(S,S)-formoterol | 73573-87-2

• 物质功能分类: 原料药 - 呼吸系统用药 - 平喘药
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (S,S)-formoterol
• 英文别名: (+)-Formoterol；N-[2-hydroxy-5-[(1S)-1-hydroxy-2-[[(2S)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]phenyl]formamide
• CAS: 73573-87-2
• 化学式: C₁₉H₂₄N₂O₄
• 分子量: 344.411
• InChiKey: BPZSYCZIITTYBL-ORAYPTAESA-N

物化性质

• 沸点：
  603.2±55.0 °C(Predicted)
• 密度：
  1.233±0.06 g/cm3(Predicted)
• 溶解度：
  在DMSO中的溶解度为20 mg/mL
• 蒸汽压力：
  5.0X10-14 mm Hg at 25 °C /Estimated/

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  25
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  90.8
• 氢给体数：
  4
• 氢受体数：
  5

ADMET

代谢

Formoterol主要通过直接在酚羟基或脂肪族羟基上进行葡萄糖苷酸化以及O-去甲基化随后在酚羟基上进行葡萄糖苷酸化代谢。次要途径涉及Formoterol的硫酸盐结合和去甲基化随后进行硫酸盐结合。最突出的途径涉及在酚羟基上的直接结合。第二个主要途径涉及O-去甲基化随后在酚的2'-羟基上进行结合。四种细胞色素P450同种物（CYP2D6、CYP2C19、CYP2C9和CYP2A6）参与Formoterol的O-去甲基化。Formoterol在治疗相关浓度下并未抑制CYP450酶。一些患者可能缺乏CYP2D6或2C19或两者兼有。尚未充分探讨这些同种物中一个或两个缺乏是否会导致Formoterol的系统暴露增加或系统不良反应。

Formoterol is metabolized primarily by direct glucuronidation at either the phenolic or aliphatic hydroxyl group and O-demethylation followed by glucuronide conjugation at either phenolic hydroxyl groups. Minor pathways involve sulfate conjugation of formoterol and deformylation followed by sulfate conjugation. The most prominent pathway involves direct conjugation at the phenolic hydroxyl group. The second major pathway involves O-demethylation followed by conjugation at the phenolic 2'-hydroxyl group. Four cytochrome P450 isozymes (CYP2D6, CYP2C19, CYP2C9 and CYP2A6) are involved in the O-demethylation of formoterol. Formoterol did not inhibit CYP450 enzymes at therapeutically relevant concentrations. Some patients may be deficient in CYP2D6 or 2C19 or both. Whether a deficiency in one or both of these isozymes results in elevated systemic exposure to formoterol or systemic adverse effects has not been adequately explored.

来源:Hazardous Substances Data Bank (HSDB)

代谢

福莫特罗被结合成了无活性的葡萄糖苷酸和一种之前未识别的硫酸盐。尿液中福莫特罗的主要代谢物是其酚葡萄糖苷酸。福莫特罗还发生了O-去甲基化和去甲酰化。这些具有药理活性的代谢物在血浆中的暴露量很低。O-去甲基化的福莫特罗主要以无活性的葡萄糖苷酸结合物形式存在，而去甲酰化的福莫特罗仅以无活性的硫酸盐结合物形式存在。完整的福莫特罗和O-去甲基化的福莫特罗在粪便中是主要的回收物质。未识别代谢物的平均回收率在尿液中为7.0%，在粪便中为2.0%。

Formoterol was conjugated to inactive glucuronides and a previously unidentified sulfate. The phenol glucuronide of formoterol was the main metabolite in urine. Formoterol was also O-demethylated and deformylated. Plasma exposure to these pharmacologically active metabolites was low. O-demethylated formoterol was seen mainly as inactive glucuronide conjugates and deformylated formoterol only as an inactive sulfate conjugate. Intact formoterol and O-demethylated formoterol dominated recovery in feces. Mean recovery of unidentified metabolites was 7. 0% in urine and 2.0% in feces.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 在妊娠和哺乳期间的影响

