Category: piperidines

Rafiq, Kiran; Saify, Zafar Saied; Kausar, Rana; Rahim, Najia; Naeem, Sabahat published an article in 2014, the title of the article was The structural modification causes the enhancement of analgesic activity of 4-(4′ chloro-phenyl)-4-hydroxy piperidine.Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

Objective- The outstanding position of piperidine analogs has proven them an important core in the structures of pharmaceutically active mols., naturally occurring alkaloids, pharmaceuticals and as synthetic intermediates with interesting biol., phys. and pharmacol. behaviors. The piperidine ring containing compound like pethidine having strong opiod analgesic activity, more potent than codein and controls the pain of smooth muscle spasm. Because of having similarity in structure the present study was aimed to estimate the analgesic activity of synthesized derivatives of 4-(4′-Chlorophenyl)-4-hydroxy piperidine. Method- The present study was conducted in animal model, mice by using Pethidine as standard drug. For which the Eddy’s hot plate method was adopted and analgesia (mean increase in latency) was observed Result- The result showed the more prominent response of substituted compound than the parent one “4-(4′-Chlorophenyl)-4-hydroxy piperidine” and it was studied that alteration in the mol. structure is accountable for a better analgesic response. Conclusion- The studies proved the pos. pharmacol. responsiveness of the combination of 4-(4′-Chlorophenyl)-4-hydroxy piperidine with phencyl halides. These synthesized derivatives will establish as potent analgesics. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to chlorophenyl hydroxy piperidine analgesic activity structural modification, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On October 14, 2021, Netherton, Matthew; Brucelle, Francois published a patent.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Preparation of substituted hydroxyphenylpyridazinamines for treating BAF complex-related disorders. And the patent contained the following:

The present disclosure features compounds I [X1 = O or NR2; each X2 = (independently) halo; k = 0-4; m = 0-4; R1 = halo or (un)substituted alkyl; R2 = H or (un)substituted alkyl; L1 = (un)substituted alkylene; L = L2(L3)n; n = 0-3; L2 = (un)substituted alkylene, heteroalkylene, or heterocyclylene; each L3 = (independently) O, (un)substituted heteroalkylene, carbocyclylene, etc.; and D = a degradation moiety] or pharmaceutically acceptable salts thereof, useful for the treatment of BAF complex-related disorders. E.g., a multi-step synthesis of II, starting from 4-bromo-6-chloropyridazin-3-amine and Et 2-(piperazin-1-yl)acetate, was described. Exemplified compounds I were evaluated for their ability to degrade a HiBit-BRM or HiBit-BRG1 fusion protein in a cell-based degradation assay (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).Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to hydroxyphenylpyridazinamine preparation baf complex related disorder, brm brg1 fusion protein degradation hydroxyphenylpyridazinamine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 2, 2021, Wang, Qiuwen; Guo, Yunhang; Wang, Zhiwei published a patent.Category: piperidines The title of the patent was Synthesis of pyridazine Tyk-2 inhibitors for treating inflammatory or autoimmune diseases. And the patent contained the following:

The synthesis of pyridazine heterocyclic Tyk-2 inhibitors I, wherein R1 can be H, or optionally substituted C1-6-alkyl or C3-6cycloalkyl groups; R2 can be a -C(O)- group with an (un)substituted 4-10 membered heterocyclic ring system; R3 is a fused bicyclic heterocyclic ring system with independently substituted H, halo, cyano or alkyl groups are prepared as pharmaceutically acceptable salts for treating inflammatory or autoimmune diseases. Of note, II was prepared and tested in biochem. and cellular assays with nM inhibition and high selectivity. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Category: piperidines

The Article related to pyridazine tyk2 inhibitor preparation antiinflammatory autoimmune disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On October 1, 2017, Schwalbe, Tobias; Kaindl, Jonas; Huebner, Harald; Gmeiner, Peter published an article.COA of Formula: C11H14ClNO The title of the article was Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. And the article contained the following:

The dopamine D2 receptor (D2R) is a common drug target for the treatment of a variety of neurol. disorders including schizophrenia. Structure based design of subtype selective D2R antagonists requires high resolution crystal structures of the receptor and pharmacol. tools promoting a better understanding of the protein-ligand interactions. Recently, we reported the development of a chem. activated dopamine derivative (FAUC150) designed to covalently bind the L94C mutant of the dopamine D2 receptor. Using FAUC150 as a template, we elaborated the design and synthesis of irreversible analogs of the potent antipsychotic drug haloperidol forming covalent D2R-ligand complexes. The disulfide- and Michael acceptor-functionalized compounds showed significant receptor affinity and an irreversible binding profile in radioligand depletion experiments 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 preparation haloperidol derivative covalently binding dopamine d2 receptor, chemical probe, covalent ligand, disulfide tethering, dopamine d(2) receptor, g protein-coupled receptor, haloperidol and other aspects.COA of Formula: C11H14ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On April 25, 2013, Connolly, Peter J.; Bian, Haiyan; Li, Xun; Liu, Li; Macielag, Mark J.; McDonnell, Mark E. published a patent.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Preparation of piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors. And the patent contained the following:

The title compounds I [Y and Z = (un)substituted aryl, heteroaryl, 1,3-dihydro-3H-benzimidazol-2-on-yl, etc.; R = H or OH], useful for treating various diseases, syndromes, conditions and disorders, including pain, were prepared E.g., a multi-step synthesis of II, starting from tert-Bu 3-iodoazetidine-1-carboxylate, was described. Exemplified compounds I were tested in the MGL activity assay (data given). Pharmaceutical composition comprising compound I is disclosed. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to piperidinylazetidine diamide amide preparation monoacylglycerol lipase inhibitor analgesic, inflammatory pain treatment piperidinylazetidine amide preparation monoacylglycerol lipase inhibitor and other aspects.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wakulik, Karolina; Wiatrak, Benita; Szczukowski, Lukasz; Bodetko, Dorota; Szandruk-Bender, Marta; Dobosz, Agnieszka; Swiatek, Piotr; Gasiorowski, Kazimierz published an article in 2020, the title of the article was Effect of novel pyrrolo[3,4-d]pyridazinone derivatives on lipopolysaccharide-induced neuroinflammation.COA of Formula: C11H14ClNO And the article contains the following content:

Neuroinflammation is considered to be one of the potential causes for the development of neurodegenerative diseases, including Alzheimer’s disease. In this study, we evaluated the effect of four newly synthesized pyrrolo[3,4-d]pyridazinone derivatives on the neuron-like PC12 cells under simulated inflammation conditions by preincubation with lipopolysaccharide (LPS). Our novel derivatives are selective cyclooxygenase-2 (COX-2) inhibitors and have similar effects to nonsteroidal anti-inflammatory drugs (NSAIDs). We assessed viability (LDH assay), metabolic activity (MTT assay), DNA damage (number of double-strand breaks measured by fast halo assay), and the neuronal features of cells (average neurite length and neurite outgrowth measured spectrofluorimetrically). DCF-DA and Griess assays were also performed, which allowed determining the impact of the tested compounds on the level of oxygen free radicals and nitrites. LPS administration significantly neg. affected the results in all tests performed, and treatment with the tested derivatives in most cases significantly reduced this neg. impact. Multiple-criteria decision anal. indicated that overall, the best results were observed for compounds 2a and 2b at a concentration of 10μM. The new derivatives showed intense activity against free oxygen radicals and nitrites. Reduced reactive oxygen species level also correlated with a decrease in the number of DNA damage. The compounds improved neuronal features, such as neurite length and outgrowth, and they also increased cell viability and mitochondrial activity. Our results suggest that derivatives 2a and 2b may also act addnl. on mechanisms other than 3a and 3b. 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 pyrrolo pyridazinone derivative neuroregenerative neuroinflammation dna damage, alzheimer’s disease, lps, nsaid, cyclooxygenase inhibitor, lipopolysaccharide, neuroinflammation, pyridazinone and other aspects.COA of Formula: C11H14ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On April 20, 2006, Burgey, Christopher S.; Deng, James Z.; Potteiger, Craig; Williams, Theresa M. published a patent.Recommanded Product: Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate The title of the patent was Preparation of oxohomopiperidinyl oxospiropiperidinepyrrolopyridinecarboxamides and related compounds as calcitonin gene-related peptide (CGRP) receptor antagonists.. And the patent contained the following:

Title compounds [I; A = bond, C(R2)2, O, SOm, NR2; B = [C(R2)2]n; R1, R2 = H, (substituted) alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl; pairs of R2 may form rings; R3 = H, F, cyano, (substituted) alkyl, CO2R4; R4 = H, (substituted) alkyl, fluoroalkyl, cycloalkyl, aryl, heteroaryl, PhCH2; X = C, S; Y = O, (R4)2, NCN, NHSO2Me, NCONH2; or Y = O2 when X = S; J = bond, C(R6)2, O, NR6; V = bond, C(R6)2, O, SOm, NR6, NR6NR6, etc.; Q = CR7a, C(R7A)2, CO, SOm, N, NR7a; T = CR7b, C(R7b)2, CO, SOm, N, NR7b; R6 = H, halo, OR4, CO2R4, alkyl, cycloalkyl, (substituted) aryl, heteroaryl, heterocyclyl, etc.; R7a, R7b = R2; R7aR7b = atoms to form cycloalkyl, aryl, heterocyclyl, heteroaryl rings; m = 0-2; n = 0, 1], were prepared for treatment of headache (no data). Thus, (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one (preparation given) and 4-nitrophenyl chloroformate in THF at 0° were treated with Et3N; after 60 min. spiro[piperidine-4,3′-pyrrolo[2,3-b]pyridin]-2′(1’H)-one dihydrochloride (preparation given) and Et3N in CHCl3 were added followed by warming to room temperature to give title compound (II). The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Recommanded Product: Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

The Article related to oxoazepanyl oxospiropiperidinepyrrolopyridinecarboxamide preparation cgrp receptor antagonist, headache treatment oxohomopiperidinyl spiropiperidinepyrrolopyridinecarboxamide preparation and other aspects.Recommanded Product: Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 14, 2021, Tong, Youzhi; Lai, Luhua published a patent.SDS of cas: 1216805-11-6 The title of the patent was C-myc protein inhibitor, and preparation method therefor and use thereof. And the patent contained the following:

Provided are a c-Myc protein inhibitor, and a preparation method therefor and use thereof. The c-Myc protein inhibitor selectively inhibits c-Myc protein. Therefore, the inhibitor can be used for prevention and treatment of diseases related to c-Myc protein disorders, such as cancers, cardiovascular and cerebrovascular diseases, diseases related to virus infection. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).SDS of cas: 1216805-11-6

The Article related to amino acid boronic acid boronate derivative preparation, myc protein inhibitor amino acid boronic acid boronate derivative, antitumor activity amino acid boronic acid boronate derivative and other aspects.SDS of cas: 1216805-11-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kaneria, A. A.; Thumar, N. M.; Ladva, K. D.; Vadodaria, M. S. published an article in 2017, the title of the article was Synthesis, characterization and antimicrobial activity studies of some new N-substituted piperidine derivatives of 2-(4-chloro-4-(4-chlorophenyl))piperidine.Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

Two series of N-substituted piperidine derivatives containing oxadiazoles I [R = H, 4-MeOC6H4, 4-BrC6H4, etc.] and acetohydrazides II were synthesized via reaction of 2-(2-chlorophenyl)-2-(4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl)acetohydrazide with aromatic carboxylic acids and aryl aldehydes resp. Compounds I and II were screened for their antimicrobial activities against various strains of bacteria and fungi. Compounds I [R = Ph, 4-FC6H4, 4-MeOC6H4, 4-O2NC6H4] and II [R = Ph, 4-OH-3-MeOC6H3, 2,4,5-FC6H2] and pyridyl derivative exhibited excellent activity against Gram pos. bacteria, Gram neg. bacteria and fungi. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to chloro piperidinyl chlorophenylmethyl aryl oxadiazole preparation antibacterial antifungal, arylidene hydroxypiperidinyl chlorophenyl acetohydrazide preparation antibacterial antifungal and other aspects.Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On August 25, 2016, Boudhar, Aicha; Ng, Xiao Wei; Loh, Chiew Yee; Chia, Wan Ni; Tan, Zhi Ming; Nosten, Francois; Dymock, Brian W.; Tan, Kevin S. W. published an article.Safety of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents. And the article contained the following:

Malaria remains a significant infectious disease with even artemisinin-based therapies now facing resistance in the field. Development of new therapies is urgently needed, either by finding new compounds with unique modes of action, or by reversing resistance towards known drugs with ‘chemosensitizers’ or ‘chemoreversal’ agents (CRA). Concerning the latter, we have focused on the resistance mechanisms developed against chloroquine (CQ). We have synthesized a series of compounds related to previously identified CRAs, and found promising novel compounds These compounds show encouraging results in a coumarin labeled chloroquine uptake assay, exhibiting a dose response in resensitizing parasites to the antimalarial effects of chloroquine. Selected compounds show consistent potency across a panel of chloroquine and artemisinin sensitive and resistant parasites, and a wide therapeutic window. This data supports further study of CRAs in the treatment of malaria and, ultimately, their use in chloroquine-based combination therapies. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Safety of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to structure malaria antimalarial chemoreversal preparation chloroquine resistance, antimalarial, artemisinin-resistant, chemoreversal, chemosensitiser, chloroquine, chloroquine-resistant and other aspects.Safety of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem