[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.
신규의 아졸실란 화합물 및 그 합성 방법 및, 해당 아졸실란 화합물을 성분으로 하는 실란 커플링제를 제공하고, 및 해당 아졸실란 화합물을 사용한 표면 처리액, 표면 처리 방법 및 재질이 다른 2개의 재료의 접착 방법을 제공하는 것을 목적으로 한다. 본 발명의 아졸실란 화합물은, 특정의 화학식 (I-1) 또는 (II-1)로 표시되는 화합물이다.
[EN] PROCESS FOR OBTAINING DROSPIRENONE<br/>[FR] PROCÉDÉ D'OBTENTION DE LA DROSPIRÉNONE
申请人:CRYSTAL PHARMA SAU
公开号:WO2012107513A1
公开(公告)日:2012-08-16
The invention relates to processes for obtaining 6β,7β; 15β, 16β-dimethylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone, commonly known as Drospirenone, as well as to intermediate compounds of formula (II) useful in said process.
To supply a derivative having a 2-acyliminopyridine structure and being represented by the following formula (I) in an amount required as a pest control agent stably and at a low cost, provided is a method comprising the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of an acylating agent, to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B):
[where Ar represents a phenyl group or a 5-to 6-membered heterocycle, R
1
represents a C
1-6
alkyl group, and Y represents a hydrogen atom; a halogen atom; a hydroxyl group; a C
1-6
alkyl group which may be substituted with a halogen atom; a C
1-6
alkyloxy group which may be substituted with a halogen atom; a cyano group; a formyl group; or a nitro group].