母乳喂养期间使用的总结：尽管没有关于在哺乳期间通过吸入器使用福莫特罗的已发表数据，但相关药物特布他林的数据表明，预计只有很少量会被分泌到母乳中。几篇综述的作者和一个专家小组一致认为，在哺乳期间使用吸入型支气管扩张剂是可以接受的，因为使用后生物利用度低，母体血清水平也低。 ◉ 对哺乳婴儿的影响：截至修订日期，没有找到相关的已发表信息。 ◉ 对泌乳和母乳的影响：截至修订日期，没有找到相关的已发表信息。

◉ Summary of Use during Lactation:Although no published data exist on the use of formoterol by inhaler during lactation, data from the related drug, terbutaline, indicate that very little is expected to be excreted into breastmilk. The authors of several reviews and an expert panel agree that use of inhaled bronchodilators is acceptable during breastfeeding because of the low bioavailability and maternal serum levels after use. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.

来源:Drugs and Lactation Database (LactMed)

毒理性

• 在妊娠和哺乳期间的影响

◈ 什么是福莫特罗？ 福莫特罗（也称为eformoterol）是一种用于治疗哮喘和慢性阻塞性肺病（COPD）的药物。它属于长效β2-激动剂类药物。β2-激动剂是支气管扩张剂。支气管扩张剂有助于打开肺部的气道。福莫特罗通过吸入（呼吸进入）来服用。它通常与吸入性皮质类固醇联合用于哮喘治疗。有关吸入性皮质类固醇的信息，请参见MotherToBaby事实表，网址为https://mothertobaby.org/fact-sheets/inhaled-corticosteroids-icss-pregnancy/pdf/。福莫特罗存在于一些复方药物中，如Symbicort®和Dulera®。 ◈ 我服用福莫特罗。它会让我更难怀孕吗？ 尚未进行福莫特罗是否会使女性更难怀孕的研究。 ◈ 我刚刚发现自己怀孕了。我应该停止使用我的福莫特罗吸入器吗？ 在更改任何药物之前，请与您的医疗保健提供者交谈。在怀孕期间控制哮喘症状的好处很重要。未经治疗的哮喘会增加孕妇和婴儿并发症的风险。有关哮喘的更多信息，请参见MotherToBaby事实表，网址为https://mothertobaby.org/fact-sheets/asthma-and-pregnancy/pdf/。如果女性在怀孕前哮喘症状通过福莫特罗得到良好控制，如果需要，在怀孕期间继续使用被认为是适当的。当福莫特罗被吸入时，药物进入血液的量非常有限，甚至更少的药物被认为会到达发育中的婴儿。 ◈ 服用福莫特罗会增加流产的风险吗？ 任何怀孕都可能导致流产。没有发表的研究探讨福莫特罗是否会增加流产的风险。 ◈ 服用福莫特罗会增加出生缺陷的风险吗？ 在每次怀孕中，女性开始时就有3-5%的几率生下有出生缺陷的婴儿。这被称为她的背景风险。关于怀孕期间使用福莫特罗的数据有限。案例报告的信息并未表明增加伤害的风险。一项关于长效β2-激动剂（LABA）使用的研究报告称，在第一季度使用时，心脏缺陷的风险增加。然而，由于孕妇的基础疾病和哮喘症状的严重程度可能影响了结果，这些结果并不确定。虽然需要更多关于福莫特罗的数据，但在需要治疗时，它通常与吸入性皮质类固醇联合在怀孕期间使用。 ◈ 怀孕期间服用福莫特罗会引起其他怀孕并发症吗？ 一份报告描述了33名在怀孕期间使用福莫特罗的女性中有5例在37周之前分娩（早产）。由于背景风险，预计会有3例早产。另一项研究比较了162例暴露于福莫特罗的怀孕与另一种长效β激动剂，并未发现出生体重、胎龄或早产风险方面的差异。怀孕期间使用福莫特罗不太可能增加早产的风险。早产与怀孕中未控制或更严重的哮喘之间可能存在关系。 ◈ 怀孕期间服用福莫特罗会导致婴儿在行为或学习上长期有问题吗？ 关于福莫特罗的研究还不够，无法知道是否存在长期问题的风险。 ◈ 我可以在哺乳期间服用福莫特罗吗？ 尚未有研究关于女性在哺乳期间服用福莫特罗的情况。关于相关药物的使用信息表明，使用福莫特罗吸入器不太可能导致女性血液中的水平足够高，从而大量进入母乳。吸入型支气管扩张剂通常被认为在哺乳期间使用是可以接受的。请务必与您的医疗保健提供者讨论所有关于哺乳的问题。 ◈ 如果男性服用福莫特罗，会影响他的生育能力（使伴侣怀孕的能力）或增加出生缺陷的风险吗？ 没有数据表明男性在受孕时使用福莫特罗会增加不育或出生缺陷的风险。一般来说，父亲接触的暴露不太可能增加怀孕的风险。更多信息，请参见MotherToBaby事实表《父亲暴露与怀孕》，网址为https://mothertobaby.org/fact-sheets/paternal-exposures-pregnancy/pdf/。

◈ What is formoterol? Formoterol (also called eformoterol) is a medication used for the treatment of asthma and chronic obstructive pulmonary disease (COPD). It is in a class of medications called long-acting beta2-agonists. Beta2-agonists are bronchodilators. Bronchodilators help to open the airways in the lungs. Formoterol is taken by inhalation (breathing it in). It is usually used in combination with an inhaled corticosteroid for asthma treatment. For information about inhaled corticosteroids, see the MotherToBaby fact sheet at https://mothertobaby.org/fact-sheets/inhaled-corticosteroids-icss-pregnancy/pdf/. Formoterol can be found in some combination medications such as Symbicort® and Dulera®. ◈ I take formoterol. Can it make it harder for me to get pregnant? Studies have not been done to see if formoterol could make it harder for a woman to get pregnant. ◈ I just found out that I am pregnant. Should I stop using my formoterol inhaler? Talk with your healthcare providers before making any changes to your medication(s). It is important to consider the benefits of controlling asthma symptoms during pregnancy. Untreated asthma increases the chance for complications for both the pregnant woman and the baby. For more information about asthma, please see the MotherToBaby fact sheet at https://mothertobaby.org/fact-sheets/asthma-and-pregnancy/pdf/.If a woman’s asthma is well-controlled with formoterol prior to pregnancy, it is considered appropriate to continue its use during pregnancy if needed. When formoterol is inhaled, very limited amounts of the drug enter the blood, and even less is thought to reach the developing baby. ◈ Does taking formoterol increase the chance for miscarriage? Miscarriage can occur in any pregnancy. There are no published studies looking at whether formoterol increases the chance of miscarriage. ◈ Can taking formoterol increase the chance of birth defects? In every pregnancy, a woman starts out with a 3-5% chance of having a baby with a birth defect. This is called her background risk.There is limited data on the use of formoterol during pregnancy. The information from case reports did not suggest an increased chance of harm. A study on the use of long acting beta2-agonists (LABA) reported an increased chance for heart defects when used in the first trimester. However, these results are not conclusive since the pregnant woman’s underlying condition and severity of her asthma symptoms could have influenced the results. While more data is needed on formoterol, it is commonly used during pregnancy in combination with inhaled corticosteroids when asthma symptoms are severe enough to require treatment. ◈ Can taking formoterol during pregnancy cause other pregnancy complications? One report of 33 women who used formoterol during pregnancy described five cases of birth before 37 weeks of pregnancy (preterm delivery). Three cases of preterm delivery would be expected due to the background risk. Another study compared 162 formoterol-exposed pregnancies to another long acting beta agonist and did not find a difference in birth weight, gestational age or chance of preterm delivery. It is unlikely that the chance for preterm delivery was increased by the use of formoterol during pregnancy. There may be a relationship between preterm delivery and poorly controlled or more severe asthma in pregnancy. ◈ Does taking formoterol in pregnancy cause long-term problems in behavior or learning for the baby? There are not enough studies on formoterol to know whether there is a chance for long-term problems. ◈ Can I take formoterol while breastfeeding? There have not been any studies on women taking formoterol while breastfeeding. Information on the use of related medications suggest that the use of a formoterol inhaler would be unlikely to result in high enough levels in the woman’s bloodstream to pass into breast milk in large amounts. Inhaled bronchodilators are generally considered acceptable for use during breastfeeding. Be sure to talk to your healthcare provider about all of your breastfeeding questions. ◈ If a man takes formoterol, could it affect his fertility (ability to get partner pregnant) or increase the chance of birth defects? There are no data to suggest a man’s use of formoterol at the time of conception increases the chance for infertility or birth defects. In general, exposures that fathers have are unlikely to increase risks to a pregnancy. For more information, please see the MotherToBaby fact sheet Paternal Exposures at https://mothertobaby.org/fact-sheets/paternal-exposures-pregnancy/pdf/.

