磺马曲坦 | 103628-46-2

• 物质功能分类: 原料药 - 解热镇痛药 - 抗偏头痛药
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 中文名称: 磺马曲坦
• 中文别名: 舒马曲坦杂质H；3-[2-(二甲氨基)乙基]-N-甲基-1H-吲哚-5-甲烷碘酰胺；4-苯肼-N-甲基甲烷磺；舒马曲坦化学名；舒马曲坦；3-[2-(二甲胺基)乙基]-N-甲基-1H-吲哚-5-甲基磺酰胺
• 英文名称: sumatripan
• 英文别名: Sumatriptan；1-(3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)-N-methylmethanesulfonamide；sumatriptan succinate；3-[2-(dimethylamino)-ethyl]-N-methyl-1H-indole-5-methanesulphonamide；1-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-methylmethanesulfonamide
• CAS: 103628-46-2
• 化学式: C₁₄H₂₁N₃O₂S
• 分子量: 295.406
• InChiKey: KQKPFRSPSRPDEB-UHFFFAOYSA-N

物化性质

• 熔点：
  169-171°C
• 沸点：
  497.7±55.0 °C(Predicted)
• 密度：
  1.1778 (rough estimate)
• 溶解度：
  可溶于DMSO（少许）、甲醇（少许）
• 物理描述：
  Solid
• 蒸汽压力：
  7.05X10-9 mm Hg at 25 °C (est)
• 解离常数：
  pKa = 10.4 (est) (amide)
• 碰撞截面：
  162.1 Ų [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]
• 保留指数：
  2730

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  20
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  73.6
• 氢给体数：
  2
• 氢受体数：
  4

ADMET

代谢

Sumatriptan 主要通过单胺氧化酶 A 代谢。主要代谢物是无效的吲哚乙酸和吲哚乙酸葡萄糖苷酸。

Sumatriptan is predominantly metabolized by monoamine oxidase A. The main metabolites are the inactive indole acetic acid and indole acetic acid glucuronide.

来源:DrugBank

代谢

Sumatriptan的主要代谢物是其无活性的吲哚乙酸类似物，这是通过N-去甲基侧链的氧化N-脱氨形成的。Sumatriptan的吲哚乙酸代谢物在血浆中的浓度是Sumatriptan的6-7倍，但其半衰期与母体化合物相似，这表明这种代谢物的清除是受形成速率限制的。Sumatriptan的其他次要代谢物，即吲哚乙酸的酯葡萄糖苷和吲哚乙醇衍生物，也已被鉴定。

The principal metabolite of sumatriptan is its inactive indole acetic acid analog, which is formed by oxidative N-deamination of the N-dimethyl side chain. The indole acetic acid metabolite of sumatriptan achieves plasma concentrations 6-7 times higher than those of sumatriptan but has a half-life similar to that of the parent compound, suggesting that clearance of this metabolite is formation-rate limited. Other minor metabolites of sumatriptan, an ester glucuronide of the indole acetic acid derivative and an indole ethyl alcohol derivative, also have been identified.

来源:Hazardous Substances Data Bank (HSDB)

代谢

代谢是舒马曲普坦主要的清除过程。舒马曲普坦在肝脏中代谢，也可能在胃肠道中代谢，并通过尿液和粪便排出体外。体外研究表明，舒马曲普坦主要通过单胺氧化酶（MAO），尤其是A亚型（MAO-A）代谢；该酶的抑制剂可能会增加舒马曲普坦的系统暴露。

Metabolism is the principal clearance process for sumatriptan. Sumatriptan is metabolized in the liver and possibly in the GI tract and is eliminated in urine and feces. In vitro studies suggest that sumatriptan is metabolized by monoamine oxidase (MAO), principally the A isoenzyme (MAO-A); inhibitors of this enzyme may increase systemic exposure to sumatriptan.

来源:Hazardous Substances Data Bank (HSDB)

代谢

肝脏。体外研究使用人微体表明，舒马曲普坦主要通过单胺氧化酶（MAO），主要是A亚型酶代谢。 消除途径：仅有3%的剂量以未改变的舒马曲普坦形式通过尿液排出；42%的剂量以主要代谢物形式排出，即舒马曲普坦的吲哚乙酸类似物。 半衰期：2.5小时

Hepatic. In vitro studies with human microsomes suggest that sumatriptan is metabolized by monoamine oxidase (MAO), predominantly the A isoenzyme. Route of Elimination: Only 3% of the dose is excreted in the urine as unchanged sumatriptan; 42% of the dose is excreted as the major metabolite, the indole acetic acid analogue of sumatriptan. Half Life: 2.5 hours

