Tag: 126.1995

Jansen, Koen et al. published their research in MedChemComm in 2014 | CAS: 93643-24-4

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Application of 93643-24-4

Selective inhibitors of fibroblast activation protein (FAP) with a xanthine scaffold was written by Jansen, Koen;De Winter, Hans;Heirbaut, Leen;Cheng, Jonathan D.;Joossens, Jurgen;Lambeir, Anne-Marie;De Meester, Ingrid;Augustyns, Koen;Van der Veken, Pieter. And the article was included in MedChemComm in 2014.Application of 93643-24-4 This article mentions the following:

Fibroblast activation protein (FAP) is a serine protease that is selectively expressed in many diseases involving activated stroma, including cancer, arthritis and hepatic and pulmonary fibrosis. FAP is closely related to dipeptidyl peptidase IV (DPPIV), of which many inhibitors are known and several are marketed as drugs. One of these is the xanthine derivative linagliptin. In a broad literature screen amongst reported DPPIV inhibitors, linagliptin was the only druglike compound identified that possessed significant FAP potency. Hence, this compound served as a starting point for a SAR study that aimed to identify structural determinants that selectively increase FAP-potency of linagliptin analogs. By investigating the influence of the substitution pattern on N1, N7 and C8 of the xanthine scaffold, we managed to decouple DPPIV and FAP potency and identified the first selective xanthine-based FAP inhibitors with low micromolar potency. Furthermore, these compounds are the only known FAP-inhibitors that do not rely on a warhead functionality to obtain potencies in this range. In the experiment, the researchers used many compounds, for example, (S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4Application of 93643-24-4).

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Application of 93643-24-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Graneto, Matthew J. et al. published their research in Journal of Medicinal Chemistry in 2007 | CAS: 93643-24-4

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C7H14N2

Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase was written by Graneto, Matthew J.;Kurumbail, Ravi G.;Vazquez, Michael L.;Shieh, Huey-Sheng;Pawlitz, Jennifer L.;Williams, Jennifer M.;Stallings, William C.;Geng, Lifeng;Naraian, Ashok S.;Koszyk, Francis J.;Stealey, Michael A.;Xu, Xiangdong D.;Weier, Richard M.;Hanson, Gunnar J.;Mourey, Robert J.;Compton, Robert P.;Mnich, Stephen J.;Anderson, Gary D.;Monahan, Joseph B.;Devraj, Rajesh. And the article was included in Journal of Medicinal Chemistry in 2007.Synthetic Route of C7H14N2 This article mentions the following:

A series of pyrazole inhibitors of p38 mitogen-activated protein (MAP) kinase were designed using a binding model based on the crystal structure of SC-102 derivative bound to p38 enzyme. New chem. using dithietanes was developed to assemble nitrogen-linked substituents at the 5-position of pyrazoles. Calculated log D was used in tandem with structure-based design to guide medicinal chem. strategy and improve the in vivo activity of a series of mols. The crystal structure of an optimized inhibitor, I (SC-806), in complex with p38 enzyme was obtained to confirm the hypothesis that the addition of a basic nitrogen to the mol. induces an interaction with Asp112 of p38伪. A compound identified from this series was efficacious in an animal model of rheumatic disease. In the experiment, the researchers used many compounds, for example, (S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4Synthetic Route of C7H14N2).

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C7H14N2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Ding, Xiao et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2018 | CAS: 93643-24-4

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 93643-24-4

Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors was written by Ding, Xiao;Stasi, Luigi Piero;Ho, Ming-Hsun;Zhao, Baowei;Wang, Hailong;Long, Kai;Xu, Qiongfeng;Sang, Yingxia;Sun, Changhui;Hu, Huan;Yu, Haihua;Wan, Zehong;Wang, Lizhen;Edge, Colin;Liu, Qian;Li, Yi;Dong, Kelly;Guan, Xiaoming;Tattersall, F. David;Reith, Alastair D.;Ren, Feng. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2018.Product Details of 93643-24-4 This article mentions the following:

Inhibition of LRRK2 kinase activity with small mols. has emerged as a potential novel therapeutic treatment for Parkinson’s disease. Herein the authors disclose the discovery of a 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amine series as potent LRRK2 inhibitors identified through a kinase-focused set screening. Optimization of the physicochem. properties and kinase selectivity led to the discovery of compound 7 ((4-((4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone), which exhibited potent in vitro inhibition of LRRK2 kinase activity, good physicochem. properties and kinase selectivity across the kinome. Moreover, compound 7 was able to penetrate into the CNS, and in vivo pharmacol. studies revealed significant inhibition of Ser 935 phosphorylation in the brain of both rats (30 and 100 mg/kg) and mice (45 mg/kg) following oral administration. In the experiment, the researchers used many compounds, for example, (S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4Product Details of 93643-24-4).