来源:Mother To Baby Fact Sheets

毒理性

• 相互作用

与单胺氧化酶抑制剂（包括呋喃唑啉和丙卡巴肼）的伴随治疗可能会延长QTc间期并增加室性心律失常的风险；可能会增加高血压反应的机会。

Concomitant treatment /with monoamine oxidase inhibitors, including furazolidine and procarbazine/ may prolong the QTc interval and increase the risk of ventricular arrhythmias; may increase chance of hypertensive reactions.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

可能会增加接受卤代烃类麻醉药物患者的心律失常风险。

May increase risk of arrhythmias in patients receiving halogenated hydrocarbon anesthesia.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

与三环类抗抑郁药、双异丙酰胺、吩噻嗪类、普鲁卡因酰胺或奎尼丁并用的治疗可能会延长QTc间期并增加室性心律失常的风险。

Concomitant treatment /with tricyclic antidepressants, disopyramide, phenothiazines, procainamide or quinidine/may prolong the QTc interval and increase the risk of ventricular arrhythmias.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

蛋白质结合：中等，61-64%。在5至500 ng/mL的浓度范围内，血清白蛋白结合率为31%至38%。

Protein binding: Moderate 61-64%. Serum albumin binding was 31% to 38% over a range of 5 to 500 ng/mL.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

生物利用度：肺：21-37%；总体系统性：46%。

Bioavailability: Pulmonary: 21-37%; Total systemic: 46%.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

尚不清楚福莫特罗是否分布在人乳中。但是，在大鼠口服给药后，它确实会分布在大鼠乳中。

It is not known whether formoterol is distributed in human breast milk. However, it is distributed in rat milk after oral administration.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在哮喘患者中，服用12或24微克剂量后，分别有10%和15至18%的药物以原形从尿液中排出。在慢性阻塞性肺病（COPD）患者中，服用12或24微克剂量后，分别有7%和6至9%的药物以原形从尿液中排出。

In asthma patients following a 12 or 24 ug dose: 10% and 15 to 18% excreted unchanged in the urine, respectively. In chronic obstructive pulmonary disease (COPD) patients following a 12 or 24 ug dose: 7% and 6 to 9% excreted unchanged in the urine; respectively.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• WGK Germany：
  3
• 海关编码：
  2924299090

SDS

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Section 1. Chemical Product and Company Identification
Formoterol
Common Name/
Trade Name
Formoterol

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Section 4. First Aid Measures
Eye Contact Check for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water for at
least 15 minutes. Get medical attention if irritation occurs.
Skin Contact Wash with soap and water. Cover the irritated skin with an emollient. Get medical attention if irritation develops.
Serious Skin Contact Not available.
Inhalation If inhaled, remove to fresh air. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get
medical attention.
Serious Inhalation Not available.
Ingestion Do NOT induce vomiting unless directed to do so by medical personnel. Never give anything by mouth to an
unconscious person. If large quantities of this material are swallowed, call a physician immediately. Loosen tight
clothing such as a collar, tie, belt or waistband.
Serious Ingestion Not available.

