-2,9,9,17,18-pentamethyl-7-oxa-6-azapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,10-trien-17-ol
• CAS: 13074-00-5
• 化学式: C₂₃H₃₃NO₂
• 分子量: 355.521
• InChiKey: AXLOCHLTNQDFFS-BESJYZOMSA-N

物化性质

• 熔点：
  178.5°C
• 沸点：
  488.52°C (rough estimate)
• 密度：
  1.14

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  26
• 可旋转键数：
  0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  46.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  阿查斯顿 在 sodium methylate 作用下， 以 四氢呋喃 为溶剂， 生成 氰基甲酮
  参考文献：
  名称：

  甾体杂环。七。雄甾烷（2,3-D）异恶唑及相关化合物。

  摘要：

  DOI：

  10.1021/jm00337a001
• 作为产物：
  描述：

  4.4.17α-Trimethyl-2-hydroxymethylen-androsten-(5)-17β-ol-3-on 在 盐酸羟胺 、 sodium acetate 作用下， 以 水 、 溶剂黄146 为溶剂， 生成 阿查斯顿
  参考文献：
  名称：

  甾体杂环。七。雄甾烷（2,3-D）异恶唑及相关化合物。

  摘要：

  DOI：

  10.1021/jm00337a001

文献信息

• COMPOSITIONS AND METHODS FOR TREATMENT OF VIRAL DISEASES
  申请人：Johansen Lisa M.

  公开号：US20100009970A1

  公开（公告）日：2010-01-14

  The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.

  本发明涉及用于治疗病毒性疾病的组合物、方法和试剂盒。在某些实施方式中，病毒性疾病是由单链RNA病毒、黄病毒科病毒或肝病毒引起的。在特定实施方式中，病毒性疾病是病毒性肝炎（例如甲型肝炎、乙型肝炎、丙型肝炎、丁型肝炎、戊型肝炎），药剂或药剂组合包括舍曲林、舍曲林类似物、UK-416244或UK-416244类似物。还包括用于鉴定可用于治疗病毒性疾病的新化合物的筛选方法。
• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Methods of contraception
  申请人：BALANCE PHARMACEUTICALS, INC.

  公开号：EP1488794A2

  公开（公告）日：2004-12-22

  Compositions and methods for use in treating benign gynecological disorders, wherein an effective amount of an antiprogestational agent [e.g., progesterone (progestin, progestogen, gestagen) antagonist or progesterone synthesis inhibitor] administered over a first period of time is combined with an effective amount of a progestogen for a second period of time. The antiprogestational agent is selected from single agents or mixture thereof. The progestogen is selected from single agents or mixtures of natural or synthetic progestogens. The formulations are effective as contraceptive agents and for treatment of benign gynecological disorders including uterine fibroids, premestrual syndrome, dysfunctional uterine bleeding, polycystic ovarian syndrome and endometriosis.

  用于治疗良性妇科疾病的组合物和方法，其中在第一时间段内给药的有效量的抗孕激素[如孕酮（孕激素、孕激素原、孕激素）拮抗剂或孕酮合成抑制剂]与第二时间段内给药的有效量的孕激素结合使用。抗孕激素选自单一制剂或其混合物。孕激素选自天然或合成孕激素的单剂或混合物。这些制剂可作为避孕药和治疗良性妇科疾病，包括子宫肌瘤、经前期综合征、功能失调性子宫出血、多囊卵巢综合征和子宫内膜异位症。
• Method of controlled ovarian hyperstimulation and pharmaceutical kit for use in such method
  申请人：Pantarhei Bioscience B.V.

  公开号：EP1862182A2

  公开（公告）日：2007-12-05

  One aspect of the present invention relates to a method of controlled ovarian hyperstimulation in a mammalian female, said method comprising administration to said female of a substance having follicle stimulating hormone activity (FSH substance) in an amount effective to stimulate follicular development and of anti-P in an effective amount to prevent a premature endogenous LH-surge, followed by the administration of a meiosis and luteinisation inducing substance (ML substance) in an amount effective to stimulate resumption of meiosis and luteinisation, and of a progestogen and/or a precursor thereof in an amount effective to prevent or suppress symptoms of progesterone antagonism and/or deficiency, wherein the progestogen and/or the precursor thereof is administered within 24 hours of the first administration of the ML substance. Another aspect of the present invention relates to a pharmaceutical kit for use in a method of controlled ovarian hyperstimulation in mammalian females, said kit comprising a parenteral dosage unit containing a FSH substance, a parenteral or oral dosage unit containing an anti-P and a parenteral or oral dosage unit containing a progestogen and/or a precursor thereof.

  本发明的一个方面涉及一种哺乳动物雌性受控卵巢过度刺激的方法，所述方法包括向所述雌性施用有效量的具有卵泡刺激素活性的物质（FSH物质）以刺激卵泡发育，以及有效量的抗P物质以防止内源性LH过早飙升、随后给予有效量的减数分裂和黄体化诱导物质（ML 物质），以刺激减数分裂和黄体化的恢复，并给予有效量的孕激素和/或其前体，以预防或抑制孕酮拮抗和/或缺乏的症状，其中孕激素和/或其前体在首次给予 ML 物质后 24 小时内给予。 本发明的另一方面涉及一种用于哺乳动物雌性受控卵巢过度刺激方法的药物试剂盒，所述试剂盒包括含有FSH物质的肠外剂量单位、含有抗P的肠外或口服剂量单位和含有孕激素和/或其前体的肠外或口服剂量单位。