Tag: 113.2007

Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable 纬-Secretase Modulator was written by Peng, Hairuo;Talreja, Tina;Xin, Zhili;Cuervo, J. Hernan;Kumaravel, Gnanasambandam;Humora, Michael J.;Xu, Lin;Rohde, Ellen;Gan, Lawrence;Jung, Mi-young;Shackett, Melanie N.;Chollate, Sowmya;Dunah, Anthone W.;Snodgrass-Belt, Pamela A.;Arnold, H. Moore;Taveras, Arthur G.;Rhodes, Kenneth J.;Scannevin, Robert H.. And the article was included in ACS Medicinal Chemistry Letters in 2011.Application of 4045-30-1 This article mentions the following:

We have investigated a novel series of acid-derived 纬-secretase modulators as a potential treatment of Alzheimer’s disease. Optimization based on cellular potency and brain pharmacodynamics after oral dosing led to the discovery of 10a (BIIB042). Compound 10a is a potent 纬-secretase modulator, which lowered A尾42, increased A尾38, but had little to no effect on A尾40 levels both in vitro and in vivo. In addition, compound 10a did not affect Notch signaling in our in vitro assessment. Compound 10a demonstrated excellent pharmacokinetic parameters in multiple species. Oral administration of 10a significantly reduced brain A尾42 levels in CF-1 mice and Fischer rats, as well as plasma A尾42 levels in cynomolgus monkeys. Compound 10a was selected as a candidate for preclin. safety evaluation. In the experiment, the researchers used many compounds, for example, 4,4-Dimethylpiperidine (cas: 4045-30-1Application of 4045-30-1).

4,4-Dimethylpiperidine (cas: 4045-30-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Application of 4045-30-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Quinazoline derivatives by cyclodehydrogenation of N-(2-substituted aryl)piperidines was written by Mohrle, H.;Jeandree, M.. And the article was included in Zeitschrift fuer Naturforschung, B: Chemical Sciences in 1999.SDS of cas: 4045-30-1 This article mentions the following:

Dehydrogenation of 2-piperidin-1-ylbenzamides using Hg(II)-EDTA yielded the corresponding quinazolinones. Increasing size of the 4-substituent in the piperidine decreased the oxidation rate and the product yield. 2-Piperidin-1-ylbenzaldehyde oximes showed a different behavior. While 2-piperidin-1-ylbenzaldehyde oxime with Hg(II)-EDTA in water produced 2-(2-oxopiperidin-1-yl)benzaldehyde oxime in quant. yield, with 4-substituted piperidines not only a lower reaction rate but also an altered product pattern was observed The double dehydrogenation to lactams was reduced and cyclic nitrones, formed by two electron withdrawal, became dominant. The mechanism of the reactions is discussed. In the experiment, the researchers used many compounds, for example, 4,4-Dimethylpiperidine (cas: 4045-30-1SDS of cas: 4045-30-1).

4,4-Dimethylpiperidine (cas: 4045-30-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.SDS of cas: 4045-30-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Preparation and atropisomerism of 1-(2-aryl)-piperidin-2-ones was written by Mohrle, H.;Jeandree, M.;Breitmaier, E.;Rohonczy, J.. And the article was included in Journal fuer Praktische Chemie (Weinheim, Germany) in 2000.Safety of 4,4-Dimethylpiperidine This article mentions the following:

Course and rate of the dehydrogenation of N-tertiary piperidines dependent on their substitution in 4-position and on the OH-bearing neighbor group were examined, using Hg(II)-EDTA and model piperidine-derived amino alcs. The results showed that increasing size of 4-substituents and neighbor groups too decreased the rate of reaction. The products from 2-substituted benzylic alcs., 2-piperidones demonstrated atropisomerism. In the case of chiral neighbor groups, diastereomeric mixtures were formed. In the experiment, the researchers used many compounds, for example, 4,4-Dimethylpiperidine (cas: 4045-30-1Safety of 4,4-Dimethylpiperidine).

4,4-Dimethylpiperidine (cas: 4045-30-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Safety of 4,4-Dimethylpiperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable γ-Secretase Modulator was written by Peng, Hairuo;Talreja, Tina;Xin, Zhili;Cuervo, J. Hernan;Kumaravel, Gnanasambandam;Humora, Michael J.;Xu, Lin;Rohde, Ellen;Gan, Lawrence;Jung, Mi-young;Shackett, Melanie N.;Chollate, Sowmya;Dunah, Anthone W.;Snodgrass-Belt, Pamela A.;Arnold, H. Moore;Taveras, Arthur G.;Rhodes, Kenneth J.;Scannevin, Robert H.. And the article was included in ACS Medicinal Chemistry Letters in 2011.Application of 4045-30-1 This article mentions the following:

We have investigated a novel series of acid-derived γ-secretase modulators as a potential treatment of Alzheimer’s disease. Optimization based on cellular potency and brain pharmacodynamics after oral dosing led to the discovery of 10a (BIIB042). Compound 10a is a potent γ-secretase modulator, which lowered Aβ42, increased Aβ38, but had little to no effect on Aβ40 levels both in vitro and in vivo. In addition, compound 10a did not affect Notch signaling in our in vitro assessment. Compound 10a demonstrated excellent pharmacokinetic parameters in multiple species. Oral administration of 10a significantly reduced brain Aβ42 levels in CF-1 mice and Fischer rats, as well as plasma Aβ42 levels in cynomolgus monkeys. Compound 10a was selected as a candidate for preclin. safety evaluation. In the experiment, the researchers used many compounds, for example, 4,4-Dimethylpiperidine (cas: 4045-30-1Application of 4045-30-1).

4,4-Dimethylpiperidine (cas: 4045-30-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Application of 4045-30-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Quinazoline derivatives by cyclodehydrogenation of N-(2-substituted aryl)piperidines was written by Mohrle, H.;Jeandree, M.. And the article was included in Zeitschrift fuer Naturforschung, B: Chemical Sciences in 1999.SDS of cas: 4045-30-1 This article mentions the following:

Dehydrogenation of 2-piperidin-1-ylbenzamides using Hg(II)-EDTA yielded the corresponding quinazolinones. Increasing size of the 4-substituent in the piperidine decreased the oxidation rate and the product yield. 2-Piperidin-1-ylbenzaldehyde oximes showed a different behavior. While 2-piperidin-1-ylbenzaldehyde oxime with Hg(II)-EDTA in water produced 2-(2-oxopiperidin-1-yl)benzaldehyde oxime in quant. yield, with 4-substituted piperidines not only a lower reaction rate but also an altered product pattern was observed The double dehydrogenation to lactams was reduced and cyclic nitrones, formed by two electron withdrawal, became dominant. The mechanism of the reactions is discussed. In the experiment, the researchers used many compounds, for example, 4,4-Dimethylpiperidine (cas: 4045-30-1SDS of cas: 4045-30-1).

4,4-Dimethylpiperidine (cas: 4045-30-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.SDS of cas: 4045-30-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Preparation and atropisomerism of 1-(2-aryl)-piperidin-2-ones was written by Mohrle, H.;Jeandree, M.;Breitmaier, E.;Rohonczy, J.. And the article was included in Journal fuer Praktische Chemie (Weinheim, Germany) in 2000.Safety of 4,4-Dimethylpiperidine This article mentions the following:

Course and rate of the dehydrogenation of N-tertiary piperidines dependent on their substitution in 4-position and on the OH-bearing neighbor group were examined, using Hg(II)-EDTA and model piperidine-derived amino alcs. The results showed that increasing size of 4-substituents and neighbor groups too decreased the rate of reaction. The products from 2-substituted benzylic alcs., 2-piperidones demonstrated atropisomerism. In the case of chiral neighbor groups, diastereomeric mixtures were formed. In the experiment, the researchers used many compounds, for example, 4,4-Dimethylpiperidine (cas: 4045-30-1Safety of 4,4-Dimethylpiperidine).

