72349-01-0

Basic information

• Product Name: Benzyl 4-(2-oxoimidazolidin-1-yl)piperidine-1-carboxylate
• Synonyms: Benzyl 4-(2-oxoimidazolidin-1-yl)piperidine-1-carboxylate
• CAS NO: 72349-01-0
• Molecular Formula: C₁₆H₂₁N₃O₃
• Molecular Weight: 303.35624
• Mol File: 72349-01-0.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Benzyl 4-(2-oxoimidazolidin-1-yl)piperidine-1-carboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: Benzyl 4-(2-oxoimidazolidin-1-yl)piperidine-1-carboxylate(72349-01-0)
• EPA Substance Registry System: Benzyl 4-(2-oxoimidazolidin-1-yl)piperidine-1-carboxylate(72349-01-0)

Safety Data

• HazardClass: IRRITANT
• Hazardous Substances Data: 72349-01-0(Hazardous Substances Data)

Upstream product

• 501-53-1 benzyl chloroformate 
• 52210-86-3 1,3,4,5-tetrahydro-1-(4-piperidinyl)-2H-imidazol-2-one 
• 120278-07-1 benzyl 4-aminopiperidine-1-carboxylate 
• 1943-83-5 2-chloroethyl isothiocyanate 
• 530-62-1 1,1'-carbonyldiimidazole 
• 19099-93-5 benzyl 4-oxo-1-piperidinecarboxylate 
• 57260-73-8 N-BOC-1,2-diaminoethane 

Downstream Products

• 72338-89-7 1-(1-carbobenzoxy-4-piperidyl)-3-[2-(2-tetrahydropyranyloxy)-ethyl]-imidazolidin-2-one 
• 52210-86-3 1,3,4,5-tetrahydro-1-(4-piperidinyl)-2H-imidazol-2-one 

Relevant articles and documents

Discovery of a tetrahydropyrimidin-2(1 H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor

Coagulation enzyme factor Xa (FXa) is a particularly promising target for the development of new anticoagulant agents. We previously reported the imidazo[1,5-c]imidazol-3-one derivative 1 as a potent and orally active FXa inhibitor. However, it was found that 1 predominantly undergoes hydrolysis upon incubation with human liver microsomes, and the human specific metabolic pathway made it difficult to predict the human pharmacokinetics. To address this issue, our synthetic efforts were focused on modification of the imidazo[1,5-c] imidazol-3-one moiety of the active metabolite 3a, derived from 1, which resulted in the discovery of the tetrahydropyrimidin-2(1H)-one derivative 5k as a highly potent and selective FXa inhibitor. Compound 5k showed no detectable amide bond cleavage in human liver microsomes, exhibited a good pharmacokinetic profile in monkeys, and had a potent antithrombotic efficacy in a rabbit model without prolongation of bleeding time. Compound 5k is currently under clinical development with the code name TAK-442.

LINEAR TRICYCLIC COMPOUNDS AS P38 KINASE INHIBITORS

The present invention comprises a new class of compounds useful for the prophylaxis and treatment of p38 kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A, B1, B2, C1-4, L1, R1, R2, R5, m and n are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use such as treatment of kinase mediated diseases by administering the compounds of Formula I or compositions including the compounds of Formula I, and intermediates and processes useful for the preparation of compounds of Formula I.

Chemical compounds

Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).

Piperidino-propanols

The invention relates to novel piperidino-propanols, especially 1-(3-heterocyclyloxy-2-hydroxy-propanol)-4-(N-diazcyclyl)-piperidines of the formula STR1 in which R1 is a substituted or unsubstituted heteroaryl radical, R2 is hydrogen or a substituted or unsubstituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic hydrocarbon radical or an acyl radical and alk is lower alkylene which separates the two nitrogen atoms from one another by 2 or 3 carbon atoms, or is a substituted or unsubstituted 1,2-phenylene radical, and salts thereof, as well as processes for their preparation, and also to pharmaceutical preparations containing these compounds and the use thereof, preferably in the form of pharmaceutical preparations as antihypertensive agents, antitachycardiac agents and α-sympathicolytic agents.