[EN] HINDERED DISULFIDE DRUG CONJUGATES<br/>[FR] CONJUGUÉS MÉDICAMENTEUX À PONT DISULFURE ENCOMBRÉ
申请人:GENENTECH INC
公开号:WO2017064675A1
公开(公告)日:2017-04-20
The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.
The invention relates to a method for labeling and fragmenting a single- or double-stranded deoxyribonucleic acid (DNA) comprising the following steps:
chemically fragmenting the DNA by creating at least one abasic site on said DNA,
attaching a marker to at least one of the fragments by means of a labeling reagent, said reagent covalently and predominantly coupling to at least one phosphate of said fragment.
The invention finds a preferred application in the field of diagnosis.
[EN] PURINE DERIVATIVES INHIBITORS OF TYROSINE PROTEIN KINASE SYK<br/>[FR] INHIBITEURS DE DERIVES DE PURINE DE LA TYROSINE KINASE SYK
申请人:NOVARTIS AG
公开号:WO2001009134A1
公开(公告)日:2001-02-08
Compounds of formula (I) in free or salt form, where X, R?1, R2, R3 and R4¿ are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of inflammatory or obstructive airways disease.