来源:Toxin and Toxin Target Database (T3DB)

毒理性

• 毒性总结

5-HT_1B和5-HT_1D受体作为自受体，可以抑制血清素神经元的放电，并在激活时减少血清素的合成和释放。当舒马曲普坦与这些受体结合后，通过调节性G蛋白，抑制腺苷酸环化酶的活性，增加细胞内钙，并影响其他细胞内事件。这导致血管收缩和抑制感觉伤害性（三叉神经）神经放电和血管活性神经肽的释放。舒马曲普坦刺激5-HT受体的1D亚型，很可能是突触前的受体，导致颈动脉循环中发炎和扩张的颅血管的选择性血管收缩。在偏头痛期间，舒马曲普坦还阻止了硬脊膜周围三叉神经轴突释放血管活性神经肽，并可能抑制三叉神经释放炎症介质。

The 5-HT_1B and 5-HT_1D receptors function as autoreceptors, which inhibit the firing of serotonin neurons and a reduction in the synthesis and release of serotonin upon activation. After sumatriptan binds to these receptors, adenylate cyclase activity is inhibited via regulatory G proteins, incrases intracellular calcium, and affects other intracellular events. This results in vasoconstriction and inhibtion of sensory nociceptive (trigeminal) nerve firing and vasoactive neuropeptide release. Sumatriptan stimulates 5-HT receptors of the 1D subtype, most likely presynaptic receptors, resulting in selective vasoconstriction of inflamed and dilated cranial blood vessels in the carotid circulation. Sumatriptan also blocks the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater during migraine and may inhibit the release of inflammatory mediators from the trigeminal nerve.

来源:Toxin and Toxin Target Database (T3DB)

毒理性

• 药物性肝损伤

化合物：舒马曲普坦

Compound:sumatriptan

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

DILI 注解：模糊的 DILI 关注

DILI Annotation:Ambiguous DILI-concern

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

严重性等级：3

Severity Grade:3

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

“标签部分：不良反应”

Label Section:Adverse reactions

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

吸收、分配和排泄

• 吸收

6毫克舒马曲普坦皮下注射后，其血药浓度峰值（Cmax）达到69.5纳克/毫升（95%置信区间为62.8-76.9纳克/毫升），达到峰值时间（Tmax）为0.17小时（95%置信区间为0.08-0.33小时），药时曲线下面积（AUC）为9.0小时*纳克/毫升（95%置信区间为7.5-10.9小时*纳克/毫升），生物利用度为100%。25毫克舒马曲普坦口服后，其血药浓度峰值（Cmax）达到16.5纳克/毫升（95%置信区间为13.5-20.1纳克/毫升），达到峰值时间（Tmax）为1.50小时（95%置信区间为0.50-2.00小时），药时曲线下面积（AUC）为8.7小时*纳克/毫升（95%置信区间为6.1-12.5小时*纳克/毫升），生物利用度为14.3%（95%置信区间为11.4-17.9%）。20毫克舒马曲普坦鼻内给药后，其血药浓度峰值（Cmax）达到12.9纳克/毫升（95%置信区间为10.5-15.9纳克/毫升），达到峰值时间（Tmax）为1.50小时（95%置信区间为0.25-3.00小时），药时曲线下面积（AUC）为7.4小时*纳克/毫升（95%置信区间为5.0-10.8小时*纳克/毫升），生物利用度为15.8%（95%置信区间为12.6-19.8%）。25毫克舒马曲普坦直肠给药后，其血药浓度峰值（Cmax）达到22.9纳克/毫升（95%置信区间为18.4-28.6纳克/毫升），达到峰值时间（Tmax）为1.00小时（95%置信区间为0.75-3.00小时），药时曲线下面积（AUC）为14.6小时*纳克/毫升（95%置信区间为11.3-18.8小时*纳克/毫升），生物利用度为19.2%（95%置信区间为15.3-24.1%）。

