Category: 109384-19-2

《Discovery of Potent, Selective, and Orally Bioavailable Inhibitors of USP7 with In Vivo Antitumor Activity》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Leger, Paul R.; Hu, Dennis X.; Biannic, Berenger; Bui, Minna; Han, Xinping; Karbarz, Emily; Maung, Jack; Okano, Akinori; Osipov, Maksim; Shibuya, Grant M.; Young, Kyle; Higgs, Christopher; Abraham, Betty; Bradford, Delia; Cho, Cynthia; Colas, Christophe; Jacobson, Scott; Ohol, Yamini M.; Pookot, Deepa; Rana, Payal; Sanchez, Jerick; Shah, Niket; Sun, Michael; Wong, Steve; Brockstedt, Dirk G.; Kassner, Paul D.; Schwarz, Jacob B.; Wustrow, David J.. Safety of tert-Butyl 4-hydroxypiperidine-1-carboxylate The article mentions the following:

USP7 is a promising target for cancer therapy as its inhibition is expected to decrease function of oncogenes, increase tumor suppressor function, and enhance immune function. Using a structure-based drug design strategy, a new class of reversible USP7 inhibitors has been identified that is highly potent in biochem. and cellular assays and extremely selective for USP7 over other deubiquitinases. The succinimide was identified as a key potency-driving motif, forming two strong hydrogen bonds to the allosteric pocket of USP7. Redesign of an initial benzofuran-amide scaffold yielded a simplified ether series of inhibitors, utilizing acyclic conformational control to achieve proper amine placement. Further improvements were realized upon replacing the ether-linked amines with carbon-linked morpholines, a modification motivated by free energy perturbation (FEP+) calculations This led to the discovery of compound 41(I), a highly potent, selective, and orally bioavailable USP7 inhibitor. In xenograft studies, compound 41 demonstrated tumor growth inhibition in both p53 wildtype and p53 mutant cancer cell lines, demonstrating that USP7 inhibitors can suppress tumor growth through multiple different pathways.tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Safety of tert-Butyl 4-hydroxypiperidine-1-carboxylate) was used in this study.

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Safety of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Catalytic Transfer Hydrogenation of Arenes and Heteroarenes》 was published in Chemistry – A European Journal in 2020. These research results belong to Gelis, Coralie; Heusler, Arne; Nairoukh, Zackaria; Glorius, Frank. Category: piperidines The article mentions the following:

Transfer hydrogenation reactions are of great interest to reduce diverse mols. under mild reaction conditions. To date, this type of reaction has only been successfully applied to alkenes, alkynes and polarized unsaturated compounds such as ketones, imines, pyridines, etc. The reduction of benzene derivatives by transfer hydrogenation has never been described, which is likely due to the high energy barrier required to dearomatize these compounds In this context, a catalytic transfer hydrogenation reaction for the reduction of benzene derivatives and heteroarenes to form complex 3-dimensional scaffolds bearing various functional groups at room temperature without needing compressed hydrogen gas has been developed. In the experiment, the researchers used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Category: piperidines)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Highly Selective Sub-Nanomolar Cathepsin S Inhibitors by Merging Fragment Binders with Nitrile Inhibitors》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Schade, Markus; Merla, Beatrix; Lesch, Bernhard; Wagener, Markus; Timmermanns, Simone; Pletinckx, Katrien; Hertrampf, Torsten. Computed Properties of C10H19NO3 The article mentions the following:

Pharmacol. inhibition of cathepsin S (CatS) allows for a specific modulation of the adaptive immune system and many major diseases. Here, we used NMR fragment screening and crystal structure-aided merging to synthesize novel, highly selective CatS inhibitors with picomolar enzymic Ki values and nanomolar functional activity in human Raji cells. Noncovalent fragment hits revealed binding hotspots, while the covalent inhibitor structure-activity relationship enabled efficient potency optimization. In addition to this study using tert-Butyl 4-hydroxypiperidine-1-carboxylate, there are many other studies that have used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Computed Properties of C10H19NO3) was used in this study.

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Computed Properties of C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zhang, Zhuming; Connolly, Peter J.; Lim, Heng Keang; Pande, Vineet; Meerpoel, Lieven; Teleha, Christopher; Branch, Jonathan R.; Ondrus, Janine; Hickson, Ian; Bush, Tammy; Luistro, Leopoldo; Packman, Kathryn; Bischoff, James R.; Ibrahim, Salam; Parrett, Christopher; Chong, Yolanda; Gottardis, Marco M.; Bignan, Gilles published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC)》.Related Products of 109384-19-2 The article contains the following contents:

Persistent androgen receptor (AR) activation drives therapeutic resistance to second-generation AR pathway inhibitors and contributes to the progression of advanced prostate cancer. One resistance mechanism is point mutations in the ligand binding domain of AR that can transform antagonists into agonists. The AR F877L mutation, identified in patients treated with enzalutamide or apalutamide, confers resistance to both enzalutamide and apalutamide. Compound 4 (JNJ-pan-AR) was identified as a pan-AR antagonist with potent activity against wild-type and clin. relevant AR mutations including F877L. Metabolite identification studies revealed a latent bioactivation pathway associated with 4. Subsequent lead optimization of 4 led to amelioration of this pathway and nomination of 5 (JNJ-63576253) as a clin. stage, next-generation AR antagonist for the treatment of castration-resistant prostate cancer (CRPC). The results came from multiple reactions, including the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Related Products of 109384-19-2)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Related Products of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Amine-Responsive Disassembly of AuI-CuI Double Salts for Oxidative Carbonylation》 was published in Angewandte Chemie, International Edition in 2020. These research results belong to Cao, Yanwei; Yang, Jian-Gong; Deng, Yi; Wang, Shengchun; Liu, Qi; Shen, Chaoren; Lu, Wei; Che, Chi-Ming; Chen, Yong; He, Lin. Application In Synthesis of tert-Butyl 4-hydroxypiperidine-1-carboxylate The article mentions the following:

A sensitive amine-responsive disassembly of self-assembled AuI-CuI double salts was observed and its use for the synergistic catalysis was enlightened. Study of the disassembly of [Au(NHC)2][CuI2] revealed the contribution of Cu-assisted ligand exchange of N-heterocyclic carbene (NHC) by amine in [Au(NHC)2]+ and the capacity of [CuI2]- on the oxidative step. By integrating the implicative information coded in the responsive behavior and inherent catalytic functions of d10 metal complexes, a catalyst for the oxidative carbonylation of amines was developed. The advantages of this method were clearly reflected on mild reaction conditions and the significantly expanded scope (51 examples); both primary and steric secondary amines can be employed as substrates. The cooperative reactivity from Au and Cu centers, as an indispensable prerequisite for the excellent catalytic performance, was validated in the synthesis of (un)sym. ureas and carbamates. The results came from multiple reactions, including the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Application In Synthesis of tert-Butyl 4-hydroxypiperidine-1-carboxylate)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Application In Synthesis of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Luo, Guoshun; Lin, Xin; Li, Zhenbang; Xiao, Maoxu; Li, Xinyu; Zhang, Dayong; Xiang, Hua published an article in 2021. The article was titled 《Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator》, and you may find the article in European Journal of Medicinal Chemistry.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate The information in the text is summarized as follows:

Farnesoid X receptor (FXR) agonists are emerging as potential therapeutics for the treatment of various metabolic diseases, as they display multiple effects on bile acid, lipid, and glucose homeostasis. Although the steroidal obeticholic acid, a full FXR agonist, was recently approved, several side effects probably due to insufficient pharmacol. selectivity impede its further clin. application. Activating FXR in a partial manner is therefore crucial in the development of novel FXR modulators. Our efforts focusing on isoxazole-type FXR agonists, common nonsteroidal agonists for FXR, led to the discovery a series of novel FXR agonists bearing aryl urea moieties through structural simplification of LJN452 (phase 2). Encouragingly, compound I was discovered as a potent FXR agonist which exhibited similar FXR agonism potency but lower maximum efficacy compared to full agonists GW4064 and LJN452 in cell-based FXR transactivation assay. Extensive in vitro evaluation further confirmed partial efficacy of I in cellular FXR-dependent gene modulation, and revealed its lipid-reducing activity. More importantly, orally administration of I in mice exhibited desirable pharmacokinetic characters resulting in promising in vivo FXR agonistic activity. The results came from multiple reactions, including the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Huang, Mingming; Hu, Jiefeng; Krummenacher, Ivo; Friedrich, Alexandra; Braunschweig, Holger; Westcott, Stephen A.; Radius, Udo; Marder, Todd B. published an article in Chemistry – A European Journal. The title of the article was 《Base-Mediated Radical Borylation of Alkyl Sulfones》.Reference of tert-Butyl 4-hydroxypiperidine-1-carboxylate The author mentioned the following in the article:

A practical and direct method was developed for the production of versatile alkyl boronate esters via transition metal-free borylation of primary and secondary alkyl sulfones. The key to the success of the strategy is the use of bis(neopentyl glycolato) diboron (B2neop2), with a stoichiometric amount of base as a promoter. The practicality and industrial potential of this protocol are highlighted by its wide functional group tolerance, the late-stage modification of complex compounds, no need for further transesterification, and operational simplicity. Radical clock, radical trap experiments, and EPR studies were conducted which show that the borylation process involves radical intermediates. In the experiment, the researchers used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Reference of tert-Butyl 4-hydroxypiperidine-1-carboxylate)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Reference of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zhang, Zhuming; Connolly, Peter J.; Trabalon Escolar, Luis; Rocaboy, Christian; Pande, Vineet; Meerpoel, Lieven; Lim, Heng-Keang; Branch, Jonathan R.; Ondrus, Janine; Hickson, Ian; Bush, Tammy L.; Bischoff, James R.; Bignan, Gilles published their research in ACS Medicinal Chemistry Letters in 2021. The article was titled 《Spirocyclic Thiohydantoin Antagonists of F877L and Wild-Type Androgen Receptor for Castration-Resistant Prostate Cancer》.Formula: C10H19NO3 The article contains the following contents:

Androgen receptor (AR) transcriptional reactivation plays a key role in the development and progression of lethal castration-resistant prostate cancer (CRPC). Recurrent alterations in the AR enable persistent AR pathway signaling and drive resistance to the treatment of second-generation antiandrogens. AR F877L, a point mutation in the ligand binding domain of the AR, was identified in patients who acquired resistance to enzalutamide or apalutamide. In parallel to our previous structure-activity relationship (SAR) studies of compound 4 (JNJ-pan-AR) and clin. stage compound 5 (JNJ-63576253), we discovered addnl. AR antagonists that provide opportunities for future development. Here we report a highly potent series of spirocyclic thiohydantoins as AR antagonists for the treatment of the F877L mutant and wild-type CRPC. A chirally pure enantiomer,(R)-29 (I) is a full antagonist against AR F877L. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Formula: C10H19NO3)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Formula: C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Yang, Xiao-Guang; Du, Feng-Huan; Li, Jun-Jie; Zhang, Chi published an article in 2022. The article was titled 《Late-Stage Dehydroxyazidation of Alcohols Promoted by Trifunctional Hypervalent Azido-Iodine(III) Reagents》, and you may find the article in Chemistry – A European Journal.Related Products of 109384-19-2 The information in the text is summarized as follows:

A practical method for dehydroxyazidation of alcs. via an SN2 pathway involving PPh3 and trifunctional benziodazolone-based hypervalent azido-iodine(III) reagents, which function as an electrophilic center, an azido source and a base was reported. This mild, chemoselective method was used for late-stage azidation of structurally complex alcs., as well as for a new synthetic route to the antiepileptic drug rufinamide. The reaction mechanism was also investigated both exptl. and computationally. The experimental process involved the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Related Products of 109384-19-2)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Related Products of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models》 was written by Romussi, Alessia; Cappa, Anna; Vianello, Paola; Brambillasca, Silvia; Cera, Maria Rosaria; Dal Zuffo, Roberto; Faga, Giovanni; Fattori, Raimondo; Moretti, Loris; Trifiro, Paolo; Villa, Manuela; Vultaggio, Stefania; Cecatiello, Valentina; Pasqualato, Sebastiano; Dondio, Giulio; So, Chi Wai Eric; Minucci, Saverio; Sartori, Luca; Varasi, Mario; Mercurio, Ciro. HPLC of Formula: 109384-19-2 And the article was included in ACS Medicinal Chemistry Letters in 2020. The article conveys some information:

Lysine-specific demethylase 1 (LSD1 or KDM1A) is a FAD-dependent enzyme that acts as a transcription corepressor or coactivator by regulating the methylation status of histone H3 lysines K4 and K9, resp. KDM1A represents an attractive target for cancer therapy. While, in the past, the main medicinal chem. strategy toward KDM1A inhibition was based on the optimization of ligands that irreversibly bind the FAD cofactor within the enzyme catalytic site, we and others have also identified reversible inhibitors. Herein we reported the discovery of 5-imidazolylthieno[3,2-b]pyrroles, a new series of KDM1A inhibitors endowed with picomolar inhibitory potency, active in cells and efficacious after oral administration in murine leukemia models. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2HPLC of Formula: 109384-19-2)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.HPLC of Formula: 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem