溴化钠 | 7647-15-6

• 物质功能分类: 原料药 - 神经系统用药 - 2镇静与催眠药
• 分子结构分类: 无机化合物 - 混合金属/非金属化合物 - 碱金属盐
• 中文名称: 溴化钠
• 中文别名: 钠臭
• 英文名称: sodium bromide
• 英文别名: sodium;bromide
• CAS: 7647-15-6
• 化学式: BrNa
• 分子量: 102.894
• InChiKey: JHJLBTNAGRQEKS-UHFFFAOYSA-M

物化性质

• 熔点：
  755 °C (lit.)
• 沸点：
  1390 °C
• 密度：
  3,203 g/cm3
• 闪点：
  1390°C
• 溶解度：
  H2O:1 Mat 20 °C,透明，无色
• 最大波长(λmax)：
  λ: 260 nm Amax: 0.01λ: 280 nm Amax: 0.01
• 介电常数：
  6.3399999999999999
• LogP：
  0 at 25℃
• 物理描述：
  DryPowder; DryPowder, WetSolid; Liquid; OtherSolid
• 颜色/状态：
  White crystals, granules, or powder
• 味道：
  Saline, feebly bitter taste
• 分解：
  When heated to decomposition it emits toxic fumes of /bromine and sodium oxide/.
• 折光率：
  Index of refraction: 1.6412
• 稳定性/保质期：
  1. 在空气中具有吸湿性，易溶于水（100℃时溶解度为121 g/100 ml水），其水溶液呈中性。微溶于醇。51℃时溶液中析出无水溴化钠结晶；温度低于51℃则生成二水物。其中的溴离子可被氟或氯所取代。在酸性条件下，能被氧气氧化并释放出溴。与稀硫酸反应可生成溴化氢。 2. 在酸性条件下，同样能够被氧氧化释放出溴，并且可以与稀硫酸反应生成溴化氢。工作人员应做好防护措施；如不慎触及眼睛，请立即用大量流动清水冲洗。工作环境应保持良好的通风条件。

计算性质

• 辛醇/水分配系数(LogP)：
  -5.99
• 重原子数：
  2
• 可旋转键数：
  0
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  1

ADMET

代谢

溴主要通过吸入进入人体，但也可以通过皮肤接触。溴盐可以摄入。由于溴的活性，它会迅速形成溴化物并可能沉积在组织中，取代其他卤素。

Bromine is mainly absorbed via inhalation, but may also enter the body through dermal contact. Bromine salts can be ingested. Due to its reactivity, bromine quickly forms bromide and may be deposited in the tissues, displacing other halogens. (L626)

来源:Toxin and Toxin Target Database (T3DB)

毒理性

• 毒性总结

溴是一种强大的氧化剂，能够从粘膜的水分中释放出氧自由基。这些自由基也是有力的氧化剂，能够造成组织损伤。此外，氢溴酸和溴酸的形成将导致二次刺激。溴离子还已知会影响中枢神经系统，导致溴中毒。这被认为是溴离子取代神经递质和传输系统中的氯离子的结果，从而影响许多突触过程。（L626, L627, A543）

Bromine is a powerful oxidizing agent and is able to release oxygen free radicals from the water in mucous membranes. These free radicals are also potent oxidizers and produce tissue damage. In additon, the formation of hydrobromic and bromic acids will result in secondary irritation. The bromide ion is also known to affect the central nervous system, causing bromism. This is believed to be a result of bromide ions substituting for chloride ions in the in actions of neurotransmitters and transport systems, thus affecting numerous synaptic processes. (L626, L627, A543)

来源:Toxin and Toxin Target Database (T3DB)

毒理性

• 致癌物分类

对人类无致癌性（未列入国际癌症研究机构IARC清单）。

No indication of carcinogenicity to humans (not listed by IARC).

来源:Toxin and Toxin Target Database (T3DB)

毒理性

• 健康影响

溴蒸气会引起刺激和对粘膜的直接损害。元素溴也会烧伤皮肤。溴化物离子是一种中枢神经系统抑制剂，长期暴露会产生神经元效应。这被称为溴中毒，可能导致从中睡意到昏迷、恶病质、昏迷、反射丧失或病理反射、阵挛性癫痫、震颤、共济失调、神经敏感性丧失、瘫痪、眼乳头水肿、言语异常、脑水肿、谵妄、攻击性和精神病的中心反应。

Bromine vapour causes irritation and direct damage to the mucous membranes. Elemental bromine also burns the skin. The bromide ion is a central nervous system depressant and chronic exposure produces neuronal effects. This is called bromism and can result in central reactions reaching from somnolence to coma, cachexia, exicosis, loss of reflexes or pathologic reflexes, clonic seizures, tremor, ataxia, loss of neural sensitivity, paresis, papillar edema of the eyes, abnormal speech, cerebral edema, delirium, aggressiveness, and psychoses. (L625, L626, L627)

来源:Toxin and Toxin Target Database (T3DB)

毒理性

• 暴露途径

口服（L626）；吸入（L626）；皮肤给药（L626）

Oral (L626) ; inhalation (L626) ; dermal (L626)

来源:Toxin and Toxin Target Database (T3DB)

毒理性

• 症状

溴蒸气会引起刺激和对粘膜的直接损害。症状包括流泪、流鼻涕、眼部刺激伴有来自咽和上呼吸道的粘液分泌、咳嗽、呼吸困难、窒息、喘息、鼻出血和头痛。溴离子是一种中枢神经系统抑制剂，会引起共济失调、言语不清、震颤、恶心、呕吐、乏力、眩晕、视觉障碍、不稳、头痛、记忆和注意力受损、定向障碍和幻觉。这被称为溴中毒。

Bromine vapour causes irritation and direct damage to the mucous membranes. Symptoms include lacrimation, rhinorrhoea, eye irritation with mucous secretions from the oropharyngeal and upper airways, coughing, dyspnoea, choking, wheezing, epistaxis, and headache. The bromide ion is a central nervous system depressant producing ataxia, slurred speech, tremor, nausea, vomiting, lethargy, dizziness, visual disturbances, unsteadiness, headaches, impaired memory and concentration, disorientation and hallucinations. This is called bromism. (L626, L627)

来源:Toxin and Toxin Target Database (T3DB)

吸收、分配和排泄

口服和静脉注射溴化物的药代动力学在7名成年志愿者中进行研究，他们作为自己的对照。他们接受了1毫升/公斤的3%溴化钠，相当于30毫克/公斤溴化物。口服生物利用度在75-118%之间，平均为96 +/- 6%。口服给药后的消除半衰期为11.9 +/- 1.4天，静脉给药后的消除半衰期为9.4 +/- 1.5天（P > 0.10）...

The pharmacokinetics of oral and intravenous bromide was studied in 7 adult volunteers, who served as their own controls. They received 1 mL/kg of 3% sodium bromide, equivalent to 30 mg/kg bromide. Oral bioavailability ranged between 75-118% with a mean of 96 +/- 6%. Elimination T1/2 was 11.9 +/- 1.4 days after oral administration and 9.4 +/- 1.5 days after iv administration (P > 0.10) ...

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

溴化钠静脉注射后，通过自动放射性成像技术研究小鼠体内(82)Br的分布。定量测定了各种组织中(82)Br的水平，并以血液水平的百分比表示。在给药后24小时内，以下器官的溴水平高于血液水平：胃粘膜、胃内容物、膀胱内容物、血管壁和视网膜。以下器官的浓度较高，但不超过血液中的浓度：软骨、肌腱、肺、致密骨和甲状腺。

The distribution of (82)Br in the mouse was studied by autoradiography at various intervals after IV injection /of sodium bromide/. (82)Br levels in various tissues were determined quantitiatively and expressed as percentages of the blood level. In the 24 hr after administration, the following organs had high Br levels (compared to blood levels): gastric mucosa, gastric contents, urinary bladder contents, blood vessel walls, and retina. High concentrations, but not exceeding the concentration in blood, were in: cartilage, tendons, lungs, compact bone, and thyroid.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

氟化物、溴化物、碘化物、氯化物和硫氰酸盐的分布在小鼠和大鼠中通过全身自动放射性造影、显微放射性造影、双示踪剂自动放射性造影和闪烁计数法进行了研究。溴化物在静脉注射后长时间内血液中浓度较高。溴化物在血管壁中积累。在中枢神经系统中观察到低浓度。在4-24小时后，中枢神经系统中的溴化物浓度降至血液水平的1/3。在胃粘膜、垂体、骨骼和软骨中观察到一些浓度，在唾液腺、牙齿和眼睛中观察到高浓度。在肠粘膜、肝脏、淋巴组织、卵巢、肌肉和甲状腺中几乎没有积累。

The distribution of halide ions fluoride, bromide, iodide, chloride, and thiocyanate were studied in mice and rats by whole body autoradiography, microradiography, double tracer autoradiography, and scintillation counting methods. Bromide showed a high concentration in blood after IV injection for a long time. Bromide accumulated in the blood vessel walls. A low concentration was seen in the central nervous system. After 4 - 24 hr bromide concentrations in the central nervous system were 1/3 of blood level. Some concentration was seen in gastric mucosa, pituitary gland, bone, and cartilage, and high concentrations in the salivary glands, teeth, and eyes. Little to no accumulation was seen in the intestinal mucosa, liver, lymphatic tissue, ovaries, muscles, and thyroid.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

溴化物在兔神经系统中的稳态分布受到血浆浓度水平（0.5 - 20 nM）的影响。通过使用室间孔脑室灌注系统，在不同实验条件下测量了溴化物在脑脊液和血液之间的通量。脑脊液中溴化物的稳态分布与浓度有关，且大脑起到了血浆和脑脊液中溴化物的汇。通量实验揭示了从灌注液中外排的溴化物比从血液中流入的溴化物多约30%。随着溴化物浓度的增加和动物死亡，溴化物从灌注液中的移出被减弱。建议在低浓度水平下，溴化物通过一个主动转运系统从脑脊液中快速清除，并从大脑中清除（可能是通过相同的机制或氧化成溴酸盐），而在高浓度水平下，所提出的系统效果不佳，导致溴化物积累，并在血液、大脑和脑脊液之间建立平衡状态。

The steady-state distribution of bromide in the nervous system of the rabbit was studied at various plasma concentration levels (0.5 - 20 nM). Utilizing a ventriculo-cisternal perfusion system, the flux of bromide between cerebrospinal fluid and blood was measured under various experimental conditions. The steady-state distribution of bromide in brain and cerebrospinal fluid was concentration dependent, and the brain served as a sink for the plasma and cerebrospinal fluid. The flux experiments revealed that the efflux of bromide from the perfusion fluid was some 30% greater than the influx of bromide from the blood. The movement of bromide out of the perfusate was attenuated with increasing concentrations of bromide and on death of the animal. /It was/ suggested that at low concentration levels, bromide is rapidly cleared from the cerebrospinal fluid (by an active transport system) and the brain (by either the same or oxidation to bromate), while at high concentration levels the relative ineffectiveness of the proposed systems results in accumulation of bromide and the establishment of a state of equilibrium between blood, brain, and cerebrospinal fluid.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• TSCA：
  Yes
• 危险品标志：
  Xi
• 安全说明：
  S24/25,S25
• 危险类别码：
  R36/37/38
• WGK Germany：
  1
• 海关编码：
  2827510000
• 危险品运输编号：
  NONH for all modes of transport
• RTECS号：
  VZ3150000
• 储存条件：
  1. 应贮存在干燥、阴凉、通风良好的地方。要防止日光曝晒，并与火种和热源隔离，不得与氨、氧、磷、锑粉和碱类共贮混运。应远离木屑、刨花、稻草等，以防燃烧。 2. 失火时，可用沙土或二氧化碳灭火器扑救。

SDS

Name:	Sodium bromide p.a. Material Safety Data Sheet
Synonym:	Bromide salt of sodium, Sedoneura
CAS:	7647-15-6

Section 1 - Chemical Product MSDS Name:Sodium bromide p.a. Material Safety Data Sheet
Synonym:Bromide salt of sodium, Sedoneura

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Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS

CAS#	Chemical Name	content	EINECS#
7647-15-6	Sodiumbromide	100%	231-599-9

Hazard Symbols: None Listed.
Risk Phrases: None Listed.

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Section 3 - HAZARDS IDENTIFICATION
EMERGENCY OVERVIEW
Hygroscopic.
Potential Health Effects
Eye:
May cause eye irritation.
Skin:
May cause skin irritation.
Ingestion:
May cause gastrointestinal irritation with nausea, vomiting and diarrhea. Effects may be cumulative. May cause central nervous system effects such as psychosis, hallucinations, depression, visual changes and mental changes. Ingestion may cause skin eruptions and rash.
Inhalation:
May cause effects similar to those described for ingestion.
Chronic:
Chronic inhalation and ingestion may cause effects similar to those of acute inhalation and ingestion. May cause incoordination and mental disturbances.

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Section 4 - FIRST AID MEASURES
Eyes: Flush eyes with plenty of water for at least 15 minutes, occasionally lifting the upper and lower eyelids. Get medical aid immediately.
Skin:
Flush skin with plenty of soap and water for at least 15 minutes while removing contaminated clothing and shoes. Get medical aid if irritation develops or persists.
Ingestion:
If victim is conscious and alert, give 2-4 cupfuls of milk or water.
Never give anything by mouth to an unconscious person. Get medical aid immediately.
Inhalation:
Remove from exposure to fresh air immediately. If not breathing, give artificial respiration. If breathing is difficult, give oxygen.
Get medical aid.
Notes to Physician:
Treatment includes hydration, mild diuresis, and possible hemodialysis. Consider the use of ammonium chloride in divided doses with a diuretic.

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Section 5 - FIRE FIGHTING MEASURES
General Information:
As in any fire, wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. Substance is noncombustible.
Extinguishing Media:
Use extinguishing media most appropriate for the surrounding fire.

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Section 6 - ACCIDENTAL RELEASE MEASURES
General Information: Use proper personal protective equipment as indicated in Section 8.
Spills/Leaks:
Vacuum or sweep up material and place into a suitable disposal container.

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Section 7 - HANDLING and STORAGE
Handling:
Wash thoroughly after handling. Use with adequate ventilation. Avoid contact with skin and eyes.
Storage:
Store in a cool, dry place. Store in a tightly closed container.

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Section 8 - EXPOSURE CONTROLS, PERSONAL PROTECTION
Engineering Controls:
Facilities storing or utilizing this material should be equipped with an eyewash facility and a safety shower. Use process enclosure, local exhaust ventilation, or other engineering controls to control airborne levels.
Personal Protective Equipment Eyes: Wear appropriate protective eyeglasses or chemical safety goggles as described by OSHA's eye and face protection regulations in 29 CFR 1910.133 or European Standard EN166.
Skin:
Wear appropriate protective gloves to prevent skin exposure.
Clothing:
Wear a chemical apron.
Respirators:
Follow the OSHA respirator regulations found in 29CFR 1910.134 or European Standard EN 149. Always use a NIOSH or European Standard EN 149 approved respirator when necessary.

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Section 9 - PHYSICAL AND CHEMICAL PROPERTIES

Physical State: Solid
Appearance: white
Odor: Odorless
pH: 6.5-8.0
Vapor Pressure: 1 mm Hg @ 806 deg C
Viscosity: Not available.
Boiling Point: 1390 deg C @ 760.00mm Hg
Freezing/Melting Point: 755 deg C
Autoignition Temperature: Not available.
Flash Point: 800 deg C ( 1,472.00 deg F)
Explosion Limits, lower: Not available.
Explosion Limits, upper: Not available.
Decomposition Temperature: 800 deg C
Solubility in water: 95g/100ml water (25 c)
Specific Gravity/Density: 3.21g/cm3
Molecular Formula: BrNa
Molecular Weight: 102.8938

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Section 10 - STABILITY AND REACTIVITY
Chemical Stability:
Stable under normal temperatures and pressures.
Conditions to Avoid:
Incompatible materials, heating to decomposition, exposure to moist air or water.
Incompatibilities with Other Materials:
Strong acids - alkaloidal and heavy metal salts (lead, silver, manganese, antimony, mercury, etc.) - strong oxidizing agents - halogen halides - bromine trifluoride.
Hazardous Decomposition Products:
Hydrogen bromide, sodium oxide, bromine fumes.
Hazardous Polymerization: Has not been reported

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Section 11 - TOXICOLOGICAL INFORMATION
RTECS#:
CAS# 7647-15-6: VZ3150000 LD50/LC50:
CAS# 7647-15-6: Oral, mouse: LD50 = 7 gm/kg; Oral, rat: LD50 = 3500 mg/kg.
Carcinogenicity:
Sodiumbromide - Not listed by ACGIH, IARC, NIOSH, NTP, or OSHA.
Other:
See actual entry in RTECS for complete information.

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Section 12 - ECOLOGICAL INFORMATION
Ecotoxicity:
Water danger/protection: WGK 1 Bluegill sunfish LC50: >1000 mg/l/96H Rainbow trout LC50: >1000 mg/l/96H Daphnia magna LC50: >1000 mg/l/48H Bobwhite quail LD50: >2250 mg/kg Mallard duck LC50: >5633 ppm Bobwhite quail LC50: >5633 ppm

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Section 13 - DISPOSAL CONSIDERATIONS
Dispose of in a manner consistent with federal, state, and local regulations.

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Section 14 - TRANSPORT INFORMATION

IATA
Not regulated as a hazardous material.
IMO
Not regulated as a hazardous material.
RID/ADR
Shipping Name: Not regulated.
Dangerous Goods Code:
UN Number:

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Section 15 - REGULATORY INFORMATION

European/International Regulations
European Labeling in Accordance with EC Directives
Hazard Symbols: Not available.
Risk Phrases:
Safety Phrases:
S 24/25 Avoid contact with skin and eyes.
WGK (Water Danger/Protection)
CAS# 7647-15-6: 1
United Kingdom Occupational Exposure Limits
Canada
CAS# 7647-15-6 is listed on Canada's DSL List.
CAS# 7647-15-6 is listed on Canada's Ingredient Disclosure List.
Exposure Limits
US FEDERAL
TSCA
CAS# 7647-15-6 is listed on the TSCA inventory.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

物化性质

溴化钠在常温下是一种无色立方晶系晶体或白色颗粒状粉末，属于等轴晶系。它没有气味，味道碱而略带苦涩，并且具有毒性。该物质容易在空气中吸收水分并结块，但不会潮解，微溶于醇，易溶于水（100℃时每100毫升水中溶解度为121克）。其水溶液呈中性且具有导电性。51℃时的溶液会析出无水溴化钠结晶，低于此温度则生成二水物。溴离子可以被氟或氯取代。在酸性条件下，溴化钠能被氧化成溴，工业上利用这一特性来制备溴。与稀硫酸反应可生成溴化氢。

不良反应

服用溴化钠后的不良反应包括个别患者可能会出现皮疹、剥脱性皮炎以及嗜睡、眩晕、哮喘等反应，这些症状一般在停药后自行消失。过量服用会引发昏睡。在服药过程中，不可突然停止使用药物，否则可能引发癫痫持续状态或反跳现象。如出现严重不良反应，应立即就医。该物质对过敏患者禁用，肝、肾、肺功能严重障碍的患者亦不宜使用。孕妇及哺乳期妇女也应避免使用。

水中溶解度(g/100ml)

不同温度时每100毫升水中的溶解克数如下：

• 80.2g/0℃
• 85.2g/10℃
• 90.8g/20℃
• 98.4g/30℃
• 107g/40℃
• 118g/60℃
• 120g/80℃
• 121g/90℃
• 121g/100℃

毒性

为防止摄入、吸入，避免溴化钠接触眼睛和皮肤。若误食或吸入，会引发眩晕、恶心及呕吐等症状。不可燃烧，在火场会产生有毒的氧化钠与溴化物烟雾。

储存时需在低温、通风干燥的地方保存。

灭火剂

• 水
• 二氧化碳
• 干粉
• 泡沫

类别

溴化钠属于有毒物品，毒性分级为中毒。急性口服毒性测试结果：大鼠LD50为3500毫克/公斤；小鼠为7000毫克/公斤。

急性毒性

• 口服- 大鼠 LD50 3500 毫克/ 公斤
• 口服- 小鼠 LD50: 7000 毫克/公斤

生产方法

尿素还原法将纯碱（碳酸钠）与尿素用热水溶解，送入反应器中后缓慢加入溴素进行反应，生成溴化钠。随后使用活性炭脱色，经过滤、蒸发结晶、离心分离并干燥，最终制得溴化钠成品。

中和法制备方法是将约40%的氢溴酸加入反应器中，在搅拌下缓慢加入40%烧碱溶液，直至pH值达到7.5至8时生成溴化钠。随后进行离心分离、蒸发结晶及离心分离制得最终产品。

用途

• 感光工业用于配制胶片感光液。
• 医药上用于生产利尿剂和镇静剂。
• 香料工业中用于生产合成香料。
• 印染工业用作溴化剂，也可用于有机合成等方面。

此外，它还被用于分析试剂、无机和有机化合物的合成及制药工业。在感光胶片、医药、香料、染料等行业也有广泛应用，并可用于微量测定镉。

反应信息

• 作为反应物：
  描述：

  溴化钠 生成 双氧水
  参考文献：
  名称：

  BOUGHTON, JOHN H.;BUTZ, RALPH A.;CHENG, HERMAN C. T.;DENNIS, JONATHAN R.;+

  摘要：

  DOI：
• 作为产物：
  描述：

  sodium hypobromide 生成 溴化钠
  参考文献：
  名称：

  SCHMIDT, KARIN;LENZ, UWE

  摘要：

  DOI：
• 作为试剂：
  描述：

  葡萄糖 在 溴化钠 作用下， 以 二氯甲烷 为溶剂， 生成 2,3,4,6-O-四特戊酰基-alpha-D-溴代吡喃葡萄糖 、 三甲基乙酰氯
  参考文献：
  名称：

  METHOD FOR PRODUCING a-HALO-TETRAACYL-GLUCOSE

  摘要：

  提供了一种适用于工业制备的高效、优秀的α-卤代四酰基葡萄糖的制备方法，该方法包括将D-葡萄糖或低级烷基D-葡萄糖苷与羧酸的活性衍生物和金属卤化物反应，以制备由公式(III)表示的α-卤代四酰基葡萄糖：其中R代表一个可选地被取代的低级烷基团或一个可选地被取代的芳基团，X代表一个卤素原子，一步完成，并且得到的α-卤代四酰基葡萄糖(III)可以通过常规方法转化为公式(I)的化合物或其盐。

  公开号：

  US20160002276A1

文献信息

• Benzimidazole Derivatives As PI3 Kinase Inhibitors
  申请人：GlaxoSmithKline LLC

  公开号：US20140378456A1

  公开（公告）日：2014-12-25

  This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.

  本发明涉及苯并咪唑衍生物的使用，用于调节磷脂酰肌醇3′ OH激酶家族（以下简称PI3激酶）的活性或功能，特别是抑制其活性或功能，适当地，PI3Kα、PI3Kδ、PI3Kβ和/或PI3Kγ。适当地，本发明涉及苯并咪唑在治疗以下一种或多种疾病状态中的使用：自身免疫性疾病、炎症性疾病、心血管疾病、神经退行性疾病、过敏、哮喘、胰腺炎、多器官衰竭、肾脏疾病、血小板聚集、癌症、精子运动能力、移植排斥、移植物排斥和肺部损伤。更适当地，本发明涉及PI3Kβ选择性苯并咪唑化合物用于治疗癌症。
• PIPERIDINONE CARBOXAMIDE AZAINDANE CGRP RECEPTOR ANTAGONISTS
  申请人：Bell Ian M.

  公开号：US20120122899A1

  公开（公告）日：2012-05-17

  The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

  本发明涉及吡啶酮羧酰胺吡嗪衍生物，其为CGRP受体拮抗剂，可用于治疗或预防CGRP参与的疾病，如偏头痛。本发明还涉及包含这些化合物的药物组合物以及在预防或治疗CGRP参与的这些疾病中使用这些化合物和组合物。
• Process for preparing a substituted imidazopyridine compound
  申请人：——

  公开号：US20040039013A1

  公开（公告）日：2004-02-26

  The present invention provides a new process for large-scale preparation of substituted imidazopyridine compound of formula (1) wherein R 1 is C 1 -C 6 alkoxy or NH 2 group, comprising the step of reacting a compound of formula (2) with a 3-halo-2-butanone compound in cyclohexanone.

  本发明提供了一种新的大规模制备式（1）中取代咪唑吡啶化合物的过程，其中R1是C1-C6烷氧基或NH2基团，包括将式（2）化合物与3-卤代-2-丁酮化合物在环已酮中反应的步骤。
• AMINE COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES
  申请人：MITSUBISHI TANABE PHARMA CORPORATION

  公开号：US20140296183A1

  公开（公告）日：2014-10-02

  A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(═O)(OH) 2 , X is an oxygen atom or a sulfur atom, Y is CH 2 CH 2 or CH═CH, R 1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R 2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R 3 and R 4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.

  以下是一种新型胺化合物的化学式（I），它在免疫抑制作用、抗排斥作用等方面具有优异的表现，并显示出缩短心跳等副作用的减少，或其药学上可接受的酸盐、水合物或溶剂化物，以及包含该化合物和药学上可接受的载体的制药组合物。其中，R是氢原子或P（═O）（OH）2，X是氧原子或硫原子，Y是CH2CH2或CH═CH，R1是氰基或具有1至4个碳原子的烷基，并被卤素原子取代，R2是具有1至4个碳原子的烷基，可选择地被羟基或卤素原子取代，R3和R4可能相同也可能不同，每个都是氢原子或具有1至4个碳原子的烷基，n为5-8。
• Method for preparing (2S, 3R, 4S) -4-hydroxyisoleucine and analogues thereof
  申请人：Ouazzani Jamal

  公开号：US20050079587A1

  公开（公告）日：2005-04-14

  The invention concerns a method for preparing a-amino acids of general formula (2S-1) wherein: the group R1 represents a hydrogen atom, a group protecting the amino group or a group of formula —COOR2 wherein the group R2 represents a C1-C6 alkyl group, an aryl or aralkyl group. The invention also concerns a-amino acids of general formula (2S-1) wherein the group R1 represents a group protecting the amino group or a group of formula —COOR2 wherein the group R2 represents a C1-C6 alkyl group, an aryl or aralkyl group and their use as medicine.

  该发明涉及一种制备通式（2S-1）的α-氨基酸的方法，其中：基团R1代表氢原子、保护氨基的基团或者通式—COOR2的基团，其中基团R2代表C1-C6烷基、芳基或芳基烷基。该发明还涉及通式（2S-1）的α-氨基酸，其中基团R1代表保护氨基的基团或者通式—COOR2的基团，其中基团R2代表C1-C6烷基、芳基或芳基烷基，并且它们的用途为药物。

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