[EN] GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONISTS, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME<br/>[FR] ANTAGONISTES DES RÉCEPTEURS DE L'HORMONE DE LIBÉRATION DES GONADOTROPHINES, LEUR PROCÉDÉ DE PRÉPARATION ET COMPOSITION PHARMACEUTIQUE LES COMPRENANT
申请人:SK CHEMICALS CO LTD
公开号:WO2013129879A1
公开(公告)日:2013-09-06
The present invention provides gonadotropin releasing hormone receptor antagonists and the pharmaceutical composition comprising the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid-dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.
Reactions of HDDA-Derived Benzynes with Sulfides: Mechanism, Modes, and Three-Component Reactions
作者:Junhua Chen、Vignesh Palani、Thomas R. Hoye
DOI:10.1021/jacs.6b01025
日期:2016.4.6
We report here reactions of alkyl sulfides with benzynes thermally generated by the hexadehydro-Diels-Alder (HDDA) cycloisomerization. The initially produced 1,3-betaine (o-sulfonium/aryl carbanion) undergoes intramolecular proton transfer to generate a more stable S-aryl sulfur ylide. This can react in various manners, including engaging weak acids (HA) in the reaction medium. This can produce transient
Selectively switching on europium emission in drug site one of human serum albumin
作者:Sergey Shuvaev、Robert Pal、David Parker
DOI:10.1039/c7cc03071a
日期:——
A luminescent europium probe has been discovered that binds selectively to drug-site I in human serum albumin, signalled by a ‘switching on’ of europium emission, accompanied by strong inducedcircularlypolarisedluminescence.
A near-IR luminescent ratiometric ytterbium pH probe
作者:Sergey Shuvaev、David Parker
DOI:10.1039/c9dt00411d
日期:——
The hypersensitive 2F5/2 to 2F7/2 transition of Yb3+ can be used to monitor perturbations of the coordination sphere in ytterbium(III) complexes. An envelope of Stark components gives rise to a relatively broad and asymmetric emission band, whilst changes in their relative intensity and energy enable a ratiometric response. We report a new ytterbium complex with a sulphonamide arm that binds reversibly
A bright and responsive europium probe for determination of pH change within the endoplasmic reticulum of living cells
作者:Brian K. McMahon、Robert Pal、David Parker
DOI:10.1039/c3cc42308e
日期:——
A ratiometric Eu(III) complex has been developed that localises selectively within the endoplasmicreticulum of livingcells. Careful calibration, using a time-gated spectral imaging microscope, allows the intensity ratio of emission bands and the variation of excited state lifetime to be used for pH determination, with a pKa of 7.15.