C07D213/61

ArylSulfonamide-based matrix metalloprotease inhibitors

The present invention provides a compound of formula (I): ##STR00001##
said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

Heteroaromatic electrophiles and methods of using thereof

Disclosed herein are compounds, compositions, and methods for reactivating or realkylating aged acetylcholinesterase inhibited by or conjugated to the organophosphorus compound. The organophosphorus compound can be a nerve agent. The acetylcholinesterase can be in the central nerve system (CNS) and/or the peripheral nervous system (PNS) of a subject. Accordingly, methods for ameliorating, diminishing, reversing, treating or preventing the toxic effects of an organophosphorus compound in a subject are provided herein. Methods for prophylactic or therapeutic treatment of exposure to an organophosphorus nerve agent are also provided.

PROCESS FOR THE PREPARATION OF A PDE4 INHIBITOR

The present invention relates to a process for the preparation of compounds endowed with phosphodiesterase (PDE4) inhibitory activity having formula (I). The invention also relates to the process for the isolation by crystallization of the compound (I) and to its use for the preparation of pharmaceutical compositions for inhalation in combination with suitable carriers or vehicles. The present invention also relates to solvates and crystal forms of a compound of formula (I). The synthesized product is suitable for use in pharmaceutical applications for instance in the treatment of respiratory diseases.

PROCESS FOR THE PREPARATION OF A PDE4 INHIBITOR

The present invention relates to a process for the preparation of compounds endowed with phosphodiesterase (PDE4) inhibitory activity having formula (I). The invention also relates to the process for the isolation by crystallization of the compound (I) and to its use for the preparation of pharmaceutical compositions for inhalation in combination with suitable carriers or vehicles. The present invention also relates to solvates and crystal forms of a compound of formula (I). The synthesized product is suitable for use in pharmaceutical applications for instance in the treatment of respiratory diseases.

HERBICIDAL COMPOUNDS

The present invention relates to 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 and G are as defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof.

##STR00001##

PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF VOXELOTOR

The invention relates to a process for the preparation of Voxelotor, or a salt or solvate thereof, according to the following scheme (Formula 1).

##STR00001##

METHOD OF PREPARING MALONONITRILE OXIME ETHER COMPOUND AND INTERMEDIATE COMPOUND

Provided are a method of preparing a malononitrile oxime ether compound and an intermediate compound. The malononitrile oxime ether compound has a structure as shown in formula (VII), wherein W is selected from aryl or heteroaryl. The preparation method comprises steps: reacting a first raw material with a second raw material in the presence of a first solvent and a catalyst to obtain the intermediate compound, wherein the first raw material has a structure as shown in formula (IV), and the second raw material has a structure as shown in formula (V); and subjecting the intermediate compound as shown in formula (VI), and, a dehyclrant to a dehydrantion reaction in the presence of a second solvent to obtain the malononitrile oxime ether compound. In the preparation process for the intermediate, a cheaper cyanoacetamide is used as a raw material, the reaction conditions are mild. Moreover, the yield of the intermediate compound is high and the cost of the process is low. Furthermore, the required malononitrile oxime ether compound, is obtained only through one-step dehydration reaction. Using the preparation method, is advantageous for improving the yield of malononitrile oxime ethers and reducing the cost of the process.

##STR00001##

INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth:

##STR00001##

INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth:

##STR00001##

Compositions and Methods for Inhibiting BMP
20170305883 · 2017-10-26 ·

The present invention provides small molecule inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.