Nucleophilic substitution in 1-substituted 3-iodobicyclo[1.1.1]pentanes. A new synthetic route to functionalized bicyclo[1.1.1]pentane derivatives
摘要:
Nucleophilic substitution of the iodine in 1-substituted 3-iodobicyclo[1.1.1]pentanes [R = I (1), CF3 (2)] was investigated. The results of the reaction are strongly dependent on the nature of the nucleophile and the substituent. Whereas the trifluoromethyl derivative 2 is found to be inert in the reactions and gave substitution products only with organolithium reagents, the 1,3-diiodide 1 is much more reactive and affords normal substitution products with nitrogen bases and MeONa but gives [1.1.1]propellane with Grignard and organolithium reagents and with triaryl(alkyl)phosphines. Other synthesized 3-iodobicyclo[1.1.1]pentanes did not give substitution products. A general scheme for the transformations of 1 is also proposed.
[EN] COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS ET UTILISATIONS DE CES DERNIERS
申请人:YUMANITY THERAPEUTICS
公开号:WO2018081167A1
公开(公告)日:2018-05-03
The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
[EN] COMPOUNDS USEFUL FOR INHIBITING RET KINASE<br/>[FR] COMPOSÉS UTILES POUR INHIBER LA KINASE RET
申请人:LILLY CO ELI
公开号:WO2021222017A1
公开(公告)日:2021-11-04
Provided herein are RET kinase inhibitors according to the formula (I): pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods for their use in the treatment of diseases that can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders. A, R1, n, X1, X2, X3, X4, and R2 have the meanings given in the specification.
[EN] HETEROCYCLIC COMPOUNDS AS TRIGGERING RECEPTOR EXPRESSED ON MYELOID CELLS 2 AGONISTS AND METHODS OF USE<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES UTILISÉS EN TANT QUE RÉCEPTEUR DE DÉCLENCHEMENT EXPRIMÉ SUR DES AGONISTES DE CELLULES MYÉLOÏDES 2 ET PROCÉDÉS D'UTILISATION
申请人:AMGEN INC
公开号:WO2021226629A1
公开(公告)日:2021-11-11
The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ("TREM2"). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
[EN] PIPERIDIN-1- YL-N-PYRYDI NE-3-YL-2-OXOACET AM IDE DERIVATIVES USEFUL FOR THE TREATMENT OF MTAP-DEFICIENT AND/OR MT A-ACCUMULATING CANCERS<br/>[FR] DÉRIVÉS DE PIPÉRIDIN-1-YL-N-PYRYDINE-3-YL-2-OXO-ACÉTAMIDE UTILES POUR LE TRAITEMENT DE CANCERS DÉFICIENTS EN MTAP ET/OU ACCUMULANT MTA
申请人:TANGO THERAPEUTICS INC
公开号:WO2022026892A1
公开(公告)日:2022-02-03
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3, R4, R6, R7, R8 and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
Compounds of Formula (IV), as well as pharmaceutically acceptable salts thereof, are disclosed:
The compounds are useful in the treatment of Hepatitis C infections.