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Section 5. Fire and Explosion Data
Flammability of the Product May be combustible at high temperature.
Auto-Ignition Temperature Not available.
Flash Points Not available.
Flammable Limits Not available.
Products of Combustion These products are carbon oxides (CO, CO2), nitrogen oxides (NO, NO2...).
Fire Hazards in Presence of Slightly flammable to flammable in presence of heat.
Various Substances
Explosion Hazards in Presence Risks of explosion of the product in presence of mechanical impact: Not available.
Slightly explosive in presence of open flames and sparks.
of Various Substances
SMALL FIRE: Use DRY chemical powder.
Fire Fighting Media
and Instructions LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
As with most organic solids, fire is possible at elevated temperatures
Special Remarks on
Fire Hazards
Special Remarks on Explosion Fine dust dispersed in air in sufficient concentrations, and in the presence of an ignition source is a potential dust
Hazards explosion hazard.

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Section 6. Accidental Release Measures
Small Spill Use appropriate tools to put the spilled solid in a convenient waste disposal container. Finish cleaning by
spreading water on the contaminated surface and dispose of according to local and regional authority
requirements.
Large Spill Use a shovel to put the material into a convenient waste disposal container. Finish cleaning by spreading water
on the contaminated surface and allow to evacuate through the sanitary system.
Formoterol

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Section 7. Handling and Storage
Precautions Keep away from heat. Keep away from sources of ignition. Ground all equipment containing material. Do not
breathe dust. Keep away from incompatibles such as oxidizing agents.
Storage Keep container tightly closed. Keep container in a cool, well-ventilated area.

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Section 8. Exposure Controls/Personal Protection
Engineering Controls Use process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below
recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep exposure to
airborne contaminants below the exposure limit.
Personal Protection
Safety glasses. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent. Gloves.
Personal Protection in Case of Splash goggles. Full suit. Dust respirator. Boots. Gloves. A self contained breathing apparatus should be used
a Large Spill to avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a specialist
BEFORE handling this product.
Exposure Limits Not available.

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Section 9. Physical and Chemical Properties
Physical state and appearance Solid. (Powdered solid.) Odor Not available.
Taste Not available.
Molecular Weight 344.41 g/mole
Color White to yellowish.
pH (1% soln/water) Not applicable.
Boiling Point Not available.
Melting Point Not available.
Critical Temperature Not available.
Not available.
Specific Gravity
Vapor Pressure Not applicable.
Vapor Density Not available.
Volatility Not available.
Odor Threshold Not available.
Not available.
Water/Oil Dist. Coeff.
Ionicity (in Water) Not available.
Not available.
Dispersion Properties
Solubility Insoluble in cold water.
Soluble in Dimethyl Sulfoxide (DMSO). The solubility in DMSO is 20 mg/ml

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Section 10. Stability and Reactivity Data
Stability The product is stable.
Instability Temperature Not available.
Conditions of Instability Not available.
Incompatibility with various Reactive with oxidizing agents.
substances
Corrosivity Not available.
Formoterol
Not available.
Special Remarks on
Reactivity
Not available.
Special Remarks on
Corrosivity
Polymerization Will not occur.

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Section 11. Toxicological Information
Routes of Entry Inhalation. Ingestion.
Toxicity to Animals LD50: Not available.
LC50: Not available.
Chronic Effects on Humans May cause damage to the following organs: cardiovascular system, upper respiratory tract.
Other Toxic Effects on
Slightly hazardous in case of skin contact (irritant), of ingestion, of inhalation.
Humans
Special Remarks on Not available.
Toxicity to Animals
Special Remarks on Not available.
Chronic Effects on Humans
Special Remarks on other Acute Potential Health Effects:
Toxic Effects on Humans Skin: May cause skin irritation.
Eyes: May cause eye irritation.
Inhalation: May cause respiratory tract irritation, dry mouth, nausea. May affect cardiovascular system(angina,
arrhythmias, hypertension, hypotension, palpitations, tachydcardia), respiration (may lead to paradoxical
bronchospasm). It may also affect behavior/central nervous system (dizziness, fatigue, headache, tremors,
insomnia, malaise, nervousness), metabolism (hyperglycemia, metabolic acidosis. May cause allergic reaction
(anaphylaxis)
Ingestion: May cause dry mouth, nausea. It is expected to be a low hazard during usual industrial handling.
Chronic Potential Health Effects:
Inhalation: Prolonged or repeated overexposure by inhalation may affect respiration (bronchiolar dilation,
paradoxical bronchospasm), cardiovascular system (increased pulse rate and other symptoms similar to acute
inhalation). It may cause allergic reaction (anaphylaxis).
Medical Conditions Aggravated by Exposure: Hypersensitivity to material, acute attack of asthma, cardiovascular
disease (including agina, hypertension), Diabetes, Glaucoma, Hyperthyroidism, Pheochromocytoma.

