三氯噻嗪 | 133-67-5

• 物质功能分类: 原料药 - 泌尿系统用药 - 利尿药
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻二嗪
• 中文名称: 三氯噻嗪
• 中文别名: 6-氯-3-(二氯甲基)-3,4-二氢-7-氨基磺酰基-1,2,4-苯并噻二嗪-1,1-二氧化物
• 英文名称: trichloromethiazide
• 英文别名: Trichlormethiazide；(3RS)-6-chloro-3-dichloromethyl-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide；trichloromethazide；trichlormethazide；SJ000286143；6-chloro-3-(dichloromethyl)-1,1-dioxo-3,4-dihydro-2H-1λ6,2,4-benzothiadiazine-7-sulfonamide
• CAS: 133-67-5
• 化学式: C₈H₈Cl₃N₃O₄S₂
• mdl: MFCD00057315
• 分子量: 380.66
• InChiKey: LMJSLTNSBFUCMU-UHFFFAOYSA-N

物化性质

• 熔点：
  248-250℃
• 沸点：
  631.3±65.0 °C(Predicted)
• 密度：
  1.748
• 溶解度：
  可溶于DMSO（少许）、甲醇（少许）
• 物理描述：
  Solid
• 颜色/状态：
  CRYSTALS FROM METHANOL + ACETONE + WATER
• 气味：
  ODORLESS OR HAS SLIGHT CHARACTERISTIC ODOR
• 水溶性：
  -2.68
• 稳定性/保质期：
  LIGHT-SENSITIVE, BUT STABLE IN AIR & HEAT
• 分解：
  When heated to decomposition it emits very toxic fumes such as sulfoxides, /hydrogen chloride/, and nitroxides.
• 解离常数：
  PKA: 8.6

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  135
• 氢给体数：
  3
• 氢受体数：
  7

ADMET

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用总结：目前没有关于母乳中三氯甲噻嗪含量的信息。大剂量强力利尿可能会减少母乳产量。在低剂量下，其他利尿剂比三氯甲噻嗪更受欢迎。 ◉ 对哺乳婴儿的影响：截至修订日期，没有找到相关的已发布信息。 ◉ 对泌乳和母乳的影响：截至修订日期，没有找到关于三氯甲噻嗪的相关已发布信息。噻嗪类和噻嗪样利尿剂的强力利尿、限制液体摄入和乳房束缚已被用来抑制产后泌乳。利尿剂对这些有效抑制泌乳的措施的贡献尚未进行研究。目前没有关于利尿剂对已建立、正在进行的泌乳影响的数据。

◉ Summary of Use during Lactation:No information is available on the amount of trichlormethiazide in breastmilk. Intense diuresis with large doses may decrease breastmilk production. Other diuretics in low doses are preferred over trichlormethiazide. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk:Relevant published information on trichlormethiazide was not found as of the revision date. Intense diuresis with thiazides and thiazide-like diuretics, fluid restriction and breast binding have been used to suppress postpartum lactation. The added contribution of the diuretic to these measures, which are effective in suppressing lactation, has not been studied. There are no data on the effects of diuretics on established, ongoing lactation.

来源:Drugs and Lactation Database (LactMed)

毒理性

• 相互作用

许多使用氯丙酰胺或其他磺酰脲类药物控制血糖的糖尿病患者，在加入任何噻嗪类利尿剂到药物治疗方案时，会出现糖尿病控制受损的情况。/噻嗪类利尿剂/

MANY DIABETIC PATIENTS REGULATED BY CHLORPROPAMIDE OR OTHER SULFONYLUREAS EXHIBIT IMPAIRED DIABETIC CONTROL WHEN ANY THIAZIDE DIURETIC IS ADDED TO DRUG REGIMEN. /THIAZIDE DIURETICS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

