Compounds with bridgehead nitrogen. 42—1H NMR and stereochemistry of isomeric 6a-methylperhydroindolo[3,2,1-i,j]benzoxazines and the position of conformational equilibrium in perhydropyrrolo[1,2-c][1,3]oxazine
摘要:
AbstractThe 1H NMR parameters of the NCH2O protons in the spectrum of perhydropyrrolo[1,2‐c][1,3]oxazine show its existence in solution at room temperature in the O‐inside cis‐fused conformation. rel‐(3aS,6aS,6bR,10aS,11aS)‐6a‐Methylperhydroindolo[3,2,1‐i,j]benzoxazine and rel‐(3aS,6aS,6bS,10aR,11aS)‐6a‐methylperhydroindolo[3,2,1‐i,j]benzoxazine are shown to adopt cis‐ and trans‐fused conformations, respectively, for the corresponding bicyclic moiety.
A compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
CYCLOALKYLIDENE AND HETEROCYCLOALKYLIDENE INHIBITOR COMPOUNDS
申请人:Melvin, JR. Lawrence S.
公开号:US20100022543A1
公开(公告)日:2010-01-28
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
[EN] QUINAZOLINE DERIVATIVES FOR USE AGAINST CANCER<br/>[FR] DERIVES DE QUINAZOLINE A UTILISER CONTRE LE CANCER
申请人:ASTRAZENECA AB
公开号:WO2006040526A1
公开(公告)日:2006-04-20
The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of p, R1, q, R2, R3, R4, R5, Ring A, X1, R6, r and R7 has any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.
[EN] QUINAZOLINE DERIVATIVES<br/>[FR] DERIVES DE QUINAZOLINE
申请人:ASTRAZENECA AB
公开号:WO2006040520A1
公开(公告)日:2006-04-20
The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.