C07D213/58

GPBP inhibition using Q2 peptidomimetics

Disclosed are compounds of formula: ##STR00001##
that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.

GPBP inhibition using Q2 peptidomimetics

Disclosed are compounds of formula: ##STR00001##
that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.

Gonadotropin-releasing hormone receptor antagonists and methods relating thereto

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ##STR00001##
wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Gonadotropin-releasing hormone receptor antagonists and methods relating thereto

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ##STR00001##
wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Mcl-1 modulating compounds for cancer treatment

The invention relates to compounds of formula (I), and to their therapeutic use in the treatment of cancer: ##STR00001## Wherein Y.sub.1, Y.sub.2, Ar.sub.1, Ar.sub.2, R.sub.1, R.sub.2, i, j, k, l are as defined in claim 1.

Mcl-1 modulating compounds for cancer treatment

The invention relates to compounds of formula (I), and to their therapeutic use in the treatment of cancer: ##STR00001## Wherein Y.sub.1, Y.sub.2, Ar.sub.1, Ar.sub.2, R.sub.1, R.sub.2, i, j, k, l are as defined in claim 1.

GPBP inhibition using Q2 peptidomimetics

Disclosed are compounds of formula:

##STR00001##

that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.

GPBP inhibition using Q2 peptidomimetics

Disclosed are compounds of formula:

##STR00001##

that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.

MERCAPTOACETOPHENONE AMINOHYDRAZONES, THEIR SALTS AND USES THEREOF

A new class of antibiotics, namely, mercaptoacetophenone aminohydrazones, their analogues, their method of preparation, their salts, and their use in cases of bacterial infections, either alone or with other compounds.

Process for preparing atazanavir sulphate

The present invention relates to a process for the preparation of Compound (A): ##STR00001##
wherein the process comprises contacting atazanavir base (Compound (II)) ##STR00002##
with sulphuric acid in a combination of two or more solvents and isolating compound (A). The present invention also relates to substantially pure Compound (A), and to Compound (A) devoid of mesityl oxide impurity. Mesityl oxide has the following formula: ##STR00003##