55661-33-1

Usage

Chemical Properties

Off-white to cream color solid

Uses

(2-Thiazolyl)methylamine is a useful compound in the preparation of cephalosporins

InChI:InChI=1/C4H6N2S.2ClH/c5-3-4-6-1-2-7-4;;/h1-2H,3,5H2;2*1H

Upstream product

• 107-20-0 2-chloroethanal 
• 55443-42-0 N-(2-amino-2-thioxoethyl)benzamide 
• 17356-08-0 thiourea 
• 78-95-5 chloroacetone 
• 103863-35-0 N-thiazol-2-ylmethyl-phthalimide 
• 171268-82-9 thiazol-2-yl-methylazide 
• 7732-18-5 water 
• 10200-59-6 Thiazole-2-carbaldehyde 
• 13838-77-2 1,3-thiazole-2-carbaldehyde oxime 

Downstream Products

• 1596-65-2 2-amino-3-(2-thiazolyl)propanoic acid 
• 530090-23-4 (Z)-2-{1-[2-chloro-4-(3-methyl-1H-pyrazol-1-yl)benzoyl]-4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene}-N-(thiazol-2-ylmethyl)acetamide 
• 1191942-78-5 3,5-di-tert-butyl-4-hydroxy-N-(1-(thiazol-2-ylmethylcarbamoyl)cyclopropyl)benzamide 
• 1202927-41-0 2-(2-oxo-3-(4-(trifluoromethyl)benzyl)imidazolidin-1-yl)-N-(thiazol-2-ylmethyl)isonicotinamide 
• 1417790-13-6 C₂₁H₁₉F₃N₆O₂S 
• 185747-16-4 (thiazol-2-yl)methylcarbamic acid t-butyl ester 
• 1072804-38-6 2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(thiazol-2-ylmethyl)thiazole-5-carboxamide 
• 1123819-38-4 C₂₆H₁₇F₃N₄O₂S 
• 1123819-30-6 C₂₅H₁₇F₃N₄O₂S 
• 1123819-11-3 C₂₄H₁₇ClN₄O₂S 
• 1123818-90-5 C₂₄H₁₈N₄O₂S 
• 1219623-44-5 2-(2-oxo-3,3-diphenylpyrrolidin-1-yl)-N-(1,3-thiazol-2-ylmethyl)acetamide 
• 1018480-47-1 C₁₆H₁₃F₃N₄O₂S₂ 

Relevant academic research and scientific papers

Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model

Colony-stimulating factor-1 receptor (CSF1R) is implicated in tumor-associated macrophage (TAM) repolarization and has emerged as a promising target for cancer immunotherapy. Herein, we describe the discovery of orally active and selective CSF1R inhibitors by property-driven optimization of BPR1K871 (9), our clinical multitargeting kinase inhibitor. Molecular docking revealed an additional nonclassical hydrogen-bonding (NCHB) interaction between the unique 7-aminoquinazoline scaffold and the CSF1R hinge region, contributing to CSF1R potency enhancement. Structural studies of CSF1R and Aurora kinase B (AURB) demonstrated the differences in their back pockets, which inspired the use of a chain extension strategy to diminish the AURA/B activities. A lead compound BPR1R024 (12) exhibited potent CSF1R activity (IC50 = 0.53 nM) and specifically inhibited protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth. In vivo, oral administration of 12 mesylate delayed the MC38 murine colon tumor growth and reversed the immunosuppressive tumor microenvironment with the increased M1/M2 ratio.

Development of Glucose Regulated Protein 94-Selective Inhibitors Based on the BnIm and Radamide Scaffold

Glucose regulated protein 94 (Grp94) is the endoplasmic reticulum resident of the heat shock protein 90 kDa (Hsp90) family of molecular chaperones. Grp94 associates with many proteins involved in cell adhesion and signaling, including integrins, Toll-like receptors, immunoglobulins, and mutant myocilin. Grp94 has been implicated as a target for several therapeutic areas including glaucoma, cancer metastasis, and multiple myeloma. While 85% identical to other Hsp90 isoforms, the N-terminal ATP-binding site of Grp94 possesses a unique hydrophobic pocket that was used to design isoform-selective inhibitors. Incorporation of a cis-amide bioisostere into the radamide scaffold led to development of the original Grp94-selective inhibitor, BnIm. Structure-activity relationship studies have now been performed on the aryl side chain of BnIm, which resulted in improved analogues that exhibit better potency and selectivity for Grp94. These analogues also manifest superior antimigratory activity in a metastasis model as well as enhanced mutant myocilin degradation in a glaucoma model compared to BnIm.

COMPOUNDS FOR THE TREATMENT OF ABNORMAL CELL GROWTH

The invention relates to compounds of the formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R4, R5, n, A and B are as defined herein. The inventi

THIADIAZOLEDIOXIDES AND THIADIAZOLEOXIDES AS CXC- AND CC-CHEMOKINE RECEPTOR LIGANDS

Disclosed are novel compounds of the formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula (IA).

3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands

There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.

3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands

There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.

Thiazole benzamide derivatives and pharmaceutical compositions for inhibiting cell proliferation, and methods for their use

Aminothiazole compounds with mono-/di-substituted benzamide are represented by the Formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, pharmaceutically active metabolites, and pharmaceutically acceptable salts of said metabolites are described. These agents modulate and/or inhibit the cell proliferation and activity of protein kinases and are useful as pharmaceuticals for treating malignancies and other disorders.

Hypocholesterolemic agents

This invention relates to certain steroidal glycosides useful as hypocholesterolemic agents and antiatherosclerosis agents and certain protected intermediates useful in the preparation of said steroidal glycosides.

Steroidal glycosides

This invention relates to certain steroidal glycosides of Formula I STR1 wherein the values for the variables are described herein, which are useful as hypocholesterolemic agents and antiatherosclerosis agents and certain protected intermediates useful in the preparation of said steroidal glycosides.

Alkylation of camphor and pinanone imines of 2-(aminomethyl)thiazole. Enantioselective synthesis of 2-(1-aminoalkyl)thiazoles

A method is described for the enantioselective synthesis of 2-(1-aminoalkyl)thiazoles 6 via stereoselective alkylation of the carbanions of (+)-(R)-camphor and (-)-(1S, 2S, 5S)-2-hydroxypinan-3-one imines 2 and 3 derived from 2-(aminomethyl)thiazole (2-AMT, 1). Compounds 6 serve as α-amino aldehyde precursors via thiazolyl-to-formyl conversion.