679409-18-8

Usage

Uses

Used in Pharmaceutical Industry:
1-BOC-4-(3-FLUORO-PHENYLAMINO)-PIPERIDINE is used as a synthetic intermediate for the development of new pharmaceuticals, leveraging its enhanced bioactivity due to the presence of fluorine. 1-BOC-4-(3-FLUORO-PHENYLAMINO)-PIPERIDINE's structure allows for its integration into drug molecules to improve their efficacy and pharmacokinetic properties.
Used in Scientific Research:
In the realm of scientific research, 1-BOC-4-(3-FLUORO-PHENYLAMINO)-PIPERIDINE serves as a key compound in studying the effects of structural modifications on biological activity. Researchers use 1-BOC-4-(3-FLUORO-PHENYLAMINO)-PIPERIDINE to explore the influence of fluorination and amine protection on the interactions of molecules with biological targets, contributing to the advancement of medicinal chemistry.
Used in Medicinal Chemistry:
1-BOC-4-(3-FLUORO-PHENYLAMINO)-PIPERIDINE is utilized as a building block in the synthesis of various drug candidates. Its unique structural features make it a valuable component in the creation of molecules with potential therapeutic applications, particularly in the areas of central nervous system disorders, cardiovascular diseases, and other conditions where piperidine-based compounds have shown promise.
Used in Drug Synthesis Process:
The BOC-protected amine group in 1-BOC-4-(3-FLUORO-PHENYLAMINO)-PIPERIDINE is used to facilitate the synthesis of complex drug molecules. The BOC group protects the amine during the initial stages of synthesis, preventing unwanted side reactions, and is later removed to reveal the free amine group, enabling further functionalization and the formation of the final drug product.

Upstream product

• 372-19-0 meta-fluoroaniline 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 

Downstream Products

• 1161086-48-1 1,1-dimethylethyl 4-((3-fluorophenyl){[(4-fluorophenyl)amino]carbonyl}amino)-1-piperidinecarboxylate 
• 1150103-06-2 1,1-dimethylethyl 4-[{[(6-cyano-3-pyridinyl)amino]carbonyl}(3-fluorophenyl)amino]-1-piperidinecarboxylate 
• 1150100-35-8 1,1-dimethylethyl 4-[[({2,4-difluoro-5-[(methyloxy)carbonyl]phenyl}amino)carbonyl](3-fluorophenyl)amino]-1-piperidinecarboxylate 
• 1344734-71-9 C₂₃H₂₅F₂N₅O₃ 
• 1344734-65-1 C₂₃H₂₈BrFN₄O₃ 
• 1344734-62-8 C₂₄H₂₈FN₅O₃ 
• 1344734-75-3 C₃₂H₃₃F₂N₇O₅S 
• 1344734-74-2 C₃₃H₃₆FN₇O₅S 
• 1344734-73-1 C₃₃H₃₆FN₇O₅S 

Relevant academic research and scientific papers

Synthesis and antimalarial activity of 1,4-disubstituted piperidine derivatives

In order to prepare, at low cost, new compounds active against Plasmodium falciparum, and with a less side-effects, we have designed and synthesized a library of 1,4-disubstituted piperidine derivatives from 4-aminopiperidine derivatives 6. The resulting compound library has been evaluated against chloroquine-sensitive (3D7) and chloroquine-resistant (W2) strains of P. falciparum. The most active molecules—compounds 12d (13.64 nM (3D7)), 13b (4.19 nM (3D7) and 13.30 nM (W2)), and 12a (11.6 nM (W2))—were comparable to chloroquine (22.38 nM (3D7) and 134.12 nM (W2)).

NITROGENOUS HETEROCYCLIC DERIVATIVES AND THEIR APPLICATION IN DRUGS

The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, IPF, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.

Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats

A novel series of pyridyl carboxamide-based CCR5 inhibitors was designed, synthesized, and demonstrated to be highly potent against HIV-1 infection in both HOS and PBL assays. Attempts to evaluate this series of compounds in a rat PK model revealed its instability in rat plasma. A hypothesis for this liability was proposed, and strategies to overcome this issue were pursued, leading to discovery of highly potent 40 and 41, which featured dramatically improved rat PK profiles. 2011 Elsevier Ltd. All rights reserved.

Discovery of N-benzyl-N′-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): Modification of the acyl portion

Modification of the acyl moiety in the CCR5 lead molecule 2 led to identification of several new classes of CCR5 antagonists. Antiviral activity and pharmacokinetic properties of the synthesized compounds were evaluated. Structure-activity relationship (S

CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS

The present invention relates to compounds useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acq

CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS

The present invention relates to compounds useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acq

CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS

The present invention relates to compounds useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).

CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS

The present invention relates to compounds useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).

Discovery of N-(3-fluorophenyl)-1-[(4-([(35)-3-methyl-1-piperazinyl]methyl) phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate

N-(3-Fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl) acetyl]-4-piperidinamine 12 (GSK962040) is a novel small molecule motilin receptor agonist. It possesses excellent activity at the recombinant human motilin receptor and also at the native rabbit motilin receptor where its agonist activity results in potentiation of the amplitude of neuronal-mediated contractions of isolated gastric antrum tissue. Compound 12 also possesses highly promising pharmacokinetic profiles in both rat and dog, and these results, in combination with further profiling in human native tissue and an in vivo model of gastrointestinal transit in the rabbit, have led to its selection as a candidate for further development.

The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor

Optimisation of urea (5), identified from high throughput screening and subsequent array chemistry, has resulted in the identification of pyridine carboxamide (33) which is a potent motilin receptor agonist possessing favourable physicochemical and ADME profiles. Compound (33) has demonstrated prokinetic-like activity both in vitro and in vivo in the rabbit and therefore represents a promising novel small molecule motilin receptor agonist for further evaluation as a gastroprokinetic agent.