Category: 126832-81-3

HPLC of Formula: 126832-81-3On May 19, 2005 ,《Synthesis and Structure-Activity Relationships of Novel Selective Factor Xa Inhibitors with a Tetrahydroisoquinoline Ring》 appeared in Journal of Medicinal Chemistry. The author of the article were Ueno, Hiroshi; Yokota, Katsuyuki; Hoshi, Jun-Ichi; Yasue, Katsutaka; Hayashi, Mikio; Hase, Yasunori; Uchida, Itsuo; Aisaka, Kazuo; Katoh, Susumu; Cho, Hidetsura. The article conveys some information:

A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds I.2HCl and I.MsOH exhibited potent inhibitory activity against factor Xa (FXa) and good selectivity with respect to other serine proteases (thrombin, plasmin, and trypsin). In addition, I.MsOH exhibited potent anti-FXa activity after i.v. and oral administration to cynomolgus monkeys, showed a dose-dependent antithrombotic effect at 0.1, 0.3, and 1 mg kg-1 h-1 in a rat model of venous thrombosis, and significantly reduced the size of brain infarction in a middle cerebral artery occlusion model at a dose of 0.1 mg kg-1 h-1. These results suggest that I.MsOH (JTV-803) is likely to be useful as both a venous and arterial antithrombotic agent. The results came from multiple reactions, including the reaction of 1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3HPLC of Formula: 126832-81-3)

1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. HPLC of Formula: 126832-81-3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Application of 126832-81-3On March 1, 2008, Imaeda, Yasuhiro; Miyawaki, Toshio; Sakamoto, Hiroki; Itoh, Fumio; Konishi, Noriko; Hiroe, Katsuhiko; Kawamura, Masaki; Tanaka, Toshimasa; Kubo, Keiji published an article in Bioorganic & Medicinal Chemistry. The article was 《Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors》. The article mentions the following:

Factor Xa (FXa) is a trypsin-like serine protease involved in the coagulation cascade and has received great interest as a potential target for the development of new antithrombotic agents. Most of amidine-type FXa inhibitors reported have been found to show extremely poor oral bioavailability. I is one of the first reported non-amidine type FXa inhibitors. To discover novel and orally active FXa inhibitors, we investigated flexible linear linkers between the 6-chloronaphthalene ring and the 1-(pyridin-4-yl)piperidine moiety of I and found an orally active sulfonylalkylamide with an FXa IC50 of 0.05 μM, comparable with that of I. Further modification to reduce the CYP3A4 inhibitory activity of the sulfonylalkylamide resulted in a potent, selective, and orally active 2-methylpyridine analog (FXa IC50 of 0.061 μM), for which the liability of CYP3A4 inhibition was significantly weakened compared to the sulfonylalkylamide. the 2-methylpyridine sulfonylalkylamide analog also showed long lasting anticoagulant activity in cynomolgus monkeys. The experimental part of the paper was very detailed, including the reaction process of 1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3Application of 126832-81-3)

1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. Application of 126832-81-3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ishihara, Tsukasa; Seki, Norio; Hirayama, Fukushi; Orita, Masaya; Koshio, Hiroyuki; Taniuchi, Yuta; Sakai-Moritani, Yumiko; Iwatsuki, Yoshiyuki; Kaku, Seiji; Kawasaki, Tomihisa; Matsumoto, Yuzo; Tsukamoto, Shin-ichi published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors》.HPLC of Formula: 126832-81-3 The author mentioned the following in the article:

We describe here our investigation of a new series of orally active fXa inhibitors based on a prodrug strategy. Solid-phase parallel synthesis identified a unique series of fXa inhibitors with a substituted benzenesulfonyl group as a novel S4 binding element. This series resulted in compound 39 (I), which exhibited potent inhibitory activity against fXa (IC50 = 13 nM) and excellent selectivity over thrombin (>7000-fold). The masking of its highly hydrophilic groups led to the creation of related prodrug 28, which demonstrated an anticoagulant effect after oral dosing. In addition to this study using 1-Pyridin-4-ylpiperidin-4-one, there are many other studies that have used 1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3HPLC of Formula: 126832-81-3) was used in this study.

1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. HPLC of Formula: 126832-81-3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Related Products of 126832-81-3On October 20, 2017 ,《Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation》 was published in European Journal of Medicinal Chemistry. The article was written by Wang, Zhengyu; Shi, Xiaofan; Zhang, Huan; Yu, Liang; Cheng, Yanhua; Zhang, Hefeng; Zhang, Huibin; Zhou, Jinpei; Chen, Jing; Shen, Xu; Duan, Wenhu. The article contains the following contents:

Glucokinase (GK) activators are being developed for the treatment of type 2 diabetes mellitus (T2DM). However, existing GK activators have risks of hypoglycemia caused by over-activation of GK in islet cells and dyslipidemia caused by over-activation of intrahepatic GK. In the effort to mitigate risks of hypoglycemia and dyslipidemia while maintaining the promising efficacy of GK activator, the authors investigated a series of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific partial GK activators. This led to the identification of compound 72 (tert-Bu(S)-2-(3-(4-(azetidine-1-carbonyl)phenoxy)-5-((1-methoxypropan-2-yl)oxy)benzamido)-6,7-dihydrothiazolo[5,4-c]pyridine-5(4H)-carboxylate) that showed a good balance between in vitro potency and enzyme kinetic parameters. Compound 72 also protected β-cells from streptozotocin-induced apoptosis. Chronic treatment of compound 72 demonstrated its potent activity in regulation of glucose homeostasis and low risk of dyslipidemia with diabetic db/db mice in oral glucose tolerance test (OGTT). Moreover, acute treatment of compound 72 did not induce hypoglycemia in C57BL/6J mice even at 200 mg/kg via oral administration. The results came from multiple reactions, including the reaction of 1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3Related Products of 126832-81-3)

1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. Related Products of 126832-81-3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Computed Properties of C10H12N2OOn October 31, 1994 ,《Synthesis of 3,5-lutidine by catalytic transfer hydrogenation via 1,2,5,6-tetrahydropyridine》 was published in Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry. The article was written by Sathe, Dhananjay G.; Kulkarni, Vithal M.. The article contains the following contents:

Substituted pyridines, e.g. 3,5-lutidine, have been prepared from the corresponding N-benzyl-1,2,5,6-tetrahydropyridines by catalytic transfer hydrogenation in one stage. A mechanism for such a catalytic transfer hydrogenation (CTH) has been proposed. In the experiment, the researchers used 1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3Computed Properties of C10H12N2O)

1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. Computed Properties of C10H12N2O

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Application of 126832-81-3On October 31, 1994 ,《Synthesis of 3,5-lutidine by catalytic transfer hydrogenation via 1,2,5,6-tetrahydropyridine》 was published in Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry. The article was written by Sathe, Dhananjay G.; Kulkarni, Vithal M.. The article contains the following contents:

Substituted pyridines, e.g. 3,5-lutidine, have been prepared from the corresponding N-benzyl-1,2,5,6-tetrahydropyridines by catalytic transfer hydrogenation in one stage. A mechanism for such a catalytic transfer hydrogenation (CTH) has been proposed. In the experiment, the researchers used 1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3Application of 126832-81-3)

1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. Application of 126832-81-3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem