197979-67-2

Upstream product

• 197979-66-1 methyl (Z)-3-(3',5'-dimethoxyphenyl)-2-[(E)-1-(4-methylpiperazin-1-ylcarbamoyl)-2-phenylvinyl]-2-butenoate 
• 6928-85-4 N-amino-N'-methylpiperazine 
• 197979-64-9 2-[1-(3',5'-dimethoxyphenyl)-ethylidene]-3-[1-phenyl-(E)-methylidene]-succinic acid 1-methyl ester 

Relevant academic research and scientific papers

Synthesis and evaluation of 1,4-diphenylbutadiene derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) production

Butadiene-imide 1 (T-686) derivatives were synthesized and evaluated for their inhibitory activity against PAI-1 production and their ADMET (DMPK and toxicology) profiles. Among these derivatives, compound 15k (T-2639) showed good antithrombotic activity in two rat thrombosis models without affecting bleeding time, indicating reduction of haemorrhagic risk. We also describe in this report a practical synthesis of 15k suitable for scale-up using Z,E-selective Stobbe condensation.

Practical synthetic method of (2Z,3E)-1,4-Diphenylbutadiene T-2639, an inhibitor of plasminogen activator inhibitor-1 (PAI-1) production

A practical synthetic method of (2Z,3E)-1,4-diphenylbutadiene derivative T-2369 (1), a potent inhibitor of plasminogen activator inhibitor-1 (PAI-1) production, is described. Conditions of Stobbe condensation in the conventional synthesis of T-2369 were e

Design, synthesis, and evaluation of orally active inhibitors of plasminogen activator inhibitor-1 (PAI-1) production

A novel series of butadiene-imide 1 (T-686) derivatives having an inhibitory activity against PAI-1 production was synthesized and evaluated their biological activities and DMPK profiles, in which 15k (T-2639) was selected as the best compound based on its strong antithrombotic activity and good bioavailability.

Butadiene derivatives and process for preparing thereof

A novel butadiene derivative of the formula: wherein Ring A is heterocycle, or benzene being optionally substituted by lower alkyl, alkoxy, nitro, hydroxy, substituted or unsubstituted amino or halogen, Ring B is heterocycle, or benzene being optionally substituted by lower alkoxy, lower alkylenedioxy or di-lower alkylamino, R1and R2are each H or lower alkyl, one of —COR32and —COR42is carboxyl, and the other is carboxyl being optionally esterified, or the corresponding amide or pyrrolidine derivatives, or a pharmaceutically acceptable salt thereof. Said compounds show excellent PAI-1 inhibitory activity and are useful in the prophylaxis or treatment of various thromboses such as myocardial infarction, intra-atrial thrombus in atrial fibrillation, cerebral infarction, angina pectoris, stroke, pulmonary infarction, deep venous thrombus (DVT), disseminated intravascular coagulation syndrome (DIC), diabetic complications, restenosis after percutaneous transluminal coronary angioplasty (PTCA), etc.