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The design, synthesis and SAR of a novel class of valerolactam-based arylsulfonamides as potent and selective FXa inhibitors is reported. The arylsulfonamide-valerolactam scaffold was derived based on the proposed bioisosterism to the arylcyanoguanidine-caprolactam core in known FXa inhibitors. The SAR study led to compound 46 as the most potent FXa inhibitor in this series, with an IC50 of 7 nM and EC2×PT of 1.7 muM. The X-ray structure of compound 40 bound to FXa shows that the sulfonamide-valerolactam scaffold anchors the aryl group in the S1 and the novel acylcytisine pharmacophore in the S4 pockets.

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Piperidine – Wikipedia,
Piperidine | C5H16841N – PubChem

 

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Proviral insertion of Moloney virus (PIM) 1, 2, and 3 kinases are serine/threonine kinases that normally function in survival and proliferation of hematopoietic cells. As high expression of PIM1, 2, and 3 is frequently observed in many human malignancies, including multiple myeloma, non-Hodgkins lymphoma, and myeloid leukemias, there is interest in determining whether selective PIM inhibition can improve outcomes of these human cancers. Herein, we describe our efforts toward this goal. The structure guided optimization of a singleton high throughput screening hit in which the potency against all three PIM isoforms was increased >10,000-fold to yield compounds with pan PIM Kis < 10 pM, nanomolar cellular potency, and in vivo activity in an acute myeloid leukemia Pim-dependent tumor model is described. I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 142643-29-6, help many people in the next few years.Safety of 3-(Boc-aminomethyl)piperidine

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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, 142643-29-6, molcular formula is C11H22N2O2, introducing its new discovery. category: piperidines

This invention relates to substituted quinazolinone derivatives, compositions, and methods for treating diabetes, obesity and related disorders, and regulation of food intake (e.g., stimulation and suppression).

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Properties and Exciting Facts About 3-(Boc-aminomethyl)piperidine

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In order to identify novel anti-hepatitis C virus (HCV) agents we devised cell-based strategies and screened phenotypically small molecule chemical libraries with infectious HCV particles, and identified a hit compound (1) containing a hexahydropyrimidine (HHP) core. During our cell-based SAR study, we observed a conversion of HHP 1 into a linear diamine (6), which is the active component in inhibiting HCV and exhibited comparable antiviral activity to the cyclic HHP 1. In addition, we engaged into the biological characterization of HHP and demonstrated that HHP does not interfere with HCV RNA replication, but with entry and release of viral particles. Here we report the results of the preliminary SAR and mechanism of action studies with HHP.

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Piperidine – Wikipedia,
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Compounds of the formula STR1 wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 142643-29-6, name is 3-(Boc-aminomethyl)piperidine, introducing its new discovery. Recommanded Product: 3-(Boc-aminomethyl)piperidine

Solid dispersions containing an apoptosis-inducing agent

A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

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Piperidine – Wikipedia,
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Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based Drug Design

A HTS campaign identified compound 1, an excellent hit-like molecule to initiate medicinal chemistry efforts to optimize a dual ROCK1 and ROCK2 inhibitor. Substitution (2-Cl, 2-NH2, 2-F, 3-F) of the pyridine hinge binding motif or replacement with pyrimidine afforded compounds with a clean CYP inhibition profile. Cocrystal structures of an early lead compound were obtained in PKA, ROCK1, and ROCK2. This provided critical structural information for medicinal chemistry to drive compound design. The structural data indicated the preferred configuration at the central benzylic carbon would be (R), and application of this information to compound design resulted in compound 16. This compound was shown to be a potent and selective dual ROCK inhibitor in both enzyme and cell assays and efficacious in the retinal nerve fiber layer model after oral dosing. This tool compound has been made available through the AbbVie Compound Toolbox. Finally, the cocrystal structures also identified that aspartic acid residues 176 and 218 in ROCK2, which are glutamic acids in PKA, could be targeted as residues to drive both potency and kinome selectivity. Introduction of a piperidin-3-ylmethanamine group to the compound series resulted in compound 58, a potent and selective dual ROCK inhibitor with excellent predicted drug-like properties.

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Piperidine – Wikipedia,
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PIPERIDINE AMIDES AS MODULATORS OF THE GHRELIN RECEPTOR

Compounds of formula (I) or pharmaceutically acceptable salts thereof, are useful for the treatment of diabetes and obesity.

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Piperidine – Wikipedia,
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142643-29-6, 3-(Boc-aminomethyl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

64a) {1-[2-(3-Chloro-6-methoxy-quinolin-4-yl)-2-hydroxy-ethyl]-piperidin-3-ylmethyl}-carbamic acid tert-butyl ester (enantiomer1)Epoxide (56f) (900 mg), 3-(N-Boc-aminomethyl)piperidine (819ing) i potassium carbonate (555 mg) and lithium perchlorate (405mg) were suspended in DMF (9 ml) and heated in the microwave for35 minutes at 130C. The mixture was concentrated, the residuedissolved in ethyl acetate and washed with water and brine. Theorganic layer was dried over magnesium sulfate, filtered andevaporated. The residue was purified by flash chromatography(silica gel, dichloromethane/methanol 97:3) to give the desiredproduct (1.6 g).MS (El): m/z: 450 [M+H]+, 142643-29-6

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Reference£º
Patent; MORPHOCHEM AKTIENGESELLSCHAFT FUeR KOMBINATORISCHE CHEMIE; WO2006/21448; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.142643-29-6,3-(Boc-aminomethyl)piperidine,as a common compound, the synthetic route is as follows.

Step 1. Preparation of tert-butvlin-(cvclopropvlmethvnpiperidin-3-vl1methyl)carbamate; ,NHNCH3O CH3[114] To a dry 10 mL round-bottom flask was added 3-/V-(tert-butoxycarbonylaminomethylpiperidine (500 mg, 2.33 mmol) followed by anhydrous dichloroethane (5.0 mL). The mixture wasstirred at rt under an atmosphere of N2 for 5 min, and then cyclopropanecarboxaldehyde (0.17 mL,2.33 mmol) and glacial acetic acid (0.80 mL, 14.0 mmol) were added. After stirring for 10 min,NaB(OAc)3H (1.98 g, 9.33 mmol) was added, and the milky white reaction mixture was stirred for15 h. The mixture was quenched with saturated aq Na2CO3 (10 mL) and was extracted withCH2CI2 (3 x 20 mL). The combined organic layers were washed with water (2 x 20 mL), dried overMgSO4> filtered, and concentrated under reduced pressure. Purification by flash silica gelchromatography (95% CH2CI2: 5% 2M NH3 in MeOH) gave the product as a yellow oil (388 mg,62%). R,= 0.23 (97% CH2CI2: 3% 2M NH3 in MeOH); 1H NMR (300 MHz, CDCI3) 6 4.60 (br s,351 H), 3.05-2.96 (m, 4H), 2.27 (d, 2H), 1 .96 (dd, 1 H), 1 .76-1 .61 (m, 5H), 1 .44 (s, 9H), 0.98-0.85 (m,2H), 0.55-0.49 (m, 2H), 0.13-0.09 (dd, 2H); ES-MS m/z269 (MH+).

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Reference£º
Patent; BAYER PHARMACEUTICALS CORPORATION; WO2006/12577; (2006); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem