[4-[(E)-1-[4-(2-二甲基氨基乙氧基)苯基]-2-(4-丙-2-基苯基)丁-1-烯基]苯基]磷酸二氢酯 | 115767-74-3

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 中文名称: [4-[(E)-1-[4-(2-二甲基氨基乙氧基)苯基]-2-(4-丙-2-基苯基)丁-1-烯基]苯基]磷酸二氢酯
• 英文名称: Miproxifene phosphate
• 英文别名: [4-[(E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-(4-propan-2-ylphenyl)but-1-enyl]phenyl] dihydrogen phosphate
• CAS: 115767-74-3
• 化学式: C₂₉H₃₆NO₅P
• 分子量: 509.6
• InChiKey: QZUHFMXJZOUZFI-ZQHSETAFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  36
• 可旋转键数：
  11
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  79.2
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  [4-[(E)-1-[4-(2-二甲基氨基乙氧基)苯基]-2-(4-丙-2-基苯基)丁-1-烯基]苯基]磷酸二氢酯 、 哌啶 生成 [4-[(E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-(4-propan-2-ylphenyl)but-1-enyl]phenyl] dipiperidin-1-yl phosphate
  参考文献：
  名称：

  ASSO, TETSUJI;TAKEDA, SETSUO;SUGIMOTO, YOSHIKAZU;TOKO, TOSHIYUKI;YAMADA, +

  摘要：

  DOI：
• 作为产物：
  描述：

  (E)-1-<4-<2-(dimethylamino)ethoxy>phenyl>-1-(4-hydroxyphenyl)-2-(4-isopropylphenyl)-1-butene hydrochloride 以43.2的产率得到[4-[(E)-1-[4-(2-二甲基氨基乙氧基)苯基]-2-(4-丙-2-基苯基)丁-1-烯基]苯基]磷酸二氢酯
  参考文献：
  名称：

  1,1,2-triaryl-1-alkene derivatives

  摘要：

  本发明提供了一种公式为##STR1##的1,1,2-三芳基-1-丁烯衍生物，其中R.sub.1和R.sub.2分别代表低碳基团，R.sub.3和R.sub.4中的一个是低碳基团，另一个是公式##STR2##的基团（其中R.sub.5是氢原子，低碳基团，低碳氧基基团，卤原子或--OPO(OH).sub.2基团）；或其药学上可接受的盐，其制备和含有该衍生物的制剂用于治疗乳腺癌和排卵障碍不孕症。

  公开号：

  US04897503A1

文献信息

• TREATMENT OF MALE ANDROGEN DEFICIENCY SYMPTOMS OR DISEASES WITH SEX STEROID PRECURSOR COMBINED WITH SERM
  申请人：Labrie Fernand

  公开号：US20150250802A1

  公开（公告）日：2015-09-10

  Novel methods for prevention, reduction or elimination of the incidence of male androgen deficiency symptoms or diseases including male hypogonadism-associated symptoms and diseases associated with low serum testosterone and/or low DHEA or low total androgens in susceptible warm-blooded animals including humans involving administration of an amount of a sex steroid precursor, particularly dehydroepiandrosterone (DHEA) and a selective estrogen receptor modulator (SERM) (particularly acolbifene), an antiestrogen or a prodrug of the two. The symptoms or diseases are loss of libido, erectile dysfunction, tiredness, loss of energy, depression, bone loss, muscle loss, muscle weakness, fat accumulation, memory loss, cognition loss, Alzheimer's disease, dementia, loss of body hair, fertility problems, insomnia, gynecomastia, anemia, hot flushes, sweats, decreased sense of well-being, obesity, osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, cardiovascular disease and type 2 diabetes. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

  预防、减少或消除男性雄激素缺乏症状或疾病的新方法，包括男性睾丸功能减退相关症状和与低血清睾酮和/或低DHEA或低总雄激素有关的疾病，涉及给予一定量的性激素前体，特别是去氢表雄酮（DHEA）和选择性雌激素受体调节剂（SERM）（特别是阿科比芬），一种抗雌激素或两者的前药。这些症状或疾病包括性欲减退、勃起功能障碍、疲劳、精力下降、抑郁、骨质流失、肌肉流失、肌肉无力、脂肪积累、记忆力减退、认知能力减退、阿尔茨海默病、痴呆、体毛减少、生育问题、失眠、男性乳房发育、贫血、潮热、出汗、幸福感降低、肥胖、骨质疏松症、高胆固醇血症、高脂血症、动脉粥样硬化、高血压、胰岛素抵抗、心血管疾病和2型糖尿病。还公开了用于给药活性成分的药物组合物和有用于该发明的工具包。
• TREATMENT OF HOT FLUSHES, VASOMOTOR SYMPTOMS, AND NIGHT SWEATS WITH SEX STEROID PRECURSORS IN COMBINATION WITH SELECTIVE ESTROGEN RECEPTOR MODULATORS
  申请人：Endorecherche, Inc.

  公开号：EP3178480A1

  公开（公告）日：2017-06-14

  Novel methods for reduction or elimination of the incidence of hot flushes, vasomotor symptoms, and night sweats while decreasing the risk of acquiring breast, uterine or endometrial cancer and furthermore having beneficial effect by inhibiting the development of osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, diabetes type 2, loss of muscle mass, adiposity, Alzheimer's disease, loss of cognition, loss of memory, or vaginal dryness in susceptible warm-blooded animals including humans involving administration of an amount of a sex steroid precursor, particularly dehydroepiandrosterone (DHEA) and an antiestrogen or a selective estrogen receptor modulator, particularly benzopyran compounds. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

  用于减少或消除潮热、血管运动症状和夜间盗汗的新方法，同时降低乳腺、子宫或子宫内膜癌症的发病风险，并通过抑制骨质疏松症、高胆固醇血症、高脂血症、动脉粥样硬化、高血压、胰岛素抵抗、2型糖尿病、肌肉流失、脂肪堆积、阿尔茨海默病、认知能力丧失、记忆力丧失或阴道干燥等疾病的发展具有益处的影响的方法，涉及给予一定量的性激素前体，特别是去氢表雄酮（DHEA）和抗雌激素或选择性雌激素受体调节剂，特别是苯并吡喃化合物。还公开了用于传递活性成分的药物组合物和有益于该发明的工具。
• COMPOSITION FOR SOLID PHARMACEUTICAL PREPARATION OF SOLIFENACIN OR SALT THEREOF
  申请人：Astellas Pharma Inc.

  公开号：EP1728791A1

  公开（公告）日：2006-12-06

  A solid pharmaceutical preparation of solifenacin or a salt thereof, the preparation being stable and inhibited from decomposing with time when supplied to clinical fields. In a pharmaceutical preparation containing solifenacin or a salt thereof, the compound in an amorphous form was revealed to be causative of cardinal-drug decomposition with time. The composition for a solid pharmaceutical preparation of solifenacin or a salt thereof contains solifenacin or its salt each in a crystalline from, and the content provided are: a process for producing the composition; and a medicinal composition for solid pharmaceutical preparations which contains solifenacin and an amorphization inhibitor.

  一种索利那新或其盐的固体药物制剂，该制剂在供应到临床领域时非常稳定，并可抑制其随时间的推移而分解。在一种含有索利那新或其盐的药物制剂中，发现无定形形式的化合物会随着时间的推移而导致主药分解。索非那新或其盐的固体药物制剂组合物含有结晶状的索非那新或其盐，所提供的内容包括：一种生产该组合物的工艺；一种用于固体药物制剂的药物组合物，其中含有索非那新和一种非晶化抑制剂。
• Composition of solifenacin or salt thereof for use in solid formulation
  申请人：Astellas Pharma Inc.

  公开号：EP2156824A1

  公开（公告）日：2010-02-24

  In a pharmaceutical preparation containing solifenacin or a salt thereof, the compound in an amorphous form was revealed to be causative of cardinal-drug decomposition with time. Thus, a solid pharmaceutical composition of solifenacin or a salt thereof is provided, which is stable and inhibited from decomposing with time when supplied to clinical fields. The composition for a solid pharmaceutical preparation of solifenacin or a salt thereof contains crystalline and amorphous solifenacin or a crystalline and amorphous salt thereof together with an amorphization inhibitor.

  在含有索利那新或其盐的药物制剂中，发现无定形形式的化合物会随着时间的推移而导致主药分解。因此，本发明提供了一种索利那新或其盐的固体药物组合物，这种组合物在供应到临床领域时是稳定的，并可抑制其随时间的推移而分解。索非那新或其盐的固体药物制剂组合物包含结晶和无定形的索非那新或其结晶和无定形盐，以及一种无定形化抑制剂。
• Treatment of Alzheimer's disease, loss of cognition, memory loss and dementia with sex steroid precursors in combination with selective estrogen receptor modulators
  申请人：Labrie Fernand

  公开号：US10342805B2

  公开（公告）日：2019-07-09

  Novel methods for reduction or elimination the incidence of hot flushes, vasomotor symptoms, and night sweats while decreasing the risk of acquiring breast, uterine or endometrial cancer and furthermore having beneficial effect by inhibiting the development of osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, diabetes type 2, loss of muscle mass, adiposity, Alzheimer's disease, loss of cognition, loss of memory, or vaginal dryness in susceptible warm-blooded animals including humans involving administration of an amount of a sex steroid precursor, particularly dehydroepiandrosterone (DHEA) and an antiestrogen or a selective estrogen receptor modulator, particularly compounds having the general structure: Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

  减少或消除潮热、血管运动症状和盗汗发生率的新方法，同时降低罹患乳腺癌、子宫癌或子宫内膜癌的风险，并通过抑制骨质疏松症、高胆固醇血症、高脂血症、动脉粥样硬化、高血压、胰岛素抵抗、2 型糖尿病、肌肉质量下降、肥胖症、老年痴呆症、认知能力下降、记忆力减退或阴道干涩等疾病的发展而产生益处、对包括人类在内的易感温血动物的肌肉质量下降、肥胖、老年痴呆症、认知能力下降、记忆力减退或阴道干涩等症状有抑制作用，其中涉及给药一定量的性类固醇前体，特别是脱氢表雄酮（DHEA）和抗雌激素或选择性雌激素受体调节剂，特别是具有一般结构的化合物： 此外，还公开了用于输送活性成分的药物组合物和对本发明有用的试剂盒。