The Experts below are selected from a list of 135 Experts worldwide ranked by ideXlab platform
Martin L Neitzel - One of the best experts on this subject based on the ideXlab platform.
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discovery of r 4 cyclopropyl 7 8 difluoro 5 4 trifluoromethyl phenylsulfonyl 4 5 dihydro 1h pyrazolo 4 3 c quinoline elnd006 and r 4 cyclopropyl 8 fluoro 5 6 trifluoromethyl pyridin 3 ylsulfonyl 4 5 dihydro 2h pyrazolo 4 3 c quinoline elnd007 metabol
Journal of Medicinal Chemistry, 2013Co-Authors: Gary Probst, Danielle L Aubele, Simeon Bowers, Darren B Dressen, Albert W Garofalo, Roy K Hom, Andrei W Konradi, Jennifer Marugg, Matthew N Mattson, Martin L NeitzelAbstract:Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006) and 34 (ELND007) both entered human clinical trials. The in vitro and in vivo characteristics for these two compounds are described. A comparison of inhibition of Aβ generation in vivo between 30, 34, Semagacestat 41, Begacestat 42, and Avagacestat 43 in mice is made. 30 lowered Aβ in the CSF of healthy human volunteers.
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Discovery of (R)‑4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro‑1H‑pyrazolo[4,3‑c]quinoline (ELND006) and (R)‑4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro‑2H‑pyrazolo[4,3‑c]quinoline (EL
2013Co-Authors: Gary Probst, Danielle L Aubele, Simeon Bowers, Darren B Dressen, Albert W Garofalo, Roy K Hom, Andrei W Konradi, Jennifer Marugg, Matthew N Mattson, Martin L NeitzelAbstract:Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006) and 34 (ELND007) both entered human clinical trials. The in vitro and in vivo characteristics for these two compounds are described. A comparison of inhibition of Aβ generation in vivo between 30, 34, Semagacestat 41, Begacestat 42, and Avagacestat 43 in mice is made. 30 lowered Aβ in the CSF of healthy human volunteers
Gary Probst - One of the best experts on this subject based on the ideXlab platform.
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discovery of r 4 cyclopropyl 7 8 difluoro 5 4 trifluoromethyl phenylsulfonyl 4 5 dihydro 1h pyrazolo 4 3 c quinoline elnd006 and r 4 cyclopropyl 8 fluoro 5 6 trifluoromethyl pyridin 3 ylsulfonyl 4 5 dihydro 2h pyrazolo 4 3 c quinoline elnd007 metabol
Journal of Medicinal Chemistry, 2013Co-Authors: Gary Probst, Danielle L Aubele, Simeon Bowers, Darren B Dressen, Albert W Garofalo, Roy K Hom, Andrei W Konradi, Jennifer Marugg, Matthew N Mattson, Martin L NeitzelAbstract:Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006) and 34 (ELND007) both entered human clinical trials. The in vitro and in vivo characteristics for these two compounds are described. A comparison of inhibition of Aβ generation in vivo between 30, 34, Semagacestat 41, Begacestat 42, and Avagacestat 43 in mice is made. 30 lowered Aβ in the CSF of healthy human volunteers.
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Discovery of (R)‑4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro‑1H‑pyrazolo[4,3‑c]quinoline (ELND006) and (R)‑4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro‑2H‑pyrazolo[4,3‑c]quinoline (EL
2013Co-Authors: Gary Probst, Danielle L Aubele, Simeon Bowers, Darren B Dressen, Albert W Garofalo, Roy K Hom, Andrei W Konradi, Jennifer Marugg, Matthew N Mattson, Martin L NeitzelAbstract:Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006) and 34 (ELND007) both entered human clinical trials. The in vitro and in vivo characteristics for these two compounds are described. A comparison of inhibition of Aβ generation in vivo between 30, 34, Semagacestat 41, Begacestat 42, and Avagacestat 43 in mice is made. 30 lowered Aβ in the CSF of healthy human volunteers
Andrei W Konradi - One of the best experts on this subject based on the ideXlab platform.
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discovery of r 4 cyclopropyl 7 8 difluoro 5 4 trifluoromethyl phenylsulfonyl 4 5 dihydro 1h pyrazolo 4 3 c quinoline elnd006 and r 4 cyclopropyl 8 fluoro 5 6 trifluoromethyl pyridin 3 ylsulfonyl 4 5 dihydro 2h pyrazolo 4 3 c quinoline elnd007 metabol
Journal of Medicinal Chemistry, 2013Co-Authors: Gary Probst, Danielle L Aubele, Simeon Bowers, Darren B Dressen, Albert W Garofalo, Roy K Hom, Andrei W Konradi, Jennifer Marugg, Matthew N Mattson, Martin L NeitzelAbstract:Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006) and 34 (ELND007) both entered human clinical trials. The in vitro and in vivo characteristics for these two compounds are described. A comparison of inhibition of Aβ generation in vivo between 30, 34, Semagacestat 41, Begacestat 42, and Avagacestat 43 in mice is made. 30 lowered Aβ in the CSF of healthy human volunteers.
