157025-33-7

Usage

Uses

Used in Pharmaceutical Industry:
5-(Tributylstannyl)thiazole is used as a synthetic intermediate for the preparation of hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors. These inhibitors are of significant interest due to their potential therapeutic applications in the treatment of neurodegenerative diseases, such as Alzheimer's disease, by targeting the enzyme responsible for the production of amyloid-beta peptides, which are implicated in the pathology of the disease.

InChI:InChI=1/3C4H9.C3H2NS.Sn/c3*1-3-4-2;1-2-5-3-4-1;/h3*1,3-4H2,2H3;1,3H;/rC15H29NSSn/c1-4-7-10-18(11-8-5-2,12-9-6-3)15-13-16-14-17-15/h13-14H,4-12H2,1-3H3

Upstream product

• 3034-55-7 5-bromo-1,3-thiazole 
• 1461-22-9 tributyltin chloride 
• 79265-30-8 2-(trimethylsilyl)thiazole 
• 288-47-1 1,3-thiazole 
• 1461-22-9 tri-n-butylstannyl chloride 
• 263868-71-9 5-(tributylstannyl)-2-(trimethylsilyl)thiazole 

Downstream Products

• 157025-18-8 (6R,7R)-8-Oxo-7-phenylacetylamino-3-thiazol-5-ylmethyl-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid benzhydryl ester 
• 177553-56-9 (6R,7R)-8-Oxo-7-phenylacetylamino-3-thiazol-5-yl-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid benzhydryl ester 
• 1025902-20-8 (5R,6S)-6-((R)-1-Hydroxy-ethyl)-7-oxo-3-thiazol-5-yl-1-aza-bicyclo[3.2.0]hept-2-ene-2-carboxylic acid 4-nitro-benzyl ester 
• 332113-80-1 5-(4-acetylphenyl)thiazole 
• 946126-13-2 4-methyl-3-(3-nitrobenzyl)-7-(thiazol-5-yl)-2-oxo-2H-1-benzopyran 
• 1163692-41-8 C₃₀H₂₆ClF₄N₃O₆S 
• 1216771-64-0 4-(2-amino-5-(thiazol-5-yl)pyridin-3-yl)benzamide 
• 1221403-62-8 C₂₄H₂₂N₄O₂S 
• 1245510-06-8 C₂₇H₂₈N₄O₂S 
• 1450019-91-6 5-(2-(4-fluorophenyl)-5-(thiazol-2-yl)-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-imidazol-4-yl)-3-methoxypyridin-2-amine trifluoroaceate 
• 1272354-00-3 C₂₃H₁₇N₅S 

Relevant academic research and scientific papers

Synthesis by direct arylation of thiazole-derivatives: Regioisomer configurations-optical properties relationship investigation

The synthesis of thiazole(Tz)-based regioisomer materials using selective direct arylation to avoid any protection steps has been developed. A series of trimers in which the Tz groups sandwich either an electron-rich or an electron-deficient unit, with a regioselective orientation of the respective Tz unit, has therefore been synthesized. This chemical strategy has also been followed to synthesize a second series of pentamers in which the Tz group is used as a conjugated bridge between an electron-rich central unit and electron-deficient end-capping groups and vice versa. On both trimers and pentamers, the effect of Tz orientation on the conjugation properties of the synthesized materials was investigated by a combination of experimental measurements and density functional theory calculations. This study highlights that control of the orientation of the Tz unit leads to the synthesis of the most conjugated regioisomer derivative. The present work gives chemical synthesis tools for the synthesis of selectively oriented Tz-based materials as well as a general guideline for the design of Tz-based materials with the highest conjugation length, including the Tz-orientation effect.

HEPATITIS B VIRAL ASSEMBLY EFFECTORS

Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.

p27 PROTEIN INDUCER

The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G 1 , G 2 , G 3 and G 8 are each independently selected from -N= etc., Ring G 6 is selected from divalent aryl etc., A is selected from amino etc., G 4 is selected from oxygen etc., G 5 is selected from oxygen etc., G 7 is selected from -CH 2 - etc., and R 2 is selected from C 1-6 alkyl etc.

INHIBITORS OF POLO-LIKE KINASE

The present invention provides compounds having a structure according to Formula (I):or a salt or solvate thereof, wherein ring A, U1, U2, U3, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.

p27 PROTEIN INDUCER

The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G1, G2, G3 and G8 are each independently selected from -N= etc., Ring G6 is selected from divalent aryl etc., A is selected from amino etc., G4 is selected from oxygen etc., G5 is selected from oxygen etc., G7 is selected from -CH2- etc., and R2 is selected from C1-6 alkyl etc.

FUSED HETEROCYCLIC DERIVATIVES AND METHODS OF USE

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

NOVEL COUMARIN DERIVATIVE HAVING ANTITUMOR ACTIVITY

The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from -N= etc., Y3 and Y4 are selected from -CH= etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.

Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives

This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

HETEROCYCLIC COMPOUNDS

Compounds of formula I : and pharmaceutically-acceptable salts thereof, wherein Ar and R are as defined in the specification, compositions containing such compounds and the use of such compounds and compositions for use in therapy.