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Section 12. Ecological Information
Not available.
Ecotoxicity
BOD5 and COD Not available.
Products of Biodegradation Possibly hazardous short term degradation products are not likely. However, long term degradation products may
arise.
The product itself and its products of degradation are not toxic.
Toxicity of the Products
of Biodegradation
Special Remarks on the Not available.
Products of Biodegradation

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Section 13. Disposal Considerations
Waste Disposal Waste must be disposed of in accordance with federal, state and local environmental
control regulations.
Formoterol

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Section 14. Transport Information
DOT Classification Not a DOT controlled material (United States).
Identification Not applicable.
Not applicable.
Special Provisions for
Transport
DOT (Pictograms)

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Section 15. Other Regulatory Information and Pictograms
No products were found.
Federal and State
Regulations
California California prop. 65: This product contains the following ingredients for which the State of California has found
to cause cancer which would require a warning under the statute: No products were found.
Proposition 65
Warnings
California prop. 65: This product contains the following ingredients for which the State of California has found
to cause birth defects which would require a warning under the statute: No products were found.
Other Regulations Not available.
Other Classifications WHMIS (Canada) Not controlled under WHMIS (Canada).
DSCL (EEC) This product is not classified according Not applicable.
to the EU regulations.
Health Hazard
HMIS (U.S.A.) 1 National Fire Protection
1 Flammability
1 Association (U.S.A.)
Fire Hazard
1 0 Reactivity
Health
Reactivity
0
Specific hazard
Personal Protection
E
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
TDG (Canada)
(Pictograms)
ADR (Europe)
(Pictograms)
Formoterol
Protective Equipment
Gloves.
Lab coat.
Dust respirator. Be sure to use an
approved/certified respirator or
equivalent.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

该药物对支气管哮喘、慢性喘息性支气管炎及肺气肿等气道阻塞性疾病引起的呼吸困难具有缓解作用。由于其长效特性，主要用于维持治疗和预防发作，特别适合夜间哮喘发作的患者，并能有效预防运动诱发的哮喘发作。

反应信息

• 作为反应物：
  描述：

  (S,S)-formoterol 、 孟鲁司特 以 正己烷 、 乙酸乙酯 为溶剂， 反应 16.0h， 以80%的产率得到N-(2-(3-formamido-4-hydroxyphenyl)-2-hydroxyethyl)-1-(4-methoxyphenyl)propan-2-aminium 2-(1-(((1-(3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propyl)thio)methyl)cyclopropyl)acetate
  参考文献：
  名称：

  [EN] MONTELUKAST SALTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
  [FR] SELS DE MONTÉLUKAST ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT

  摘要：

  本发明涉及蒙特卢卡斯特盐与β2肾上腺素激动剂，含有它们的制药组合物以及在治疗呼吸道炎症病理、阻塞性病理和致敏原引起的气道功能障碍中使用它们的用途。本发明还涉及制备上述盐的过程。

  公开号：

  WO2020245358A1
• 作为产物：
  描述：

  甲酰胺,N-[5-[(1R)-1-羟基-2-[[(1R)-1-甲基-2-(4-甲氧苯基)乙基](苯基甲基)氨基]乙基]-2-(苯基甲氧基)苯基]- 在 palladium over charcoal 氢气 作用下， 以 甲醇 、 乙酸乙酯 为溶剂， 生成 (S,S)-formoterol
  参考文献：
  名称：

  WO2008/35380

  摘要：

  公开号：

文献信息

• [EN] COMPOSITIONS AND METHODS OF REGULATING CANCER RELATED DISORDERS AND DISEASES<br/>[FR] COMPOSITIONS ET MÉTHODES DE RÉGULATION DE TROUBLES ET MALADIES ASSOCIÉS AU CANCER
  申请人：ONCO THERAPIES LLC

  公开号：WO2017070052A1

  公开（公告）日：2017-04-27

  Provided herein are naphthylic derivative compounds, or pharmaceutically acceptable salts thereof, that are useful for inhibiting cancers. Also provided herein are methods of using effective amounts of said compounds, optionally with pharmaceutical carriers, for the treatment of cancers within human subjects.

  本文提供了萘基衍生物化合物或其药用盐，用于抑制癌症。本文还提供了使用有效量的该化合物的方法，可选地与药用载体一起，用于治疗人体内的癌症。
• Bronchodilating compositions and methods
  申请人：Dey L.P.

  公开号：US20020151597A1

  公开（公告）日：2002-10-17

  Bronchodilating compositions and methods are provided. The compositions are intended for administration as a nebulized aerosol. In certain embodiments, the compositions contain formoterol, or a derivative thereof. Methods for treatment, prevention, or amelioration of one or more symptoms of bronchoconstrictive disorders using the compositions provided herein are also provided.

  提供支气管扩张剂组合物和方法。这些组合物旨在作为雾化气溶胶进行管理。在某些实施例中，这些组合物含有福莫特罗或其衍生物。还提供使用此处提供的组合物治疗、预防或改善支气管收缩性疾病的一个或多个症状的方法。
• NMR characterisation of structure in solvates and polymorphs of formoterol fumarate
  作者：David C. Apperley、A. Fraser Markwell、Robin K. Harris、Paul Hodgkinson

  DOI：10.1002/mrc.3862

  日期：2012.10

  The solid-state structures of two polymorphs and two alcoholates (ethanol and isopropanol) of formoterol fumarate have been investigated by a combination of NMR techniques. First-principles shielding computations are combined with NMR data to successfully relate peaks to their crystallographic positions for the solvates, including atoms that are in equivalent molecular positions. The uncharacterised

  富马酸福莫特罗的两种多晶型物和两种醇化物（乙醇和异丙醇）的固态结构已通过NMR技术进行了研究。第一性原理的屏蔽计算与NMR数据相结合，成功地将峰与溶剂化物的晶体学位置相关联，包括处于等效分子位置的原子。发现无溶剂化物形式C的未表征结构在其不对称单元中包含单个福莫特罗离子和半个富马酸酯离子。乙醇化物和C型的HETCOR实验可以确定质子的化学位移，并可以提高前一种化合物的（13）C拆分度。在NMR实验的条件下监测了溶剂合物形成C的溶剂化。以不同形式观察到亚苯基环翻转的不同速率。碳13弛豫时间和（2）H NMR用于探测富马酸根离子的动力学。
• Active agent delivery systems and methods for protecting and administering active agents
  申请人：Mickle Travis

  公开号：US20070232529A1

  公开（公告）日：2007-10-04

  The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

  本发明涉及活性物质输送系统，更具体地涉及包含氨基酸（作为单个氨基酸或肽）与活性物质共价连接的组合物以及用于给予共轭活性物质组合物的方法。
• Combination I
  申请人：Boughton-Smith Nigel

  公开号：US20080207577A1

  公开（公告）日：2008-08-28

  The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a P2X 7 receptor antagonist, and a second active ingredient which is a corticosteroid, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.

  本发明提供了一种药物产品、试剂盒或组合物，包括第一活性成分，该成分是P2X7受体拮抗剂，以及第二活性成分，该成分是皮质类固醇，用于治疗呼吸系统疾病，如慢性阻塞性肺疾病和哮喘。