普罗孕酮 | 23873-85-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氧环庚烷
• 中文名称: 普罗孕酮
• 英文名称: Proligestone
• 英文别名: (1R,2R,10R,11S,14S,15R)-15-acetyl-17-ethyl-10,14-dimethyl-16,18-dioxapentacyclo[13.3.2.01,14.02,11.05,10]icos-5-en-7-one
• CAS: 23873-85-0
• 化学式: C₂₄H₃₄O₄
• 分子量: 386.5
• InChiKey: MQSDUYIXZDSLSZ-QSDCUGRSSA-N

物化性质

• 熔点：
  93-94 °C
• 沸点：
  516.1±50.0 °C(Predicted)
• 密度：
  1.16±0.1 g/cm3(Predicted)
• 溶解度：
  soluble in No data available

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  28
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  52.6
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• 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。
• New process for the preparation of certain steroids, especially intermediates for the preparation of proligestone and related compounds, and new intermediates formed in this process
  申请人：AKZO N.V.

  公开号：EP0189951A1

  公开（公告）日：1986-08-06

  The invention relates to a new process for the preparation of 14-alpha-17-alpha-dihydroxy-17-beta-substituted steriods by reaction of 14-alpha-hydroxy-17-oxo-steroids with metal organic compounds. Furthermore, the invention relates to the 14-alpha-17-alpha-dihydroxy-17-beta- substituted steroids prepared by the new process and their use in the production of 14-alpha-17-alpha- methylenedioxypregnane derivatives.

  本发明涉及一种通过 14-α-羟基-17-氧代类固醇与金属有机化合物反应制备 14-α-17-α-二羟基-17-β-取代类固醇的新工艺。 此外，本发明还涉及通过新工艺制备的 14-α-17-α-二羟基-17-β-取代类固醇及其在生产 14-α-17-α-亚甲基二氧孕甾烷衍生物中的用途。
• Process for the preparation of a pharmaceutical granulate
  申请人：YAMANOUCHI EUROPE B.V.

  公开号：EP0330284A2

  公开（公告）日：1989-08-30

  A wet granulate is provided containing a therapeutically useful substance having a water solubility 10 wt% or less and microcrystalline or microfine cellulose or a mixture of both, characterised in that substantial amounts of wet binders are avoided. Tableting mixtures with the new granulate possess a good flow pattern and may be compressed to tablets which show an excellent disintegration behaviour.

  提供了一种湿颗粒剂，其中含有水溶性为 10 wt%或更低的治疗用物质和微晶或微细纤维素或二者的混合物，其特点是避免了大量湿粘合剂。 含有新颗粒的片剂混合物具有良好的流动性，可压制成片剂，并显示出极佳的崩解性能。
• Transdermal administration to humans and animals
  申请人：DERMAMED

  公开号：EP0463454A2

  公开（公告）日：1992-01-02

  A pharmaceutical composition for use in the transdermal administration of a medicament to both humans and animals, which composition comprises at least ingredients (1) and (2) of the following ingredients (1), (2) and (3), namely: (1) an effective amount of a medicament adapted for transdermal administration; (2) a transdermally transporting effective amount of a carrier for the medicament, which carrier is selected from semisolids and liquids at ambient temperatures, and which carrier comprises at least one compound selected from esters of C₈₋₂₄ fatty acids, pharmaceutically acceptable aliphatic polyhydroxy compounds and non-volatile paraffins; (3) an optional medicament selected from antiinflammatory agents and antihistamines, effective to mitigate any skin-incompatibility characteristic which may otherwise be present. Administration is preferably by means of a matrix which comprises a porous, absorbent, perforate and flexible laminar solid support, having the composition absorbed thereon. The invention includes a device for use in transdermal administration, which comprises such a matrix, preferably included in a multilayer system providing a desired controlled or sustained release pattern for said medicament; as well as apparatus for applying a medicament non-adhesively to the skin of an animal, which comprises a removable enclosure bearing such a matrix or device, the apparatus being arranged for non-invasive mounting onto an animal ear.

