6517-69-7

Usage

Uses

Used in Pharmaceutical Development:
alpha-[1-(phenylmethyl)piperidin-4-ylidene]phenylacetonitrile is used as a potential ligand or inhibitor in drug development, particularly targeting the central nervous system. Its unique structure allows for the exploration of its interactions with neurotransmitter receptors or enzymes, which could lead to the creation of new therapeutic agents.
Used in Research and Development:
In the scientific community, alpha-[1-(phenylmethyl)piperidin-4-ylidene]phenylacetonitrile serves as a subject of study for understanding its pharmacological properties and potential applications. Researchers are interested in its effects on the central nervous system and how it may be utilized in the development of medications for various neurological conditions.
Used in Drug Discovery for Neurological Conditions:
Given its potential impact on the central nervous system, alpha-[1-(phenylmethyl)piperidin-4-ylidene]phenylacetonitrile is used as a starting point for the discovery of new drugs to treat neurological disorders. Its interaction with neurotransmitter systems could provide insights into the development of treatments for conditions such as Parkinson's disease, Alzheimer's disease, or other cognitive disorders.

Upstream product

• 3612-20-2 1-phenylmethyl-4-piperidone 
• 140-29-4 phenylacetonitrile 

Downstream Products

• 79139-64-3 (1-benzyl-4-phenylacetonitrile-piperidyl-4)nitromethane 
• 7254-21-9 N-benzyl-2-phenyl-2-(piperidin-4-yl)acetonitrile 

Relevant academic research and scientific papers

Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein-Protein Interaction

Inhibition of the menin-mixed lineage leukemia (MLL) protein-protein interaction is a promising new therapeutic strategy for the treatment of acute leukemia carrying MLL fusion (MLL leukemia). We describe herein our structure-based design, synthesis, and evaluation of a new class of small-molecule inhibitors of the menin-MLL interaction (hereafter called menin inhibitors). Our efforts have resulted in the discovery of highly potent menin inhibitors, as exemplified by compound 42 (M-89). M-89 binds to menin with a Kd value of 1.4 nM and effectively engages cellular menin protein at low nanomolar concentrations. M-89 inhibits cell growth in the MV4;11 and MOLM-13 leukemia cell lines carrying MLL fusion with IC50 values of 25 and 55 nM, respectively, and demonstrates >100-fold selectivity over the HL-60 leukemia cell line lacking MLL fusion. The determination of a co-crystal structure of M-89 in a complex with menin provides the structural basis for their high-affinity interaction. Further optimization of M-89 may lead to a new class of therapy for the treatment of MLL leukemia.

PIPERIDINES AS MENIN INHIBITORS

The present disclosure provides compounds represented by Formula (I): (Formula(I)) and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R2, R3a, R3b, A, G, X, and Y are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat a condition or disorder responsive to menin inhibition such as cancer.

Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists

The synthesis and evaluation of benzetimide derivatives showing potent CXCR3 antagonism are described. Optimization of the screening hits led to the identification of more potent CXCR3 antagonists devoid of anti-cholinergic activity and identification of the key pharmacophore moieties of the series.

Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor

The invention relates to compounds of the formula wherein R1 is hydrogen, lower alkyl, lower alkenyl, phenyl or the following groups —(CH2)m-non aromatic heterocyclyl, which is optionally substituted by lower alkyl, or is —(CH2)m-heteroaryl, which is optionally substituted by one or two substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, CF3, benzyl or cyano, or is —(CH2)m—C(O)—NRR′, —(CH2)m—C(O)-lower alkyl, —(CH2)m—C(O)—O-lower alkyl, —(CH2)m—O-lower alkyl, —(CH2)m—CH[C(O)—O-lower alkyl]2, —(CH2)mCH(OH)—CH2—O-phenyl, —(CH2)m—CH(CF3)OH, —(CH2)m—OH, —(CH2)m—CN, —(CH2)m—NRR′, —(CH2)m-cycloalkyl or —(CH2)m—CHF2; R2 is hydrogen, lower alkyl, halogen or lower alkoxy; R3 is lower alkyl, lower alkoxy, halogen or CF3; R,R′ are the same or different and are hydrogen or lower alkyl; X is >N—, >C═ or >CH—; X1/X2 are independently from each other hydrogen, hydroxy or lower alkoxy or may be together an oxo group; Y1/Y2 are independently from each other hydrogen, lower alkyl, —CH2)m-phenyl or may be together an oxo group; Z is a bond, —CH2— or —C(O)—; m is 0, 1,2, 3 or 4; n is 2 or 3; n′ 0, 1 or 2; and pharmaceutically acceptable acid addition salts thereof. The described compounds have a good affinity to the NK1 receptor.

THE SYNTHESIS OF 1-PHENYL-3,8-DIAZASPIRODECANES

The synthesis of some substituted 3,8-diazaspirodecanes is described.Two routes starting from 1-benzyl-4-oxo-piperidine have been explored.The title compounds are isosteric to the 1,3,8-triazaspirodecane structure present in important neuroleptic agents.