卡利普多 | 78-44-4

• 物质功能分类: 原料药 - 神经系统用药 - 抗焦虑药
• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 卡利普多
• 中文别名: 异庚二酯；异丙基甲丁双脲；卡立普多
• 英文名称: carisoprodol
• 英文别名: [2-(carbamoyloxymethyl)-2-methylpentyl] N-propan-2-ylcarbamate
• CAS: 78-44-4
• 化学式: C₁₂H₂₄N₂O₄
• 分子量: 260.334
• InChiKey: OFZCIYFFPZCNJE-UHFFFAOYSA-N

物化性质

• 熔点：
  92-92°C
• 沸点：
  403.59°C (rough estimate)
• 密度：
  1.1035 (rough estimate)
• 溶解度：
  极微溶于水，易溶于丙酮、酒精和二氯甲烷。
• 物理描述：
  Carisoprodol is a white powder. (NTP, 1992)
• 颜色/状态：
  Crystals
• 味道：
  Slightly bitter taste
• 蒸汽压力：
  3.01X10-4 mm Hg at 25 °C (est)
• 水溶性：
  -2.5
• 稳定性/保质期：
  STABLE IN DIL ACIDS & ALKALIES.
• 碰撞截面：
  149.1 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]
• 保留指数：
  1861;1847;1847;1855;1850;1841;1830

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  18
• 可旋转键数：
  9
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  90.6
• 氢给体数：
  2
• 氢受体数：
  4

ADMET

代谢

卡瑞斯奥洛尔的主要代谢途径是通过细胞色素酶CYP2C19在肝脏中代谢形成美普巴胺。这种酶表现出遗传多态性，可能会影响该药物的代谢。

The main pathway of carisoprodol is liver metabolism is by the cytochrome enzyme CYP2C19 to form meprobamate. This enzyme exhibits genetic polymorphism, which may affect the metabolism of this drug.

来源:DrugBank

代谢

肌安宁的主要代谢途径是通过肝脏的细胞色素酶CYP2C19形成美普巴胺。这种酶表现出遗传多态性。

The major pathway of carisoprodol metabolism is via the liver by cytochrome enzyme CYP2C19 to form meprobamate. This enzyme exhibits genetic polymorphism.

来源:Hazardous Substances Data Bank (HSDB)

代谢

"Carisoprodol 在肝脏中被代谢；动物研究显示该药物可能诱导肝微粒体酶。动物研究还表明，该药物主要以羟基卡立司琼和羟基美普巴amate形式在尿液中排出，其次是以美普巴amate形式；尿液中也有少量未经改变的卡立司琼。该药物可以通过血液透析或腹膜透析去除。"

Carisoprodol is metabolized in the liver; animal studies indicate the drug may induce liver microsomal enzymes. Animal studies also indicate that the drug is excreted in urine, principally as hydroxycarisoprodol and hydroxymeprobamate, and to a lesser extent as meprobamate; trace amounts of carisoprodol are excreted unchanged in urine. The drug may be removed by hemodialysis or peritoneal dialysis.

来源:Hazardous Substances Data Bank (HSDB)

代谢

甲氧苯丙甲酯是一种肌肉松弛剂和镇痛剂，它有一个活性代谢物，即眠尔通（meprobamate）。我们进行了一项开放标签的三组单次给药研究，研究对象为15名健康志愿者：5名甲氧苯妥英（mephenytoin）差代谢者，5名去甲丙嗪（debrisoquine）差代谢者和5名对两种底物都有广泛代谢能力的个体。研究目的是调查甲氧苯丙甲酯和眠尔通的消除是否依赖于甲氧苯妥英和去甲丙嗪的两种代谢多态性。受试者在不同时间接受了单次口服700毫克甲氧苯丙甲酯和400毫克眠尔通的剂量。甲氧苯丙甲酯的处置与甲氧苯妥英羟化表型明显相关。甲氧苯妥英差代谢者的甲氧苯丙甲酯平均血清清除率是广泛代谢者的四分之一，这证实了我们之前研究的假设，即甲氧苯丙甲酯的N-脱烷基化与甲氧苯妥英羟化多态性共分离。然而，眠尔通的平均血清清除率在两组之间没有差异。此外，多态性去甲丙嗪羟化并没有影响甲氧苯丙甲酯或眠尔通的消除。因此，甲氧苯妥英差代谢者代谢甲氧苯丙甲酯的能力较低，如果使用普通剂量的甲氧苯丙甲酯治疗，他们可能面临增加浓度的依赖性副作用风险，如嗜睡和低血压。

Carisoprodol is a muscle relaxant analgesic, which has an active metabolite i.e. meprobamate. We conducted an open three-panel single-dose administration study with 15 healthy volunteers: five poor metabolizers of mephenytoin, five poor metabolizers of debrisoquine and five extensive metabolizers of both substrates. The aim was to investigate if the elimination of carisoprodol and meprobamate is dependent on the two metabolic polymorphisms of mephenytoin and debrisoquine. The subjects were given single oral doses of 700 mg carisoprodol and 400 mg meprobamate on separate occasions. The disposition of carisoprodol was clearly correlated to the mephenytoin hydroxylation phenotype. The mean serum clearance of carisoprodol was four times lower in poor metabolizers of mephenytoin than in extensive metabolizers, which confirms the hypothesis from our previous study that N-dealkylation of carisoprodol cosegregates with the mephenytoin hydroxylation polymorphism. However, mean serum clearance of meprobamate did not differ between the two groups. Also, polymorphic debrisoquine hydroxylation did not influence the elimination of carisoprodol or meprobamate. Poor metabolizers of mephenytoin thus have a lower capacity to metabolize carisoprodol and may therefore have an increased risk of developing concentration dependent side-effects such as drowsiness and hypotension, if treated with ordinary doses of carisoprodol.

来源:Hazardous Substances Data Bank (HSDB)

代谢

肝脏。通过细胞色素P450氧化酶同种型CYP2C19在肝脏中代谢。 消除途径：卡立司酮通过肾脏和非肾脏途径消除。 半衰期：8小时

Hepatic. Metabolized in the liver via the cytochrome P450 oxidase isozyme CYP2C19. Route of Elimination: Carisoprodol is eliminated by both renal and non-renal routes. Half Life: 8 hours

来源:Toxin and Toxin Target Database (T3DB)

毒理性

• 毒性总结

佳静安定是一种中枢神经系统抑制剂，具有镇静和骨骼肌松弛作用。它不是直接作用于骨骼肌，而是通过干扰网状结构和脊髓内的神经元通信，从而导致镇静和疼痛感知的改变。其确切的作用机制尚不完全清楚。

Carisoprodol is a central nervous system depressant that acts as a sedative and skeletal muscle relaxant. Rather than acting directly on skeletal muscle, carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. Its exact mechanism of action is not yet known.

来源:Toxin and Toxin Target Database (T3DB)

毒理性

• 肝毒性

在推荐的剂量以上，这种药物作为滥用物质的报道越来越多。 可能性评分：E（不太可能导致临床上明显的肝损伤）。 药物类别：肌肉松弛剂

There have been no adequate prospective studies demonstrating the rates of aminotransferase elevations on carisoprodol therapy or convincing case reports of clinically apparent liver injury due to carisoprodol. Thus, the hepatotoxic potential of this medication is low. It has been increasingly reported as a substance of abuse, taken in higher than recommended doses. Likelihood score: E (Unlikely cause of clinically apparent liver injury). Drug Class: Muscle Relaxants

来源:LiverTox

毒理性

• 药物性肝损伤

混合物：卡立司唑仑

Compound:carisoprodol

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

DILI 注释：无 DILI（药物性肝损伤）担忧

DILI Annotation:No-DILI-Concern

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

标签部分：无匹配

Label Section:No match

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

吸收、分配和排泄

• 吸收

卡力索普罗多的绝对生物利用度尚未确定。在临床研究中，该药物达到峰值血浆浓度（Tmax）的平均时间约为1.5-2小时。与卡力索普罗多（350毫克片剂）共同服用高脂肪餐对卡力索普罗多的药代动力学没有影响。

The absolute bioavailability of carisoprodol has not yet been established. The mean time to peak plasma concentrations (Tmax) of this drug was about 1.5-2 hours in clinical studies. Co-administration of a fatty meal with carisoprodol (350 mg tablet) had no impact on carisoprodol pharmacokinetics.

来源:DrugBank

吸收、分配和排泄

• 消除途径

卡立索布洛尔通过肾脏以及其他途径排出。美普洛巴莫的半衰期大约为10小时。

Carisoprodol is eliminated by the kidneys as well as other routes. The half-life of meprobamate is approximately 10 hours.

来源:DrugBank

吸收、分配和排泄

• 分布容积

根据4项不同的临床研究，0.93至1.3升/公斤。

0.93 to 1.3 L/kg, according to 4 different clinical studies.

来源:DrugBank

吸收、分配和排泄

• 清除

在服用卡利斯托罗后，口服清除率（Cl/F）为39.52 ± 16.83升/小时。

Following an oral dose of carisoprodol, the oral clearance (Cl/F) was 39.52 ± 16.83 L/hour.

来源:DrugBank

吸收、分配和排泄

卡立司琼可以穿过胎盘。该药物在乳汁中的浓度是同期母体血浆浓度的2-4倍。

Carisoprodol crosses the placenta. The drug distributes into milk in concentrations 2-4 times higher than concurrent maternal plasma concentrations.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险品标志：
  Xn
• 安全说明：
  S36
• 危险类别码：
  R22
• 海关编码：
  2924199090
• RTECS号：
  FB3325000
• WGK Germany：
  3
• 储存条件：
  2-8°C

SDS

---

Section 1. Chemical Product and Company Identification
Carisoprodol Catalog
Common Name/
Number(s).
Trade Name
CAS# 78-44-4
Manufacturer
RTECS FB3325000
SPECTRUM QUALITY PRODUCTS INC.
TSCA TSCA 8(b) inventory: No
products were found.
Commercial Name(s) Not available.
CI# Not available.
Synonym 2-Methyl-2-Propyl-1,3-Propanediol Carbamate Isopropylcarbamate
IN CASE OF EMERGENCY
Carisoprodol
Chemical Name
Chemical Family Not available. CALL [phone]
C12-H24-N2-O4
Chemical Formula
SPECTRUM QUALITY PRODUCTS INC.

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Section 2.Composition and Information on Ingredients
Exposure Limits
TWA (mg/m3) STEL (mg/m3) CEIL (mg/m3)
Name CAS # % by Weight
1) Carisoprodol 78-44-4 100
Toxicological Data Carisoprodol:
on Ingredients ORAL (LD50): Acute: 1320 mg/kg [Rat]. 1800 mg/kg [Mouse].

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Section 3. Hazards Identification
Potential Acute Health Effects Hazardous in case of ingestion, of inhalation.
Potential Chronic Health CARCINOGENIC EFFECTS: Not available.
MUTAGENIC EFFECTS: Not available.
Effects
TERATOGENIC EFFECTS: Not available.
DEVELOPMENTAL TOXICITY: Classified Development toxin [POSSIBLE].
The substance may be toxic to lungs, liver, upper respiratory tract, central nervous system (CNS), throat.
Repeated or prolonged exposure to the substance can produce target organs damage.
Carisoprodol

---

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. Remove contaminated clothing and shoes. Wash
clothing before reuse. Thoroughly clean shoes before reuse. Get medical attention.
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.
These products are carbon oxides (CO, CO2), nitrogen oxides (NO, NO2...).
Products of Combustion
Fire Hazards in Presence of Not available.
Various Substances
Explosion Hazards in Presence Risks of explosion of the product in presence of mechanical impact: Not available.
of Various Substances Risks of explosion of the product in presence of static discharge: Not available.
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 Not available.
Fire Hazards
Special Remarks on Explosion Not available.
Hazards

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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.
Carisoprodol

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Section 7. Handling and Storage
Precautions Keep locked up.. Keep away from heat. Keep away from sources of ignition. Empty containers pose a fire risk,
evaporate the residue under a fume hood. Ground all equipment containing material. 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.
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.
Personal Protection in Case of Splash goggles. Full suit. Boots. Gloves. Suggested protective clothing might not be sufficient; consult a
a Large Spill 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.) Odor Not available.
Bitter. (Slight.)
Taste
Molecular Weight 260.33 g/mole
Not available.
Color
Not applicable.
pH (1% soln/water)
Boiling Point Not available.
92.5°C (198.5°F)
Melting Point
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 Very slightly dispersed in methanol, diethyl ether, n-octanol, acetone.
Is not dispersed in cold water, hot water.
Solubility Very slightly soluble in methanol, diethyl ether, n-octanol, acetone.
Insoluble in cold water, hot water.

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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 Not available.
substances
Carisoprodol
Corrosivity Not available.
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 Inhalation. Ingestion.
Toxicity to Animals Acute oral toxicity (LD50): 1320 mg/kg [Rat].
Chronic Effects on Humans CARCINOGENIC EFFECTS: (Inadequate study.) by NTP.
DEVELOPMENTAL TOXICITY: Classified Development toxin [POSSIBLE].
May cause damage to the following organs: lungs, liver, upper respiratory tract, central nervous system (CNS),
throat.
Other Toxic Effects on Hazardous in case 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 Not available.
Toxic Effects on Humans

---

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 less toxic than the product itself.
of Biodegradation
Special Remarks on the Not available.
Products of Biodegradation

---

Section 13. Disposal Considerations
Waste Disposal

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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
Carisoprodol
DOT (Pictograms)

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Section 15. Other Regulatory Information and Pictograms
California prop. 65: This product contains the following ingredients for which the State of California has found to
Federal and State
cause cancer, birth defects or other reproductive harm, which would require a warning under the statute:
Regulations
Carisoprodol
California prop. 65: This product contains the following ingredients for which the State of California has found to
cause reproductive harm (female) which would require a warning under the statute: Carisoprodol
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: Carisoprodol
TSCA 8(d) H and S data reporting: Carisoprodol: June 1999
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: Carisoprodol
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) R22- Harmful if swallowed.
R40- Possible risks of irreversible
effects.
R63- Possible risk of harm to the
unborn child.
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
a
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
TDG (Canada)
(Pictograms)
ADR (Europe)
(Pictograms)
Protective Equipment
Not applicable.
Carisoprodol
Lab coat.
Not applicable.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

药理作用

卡利普多是甲丙氨酯的一种衍生物，除了具备镇静及抗焦虑的作用外，还具有较强的中枢性肌肉松弛效果，对局部肌肉痉挛及某些神经疾病有一定的治疗价值。

副作用

尽管卡利普多在缓解背痛和活化患者方面表现优异，但其滥用潜力和过量服用后的毒副作用也引发了广泛批评。常见副作用包括头晕、嗜睡、恶心以及心理损伤等。

反应信息

• 作为反应物：
  描述：

  卡利普多 、 环己烷 在 二叔丁基过氧化物 、 copper diacetate 、 4,4'-二叔丁基-2,2'-二吡啶 作用下， 以 乙腈 为溶剂， 反应 12.0h， 以60%的产率得到
  参考文献：
  名称：

  铜（II）与烷烃的光催化NH烷基化

  摘要：

  我们报告了一种使用光诱导的过氧化铜（II）催化体系与烷烃进行N–H键烷基化的实用方法。在光照射下，过氧化物充当氢原子转移试剂，以激活稳定的C（sp 3）–H键，从而与各种氮亲核试剂反应。该方法可实现酰胺的化学选择性烷基化，并用于具有良好收率或优异收率的含N-H键的药物的后期功能化。通过自由基捕获实验和光谱方法初步研究了反应机理。

  DOI：

  10.1021/acscatal.0c01924
• 作为产物：
  描述：

  2-甲基-2-丙基-1,3-丙二醇 在 正丁基锂 、 aluminum;2-[[bis[(3,5-ditert-butyl-2-oxidophenyl)methyl]amino]methyl]-4,6-ditert-butylphenolate;oxolane 、 bis(triphenylphosphoranylidene)ammonium iodide 、 对甲苯磺酰氯 作用下， 以 甲醇 、 二氯甲烷 、 丁酮 为溶剂， 100.0 ℃ 、1.0 MPa 条件下， 反应 88.0h， 生成 卡利普多
  参考文献：
  名称：

  催化一锅氧杂环丁烷到氨基甲酸酯的转化：药物相关分子的形式合成

  摘要：

  氧杂环丁烷是药物相关合成中的多功能构建基块，可诱导性能调节作用。尽管相关的氧杂环丁烷广泛用于与二氧化碳（CO 2）偶联的化学反应中，以提供增值的商品化学品，但是尽管这些四元杂环的合成取得了新进展，但氧杂环丁烷/ CO 2的偶联仍然极为有限。在这里，我们报告了一种有效的单锅三组分反应（3CR）策略，用于偶联（取代的）氧杂环丁烷，胺和CO 2可以提供具有出色的化学选择性和高收率的各种功能化氨基甲酸酯。该过程由铝基催化剂在相对温和的条件下介导，并且已开发的催化方法可用于两种药学上相关的氨基甲酸酯的正式合成，其中3CR是关键步骤。

  DOI：

  10.1002/adsc.201500895

文献信息

• [EN] QUINAZOLINE DERIVATIVES, COMPOSITIONS, AND USES RELATED THERETO<br/>[FR] DÉRIVÉS DE QUINAZOLINE, COMPOSITIONS ET UTILISATIONS ASSOCIÉES
  申请人：UNIV EMORY

  公开号：WO2013181135A1

  公开（公告）日：2013-12-05

  The disclosure relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidases (Nox enzymes) and/or myeloperoxidase.

  该披露涉及喹唑啉衍生物、组合物以及相关方法。在某些实施例中，该披露涉及NADPH-氧化酶（Nox酶）和/或髓过氧化物酶的抑制剂。
• PRODUCTION METHOD AND PRODUCTION INTERMEDIATE FOR GUANOSINE-3',5'-BISDIPHOSPHATE
  申请人：TOKYO INSTITUTE OF TECHNOLOGY

  公开号：US20210094980A1

  公开（公告）日：2021-04-01

  The present invention relates to a production method and a production intermediate for guanosine-3′,5′-bisdiphosphate.

  本发明涉及一种鸟苷-3′,5′-双磷酸盐的生产方法和生产中间体。
• Chemical Compounds
  申请人：Brown Alan Daniel

  公开号：US20120010182A1

  公开（公告）日：2012-01-12

  The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z 1 , R a , R b , R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

  该发明涉及磺胺衍生物，其在医学上的应用，含有它们的组合物，其制备方法以及用于这些方法的中间体。 更具体地，该发明涉及公式（I）的新磺胺基Nav1.7抑制剂： 或其药学上可接受的盐，其中Z 1 ，R a ，R b ，R 1 ，R 2 ，R 3 ，R 4 和R 5 如描述中所定义。 Nav 1.7抑制剂在治疗各种疾病，特别是疼痛方面具有潜在用途。
• [EN] DIPEPTIDE AND TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS<br/>[FR] INHIBITEURS DE DIPEPTIDE ET DE TRIPEPTIDE ÉPOXY CÉTONE PROTÉASES
  申请人：ONYX THERAPEUTICS INC

  公开号：WO2014152127A1

  公开（公告）日：2014-09-25

  Provided herein are dipeptide and tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of proliferative diseases including cancer and autoimmune diseases.

  本文提供了二肽和三肽环氧酮蛋白酶抑制剂，其制备方法，相关的药物组合物，以及使用它们的方法。例如，本文提供了化合物的化学式（X）：及其药用盐和包括这些化合物的组合物。本文提供的化合物和组合物可以用于治疗增生性疾病，包括癌症和自身免疫疾病。
• [EN] COMBINATIONS COMPRISING ALPHA-2-DELTA LIGANDS<br/>[FR] COMBINAISONS CONTENANT DES LIGANDS DE ALPHA-2-DELTA
  申请人：PFIZER LTD

  公开号：WO2005092318A1

  公开（公告）日：2005-10-06

  The instant invention relates to a combination, particularly a synergistic combination, of an alpha-2-delta ligand and an atypical antipsychotic, and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain.

  这项即时发明涉及一种组合，特别是α-2-δ配体和非典型抗精神病药物的协同组合，以及其药用盐、药物组合物及其在治疗疼痛，特别是神经病痛中的应用。

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