630125-91-6

Usage

Uses

Used in Pharmaceutical Industry:
4-((4-Ethylpiperazin-1-yl)Methyl)-3-(trifluoroMethyl)aniline is used as a reactant in the synthesis of pyrrolo[3,2-c]pyridine derivatives, specifically in the production of an anticancer diarylurea derivative with multiple-kinase inhibitory effects. This derivative, N-[1-[4-[[[[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]phenyl]-1H-pyrrolo[3,2-c]pyridin-4-yl]benzamide (I), has potential applications in cancer treatment.
Additionally, 4-((4-Ethylpiperazin-1-yl)Methyl)-3-(trifluoroMethyl)aniline is used as an intermediate in the synthesis of N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoroMethyl)phenyl]-N''-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea (E926495), a compound that acts as an inhibitor of various kinases, including RET, FLT3, KDR, c-Abl, and c-Kit. This makes it a valuable component in the development of targeted cancer therapies.
Furthermore, 4-((4-Ethylpiperazin-1-yl)Methyl)-3-(trifluoroMethyl)aniline contributes to the prevention of human thyroid cancer cell growth, highlighting its potential role in the development of treatments for thyroid cancer.

Upstream product

• 654-70-6 4-amino-2-trifluoromethylbenzonitrile 
• 5308-25-8 4-ethylpiperazine 
• 876322-73-5 4-amino-2-(trifluoromethyl)benzaldehyde 
• 65934-74-9 3-(trifluoromethyl)-4-methylaniline 
• 630125-84-7 N-(4-bromomethyl-3-trifluoromethylphenyl)-2,2,2-trifluoroacetamide 
• 350-96-9 2,2,2-trifluoro-N-(4-methylphenyl)acetamide 
• 393-06-6 4-amino-2-(trifluoromethyl)benzoic acid 
• 1609677-80-6 (4-amino-2-trifluoromethyl-phenyl)-(4-ethyl-piperazin-1-yl)-methanone 
• 89976-12-5 1-methyl-4-nitro-2-(trifluoromethyl) benzene 
• 694499-22-4 1-(bromomethyl)-4-nitro-2-(trifluoromethyl) benzene 
• 630125-92-7 N-[4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-2,2,2-trifluoro-acetamide 
• 859027-20-6 1-ethyl-4-(4-nitro-2-(trifluoromethyl)benzyl)piperazine 

Downstream Products

• 872332-66-6 N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methyl-3-nitrobenzamide 
• 1228451-30-6 ethyl 6-(3-(3-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenyl)-1H-indazole-3-carboxylate 
• 1232836-35-9 N-[4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-3-iodo-4-methyl-benzamide 
• 853299-52-2 1-[4-(2-aminopyrimidin-4-yloxy)phenyl]-3-[4-(4-ethylpiperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]urea 
• 630124-46-8 AST-487 
• 1609678-54-7 3-bromo-N-[4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-benzenesulfonamide 
• 1609679-16-4 1-[4-(4-ethyl-piperazin-1-yl methyl)-3-trifluoromethyl-phenyl]-3-(3-ethynyl-phenyl)-urea 
• 1609678-73-0 6-iodo-2,3-dihydro-indole-1-carboxylic acid [4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethylphenyl]-amide 
• 1609679-49-3 2-[2-amino-5-(3-{3-[4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-ureido}-phenylethynyl)pyrimidin-4-yl]-1-methyl-4-oxo-1,4,6,7-tetrahydro-pyrrolo[3,2-c]pyridine-5-carboxylic acid tert-butyl ester 
• 1609677-89-5 3-bromo-N-[4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-5-fluoro-benzamide 
• 1186206-79-0 ALW-II-41-27 
• 1609678-68-3 N-{4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}-3-ethynylbenzamide 

Relevant academic research and scientific papers

6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS

The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.

A Putative Single-Photon Emission CT Imaging Tracer for Erythropoietin-Producing Hepatocellular A2 Receptor

Erythropoietin-producing hepatocellular (Eph) receptors are receptor tyrosine kinases involved in cell-cell contact. The EphA2 receptor is associated with cancer proliferation and migration. Therefore, EphA2 receptor imaging has the potential for cancer d

Discovery of potent colony-stimulating factor 1 receptor inhibitors by replacement of hinge-binder moieties

Tumor-associated macrophages (TAMs) are predominantly associated with tumor growth. Colony-stimulating factor 1 receptor (CSF1R) acts as a key regulator of TAM survival and differentiation and is a molecular target for cancer therapies. Herein, novel CSF1

Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS

Abdominal pain and abnormal bowel habits represent major symptoms for irritable bowel syndrome (IBS) patients that are not adequately managed. Although the etiology of IBS is not completely understood, many of the functions of the gastrointestinal (GI) tract are regulated by the enteric nervous system (ENS). Inflammation or stress-induced expression of growth factors or cytokines may lead to hyperinnervation of visceral afferent neurons in GI tract and contribute to the pathophysiology of IBS. Rearranged during transfection (RET) is a neuronal growth factor receptor tyrosine kinase critical for the development of the ENS as exemplified by Hirschsprung patients who carry RET loss-of-function mutations and lack normal colonic innervation leading to colonic obstruction. Similarly, RET signaling in the adult ENS maintains neuronal function by contributing to synaptic formation, signal transmission, and neuronal plasticity. Inhibition of RET in the ENS represents a novel therapeutic strategy for the normalization of neuronal function and the symptoms of IBS patients. Herein, we describe our screening effort and subsequent structure-activity relationships (SARs) in optimizing potency, selectivity, and mutagenicity of the series, which led to the discovery of a first-in-class, gut-restricted RET kinase inhibitor, 2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamide (15, GSK3179106), as a clinical candidate for the treatment of IBS. GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo.

NOVEL INHIBITORS OF MAP4K1

The invention relates to novel inhibitors of MAP4K1 (HPK1) useful for the treatment of diseases or disorders characterised by dysregulation of the signal transduction pathways associated with MAPK activation, including hyperproliferative diseases, diseases of immune system dysfunction, inflammatory disorders, neurological diseases, and cardiovascular diseases. The invention further relates to pharmaceutical compositions comprising the same and methods of treatment of said diseases and disorders. The inhibitors are of formula (I) wherein the definitions for A, D, E, F, R5, R6, R7, Z, ring Q, n, x and y are as given in the application.

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8

Using Sorafenib as a starting point, a series of potent and selective inhibitors of CDK8 was developed. When cocrystallized with CDK8 and cyclin C, these compounds exhibit a Type-II (DMG-out) binding mode.

NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS

This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.

Discovery of a Nanomolar Multikinase Inhibitor (KST016366): A New Benzothiazole Derivative with Remarkable Broad-Spectrum Antiproliferative Activity

Herein we report the discovery of compound 6 [KST016366; 4-((2-(3-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)benzo[d]thiazol-6-yl)oxy)picolinamide] as a new potent multikinase inhibitor through minor structural modification of our

ISOQUINOLINE-5-CARBOXAMIDE DERIVATIVE HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASE

A compound selected from the group consisting of an isoquinoline-5-carboxamide derivative of formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate and a solvate thereof is effective for the prevention or treatment of diseases associated with abnormal cell growth, which are caused by abnormal activation of a protein kinases.

ISOQUINOLINE-5-CARBOXAMIDE DERIVATIVE HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASE

A compound selected from the group consisting of an isoquinoline-5-carboxamide derivative of formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate and a solvate thereof is effective for the prevention or treatment of diseases associated with abnormal cell growth, which are caused by abnormal activation of a protein kinases.