C07D513/08

Macrocycles as factor XIa inhibitors

The present invention provides compounds of Formula (I): ##STR00001##
or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

EPIDITHIODIOXOPIPERAZINE COMPOUND OR ITS DERIVATIVES, AND THE USE THEREOF
20170239261 · 2017-08-24 ·

The present invention relates to an epidithiodioxopiperazine derivative represented by the following Chemical Formula 1 or its reduced derivative; a method for preparing a compound represented by Chemical Formula 1 having improved intracellular permeability and mimicking the activity of 2-Cys-Prx in its reduced form in the cells; a pharmaceutical composition for preventing or treating vascular diseases comprising an epidithiodioxopiperazine compound or its derivatives or pharmaceutically acceptable salts thereof as an active ingredient; a drug delivery device for local administration including the pharmaceutical composition; and a pharmaceutical composition for inhibiting melanoma metastasis comprising the epidithiodioxopiperazine compound or its derivatives or pharmaceutically acceptable salts thereof as an active ingredient.

##STR00001##

Oridonin analogs, compositions, and methods related thereto

Certain embodiments are directed to oridonin analogs or derivatives. In certain aspects, the derivatives are used as anticancer or anti-inflammatory agents.

Oridonin analogs, compositions, and methods related thereto

Certain embodiments are directed to oridonin analogs or derivatives. In certain aspects, the derivatives are used as anticancer or anti-inflammatory agents.

Pyrimidine compounds for the treatment of cancer

Compounds of Formula I or II: ##STR00001##
are described, along with pharmaceutical compositions containing the same and methods of using such compounds for the treatment of cancer.

6-bridged heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis B virus infection

The invention provides novel compounds having the general formula: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.

6-bridged heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis B virus infection

The invention provides novel compounds having the general formula: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.

Thioester prodrugs of macrocycles as inhibitors of histone deacetylases
11203602 · 2021-12-21 · ·

The present invention provides a novel macrocyclic prodrug compound of general Formula (I), a pharmaceutical composition comprising a compound of Formula (I), and a method for treating diseases mediated by HDAC enzymes by administering a compound of Formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, A and Z are defined herein. ##STR00001##

Thioester prodrugs of macrocycles as inhibitors of histone deacetylases
11203602 · 2021-12-21 · ·

The present invention provides a novel macrocyclic prodrug compound of general Formula (I), a pharmaceutical composition comprising a compound of Formula (I), and a method for treating diseases mediated by HDAC enzymes by administering a compound of Formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, A and Z are defined herein. ##STR00001##

Antibacterial compounds

Novel compounds having antimicrobial activity, in particular against Pseudomonas aeruginosa, Burkholderia cepacia and/or Clostridium difficile, and a pharmaceutical composition containing the novel compound. ##STR00001##