诸如...噻嗪类利尿剂...这类药物可以提高尿液的pH值，可能有助于增加奎尼丁的脂溶性以及其在肾小管的重吸收，从而延长其治疗效应。/噻嗪类利尿剂/

...DRUGS SUCH AS...THIAZIDE DIURETICS...WHICH INCR URINARY PH, MAY SERVE TO INCR LIPID SOLUBILITY & TUBULAR REABSORPTION OF QUINIDINE & THUS PROLONG ITS THERAPEUTIC EFFECTS. /THIAZIDE DIURETICS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

噻嗪类利尿剂会增加锂的心脏毒性和神经毒性，这些药物不应同时使用。/噻嗪类/

...THIAZIDE DIURETICS ENHANCE CARDIOTOXIC & NEUROTOXIC EFFECTS OF LITHIUM & THESE DRUGS SHOULD NOT BE ADMINISTERED CONCURRENTLY. /THIAZIDES/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

噻嗪类药物增强胍乙啶的抗高血压作用，使得胍乙啶的剂量可以降低并减少不良反应的发生率，尤其是直立性和运动相关的低血压。/噻嗪类药物/

THIAZIDES ENHANCE ANTIHYPERTENSIVE ACTION OF GUANETHIDINE, ALLOWING DOSE OF GUANETHIDINE TO BE REDUCED & DECR INCIDENCE OF ADVERSE REACTIONS, PARTICULARLY ORTHOSTATIC & EXERCISE-ASSOC HYPOTENSION. /THIAZIDES/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

三氯甲噻嗪从胃肠道吸收。关于三氯甲噻嗪吸收程度和在体内的去向的信息很少，尽管它被认为主要是以未改变的药物形式通过尿液排出体外。

Trichlormethiazide is absorbed from the GI tract. Little information is available on the extent of absorption and the fate of trichlormethiazide in the body, although it is believed to be excreted principally as unchanged drug in urine.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

大多数化合物在3-6小时内迅速排泄。/噻嗪类利尿剂/

MOST CMPD ARE RAPIDLY EXCRETED WITHIN 3-6 HR. /THIAZIDE DIURETICS/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

利尿作用在2小时内发生，在6小时内达到高峰，并持续超过24小时。

DIURESIS OCCURS WITHIN 2 HR, REACHES PEAK IN 6 HR, & LASTS MORE THAN 24 HR.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

噻嗪类药物从胃肠道吸收，它们的有用性在很大程度上归功于它们通过口服途径的有效性。吸收相对较快。大多数药物在口服给药后一小时内显示出明显的利尿作用。/噻嗪利尿剂/

THIAZIDES ARE ABSORBED FROM GI TRACT & OWE THEIR USEFULNESS LARGELY TO THEIR EFFECTIVENESS BY ORAL ROUTE. ABSORPTION IS RELATIVELY RAPID. MOST AGENTS SHOW DEMONSTRABLE DIURETIC EFFECT WITHIN HR AFTER ORAL ADMIN. /THIAZIDE DIURETICS/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

总的来说，具有相对较长作用时间的噻嗪类药物与血浆蛋白的结合程度较高，并且可以被肾小管再吸收......药物容易通过胎盘屏障到达胎儿。所有噻嗪类药物可能在近端小管进行积极分泌。/噻嗪类利尿剂/

IN GENERAL, THIAZIDES WITH RELATIVELY LONG DURATIONS OF ACTION SHOW PROPORTIONATELY HIGH DEGREE OF BINDING TO PLASMA PROTEINS & ARE REABSORBED... BY RENAL TUBULES. ... DRUG PASSES READILY THROUGH PLACENTAL BARRIER TO FETUS. ALL THIAZIDES PROBABLY UNDERGO ACTIVE SECRETION IN PROXIMAL TUBULE. /THIAZIDE DIURETICS/

