醋酸氟轻松 | 67-73-2

• 物质功能分类: 原料药 - 激素及调节内分泌功能类药 - 肾上腺皮质激素类药
• 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: 醋酸氟轻松
• 中文别名: 醋酸肤轻松；氟轻松；肤轻松；仙乃乐；11b-羟基-16a,17-[(1-甲基亚乙基)-双(氧)]-21-(乙酰氧基)-6a,9-二氟孕甾-1,4-二烯-3,20-二酮；乙酸肤轻松；11b-羟基-16a,17-[(1-甲基亚乙基)-双(氧)]-21-(乙酰氧基)-6a,9-二氟孕甾-1,4-二烯-3
• 英文名称: fluocinolone Acetonide
• 英文别名: (2S,6aS,6bR,7S,8aS,8bS,11aR,12aS,12bS)-2,6b-difluoro-7-hydroxy-8b-(2-hydroxyacetyl)-6a,8a,10,10-tetramethyl-1,2,6a,6b,7,8,8a,8b,11a,12,12a,12b-dodecahydro-4H-naphtho-[2',1':4,5]indeno[1,2-d][1,3]dioxol-4-one；(1S,2S,4R,8S,9S,11S,12R,13S,19S)-12,19-difluoro-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one
• CAS: 67-73-2
• 化学式: C₂₄H₃₀F₂O₆
• mdl: MFCD00010525
• 分子量: 452.495
• InChiKey: FEBLZLNTKCEFIT-VSXGLTOVSA-N

物化性质

• 熔点：
  267-269 °C(lit.)
• 比旋光度：
  D +95° (chloroform)
• 沸点：
  578.5±50.0 °C(Predicted)
• 密度：
  1.1826 (estimate)
• 溶解度：
  几乎不溶于水，溶于丙酮和乙醇
• 物理描述：
  Solid
• 颜色/状态：
  CRYSTALS FROM ACETONE & HEXANE
• 气味：
  ODORLESS
• 稳定性/保质期：
  STABLE IN LIGHT
• 旋光度：
  SPECIFIC OPTICAL ROTATION: +95 DEG @ 25 °C/D (CHLOROFORM); MAX ABSORPTION: 238 NM (LOG E= 4.21)
• 碰撞截面：
  199.7 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  32
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  93.1
• 氢给体数：
  2
• 氢受体数：
  8

ADMET

代谢

紧随吸收之后，氟轻松醋酸酯的代谢主要发生在肝脏。值得注意的是，系统吸收的剂量非常小。

Following absorption, fluocinolone acetonide metabolism is primarily hepatic. It is important to mention that the systemically absorbed dose is very minimal.

来源:DrugBank

代谢

...通常认为皮质醇及其同类物和合成衍生物的代谢在性质上是相似的。...主要通过环A的还原、C20位置上酮的还原和侧链的断裂来进行代谢。代谢物以葡萄糖苷酸、硫酸盐和非结合化合物形式排出。...皮质类固醇/

...IT IS GENERALLY ASSUMED THAT METAB OF /CORTISOL &/ ITS CONGENERS & SYNTH DERIV IS QUALITATIVELY SIMILAR. ...METABOLIZED PRINCIPALLY BY REDN OF RING A, REDN OF KETONE AT C 20, & CLEAVAGE OF SIDE CHAIN. METABOLITES ARE EXCRETED...AS GLUCURONIDES, SULFATES, & UNCONJUGATED COMPOUNDS. /CORTICOSTEROIDS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

皮质类固醇引起的伤口愈合受损，在局部应用维生素A后有所逆转。

REVERSAL OF CORTICOSTEROID-INDUCED IMPAIRMENT OF WOUND HEALING HAS BEEN REPORTED AFTER TOPICAL APPLICATION OF VITAMIN /VITAMIN A/. /CORTICOSTEROIDS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

...毛囊炎或条纹是常见的并发症，尤其是在使用封闭敷料时。

...FOLLICULITIS OR STRIAE IS FREQUENT COMPLICATION, ESP IF OCCLUSIVE DRESSINGS ARE USED.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

药理剂量的糖皮质激素会延缓或中断儿童的生长，这表明对生长板软骨有不良影响。抑制生长是一个相当普遍的效应... /糖皮质激素/

PHARMACOLOGICAL DOSES OF GLUCOCORTICOIDS RETARD OR INTERRUPT GROWTH OF CHILDREN, INDICATING ADVERSE EFFECT ON EPIPHYSEAL CARTILAGE. INHIBITION OF GROWTH IS RATHER WIDESPREAD EFFECT... /GLUCOCORTICOIDS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

长期使用皮质类固醇治疗可能会导致垂体-肾上腺功能的抑制，这种抑制可能需要较长时间才能恢复正常。/皮质类固醇/

PROLONGED THERAPY WITH CORTICOSTEROIDS MAY RESULT IN SUPPRESSION OF PITUITARY-ADRENAL FUNCTION THAT CAN BE SLOW IN RETURNING TO NORMAL. /CORTICOSTEROIDS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

长期治疗的主要并发症包括液体和电解质紊乱、高血糖和糖尿、感染易感性增加，包括结核病、可能会出血或穿孔的消化性溃疡、骨质疏松、特征性肌病和行为障碍/皮质类固醇/。

...PRINCIPAL COMPLICATIONS RESULTING FROM PROLONGED THERAPY...ARE FLUID & ELECTROLYTE DISTURBANCES; HYPERGLYCEMIA & GLYCOSURIA; INCR SUSCEPTIBILITY TO INFECTIONS, INCL TUBERCULOSIS; PEPTIC ULCERS, WHICH MAY BLEED OR PERFORATE; OSTEOPOROSIS; CHARACTERISTIC MYOPATHY; BEHAVIORAL DISTURBANCES... /CORTICOSTEROIDS/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

• 吸收

作为眼内植入物使用时，醋酸氟轻松可以持续释放达12个月。醋酸氟轻松在玻璃体和视网膜中的浓度通常较高，而在房水中的分布较少。有报道称，局部应用醋酸氟轻松会产生经皮吸收，这种吸收受药物载体、表皮屏障的完整性以及使用封闭敷料的影响。无论给药途径如何，醋酸氟轻松的系统吸收量低于0.1 ng/ml，这表明其系统分布非常有限，醋酸氟轻松的效果主要是局部的。

When administered as an eye implant, fluocinolone acetonide presents a sustained delivery for even 12 months in which there can be observed a sustained release. The concentration of fluocinolone acetonide are generally higher in the vitreous and retina with a little dispersion to the aqueous humor. There are reports indicating that topical administration of fluocinolone acetonide produces a percutaneous absorption which is determined by the vehicle, integrity of the epidermal barrier and the use of occlusive dressing. Independently of the route of administration, the systemic absorption of fluocinolone acetonide is below 0.1 ng/ml which indicates that the systemic distribution is very minimal and the effect of fluocinolone is mainly local.

来源:DrugBank

吸收、分配和排泄

• 消除途径

氟轻松醋酸酯主要通过肾脏排泄。重要的是要提到，系统吸收的剂量非常小。

Fluocinolone acetonide is mainly excreted by the kidneys. It is important to mention that the systemically absorbed dose is very minimal.

来源:DrugBank

吸收、分配和排泄

• 分布容积

这个药代动力学参数不相关，因为氟轻松醋酸的系统性吸收非常小。

This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal.

来源:DrugBank

吸收、分配和排泄

• 清除

这个药代动力学参数不相关，因为氟轻松醋酸的系统性吸收非常小，尿中的浓度低于最低定量限。

This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal and the concentration in urine is lower than the minimum quantitation limit.

来源:DrugBank

吸收、分配和排泄

皮质类固醇的代谢通过在分子中引入1,2双键或氟原子而被大大减缓，其半衰期相应地延长。/皮质类固醇/

METABOLISM OF CORTICOSTEROIDS IS GREATLY SLOWED BY INTRODUCTION OF THE 1,2 DOUBLE BOND OR A FLUORINE ATOM INTO MOLECULE, & HALF-LIFE IS CORRESPONDINGLY PROLONGED. /CORTICOSTEROIDS/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险品标志：
  Xn
• 安全说明：
  S22,S26,S36
• 危险类别码：
  R20/21/22,R40,R36/37/38
• WGK Germany：
  3
• 海关编码：
  2937210000
• 危险品运输编号：
  NONH for all modes of transport
• RTECS号：
  TU3830000
• 储存条件：
  | 冰箱 |

SDS

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

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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.
Skin Contact In case of contact, immediately flush skin with plenty of water. Cover the irritated skin with an emollient. Remove
contaminated clothing and shoes. Wash clothing before reuse. Thoroughly clean shoes before reuse. Get
medical attention.
Serious Skin Contact Wash with a disinfectant soap and cover the contaminated skin with an anti-bacterial cream. Seek medical
attention.
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. Loosen tight clothing such as a collar, tie, belt or waistband. Get medical attention if
symptoms appear.
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), halogenated compounds.
Fire Hazards in Presence of Slightly flammable to flammable in presence of heat.
Various Substances Non-flammable in presence of shocks.
Explosion Hazards in Presence Slightly explosive in presence of open flames and sparks.
of Various Substances Non-explosive in presence of shocks.
Fire Fighting Media SMALL FIRE: Use DRY chemical powder.
and Instructions LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
Special Remarks on As with most organic solids, fire is possible at elevated temperatures When heated to decomposition it emits toxic
Fire Hazards fumes of Carbon Monoxide, Carbon Dioxide, and Hydrogen Fluoride
Special Remarks on Explosion Fine dust dispersed in air in sufficient concentrations, and in the presences 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.
Fluocinolone acetonide

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Section 7. Handling and Storage
Precautions Keep locked up.. Keep away from heat. Keep away from sources of ignition. Do not ingest. Do not breathe dust.
Wear suitable protective clothing. In case of insufficient ventilation, wear suitable respiratory equipment. If
ingested, seek medical advice immediately and show the container or the label. Avoid contact with skin and eyes.
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 Splash goggles. 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. (Crystalline solid. Crystalline powder.) Odor Odorless.
Not available.
Taste
Molecular Weight 452.49 g/mole
White.
Color
Not applicable.
pH (1% soln/water)
Boiling Point Not available.
Melting Point 266°C (510.8°F)
Critical Temperature Not available.
Specific Gravity Not available.
Not applicable.
Vapor Pressure
Vapor Density Not available.
Not available.
Volatility
Odor Threshold Not available.
Water/Oil Dist. Coeff. Not available.
Ionicity (in Water) Not available.
Dispersion Properties See solubility in water, methanol, acetone.
Solubility Soluble in methanol, acetone.
Insoluble in cold water, hot water.
Soluble in alcohol.
Slightly soluble in Chloroform.
Fluocinolone acetonide

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Section 10. Stability and Reactivity Data
The product is stable.
Stability
Instability Temperature Not available.
Excess heat, dust generation, incompatible materials
Conditions of Instability
Reactive with oxidizing agents.
Incompatibility with various
substances
Corrosivity Non-corrosive in presence of glass.
Special Remarks on Not available.
Reactivity
Special Remarks on Not available.
Corrosivity
Polymerization Will not occur.

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Section 11. Toxicological Information
Routes of Entry Absorbed through skin. Inhalation. Ingestion.
Toxicity to Animals Acute oral toxicity (LD50): >4000 mg/kg [Mouse].
Chronic Effects on Humans DEVELOPMENTAL TOXICITY: Classified Reproductive system/toxin/female [POSSIBLE].
Other Toxic Effects on Hazardous in case of skin contact (irritant), of ingestion, of inhalation.
Humans Slightly hazardous in case of skin contact (permeator).
Special Remarks on Not available.
Toxicity to Animals
Special Remarks on May cause adverse reproductive effects.
Chronic Effects on Humans
May affect genetic material (mutagenic)
Special Remarks on other Potential Health Effects:
Toxic Effects on Humans Skin: May cause skin irritation with itching and burning feeling, skin dryness, folliculitis, acneifom erruptions,
perioral dermatitis, allergic contact dermatitis, hypertrichosis. It may be absorbed by the skin and cause systemic
effects.
Eyes: Causes eye irritation.
Inhalation: Causes upper respiratory tract and mucous membrane irritation.
Ingestion: May cause gastrointestinal tract irritation. Prolonged or repeated ingestion may affect metabolism

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

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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.

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Section 14. Transport Information
DOT Classification Not a DOT controlled material (United States).
Not applicable.
Identification
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
Proposition 65
Warnings
Other Regulations EINECS: This product is on the European Inventory of Existing Commercial Chemical Substances.
WHMIS (Canada) Not controlled under WHMIS (Canada).
Other Classifications
DSCL (EEC) R36/38- Irritating to eyes and skin. S2- Keep out of the reach of children.
R40- Possible risks of irreversible S36/37- Wear suitable protective clothing and
effects. gloves.
R62- Possible risk of impaired fertility. S46- If swallowed, seek medical advice
immediately and show this container or label.
Health Hazard
HMIS (U.S.A.) 2 National Fire Protection
1 Flammability
1 Association (U.S.A.)
Fire Hazard
2 0 Reactivity
Health
Reactivity
0
Specific hazard
Personal Protection
E
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
TDG (Canada)
(Pictograms)
Fluocinolone acetonide
ADR (Europe)
(Pictograms)
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

皮质激素类药物

醋酸肤轻松

又称醋酸氟轻松、氟西奈德、氟去炎舒松、肤轻松、氟轻松、仙乃乐、丙酮化氟新龙，是目前我国外用皮质激素中疗效显著且副作用较小的一种。它可通过使真皮毛细血管收缩，抑制结缔组织细胞增殖或再生；稳定细胞内溶酶体膜，防止组胺释放而造成组织损伤。其抗炎作用是氢化可的松的100倍，使用最低浓度（0.025%）即可产生明显疗效，并能迅速奏效，在数日内显著减轻或痊愈症状，止痒效果较好。

醋酸肤轻松主要用于治疗对糖皮质激素有效的皮肤病，如接触性皮炎、特应性皮炎、脂溢性皮炎、神经性皮炎、日光性皮炎、湿疹（特别是婴儿湿疹）、皮肤瘙痒症、银屑病、盘状红斑狼疮、扁平苔藓及外耳炎。与新霉素等抗菌素配伍可用于治疗化脓性皮肤病。

理化性质

白色或类白色的结晶性粉末，无味无臭。[α]D20+80—+88°（二氧六环）。溶于丙酮，略溶于乙醇、二氧六环，不溶于水和石油醚。由11α-羟基 -16α, 17α-环氧孕甾烷-4-烯-3,20-二酮经磺酯化、开环等16步反应而得。

药理作用

醋酸氟轻松是一种含氟的糖皮质激素。外用制剂中，0.01%为中效，0.025%为强效。它能收缩真皮毛细血管，抑制表皮细胞增殖或再生，抑制结缔组织内纤维细胞新生，稳定溶酶体膜，并减少炎性渗出和抑制组胺及其他炎症介质的形成与释放，具有抗过敏、抗炎及止痒的作用。

适应症

用于接触性皮炎、过敏性皮炎、脂溢性皮炎、神经性皮炎、日光性皮炎、湿疹、银屑病、扁平苔癣及皮肤瘙痒症等。

醋酸肤轻松

醋酸肤轻松是一种合成的含氟强效类固醇。外用可使真皮毛细血管收缩，抑制表皮细胞增殖或再生，抑制结缔组织内纤维细胞新生，稳定溶酶体膜，并具有抗炎、止痒的作用。外用后可通过完整的皮肤吸收，在肝脏代谢并经肾脏排出。

醋酸肤轻松适用于治疗湿疹（特别是婴儿湿疹）、神经性皮炎、皮肤瘙痒症、接触性皮炎、牛皮癣、盘状红斑狼疮、扁平苔藓及外耳炎等，但需注意长期或大面积使用可能引起的皮肤萎缩、毛细血管扩张、痤疮样皮炎、口周皮炎和增加感染易感性等问题。

不良反应

长期或大面积应用可导致全身不良反应，如库欣综合征、高血糖症、糖尿等；也可引起皮肤萎缩、毛细血管扩张、痤疮样皮炎、口周皮炎及感染等症状。因此，在面部或皮肤皱褶部位使用需谨慎，并须同时考虑抗感染治疗。

注意事项

1. 避免长期大面积 使用。
2. 面部和皮肤皱褶处 使用时应谨慎评估利弊。
3. 若有皮肤感染，必须同时应用抗菌药物。感染症状未及时改善时需停药直至感染控制。
4. 孕妇及哺乳期妇女应权衡利弊后慎用，并禁止长期大面积使用。
5. 该药物不可用于眼部。
6. 儿童及婴儿由于体表面积较大，应在考虑利弊后谨慎使用。

生物活性

Fluocinolone Acetonide（Flucort-N）是一种皮质类固醇，与胞浆中的糖皮质激素受体结合。

靶点

Target	Value
Glucocorticoid receptor	()

该药物适用于治疗过敏性皮炎、接触性皮炎、脂溢性皮炎及湿疹等多种皮肤病。

反应信息

• 作为反应物：
  描述：

  醋酸氟轻松 在 Wilkinson's catalyst 、 超重氢 作用下， 以 四氢呋喃 、 甲苯 为溶剂， 以100%的产率得到(1S,2S,4R,8S,9S,11S,12R,13S,19S)-12,19-difluoro-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-14,15-ditritio-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icos-17-en-16-one
  参考文献：
  名称：

  Preparation of high specific activity tritium labeled 6α,9,-difluoro-11β,21-dihydroxy-16α,17-[(1-methylethylidene)bis(oxy)]pregna-1,4-diene-3,20-one, fluocinolone acetonide

  摘要：

  氟轻松醋酸酯通过在氚下选择性还原其O-保护类似物的1,2-双键，随后重新建立1,2-双键并去保护，从而实现了氚标记。两个羟基功能团都需要保护。所得产品的比活性为36.8 Ci/mmol。版权所有 © 2009 John Wiley & Sons, Ltd.

  DOI：

  10.1002/jlcr.1575
• 作为产物：
  描述：

  delta皮质素烯乙酸酯 在 吡啶 、 potassium permanganate 、 甲酸 、 高氯酸 、 乙酸异丙烯酯 、 N,N-二甲基乙酰胺 、 氢氟酸 、 potassium acetate 、 对甲苯磺酸 、 sodium hydroxide 作用下， 以 甲醇 、 二氯甲烷 、 水 、 N,N-二甲基甲酰胺 、 丙酮 、 乙腈 为溶剂， 反应 35.0h， 生成 醋酸氟轻松
  参考文献：
  名称：

  氟轻松的改进合成及6α,9α-氟化反应工艺研究

  摘要：

  从 21-乙酰氧基-17α-羟基-4,9(11)-二烯-3,20-二酮 (1a) 开发了一种高效、改进的氟轻松与生物发酵相结合的合成路线。研究了 6α 和 9α 氟化步骤的过程，观察到 6α 氟化的立体选择性高度依赖于底物。在对氟化试剂和活化试剂进行广泛筛选后，6α-F 以 85% 的收率和 98.9% 的立体选择性引入。代替 HF 气体，在 9α 氟化步骤中应用 HF 水溶液，以 89% 的收率提供所需的产物。从 1a 开始，氟轻松分 9 个步骤制备，总产率为 38.5%。

  DOI：

  10.1246/cl.170923

文献信息

• [EN] QUINONE BASED NITRIC OXIDE DONATING COMPOUNDS<br/>[FR] COMPOSÉS DONNEURS D'OXYDE NITRIQUE À BASE DE QUINONE
  申请人：NICOX SA

  公开号：WO2013060673A1

  公开（公告）日：2013-05-02

  The present invention relates to nitric oxide donor compounds having a quinone based structure, to processes for their preparation and to their use in the treatment of pathological conditions where a deficit of NO plays an important role in their pathogenesis.

  本发明涉及具有喹诚基结构的一氧化氮供体化合物，涉及其制备方法以及它们在治疗病理状况中的应用，其中一氧化氮缺乏在它们的发病机制中起重要作用。
• [EN] PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS<br/>[FR] DÉRIVÉS DE PYRROLOTRIAZINONE EN TANT QU'INHIBITEURS DES PI3K
  申请人：ALMIRALL SA

  公开号：WO2014060432A1

  公开（公告）日：2014-04-24

  New pyrrolotriazinone derivatives having the chemical structure of formula (I), are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks)

  新的吡咯三唑酮衍生物具有化学结构式（I），公开；以及它们的制备方法，包括它们的药物组合物和它们作为磷脂酰肌醇3-激酶（PI3Ks）抑制剂在治疗中的应用。
• CYCLOPROPYLAMINES AS LSD1 INHIBITORS
  申请人：Incyte Corporation

  公开号：US20150225379A1

  公开（公告）日：2015-08-13

  The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

  本发明涉及环丙胺衍生物，这些衍生物是LSD1抑制剂，可用于治疗癌症等疾病。
• Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith
  申请人：D'Sidocky Neil R.

  公开号：US20080242694A1

  公开（公告）日：2008-10-02

  Provided herein are Heterocyclic Compounds having the following structure: wherein R 1 , R 2 , X, Y and Z are as defined herein, compositions comprising an effective amount of a Heterocyclic Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heterocyclic Compound to a patient in need thereof.

  本文提供具有以下结构的杂环化合物： 其中R1、R2、X、Y和Z如本文所定义，包含有效量杂环化合物的组合物，以及治疗或预防癌症、炎症性疾病、免疫疾病、代谢性疾病以及通过给予患者需要的有效量杂环化合物来抑制激酶途径治疗或预防的疾病的方法。
• [EN] PLANT STEROIDS AND USES THEREOF<br/>[FR] STÉROÏDES VÉGÉTAUX ET LEURS UTILISATIONS
  申请人：DAVIDSON LOPEZ LLC

  公开号：WO2013040441A1

  公开（公告）日：2013-03-21

  The invention relates to a drug conjugate including a drug and a plant steroid. The drug conjugate may target the drug for intestinal cell delivery, and thus may be used to treat diseases, including intestinal diseases, or to affect intestinal metabolism. The invention therefore also relates to treating intestinal diseases and affecting intestinal metabolism with the drug conjugate.

  这项发明涉及一种药物结合物，包括药物和植物类固醇。该药物结合物可以将药物定位到肠细胞传递，因此可用于治疗疾病，包括肠道疾病，或影响肠道代谢。因此，该发明还涉及使用药物结合物治疗肠道疾病和影响肠道代谢。