  一种用于人和动物透皮给药的药物组合物，该组合物至少包括以下成分(1)、(2)和(3)中的成分(1)和(2)，即：(1) 适于透皮给药的有效量的药物； (2) 透皮运输有效量的药物载体，该载体选自环境温度下的半固体和液体，该载体 包括至少一种选自 C₈₋₂₄ 脂肪酸的酯、药学上可接受的脂肪族多羟基化合物和非挥发性石蜡的化合物；(3) 可选的药物，选自消炎剂和抗组胺剂，可有效缓解可能存在的皮肤不相容特性。给药最好是通过基质进行，基质包括多孔的、可吸收的、穿孔的和柔韧的层状固体支撑物，其上可吸收组合物。本发明包括一种用于透皮给药的装置，它包括这样一种基质，最好包含在一个多层系统中，为所述药物提供所需的控制或持续释放模式；还包括用于将药物非粘附性地涂抹到动物皮肤上的装置，它包括一个可移动的外壳，外壳上有这样一种基质或装置，该装置被安排用于非侵入性地安装到动物耳朵上。
• METHOD FOR CONTROLLING SEXUAL BEHAVIOUR AND CONTRACEPTION IN FEMALE MAMMALS
  申请人：Obshchestvo S Ogranichennoj Otvetstvennost'yu "Nauchno-Vnedrencheskij Centr Agrovetzashchita"

  公开号：EP3318250A2

  公开（公告）日：2018-05-09

  The invention relates to the veterinary field in particular to a method for temporarily blocking sexual functions in female mammals, including behavioural phenomena (search for a partner, vocalization, etc.). The method for controlling sexual behaviour and contraception in female animals comprises administration of melatonin, gestagen and α-adrenergic blocking agent tropic to the posterior nuclei of the hypothalamus, while the combination of specified biologically active substances (BAS) is administered in therapeutic doses once during any period of the estrous cycle. A pharmaceutical composition for controlling sexual behaviour of female animals intended for the "Spot-on" transdermal administration, having pH in the range of 4.0 to 6.0 and containing therapeutic quantities of melatonin, gestagen and α-adrenergic blocking agent tropic to the posterior nuclei of the hypothalamus with the following ratio of the components (mass%): gestagen - therapeutic quantities; melatonin - therapeutic quantities; α-adrenergic blocking agent tropic to the posterior nuclei of the hypothalamus - therapeutic quantities; N-methyl-N-(1,2R,3R,4R,5S-pentahydroxyhexyl)-octadecanamide - 0.5; D-panthenol - 0.5; polyoxyethylated α-tocopherol - 10; polyoxyethylated lanolin - 1; 3-(octadecyloxy)-1,2-propanediol - 0.1; carboxylic acid - 0.1-1.1; N,N-diethyltoluamid - 15; 1,2-isopropylidene glycerol - 20; 1,2,3-triacetoxypropane - up to 100. The invention makes it possible, while using the minimal dose of the steroid hormone harmful to health of animals, to inhibit sexual behaviour of female animals for the period of 2 months to half a year (depending on the length of the daytime period). The pharmaceutical composition is intended for transdermal administration. The pharmaceutical composition also can be used in humane medicine for effective and safe contraception in the form of metered dose transdermal sprays for convenient application.

  本发明涉及兽医领域，特别是一种暂时阻断雌性哺乳动物性功能的方法，包括行为现象（寻找伴侣、发声等）。这种控制雌性动物性行为和避孕的方法包括在下丘脑后核施用褪黑素、孕激素和α-肾上腺素能阻断剂，同时在发情周期的任何时期以治疗剂量施用一次特定生物活性物质（BAS）组合。一种控制雌性动物性行为的药物组合物，用于 "点滴 "透皮给药，pH 值在 4.0 至 6.0，并含有治疗量的褪黑素、孕酮素和α-肾上腺素能阻断剂，其对下丘脑后核的滋养成分比例如下（质量％）：孕酮素--治疗量；褪黑素--治疗量；α-肾上腺素能阻断剂--对下丘脑后核的滋养成分--治疗量；N-甲基-N-(1,2R,3R,4R,5S-五羟基己基)-十八烷酰胺--0.5；D-泛醇--0.5；α-肾上腺素能阻断剂--对下丘脑后核的滋养成分--治疗量；N-甲基-N-(1,2R,3R,4R,5S-五羟基己基)-十八烷酰胺--0.5；D-泛醇 - 0.5；聚氧乙烯化α-生育酚 - 10；聚氧乙烯化羊毛脂 - 1；3-(十八烷氧基)-1,2-丙二醇 - 0.1；羧酸 - 0.1-1.1；N,N-二乙基甲苯酰胺 - 15；1,2-异亚丙基甘油 - 20；1,2,3-三乙酰氧基丙烷 - 高达 100。本发明可以在使用对动物健康有害的最小剂量类固醇激素的情况下，抑制雌性动物的性行为 2 个月至半年（取决于白天时间的长短）。该药物组合物用于透皮给药。该药物组合物还可用于人道医疗，以计量剂量透皮喷雾剂的形式进行有效、安全的避孕，使用方便。