[EN] TYROSINE KINASE 2 (TYK2) DEGRADATION COMPOUNDS AND METHODS OF USE<br/>[FR] COMPOSÉS DE DÉGRADATION DE LA TYROSINE KINASE 2 (TYK2) ET PROCÉDÉS D'UTILISATION
申请人:CULLGEN SHANGHAI INC
公开号:WO2022100710A1
公开(公告)日:2022-05-19
This disclosure relates to heterobifunctional compounds (e.g., bi-functional small molecule compounds), compositions comprising one or more of the heterobifunctional compounds, and to methods of use the heterobifunctional compounds for the treatment of certain disease in a subject in need thereof. The disclosure also relates to methods for identifying such heterobifunctional compounds.
It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1):
In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(═O) or NR11; and D is a group represented by the following general formula (4) or (6).
In the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7).
z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26. In the above formulae, R1 to R26 each represents hydrogen, alkyl, alkenyl or alkynyl.
1,4 Substituted Pyrazolopyrimidines as Kinase Inhibitors
申请人:Schmiedeberg Niko
公开号:US20080096868A1
公开(公告)日:2008-04-24
The invention relates to 1,4-substituted pyrazolopyrimidine compounds of the formula I,
pharmaceuticals comprising a 1,4-substituted pyrazolopyrimidine compound, the use of a 1,4-substituted pyrazolopyrimidine compound in the treatment or the use thereof in the manufacture of a pharmaceutical formulation for the treatment of a disease that depends on inadequate activity of a protein kinase, methods of treatment comprising administering a 1,4-substituted pyrazolopyrimidine compound, methods for the manufacture of a novel compound of that class, and novel intermediates and partial steps for their synthesis.
It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1):
In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(═O) or NR11; and D is a group represented by the following general formula (4) or (6).
In the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7).
z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26. In the above formulae, R1 to R26 each represents hydrogen, alkyl, alkenyl or alkynyl.
3-imidazolyl-indoles for the treatment of proliferative diseases
申请人:Novartis AG
公开号:US08053457B2
公开(公告)日:2011-11-08
The invention relates to 3-heterocyclyl indolyl compounds of formula I capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively:
wherein
R1, R2, R3, R4, RA, Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.