盐酸阿那格雷 - CAS号 58579-51-4

物化性质

熔点：

>280°C
溶解度：

DMSO：可溶1mg/mL，澄清（加热）
碰撞截面：

147.9 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

计算性质

辛醇/水分配系数(LogP)：

1.94
重原子数：

17
可旋转键数：

0
环数：

3.0
sp3杂化的碳原子比例：

0.2
拓扑面积：

44.7
氢给体数：

2
氢受体数：

2

安全信息

危险品标志：

Xn
安全说明：

S26
危险类别码：

R22,R36/37/38
WGK Germany：

3
海关编码：

2933990090
危险标志：

GHS07
危险性描述：

H302,H315,H319,H335
危险性防范说明：

P261,P305 + P351 + P338
储存条件：

Dehydrate at +4°C

SDS

SDS：5e75dbd885503015d68e0e856384e2c9

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SECTION 1: Identification of the substance/mixture and of the company/undertaking
Product identifiers
Product name : Anagrelide hydrochloride
REACH No. : A registration number is not available for this substance as the substance
or its uses are exempted from registration, the annual tonnage does not
require a registration or the registration is envisaged for a later
registration deadline.
CAS-No. : 58579-51-4
Relevant identified uses of the substance or mixture and uses advised against
Identified uses : Laboratory chemicals, Manufacture of substances

SECTION 2: Hazards identification
Classification of the substance or mixture
Classification according to Regulation (EC) No 1272/2008
Acute toxicity, Oral (Category 4), H302
Skin irritation (Category 2), H315
Eye irritation (Category 2), H319
Specific target organ toxicity - single exposure (Category 3), Respiratory system, H335
For the full text of the H-Statements mentioned in this Section, see Section 16.
Classification according to EU Directives 67/548/EEC or 1999/45/EC
Xn Harmful R22, R36/37/38
For the full text of the R-phrases mentioned in this Section, see Section 16.
Label elements
Labelling according Regulation (EC) No 1272/2008
Pictogram
Signal word Warning
Hazard statement(s)
H302 Harmful if swallowed.
H315 Causes skin irritation.
H319 Causes serious eye irritation.
H335 May cause respiratory irritation.
Precautionary statement(s)
P261 Avoid breathing dust.
P305 + P351 + P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove
contact lenses, if present and easy to do. Continue rinsing.
Supplemental Hazard none
Statements
Other hazards - none

SECTION 3: Composition/information on ingredients
Substances
Synonyms : 6,7-Dichloro-1,5-dihydro-imidazo[2,1-b]quinazolin-2(3H)-one
hydrochloride
Formula : C10H7Cl2N3O . HCl
Molecular Weight : 292,55 g/mol
CAS-No. : 58579-51-4
Hazardous ingredients according to Regulation (EC) No 1272/2008
Component Classification Concentration
Anagrelide hydrochloride
CAS-No. 58579-51-4 Acute Tox. 4; Skin Irrit. 2; Eye <= 100 %
Irrit. 2; STOT SE 3; H302,
H315, H319, H335
Hazardous ingredients according to Directive 1999/45/EC
Component Classification Concentration
Anagrelide hydrochloride
CAS-No. 58579-51-4 Xn, R22 - R36/37/38 <= 100 %
For the full text of the H-Statements and R-Phrases mentioned in this Section, see Section 16

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
Rinse thoroughly with plenty of water for at least 15 minutes and consult a physician.
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
The most important known symptoms and effects are described in the labelling (see section 2.2) and/or in
section 11
Indication of any immediate medical attention and special treatment needed
no data available

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
no data available
Advice for firefighters
Wear self contained breathing apparatus for fire fighting if necessary.
Further information
no data available

SECTION 6: Accidental release measures
Personal precautions, protective equipment and emergency procedures
Use personal protective equipment. Avoid dust formation. Avoid breathing vapours, mist or gas. Ensure
adequate ventilation. Evacuate personnel to safe areas. Avoid breathing dust.
For personal protection see section 8.
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.

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.
For precautions see section 2.2.
Conditions for safe storage, including any incompatibilities
Store in cool place. Keep container tightly closed in a dry and well-ventilated place.
Recommended storage temperature: 2 - 8 °C
Store with desiccant.
Specific end use(s)
A part from the uses mentioned in section 1.2 no other specific uses are stipulated

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
Safety glasses with side-shields conforming to EN166 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).
Control of environmental exposure
Do not let product enter drains.

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) Evapouration 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) Auto-ignition 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

SECTION 10: Stability and reactivity
Reactivity
no data available
Chemical stability
Stable under recommended storage conditions.
Possibility of hazardous reactions
no data available
Conditions to avoid
no data available
Incompatible materials
Strong oxidizing agents
Hazardous decomposition products
Other decomposition products - no data available
In the event of fire: see section 5

SECTION 11: Toxicological information
Information on toxicological effects
Acute toxicity
no data available
Skin corrosion/irritation
no data available
Serious eye damage/eye irritation
no data available
Respiratory or skin sensitisation
no data available
Germ cell mutagenicity
no data available
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
Additional Information
RTECS: Not available
To the best of our knowledge, the chemical, physical, and toxicological properties have not been
thoroughly investigated.

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
PBT/vPvB assessment not available as chemical safety assessment not required/not conducted
Other adverse effects
no data available

SECTION 13: Disposal considerations
Waste treatment methods
Product
Offer surplus and non-recyclable solutions to a licensed disposal company. 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.

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

SECTION 15: Regulatory information
This safety datasheet complies with the requirements of Regulation (EC) No. 1907/2006.
Safety, health and environmental regulations/legislation specific for the substance or mixture
no data available
Chemical Safety Assessment
For this product a chemical safety assessment was not carried out

SECTION 16: Other information
Full text of H-Statements referred to under sections 2 and 3.
Acute Tox. Acute toxicity
Eye Irrit. Eye irritation
H302 Harmful if swallowed.
H315 Causes skin irritation.
H319 Causes serious eye irritation.
H335 May cause respiratory irritation.
Skin Irrit. Skin irritation
Full text of R-phrases referred to under sections 2 and 3
Xn Harmful
R22 Harmful if swallowed.
R36/37/38 Irritating to eyes, respiratory system and skin.
Further information
Copyright 2013 Co. LLC. License granted to make unlimited paper copies for internal use
only.
The above information is believed to be correct but does not purport to be all inclusive and shall be
used only as a guide. The information in this document is based on the present state of our knowledge
and is applicable to the product with regard to appropriate safety precautions. It does not represent any
guarantee of the properties of the product. Corporation and its Affiliates shall not be held
liable for any damage resulting from handling or from contact with the above product. See
and/or the reverse side of invoice or packing slip for additional terms and conditions of sale.

制备方法与用途

药理作用

盐酸阿那格雷主要减缓骨髓内巨核细胞分化成熟，减少血小板生成，缓解原发性血小板增多症患者的临床症状。它不影响巨核细胞的分裂增殖，对DNA、RNA无伤害且无致癌性。非治疗剂量时，可作为血小板聚集抑制剂。

适应症

盐酸阿那格雷适用于治疗原发性血小板增多症、慢性粒细胞白血病、真红细胞性贫血等慢性骨髓增生性疾病中难以控制的血小板增多症状。

用法用量

成人通常每日4次，每次0.5 mg口服；或每日2次，每次1 mg。若疗效不佳，可每5～7天增加0.5 mg/d，最大剂量为10 mg/d，单次最大量为2.5 mg。老年人建议每日1次，每次0.5 mg，每周逐步增加0.5 mg/d；肾肝功能异常者应每日分两次，每次0.5 mg口服。用药前1小时及用药后避免摄入咖啡因。开始使用阿那格雷的第1周，需每2～3天检查一次血小板数量，并在维持剂量期间每周进行1次检查。

不良反应

约有25%至37%接受盐酸阿那格雷治疗的患者会出现不同程度的不良反应，主要包括头痛、低血压、腹泻、体液潴留、心悸、心律失常、咳嗽、恶心及呕吐等。这些症状大多轻微且多在早期自行缓解；约10%的患者因严重不良反应而停止使用该药。长期治疗可能引起轻微短暂贫血，罕见情况下可导致严重的过敏性肺炎和充血性心力衰竭。阿那格雷产生抗凝作用所需的剂量比其用于抗血小板时要高约10倍，因此常规使用的抗血小板剂量不会影响血小板的凝血功能。

生物活性

盐酸阿那格雷（BL-4162A）是一种口服imidazoquinazoline类药物，具有抑制环腺苷酸磷酸二酯酶的活性，在人类及动物模型中均能有效抑制血小板聚集。其通过抑制巨核细胞分化为成熟的血小板来发挥作用。

靶点

Target	Value
PDE

体内研究

盐酸阿那格雷（BL-4162A）是一种口服imidazoquinazoline类药物，具有抑制环腺苷酸磷酸二酯酶的活性，并在人类和动物中能够有效抑制血小板聚集。通过抑制巨核细胞分化为成熟的血小板来起作用。

反应信息

作为反应物：

描述：

甲酸、盐酸阿那格雷以5.83 g的产率得到anagrelide hemiformate

参考文献：

名称：

[EN] PROCESS FOR MAKING ANAGRELIDE
[FR] PROCÉDÉ DE PRÉPARATION D'ANAGRÉLIDE

摘要：

该发明涉及一种制备和纯化药用活性化合物阿格雷利特（分子式为(1)）的方法。该方法基于将阿格雷利特或其酸盐转化为阿格雷利特的甲酸盐，特别是阿格雷利特半甲酸盐。

公开号：

WO2014206484A1
作为产物：

描述：

(2-amino-5,6-dichloroquinazolin-3(4H)-yl)acetic acid methyl ester hydrochloride 在盐酸作用下，以水为溶剂，反应 1.0h，生成盐酸阿那格雷

参考文献：

名称：

[DE] VERWENDUNG VON 2-AMINO-2H-CHINAZOLIN-DERIVATEN ZUR HERSTELLUNG VON THERAPEUTISCHEN MITTELN
[EN] USE OF 2-AMINO-2H-QUINAZOLINE DERIVATIVES FOR PRODUCING THERAPEUTIC AGENTS
[FR] UTILISATION DE DERIVES DE 2-AMINO-2H-QUINAZOLINE POUR LA PREPARATION DE PRODUITS THERAPEUTIQUES

摘要：

这项发明涉及使用一般化学式(I)中的2-氨基-2H-喹唑啉衍生物，其中R1代表具有1-5个碳原子的烷基基团，R2、R3、R4和R5分别独立地代表氯或氢原子，以及它们的药用相容盐，用于制备治疗多发性增生性疾病、高血压和支气管扩张的药物。

公开号：

WO2004063172A1

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文献信息

Piperidine derivative rennin inhibitors

申请人：——

公开号：US20040204455A1

公开（公告）日：2004-10-14

Disclosed are piperidine derivatives, their manufacture and use as inhibitors of renin.

公开了哌啶衍生物，它们的制造方法及其作为肾素抑制剂的用途。
Combinations of lipid modulating agents and substituted azetidinones and treatments for vascular conditions

申请人：Graziano P. Michael

公开号：US20050096307A1

公开（公告）日：2005-05-05

The present invention provides compositions, therapeutic combinations and methods including: (a) at least one lipid modulating agent; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols or 5α-stanols.

本发明提供了包括以下内容的组合物、治疗组合和方法：(a)至少一种脂质调节剂；和(b)至少一种取代的噁唑烷酮或取代的β-内酰胺甾醇吸收抑制剂，可用于治疗血管疾病、糖尿病、肥胖以及降低血浆中甾醇或5α-甾烷醇的水平。
Combinations of substituted azetidinones and CB1 antagonists

申请人：Veltri P. Enrico

公开号：US20060069080A1

公开（公告）日：2006-03-30

The present invention provides compositions, therapeutic combinations and methods including: (a) at least one selective CB 1 antagonist; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity, metabolic syndrome and lowering plasma levels of sterols or 5α-stanols.

本发明提供了包括以下内容的组合物、治疗组合和方法：(a)至少一种选择性CB1拮抗剂；和(b)至少一种取代的氮杂环丁烷或取代的β-内酰胺甾醇吸收抑制剂，可用于治疗血管疾病、糖尿病、肥胖、代谢综合征以及降低血浆中的甾醇或5α-甾烷醇水平。
[EN] DIPHENYLAZETIDINONE DERIVATES PROCESSING CHOLESTEROL ABSORPTION INHIBITORY ACTIVITY<br/>[FR] DERIVES DIPHENYLAZETIDINONE PRESENTANT UNE ACTIVITE D'INHIBITION D'ABSORPTION DU CHOLESTEROL

申请人：ASTRAZENECA AB

公开号：WO2005061451A1

公开（公告）日：2005-07-07

Compounds of formula (XV): [Chemical formula should be inserted here. Please see paper copy] (XV) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.

公式（XV）的化合物：[应在此处插入化学公式。请参见纸质副本]（XV）（其中变量组如内部定义）药物可接受的盐、溶剂化物、这些盐的溶剂化物和前药及其用作治疗高脂血症的胆固醇吸收抑制剂。还描述了它们的制造过程和含有它们的药物组合物。
[EN] PIPERAZINE DERIVATIVE RENIN INHIBITORS<br/>[FR] DERIVES DE PIPERAZINE AGISSANT COMME INHIBITEURS DE LA RENINE

申请人：WARNER LAMBERT CO

公开号：WO2004089915A1

公开（公告）日：2004-10-21

Disclosed are piperazine derivatives, their manufacture and use as inhibitors of renin. Formula (I):

揭示了哌嗪衍生物，它们的制备以及作为肾素抑制剂的用途。化学式（I）：

盐酸阿那格雷 | 58579-51-4

物质功能分类

分子结构分类

物化性质

计算性质

安全信息

SDS

制备方法与用途

反应信息

文献信息

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