59727-98-9

Upstream product

• 59-92-7 levodopa 
• 37169-36-1 methyl (S)-2-(tert-butoxycarbonylamino)-3-(3,4-dihydroxyphenyl)propanoate 
• 100-39-0 benzyl bromide 
• 125279-74-5 (R)-2-tert-Butoxycarbonylamino-3-(3,4-dihydroxy-phenyl)-propionic acid methyl ester 
• 125228-11-7 (R)-3-(3,4-Bis-benzyloxy-phenyl)-2-tert-butoxycarbonylamino-propionic acid methyl ester 
• 30033-24-0 (2S)-3-(3,4-dihydroxyphenyl)-2-[(tert-butoxy)carbonylamino]propanoic acid 
• 1421-65-4 L-dopa methyl ester hydrochloride 
• 24424-99-5 di-tert-butyl dicarbonate 
• 7101-51-1 L-DOPA methyl ester 
• 130962-23-1 (S)-benzyl 3-(3,4-bis-benzyloxyphenyl)-2-(tert-butoxycarbonylamino)propanoate 
• 100-44-7 benzyl chloride 
• 125228-11-7 3-(3,4-bis-benzyloxyphenyl)-2-tert-(butoxycarbonylamino)propionic acid methyl ester 

Downstream Products

• 503416-71-5 Boc-(L)-DOPA[OBn]2-CHN₂ 
• 125228-11-7 3-(3,4-bis-benzyloxyphenyl)-2-tert-(butoxycarbonylamino)propionic acid methyl ester 
• 913259-53-7 Benzyl-DOPA-NH-Boc-COOCH₂CH₂OH 
• 934290-08-1 3-(3,4-bis-benzyloxy-phenyl)-2-tert-butoxycarbonylamino-propionic acid 2-[3-(3,4-bis-benzyloxy-phenyl)-2-tert-butoxycarbonylamino-propionyloxy]-ethyl ester 
• 871580-95-9 (1R,2R)-2-hydroxy-1-methylpropyl (2S)-2-[(tert-butoxy)carbonylamino]-3-[3,4-bis(phenylmethoxy)phenyl]propanoate 

Relevant academic research and scientific papers

The effect of l-DOPA hydroxyl groups on the formation of supramolecular hydrogels

Fmoc-l-DOPA-d-Oxd-OH was prepared starting from commercially available l-DOPA. Its gelation ability was tested by comparison with Fmoc-l-Tyr-d-Oxd-OH and Fmoc-l-Phe-d-Oxd-OH using ten different triggers. Among them, only GdL, CaCl2 and ZnCl2 form strong hydrogels with the three gelators. The analysis of the aerogels obtained by freeze drying the hydrogels show that the three gelators always induce the formation of dense networks, which strongly depend on the nature of the gelator. Rheological analysis of these samples demonstrates that stronger gels were obtained using the l-Tyr containing gelator, while the l-DOPA containing hydrogels were characterized by a storage modulus approximately one order of magnitude lower. Finally, the l-Phe containing gelators show a different trend with respect to the other samples depending on the trigger used. All the hydrogels show a thixotropic behaviour at the molecular level. These results indicate that hydrogel formation is sensitive to both the number of the hydroxyl moieties on the aromatic rings and trigger used.

COMPOSITIONS AND METHODS FOR THE TREATMENT OF PAIN AND DEPENDANCE DISORDERS

Provided herein are (e.g., controlled release) compositions for the treatment of acute or chronic diseases or disorders. Described herein are processable opioid conjugates. Also described herein are compositions and methods for the treatment of central nervous system (CNS) diseases or disorders including chronic pain (e.g., cancer pain), acute pain, opioid addiction, alcohol addiction, alcohol dependence, opioid-induced constipation, and narcotic depression. Said compositions and methods comprise opioid agonists and/or opioid antagonists, which demonstrate CNS activity and/or other desirable activities. Injection of said compositions subcutaneously or intraspinally provides therapeutic benefit to individuals suffering from CNS diseases or disorders

Genetically Engineered Polypeptide Adhesive Coacervates for Surgical Applications

Adhesive hydrogels have been developed for wound healing applications. However, their adhesive performance is impaired dramatically due to their high swelling on wet tissues. To tackle this challenge, we fabricated a new type of non-swelling protein adhesive for underwater and in vivo applications. In this soft material, the electrostatic complexation between supercharged polypeptides with oppositely charged surfactants containing 3,4-dihydroxylphenylalanine or azobenzene moieties plays an important role for the formation of ultra-strong adhesive coacervates. Remarkably, the adhesion capability is superior to commercial cyanoacrylate when tested in ambient conditions. Moreover, the adhesion is stronger than other reported protein-based adhesives in underwater environment. The ex vivo and in vivo experiments demonstrate the persistent adhesive performance and outstanding behaviors for wound sealing and healing.

Water-soluble L-DOPA esters

The present invention relates to novel compounds of the formula I, methods for their preparation and their use for treatment of diseases. The invention discloses the synthesis of levodopa (L-DOPA) esters by coupling polyhydroxy compounds or their derivatives to the L-DOPA carboxyl group. The synthesis allows to produce L-DOPA derivatives which are highly soluble in water as well as aqueous and biocompatible liquids and have an improved hydrolytic stability in water or aqueous and biocompatible media for an application over several days. The invention helps producing L-DOPA substances for applications in the fields of medicine, biology and medical engineering as well as in the pharmaceutical industry.

Large Amino Acid Transporter 1 Selective Liposomes of l -DOPA Functionalized Amphiphile for Combating Glioblastoma

Despite significant progress in neurosurgery and radiation therapy during the past decade, overall survivability (OS) of glioblastoma patients continues to be less than 2 years. The scope of systemic chemotherapy is greatly limited by poor drug transport

Similar EDTA ligand containing O-phenolic hydroxyl, as well as non-gadolinium magnetic resonance contrast agent and preparation method thereof

The invention discloses a similar EDTA ligand namely 2,2',2'',2'''-((3-(3,4-dihydroxyphenyl) propane-1,2diyl) ethylene diamine tetraacetic containing O-phenolic hydroxyl, a non-gadolinium paramagnetic metal coordination compound namely a magnetic resonanc

MULTIMODAL CONTRAST AND RADIOPHARMACEUTICAL AGENT FOR AN IMAGING AND A TARGETED THERAPY GUIDED BY IMAGING

The present invention relates to a multimodal contrast and radiopharmaceutical agent for an imaging and a targeted therapy guided by imaging.

Design, synthesis, and preliminary pharmacological evaluation of new imidazolinones as l-DOPA prodrugs

l-DOPA, the immediate biological precursor of dopamine, is still considered the drug of choice in the treatment of Parkinson's disease. However, therapy with l-DOPA is associated with a number of acute problems. With the aim to increase the bioavailability after oral administration, we designed a multi-protected l-DOPA prodrugs able to release the drug by both spontaneous chemical or enzyme catalyzed hydrolysis. The new compounds have been synthesized and preliminarily evaluated for their water solubility, log P, chemical stability, and enzymatic stability. The results indicate that the incorporation of the amino acidic moiety of l-DOPA into an imidazoline-4-one ring provides prodrugs sufficiently stable to potentially cross unchanged the acidic environment of the stomach, and to be absorbed from the intestine. They also might be able to release l-DOPA in human plasma after enzymatic hydrolysis. The ability of prodrugs 6a-b to increase basal levels of striatal DA, and influence brain neurochemistry associated with dopaminergic activity following oral administration, as well as the radical-scavenging activity against DPPH for compounds 6a-b and 15a are also reported.

Design, synthesis and biological evaluation of l-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease

A range of amide derivatives of l-dopa were synthesized and investigated for their pharmacological activity and their ability to be converted to l-dopa using the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat, as an experimental model of Parkinson's

METHOD OF PREPARING DENDRITIC DRUGS

Synthetic design of drug-incorporated novel dendrimer structures for quantitatively controlled drug delivery. The dendritic drugs have better control and thus a quantitative drug release can be obtained. There are no prior art dendritic drugs that control release both sequentially and quantitatively like the dendritic drugs disclosed herein. The dendritic drugs are formed by incorporating multiple same type drug units or more than two different drug types into a dendritic cascade structure to form a dendrimer drug.