Olga M. Fryszman - San Diego CA, US Hengyuan Lang - San Diego CA, US Jiong Lan - San Diego CA, US Edcon Chang - San Diego CA, US Yunfeng Fang - San Diego CA, US
Assignee:
Novartis AG - Basel
International Classification:
A01N 43/56 C07D 231/00
US Classification:
514407, 5483714
Abstract:
Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38α and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
Olga M. Fryszman - San Diego CA, US Hengyuan Lang - San Diego CA, US Jiong Lan - Emeryville CA, US Edcon Chang - San Diego CA, US Yunfeng Fang - San Diego CA, US
Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38α and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
Olga M. Fryszman - San Diego CA, US Hengyuan Lang - San Diego CA, US Jiong Lan - Moraga CA, US Edcon Chang - San Diego CA, US Yunfeng Fang - San Diego CA, US
Assignee:
Novartis AG - Basel
International Classification:
A61K 31/415 A61P 13/12 A61P 9/00 A61P 11/00
US Classification:
514407
Abstract:
Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38α, and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
- Basel, CH Olga M. Fryszman - San Diego CA, US Edcon Chang - San Diego CA, US Jiong Lan - Morago CA, US Yunfeng Fang - San Diego CA, US
Assignee:
Novartis AG - Basel
International Classification:
A61K 31/415 A61P 13/12 A61P 9/00 A61P 11/00
US Classification:
514407
Abstract:
Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38α, and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
R. Michael Lawrence - Yardley PA Scott A. Biller - Ewing NJ Olga M. Fryszman - Princeton NJ
Assignee:
Bristol-Myers Squibb Company - Princeton NJ
International Classification:
A61K 3166 C07F 938 C07F 940
US Classification:
514129
Abstract:
alpha. -Phosphonosulfinate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R. sup. 2 is OR. sup. 5 or R. sup. 5a ; R. sup. 3 and R. sup. 5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R. sup. 5a is alkyl, arylalkyl or aryl; R. sup. 4 is H or pharmaceutically acceptable cation;, Z is H, halogen, lower alkyl or lower alkenyl; and R. sup. 1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts.
Methods Of Preparing .Alpha.-Phosphonosulfinate Squalene Synthetase Inhibitors
R. Michael Lawrence - Yardley PA Scott A. Biller - Ewing NJ Olga M. Fryszman - Princeton NJ
International Classification:
C07F 938 C07F 940
US Classification:
558 87
Abstract:
alpha. -Phosphonosulfinate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R. sup. 2 is OR. sup. 5 or R. sup. 5a ; R. sup. 3 and R. sup. 5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R. sup. 5a is alkyl, arylalkyl or aryl; R. sup. 4 is H or a pharmaceutically acceptable cation; Z is H, halogen, lower alkyl or lower alkenyl; and R. sup. 1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; including pharmaceutically acceptable salts.
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