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COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY

The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists, to processes for their preparation, to compositions comprising them, to therapeutic uses and combinations with other pharmaceutical active ingredients.

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Piperidine – Wikipedia,
Piperidine | C5H12640N – PubChem

 

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Aminopyridazines as acetylcholinesterase inhibitors

Following the discovery of the weak, competitive and reversible acetylcholinesterase (AChE)-inhibiting activity of minaprine (3c) (IC50 = 85 muM on homogenized rat striatum AChE), a series of 3-amino-6- phenylpyridazines was synthesized and tested for inhibition of AChE. A classical structure-activity relationship exploration suggested that, in comparison to minaprine, the critical elements for high AChE inhibition are as follows: (i) presence of a central pyridazine ring, (ii) necessity of a lipophilic cationic head, (iii) change from a 2- to a 4-5-carbon units distance between the pyridazine ring and the cationic head. Among all the derivatives investigated, 3-[2-(1-benzylpiperidin-4-yl)ethylamino]-6- phenylpyridazine (3y), which shows an IC50 of 0.12 muM on purified AChE (electric eel), was found to be one of the most potent anti-AChE inhibitors, representing a 5000-fold increase in potency compared to minaprine.

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Piperidine – Wikipedia,
Piperidine | C5H4562N – PubChem

 

More research is needed about 127294-73-9

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8-(3-AMINO-PIPERIDIN-1-YL)-XANTHINES, THEIR PREPARATION, AND THEIR USE AS PHARMACEUTICALS

The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.

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Piperidine | C5H533N – PubChem

 

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Novel SAR for quinazoline inhibitors of EHMT1 and EHMT2

Detailed structure activity relationship of two series of quinazoline EHMT1/EHMT2 inhibitors (UNC0224 and UNC0638) have been elaborated. New and active alternatives are presented for the ubiquitous substitution patterns found in literature for the linker to the lysine mimicking region and the lysine mimic itself. These findings could allow for advancing EHMT1/EHMT2 inhibitors of that type beyond tool compounds by fine-tuning physicochemical properties making these inhibitors more drug-like.

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Piperidine – Wikipedia,
Piperidine | C5H2027N – PubChem

 

A new application about 2-(Hydroxymethyl)piperidine

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Recent advances in quantum-mechanical molecular dynamics simulations of proton transfer mechanism in various water-based environments

Proton transfer in water-based environments occurs because of hydrogen-bond interaction. There are many interesting physicochemical phenomena in this field, causing fast structural diffusion of hydronium and hydroxide ions. During the last few decades, to support experimental observations and measurements, quantum-mechanical molecular dynamics (QMMD) simulations with reasonable accuracy and efficiency have significantly unraveled structural, energetic, and dynamical properties of excess proton in aqueous environments. This review summarizes the state-of-the-art QMMD studies of proton transfer processes in aqueous solutions and complex systems including bulk liquid water, ice phases, and confined water in nanochannel/nanoporous materials as well as reports on CO2 scrubbing by amine-based chemical absorption. This article is categorized under: Structure and Mechanism > Reaction Mechanisms and Catalysis Molecular and Statistical Mechanics > Molecular Dynamics and Monte-Carlo Methods Electronic Structure Theory > Semiempirical Electronic Structure Methods Theoretical and Physical Chemistry > Reaction Dynamics and Kinetics.

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Piperidine – Wikipedia,
Piperidine | C5H2802N – PubChem

 

More research is needed about 4,4-Difluoropiperidine

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Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines

Based on the initial optimization of orally active antimalarial 2,4-diamino-thienopyrimidines and with the help of metabolite identification studies, a second generation of derivatives involving changes at the 2- and 4-positions of the thienopyrimidine core were synthesized. Improvements in the physiochemical properties resulted in the identification of 15a, 17a, 32, and 40 as lead molecules with improved in vivo exposure. Furthermore, analogue 40 exhibited excellent in vivo antimalarial activity when dosed orally at 50 mg/kg once daily for 4 days in the Plasmodium berghei mouse model, which is superior to the activity seen with previously reported compounds, and with a slightly improved hERG profile.

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Piperidine – Wikipedia,
Piperidine | C5H3105N – PubChem

 

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The discovery and SAR of indoline-3-carboxamides – A new series of 5-HT6 antagonists

Antagonists of the 5-HT6 receptor have been shown to improve cognitive function in a wide range of animal models and as such may prove to be attractive agents for the symptomatic treatment of cognitive disorders such as Alzheimer’s disease (AD) and schizophrenia. We report herein the identification and SAR around N-(2-aminoalkyl)-1-(arylsulfonyl)indoline-3-carboxamides – a novel chemotype of 5-HT6 antagonists.

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Piperidine – Wikipedia,
Piperidine | C5H11929N – PubChem

 

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Unusually Large 13C NMR Chemical Shift Differences between Neutral and Protonated Glycocyamidines. New Insights on Previously Reported Chemical Shift Assignments and Chemical Properties

Unusually large 13C chemical shift differences are observed between neutral and protonated glycocyamidine (2-aminoimidazolinone) derivatives. Upon protonation, the guanidine (N-C=N) and carbonyl (C=O) carbons undergo an upfield shift of approximately 12 and 17 ppm, respectively, relative to the neutral species. For neutral glycocyamidine derivatives, the 13C chemical shifts for the carbonyl carbon reside above 190 ppm. In the protonated form, the carbonyl resonances are in the mid to lower 170s. These values are indicative of the protonation state of the glycocyamidine moiety. The present study serves as a useful reference in assisting the characterization of future glycocyamidine-based natural products and derivatives.

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Piperidine – Wikipedia,
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Phase Transition Enthalpy Measurements of Organic and Organometallic Compounds. Sublimation, Vaporization and Fusion Enthalpies From 1880 to 2015. Part 1. C1-C10

A compendium of phase change enthalpies published in 2010 is updated to include the period 1880-2015. Phase change enthalpies including fusion, vaporization, and sublimation enthalpies are included for organic, organometallic, and a few inorganic compounds. Part 1 of this compendium includes organic compounds from C1-C10. Part 2 of this compendium, to be published separately, will include organic and organometallic compounds from C11 to C192. Sufficient data are presently available to permit thermodynamic cycles to be constructed as an independent means of evaluating the reliability of the data. Temperature adjustments of phase change enthalpies from the temperature of measurement to the standard reference temperature, T = 298.15 K, and a protocol for doing so are briefly discussed.

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Piperidine – Wikipedia,
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Application of 68947-43-3, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.68947-43-3, Name is 1-Methylpiperidine-4-carboxylic acid, molecular formula is C7H13NO2. In a article£¬once mentioned of 68947-43-3

INDOLE, INDAZOLE, AND BENZAZOLE DERIVATIVE

The compound of the formula (I): wherein W is a group of the following formula (VIII) binding to any possible position on the Q: Q is, together with W, a group of the formula: -C(M=C(R3A)-N(R3)-, etc.; R3A is H or optionally substituted lower alkyl; R4, R5, R6, and R7 are independently H or optionally substituted lower alkyl; R1 is optionally substituted lower alkyl, etc.; R2 is H, etc.; R3 is H, etc.; Ar is phenyl, etc., or a pharmaceutically acceptable salt thereof, where these compounds exhibiting beta3-adrenoceptor-stimulating activity and being useful as a medicament for treatment of obesity, etc.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H6932N – PubChem