189442-87-3

Usage

Uses

Used in Pharmaceutical Industry:
Ethyl N-Boc-4-methylpiperidine-4-carboxylate is used as a reactant for the synthesis of Dipeptidyl peptidase-4 (DPP-4) inhibitors, such as ABT-279. These inhibitors play a crucial role in the treatment of type 2 diabetes by regulating glucose levels in the body. The compound's unique structure allows for the development of potent and selective DPP-4 inhibitors, which can help improve the management of diabetes and its associated complications.
Used in Medicinal Chemistry:
Ethyl N-Boc-4-methylpiperidine-4-carboxylate is used as a building block for the synthesis of piperazine-based CCR5 antagonists. These antagonists are important in the field of medicinal chemistry, as they have the potential to modulate the immune system and exhibit anti-inflammatory, anti-allergic, and anti-cancer properties. The compound's structural diversity and reactivity make it an ideal candidate for the development of novel piperazine-based CCR5 antagonists with improved pharmacological profiles.

InChI:InChI=1/C14H25NO4/c1-6-18-11(16)14(5)7-9-15(10-8-14)12(17)19-13(2,3)4/h6-10H2,1-5H3

Upstream product

• 1126-09-6 4-carbethoxypiperidine 
• 74-88-4 methyl iodide 
• 24424-99-5 di-tert-butyl dicarbonate 
• 84358-13-4 N-[(tert-butoxy)carbonyl]piperidine-4-carboxylic acid 
• 498-94-2 isonipecotic acid 
• 142851-03-4 1-tert-butyl 4-ethyl piperidine-1,4-dicarboxylate 

Downstream Products

• 225240-71-1 ethyl 4-methylpiperidine-4-carboxylate monohydrochloride 
• 236406-21-6 4-(hydroxymethyl)-4-methylpiperidine-1-carboxylic acid tert-butyl ester 
• 189321-63-9 1-(tert-butoxycarbonyl)-4-methylpiperidine-4-carboxylic acid 
• 1403232-16-5 1-{4-[5-(3-chloro-4-isobutylphenyl)-[1,2,4]-oxadiazol-3-yl]benzyl}-4-methylpiperidine-4-carboxylic acid 
• 1403232-18-7 1-{4-[5-(3-chloro-4-isobutylphenyl)-[1,2,4]-oxadiazol-3-yl]benzyl}-4-methylpiperidine-4-carboxylic acid, sodium salt 
• 1403234-00-3 4-methyl-1-{4-[5-(3-chloro-4-cyclohexylphenyl)-[1,2,4]-oxadiazol-3-yl]benzyl}piperidine-4-carboxylic acid ethyl ester 
• 1403232-15-4 1-{4-[5-(3-chloro-4-cyclohexylphenyl)-[1,2,4]-oxadiazol-3-yl]benzyl}-4-methylpiperidine-4-carboxylic acid 
• 1403234-03-6 1-{4-[5-(3-chloro-4-isobutylphenyl)-[1,2,4]-oxadiazol-3-yl]-benzyl}-4-methylpiperidine-4-carboxylic acid ethyl ester 
• 1403232-17-6 1-{4-[5-(3-chloro-4-isobutylphenyl)-[1,2,4]-oxadiazol-3-yl]benzyl}-4-methylpiperidine-4-carboxylic acid tert-butyl amine salt 
• 297172-16-8 (4-methylpiperidin-4-yl)methanol 
• 878167-05-6 ethyl 4-formyl-4-methylpiperidine-1-carboxylate 
• 236406-22-7 tert-butyl 4-(aminomethyl)-4-methylpiperidine-1-carboxylate 
• 236406-15-8 (4-methyl-piperidin-4-yl)-carbamic acid benzyl ester 
• 1067914-49-1 benzyl 1-(2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinolin-8-yl)-4-methylpiperidin-4-ylcarbamate 

Relevant academic research and scientific papers

Synthesis and biological activity of conformationally restricted indole-based inhibitors of neurotropic alphavirus replication: Generation of a three-dimensional pharmacophore

We have previously reported the development of indole-based CNS-active antivirals for the treatment of neurotropic alphavirus infection, but further optimization is impeded by a lack of knowledge of the molecular target and binding site. Herein we describe the design, synthesis and evaluation of a series of conformationally restricted analogues with the dual objectives of improving potency/selectivity and identifying the most bioactive conformation. Although this campaign was only modestly successful at improving potency, the sharply defined SAR of the rigid analogs enabled the definition of a three-dimensional pharmacophore, which we believe will be of value in further analog design and virtual screening for alternative antiviral leads.

KINASE ANTAGONISTS AND METHODS FOR MAKING AND USING THEM

Disclosed herein are small molecule compounds that are SGK1 antagonists, formulations and pharmaceutical compositions comprising the compounds, and methods of making and using them, for treating, ameliorating, preventing, reversing or slowing the progression of: a cancer, a tumor, a metastasis or a dysplastic or a dysfunctional cell condition responsive to inhibition of a kinase enzyme of the AGC group of kinases including SGK1, by administration of an AGC kinase inhibitor or antagonist.

CASPASE INHIBITOR AND PHARMACEUTICAL COMPOSITION, USE AND THERAPEUTIC METHOD THEREOF

Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.

Novel heterocyclic derivative capable of being used as SHP2 inhibitor

The invention relates to a novel heterocyclic derivative capable of being used as an SHP2 inhibitor, specifically relates to a compound shown by a formula I or pharmaceutically acceptable salts thereof, further relates to a use of the compound shown by the formula I or the pharmaceutically acceptable salts thereof and a pharmaceutical composition thereof in drug preparation, and particularly relates to a use in preparation of drugs for treatment, inhibition or prevention of diseases or discomforts mediated by SHP2 activity.

NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS

This invention relates to certain novel pyrazine derivatives (Formula I) as SHP2 inhibitors which is shown as formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention is directed to fused heterocyclic group derivatives useful as inhibitors of SHP2, methods for producing such compounds and methods for treating a SHP2-mediated disorder.

Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels

Transient receptor potential canonical 3/6/7 (TRPC3/6/7) are highly homologous receptor-operated nonselective cation channels. Despite their physiological significance, very few selective and potent agonists are available for functional examination of these channels. Using a cell-based high throughput screening approach, a lead compound with the pyrazolopyrimidine skeleton was identified as a TRPC6 agonist. Synthetic schemes for the lead and its analogues were established, and structural-activity relationship studies were carried out. A series of potent and direct agonists of TRPC3/6/7 channels were identified, and among them, 4m-4p have a potency order of TRPC3 > C7 > C6, with 4n being the most potent with an EC50 of 20 nM on TRPC3. Importantly, these compounds exhibited no stimulatory activity on related TRP channels. The potent and selective compounds described here should be suitable for evaluation of the roles of TRPC channels in the physiology and pathogenesis of diseases, including glomerulosclerosis and cancer.

FUSED TRICYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY

A series of substituted fused tricyclic imidazole derivatives, in particular dihydro- 1H-pyrano[4',3':4,5]imidazo[1,2-a]pyridine, 1,2,3,4-tetrahydroimidazo[1,2-a:5,4- c']dipyridine, dihydro-1H-pyrano[3',4':4,5]imidazo[1,2-a]pyridine and tetrahydro-6H- cyc

FUSED TRICYCLIC BENZIMIDAZOLES DERIVATIVES AS MODULATORS OF TNF ACTIVITY

A series of tricyclic benzimidazole derivatives, in particular dihydro-1H- imidazo [1,2-a]benzimidazo le, dihydro-1H-pyrrolo [1,2-a]benzimidazo le, dihydro-1H- pyrazino[1,2-a]benzimidazole, dihydro-1H-[1,4]oxazino[4,3-a]benzimidazole and dihydrothiazolo[3,4-a]benzimidazolem, and analogues thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

TNF -Alpha Modulating Benzimidazoles

A series of benzimidazole derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Synthesis and SAR of Imidazo[1,5-a[pyridine derivatives as 5-HT4 receptor partial agonists for the treatment of cognitive disorders associated with Alzheimer's disease

Alzheimer's disease (AD) is a neurodegenerative disease which has a higher prevalence and incidence in older people. The need for improved AD therapies is unmet. The 5-hydroxytryptamine4 receptor (5-HT4R) partial agonists may be of benefit for both the symptomatic and disease-modifying treatment of cognitive disorders associated with AD. Herein, we report the design, synthesis and SAR of imidazo[1,5-a] pyridine derivatives as 5-HT4R partial agonists. The focused SAR, optimization of ADME properties resulted the discovery of compound 5a as potent, selective, brain penetrant 5-HT4 partial agonist as a lead compound with good ADME properties and efficacy in both symptomatic and disease modifying animal models of cognition.