C07D401/06

IMINO SULFANONE INHIBITORS OF ENPP1

The present disclosure relates generally to inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions thereof, and methods of using said compounds and compositions thereof. More specifically, the present disclosure relates to sulfoximine-based inhibitors of ENPP1 and methods of their use for treating disease mediated by ENPP1.

ARYLAMIDE DERIVATIVE HAVING ANTITUMOR ACTIVITY

The present disclosure provides, for example, a compound represented by general formula (6) below or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of the compound or salt:

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wherein X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are each independently —CR.sub.2═ or —N═, R.sub.2 is, for example, a halogen atom, R.sub.1 is, for example, —S(═O).sub.2—NH—R.sub.8, R.sub.8 is, for example, a C1-6 alkyl group, R.sub.3 is, for example, a hydrogen atom, R.sub.5 is, for example, a halogen atom, R.sub.6 is, for example, a hydrogen atom, and R.sub.4 is, for example, a cyclopropyl group. The compounds, salts or solvates provided by the present disclosure exhibit high RAF/MEK complex-stabilizing activity and can be used for the treatment or prevention of cell proliferative disorders, particularly cancers.

Viral replication inhibitors

The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds. ##STR00001##

Viral replication inhibitors

The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds. ##STR00001##

STRIGOLACTONE RECEPTOR INHIBITOR, AGRICULTURAL COMPOSITION AND USE THEREOF, STRIGA SEED GERMINATION INHIBITOR, AND TRIAZOLE UREA COMPOUND

The strigolactone receptor inhibitor for plants contains at least one kind of triazole urea compounds represented by the following formula (I) as an active ingredient. It can be applicable to an agricultural composition; a method for using the agricultural composition as, for example, a branching enhancer for plants; a germination inhibitor for Striga seeds, the germination inhibitor containing the triazole urea compound; and a novel triazole urea compound that is useful as a strigolactone receptor inhibitor for plants. In the formula, A represents a group represented by (A-1) or (A-2). R.sup.1 and R.sup.2 represent a hydrogen atom and so forth. R.sup.3 and R.sup.4 represent a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, a cycloalkyl group having 3 to 20 carbon atoms, or an aryl group having 6 to 20 carbon atoms and so forth. R.sup.3 and R.sup.4 may form a ring together.

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COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

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COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

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MrgprX2 Antagonists and Uses Thereof

The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pharmaceutically or orally acceptable carrier for administration.

MrgprX2 Antagonists and Uses Thereof

The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pharmaceutically or orally acceptable carrier for administration.

ARYL HETEROCYCLIC COMPOUNDS AS Kv1.3 POTASSIUM SHAKER CHANNEL BLOCKERS

A compound of Formula (I), or a pharmaceutically-acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.

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