2033-77-4

Upstream product

• 61711-86-2 2-(3,4-dimethoxy-phenoxy)-ethanol 
• 2033-89-8 3,4-dimethoxyphenol 
• 106-93-4 ethylene dibromide 
• 558-13-4 carbon tetrabromide 
• 603-35-0 triphenylphosphine 
• 5150-42-5 2,3-dimethoxyphenol 

Downstream Products

• 91005-67-3 2-(3,4-Dimethoxy-phenoxy)-ethylhydrazin 
• 667936-09-6 1-{4-[2-(3,4-dimethoxy-phenoxy)-ethyl]-piperazin-1-yl}-6,6-bis-(4-fluoro-phenyl)-hexan-1-one 
• 1373830-22-8 (S)-2-(3,4-dimethoxyphenoxy)ethyl piperidine-2-carboxylate 
• 1374119-60-4 (S)-1-tert-butyl 2-(2-(3,4-dimethoxyphenoxy)ethyl) piperidine-1,2-dicarboxylate 
• 1374118-94-1 (S)-2-(3,4-dimethoxyphenoxy)ethyl-1-(3,3-dimethyl-2-oxopentanoyl)piperidine-2-carboxylate 
• 1433826-67-5 (S)-2-(3,4-dimethoxyphenoxy)ethyl 1-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carboxylate 
• 1373829-77-6 2-(3,4-dimethoxyphenoxy)ethyl (S)-1-(3,5-dichlorophenylsulfonyl)piperidine-2-carboxylate 
• 1373829-78-7 2-(3,4-dimethoxyphenoxy)ethyl (S)-1-(benzo[d]thiazol-6-ylsulfonyl)piperidine-2-carboxylate 
• 1433826-80-2 (S)-2-(3,4-dimethoxyphenoxy)ethyl 1-(2-oxo-2,3-dihydrobenzo[d]thiazol-6-ylsulfonyl)piperidine-2-carboxylate 
• 1422463-27-1 2-(2-((2-(3,4-dimethoxyphenoxy)ethyl)amino)ethyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione 
• 1542785-75-0 tert-butyl 2-(3,4-dimethoxyphenoxy)ethyl(4-(trimethylsilyl)but-2-enyl)carbamate 
• 1542785-96-5 N-(2-(3,4-dimethoxyphenoxy)ethyl)-4-(trimethylsilyl)but-2-en-1-amine 
• 1542785-98-7 (S)-N-(2-(3,4-dimethoxyphenoxy)ethyl)-6-oxo-N-(4-(trimethylsilyl)but-2-en-1-yl)piperidine-2-carboxamide 
• 1542786-00-4 (S)-tert-butyl 2-((2-(3,4-dimethoxyphenoxy)ethyl)(4-(trimethylsilyl)but-2-en-1-yl)carbamoyl)-6-oxopiperidine-1-carboxylate 

Relevant academic research and scientific papers

Synthesis and pharmacological activity of a new series of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)-propan-2-ol analogs

β-Adrenergic receptor antagonists are important therapeutics for the treatment of cardiovascular disorders. In the group of β-blockers, much attention is being paid to the third-generation drugs that possess important ancillary properties besides inhibiting β-adrenoceptors. Vasodilating activity of these drugs is produced through different mechanisms, such as nitric oxide (NO) release, β2-agonistic action, α1-blockade, antioxidant action, and Ca2t entry blockade. Here, a study on evaluation of the cardiovascular activity of five new compounds is presented. Compound 3a is a methyl and four of the tested compounds (3b–e) are dimethoxy derivatives of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)-ethylamino)propan-2-ol. The obtained results confirmed that the methyl and dimethoxy derivatives of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and their enantiomers possess α1- and β1-adrenolytic activities and that the antiarrhythmic and hypotensive effects of the tested compounds are related to their adrenolytic properties.

Bicyclic aza-amides for treatment of psychiatric disorders

The present invention relates to compounds of formula (I) having a bicyclic aza-amides scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said bicyclic aza-amides compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.

BICYCLIC AZA-AMIDES FOR TREATMENT OF PSYCHIATRIC DISORDERS

The present invention relates to compounds of formula (I) having a bicyclic aza-amides scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said bicyclic aza- amides compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.

Pipecolate-diketoamides for treatment of psychiatric disorders

The present invention relates to compounds having a pipecolate diketoamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable

PIPECOLATE-DIKETOAMIDES FOR TREATMENT OF PSYCHIATRIC DISORDERS

The present invention relates to compounds having a pipecolate diketoamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pipecolate diketoamide compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.

Development of unsymmetrical dyads as potent noncarbohydrate-based inhibitors against human β-N-acetyl-D-hexosaminidase

Human β-N-acetyl-D-hexosaminidase has gained much attention due to its roles in several pathological processes and been considered as potential targets for disease therapy. A novel and efficient skeleton, which was an unsymmetrical dyad containing naphthalimide and methoxyphenyl moieties with an alkylamine spacer linkage as a noncarbohydrate-based inhibitor, was synthesized, and the activities were valuated against human β-N-acetyl-D- hexosaminidase. The most potent inhibitor exhibits high inhibitory activity with Ki values of 0.63 μM. The straightforward synthetic manners of these unsymmetrical dyads and understanding of the binding model could be advantageous for further structure optimization and development of new therapeutic agents for Hex-related diseases.

Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52

The FK506-binding proteins (FKBP) 51 and 52 are cochaperones that modulate the signal transduction of steroid hormone receptors. Both proteins have been implicated in prostate cancer. Furthermore, single nucleotide polymorphisms in the gene encoding FKBP51 have been associated with a variety of psychiatric disorders. Rapamycin and FK506 are two macrocyclic natural products that bind to these proteins indiscriminately but with nanomolar affinity. We here report the cocrystal structure of FKBP51 with a simplified α-ketoamide analogue derived from FK506 and the first structure-activity relationship analysis for FKBP51 and FKBP52 based on this compound. In particular, the tert-pentyl group of this ligand was systematically replaced by a cyclohexyl ring system, which more closely resembles the pyranose ring in the high-affinity ligands rapamycin and FK506. The interaction with FKBPs was found to be surprisingly tolerant to the stereochemistry of the attached cyclohexyl substituents. The molecular basis for this tolerance was elucidated by X-ray cocrystallography.

Calcium channel inhibitors comprising benzhydril spaced from piperazine

Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Calcium channel inhibitors comprising benzhydril spaced from piperazine

Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Calcium channel inhibitors comprising benzhydril spaced from piperazine

Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.