4,4-Dimethylpiperidine (cas: 4045-30-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Safety of 4,4-Dimethylpiperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable γ-Secretase Modulator was written by Peng, Hairuo;Talreja, Tina;Xin, Zhili;Cuervo, J. Hernan;Kumaravel, Gnanasambandam;Humora, Michael J.;Xu, Lin;Rohde, Ellen;Gan, Lawrence;Jung, Mi-young;Shackett, Melanie N.;Chollate, Sowmya;Dunah, Anthone W.;Snodgrass-Belt, Pamela A.;Arnold, H. Moore;Taveras, Arthur G.;Rhodes, Kenneth J.;Scannevin, Robert H.. And the article was included in ACS Medicinal Chemistry Letters in 2011.Application of 4045-30-1 This article mentions the following:

We have investigated a novel series of acid-derived γ-secretase modulators as a potential treatment of Alzheimer’s disease. Optimization based on cellular potency and brain pharmacodynamics after oral dosing led to the discovery of 10a (BIIB042). Compound 10a is a potent γ-secretase modulator, which lowered Aβ42, increased Aβ38, but had little to no effect on Aβ40 levels both in vitro and in vivo. In addition, compound 10a did not affect Notch signaling in our in vitro assessment. Compound 10a demonstrated excellent pharmacokinetic parameters in multiple species. Oral administration of 10a significantly reduced brain Aβ42 levels in CF-1 mice and Fischer rats, as well as plasma Aβ42 levels in cynomolgus monkeys. Compound 10a was selected as a candidate for preclin. safety evaluation. In the experiment, the researchers used many compounds, for example, 4,4-Dimethylpiperidine (cas: 4045-30-1Application of 4045-30-1).

4,4-Dimethylpiperidine (cas: 4045-30-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Application of 4045-30-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Quinazoline derivatives by cyclodehydrogenation of N-(2-substituted aryl)piperidines was written by Mohrle, H.;Jeandree, M.. And the article was included in Zeitschrift fuer Naturforschung, B: Chemical Sciences in 1999.SDS of cas: 4045-30-1 This article mentions the following:

Dehydrogenation of 2-piperidin-1-ylbenzamides using Hg(II)-EDTA yielded the corresponding quinazolinones. Increasing size of the 4-substituent in the piperidine decreased the oxidation rate and the product yield. 2-Piperidin-1-ylbenzaldehyde oximes showed a different behavior. While 2-piperidin-1-ylbenzaldehyde oxime with Hg(II)-EDTA in water produced 2-(2-oxopiperidin-1-yl)benzaldehyde oxime in quant. yield, with 4-substituted piperidines not only a lower reaction rate but also an altered product pattern was observed The double dehydrogenation to lactams was reduced and cyclic nitrones, formed by two electron withdrawal, became dominant. The mechanism of the reactions is discussed. In the experiment, the researchers used many compounds, for example, 4,4-Dimethylpiperidine (cas: 4045-30-1SDS of cas: 4045-30-1).

4,4-Dimethylpiperidine (cas: 4045-30-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.SDS of cas: 4045-30-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Preparation and atropisomerism of 1-(2-aryl)-piperidin-2-ones was written by Mohrle, H.;Jeandree, M.;Breitmaier, E.;Rohonczy, J.. And the article was included in Journal fuer Praktische Chemie (Weinheim, Germany) in 2000.Safety of 4,4-Dimethylpiperidine This article mentions the following:

Course and rate of the dehydrogenation of N-tertiary piperidines dependent on their substitution in 4-position and on the OH-bearing neighbor group were examined, using Hg(II)-EDTA and model piperidine-derived amino alcs. The results showed that increasing size of 4-substituents and neighbor groups too decreased the rate of reaction. The products from 2-substituted benzylic alcs., 2-piperidones demonstrated atropisomerism. In the case of chiral neighbor groups, diastereomeric mixtures were formed. In the experiment, the researchers used many compounds, for example, 4,4-Dimethylpiperidine (cas: 4045-30-1Safety of 4,4-Dimethylpiperidine).

4,4-Dimethylpiperidine (cas: 4045-30-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Safety of 4,4-Dimethylpiperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem