- 6,7-DIHYDRO-5H-PYRIDO[2,3-C]PYRIDAZINE DERIVATIVES AND RELATED COMPOUNDS AS BCL-XL PROTEIN INHIBITORS AND PRO-APOPTOTIC AGENTS FOR TREATING CANCER
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The present invention discloses 6,7-dihydro-5H-pyrido[2,3- c]pyridazine, 1,2,3,4-tetrahydroquinoline, 1H-indole, 3,4- dihydro-2H-1,4-benzoxazine, 1H-pyrrolo[2,3-b]pyridin-1-yl, 7H- pyrrolo[2,3-c]pyridazine, 5H,6H,7H,8H,9H-pyridazino[3,4-b]azepine derivatives and related compounds of formula (I) as Bcl-xL protein inhibitors for use as pro-apoptotic agents for treating cancer, autoimmune diseases or immune system diseases. Formula (I). The description discloses the preparation of exemplary compounds (e.g. pages 113 to 354 examples 1 to 221) as well as pharmacological studies with relevant data (e.g. pages 355 to 367; examples A to E; tables 1 to 5). Exemplary compounds are e.g. 2-{6-[(1,3-benzothiazol-2-yl) amino]-1,2,3,4-tetrahydroquinolin-1-yl}-1,3-thiazole-4-carboxylic acid (example 1) or e.g. 3-{1-[(adamantan-1-yl)methyl]-5- methyl-1H-pyrazol-4-yl}-6-{3-[(1,3-benzothiazol-2-yl)amino]-4- methyl-5H,6H,7H,8H-pyrido[2,3-c]pyridazin-8-yl]pyridine-2-carboxylic acid (example 24).
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- Bifunctional Tripeptide with a Phosphonic Acid as a Br?nsted Acid for Michael Addition: Mechanistic Insights
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Enamine catalysis is a widespread activation mode in the field of organocatalysis and is often encountered in bifunctional organocatalysts. We previously described H-Pro-Pro-pAla-OMe as a bifunctional catalyst for Michael addition between aldehydes and ar
- Cortes-Clerget, Margery,Jover, Jesús,Dussart, Jade,Kolodziej, Emilie,Monteil, Maelle,Migianu-Griffoni, Evelyne,Gager, Olivier,Deschamp, Julia,Lecouvey, Marc
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supporting information
p. 6654 - 6662
(2017/05/15)
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- Kinetic deconjugation: A gateway to the synthesis of Xxx-Gly (E)-alkene dipeptide isosteres
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A new method for the preparation of Xxx-Gly (E)-alkene dipeptide isosteres (EADIs), using LDA deprotonation followed by 1 N HCl quench, was explored. The method, named kinetic deconjugation, enabled the synthesis of Tyr-Gly, Gly-Gly, Ser-Gly, Pro-Gly, and
- Proteau-Gagné, Arnaud,Nadon, Jean-Franois,Bernard, Sylvain,Guérin, Brigitte,Gendron, Louis,Dory, Yves L.
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p. 6603 - 6605
(2012/02/03)
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- Synthesis of 2-amino-octa-4,7-dien-1-ol (2): Key intermediate for mycothiazole natural product and analogs
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Starting from L-aminoacids, facile methods for the preparation 2-aminocta-4,7-dien-ol with different stereochemistry have been developed as key intermediates of mycothiazole and analogs. Copyright Taylor & Francis, Inc.
- Mahler, Graciela,Serra, Gloria,Manta, Eduardo
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p. 1481 - 1492
(2007/10/03)
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- Synthesis of sphingosine analogues: Stereoselective synthesis of 3- deoxysphingosine and cis-isomers
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Both enantiomers of 3-deoxysphingosine as well as their cis-isomers were synthesized stereoselectively from L- and D-serine.
- Kawate, Tomohiko,Fukuta, Natsuko,Nishida, Atsushi,Nakagawa, Masako
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p. 2116 - 2118
(2007/10/03)
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