494769-34-5

Usage

Uses

Used in Pharmaceutical Research and Development:
TFFCA is utilized as a pharmaceutical intermediate for the synthesis of potential antitumor agents, contributing to the development of new cancer treatments.
Used in the Synthesis of Heterocycles:
TFFCA serves as a building block in the synthesis of various heterocycles, which are important in the creation of complex organic compounds with diverse applications in the pharmaceutical industry.
Used in the Development of 5-HT1A Receptor Agonists:
TFFCA is employed as a key component in the development of 5-HT1A receptor agonists, which are significant in the treatment of neurological disorders and other related conditions.
Used in the Development of Neurological Disorder Treatments:
TFFCA is used in the research and development of potential treatments for neurological disorders, highlighting its versatility and importance in the pharmaceutical sector.

InChI:InChI=1/C9H12N2O3S/c1-9(2,3)14-8(13)11-7-10-6(4-12)5-15-7/h4-5H,1-3H3,(H,10,11,13)

Upstream product

• 494769-44-7 (4-hydroxymethylthiazol-2-yl)carbamic acid tert-butyl ester 
• 189512-01-4 ethyl 2-[(tert-butoxycarbonyl)amino]thiazole-4-carboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1100350-49-9 tert-butyl (4-((methoxy(methyl)amino)methyl)thiazol-2-yl)carbamate 
• 1108653-08-2 tert-butyl (5-fluoro-4-((methoxy(methyl)amino)methyl)thiazol-2-yl)carbamate 
• 850429-62-8 methyl 2-[[(tert-butoxy)carbonyl]amino]-1,3-thiazole-4-carboxylate 

Downstream Products

• 98020-38-3 2-Amino-4-formyl-thiazol 
• 947179-19-3 (4-Difluoromethylthiazol-2-yl)-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

4,6-Substituted-1H-Indazoles as potent IDO1/TDO dual inhibitors

Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are constitutively overexpressed in many types of cancer cells and exert important immunosuppressive functions. In this article, a series of 4,6-substituted-1H-indazole derivatives were synthesized and evaluated the inhibitory activities against IDO1 and TDO, as well as their structure-activity relationships (SARs). Among these, compound 35 displayed the most IDO1 inhibitory potency with an IC50 value of 0.74 μM in an enzymatic assay and 1.37 μM in HeLa cells. Quantitative analysis of the Western blot results indicated that 35 significantly decreased the INFγ-induced IDO1 expression in a concentration-dependent manner. In addition, 35 showed promising TDO inhibition with an IC50 value of 2.93 μM in the enzymatic assay and 7.54 μM in A172 cells. Moreover, compound 35 exhibited in vivo antitumor activity in the CT26 xenograft model. These findings suggest that 1H-indazole derivative 35 is a potent IDO1/TDO dual inhibitor, and has the potential to be developed for IDO1/TDO-related cancer treatment.

SPIROCYCLIC HAT INHIBITORS AND METHODS FOR THEIR USE

Compounds having a structure of Formula (IX) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, Q1----Q2, R6, R7, A, B, W, x, and y are as defined herein and are provided. Pharmaceutical compositions comprising such compounds and methods for treating various HAT-related conditions or diseases, including cancer, by administration of such compounds are also provided.

Novel 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis B virus infection

The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.

TRICYCLIC PIPERIDINE COMPOUNDS

The present invention relates to compounds of the formula (I), wherein R, R1a, R1b, R2, R3, and X are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), to methods for the preparation of such compounds of formula (I), and especially to their use as TPH modulators.

6-AMINO ACID HETEROARYLDIHYDROPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION

The invention provides novel compounds having the general formula:, wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.

1-[M-CARBOXAMIDO(HETERO)ARYL-METHYL]-HETEROCYCLYL-CARBOXAMIDE DERIVATIVES

The present invention relates to 1-[m-carboxamido(hetero)aryl-methyl]-heterocycyl- carboxamide compounds of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5a, R5b and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.

1-[M-CARBOXAMIDO(HETERO)ARYL-METHYL]-PIPERIDINE-4-CARBOXAMIDE DERIVATIVES

The present invention relates to 1-[m-Carboxamido(hetero)aryl-methyl]-piperidine-4-carboxamide derivatives of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5 and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.

TRICYCLIC SPIROCYCLE DERIVATIVES AND METHODS OF USE

The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or aired fasting glucose.

NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME

Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring; R4 is —(CH2)n-Z-(CH2)m—PO(OR7)(OR8), —(CH2)nZ-(CH2)m—PO(OR7)Rg, —(CH2)n-Z-(CH2)m—OPO(OR7)Rg, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10);R5 and R6 are independently selected from H, alkyl and halogen;Y is R7(CH2)s or is absent; andX, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

Naphthyridin derivatives

The present invention relates to heterocyclic derivatives of formula I wherein R1, R2 and R3 are as defined in the description and claims, which compounds are metabotropic glutamate receptor 5 antagonists.