奎孕醇 | 10592-65-1

• 物质功能分类: 原料药 - 激素及调节内分泌功能类药 - 避孕药
• 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: 奎孕醇
• 中文别名: 醋炔醚；喹孕醇
• 英文名称: Quingestanol
• 英文别名: (8R,9S,10R,13S,14S,17R)-3-cyclopentyloxy-17-ethynyl-13-methyl-2,7,8,9,10,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-ol
• CAS: 10592-65-1
• 化学式: C₂₅H₃₄O₂
• 分子量: 366.5
• InChiKey: PCJFRMOEZQQSAX-AIOSZGMZSA-N

物化性质

• 沸点：
  520.2±50.0 °C(Predicted)
• 密度：
  1.13±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  27
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.76
• 拓扑面积：
  29.5
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• 6,7-Dihydro-5H-benzo[7]annulene derivatives, processes for their preparation, pharmaceutical products comprising them and their use for preparing medicaments
  申请人：Bayer Intellectual Property GmbH

  公开号：US20150080438A1

  公开（公告）日：2015-03-19

  The invention relates to selective oestrogen receptor modulators (SERMs) and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception.

  该发明涉及选择性雌激素受体调节剂（SERMs），以及它们的制备方法，它们用于治疗和/或预防疾病的用途，以及它们用于制备用于治疗和/或预防疾病的药物，特别是用于治疗出血障碍、骨质疏松症、子宫内膜异位症、子宫肌瘤、激素依赖性肿瘤、激素替代疗法和避孕的用途。
• 6,7-DIHYDRO-5H-BENZO[7]ANNULENE DERIVATIVES, PROCESS FOR PREPARATION THEREOF, PHARMACEUTICAL PREPARATIONS COMPRISING THEM, AND THE USE THEREOF FOR PRODUCTION OF MEDICAMENTS
  申请人：Wintermantel Tim

  公开号：US20130252890A1

  公开（公告）日：2013-09-26

  The invention relates to selective oestrogen receptor modulators (SERM) and methods of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception.

  该发明涉及选择性雌激素受体调节剂（SERM）及其生产方法，以及将其用于治疗和/或预防疾病以及将其用于生产用于治疗和/或预防疾病的药物产品，特别是用于出血性疾病、骨质疏松症、子宫内膜异位症、子宫肌瘤、激素依赖性肿瘤、激素替代疗法和避孕。
• CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS FOR PROLONGED EFFECT
  申请人：Hemmingsen Pernille Hoyrup

  公开号：US20100239667A1

  公开（公告）日：2010-09-23

  Layered pharmaceutical composition suitable for oral use in the treatment of diseases where absorption takes place over a large part of the gastrointestinal tract. The composition comprising A) a solid inner layer comprising i) an active substance, and ii) one or more disintegrants/exploding agents, one of more effervescent agents or a mixture thereof. the solid inner layer being sandwiched between two outer layers B1) and B2), each outer layer comprising iii) a substantially water soluble and/or crystalline polymer or a mixture of substantially water soluble and/or crystalline polymers, the polymer being a polyglycol in the form of one of a) a homopolymer having a MW of at least about 100,000 daltons, and b) a copolymer having a MW of at least about 2,000 daltons, or a mixture thereof, and iv) an active substance, which is the same as in said solid inner layer A), and layer A being different from layer B, the layered composition being coated with a coating C) that has at least one opening exposing at least one surface of said outer layer, the coating being substantially insoluble in and impermeable to fluids and comprising a polymer, and the composition having a cylindrical form optionally with one or more tapered ends, wherein the ratio between the surface area of one end surface of the cylinder and the length of the cylinder is in a range of from 0.02 to 45 mm.

  分层制药组合物，适用于口服治疗吸收发生在胃肠道大部分的疾病。该组合物包括A) 一个固体内层，其中包括i) 一种活性物质，和ii) 一种或多种分散剂/爆炸剂，一种或多种泡腾剂或其混合物。该固体内层被夹在两个外层B1)和B2)之间，每个外层包括iii) 一种或多种水溶性和/或结晶聚合物，或者水溶性和/或结晶聚合物的混合物，聚合物为聚乙二醇，形式为a) 分子量至少为约100,000道尔顿的同聚物，和b) 分子量至少为约2,000道尔顿的共聚物，或其混合物，和iv) 一种活性物质，其与所述固体内层A)中的活性物质相同，且层A与层B不同，该分层组合物被涂覆有一种涂层C)，该涂层具有至少一个开口，暴露出至少一个外层的表面，该涂层在液体中具有相当的不溶性和不透性，包括一种聚合物，该组合物具有圆柱形状，可选地具有一个或多个锥形端部，其中圆柱体的一个端面的表面积与圆柱体的长度之比在0.02至45毫米的范围内。
• Novel kinase inhibitors
  申请人：Thormann Michael

  公开号：US20120329785A1

  公开（公告）日：2012-12-27

  The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases.

  本发明涉及式（I）的新型化合物，这些化合物能够抑制一个或多个激酶，特别是SYK（脾酪氨酸激酶）、LRRK2（富含亮氨酸重复的激酶2）和/或MYLK（肌球蛋白轻链激酶）或其突变体。这些化合物可用于治疗各种疾病。
• Means and method for hormonal contraception
  申请人：Pantarhei Bioscience B.V.

  公开号：EP1293210A1

  公开（公告）日：2003-03-19

  The present invention is concerned with a kit containing a plurality of hormone units for use in a contraceptive method which consists of two alternating consecutive phases, sometimes referred to as a sequential method or sequential regimen. More particularly the present invention relates to a kit containing a plurality of daily hormone units for use in a contraceptive method which consists of two alternating consecutive phases - an estrogenic and a progestogenic phase - of administering a sequence of said hormone units to a female of childbearing capability, the plurality of daily hormone units consisting of: a) one or more daily hormone units, for use during the estrogenic phase, containing synthetic estrogen or a combination of synthetic estrogen and biogenic estrogen in a therapeutically effective amount to inhibit ovulation and b) at least 10 daily hormone units, for use during the progestogenic phase, containing a combination of biogenic estrogen and progestogen in a therapeutically effective amount to inhibit ovulation and to transform the endometrium from a proliferative into a secretory state.

  本发明涉及一种含有多个激素单位的试剂盒，用于由两个交替连续阶段组成的避孕方法，有时也称为连续方法或连续方案。更具体地说，本发明涉及一种含有多个日用激素单位的试剂盒，用于一种避孕方法，该方法包括两个交替连续的阶段--雌激素阶段和孕激素阶段--向有生育能力的女性施用所述激素单位的序列，所述多个日用激素单位包括： a) 一个或多个日用激素单位，用于雌激素阶段，含有治疗有效量的合成雌激素或合成雌激素和生物雌激素的组合，以抑制排卵，以及 b) 至少 10 个日用激素单位，用于孕激素阶段，含有治疗有效量的生物雌激素和孕激素的组合，以抑制排卵并使子宫内膜从增殖状态转变为分泌状态。