C07D239/62

Prolyl Hydroxylase Inhibitors

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I)

##STR00001##

which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Anticancer 1,3-dioxane-4,6-dione derivatives and method of combinatorial synthesis thereof

Compounds, methods of synthesis, and methods of cancer treatment by arylidene-1,3-dioxane-4,6-diones. A Meldrum's acid-based chemistry and hybrid solid-liquid method. The method includes protection of ketone and aldehyde components and simultaneous immobilization on the solid phase, introduction of substituents, grafts and derivatives compatible with the protection, detachment and restoration of active carbonyl reactivity, reaction of ketone library with malonate, reacting of the products with the aldehyde library in liquid phase and separation of the products by preparative HPLC.

Anticancer 1,3-dioxane-4,6-dione derivatives and method of combinatorial synthesis thereof

Compounds, methods of synthesis, and methods of cancer treatment by arylidene-1,3-dioxane-4,6-diones. A Meldrum's acid-based chemistry and hybrid solid-liquid method. The method includes protection of ketone and aldehyde components and simultaneous immobilization on the solid phase, introduction of substituents, grafts and derivatives compatible with the protection, detachment and restoration of active carbonyl reactivity, reaction of ketone library with malonate, reacting of the products with the aldehyde library in liquid phase and separation of the products by preparative HPLC.

Prolyl hydroxylase inhibitors

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) ##STR00001##
which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Prolyl hydroxylase inhibitors

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) ##STR00001##
which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

NOVEL BARBITURIC ACID DERIVATIVES, THEIR PREPARATION AND USE THEREOF AS LEUKOCYTE TRANSMIGRATION INHIBITORS AND FOR TREATING INFLAMMATORY DISEASES, AUTOIMMUNE DISEASES AND CANCER

Provided herein are novel barbituric acid derivatives, their synthesis and use thereof in blocking leukocyte transmigration. The novel barbituric acid derivatives are useful for the treatment of disorders associated with leukocyte transmigration, such as for example inflammatory diseases and disorders, autoimmune diseases and disorders, and cancers.

NOVEL BARBITURIC ACID DERIVATIVES, THEIR PREPARATION AND USE THEREOF AS LEUKOCYTE TRANSMIGRATION INHIBITORS AND FOR TREATING INFLAMMATORY DISEASES, AUTOIMMUNE DISEASES AND CANCER

Provided herein are novel barbituric acid derivatives, their synthesis and use thereof in blocking leukocyte transmigration. The novel barbituric acid derivatives are useful for the treatment of disorders associated with leukocyte transmigration, such as for example inflammatory diseases and disorders, autoimmune diseases and disorders, and cancers.

Barbituric acid derivatives comprising cationic and lipophilic groups

The present invention relates to bioactive cyclic compounds and their use as antimicrobial agents. In particular, the present invention relates to barbiturate mimics of Eusynstyelamides or small antimicrobial peptides. The compounds of the invention are represented by Formula (I). (I) ##STR00001##

Barbituric acid derivatives comprising cationic and lipophilic groups

The present invention relates to bioactive cyclic compounds and their use as antimicrobial agents. In particular, the present invention relates to barbiturate mimics of Eusynstyelamides or small antimicrobial peptides. The compounds of the invention are represented by Formula (I). (I) ##STR00001##

CRYSTALLINE FORMS OF GSK1278863, PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
20210230124 · 2021-07-29 ·

The present disclosure relates to crystalline form CS1 and CS9 of a hypoxia-inducible factor prolyl hydroxylase inhibitor compound (I) GSK1278863, processes for preparation, and uses for preparing drugs treating and/or preventing anemia thereof.

##STR00001##