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 93643-24-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Graneto, Matthew J. et al. published their research in Journal of Medicinal Chemistry in 2007 | CAS: 93643-24-4

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C7H14N2

Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase was written by Graneto, Matthew J.;Kurumbail, Ravi G.;Vazquez, Michael L.;Shieh, Huey-Sheng;Pawlitz, Jennifer L.;Williams, Jennifer M.;Stallings, William C.;Geng, Lifeng;Naraian, Ashok S.;Koszyk, Francis J.;Stealey, Michael A.;Xu, Xiangdong D.;Weier, Richard M.;Hanson, Gunnar J.;Mourey, Robert J.;Compton, Robert P.;Mnich, Stephen J.;Anderson, Gary D.;Monahan, Joseph B.;Devraj, Rajesh. And the article was included in Journal of Medicinal Chemistry in 2007.Synthetic Route of C7H14N2 This article mentions the following:

A series of pyrazole inhibitors of p38 mitogen-activated protein (MAP) kinase were designed using a binding model based on the crystal structure of SC-102 derivative bound to p38 enzyme. New chem. using dithietanes was developed to assemble nitrogen-linked substituents at the 5-position of pyrazoles. Calculated log D was used in tandem with structure-based design to guide medicinal chem. strategy and improve the in vivo activity of a series of mols. The crystal structure of an optimized inhibitor, I (SC-806), in complex with p38 enzyme was obtained to confirm the hypothesis that the addition of a basic nitrogen to the mol. induces an interaction with Asp112 of p38α. A compound identified from this series was efficacious in an animal model of rheumatic disease. In the experiment, the researchers used many compounds, for example, (S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4Synthetic Route of C7H14N2).

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C7H14N2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Ding, Xiao et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2018 | CAS: 93643-24-4

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 93643-24-4

Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors was written by Ding, Xiao;Stasi, Luigi Piero;Ho, Ming-Hsun;Zhao, Baowei;Wang, Hailong;Long, Kai;Xu, Qiongfeng;Sang, Yingxia;Sun, Changhui;Hu, Huan;Yu, Haihua;Wan, Zehong;Wang, Lizhen;Edge, Colin;Liu, Qian;Li, Yi;Dong, Kelly;Guan, Xiaoming;Tattersall, F. David;Reith, Alastair D.;Ren, Feng. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2018.Product Details of 93643-24-4 This article mentions the following:

Inhibition of LRRK2 kinase activity with small mols. has emerged as a potential novel therapeutic treatment for Parkinson’s disease. Herein the authors disclose the discovery of a 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amine series as potent LRRK2 inhibitors identified through a kinase-focused set screening. Optimization of the physicochem. properties and kinase selectivity led to the discovery of compound 7 ((4-((4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone), which exhibited potent in vitro inhibition of LRRK2 kinase activity, good physicochem. properties and kinase selectivity across the kinome. Moreover, compound 7 was able to penetrate into the CNS, and in vivo pharmacol. studies revealed significant inhibition of Ser 935 phosphorylation in the brain of both rats (30 and 100 mg/kg) and mice (45 mg/kg) following oral administration. In the experiment, the researchers used many compounds, for example, (S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4Product Details of 93643-24-4).

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 93643-24-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Graneto, Matthew J. et al. published their research in Journal of Medicinal Chemistry in 2007 | CAS: 93643-24-4

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C7H14N2

Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase was written by Graneto, Matthew J.;Kurumbail, Ravi G.;Vazquez, Michael L.;Shieh, Huey-Sheng;Pawlitz, Jennifer L.;Williams, Jennifer M.;Stallings, William C.;Geng, Lifeng;Naraian, Ashok S.;Koszyk, Francis J.;Stealey, Michael A.;Xu, Xiangdong D.;Weier, Richard M.;Hanson, Gunnar J.;Mourey, Robert J.;Compton, Robert P.;Mnich, Stephen J.;Anderson, Gary D.;Monahan, Joseph B.;Devraj, Rajesh. And the article was included in Journal of Medicinal Chemistry in 2007.Synthetic Route of C7H14N2 This article mentions the following:

A series of pyrazole inhibitors of p38 mitogen-activated protein (MAP) kinase were designed using a binding model based on the crystal structure of SC-102 derivative bound to p38 enzyme. New chem. using dithietanes was developed to assemble nitrogen-linked substituents at the 5-position of pyrazoles. Calculated log D was used in tandem with structure-based design to guide medicinal chem. strategy and improve the in vivo activity of a series of mols. The crystal structure of an optimized inhibitor, I (SC-806), in complex with p38 enzyme was obtained to confirm the hypothesis that the addition of a basic nitrogen to the mol. induces an interaction with Asp112 of p38α. A compound identified from this series was efficacious in an animal model of rheumatic disease. In the experiment, the researchers used many compounds, for example, (S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4Synthetic Route of C7H14N2).

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C7H14N2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Ding, Xiao et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2018 | CAS: 93643-24-4

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 93643-24-4

Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors was written by Ding, Xiao;Stasi, Luigi Piero;Ho, Ming-Hsun;Zhao, Baowei;Wang, Hailong;Long, Kai;Xu, Qiongfeng;Sang, Yingxia;Sun, Changhui;Hu, Huan;Yu, Haihua;Wan, Zehong;Wang, Lizhen;Edge, Colin;Liu, Qian;Li, Yi;Dong, Kelly;Guan, Xiaoming;Tattersall, F. David;Reith, Alastair D.;Ren, Feng. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2018.Product Details of 93643-24-4 This article mentions the following:

Inhibition of LRRK2 kinase activity with small mols. has emerged as a potential novel therapeutic treatment for Parkinson’s disease. Herein the authors disclose the discovery of a 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amine series as potent LRRK2 inhibitors identified through a kinase-focused set screening. Optimization of the physicochem. properties and kinase selectivity led to the discovery of compound 7 ((4-((4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone), which exhibited potent in vitro inhibition of LRRK2 kinase activity, good physicochem. properties and kinase selectivity across the kinome. Moreover, compound 7 was able to penetrate into the CNS, and in vivo pharmacol. studies revealed significant inhibition of Ser 935 phosphorylation in the brain of both rats (30 and 100 mg/kg) and mice (45 mg/kg) following oral administration. In the experiment, the researchers used many compounds, for example, (S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4Product Details of 93643-24-4).

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 93643-24-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics