Month: October 2022

On June 25, 2020, Cheng, Zhanling; Khan, Nawaz; Kramer, Christian; Lerner, Christian; Pflieger, Philippe; Stoll, Theodor; Wang, Jianhua; Wang, Yongguang; Yang, Song published a patent.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Novel imidazopyrazine derivatives as antibacterials and their preparation. And the patent contained the following:

The invention provides imidazopyrazine derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases. Compounds of formula I wherein ring A is (mono/bi)cyclic C2-9 heterocycloalkyl; R1 is H, amino, C1-6 alkyl-NH, OH, etc.; R2 is H, OH, carbamoyl, etc.; R3 is H, halo, NO2 and CN; R4, R10 and R11 are independently H, halo and C1-6 alkyl; R5, R6, R7, R8 and R9 are independently H, halo, amino, C1-6 alkoxycarbonyl-C1-6 alkoxy, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 2-chloro-4-((3-(2,3-difluoro-4-methoxyphenyl)imidazo[l,2-a]pyrazin-8-yl)amino)benzoic acid with 1-tert-Bu 2-Me piperazine-1,2-dicarboxylate; the resulting 1-tert-Bu 2-Me 4-[2-chloro-4-[[3-(2,3-difluoro-4-methoxy-phenyl)imidazo[1,2-a]pyrazin-8-yl]amino]benzoyl]piperazine-1,2-dicarboxylate underwent Boc-deprotection to give Me 4-[2-chloro-4-[[3-(2,3-difluoro-4-methoxy-phenyl)imidazo[1,2-a]pyrazin-8-yl]amino]benzoyl]piperazine-2-carboxylate, which underwent hydrolysis to give compound II. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 1.9μM. 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 imidazopyrazine preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ibis, Cemil; Ayla, Sibel Sahinler; Ozkok, Funda; Bahar, Hakan published an article in 2015, the title of the article was Synthesis of New Piperazinyl and Piperidinolyl Substituted p-Chloranil Derivatives and their Reactions with Thiols.Safety of 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

In continuation of previous studies of the nucleophilic substitution reactions of p-chloranil with nucleophiles, novel piperazinyl- and hydroxypiperidinyl-substituted quinones were synthesized. The N-substituted compounds were treated with some thiols and N,S-substituted compounds were obtained. The structures of new products were characterized by spectroscopic methods (1H NMR, 13C NMR, and MS) and elemental anal. 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 piperazinyl hydroxypiperidinyl chloranil derivative preparation thiol, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Safety of 4-(4-Chlorophenyl)piperidin-4-ol

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 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

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 September 14, 2017, Mainolfi, Nello; Moyer, Mikel P. published a patent.Electric Literature of 362703-57-9 The title of the patent was Indole-2-carboxamides as 3-phosphoglycerate dehydrogenase inhibitors and their preparation. And the patent contained the following:

The invention provides compoundsof formula I, compositions thereof, and methods of using the same. Compounds of formula I wherein R1 and R6 are independently H, C1-4 alkyl; R2 and R3 are independently halo, CN, (un)substituted C1-6 aliphatic, etc.; R4 is H, halo, CN, etc.; R8 os H, CO2H and derivs and (un)substituted C1-6 aliphatic group; R9 is H, halo and (un)substituted C1-4 alkyl; A is (un)saturated 3- to 8-membered carbocyclyl, (un)substituted 7- to 12-membered bicyclic carbocyclyl, (un)saturated 4- to 8-membered heterocyclyl, etc.; L1 is a bond and (un)branched C1-6 bivalent hydrocarbon chain wherein 1 to 5 methylene units may be replaced with O, CO, CO2, etc.; n is 0, 1, 2, 3, 4 and 5; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their PHGDH inhibitory activity (data given). The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Electric Literature of 362703-57-9

The Article related to indole carboxamide 3phosphoglycerate dehydrogenase inhibitor, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Electric Literature of 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On July 31, 1995, Nemeryuk, M. P.; Sedov, A. L.; Safonova, T. S.; Shvarts, G. Ya.; Faiermark, I. F.; Mashkovskii, M. D. published an article.COA of Formula: C9H13ClN4 The title of the article was Synthesis and pharmacological properties of 4(5)-substituted 5(4)-amidino-1,2,3-triazoles. And the article contained the following:

Title compounds I [R1 = R2 = Me; R1R2 = (CH2)5, (CH2)2O(CH2)2; R3 = Cl, MeO, PhCH2S, 3,4-Cl2C6H3CH2S] were prepared by diazotization of 4-(dialkylamino)-5-aminopyrimidines II in aqueous HCl. Triazole I [R1R2 = (CH2)2O(CH2)2; R3 = Cl] showed antihypertensive effect in rats at dose 10 mg/kg. It also showed low toxicity with LD50 > 1000 mg/kg. 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 amidinotriazole antihypertensive preparation, diazotization dialkylamino aminopyrimidine, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.COA of Formula: C9H13ClN4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On October 22, 2013, Miyamoto, Yukiko; Kalisiak, Jaroslaw; Korthals, Keith; Lauwaet, Tineke; Cheung, Dae Young; Lozano, Ricardo; Cobo, Eduardo R.; Upcroft, Peter; Upcroft, Jacqueline A.; Berg, Douglas E.; Gillin, Frances D.; Fokin, Valery V.; Sharpless, K. Barry; Eckmann, Lars published an article.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Expanded therapeutic potential in activity space of next-generation 5-nitroimidazole antimicrobials with broad structural diversity. And the article contained the following:

Metronidazole and other 5-nitroimidazoles (5-NI) are among the most effective antimicrobials available against many important anaerobic pathogens, but evolving resistance is threatening their long-term clin. utility. The common 5-NIs were developed decades ago, yet little 5-NI drug development has since taken place, leaving the true potential of this important drug class unexplored. Here we report on a unique approach to the modular synthesis of diversified 5-NIs for broad exploration of their antimicrobial potential. Many of the more than 650 synthesized compounds, carrying structurally diverse functional groups, have vastly improved activity against a range of microbes, including the pathogenic protozoa Giardia lamblia and Trichomonas vaginalis, and the bacterial pathogens Helicobacter pylori, Clostridium difficile, and Bacteroides fragilis. Furthermore, they can overcome different forms of drug resistance, and are active and nontoxic in animal infection models. These findings provide impetus to the development of structurally diverse, next-generation 5-NI drugs as agents in the antimicrobial armamentarium, thus ensuring their future viability as primary therapeutic agents against many clin. important infections. 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 nitroimidazole library preparation azide alkyne cycloaddition antimicrobial sar, antibiotics, infectious diseases, medicinal chemistry, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 8, 2017, Himmelsbach, Frank; Blum, Andreas; Peters, Stefan published a patent.HPLC of Formula: 1251006-64-0 The title of the patent was Preparation of 4-cyanobenzyl carbamimidoylcarbamate derivatives as AOC3 inhibitors. And the patent contained the following:

The invention relates to new benzonitrile derivatives I [R1 = H or halo; R2 = H or halo;R3 = H or halo (with the proviso that not more than one of R1-R3 is halo); A = II-IV, etc. (R4 = pyrrolidinyl, piperidinyl, piperazinyl; a CH2 group of the pyrrolidinyl, oxazolidinyl, piperidinyl or piperazinyl group of R4 is optionally replaced with a C(O) group)] or a pharmaceutically acceptable salt thereof, to their medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them. Over ninety compounds I were prepared E.g., a multi-step synthesis of compound V, starting from 4-bromo-2,5-difluoro-benzonitrile and 4-(piperazinyl)benzonitrile, was described. Exemplified compounds I were tested in the AOC3 assay (IC50 values given). The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).HPLC of Formula: 1251006-64-0

The Article related to cyanobenzyl carbamimidoylcarbamate aoc3 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 1251006-64-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On April 30, 2020, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Crews, Craig M.; Jaime-Figueroa, Saul; Dong, Hanqing; Qian, Yimin; Zimmermann, Kurt published a patent.HPLC of Formula: 1251006-64-0 The title of the patent was Bifunctional heterocycles, their use in targeted degradation of rapidly accelerated fibrosarcoma polypeptides and their preparation. And the patent contained the following:

The present disclosure relates bifunctional compounds of formula ULM-L-PTM, their use in modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein) and treatment of diseases that result from aggregation or accumulation of the target protein. and their preparation Compounds of formula ULM-L-PTM, wherein ULM is a small mol. E3 ubiquitin ligase binding moiety; PTM is a small mol. comprising a RAF protein targeting moiety; L is a bond or chem. linking moiety connecting ULM and PTM; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorph and prodrug thereof, are claimed. Compound I was prepared using a multistep procedure (procedure given). The present disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein (data given). The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).HPLC of Formula: 1251006-64-0

The Article related to bifunctional heterocycle preparation raf modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 1251006-64-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem