Tag: 200-300

On August 25, 2016, Damont, Annelaure; Goutal, Sebastien; Auvity, Sylvain; Valette, Heric; Kuhnast, Bertrand; Saba, Wadad; Tournier, Nicolas published an article.Reference of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Imaging the impact of cyclosporin A and dipyridamole on P-glycoprotein (ABCB1) function at the blood-brain barrier: A [11C]-N-desmethyl-loperamide PET study in nonhuman primates. And the article contained the following:

Cyclosporin A (CsA) and dipyridamole (DPy) are potent inhibitors of the P-glycoprotein (P-gp; ABCB1) in vitro. Their efficacy at inhibiting P-gp at the blood-brain barrier (BBB) is difficult to predict. Efficient and readily available (i.e. marketed) P-gp inhibitors are needed as probes to investigate the role of P-gp at the human BBB. In this study, the P-gp inhibition potency at the BBB of therapeutic doses of CsA or DPy was evaluated in baboons using Positron Emission Tomog. (PET) imaging with [11C]-N-desmethyl-loperamide ([11C]dLop), a radiolabeled P-gp substrate. The preparation of dLop as authentic standard and [11C]dLop as radiotracer were revisited so as to improve their production yields. [11C]dLop PET imaging was performed in the absence (n = 3, baseline condition) and the presence of CsA (15 mg/kg/h i.v., n = 3). Three animals were injected with i.v. DPy at either 0.56 or 0.96 or 2 mg/kg (n = 1), corresponding to the usual, maximal and twice the maximal dose in patients, resp., administered immediately before PET. [11C]dLop brain kinetics as well as [11C]dLop kinetics and radiometabolites in arterial plasma were measured to calculate [11C]dLop area-under the time-activity curve from 10 to 30 min in the brain (AUCbrain) and in plasma (AUCplasma). [11C]dLop brain uptake was described by AUCR = AUCbrain/AUCplasma. CsA as well as DPy did not measurably influence [11C]dLop plasma kinetics and metabolism Baseline AUCR (0.85 ± 0.29) was significantly enhanced in the presence of CsA (AUCR = 10.8 ± 3.6). Injection of pharmacol. dose of DPy did not enhance [11C]dLop brain distribution with AUCR being 1.2, 0.9 and 1.1 after administration of 0.56, 0.96 and 2 mg/kg DPy doses, resp. We used [11C]dLop PET imaging in baboons, a relevant in vivo model of P-gp function at the BBB, to show the P-gp inhibition potency of therapeutic dose CsA. Despite in vitro P-gp inhibition potency, usual doses DPy are not likely to inhibit P-gp function at the BBB. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Reference of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to cyclosporin a dipyridamole pgp inhibitor abcb1 drug interaction, bbb, drug-drug interaction, positron emission tomography, radiochemistry, stress-test, Pharmacology: Effects Of Inflammation Inhibitors and Immune Agents and other aspects.Reference of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 23, 2021, Barbaraci, Carla; Giurdanella, Giovanni; Leotta, Claudia Giovanna; Longo, Anna; Amata, Emanuele; Dichiara, Maria; Pasquinucci, Lorella; Turnaturi, Rita; Prezzavento, Orazio; Cacciatore, Ivana; Zuccarello, Elisa; Lupo, Gabriella; Pitari, Giovanni Mario; Anfuso, Carmelina Daniela; Marrazzo, Agostino published an article.Synthetic Route of 39512-49-7 The title of the article was Haloperidol Metabolite II Valproate Ester (S)-(-)-MRJF22: Preliminary Studies as a Potential Multifunctional Agent Against Uveal Melanoma. And the article contained the following:

Increased angiogenesis and vascular endothelial growth factor (VEGF) levels contribute to higher metastasis and mortality in uveal melanoma (UM), an aggressive malignancy of the eye in adults. (±)-MRJF22, a prodrug of the sigma (σ) ligand haloperidol metabolite II conjugated with the histone deacetylase (HDAC) inhibitor valproic acid, has previously demonstrated a promising antiangiogenic activity. Herein, the asym. synthesis of (R)-(+)-MRJF22 and (S)-(-)-MRJF22 was performed to investigate their contribution to (±)-MRJF22 antiangiogenic effects in human retinal endothelial cells (HREC) and to assess their therapeutic potential in primary human uveal melanoma (UM) 92-1 cell line. While both enantiomers displayed almost identical capabilities to reduce cell viability than the racemic mixture, (S)-(-)-MRJF22 exhibited the highest antimigratory effects in endothelial and tumor cells. Given the fundamental contribution of cell motility to cancer progression, (S)-(-)-MRJF22 (I) may represent a promising candidate for novel antimetastatic therapy in patients with UM. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Synthetic Route of 39512-49-7

The Article related to melanoma antimetastatic therapy vegf enantiomers antiangiogenic antiproliferative valproate ester, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Synthetic Route of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On August 13, 2020, Robles, Omar; Jackson, Jeffrey J.; Marshall, Lisa; Talay, Oezcan; Chian, David; Cutler, Gene; Diokno, Raymond; Hu, Dennis X.; Jacobson, Scott; Karbarz, Emily; Kassner, Paul D.; Ketcham, John M.; McKinnell, Jenny; Meleza, Cesar; Reilly, Maureen K.; Riegler, Erin; Shunatona, Hunter P.; Wadsworth, Angela; Younai, Ashkaan; Brockstedt, Dirk G.; Wustrow, David J.; Zibinsky, Mikhail published an article.Application In Synthesis of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the article was Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors. And the article contained the following:

The C-C chemokine receptor 4 (CCR4) is broadly expressed on regulatory T cells (Treg) as well as other circulating and tissue-resident T cells. Treg can be recruited to the tumor microenvironment (TME) through the C-C chemokines CCL17 and CCL22. Treg accumulation in the TME has been shown to dampen the antitumor immune response and is thought to be an important driver in tumor immune evasion. Preclin. and clin. data suggest that reducing the Treg population in the TME can potentiate the antitumor immune response of checkpoint inhibitors. We have developed small-mol. antagonists of CCR4, featuring a novel piperidinyl-azetidine motif, that inhibit the recruitment of Treg into the TME and elicit antitumor responses as a single agent or in combination with an immune checkpoint blockade. The discovery of these potent, selective, and orally bioavailable CCR4 antagonists(I), and their activity in in vitro and in vivo models, is described herein. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Application In Synthesis of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to antitumor ccr4 antagonists checkpoint inhibitors combination immune response bioavailability, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application In Synthesis of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 30, 1990, Nemeryuk, M. P.; Sedov, A. L.; Ryabokon, N. A.; Ershova, Yu. A.; Sokolova, A. S.; Losev, A. G.; Chernov, V. A.; Safonova, T. S. published an article.Application In Synthesis of 4-Chloro-6-(piperidin-1-yl)pyrimidin-5-amine The title of the article was 4(5)-Substituted 1,2,3-triazole-5(4)-carboxylic acid derivatives: synthesis and antitumor activity. And the article contained the following:

The title compounds [I, X = e.g., CO2Me, C(:NH)SMe, piperidino- or morpholino(imino)methyl, and Y = SMe, Cl, CN, OMe, SCH2Ph, 1-methyl-1-isobutyl-4-nitroimidazolyl-5-thio) were prepared by the diazotization of aminopyrimidines. The structure of the products was dependent on the type of substituents present and the conditions of carrying out the reaction. The compounds had antitumor activity both in vitro and in vivo. The highest activity was shown by I (X = CO2Me, Y = 2-nitro-5-acetyl-3-thienylthio) or X = C(:NH)NMe2 and Y = OMe). I had low toxicity. The experimental process involved the reaction of 4-Chloro-6-(piperidin-1-yl)pyrimidin-5-amine(cas: 84762-70-9).Application In Synthesis of 4-Chloro-6-(piperidin-1-yl)pyrimidin-5-amine

The Article related to triazolecarboxylate derivative preparation antitumor, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application In Synthesis of 4-Chloro-6-(piperidin-1-yl)pyrimidin-5-amine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On March 13, 2013, Bao, Xiaofeng; Liu, Duliang published an article.COA of Formula: C11H14ClNO The title of the article was Radiosynthesis of 18F-labeled N-desmethyl-loperamide analogues for prospective molecular imaging radiotracers. And the article contained the following:

A simple procedure for preparing fluoroethyl-N-desmethyl-loperamide and its analog I [X = (CH2)2, (CH2)3, Y = F] was developed. Standard compound I [X = (CH2)2, Y = F] was synthesized in useful yields for radiolabeling anal. [N-Ethyl-18F]N-desmethyl-loperamide, I [X = (CH2)2, Y = 18F], was rapidly and efficiently labeled with no-carrier added fluorine-18 (t1/2 = 109.7 min) by treatment of readily prepared [18F]1-bromo-2-fluoroethane with a N-desmethyl-loperamide precursor at a consistent 7% radiochem. yield. This procedure was also adapted to the radiosynthesis of I [X = (CH2)2, Y = 18F] by [18F]ethylene tosylate, but at a lower 3% radiochem. yield. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).COA of Formula: C11H14ClNO

The Article related to loperamide analog radiosynthesis loperamide fluorine 18 pet permeability glycoprotein, Heterocyclic Compounds (One Hetero Atom): Other 6-Membered Rings and other aspects.COA of Formula: C11H14ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 9, 2020, Ji, Nan; Mainolfi, Nello; Weiss, Matthew published a patent.Synthetic Route of 1251006-64-0 The title of the patent was Preparation of novel bifunctional compounds as MerTK degraders and uses thereof. And the patent contained the following:

The present invention provides compounds I [TAMBM is an TAM receptor kinase binding moiety; L is a bivalent moiety that connects TAMBM to DIM; and DIM is a degradation inducing moiety selected from LBM, a lysine mimetic, and H] or pharmaceutically acceptable salts thereof, compositions thereof, and methods of using the same. E.g., a multi-step synthesis of trans-II, starting from Et 4-chloro-2-(methylsulfanyl)pyrimidine-5-carboxylate, was described. Exemplified compounds I were tested for MerTK degradation in vitro (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Synthetic Route of 1251006-64-0

The Article related to bifunctional compound preparation mertk degrader, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 1251006-64-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Cabrero-Antonino, Jose R.; Leyva-Perez, Antonio; Corma, Avelino published an article in 2012, the title of the article was Regioselective Hydration of Alkynes by Iron(III) Lewis/Bronsted Catalysis.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

The triflimide iron(III) salt [Fe(NTf2)3] promotes the direct hydration of terminal and internal alkynes with very good Markovnikov regioselectivities and high yields. The enhanced carbophilic Lewis acidity of the FeIII cation mediated by the weakly-coordinating triflimide anion is crucial for the catalytic activity. The iron(III) metal salt can be recycled as the OPPh3/[Fe(NTf2)3] system with similar activity and selectivity. However, spectroscopic and kinetic studies show that [Fe(NTf2)3] hydrolyzes under the reaction conditions and that catalytically less active Broensted species are formed, which points to a Lewis/Broensted co-catalysis. This triflimide-based catalytic system is regioselective for the hydration of internal aryl-alkynes and opens the door to a new synthetic route to alkyl ketophenones. As a proof of concept, the synthesis of two antipsychotics Haloperidol and Melperone, with general butyrophenone-like structure, is shown. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to regioselective hydration alkyne iron lewis broensted catalysis, Physical Organic Chemistry: Addition, Elimination, and Substitution Reactions and other aspects.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Klochkov, S. G.; Anan’ev, I. V.; Pukhov, S. A.; Afanas’eva, S. V. published an article in 2012, the title of the article was Stereochemistry of the aza-Michael reaction with natural alantolactones.Related Products of 39512-49-7 And the article contains the following content:

Hydrogenated 3-aminomethylnaphtho[2,3-b]furan-2-ones were synthesized by the reaction of natural alantolactones with pharmacophoric amines. Determination of the newly formed asym. center configuration by two-dimensional NMR data is presented. The structure of the obtained compounds was proved by X-ray structural anal. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Related Products of 39512-49-7

The Article related to stereochem aza michael reaction natural alantolactone, Physical Organic Chemistry: Addition, Elimination, and Substitution Reactions and other aspects.Related Products of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zhu, Xue Y.; Etukala, Jagan R.; Eyunni, Suresh V. K.; Setola, Vincent; Roth, Bryan L.; Ablordeppey, Seth Y. published an article in 2012, the title of the article was Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): A search for new dual-acting agents as potential antidepressants.HPLC of Formula: 39512-49-7 And the article contains the following content:

The synthesis and evaluation of several benzothiazole-based compounds are described in an attempt to identify novel dual-acting 5HT1A receptor and SERT inhibitors as new antidepressants. Binding affinities at the 5HT1A receptor and the serotonin transporter do not appear to be congruent and other areas of the binding sites would need to be explored in order to improve binding simultaneously at both sites. Compounds I and II show moderate binding affinity at the 5HT1A receptor and the SERT site and thus, have the potential to be further explored as dual-acting agents. In addition, compound I binds with low affinity to the dopamine transporter (DAT), the norepinephrine transporter (NET) and 5HT2C receptor, which are desirable properties as selectivity for SERT (and not DAT or NET) is associated with an absence of cardiovascular side effects. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).HPLC of Formula: 39512-49-7

The Article related to benzothiazole preparation 5ht1a receptor sert inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.HPLC of Formula: 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 31, 1985, Levkovskaya, L. G.; Sazonov, N. V.; Grineva, N. A.; Mamaeva, I. E.; Serochkina, L. A.; Safonova, T. S. published an article.COA of Formula: C9H13ClN4 The title of the article was Study of nitrogen- and oxygen-containing heterocycles. 42. Pyrimido[4,5-b]- and pyrido[2,3-b]-1,4-benzoxazepines. And the article contained the following:

Oxazepines I (R = H, Cl, R1X = N, CH, ClCH, R2 = NHCH2Ph, NHPh, piperidino, morpholino, NH2, Cl, OH, 1-methylpiperazinyl, H) were prepared in 25-95% yields by cyclocondensation of pyridines or pyrimidines II wiwth 5,2-R3YC6H3CHO in DMF containing NaH. Reduction of I by NaBH4 in absolute EtOH gave 76-100% of the corresponding 5,6-dihydro derivatives The experimental process involved the reaction of 4-Chloro-6-(piperidin-1-yl)pyrimidin-5-amine(cas: 84762-70-9).COA of Formula: C9H13ClN4

The Article related to benzopyridooxazepine, benzopyrimidooxazepine, pyridooxazepine benzo, pyrimidooxazepine, oxazepine pyrido pyrimido, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.COA of Formula: C9H13ClN4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem