101623-70-5

Upstream product

• 50780-50-2 4-chloromethoxycarbonyloxy-1-nitrobenzene 
• 101623-71-6 iodomethyl(4-nitrophenyl)carbonate 
• 100-02-7 4-nitro-phenol 
• 563-63-3 silver(I) acetate 

Downstream Products

• 1541195-88-3 (2S,3S,4R)-2-acetoxymethoxycarbonylamino-1-O-α-D-galactopyranosyl-4-O-(6-phenylhexanoyl)octadecane-1,3,4-triol 
• 1036708-92-5 4-dibenzo[b,f][1,4]thiazepin-11-yl-piperazine-1-carboxylic acid acetoxymethyl ester 

Relevant academic research and scientific papers

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.

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.

N-acylamino acid amide compounds and intermediates for preparation thereof

The present invention discloses the compound represented by the formula (I): wherein A represents the following formula (a-1) or the following formula (a-2): B represents the following formula (b): (wherein the symbols are each as defined in the specification) or a pharmaceutically acceptable salts thereof, and intermediates for the preparation thereof, which have excellent platelet aggregation inhibitory activity and other properties and useful as prophylactic or therapeutic agents for diseases associated with a fibrinogen receptor, thrombosis, infarction and the like.

Process for preparing novel N-(acyloxy-alkoxy)carbonyl derivatives useful as bioreversible prodrug moieties for primary and secondary amine functions in drugs

This invention relates to a new one-step process for preparation of novel N-(acyloxyalkoxy)carbonyl derivatives useful as bioreversible prodrug moieties for drugs having a primary or secondary amine function thereon.

(Acyloxy)alkyl Carbamates as Novel Bioreversible Prodrugs for Amines: Increased Permeation through Biological Membranes

(Acyloxy)alkyl carbamates of the type R1R2N-CO-O-CHR3-OCO-R4 are described as novel bioreversible prodrugs for primary and secondary amines.These were prepared either by a one-step reaction involving nucleophilic attack on p-nitrophenyl α-(acyloxy)alkyl carbonates with displacement of p-nitrophenol or by reaction of α-haloalkyl carbamates with silver or mercury salts of carboxylic acids.Enzymatic hydrolysis of the ester bond in these ester carbamates leads to a cascade reaction resulting in rapid regeneration of the parent amine.Permeability measurements of such nonionic derivatives of atenolol, betaxolol, pindolol, propranolol, and timolol through fuzzy rat skin and rabbit cornea mounted on diffusion cells show that derivatization of the hydrophilic β-blockers results in several-fold increase in permeation through these biological membranes.However, prodrug modification of the lipophilic β-blockers leads to little advantage in permeability characteristics.