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Reactions of available diethyl 1-acylamino-2,2-dichloroethenylphosphonates with amino acids esters were studied, which in the case of esters of proline, nipecotic and isonipecotic acids resulted in N-substituted derivatives of 5-amino-4-diethoxyphosphoryloxazol in high yields. Their behavior in the acidic and alkaline media was investigated by the example of methyl N-(4-diethoxyphosphoryl-2-R-oxazol-5-yl)isonipecotinate.

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Piperidine – Wikipedia,
Piperidine | C5H8034N – PubChem

 

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Compounds of formula (I) wherein A, W, R3b, Z and p have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer’s disease.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H8107N – PubChem

 

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Inhibitors of the aldo-keto reductase enzyme AKR1C3 are of interest as potential drugs for leukemia and hormone-related cancers A series of non-carboxylate morpholino(phenylpiperazin-1-yl)methanones were prepared by palladium-catalysed coupling of substituted phenyl or pyridyl bromides with the known morpholino(piperazin-1-yl)methanone, and shown to be potent (IC 50 ? 100 nM) and very isoform-selective inhibitors of AKR1C3 Lipophilic electron-withdrawing substituents on the phenyl ring were positive for activity, as was an H-bond acceptor on the other terminal ring, and the ketone moiety (as a urea) was essential These structure-activity relationships are consistent with an X-ray structure of a representative compound bound in the AKR1C3 active site, which showed H-bonding between the carbonyl oxygen of the drug and Tyr55 and His117 in the ‘oxyanion hole’ of the enzyme, with the piperazine bridging unit providing the correct twist to allow the terminal benzene ring to occupy the lipophilic pocket and align with Phe311

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H8061N – PubChem

 

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SUBSTITUTED AMIDE COMPOUNDS

Substituted amide compounds corresponding to formula I:processes for preparing them, pharmaceutical compositions containing these compounds, and the use of substituted amide derivatives for the preparation of medicaments for the treatment of pain and various other conditions.

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Piperidine – Wikipedia,
Piperidine | C5H8024N – PubChem

 

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SULFONAMIDES AS INHIBITORS OF THE UPTAKE OF EXTRACELLULAR CITRATE

Sulfonamides of formula (I), wherein A, R1, and R2 are as defined in the specification and the claims, can be used as medicaments for the treatment of metabolic and/or cardiovascular diseases.

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Piperidine – Wikipedia,
Piperidine | C5H8021N – PubChem

 

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SULFONAMIDES AS INHIBITORS OF THE UPTAKE OF EXTRACELLULAR CITRATE

Sulfonamides of formula (I), wherein A, R1, and R2 are as defined in the specification and the claims, can be used as medicaments for the treatment of metabolic and/or cardiovascular diseases.

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Piperidine – Wikipedia,
Piperidine | C5H8021N – PubChem

 

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Design and synthesis of a novel series of histamine H3 receptor antagonists through a scaffold hopping strategy

Lead compounds 5-fluoro-2-methyl-N-[2-methyl-4-(2-methyl-[1,3?]bipyrrolidinyl-1?-yl)-phenyl]-benzamide (1), tetrahydro-pyran-4-carboxylic acid [((2S,3?S)-2-methyl-[1,3?]bipyrrolidinyl-1?-yl)-phenyl]-amide (2), and 3,5-dimethyl-isoxazole-4-carboxylic acid [((2S,3?S)-2-methyl-[1,3?]bipyrrolidinyl-1?-yl)-phenyl]-amide (3) discovered in our laboratory, displayed high histamine H3 receptor (H3R) affinity, good selectivity and weak human Ether–go-go-Related Gene (hERG) channel affinity with desirable overall physico-chemical and pharmacokinetic (PK) profiles. Herein, we describe the design and synthesis of a novel series of H3R antagonists utilizing a scaffold hopping strategy. Further structure-activity relationship (SAR) studies of the series culminated in the identification of ((2S,3?S)-2-methyl-[1,3?]bipyrrolidinyl-1?-yl)-naphthalene-2-carboxylic acid (tetrahydro-pyran-4-yl)-amide (4c) and -[4-((2S,3?S)-2-methyl-[1,3?]bipyrrolidinyl-1?-yl)-phenyl]-N-(tetrahydro-pyran-4-yl)-acetamide (4d), which exhibited good H3R affinity in vitro, good selectivity, and desirable PK properties. Compounds 4c and 4d were also assessed in cardiac safety experiments. In particular, the effects of the compounds on action potentials recorded from ventricular myocytes isolated from guinea pigs were used to screen compounds that not only displayed a low affinity towards hERG channel, but also had lower interference with other cardiac ion channels. Compound 4c did not alter the major parameters in this model system at ?10 muM, and no significant induction of any major haemodynamic effect when intravenously administered at 3 mg/kg dose to anaesthetized mongrel dogs. Compound 4c is a new promising lead as orally potent and selective H3R antagonist belonging to a distinct structural class.

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Piperidine – Wikipedia,
Piperidine | C5H8057N – PubChem

 

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INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN

Disclosed are small molecule inhibitors of alphavbeta6 integrin, and methods of using them to treat a number of diseases and conditions.

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Piperidine – Wikipedia,
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Electric Literature of 2971-79-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.2971-79-1, Name is Methyl piperidine-4-carboxylate, molecular formula is C7H13NO2. In a Patent£¬once mentioned of 2971-79-1

2-PROPYNYL ADENOSINE ANALOGS WITH MODIFIED 5′-RIBOSE GROUPS HAVING A2A AGONIST ACTIVITY

The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described herein.

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Piperidine – Wikipedia,
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Synthesis of 5-amino-2-aminoalkyl-1,3-oxazol-4-ylphosphonic acid derivatives and their use in the preparation of phosphorylated peptidomimetics

Starting from phthalimidoalkanoylamines 1 (amino-protected derivatives of glycine, beta-alanine, gamma-amino butyric, delta-amino valeric, and epsilon-amino caproic acids), a facile synthetic method has been developed to obtain diethyl 5-alkyl(dialkyl)amino-2-aminoalkyl-1,3-oxazol-4-ylphosphonates 7, which have been further used in the preparation of phosphorylated peptidomimetics 10 and 12.

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Reference£º
Piperidine – Wikipedia,
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