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：
  R42/43
• WGK Germany：
  2
• 海关编码：
  2935009090
• RTECS号：
  DK8925000
• 包装等级：
  III
• 危险类别：
  6.1
• 危险性防范说明：
  P261,P280,P342+P311
• 危险品运输编号：
  2811
• 危险性描述：
  H317,H334
• 储存条件：
  室温

SDS

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Section 1. IDENTIFICATION OF THE SUBSTANCE/MIXTURE
Product identifiers
Product name : Trichlormethiazide
CAS-No. : 133-67-5
Relevant identified uses of the substance or mixture and uses advised against
Identified uses : Laboratory chemicals, Manufacture of substances

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Section 2. HAZARDS IDENTIFICATION
Classification of the substance or mixture
Classification according to Regulation (EC) No 1272/2008 [EU-GHS/CLP]
Respiratory sensitization (Category 1)
Skin sensitization (Category 1)
Classification according to EU Directives 67/548/EEC or 1999/45/EC
May cause sensitization by inhalation and skin contact.
Label elements
Labelling according Regulation (EC) No 1272/2008 [CLP]
Pictogram
Signal word Danger
Hazard statement(s)
H317 May cause an allergic skin reaction.
H334 May cause allergy or asthma symptoms or breathing difficulties if inhaled.
Precautionary statement(s)
P261 Avoid breathing dust/ fume/ gas/ mist/ vapours/ spray.
P280 Wear protective gloves.
P342 + P311 If experiencing respiratory symptoms: Call a POISON CENTER or doctor/
physician.
Supplemental Hazard none
Statements
According to European Directive 67/548/EEC as amended.
Hazard symbol(s)
R-phrase(s)
R42/43 May cause sensitization by inhalation and skin contact.
S-phrase(s)
S36 Wear suitable protective clothing.
Other hazards
Photosensitizer.

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Section 3. COMPOSITION/INFORMATION ON INGREDIENTS
Substances
Formula : C8H8Cl3N3O4S2
Molecular Weight : 380,66 g/mol
Component Concentration
Trichlormethiazide
CAS-No. 133-67-5 -
EC-No. 205-118-8

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Section 4. FIRST AID MEASURES
Description of first aid measures
General advice
Consult a physician. Show this safety data sheet to the doctor in attendance.
If inhaled
If breathed in, move person into fresh air. If not breathing, give artificial respiration. Consult a physician.
In case of skin contact
Wash off with soap and plenty of water. Consult a physician.
In case of eye contact
Flush eyes with water as a precaution.
If swallowed
Never give anything by mouth to an unconscious person. Rinse mouth with water. Consult a physician.
Most important symptoms and effects, both acute and delayed
Muscle cramps/spasms., Anorexia., Weakness, Central nervous system depression, Dermatitis, Nausea,
Dizziness, Headache, Vomiting, Diarrhoea
Indication of any immediate medical attention and special treatment needed
no data available

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Section 5. FIREFIGHTING MEASURES
Extinguishing media
Suitable extinguishing media
Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide.
Special hazards arising from the substance or mixture
Carbon oxides, nitrogen oxides (NOx), Sulphur oxides, Hydrogen chloride gas
Advice for firefighters
Wear self contained breathing apparatus for fire fighting if necessary.
Further information
no data available

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Section 6. ACCIDENTAL RELEASE MEASURES
Personal precautions, protective equipment and emergency procedures
Use personal protective equipment. Avoid dust formation. Avoid breathing vapors, mist or gas. Ensure
adequate ventilation. Evacuate personnel to safe areas. Avoid breathing dust.
Environmental precautions
Do not let product enter drains.
Methods and materials for containment and cleaning up
Pick up and arrange disposal without creating dust. Sweep up and shovel. Keep in suitable, closed
containers for disposal.
Reference to other sections
For disposal see section 13.

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Section 7. HANDLING AND STORAGE
Precautions for safe handling
Avoid contact with skin and eyes. Avoid formation of dust and aerosols.
Provide appropriate exhaust ventilation at places where dust is formed.Normal measures for preventive fire
protection.
Conditions for safe storage, including any incompatibilities
Store in cool place. Keep container tightly closed in a dry and well-ventilated place.
Specific end uses
no data available

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Section 8. EXPOSURE CONTROLS/PERSONAL PROTECTION
Control parameters
Components with workplace control parameters
Exposure controls
Appropriate engineering controls
Handle in accordance with good industrial hygiene and safety practice. Wash hands before breaks and
at the end of workday.
Personal protective equipment
Eye/face protection
Face shield and safety glasses Use equipment for eye protection tested and approved under
appropriate government standards such as NIOSH (US) or EN 166(EU).
Skin protection
Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique
(without touching glove's outer surface) to avoid skin contact with this product. Dispose of
contaminated gloves after use in accordance with applicable laws and good laboratory practices.
Wash and dry hands.
The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and
the standard EN 374 derived from it.
Body Protection
Complete suit protecting against chemicals, The type of protective equipment must be selected
according to the concentration and amount of the dangerous substance at the specific workplace.
Respiratory protection
For nuisance exposures use type P95 (US) or type P1 (EU EN 143) particle respirator.For higher
level protection use type OV/AG/P99 (US) or type ABEK-P2 (EU EN 143) respirator cartridges.
Use respirators and components tested and approved under appropriate government standards
such as NIOSH (US) or CEN (EU).

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Section 9. PHYSICAL AND CHEMICAL PROPERTIES
Information on basic physical and chemical properties
a) Appearance Form: solid
b) Odour no data available
c) Odour Threshold no data available
d) pH no data available
e) Melting point/freezing no data available
point
f) Initial boiling point and no data available
boiling range
g) Flash point no data available
h) Evaporation rate no data available
i) Flammability (solid, gas) no data available
j) Upper/lower no data available
flammability or
explosive limits
k) Vapour pressure no data available
l) Vapour density no data available
m) Relative density no data available
n) Water solubility no data available
o) Partition coefficient: n- no data available
octanol/water
p) Autoignition no data available
temperature
q) Decomposition no data available
temperature
r) Viscosity no data available
s) Explosive properties no data available
t) Oxidizing properties no data available
Other safety information
no data available

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Section 10. STABILITY AND REACTIVITY
Reactivity
no data available
Chemical stability
no data available
Possibility of hazardous reactions
no data available
Conditions to avoid
no data available
Incompatible materials
no data available
Hazardous decomposition products
Other decomposition products - no data available

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Section 11. TOXICOLOGICAL INFORMATION
Information on toxicological effects
Acute toxicity
LD50 Oral - rat - 5.600 mg/kg
Skin corrosion/irritation
no data available
Serious eye damage/eye irritation
no data available
Respiratory or skin sensitization
no data available
May cause allergic respiratory and skin reactions
Germ cell mutagenicity
Genotoxicity in vitro - Hamster - Lungs
Cytogenetic analysis
Genotoxicity in vitro - Hamster - fibroblast
Cytogenetic analysis
Carcinogenicity
IARC: No component of this product present at levels greater than or equal to 0.1% is identified as
probable, possible or confirmed human carcinogen by IARC.
Reproductive toxicity
no data available
Specific target organ toxicity - single exposure
no data available
Specific target organ toxicity - repeated exposure
no data available
Aspiration hazard
no data available
Potential health effects
Inhalation May be harmful if inhaled. May cause respiratory tract irritation.
Ingestion May be harmful if swallowed.
Skin May be harmful if absorbed through skin. May cause skin irritation.
Eyes May cause eye irritation.
Signs and Symptoms of Exposure
Muscle cramps/spasms., Anorexia., Weakness, Central nervous system depression, Dermatitis, Nausea,
Dizziness, Headache, Vomiting, Diarrhoea
Additional Information
RTECS: DK8925000

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Section 12. ECOLOGICAL INFORMATION
Toxicity
no data available
Persistence and degradability
no data available
Bioaccumulative potential
no data available
Mobility in soil
no data available
Results of PBT and vPvB assessment
no data available
Other adverse effects
no data available

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Section 13. DISPOSAL CONSIDERATIONS
Waste treatment methods
Product
Offer surplus and non-recyclable solutions to a licensed disposal company. Contact a licensed
professional waste disposal service to dispose of this material. Dissolve or mix the material with a
combustible solvent and burn in a chemical incinerator equipped with an afterburner and scrubber.
Contaminated packaging
Dispose of as unused product.

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Section 14. TRANSPORT INFORMATION
UN number
ADR/RID: - IMDG: - IATA: -
UN proper shipping name
ADR/RID: Not dangerous goods
IMDG: Not dangerous goods
IATA: Not dangerous goods
Transport hazard class(es)
ADR/RID: - IMDG: - IATA: -
Packaging group
ADR/RID: - IMDG: - IATA: -
Environmental hazards
ADR/RID: no IMDG Marine pollutant: no IATA: no
Special precautions for user
no data available

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SECTION 15 - REGULATORY INFORMATION
N/A

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

生物活性

Trichlormethiazide 是一种利尿剂，其特性与 Hydrochlorothiazide 相似。

体内研究

在高盐摄入 (HS) 大鼠中，通过静脉注射 Trichlormethiazide (10 mg/kg，每日一次，共5天)，24小时内显著降低了在接受血管紧张素 II 的大鼠的平均动脉压 (MAP)，但在其他组别并未观察到此效果。

实验模型：

• 动物种类与体重：雄性 Sprague-Dawley 大鼠（350-450 g）
• 剂量：10 mg/kg
• 给药途径与频率：静脉注射，每日一次，共 15 天
• 结果：显著降低了同时接受血管紧张素 II 和高盐摄入大鼠的 MAP。

用途

利尿剂。

反应信息

• 作为反应物：
  描述：

  三氯噻嗪 以 乙醇 为溶剂， 生成 3-Dichloromethylhydrothiazide
  参考文献：
  名称：

  Ulvi; Mesilaakso; Matikainen, Pharmazie, 1996, vol. 51, # 10, p. 774 - 775

  摘要：

  DOI：
• 作为产物：
  描述：

  5-氯-2,4-二磺酰胺基苯胺 、 二氯乙醛 在 盐酸 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 三氯噻嗪
  参考文献：
  名称：

  CRAVERI; ZONI, Bollettino Chimico Farmaceutico, 1961, vol. 100, p. 956 - 971

  摘要：

  DOI：

文献信息

• DISUBSTITUTED TRIFLUOROMETHYL PYRIMIDINONES AND THEIR USE
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20160221965A1

  公开（公告）日：2016-08-04

  The present application relates to novel 2,5-disubstituted 6-(trifluoromethyl)pyrimidin-4(3H)-one derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular, renal, inflammatory and fibrotic diseases.

  本申请涉及新颖的2,5-二取代6-(三氟甲基)嘧啶-4(3H)-酮衍生物，其制备方法，其单独或与其他药物联合用于治疗和/或预防疾病，以及用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管、肾脏、炎症和纤维化疾病。
• NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME
  申请人：Ryono Denis E.

  公开号：US20080009465A1

  公开（公告）日：2008-01-10

  Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring; R 4 is —(CH 2 ) n -Z-(CH 2 ) m —PO(OR 7 )(OR 8 ), —(CH 2 ) n Z-(CH 2 ) m —PO(OR 7 )R g , —(CH 2 ) n -Z-(CH 2 ) m —OPO(OR 7 )R g , —(CH 2 ) n Z—(CH 2 ) m —OPO(R 9 )(R 10 ), or —(CH 2 ) n Z—(CH 2 ) m —PO(R 9 )(R 10 ); R 5 and R 6 are independently selected from H, alkyl and halogen; Y is R 7 (CH 2 ) s or is absent; and X, n, Z, m, R 4 , R 5 , R 6 , R 7 , and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

  提供了磷酸酯和磷酸酯激活剂，因此在治疗糖尿病和相关疾病方面非常有用，并具有以下结构： 其中 是杂环芳基环； R 4 为—(CH 2 ) n -Z-(CH 2 ) m —PO(OR 7 )(OR 8 )、—(CH 2 ) n Z-(CH 2 ) m —PO(OR 7 )R g 、—(CH 2 ) n -Z-(CH 2 ) m —OPO(OR 7 )R g 、—(CH 2 ) n Z—(CH 2 ) m —OPO(R 9 )(R 10) 或—(CH 2 ) n Z—(CH 2 ) m —PO(R 9 )(R 10) ； R 5 和R 6 分别选择自H、烷基和卤素； Y为R 7 (CH 2 ) s 或不存在；以及 X、n、Z、m、R 4 、R 5 、R 6 、R 7 和s如本文所定义；或其药用盐。 还提供了一种利用上述化合物治疗糖尿病和相关疾病的方法。
• [EN] HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF STRESS-RELATED CONDITIONS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES POUR LE TRAITEMENT D'ÉTATS LIÉS AU STRESS
  申请人：OTSUKA PHARMA CO LTD

  公开号：WO2010137738A1

  公开（公告）日：2010-12-02

  The present invention provides a novel heterocyclic compound. A heterocyclic compound represented by general formula (1) wherein, R1 and R2, each independently represent hydrogen; a phenyl lower alkyl group that may have a substituent(s) selected from the group consisting of a lower alkyl group and the like on a benzene ring and/or a lower alkyl group; or a cyclo C3-C8 alkyl lower alkyl group; or the like; R3 represents a lower alkynyl group or the like; R4 represents a phenyl group that may have a substituent(s) selected from the group consisting of a 1,3,4-oxadiazolyl group that may have e.g., halogen or a heterocyclic group selected from pyridyl group and the like; the heterocyclic group may have at least one substituent(s) selected from a lower alkoxy group and the like or a salt thereof.

  本发明提供了一种新颖的杂环化合物。一种由通式（1）表示的杂环化合物，其中，R1和R2分别独立表示氢；苯基较低烷基基团，可能在苯环和/或较低烷基基团上具有从较低烷基基团等组成的取代基；或环C3-C8烷基较低烷基基团；或类似物；R3表示较低炔基基团或类似物；R4表示可能具有从1,3,4-噁二唑基团（例如，卤素）或从吡啶基团等组成的取代基的苯基团；所述杂环基可能具有至少一个从较低烷氧基等选择的取代基或其盐。
• PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLES AND THEIR USE IN CANCER THERAPY
  申请人：Rewcastle Gordon William

  公开号：US20110009405A1

  公开（公告）日：2011-01-13

  Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.

  本文提供了式I的嘧啶基和1,3,5-三嗪基苯并咪唑化合物，以及它们的药物组合物、制备方法，以及作为抗癌治疗药物或药剂的用途，可以单独使用，也可以与放疗和/或其他抗癌药物联合使用。
• Dibenzyl Amine Compounds and Derivatives
  申请人：Chang George

  公开号：US20070213371A1

  公开（公告）日：2007-09-13

  Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

  二苯基胺化合物及其衍生物，含有这种化合物的药物组合物以及使用这种化合物提高某些血浆脂质水平，包括高密度脂蛋白胆固醇，并降低其他一些血浆脂质水平，如低密度脂蛋白胆固醇和甘油三酯，并据此治疗由高密度脂蛋白胆固醇水平低和/或低密度脂蛋白胆固醇和甘油三酯水平高加重的疾病，如动脉粥样硬化和心血管疾病在某些哺乳动物，包括人类。

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