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The present invention relates to piperidine sulphonamide derivatives of formulawherein Ar1, Ar2, R1, R2, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9258N – PubChem

 

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Chemistry is traditionally divided into organic and inorganic chemistry. Formula: C11H15N. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent,Which mentioned a new discovery about 3466-80-6

The thermolysis of 1-methyl-2-vinylpiperidine N-oxide (13) resulted in Meisenheimer <1,2> rearrangement to give the hexahydro-1,2-oxazepine (23) and no <2,3>-sigmatropic rearrangement product (24).Similarly, the 1-methyl-1,2,5,6-tetrahydropyridine N-oxides (15), on heating, gave only the tetrahydro-1,2-oxazepines (26,27), together with the Hofmann type elimination products (28).The thermolysis of 1-benzyl-2-phenyl-(20a) and 1-benzyl-2-vinyl-piperidine N-oxide (20b) afforded the corresponding 1-benzyloxypiperidines (32) as well as the 1,2-oxazepines (31).These results are different from those observed for open-chain allylamine N-oxides and 1-alkyl-2-vinylpiperidine N-imides and N-ylides, which are known to undergo only <2,3>-sigmatropic rearrangement. Keywords – thermolysis; ring expansion; rearrangement; Meisenheimer rearrangement; 1-alkylpiperidine N-oxide; 1-alkyltetrahydropyridine N-oxide; 1,2-oxazepine

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9252N – PubChem

 

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(Equation presented) Cyclic amines may be prepared via a sequence of deprotection followed by intramolecular reductive amination of t-Boc-protected amino ketones under asymmetric transfer hydrogenation conditions. In cases where the corresponding imine reaction proceeds with high enantioselectivity, this is reflected in the one-step process.

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Piperidine – Wikipedia,
Piperidine | C5H9335N – PubChem

 

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Lead optimization of piperidine amide HTS hits, based on an anilino-thiazole core, led to the identification of analogs which displayed low nanomolar blocking activity at the canonical transient receptor channels 3 and 6 (TRPC3 & 6) based on FLIPR (carbachol stimulated) and electrophysiology (OAG stimulated) assays. In addition, the anilino-thiazole amides displayed good selectivity over other TRP channels (TRPA1, TRPV1, and TRPV4), as well as against cardiac ion channels (CaV1.2, hERG, and NaV1.5). The high oxidation potential of the aliphatic piperidine and aniline groups, as well as the lability of the thiazole amide group contributed to the high clearance observed for this class of compounds. Conversion of an isoquinoline amide to a naphthyridine amide markedly reduced clearance for the bicyclic piperidines, and improved oral bioavailability for this compound series, however TRPC3 and TRPC6 blocking activity was reduced substantially. Although the most potent anilino-thiazole amides ultimately lacked oral exposure in rodents and were not suitable for chronic dosing, analogs such as 14-19, 22, and 23 are potentially valuable in vitro tool compounds for investigating the role of TRPC3 and TRPC6 in cardiovascular disease.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9294N – PubChem

 

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RIP1 kinase regulates necroptosis and inflammation and may play an important role in contributing to a variety of human pathologies, including inflammatory and neurological diseases. Currently, RIP1 kinase inhibitors have advanced into early clinical trials for evaluation in inflammatory diseases such as psoriasis, rheumatoid arthritis, and ulcerative colitis and neurological diseases such as amyotrophic lateral sclerosis and Alzheimer’s disease. In this paper, we report on the design of potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitors starting from a high-throughput screen and the lead-optimization of this series from a lead with minimal rat oral exposure to the identification of dihydropyrazole 77 with good pharmacokinetic profiles in multiple species. Additionally, we identified a potent murine RIP1 kinase inhibitor 76 as a valuable in vivo tool molecule suitable for evaluating the role of RIP1 kinase in chronic models of disease. DHP 76 showed efficacy in mouse models of both multiple sclerosis and human retinitis pigmentosa.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9279N – PubChem

 

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 3466-80-6, molcular formula is C11H15N, introducing its new discovery. Safety of 2-Phenylpiperidine

(Chemical Equation Presented) The facile double reduction of bicyclic aromatic sulfonamides was used to synthesize a variety of 2- and 3-aryl-substituted pyrrolidines and 2-phenylpiperidine. The method features a combined nitrogen protection and a traceless tether for the transposition of the aromatic moiety from nitrogen to carbon.

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Piperidine – Wikipedia,
Piperidine | C5H9336N – PubChem

 

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Herein we describe the continued optimization of M4 positive allosteric modulators (PAMs) within the 5-amino-thieno[2,3-c]pyridazine series of compounds. In this letter, we disclose our studies on tertiary amides derived from substituted azetidines. This series provided excellent CNS penetration, which had been challenging to consistently achieve in other amide series. Efforts to mitigate high clearance, aided by metabolic softspot analysis, were unsuccessful and precluded this series from further consideration as a preclinical candidate. In the course of this study, we found that potassium tetrafluoroborate salts could be engaged in a tosyl hydrazone reductive cross coupling reaction, a previously unreported transformation, which expands the synthetic utility of the methodology.

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Piperidine – Wikipedia,
Piperidine | C5H9299N – PubChem

 

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Several 5-HT(ID/1B) receptor agonists are now entering the marketplace as treatments for migraine. This paper describes the development of selective h5-HT(1D)receptor agonists as potential antimigraine agents which may produce fewer side effects. A series of 3-[3-(piperidin-1-yl)propyl]indoles has been synthesized which has led to the identification of 80 (L-772,405), a high- affinity h5-HT(1D) receptor full agonist having 170-fold selectivity for h5- HT(1D) receptors over h5-HT(1B) receptors. L-772,405 also shows very good selectivity over a range of other serotonin and nonserotonin receptors and has excellent bioavailability following subcutaneous administration in rats. It therefore constitutes a valuable tool to delineate the role of h5-HT(1D) receptors in migraine. Molecular modeling and physical properties have been utilized to postulate the binding conformation of these compounds in the receptor cavity.

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Piperidine – Wikipedia,
Piperidine | C5H9277N – PubChem

 

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The regioselective formation of carbon-carbon or carbon-heteroatom bonds through direct functionalisation has been widely studied in the last decade. Recently, many investigations have been focused on the use of Ru(II) complexes. Herein, the latest advances in Ru(II) catalysis for ortho-functionalisation promoted by a directing group as well as new achievements in meta-functionalisation will be discussed.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9253N – PubChem

 

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 3466-80-6, molcular formula is C11H15N, introducing its new discovery. SDS of cas: 3466-80-6

Ortho-lithiation of N,N-dimethylbenzylamine and reaction with trimethylborate gave the corresponding boronic acid in good yields.The reaction was extended to the synthesis of various aromatic boron compounds with nitrogen-containing substituents in the ortho-position, including a chiral boroxin prepared from (S)-N,N-dimethyl-1-phenylethylamine.From N-Methyl-benzylamine a stable boronium salt was obtained under certain conditions.The spectra of the newly synthesized compounds are discussed.Intramolecular B-N interaction is established by 11B NMR spectroscopy.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9286N – PubChem