55121-99-8

Usage

Uses

Used in Pharmaceutical Industry:
1-(4-aminobenzoyl)-4-methylpiperazine is used as a potential antipsychotic and antidepressant agent due to its ability to modulate dopamine and serotonin receptors in the brain. This makes it a candidate for the treatment of schizophrenia and depression, as demonstrated in animal models.
Used in Neuropsychiatric Disorder Treatment:
In the field of neuropsychiatry, 1-(4-aminobenzoyl)-4-methylpiperazine is used as a potential treatment for various disorders, including anxiety and bipolar disorder, due to its impact on neurotransmitter receptor modulation.
Further research is necessary to fully understand the therapeutic potential and safety of 1-(4-aminobenzoyl)-4-methylpiperazine, but its promising results in preclinical studies and animal models highlight its potential as a future drug in managing mental health conditions.

InChI:InChI=1/C12H17N3O/c1-14-6-8-15(9-7-14)12(16)10-2-4-11(13)5-3-10/h2-5H,6-9,13H2,1H3

Upstream product

• 72141-41-4 (4-nitro-phenyl)-piperazin-1-yl-methanone 
• 50-00-0 formaldehyd 
• 72141-42-5 4-aminobenzoylpiperazine 
• 350684-49-0 4-(4-aminobenzoyl)piperazine-1-carboxylic acid tert-butyl ester 
• 509073-62-5 tert-butyl 4-(4-nitrobenzoyl)piperazine- 1-carboxylate 
• 109-01-3 1-methyl-piperazine 
• 150-13-0 4-amino-benzoic acid 
• 62-23-7 4-nitro-benzoic acid 
• 367-24-8 4-bromo-2-fluoroaniline 
• 122-04-3 4-nitro-benzoyl chloride 
• 21091-98-5 (4-methylpiperazin-1-yl)(4-nitrophenyl)methanone 

Downstream Products

• 1313481-17-2 (4-(6-chloro-2-methoxyacridin-9-ylamino)phenyl)(4-methylpiperazin-1-yl)methanone 
• 1332327-18-0 1-[4-(4-methyl-piperazine-1-carbonyl)-phenyl]-3-[4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-urea 
• 1374203-74-3 1-[4(6-fluoro-4-morpholin-4-yl-7-pyridin-3-yl-quinazolin-2-yl)-phenyl]-3-[4-(4-methyl-piperazine-1-carbonyl)-phenyl]-urea 
• 1374203-75-4 4-(3-{4-[8-(3-hydroxy-phenyl)-4-morpholin-4-yl-quinazolin-2-yl]-phenyl}-ureido)-N,N-dimethyl-benzamide 
• 70261-82-4 4-[(4-methyl-1-piperazinyl)methyl]aniline 
• 79834-48-3 (4-Methyl-piperazin-1-yl)-{4-[(2-thioxo-benzooxazol-3-ylmethyl)-amino]-phenyl}-methanone 
• 79834-45-0 1-benzoyl>-4-methylpiperazine 
• 1075257-38-3 2-methyl-N₅-(4-(4-methylpiperazine-1-carbonyl)phenyl)-1-phenyl-6,7-dihydro-1H-pyrrolo[3,2-c]pyridine-3,5(4H)-dicarboxamide 

Relevant academic research and scientific papers

CYCLIN-DEPENDENT KINASE INHIBITING COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS

This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.

PYRIMIDINE COMPOUND, PREPARATION METHOD THEREOF AND MEDICAL USE THEREOF

The present invention discloses a pyrimidine compound, a preparation method thereof and a medical use thereof. Specifically, the present invention discloses a pyrimidine compound represented by formula (I), pharmaceutically acceptable salts thereof, a preparation method thereof, and a use thereof as a cyclin-dependent kinase 9 (CDK9) inhibitor, particularly for the treatment of cancer. The definition of each group in formula (I) is the same as that in the specification.

Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model

FLT3 mutation is among the most common genetic mutations in acute myeloid leukemia (AML), which is also related with poor overall survival and refractory in AML patients. Recently, FLT3 inhibitors have been approved for AML therapy. Herein, a series of new compounds with pyrazole amine scaffold was discovered, which showed potent inhibitory activity against FLT3-ITD and significant selectivity against both FLT3-ITD and AML cells expressing FLT3-ITD. Compound 46, possessing the most promising cellular activity, blocked the autophosphorylation of FLT3 pathway in MV4-11 cell line. Furthermore, the apoptosis and downregulation of P-STAT5 were also observed in tumor cells extracted from the MV4-11 cell xenografts model upon compound 46 treatment. Compound 46 was also metabolically stable in vitro and suppressed tumor growth significantly in MV4-11 xenografts model in vivo. Compound 46 showed no toxicity to the viscera of mice and caused no decrease in body weight of mice. In conclusion, the results of this study could provide valuable insights into discovery of new FLT3 inhibitors, and compound 46 was worthy of further development as potential drug candidate to treat AML.

Design and synthesis of 4-(Heterocyclic substituted amino)-1h-pyrazole-3-carboxamide derivatives and their potent activity against acute myeloid leukemia (AML)

Fms-like receptor tyrosine kinase 3 (FLT3) has been emerging as an attractive target for the treatment of acute myeloid leukemia (AML). By modifying the structure of FN-1501, a potent FLT3 inhibitor, 24 novel 1H-pyrazole-3-carboxamide derivatives were designed and synthesized. Compound 8t showed strong activity against FLT3 (IC50: 0.089 nM) and CDK2/4 (IC50: 0.719/0.770 nM), which is more efficient than FN-1501(FLT3, IC50: 2.33 nM; CDK2/4, IC50: 1.02/0.39 nM). Compound 8t also showed excellent inhibitory activity against a variety of FLT3 mutants (IC50 50: 1.22 nM). In addition, compound 8t significantly inhibited the proliferation of most human cell lines of NCI60 (GI50 1 μM for most cell lines). Taken together, these results demonstrated the potential of 8t as a novel compound for further development into a kinase inhibitor applied in cancer therapeutics.

Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors

Inhibition of LRRK2 kinase activity with small molecules has emerged as a potential novel therapeutic treatment for Parkinson's disease. Herein we disclose the discovery of a 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amine series as potent LRRK2 inhibitors id

POLYARYLENE FIBER WITH IMPROVED HYDROLYTIC STABILITY

A polyarylene fiber including 0.1-15% based on the weight of the fiber of an aromatic compound or a combination of aromatic compounds wherein each aromatic compound comprises an aromatic core and at least one of the substituents A or B, where A is represe

Chemoselective Hydrazine-mediated Transfer Hydrogenation of Nitroarenes by Co3O4 Nanoparticles Immobilized on an Al/Si-mixed Oxide Support

Cobalt oxide nanoparticles (size 2 to 3.5 nm) were successfully impregnated on an alumina–silica (mixed oxide) support through an experimentally viable and easily reproducible protocol. The prepared material was well characterized by XRD, HR-TEM, BET surface area, EDX and XPS analyses. Porous alumina–silica having a high surface area served as a protective heterogeneous support on which the well-dispersed Co3O4 nanoparticles served as an active catalytic species for the hydrazine-mediated transfer hydrogenation of nitroarenes. About 2 mol % of the active catalyst in ethanol at 60 °C was adequate for a successful conversion. Moreover, transfer hydrogenation of nitroarenes by the catalyst was found to take place chemoselectively in the presence of other labile functional groups such as halide, alkene, nitrile, carbonyl, and ester. This inexpensive catalyst was also able to catalyze the reaction on a gram scale reaction and found to be robust and recyclable up to eight runs.

INHIBITORS OF BRUTON'S TYROSINE KINASE

Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are describeded, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS

The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders.

SUBSTITUTED QUINAZOLINE AND PYRIDO-PYRIMIDINE DERIVATIVES

The present application provides novel substituted quinazoline and pyrido- pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.