887624-04-6

Basic information

• Product Name: 1-Piperazinecarboxylic acid, 4-(4-phenyl-2-thiazolyl)-, 1,1-dimethylethyl ester
• CAS NO: 887624-04-6
• Molecular Formula: C18H23N3O2S
• Molecular Weight: 345.466
• Mol File: 887624-04-6.mol

Chemical Properties

• CAS DataBase Reference: 1-Piperazinecarboxylic acid, 4-(4-phenyl-2-thiazolyl)-, 1,1-dimethylethyl ester(CAS DataBase Reference)
• NIST Chemistry Reference: 1-Piperazinecarboxylic acid, 4-(4-phenyl-2-thiazolyl)-, 1,1-dimethylethyl ester(887624-04-6)
• EPA Substance Registry System: 1-Piperazinecarboxylic acid, 4-(4-phenyl-2-thiazolyl)-, 1,1-dimethylethyl ester(887624-04-6)

Safety Data

• Hazardous Substances Data: 887624-04-6(Hazardous Substances Data)

Upstream product

• 1018148-64-5 tert-butyl 4-(benzoylcarbamothioyl)piperazine-1-carboxylate 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 70-11-1 α-bromoacetophenone 
• 196811-66-2 4-(tert-butoxycarbonyl)piperazine-1-thiocarboxamide 
• 57516-16-2 2-bromo-4-phenyl-1,3-thiazole 
• 1826-23-9 2-chloro-4-phenylthiazole 

Downstream Products

• 887622-89-1 C₁₉H₂₁N₅O₂S 
• 1395320-72-5 C₂₅H₂₉N₅O₂S 
• 69389-14-6 4-phenyl-2-(piperazin-1-yl)thiazole 

Relevant articles and documents

The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119

A series of xanthine compounds derived from the previous hit 20i with modification on the terminal side chain was discovered through ring formation strategy. Systematic optimization of the compounds with rigid heterocycles in the hydrophobic side chain led to the new lead compound HBK001 (21h) with the improved DPP-IV inhibition and moderate GPR119 agonism activity in vitro. As a continuing work to further study the PK and PD profiles, 21h and its hydrochloride (22) were synthesized on grams scale and evaluated on the ADME/T and oral glucose tolerance test (OGTT) in ICR mice. Compound 22 showed the improved bioavailability and blood glucose-lowering effect in vivo compared to its free base 21h probably attributed to its improved solubility and permeability. The preliminary toxicity studies on compound 22 exhibited that the result of mini-Ames was negative and the preliminary acute toxicity LD50 in mice was above 1.5 g/kg, while it showed moderate inhibition on hERG channel with IC50 4.9 μM maybe due to its high lipophilicity. These findings will be useful for the future drug design for more potent and safer dual ligand targeting DPP-IV and GPR119 for the treatment of diabetes.

ACID ADDITION SALTS OF PIPERAZINE DERIVATIVES

The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and in particular as glycosidase inhibitors.

GLYCOSIDASE INHIBITORS

Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.

Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors

A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH) inhibitors that are therapeutically effective against pain. We carried out an optimization study of the l

AMIDE COMPOUND

There is provided a FAAH inhibitor and a prophylactic or therapeutic agent for cerebrovascular disorders or sleep disorders comprising it. The prophylactic or therapeutic agent comprises a compound of the formula (I0): wherein Z is oxygen or sulfur; R1 is aryl which may be substituted, or a heterocyclic group which may be substituted; R1a is a hydrogen atom, a hydrocarbon group which may be substituted, hydroxyl, etc.; R2 is piperidin-1,4-diyl which may be substituted, or piperazin-1,4-diyl which may be substituted; R3 is a group formed by eliminating two hydrogen atoms from a 5-membered aromatic heterocyclic group having 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur, which may be further substituted, -CO-, etc.; and R4 is a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; or a salt thereof.