A 6mg subcutaneous injection of sumatriptan reaches a Cmax of 69.5ng/mL (95% CI of 62.8-76.9ng/mL) with a Tmax of 0.17h (95% CI of 0.08-0.33h), an AUC of 9.0h\*ng/mL (95% CI of 7.5-10.9h\*ng/mL), and a bioavailability of 100%. A 25mg oral dose of sumatriptan reaches a Cmax of 16.5ng/mL (95% CI of 13.5-20.1ng/mL) with a Tmax of 1.50h (95% CI of 0.50-2.00h), an AUC of 8.7h\*ng/mL (95% CI of 6.1-12.5h\*ng/mL), and a bioavailability of 14.3% (95% CI of 11.4-17.9%). A 20mg intranasal dose of sumatriptan reaches a Cmax of 12.9ng/mL (95% CI of 10.5-15.9ng/mL) with a Tmax of 1.50h (95% CI of 0.25-3.00h), an AUC of 7.4h\*ng/mL (95% CI of 5.0-10.8h\*ng/mL), and a bioavailability of 15.8% (95% CI of 12.6-19.8%). A 25mg rectal dose of sumatriptan reaches a Cmax of 22.9ng/mL (95% CI of 18.4-28.6ng/mL) with a Tmax of 1.00h (95% CI of 0.75-3.00h), an AUC of 14.6h\*ng/mL (95% CI of 11.3-18.8h\*ng/mL), and a bioavailability of 19.2% (95% CI of 15.3-24.1%).

来源:DrugBank

吸收、分配和排泄

• 消除途径

22±4% 以未改变的舒马曲普坦形式通过尿液排出，大约 38±7% 以吲哚乙酸形式通过尿液排出，大约 40% 通过粪便排出。

22±4% is excreted in the urine as unchanged sumatriptan and 38±7% in urine as indole acetic acid approximately 40% is excreted in the feces.

来源:DrugBank

吸收、分配和排泄

• 分布容积

Sumatriptan 在给予6毫克皮下剂量时的分布体积为50±8升，或者每公斤体重2.7升。

Sumatriptan has a volume of distribution of 50±8L for a 6mg subcutaneous dose, or 2.7L/kg.

来源:DrugBank

吸收、分配和排泄

• 清除

皮下注射舒马曲普坦的清除率为0.22升/分钟（95%置信区间为0.19-0.25升/分钟）。口服舒马曲普坦的清除率为0.17升/分钟（95%置信区间为0.14-0.21升/分钟）。直肠给药舒马曲普坦的清除率为0.17升/分钟（95%置信区间为0.14-0.21升/分钟）。鼻腔给药舒马曲普坦的清除率为0.21升/分钟（95%置信区间为0.18-0.25升/分钟）。舒马曲普坦的总血浆清除率大约为1200毫升/分钟。

Subcutaneous sumatriptan has a clearance of 0.22L/min (95% CI of 0.19-0.25L/min). Oral sumatriptan has a clearance of 0.17L/min (95% CI of 0.14-0.21L/min). Rectal sumatriptan has a clearance of 0.17L/min (95% CI of 0.14-0.21L/min). Intrsnasal sumatriptan has a clearance of 0.21L/min (95% CI of 0.18-0.25L/min). Total plasma clearance of sumatriptan is approximately 1200mL/min.

来源:DrugBank

吸收、分配和排泄

舒马曲普坦通过皮下或口服给药后可迅速吸收；口服吸收似乎发生在小肠。该药物在通过鼻腔给药后也能迅速吸收。舒马曲普坦皮下给药的生物利用度几乎完全，平均约为静脉给药的97%。然而，舒马曲普坦口服或鼻腔给药的生物利用度平均仅为约15%或17%，主要是因为药物的系统性代谢以及部分吸收不完全。舒马曲普坦的血浆浓度-时间曲线下面积（AUC）和峰血清浓度随单次皮下剂量（1-16毫克）的增加呈线性增加。在单次口服剂量（25-200毫克）下，舒马曲普坦的吸收程度（AUC）也是剂量成比例的；但是，100毫克口服剂量的舒马曲普坦的峰血浆浓度比从25毫克口服剂量预测的值低大约25%。

Sumatriptan is rapidly absorbed following subcutaneous or oral administration; oral absorption appears to occur in the small intestine. The drug also is absorbed rapidly following intranasal administration. The bioavailability of sumatriptan given subcutaneously is almost complete, averaging about 97% of that obtained with iv administration of the drug. The bioavailability of sumatriptan following oral or intranasal administration averages only about 15 or 17%, respectively, principally because of presystemic metabolism of the drug and in part because of incomplete absorption. The area under the plasma concentration-time curve (AUC) and peak serum concentration of sumatriptan increase linearly with single subcutaneous doses of 1-16 mg. The extent of sumatriptan absorption (AUC) also is dose-proportional following single oral doses of 25-200 mg; however, peak plasma concentrations after a 100-mg oral dose of sumatriptan are approximately 25% less than those predicted from a 25-mg oral dose.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险品标志：
  Xi
• 安全说明：
  S26,S28A,S36/37/39,S45
• 危险类别码：
  R36/37/38
• WGK Germany：
  3
• 海关编码：
  29280090
• 危险品运输编号：
  UN 3261 8/PG 2
• RTECS号：
  NL9482200
• 储存条件：
  2-8°C

制备方法与用途

产品特点

舒马曲坦作为一种抗偏头痛药物，是高度选择性5-羟色胺受体（5-HT1B/1D）激动剂。它通过逆转偏头痛时颅内血管的扩张、减轻血浆蛋白外渗来改善脑血流量，从而有效缓解偏头痛症状。

化学性质

舒马曲坦是一种白色结晶性粉末，易溶于水。熔点为169～171℃。琥珀酸舒马普坦（Sumatriptan Succinate）的化学式为C14H21N3O2·C4H5O4，分子量约为308.37，熔点为165～166℃。

用途

舒马曲坦是一种选择性地收缩颅侧血管的5-羟色胺受体激动剂，主要用于治疗偏头痛。它也常被用作专门的偏头痛治疗药物。

生产方法

通过在室温下以10%钯-炭催化、二甲胺的甲醇溶液中氢化24小时，可以制备舒马曲坦。

上下游信息

• 上游原料

  中文名称	英文名称	CAS号	化学式	分子量
  舒马曲普坦中间体	3-(2-aminoethyl)-1H-indole-5-yl-N-methyl methane sulphonamide	88919-22-6	C12H17N3O2S	267.352
  ——	3-(2-Chloroethyl)-N-methyl-1H-indole-5-methanesulphonamide	88918-69-8	C12H15ClN2O2S	286.782
  2-羧基-3-[2-(二甲氨基)乙基]-N-甲基-1H-吲哚-5-甲磺酰胺	2-carboxy-3-[2-(dimethylamino)ethyl]-N-methyl-1H-indole-5-methanesulfonamide	153654-26-3	C15H21N3O4S	339.415
  色胺	tryptamine	61-54-1	C10H12N2	160.219
  ——	1-[1-benzyl-3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-diphenylmethyl-N-methylmethanesulfonamide	——	C34H37N3O2S	551.753

• 下游产品

  中文名称	英文名称	CAS号	化学式	分子量
  舒马普坦N-氧化物	sumatriptan N-oxide	212069-94-8	C14H21N3O3S	311.405
  ——	C-{3-[2-(benzyl-methyl-amino)-ethyl]-1H-indol-5-yl}-N-methyl-methanesulfonamide	——	C20H25N3O2S	371.503
  ——	N-methyl-C-(3-{2-[methyl-(1-phenyl-ethyl)-amino]-ethyl}-1H-indol-5-yl)-methanesulfonamide	220392-07-4	C21H27N3O2S	385.53
  ——	C-[3-(2-Dimethylamino-ethyl)-1H-indol-5-yl]-N-[4-({[3-(2-dimethylamino-ethyl)-1H-indol-5-ylmethanesulfonyl]-methyl-amino}-methyl)-benzyl]-N-methyl-methanesulfonamide	——	C36H48N6O4S2	692.947
  5-羟基甲基-N,N-二甲基色胺	3-[2-(dimethylamino)ethyl]-5-indolemethanol	334981-08-7	C13H18N2O	218.299
  2-[[3-[2-(二甲基氨基)乙基]-1H-吲哚-5-基]甲基]舒马普坦	[[3-[2-(dimethylamino)ethyl]-2-[[3-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]-1H-indol-5-yl]-N-methylmethanesulfonamide	545338-89-4	C27H37N5O2S	495.689

反应信息

• 作为反应物：
  描述：

  磺马曲坦 在 ammonium chloride 、 氨 、 草酸 作用下， 以 吡啶 、 甲醇 、 乙醇 、 二氯甲烷 为溶剂， 生成 1-Benzoyl-3-[2-(dimethylamino)ethyl]-N-methyl-1 H-indole-5-methanesulphonamide oxalate
  参考文献：
  名称：

  Indole derivatives

  摘要：

  公开号：

  EP0242939B1
• 作为产物：
  描述：

  oxalate salt of 3-[2-(dimethylamino)ethyl]-N-ethoxycarbonyl-N-methyl-1H-indole-5-methanesulphonamide 在 甲醇 、 氢氧化钾 作用下， 以 水 为溶剂， 反应 5.0h， 以95%的产率得到磺马曲坦
  参考文献：
  名称：

  Synthesis of 5-Substituted Indole Derivatives, I. An Improved Method for the Synthesis of Sumatriptan

  摘要：

  An improved synthesis of sumatriptan (Ib) via Fischer cyclization was achieved by introducing the ethoxycarbonyl group on the N-atom of the sulphonamide moiety in N-methyl-4-hydrazinobenzenemethanesulphonamide (7). As a result, substitution on the benzylic carbon of the indole nucleus could be avoided; however, formation of 1,1-bis-(indol-2-yl)-4-dimethylaminobutane-type by-product (19) was observed. The indolization procedure was optimized to suppress the unwanted side reaction. The N-protection of the sulphonamide moiety was found to be beneficial regarding the purification of the 3-[2-(dimethylamino)ethyl]-N-ethoxycarbonyl-N-methyl-1H-indole-5-methanesulphonamide (18).

  DOI：

  10.3987/com-97-8087

文献信息

• [EN] COMPOUNDS AND THEIR USE AS BACE INHIBITORS<br/>[FR] COMPOSÉS ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE BACE
  申请人：ASTRAZENECA AB

  公开号：WO2016055858A1

  公开（公告）日：2016-04-14

  The present application relates to compounds of formula (I), (la), or (lb) and their pharmaceutical compositions/preparations. This application further relates to methods of treating or preventing Αβ-related pathologies such as Down's syndrome, β- amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia, including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease.

  本申请涉及式(I)、(Ia)或(Ib)的化合物及其药物组合物/制剂。本申请进一步涉及治疗或预防与Αβ相关的病理学，如唐氏综合症，β-淀粉样蛋白血管病，如但不限于脑淀粉样蛋白血管病或遗传性脑出血，与认知损害相关的疾病，如但不限于MCI（“轻度认知损害”），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与疾病如阿尔茨海默病或痴呆症相关的神经退行性疾病，包括混合性血管性和退行性起源的痴呆，早老性痴呆，老年性痴呆和与帕金森病相关的痴呆的方法。
• [EN] COMPOUNDS THAT MODULATE EGFR ACTIVITY AND METHODS FOR TREATING OR PREVENTING CONDITIONS THEREWITH<br/>[FR] COMPOSÉS MODULANT L'ACTIVITÉ DES RÉCEPTEURS EGFR ET MÉTHODES POUR TRAITER OU PRÉVENIR DES TROUBLES À L'AIDE DE CEUX-CI
  申请人：GATEKEEPER PHARMACEUTICALS INC

  公开号：WO2011140338A1

  公开（公告）日：2011-11-10

  Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.

  提供了用于治疗或预防激酶介导的疾病的化合物和方法。
• [EN] NAPHTHALENE CARBOXAMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS<br/>[FR] COMPOSÉS DE NAPHTHALÈNE CARBOXAMIDE, MODULATEURS ALLOSTÉRIQUES POSITIFS DU RÉCEPTEUR M1
  申请人：MERCK SHARP & DOHME

  公开号：WO2011149801A1

  公开（公告）日：2011-12-01

  The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

  本发明涉及式(I)的萘甲酰胺化合物，它们是M1受体阳性变构调节剂，可用于治疗M1受体参与的疾病，如阿尔茨海默病、精神分裂症、疼痛或睡眠障碍。该发明还涉及包含这些化合物的药物组合物，以及在治疗由M1受体介导的疾病中使用这些化合物和组合物。
• [EN] KINASE INHIBITORS FOR THE TREATMENT OF DISEASE<br/>[FR] INHIBITEURS DE KINASE POUR LE TRAITEMENT D'UNE MALADIE
  申请人：DANA FARBER CANCER INST INC

  公开号：WO2015006492A1

  公开（公告）日：2015-01-15

  The invention relates to compounds and their use in the treatment of disease. Novel irreversible inhibitors of wild-type and mutant forms of EGFR, FGFR, ALK, ROS, JAK, BTK, BLK, ITK, TEC, and/or TXK and their use for the treatment of cell proliferation disorders are described.

  这项发明涉及化合物及其在治疗疾病中的应用。描述了用于治疗细胞增殖紊乱的新型EGFR、FGFR、ALK、ROS、JAK、BTK、BLK、ITK、TEC和/或TXK的野生型和突变型不可逆抑制剂及其应用。
• Novel Compounds
  申请人：Chhipa Laxmikant

  公开号：US20100168110A1

  公开（公告）日：2010-07-01

  The present invention discloses a novel thyroid like compounds of formula (I), wherein R 1 R 2 , R 3 , R 4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.

  本发明公开了一种新型的甲状腺类似化合物，其化学式为（I），其中R1、R2、R3、R4和Z如规范中所定义，以及其制备方法、含有这种化合物的组合物和这种化合物及组合物作为药物的用途。此外，化合物的化学式（I）具有与甲状腺受体显著低的结合亲和力，因此在很大程度上缺乏甲状腺毒性作用。该发明还涉及将化学式（I）的化合物用于制备用于治疗肥胖、血脂异常、代谢综合征以及与代谢综合征相关的合并症等各种疾病状况的药物。

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