3-甲酰基-2-苯基噻吩 | 38695-73-7

分子结构分类

有机化合物 - 有机杂环化合物 - 噻吩类

中文名称

3-甲酰基-2-苯基噻吩

中文别名

——

英文名称

2-phenylthiophene-3-carboxylic acid

英文别名

2-Phenyl-thiophen-3-carbonsaeure；2-phenyl-3-thiophenecarboxylic acid

CAS

38695-73-7

化学式

C₁₁H₈O₂S

mdl

——

分子量

204.249

InChiKey

PQNWWRHSZQZRTB-UHFFFAOYSA-N

BEILSTEIN

——

EINECS

——

物化性质

沸点：

342.1±22.0 °C(Predicted)
密度：

1.303

计算性质

辛醇/水分配系数(LogP)：

2.8
重原子数：

14
可旋转键数：

2
环数：

2.0
sp3杂化的碳原子比例：

0.0
拓扑面积：

65.5
氢给体数：

1
氢受体数：

3

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

—— methyl 2-phenylthiophene-3-carboxylate 38695-70-4 C₁₂H₁₀O₂S 218.276

中文名称	英文名称	CAS号	化学式	分子量
——	methyl 2-phenylthiophene-3-carboxylate	38695-70-4	C₁₂H₁₀O₂S	218.276

反应信息

作为反应物：

描述：

3-甲酰基-2-苯基噻吩在叠氮磷酸二苯酯、三乙胺作用下，以甲苯为溶剂，反应 1.67h，生成

参考文献：

名称：

新型奎宁环烷基杂芳基氨基甲酸酯衍生物作为毒蕈碱受体拮抗剂

摘要：

在这里，我们描述了新的奎宁环基杂芳基氨基甲酸酯衍生物的合成和药理作用。其中，奎宁环丁-4-基噻唑基氨基甲酸酯衍生物ASP9133被确定为一种有前途的长效毒蕈碱拮抗剂（LAMA），与噻托溴铵相比，在大鼠模型中对支气管收缩的选择性抑制作用更强，起效更快。

DOI：

10.1016/j.bmc.2014.04.031
作为产物：

描述：

苯硼酸在四(三苯基膦)钯、 sodium carbonate 、 sodium hydroxide 作用下，以 1,4-二氧六环、乙醇、水为溶剂，反应 11.0h，生成 3-甲酰基-2-苯基噻吩

参考文献：

名称：

新型奎宁环烷基杂芳基氨基甲酸酯衍生物作为毒蕈碱受体拮抗剂

摘要：

在这里，我们描述了新的奎宁环基杂芳基氨基甲酸酯衍生物的合成和药理作用。其中，奎宁环丁-4-基噻唑基氨基甲酸酯衍生物ASP9133被确定为一种有前途的长效毒蕈碱拮抗剂（LAMA），与噻托溴铵相比，在大鼠模型中对支气管收缩的选择性抑制作用更强，起效更快。

DOI：

10.1016/j.bmc.2014.04.031

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文献信息

COMPOUNDS HAVING ACTIVITY AT THE GLYCINE TRANSPORTER GLYT1 AND USES THEREOF

申请人：Branch Clive Leslie

公开号：US20090227629A1

公开（公告）日：2009-09-10

The present invention relates to compounds of formula (I), salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof. wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and n are as defined in the description.

本发明涉及化合物(I)的公式，其盐或溶剂，其用于制造治疗神经和神经精神障碍的药物，特别是精神病、痴呆或注意力缺陷障碍的药物。本发明还包括制造这些化合物和药物配方的过程。其中R1、R2、R3、R4、R5、R6和n如描述中所定义。
2-Phenylthiophene Derivative

申请人：Miyata Junji

公开号：US20080027048A1

公开（公告）日：2008-01-31

The present invention relates to a 2-phenylthiophene derivative or a salt thereof, wherein the thiophene ring is substituted with a carboxyl group or the like and the benzene ring has an electron-withdrawing group such as a cyano group and an electron-donating group such as a substituted alkoxy group at the same time. Since the compound of the invention has good xanthine oxidase-inhibitory action and uric acid-lowering action and does not have a structure derived from nucleic acid, the compound has advantages of high safety and excellent effects as compared with conventional compounds and is useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory bowel diseases, diabetic kidney diseases, diabetic retinopathy, or the like.

本发明涉及一种2-苯基噻吩衍生物或其盐，其中噻吩环被羧基或类似物取代，苯环同时具有电子吸引基（如氰基）和电子供给基（如取代烷氧基）。由于该化合物具有良好的黄嘌呤氧化酶抑制作用和降尿酸作用，并且不具有源自核酸的结构，因此与传统化合物相比，该化合物具有高安全性和优异的效果，并可用作治疗或预防高尿酸血症、痛风、炎症性肠病、糖尿病肾病、糖尿病视网膜病等的药物。
AZA-BRIDGED-RING COMPOUND

申请人：Nagashima Shinya

公开号：US20100105658A1

公开（公告）日：2010-04-29

[Problems] Provided is a compound which has an antagonistic action on a muscarinic M 3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like. [Means for Solving Problems] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M 3 receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M 3 receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M 3 receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.

【问题】提供了一种具有抗胆碱能M3受体拮抗作用的化合物，可作为预防和/或治疗慢性阻塞性肺疾病（COPD）、哮喘等炎症性疾病的活性成分。【解决问题的手段】本发明人对具有抗胆碱能M3受体结合作用的化合物进行了研究，发现一种氮杂环桥合环化合物或其盐具有抗胆碱能M3受体结合作用，从而完成了本发明。本发明的氮杂环桥合环化合物具有抗胆碱能M3受体结合作用，并可用作预防和/或治疗慢性阻塞性肺疾病（COPD）、哮喘等炎症性疾病的预防和/或治疗剂。
Aza-bridged-ring compound

申请人：Nagashima Shinya

公开号：US08367696B2

公开（公告）日：2013-02-05

[PROBLEMS] Provided is a compound which has an antagonistic action on a muscarinic M3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like. [MEANS For SOLVING PROBLEMS] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M3 receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M3 receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M3 receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.

【问题】提供了一种化合物，该化合物对于肌肉型M3受体具有拮抗作用，可用作预防性和/或治疗性药物的活性成分，用于治疗炎症性疾病，例如慢性阻塞性肺疾病（COPD），哮喘等。【解决问题的方法】本发明人对具有对肌肉型M3受体结合具有拮抗作用的化合物进行了研究，并发现一种含氮桥环化合物或其盐对肌肉型M3受体结合具有拮抗作用，从而完成了本发明。本发明的含氮桥环化合物对肌肉型M3受体结合具有拮抗作用，可用作预防性和/或治疗性药物的活性成分，用于治疗炎症性疾病，例如慢性阻塞性肺疾病（COPD），哮喘等。
2-PHENYLTHIOPHENE DERIVATIVE

申请人：Astellas Pharma Inc.

公开号：EP1783124A1

公开（公告）日：2007-05-09

The present invention relates to a 2-phenylthiophene derivative or a salt thereof, wherein the thiophene ring is substituted with a carboxyl group or the like and the benzene ring has an electron-withdrawing group such as a cyano group and an electron-donating group such as a substituted alkoxy group at the same time. Since the compound of the invention has good xanthine oxidase-inhibitory action and uric acid-lowering action and does not have a structure derived from nucleic acid, the compound has advantages of high safety and excellent effects as compared with conventional compounds and is useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory bowel diseases, diabetic kidney diseases, diabetic retinopathy, or the like.

本发明涉及一种 2-苯基噻吩衍生物或其盐，其中噻吩环被羧基或类似基团取代，苯环上同时具有一个取电子基团（如氰基）和一个供电子基团（如取代的烷氧基）。由于本发明化合物具有良好的黄嘌呤氧化酶抑制作用和降尿酸作用，且不具有来自核酸的结构，因此与传统化合物相比，本发明化合物具有安全性高、效果优异的优点，可作为高尿酸血症、痛风、炎症性肠病、糖尿病肾病、糖尿病视网膜病变或类似疾病的治疗剂或预防剂。