CLEAVABLE CONJUGATES OF TLR7/8 AGONIST COMPOUNDS, METHODS FOR PREPARATION, AND USES THEREOF
申请人:Dynavax Technologies Corporation
公开号:US20190151462A1
公开(公告)日:2019-05-23
The present disclosure relates to cleavable conjugates (for example, particle-based or antibody-based conjugates) of TLR7/8 agonists (for example, 1H-imidazo[4,5-c]quinoline derivatives) containing a conjugation linker, a cleavable linker, and a self-eliminating linker. The present disclosure also related to methods for preparation of the cleavable conjugates, uses thereof for stimulating an effective immune response, and uses thereof for the treatment of cancer.
[EN] NOVEL PYRAZINE COMPOUNDS WITH OXYGEN, SULFUR AND NITROGEN LINKER FOR THE TREATMENT OF INFECTIOUS DISEASES<br/>[FR] NOUVEAUX COMPOSÉS DE PYRAZINE AYANT UN COUPLEUR D'OXYGÈNE, DE SOUFRE ET D'AZOTE POUR LE TRAITEMENT DE MALADIES INFECTIEUSES
申请人:HOFFMANN LA ROCHE
公开号:WO2017198744A1
公开(公告)日:2017-11-23
The present invention relates to compounds of the formula (I), or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R3 are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.
Copper-Catalyzed N-Directed Distal C(sp<sup>3</sup>)–H Sulfonylation and Thiolation with Sulfinate Salts
作者:Guang-Le Chen、Shi-Hui He、Liang Cheng、Feng Liu
DOI:10.1021/acs.orglett.1c03075
日期:2021.11.5
herein report a selective and catalytic C(sp3)–H functionalization approach to access amines bearing organo-sulfonyl and organo-thiol groups. This reaction proceeds through a cascade process of N-radical formation, alkyl radical formation via 1,5-HAT, and C–S bond formation, thereby offering a series of functionalized amines. This method could enable primary, secondary, and tertiary C(sp3)–H sulfonylation
The first facile one‐pot synthesis of sulfone‐containing oxindoles with easily accessible disulfides as the sulfonylating precursors is described. This reaction occurs smoothly under transition metal‐free conditions and shows excellent functional group tolerance, allowing the facile and efficient green synthesis of various sulfone‐containing oxindoles in aqueous solution. Preliminary mechanistic studies
描述了第一个简便的单锅合成含砜的吲哚类化合物,其中二硫醚作为磺酰化的前体很容易获得。该反应在不含过渡金属的条件下可平稳进行,并具有出色的官能团耐受性,可在水溶液中轻松高效地绿色合成各种含砜的羟吲哚。初步的机理研究表明,水(H 2 O)和过硫酸钾(K 2 S 2 O 8)均可以是产物中砜基的氧源。
[EN] TRI(CYCLO) SUBSTITUTED AMIDE GLUCOKINASE ACTIVATOR COMPOUNDS<br/>[FR] COMPOSES D'AMIDE A SUBSTITUTION TRI(CYCLO), ACTIVATEURS DE LA GLUCOKINASE
申请人:OSI PHARM INC
公开号:WO2004072066A1
公开(公告)日:2004-08-26
Compounds of Formula (I): (I) or pharmaceutically acceptable salts or N-oxides thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.