94992-56-0Relevant academic research and scientific papers
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
-
Page/Page column 315, (2021/02/05)
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).
Synthesis and incorporation of a simple acyclic furan containing phosphoramidite
Stevens,Madder
, p. 1359 - 1362 (2008/09/17)
A novel furan containing phosphoramidite was synthesized and incorporated into model oligonucleotides. This glycol nucleic acid based building block contains a furan unit substituting the natural base, and can be used for post synthetic oligonucleotide mo
Heterocyclic compound, composition and method for inhibiting adenosine deaminase
-
, (2008/06/13)
Heterocyclic compounds of the following formula: wherein B is ?[wherein R1is hydrogen or lower alkyl; R2is hydrogen or lower alkyl; and X is hydrogen or hydroxy protective group], lower alkanoyl or hydroxyimino(lower)alkyl A is lower
SYNTHESES OF 1-OXAQUINOLIZIDINES VIA REDUCTIVE CYCLIZATION OF HYDROXY-LACTAMS
Ahn, Kyo Han,Lee, Seok Jong
, p. 507 - 510 (2007/10/02)
The synthesis of the 1-oxaquinolizidine moiety of xestospongin A via reductive iminium ion formation from a lactam is described. Key Words: 1-oxaquinolizidine; iminium ion; "ate" complex from DIBAL and n-BuLi; xestospongin A; iminium ion-enamine tautomeri
Synthesis of 2-hydroxymethyl-1-oxaquinolizidine
Boerjesson, Lena,Welch, Christopher J.
, p. 6325 - 6334 (2007/10/02)
The synthesis of 2-hydroxymethyl-1-oxaquinolizidine from L-malic acid and 1,5 pentanediol, is reported.
Synthesis of the Oviposition-Deterring Pheromone of Rhagoletis cerasi L.
Kuechler, Birgit,Voss, Gundula,Gerlach, Hans
, p. 545 - 552 (2007/10/02)
The oviposition-deterring pheromone of Rhagoletis cerasi L. (-)-(8R,15R)-1 and a mixture of the two compounds (-)-(8R and 8S,15R)-1 have been synthesized.In the presence of the 1,5-cyclooctadiene-CuCl complex as a catalyst the Grignard reagent of (-)-(R)-
A new practical enantiospecific synthesis of unlabelled and tritium labelled 12-HETEs
Mosset, P.,Pointeau, P.,Aubert, F.,Lellouche, J. P.,Beaucourt, J. P.,Gree, R.
, p. 298 - 315 (2007/10/02)
The oxidative metabolism of arachidonic acid AA is known to yield a variety of biologically active substances.Among them, both enantiomers of 12-hydroxyeicosatetraenoic acid (12-HETE) have been the subject of much interest.In order to extend their biologi
(R)- and (S)-4-Methylaminomethyl-2,3,4,9-tetrahydrothiopyranoindole: Synthesis, Absolute Configuration, Conformation, and Analgesic Activity
Ishizuka, Natsuki,Shiro, Motoo,Makisumi, Yasuo
, p. 827 - 837 (2007/10/02)
(R)- and (S)-4-Methylaminomethyl-2,3,4,9-tetrahydrothiopyranoindole (2) have been synthesized and their conformation studied. (RS)-(2) has been found to be a potent non-narcotic analgesic agent.The crucial step was regio- and stereo-specific cycliz
SYNTHESIS OF THE ENANTIOMERS OF 1,7-DIOXASPIROUNDECANE, 4-HYDROXY-1,7-DIOXASPIROUNDECANE AND 3-HYDROXY-1,7-DIOXASPIROUNDECANE, THE COMPONENTS OF THE OLIVE FRUIT FLY PHEROMONE
Mori, Kenji,Watanabe, Hidenori,Yanagi, Kazunori,Minobe, Masao
, p. 3663 - 3672 (2007/10/02)
All of the enantiomers of the title compounds, the components of the pheromone of the olive fruit fly (Dacus oleae Gmelin), were synthesized from (S)-malic acid.
