A new procedure for the conversion of thiols into reactive sulfenylating agents
摘要:
Thiols may be converted in high yield into unsymmetrical 2-pyridyl disulfides 3. Treatment of these with alkylating agents (e.g., alkyl fluorosulfonates or oxonium salts) affords the corresponding N-alkylpyridyl disulfides 4, which are potent sulfenylating agents (Scheme II) and react smoothly with a variety of sulfur nucleophiles (e.g., thiols, thiones, thioamides, dithiocarbamates, thiocyanate, etc.) to afford disulfides, with amines to afford sulfenamides, and with beta-diketones to afford sulfides. This new method is particularly well-suited to the preparation of unsymmetrical disulfides and sulfenamides from complex and otherwise reactive thiols.
Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, L, L1, L2, L3, M and n are as defined herein. Methods associated with preparation and use of such compounds is also provided.
Tubulysin analogs of the formula (I)
where R
1
, R
2
R
3
, R
4
, R
5
, R
6
, R
7
, and Y are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.
[EN] DRUG ANTIBODY CONJUGATES<br/>[FR] CONJUGUÉS MÉDICAMENT-ANTICORPS
申请人:PHARMA MAR SA
公开号:WO2021214126A1
公开(公告)日:2021-10-28
Drug conjugates having formula [D-(X)b-(AA)w-(T)g-(L)-]n-Ab wherein: D is a drug moiety having the following formula (I) or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof, (I) wherein D is covalently attached via a hydroxy or amine group to (X)b if any, or (AA)w if any, or to (T)g if any, or (L); that are useful in the treatment of cancer.
The present invention relates to cyanine compounds, compositions comprising them, articles of manufacture, and methods of making and using them. The cyanines usefully comprise one or more carboxyl groups or derivatives thereof that are indirectly attached to an aryl ring on an alkylaryl cyanine substituent. Also provided are conjugates of the disclosed cyanines and one or more other substances. Solvates, solutions, and derivatized forms of the cyanines are also provided. The cyanines find use in a variety of bioassays, both in direct single-label applications and in energy transfer formats. Methods utilizing the disclosed cyanines for analyzing a sample for a target are provided. Also disclosed are detection complexes comprising the disclosed cyanines, as well as compositions and articles comprising the cyanines in an excited state, for example formed by direct excitation or by energy transfer. The cyanines may be used as alternatives to other known optically active species in a variety of settings. Other embodiments are described further herein.
MATERIAL, METHOD FOR PREPARING SAME, AND USES THEREOF
申请人:COMMISSARIAT À L'ÉNERGIE ATOMIQUE ET AUX ÉNERGIES ALTERNATIVES
公开号:US20150057374A1
公开(公告)日:2015-02-26
A material including a continuous aqueous phase and a dispersed phase in the form of droplets containing an amphiphilic lipid and a surfactant having the following formula (I):
(L
1
-X
1
—H
1
—Y
1
)
v
-G-(Y
2
—H
2
—X
2
-L
2
)
w
(I),
wherein:
L
1
and L
2
independently represent lipophilic groups,
X
1
, X
2
, Y
1
, Y
2
and G independently represent a linking group,
H
1
and H
2
independently represent hydrophilic groups including a polyalkoxylated chain,
v and w are independently an integer from 1 to 8,
wherein the droplets of the dispersed phase are covalently bonded by the surfactant having the formula (I). The invention also relating to the method for preparing the same and to the uses thereof.