101623-68-1

Upstream product

• 1600-27-7 mercury(II) diacetate 
• 101623-69-2 (1-chloroethyl)-(4-nitrophenyl)carbonate 
• 64-19-7 acetic acid 
• 100-02-7 4-nitro-phenol 

Downstream Products

• 101623-75-0 4-<2-hydroxy-3--N-isopropylamino>propoxy>benzeneacetamide 
• 1159589-12-4 ethyl 4-[[4-[1-(1-acetoxyethyl)oxycarbonylpiperidin-4-yl]-2-oxopiperazin-1-yl]acetyl]phenoxyacetate 
• 1041676-33-8 ethyl 2-(4-((3-((R)-3-((1-acetoxyethoxy)carbonylamino)-4-(2,4,5-trifluorophenyl)butanoyl)thiazolidine-2-carboxamido)methyl)phenoxy)-3-methylbutanoate 
• 1036708-93-6 4-dibenzo[b,f][1,4]thiazepin-11-yl-piperazine-1-carboxylic acid 1-acetoxy-ethyl ester 
• 75-07-0 acetaldehyde 
• 64-19-7 acetic acid 
• 101623-77-2 1--N-isopropylamino>-3--2-propanol 

Relevant academic research and scientific papers

Enzyme-catalyzed prodrug approaches for the histamine H3-receptor agonist (R)-α-methylhistamine

Five novel prodrug types of the potent and selective histamine H3-receptor agonist (R)-α-methylhistamine (1) were prepared and pharmacologically tested in vitro as well as in vivo. In particular, an amide of fatty acid, mono- and dicarbamates, an (acyloxy)alkylcarbamate, and a diphthalidyl derivative were synthesized, all of which require initial prodrug activation through an enzyme-catalyzed reaction in contrast to formerly developed azomethine prodrugs which are cleaved by chemical hydrolysis only. Further drug liberation may ensue spontaneously in a cascade to give 1. Since they have diverse stabilities the prodrugs were investigated for drug liberation in vitro under neutral, acidic, and basic conditions at different temperatures as well as with liver homogenates. In vivo investigation of prodrugs after oral administration to mice proved that the fatty amide 2, the Nα-methylcarbamate 4a, and the Nα-(1-(acetyloxy)ethylcarbamate) 5 showed moderate to high plasma levels of 1. Compound 5 displayed even more than 2.5 times the AUC for 1 than that of the reference azomethine prodrug BP2.94 in the periphery and also displayed a detectable drug level in the central nervous system. It was shown that prodrug approaches based on an initial enzyme-catalyzed liberation step are successfully applicable to different pro-moieties for improved bioavailability and prolonged half-live. These approaches may also be used for other aminergic compounds of this class to optimize pharmacokinetic behavior.

AZETIDINE DERIVATIVE, AND PRODRUG THEREOF

An object of the present invention is to provide a compound useful as a therapeutic or prophylactic drug for a disease involving the immune system, by suppressing a function of immune cells by suppressing proliferation of activated T cells or suppressing production of interferon alpha (IFN-α) by activated plasmacytoid dendritic cells (pDC), particularly an autoimmune disease such as systemic lupus erythematosus (SLE) and lupus nephritis in SLE patients. The present invention provides a compound represented by general formula (I) : [wherein X, R1, R2, R3, R4, R5 and R6 are as described in the description], or a pharmaceutically acceptable salt thereof.

PRODRUGS OF KALLIKREIN INHIBITORS

Disclosed are compounds of formula I, II, and III, and pharmaceutically acceptable salts thereof, which are inhibitors of kallikrein. Also provided are pharmaceutical compositions comprising such a compound, and methods involving use of the compounds and compositions in the treatment and prevention of acquired or hereditary angioedema, or other diseases and conditions characterized by aberrant kallikrein activity. (I) (II) (III)

Pharmaceutical composition for the treatment or prevention of stroke and systemic embolism

The present invention relates to a prodrug useful for treating or preventing a stroke and systemic embolism and suitable for being effectively used in the oral delivery of dabigatran, and to a compound represented by chemical formula 1, a pharmaceutically acceptable salt thereof, and a hydrate thereof or a solvate thereof. The compound represented by the chemical formula 1, the pharmaceutically acceptable salt thereof, and the hydrate thereof or the solvate thereof are useful for treating or preventing a stroke and systemic embolism, and is suitable for being effectively used in oral delivery since the absorption rate, that is, bioavailability of dabigatran is improved.(AA) DSC curve of dabigatran pivoxyl (+)-(1S)- campo-10-sulfonateCOPYRIGHT KIPO 2015

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to, the prevention and treatment of Alzheimer's disease.

COMPOUNDS AND USES THEREOF

This invention relates to novel compounds having the structural Formula (I) below: and their pharmaceutically acceptable salts or tautomers, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of at least one symptom or condition associated with schizophrenia and other psychotic disorders, dementia and other cognitive disorders, anxiety disorders, mood disorders, sleep disorders, disorders usually first diagnosed in infancy, childhood, or adolescence and neurodegenerative disorders.

3', 5' - CYCLIC NUCLEOSIDE ANALOGUES FOR TREATMENT OF HCV

This invention provides compounds according to formula (I) where B is a 6-membered monocyclic nitrogen-containing heteroaryl group or a 5 + 6 fused bicyclic nitrogen-containing heteroaryl group, and A is selected from Groups (1), (2), (3), and (4) where Groups (1), (2), (3), and (4), are defined herein. These compounds are useful in the treatment of Hepatitis C infection.

Prodrugs of GABA analogs, compositions and uses thereof

The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

PEPTIDIC THROMBIN INHIBITOR COMPOUND

The present invention relates to a novel thrombin inhibitor compound which has a good inhibitory effect against thrombosis and can be orally administered, a process for preparing the same, and to a composition for the therapeutic and/or prophylactic treatment of various diseases associated with thrombin inhibition mechanism, which comprises the same as an active ingredient.

Pro-drug and use thereof as a medicament

The invention relates to a pro-drug comprising a cyclic undecapeptide wherein the peptide chain thereof comprises at least one amino acid residue of general formula (1) wherein the carbon atom Ca is one of the links in said undecapeptide cycle;