7675-01-6

Upstream product

• 188290-36-0 thiophene 
• 590-92-1 3-Bromopropionic acid 
• 7774-74-5 Thiophene-2-thiol 
• 79-10-7 acrylic acid 

Downstream Products

• 7675-04-9 5,6-dihydro-4H-thieno[2,3-b]thiopyran-4-one 
• 1432445-18-5 3-(thiophen-2-ylthio)-1-(4-(4-(trifluoromethyl)phenyl)piperazin-1-yl)propan-1-one 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of 1,4-dihydrothieno[3′, 2′:5,6]thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives as potential estrogen receptor antagonists

The estrogen receptor is a target for therapeutic agents for hormone replacement in menopausal women, osteoporosis, reproductive cancers such as breast cancer, uterine cancer and prostate cancer. 1,4-Dihydrothieno[3′, 2′:5,6]thiopyrano[4,3-c]pyrazole-3-ca

Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase

The management of blood glucose levels and the avoidance of diabetic hyperglycemia are common objectives of many therapies in the treatment of diabetes. An aryl piperazine compound 3a (RTC1) has been described as a promoter of glucose uptake, in part through a cellular mechanism that involves inhibition of NADH:ubiquinone oxidoreductase. We report herein the synthesis of 41 derivatives of 3a (RTC1) and a systematic structure-activity-relationship study where a number of compounds were shown to effectively stimulate glucose uptake in vitro and inhibit NADH:ubiquinone oxidoreductase. The hit compound 3a (RTC1) remained the most efficacious with a 2.57 fold increase in glucose uptake compared to vehicle control and micromolar inhibition of NADH:ubiquinone oxidoreductase (IC50 = 27 μM). In vitro DMPK and in vivo PK studies are also described, where results suggest that 3a (RTC1) would not be expected to provoke adverse drug-drug interactions, yet be readily metabolised, avoid rapid excretion, with a short half-life, and have good tissue distribution. The overall results indicate that aryl piperazines, and 3a (RTC1) in particular, have potential as effective agents for the treatment of diabetes.

Trimethylamine and application of trimethylamine

The invention belongs to the field of medicine technology, and relates to a trimethylamine and apreparation method thereof and an application as the epidermal growth factor receptor tyrosine kinase inhibitor. The compounds, a prodrugs of the compounds, a pharmaceutically active metabolites and the pharmaceutically acceptable salts have the structure of formula (I) : R may be independently selectedfrom the group consisting of hydrogen, C1-C6 alkyl; R', R'' are independently selected from the group consisting of hydrogen, C1-C6 alkyl, substituted or unsubstituted phenyl, wherein the substituentis C1-C4 alkyl, C1-C4 alkoxy, halogen, halogenated C1-C4 alkyl, halogenated C1-C4 alkoxy, substituted or unsubstituted C1-C6 alkyl, wherein the substituent is dimethylamino, morpholinyl, methoxyphenoxy, methoxyphenyl; R', and R'', together with a nitrogen atom to which they are attached, form a morpholinyl or a cycloaliphatic radical. The formula is shown in the formula.

1 - (4 - Hydroxy imine base thiophen and [2, 3 - b] thiapyran formyl) piperazine compound and use thereof (by machine translation)

The invention belongs to the field of medical technology, relates to 1 - (4 - hydroxy imine base thiophen and [2, 3 - b] thiapyran formyl) piperazine compound and its application. The 1 - (4 - hydroxy imine base thiophen and [2, 3 - b] thiapyran formyl) piperazine compound comprises the following structure, wherein R is selected from hydrogen, halogen, C1 - C4 alkyl, C1 - C4 alkoxy, halogenated C1 - C4 alkyl, halogenated C1 - C4 alkoxy. The invention the 1 - (4 - hydroxy imine base thiophen and [2, 3 - b] thiapyran formyl) piperazine compound, a stereoisomer thereof, a pharmaceutically acceptable salt, or a prodrug or pharmaceutically active metabolite can be combined or separate with the prior drug use for preparation for the treatment of epidermal growth factor receptor signal transferred to the maladjustment of the related disease, wherein the epidermal growth factor receptor as HER - 1, HER - 2, HER - 3 or HER - 4, wherein the epidermal growth factor receptor signal transferred to the maladjustment of the related disease is a non-small cell lung cancer, gastric cancer, breast cancer, ovarian cancer, renal cell carcinoma, colorectal cancer, bladder and cervical squamous cell carcinoma. (by machine translation)

Thiophenothiazolacyl piperazine compound and medical use thereof

The invention belongs to the technical field of medicines, and relates to a thiophenothiazolacyl piperazine compound and a preparation method thereof as well as application of the thiophenothiazolacylpiperazine compound as an epidermal growth factor receptor tyrosine kinase inhibitor. The compound, a precursor drug thereof, an active metabolite of the drug and pharmaceutically acceptable salt are as shown in the formula (I), wherein R is independently selected from hydrogen and methyl; R' is independently selected from hydrogen, C1-C4 alkyl, C1-C4 alkoxy, hydroxyl, cyan, halogen, amino, nitryl, trifluoromethyl or trifluoromethoxy.

1-(thieno[2,3-b] thiapyran formyl-4-aliphatic piperazine compound and medicinal application thereof

The invention belongs to the technical field of medicines and relates to a 1-(thieno[2,3-b] thiapyran formyl-4-aliphatic piperazine compound and medicinal application thereof. The compound is of a structure as shown in the specification, in the formula, R is independently selected from hydrogen and methyl; R' is independently selected from methyl, benzyl, benzhydryl and (4-chlorphenyl) (phenyl) methyl. The 1-(thieno[2,3-b] thiapyran formyl-4-aliphatic piperazine compound provided by the invention and a stereisomer, a pharmaceutically acceptable salt, a precursor medicine or a medicine active metabolite thereof can be combined with a conventional medicine or are independently used to prepare medicines for related diseases such as epidermal growth factor receptor signal transferring disorder, an epidermal growth factor receptor is HER-1, HER-2, HER-3 or HER-4, the related diseases such as epidermal growth factor receptor signal transferring disorder are non-small cell lung cancer, stomach cancer, breast cancer, ovarian cancer, renal cell carcinoma, colorectal cancer, bladder cancer and head and neck squamous cell carcinoma.

4-hydroximino thieno[2,3-b] thiapyran-2-formamide compound and application thereof

The invention belongs to the technical field of medicines and relates to a 4-hydroximino thieno[2,3-b] thiapyran-2-formamide compound and medicinal application thereof. The 4-hydroximino thieno[2,3-b]thiapyran-2-formamide compound is of a structure as shown in the specification, in the formula, R', R'' and R''' are independently selected from hydrogen and phenyl, C1-C6 alkyl substituted phenyl,C1-C6 alkoxy substituted phenyl, halogen substituted phenyl, halogen C1-C6 alkoxy substituted phenyl and substituted C1-C6 alkyl; phenyl or morpholinyl is adopted as a substituent group, or R' and R''and N atoms connected with R' and R'' form the morpholinyl or piperidyl. The 4-hydroximino thieno[2,3-b] thiapyran-2-formamide compound provided by the invention and a stereisomer, a pharmaceuticallyacceptable salt, a precursor medicine or a medicine active metabolite thereof can be combined with a conventional medicine or are independently used to prepare medicines for related diseases such asepidermal growth factor receptor signal transferring disorder.

Thiophene and benzopyran pyrazole compound and its medical use

The invention belongs to the field of medical technologies, and relates to a thieno-thiopyrano pyrazole compound and pharmaceutical applications thereof. The thieno-thiopyrano pyrazole compound comprises derivatives of the thieno-thiopyrano pyrazole compound and pharmaceutical applicable salts. The thieno-thiopyrano pyrazole compound and salts added by pharmaceutically applicable acids of the compound can be combined with existing drugs or used alone as a lipoxygenase inhibitor, and used for treating related diseases such as chronic dull pains including inflammations, gout, headache, toothache, neuralgia and arthralgia which are relevant to an arachidonic acid metabolizing process.

Thiopheneglyoxylic and sulfur miscellaneous compound and use thereof

The invention belongs to the technical field of medicines and relates to a thienothio compound and an application thereof. A thienothiapyran compound comprises derivatives and pharmaceutically applicable salt of the thienothiapyran compound, and has a str

Identification of 1, 4-Dihydrothieno[3', 2':5, 6]thiopyrano [4, 3-c]pyrazole derivatives as human 5-lipooxygenase inhibitors

A series of novel 1,4-dihydrothieno[3',2':5,6]thiopyrano [4,3-c]-pyrazole-3-carboxamide derivatives were synthesized and evaluated for their inhibitory activity to human 5-lipo-oxygenase (5-LOX). Compound 7c was found to exhibit significant inhibition to human 5-LOX with IC50 value of 5.7 ± 0.9 μM. Compound 7c was further studied using molecular docking in order to delineate its structure-activity relationship and to gain insight into the design of effective 5-LOX inhibitors.