65246-99-3Relevant articles and documents
BROMODOMAIN TARGETING DEGRONIMERS FOR TARGET PROTEIN DEGRADATION
-
Page/Page column 391, (2017/12/05)
This invention provides a Degronimer that has an E3 Ubiquitin Ligase targeting moiety (Degron) that can be linked to a Targeting Ligand for a bromodomain protein selected for in vivo degradation to achieve a therapeutic effect, and methods of use and compositions thereof as well as methods for their preparation.
DIHYDROQUINAZOLINONE ANALOGUES
-
Paragraph 0223-0226, (2014/10/16)
The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4 and A1 to A5 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
DIHYDROQUINAZOLINONE ANALOGUES AS BRD4 INHIBITORS
-
Page/Page column 46; 49, (2014/10/15)
The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4 and A1 to A5 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
-
Page/Page column 45-46, (2008/06/13)
The invention relates to compounds of formula (I) their derivatives comprising a detectable label, their compositions and their use in the treatment of human immunodeficiency virus (HIV) infection. In particular, the invention provides novel inhibitors of
New vistas in quinoline synthesis
Atechian, Sarkis,Nock, Nadine,Norcross, Roger D.,Ratni, Hassen,Thomas, Andrew W.,Verron, Julien,Masciadri, Raffaello
, p. 2811 - 2823 (2007/10/03)
The gold-catalyzed Friedlander reaction was applied to the condensation of 2-aminoarylketones with β-keto-esters, β-diketones, β-keto-amides, and β-keto-sulfones to afford a diverse range of 2,3,4-trisubstituted quinolines in 3-82% yield. The seven-membered rings 1,3-cycloheptadione and azepane-2,4-dione reacted smoothly in 75% yield. An alternative procedure for the synthesis of 3-(methanesulfonyl)quinolines was developed and provided an entry into late stage manipulation of the 4-position of these quinolines. The requisite 2-aminoarylketones for the Friedlander reaction were prepared in one pot by modified Sugasawa reaction using gallium(III) chloride and boron(III) chloride in 12-54% yield.
3-Methanesulfonylquinolines as GABAB enhancers
-
Page/Page column 9, (2010/11/25)
The present invention relates to compounds of formula I wherein R1, R2 and R3 are as defined in the specification, which are active at the GABAB receptor and which can be used for the treatment of CNS disorders.
SmI2-mediated facile one-pot preparation of 2,4-diarylquinolines from 3-aryl-2,1-benzisoxazoles
Fan, Xuesen,Zhang, Yongmin
, p. 7001 - 7003 (2007/10/03)
On treatment with SmI2, 3-aryl-2,1-benzisoxazoles undergo reductive cleavage of the N-O bond leading to 2-aminobenzophenones in high yields upon protonation. If aryl methyl ketones are added to the reaction mixture prior to protonation, the desired 2,4-diarylquinolines can be obtained in moderate yields under mild conditions.