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Discovery of (R)‑4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro‑1H‑pyrazolo[4,3‑c]quinoline (ELND006) and (R)‑4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro‑2H‑pyrazolo[4,3‑c]quinoline (EL
2013Co-Authors: Gary Probst, Danielle L Aubele, Simeon Bowers, Darren B Dressen, Albert W Garofalo, Roy K Hom, Andrei W Konradi, Jennifer Marugg, Matthew N Mattson, Martin L NeitzelAbstract:Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006) and 34 (ELND007) both entered human clinical trials. The in vitro and in vivo characteristics for these two compounds are described. A comparison of inhibition of Aβ generation in vivo between 30, 34, Semagacestat 41, Begacestat 42, and Avagacestat 43 in mice is made. 30 lowered Aβ in the CSF of healthy human volunteers
Danielle L Aubele - One of the best experts on this subject based on the ideXlab platform.
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discovery of r 4 cyclopropyl 7 8 difluoro 5 4 trifluoromethyl phenylsulfonyl 4 5 dihydro 1h pyrazolo 4 3 c quinoline elnd006 and r 4 cyclopropyl 8 fluoro 5 6 trifluoromethyl pyridin 3 ylsulfonyl 4 5 dihydro 2h pyrazolo 4 3 c quinoline elnd007 metabol
Journal of Medicinal Chemistry, 2013Co-Authors: Gary Probst, Danielle L Aubele, Simeon Bowers, Darren B Dressen, Albert W Garofalo, Roy K Hom, Andrei W Konradi, Jennifer Marugg, Matthew N Mattson, Martin L NeitzelAbstract:Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006) and 34 (ELND007) both entered human clinical trials. The in vitro and in vivo characteristics for these two compounds are described. A comparison of inhibition of Aβ generation in vivo between 30, 34, Semagacestat 41, Begacestat 42, and Avagacestat 43 in mice is made. 30 lowered Aβ in the CSF of healthy human volunteers.
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Discovery of (R)‑4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro‑1H‑pyrazolo[4,3‑c]quinoline (ELND006) and (R)‑4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro‑2H‑pyrazolo[4,3‑c]quinoline (EL
2013Co-Authors: Gary Probst, Danielle L Aubele, Simeon Bowers, Darren B Dressen, Albert W Garofalo, Roy K Hom, Andrei W Konradi, Jennifer Marugg, Matthew N Mattson, Martin L NeitzelAbstract:Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006) and 34 (ELND007) both entered human clinical trials. The in vitro and in vivo characteristics for these two compounds are described. A comparison of inhibition of Aβ generation in vivo between 30, 34, Semagacestat 41, Begacestat 42, and Avagacestat 43 in mice is made. 30 lowered Aβ in the CSF of healthy human volunteers
Simeon Bowers - One of the best experts on this subject based on the ideXlab platform.
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discovery of r 4 cyclopropyl 7 8 difluoro 5 4 trifluoromethyl phenylsulfonyl 4 5 dihydro 1h pyrazolo 4 3 c quinoline elnd006 and r 4 cyclopropyl 8 fluoro 5 6 trifluoromethyl pyridin 3 ylsulfonyl 4 5 dihydro 2h pyrazolo 4 3 c quinoline elnd007 metabol
Journal of Medicinal Chemistry, 2013Co-Authors: Gary Probst, Danielle L Aubele, Simeon Bowers, Darren B Dressen, Albert W Garofalo, Roy K Hom, Andrei W Konradi, Jennifer Marugg, Matthew N Mattson, Martin L NeitzelAbstract:Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006) and 34 (ELND007) both entered human clinical trials. The in vitro and in vivo characteristics for these two compounds are described. A comparison of inhibition of Aβ generation in vivo between 30, 34, Semagacestat 41, Begacestat 42, and Avagacestat 43 in mice is made. 30 lowered Aβ in the CSF of healthy human volunteers.
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Discovery of (R)‑4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro‑1H‑pyrazolo[4,3‑c]quinoline (ELND006) and (R)‑4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro‑2H‑pyrazolo[4,3‑c]quinoline (EL
2013Co-Authors: Gary Probst, Danielle L Aubele, Simeon Bowers, Darren B Dressen, Albert W Garofalo, Roy K Hom, Andrei W Konradi, Jennifer Marugg, Matthew N Mattson, Martin L NeitzelAbstract:Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006) and 34 (ELND007) both entered human clinical trials. The in vitro and in vivo characteristics for these two compounds are described. A comparison of inhibition of Aβ generation in vivo between 30, 34, Semagacestat 41, Begacestat 42, and Avagacestat 43 in mice is made. 30 lowered Aβ in the CSF of healthy human volunteers