茶苯海明 | 523-87-5

• 物质功能分类: 原料药 - 抗变态反应药 - 抗组胺药
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 中文名称: 茶苯海明
• 中文别名: 1,3-二甲基-8-氯-3,7-二氢-1H-嘌呤-2,6-二酮N,N-二甲基-2-(二苯基甲氧基)乙胺；1,3-二甲基-8氯-3,7-二氢-1H-嘌呤,6二酮-N,N-二甲基-2-(二苯基甲氧基)乙胺盐；晕海宁；乘晕宁；捉迷明；曲拉明
• 英文名称: dimenhydrinate
• 英文别名: 2-benzhydryloxy-N,N-dimethylethanamine 8-chloro-1,3-dimethyl-7H-purine-2,6-dione；dimeithydrinate；dramamine；2-benzhydryloxy-N,N-dimethylethanamine;8-chloro-1,3-dimethyl-7H-purine-2,6-dione
• CAS: 523-87-5
• 化学式: C₇H₇ClN₄O₂*C₁₇H₂₁NO
• 分子量: 469.971
• InChiKey: NFLLKCVHYJRNRH-UHFFFAOYSA-N

物化性质

• 熔点：
  102-107°C
• 密度：
  1.2586 (rough estimate)
• 溶解度：
  微溶于水，易溶于乙醇（96%）。
• 物理描述：
  Dimenhydrinate is a crystalline white powder. (NTP, 1992)
• 颜色/状态：
  CRYSTALS
• 气味：
  ODORLESS
• 保留指数：
  1876;1910;1844

计算性质

• 辛醇/水分配系数(LogP)：
  2.97
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  81.8
• 氢给体数：
  1
• 氢受体数：
  5

ADMET

代谢

盐酸苯海拉明是一种茶碱盐，可以分解为[苯海拉明]和[8-氯茶碱]。苯海拉明可以通过尿苷酸转移酶（UGTs）进行N-葡萄糖苷酸化，形成苯海拉明N-葡萄糖苷酸，或者通过CYP2D6、CYP1A2、CYP2C9和CYP2C19进行N-去甲基化，生成N-去甲基苯海拉明。N-去甲基苯海拉明可以再次通过相同的酶进行N-去甲基化，形成N,N-双去甲基苯海拉明，后者经历氧化脱氨反应，形成二苯基甲氧基乙酸。

Dimenhydrinate is a theoclate salt that separates into [diphenhydramine] and [8-chlorotheophylline]. diphenhydramine can either be N-glucuronidated by UGTs to diphenhydramine N-glucuronide or N-demethylated by CYP2D6, CYP1A2, CYP2C9, and CYP2C19 to N-desmethyldiphenhydramine. N-desmethyldiphenhydramine can be N-demethylated again by the same enzymes to N,N-didesmethyldiphenhydramine, which undergoes oxidative deamination to form diphenylmethoxyacetic acid.

来源:DrugBank

代谢

抗组胺药的代谢命运研究仅限于少数几种化合物。代谢转化主要发生在肝脏。

EXTENSIVE STUDIES OF METABOLIC FATE OF ANTIHISTAMINES HAVE BEEN LIMITED TO A FEW COMPD. ... MAIN SITE OF METABOLIC TRANSFORMATION IS LIVER. /ANTIHISTAMINES/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 肝毒性

尽管二苯羟醇广泛使用，但它并未与肝功能测试异常或临床上明显的肝损伤有关联。其安全性可能与使用时限有关。 可能性评分：E（不太可能是临床上明显肝损伤的原因）。 关于抗组胺药的安全性和潜在肝毒性的参考资料，在抗组胺药概述部分之后给出。 药物类别：抗组胺药

Despite widespread use, dimenhydrinate has not been linked to liver test abnormalities or to clinically apparent liver injury. The reason for its safety may relate to its limited duration of use. Likelihood score: E (unlikely to be a cause of clinically apparent liver injury). References on the safety and potential hepatotoxicity of antihistamines are given together after the Overview section on Antihistamines. Drug Class: Antihistamines

来源:LiverTox

毒理性

• 药物性肝损伤

化合物：盐酸苯海拉明

Compound:dimenhydrinate

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

毒理性

• 药物性肝损伤

参考文献：M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. 美国食品药品监督管理局批准的药物标签用于研究药物诱导的肝损伤，《药物发现今日》，16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank：按人类发展药物诱导肝损伤风险排名的最大参考药物清单。《药物发现今日》2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015

References:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-Approved Drug Labeling for the Study of Drug-Induced Liver Injury, Drug Discovery Today, 16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today 2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

吸收、分配和排泄

• 吸收

一片50毫克的口服薄膜包衣片在2.7小时达到最高血药浓度72.6纳克/毫升。一枚100毫克的栓剂在5.3小时达到最高血药浓度112.2纳克/毫升。

A 50 mg oral film coated tablet reaches a Cmax of 72.6 ng/mL with a Tmax of 2.7 hours. A 100 mg suppository reaches a Cmax of 112.2 ng/mL with a Tmax of 5.3 hours.

来源:DrugBank

吸收、分配和排泄

• 消除途径

盐酸苯海拉明片说明书【适应症】用于皮肤黏膜的过敏性疾病，如荨麻疹、枯草热，过敏性鼻炎等。亦可用于预防晕船、晕车、晕飞机等晕动病。 【不良反应】（1）常见不良反应有嗜睡、口干、多尿、偶见有焦躁、失眠。（2）少数患者有药疹、药热、溶血性贫血、粒细胞减少等过敏反应，但周围神经炎等副作用极为罕见。

Dimenhydrinate is predominantly eliminated in the urine. 1-3% of the dissociated diphenhydramine is eliminated in the urine unchanged, while 64% of diphenhydramine is eliminated in the urine as metabolites. The elimination of dimenhydrinate has not been fully studied.

来源:DrugBank

吸收、分配和排泄

• 分布容积

地美尼辛的分布体积为3-4升/千克。

The volume of distribution of dimenhydrinate is 3-4 L/kg.

来源:DrugBank

吸收、分配和排泄

DIMENHYDRINATE (ETHANOLAMINES): DURATION OF ACTION (HR) 4-6. /FROM TABLE/ 二甲羟拉明（乙醇胺类）：作用持续时间（小时）4-6。/来自表格/

DIMENHYDRINATE (ETHANOLAMINES): DURATION OF ACTION (HR) 4-6. /FROM TABLE/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

H1受体拮抗剂（抗组胺药）很容易从胃肠道和注射部位吸收。口服给药后，效果在15到30分钟内开始，1小时内完全发挥，持续大约3到6小时，尽管有些药效更持久。

H1 ANTAGONISTS ARE READILY ABSORBED FROM GI TRACT & PARENTERAL SITES OF ADMIN. FOLLOWING ORAL ADMIN, EFFECTS START WITHIN 15 TO 30 MIN, ARE FULLY DEVELOPED WITHIN 1 HR, & LAST ABOUT 3 TO 6 HR, ALTHOUGH SOME...ACT LONGER. /ANTIHISTAMINES/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• TSCA：
  Yes
• 危险品标志：
  Xn
• 安全说明：
  S22,S26,S36/37/39,S53
• 危险类别码：
  R22
• WGK Germany：
  3
• 海关编码：
  2933990090
• 危险性防范说明：
  P301+P312+P330
• 危险性描述：
  H302
• 储存条件：
  2-8°C

SDS

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Section 1. Chemical Product and Company Identification
Catalog
Dimenhydrinate
Common Name/ DI127
Number(s).
Trade Name
523-87-5
CAS#
Manufacturer
SPECTRUM CHEMICAL MFG. CORP. RTECS XH5082000
TSCA TSCA 8(b) inventory:
Dimenhydrinate
Commercial Name(s) Not available.
CI# Not available.
Synonym 8-Chloro-3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione compd.
IN CASE OF EMERGENCY
with 2-(diphenylmethoxy)-N,N-dimethylethanamine (1:1);
Anautine;
Andramine;
Aviomarin;
Dimenhydrinate;
Diphenhydramine 8-chlorotheophylline;
Diphenhydrinate;
Ethylamine, N,N-dimethyl-2-(diphenylmethoxy)-,
compd. with 8-chlorotheophylline;
Gravinol
Novamin;
Novamine;
Teodramin;
O-Benzhydryldimethylaminoethanol 8-chlorotheophyllinate;
Benzhydryl-beta-dimethylaminoethylether 8-chlorotheophylline;
2-(Benzhydryloxy)-N,N-dimethylethylamine
compd. with 8-chlorotheophylline;
Chloranautine;
8-Chlorotheophylline, compd.
with 2-(diphenylmethoxy)-N,N-dimethylethylamine (1:1);
Diamarin;
Dramamin;
Dramamine;
Dramarin;
Dramyl;
Dromyl;
Eldodram;
Gravinol (antiemetic);
Gravol;
Menhydrinate;
Neo-navigan;
Permital;
Supremal;
Travelin;
Travelmin;
Vomex A;
Xamamina
Chemical Name Theophylline, 8-chloro-, compd. with
2-(diphenylmethoxy)-N,N-dimethylethylamine (1:1)
Not available. CALL [phone]
Chemical Family
Dimenhydrinate
Chemical Formula C17H21NO.C7H7ClN4O2
SPECTRUM CHEMICAL MFG. CORP.

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Section 2.Composition and Information on Ingredients
Exposure Limits
TWA (mg/m3) STEL (mg/m3) CEIL (mg/m3) % by Weight
Name CAS #
1) Dimenhydrinate 523-87-5 100
Toxicological Data Not applicable.
on Ingredients

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Section 3. Hazards Identification
Potential Acute Health Effects Slightly hazardous in case of skin contact (irritant), of eye contact (irritant), of ingestion, of inhalation.
CARCINOGENIC EFFECTS: Not available.
Potential Chronic Health
MUTAGENIC EFFECTS: Mutagenic for bacteria and/or yeast.
Effects
TERATOGENIC EFFECTS: Not available.
DEVELOPMENTAL TOXICITY: Not available.
Repeated or prolonged exposure is not known to aggravate medical condition.

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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. Cold water may be used. 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. Cold water may be used.
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.
Not available.
Flash Points
Flammable Limits Not available.
Products of Combustion These products are carbon oxides (CO, CO2), nitrogen oxides (NO, NO2...), halogenated compounds.
Fire Hazards in Presence of Slightly flammable to flammable in presence of open flames and sparks, of shocks, of heat.
Various Substances
Explosion Hazards in Presence Risks of explosion of the product in presence of mechanical impact: Not available.
Risks of explosion of the product in presence of static discharge: Not available.
of Various Substances
Dimenhydrinate
Fire Fighting Media SMALL FIRE: Use DRY chemical powder.
LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
and Instructions
Special Remarks on Material in powder form, capable of creating a dust explosion.
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 explosion hazard.
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.

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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
ingest. Do not breathe dust. Wear suitable protective clothing. If ingested, seek medical advice immediately
and show the container or the label. Keep away from incompatibles such as oxidizing agents.
Keep container tightly closed. Keep container in a cool, well-ventilated area.
Storage

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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
a Large Spill used 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 powder.) Odor Odorless.
Taste Not available.
Molecular Weight 469.96 g/mole
Color White.
pH (1% soln/water) Not available.
Not available.
Boiling Point
Melting Point 102-107°C (215.6-224.6°F)
Not available.
Critical Temperature
Specific Gravity Not available.
Vapor Pressure Not applicable.
Vapor Density Not available.
Volatility Not available.
Not available.
Odor Threshold
Water/Oil Dist. Coeff. Not available.
Not available.
Ionicity (in Water)
Dispersion Properties Not available.
Dimenhydrinate
Solubility Soluble in cold water.
Freely soluble in alcohol.
Soluble in chloroform , benzene.
Insoluble in diethyl ether.

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Section 10. Stability and Reactivity Data
Stability The product is stable.
Not available.
Instability Temperature
Conditions of Instability Excess heat, dust generation, incompatible materials
Incompatibility with various Reactive with oxidizing agents.
substances
Corrosivity Non-corrosive in presence of glass.
Not available.
Special Remarks on
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 MUTAGENIC EFFECTS: Mutagenic for bacteria and/or yeast.
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 May affect genetic material (mutagenic)
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.
Ingestion: May be harmul is swallowed. May cause dry mouth, adbominal distress vomiting, nausea,
diarrhea or constipaton, anorexia. May affect behavior (central nervous system (drowsiness, lethargy, fatigue.
excitement, hallucinations; hypnosis, convulsions, coma), cardiovascular system (cardiac arrhythmias).

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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 as toxic as the product itself.
of Biodegradation
Special Remarks on the Not available.
Products of Biodegradation
Dimenhydrinate

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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
California prop. 65: This product contains the following ingredients for which the State of California has found
Federal and State
to cause birth defects which would require a warning under the statute: No products were found.
Regulations
TSCA 8(b) inventory: Dimenhydrinate
California California prop. 65: This product contains the following ingredients for which the State of California has
Proposition 65 found to cause cancer which would require a warning under the statute: No products were found.
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 EINECS: This product is on the European Inventory of Existing Commercial Chemical Substances (EINECS
No. 208-350-8).
Canada: Listed on Canadian Domestic Substance List (DSL).
China: Not listed on National Inventory.
Japan: Not listed on National Inventory (ENCS).
Korea: Listed on National Inventory (KECI).
Philippines: Listed on National Inventory (PICCS).
Australia: Listed on AICS.
WHMIS (Canada) Not controlled under WHMIS (Canada).
Other Classifications
DSCL (EEC) R22- Harmful if swallowed. S46- If swallowed, seek medical advice
immediately and show this container or label.
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)
Dimenhydrinate
TDG (Canada)
(Pictograms)
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

茶苯海明为苯海拉明和8-氯茶碱的复盐。其抗组织胺作用较苯海拉明弱，但抗晕动病及镇吐作用较强。主要用于防治晕动病导致的恶心、呕吐、眩晕以及梅尼埃综合征。对放射治疗、妊娠期间、手术后、内耳炎和某些药物（如链霉素）引起的眩晕、呕吐也有疗效。

性状 茶苯海明是一种白色透明结晶性粉末，无臭味，微溶于水，易溶于乙醇。

作用 茶苯海明为一种复盐，其作用与盐酸苯海拉明相似，但抗组胺作用较弱。它能抑制延脑催吐化学感受区，并具有一定的中枢抑制和抗胆碱作用，从而产生镇静和止吐效果。口服后吸收迅速且完全，15～60分钟起效，作用可持续3 ～6小时，消除相半衰期（t1/2β）为4 ～6小时，血浆蛋白结合率高。主要在肝脏代谢，并以代谢物形式从尿中排泄。肝功能不全的患者服用本品时，需减量使用。

药物相互作用

1. 服药后不得饮酒，也不得与其他中枢神经抑制药合用。
2. 茶苯海明可增强乙醇、中枢神经抑制剂和三环类抗抑郁药的效果。它能短暂地影响巴比妥类和磺胺醋酰钠的吸收；与对氨基水杨酸钠同服时，可能降低后者的血药浓度。
3. 与食物或牛奶同服，可减少药物对胃部的刺激。

注意事项

1. 对本品成分或其他乙醇胺类药物过敏者、新生儿及早产儿禁用。
2. 孕妇在妊娠初期4个月内服用茶苯海明，胎儿先天性心血管异常和腹股沟疝的发生率可能增高。因此，在妊娠初期不宜使用该药。
3. 茶苯海明的止吐作用可能会干扰阑尾炎和药物引起的反应诊断。
4. 用药后可能出现嗜睡、注意力不集中等症状，不宜驾驶车辆或操作高难度机械设备。

不良反应 茶苯海明毒性较低，但大剂量时可能导致嗜睡。偶尔会引起皮疹，长期使用可能引起造血系统疾病。

以上关于茶苯海明的性状、作用、药物相互作用、注意事项和不良反应是由Chemicalbook的侍艳编辑整理。（2015-10-23）

用途 晕车药

适用于晕动症、妊娠期间、放射治疗后、手术后的恶心、呕吐及眩晕等症状。

文献信息

• [EN] 3,5-DIAMINO-6-CHLORO-N-(N-(4-PHENYLBUTYL)CARBAMIMIDOYL) PYRAZINE-2- CARBOXAMIDE COMPOUNDS<br/>[FR] COMPOSÉS 3,5-DIAMINO -6-CHLORO-N-(N- (4-PHÉNYLBUTYL)CARBAMIMIDOYL) PYRAZINE-2-CARBOXAMIDE
  申请人：PARION SCIENCES INC

  公开号：WO2014099673A1

  公开（公告）日：2014-06-26

  The present invention relates compounds of the formula: or pharmaceutically acceptable salts thereof, useful as sodium channel blockers, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including cystic fibrosis, chronic obstructive pulmonary disease, asthma, bronchiectasis, acute and chronic bronchitis, emphysema, and pneumonia.

  本发明涉及以下化合物的公式：或其药学上可接受的盐，用作钠通道阻滞剂，以及含有这些化合物的组合物，制备这些化合物的方法，以及在促进粘膜表面水合和治疗包括囊性纤维化、慢性阻塞性肺病、哮喘、支气管扩张、急性和慢性支气管炎、肺气肿和肺炎等疾病的治疗方法。
• CHLORO-PYRAZINE CARBOXAMIDE DERIVATIVES WITH EPITHELIAL SODIUM CHANNEL BLOCKING ACTIVITY
  申请人：Parion Sciences, Inc.

  公开号：US20140171447A1

  公开（公告）日：2014-06-19

  This invention provides compounds of the formula I: and their pharmaceutically acceptable salts, useful as sodium channel blockers, compositions containing the same, therapeutic methods and uses for the same and processes for preparing the same.

  这项发明提供了式I的化合物及其药用盐，可用作钠通道阻滞剂，包含这些化合物的组合物，以及用于这些化合物的治疗方法和用途，以及制备这些化合物的方法。
• Dual Pharmacophores - PDE4-Muscarinic Antagonistics
  申请人：Callahan James Francis

  公开号：US20090203657A1

  公开（公告）日：2009-08-13

  The present invention is directed to novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use as dual chromaphores having inhibitory activity against PDE4 and muscarinic acetylcholine receptors (mAChRs), and thus being useful for treating respiratory diseases.

  本发明涉及具有式（I）的新化合物及其药用盐，药物组合物及其用作对PDE4和肌胆碱受体（mAChRs）具有抑制活性的双色素，因此可用于治疗呼吸道疾病。
• [EN] DUAL PHARMACOPHORES - PDE4-MUSCARINIC ANTAGONISTICS<br/>[FR] PHARMACOPHORES DUALS, ANTAGONISTES DES RÉCEPTEURS MUSCARINIQUES ET INHIBITEURS DE L'ACTIVITÉ PDE4
  申请人：GLAXO GROUP LTD

  公开号：WO2009100169A1

  公开（公告）日：2009-08-13

  The present invention is directed to novel compounds of Formula's (I) - (VI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of and/or prophylaxis of respiratory diseases, including inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.

  本发明涉及式(I) - (VI)的新化合物，以及其药学上可接受的盐、药物组合物及其在治疗中的应用，例如作为磷酸二酯酶IV (PDE4)的抑制剂和肌碱乙酰胆碱受体 (mAChRs)的拮抗剂，用于治疗和/或预防呼吸道疾病，包括炎症性和/或过敏性疾病，如慢性阻塞性肺病（COPD）、哮喘、鼻炎（例如过敏性鼻炎）、特应性皮炎或银屑病。
• SULFOXIMINE SUBSTITUTED QUINAZOLINES FOR PHARMACEUTICAL COMPOSITIONS
  申请人：BLUM Andreas

  公开号：US20140135309A1

  公开（公告）日：2014-05-15

  This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R 1 and R 2 are as defined herein, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.

  这项发明涉及公式I的新型磺酰胺取代的喹唑啉衍生物，其中Ar、R1和R2如本文所定义，并且它们作为MNK1（MNK1a或MNK1b）和/或MNK2（MNK2a或MNK2b）激酶抑制剂的用途，含有这些化合物的药物组合物，以及将其用作治疗或改善MNK1（MNK1a或MNK1b）和/或MNK2（MNK2a或MNK2b）介导的疾病的药剂的方法。

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