C07D231/02

PYRAZOLE DERIVATIVES AS INHIBITORS OF STAT3

Compositions that modulate the activity of signal transducer and activator of transcription-3 (STAT3) activity as well as their methods of use, such as treatment and imaging are provided. Compositions contain small molecules such as substituted pyrazoles and are useful in treatment of diseases related to the activity of STAT3 including, for example, cancer and other diseases.

Necrosis inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

Necrosis inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

ANIMAL AND HUMAN ANTI-MALARIAL AGENTS
20170348316 · 2017-12-07 ·

Provided herein are Purine Comounds of Formula (I)

##STR00001## or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, compositions comprising an effective amount of a Purine Compound, and methods for treating or preventing malaria comprising the administration of an effective amount of a Purine Compound.

Necrosis Inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

Necrosis Inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

Substituted benzene fungicides

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, ##STR00001##
wherein W is O or S; V is a direct bond or NR.sup.3; Q is or CR.sup.6aR.sup.6b, O, NR.sup.7, C═N—O—R.sup.7 or C(═O); Y is —C(R.sup.5)═N—O—(CR.sup.8aR.sup.8b).sub.p—X—(CR.sup.9aR.sup.9b).sub.q—SiR.sup.10aR.sup.10bR.sup.10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, R.sup.7, R.sup.8a, R.sup.8b, R.sup.9a, R.sup.9b, R.sup.10a, R.sup.10b, R.sup.10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Substituted benzene fungicides

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, ##STR00001##
wherein W is O or S; V is a direct bond or NR.sup.3; Q is or CR.sup.6aR.sup.6b, O, NR.sup.7, C═N—O—R.sup.7 or C(═O); Y is —C(R.sup.5)═N—O—(CR.sup.8aR.sup.8b).sub.p—X—(CR.sup.9aR.sup.9b).sub.q—SiR.sup.10aR.sup.10bR.sup.10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, R.sup.7, R.sup.8a, R.sup.8b, R.sup.9a, R.sup.9b, R.sup.10a, R.sup.10b, R.sup.10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Pyrazole derivatives as inhibitors of STAT3

Compositions that modulate the activity of signal transducer and activator of transcription-3 (STAT3) activity as well as their methods of use, such as treatment and imaging are provided. Compositions contain small molecules such as substituted pyrazoles and are useful in treatment of diseases related to the activity of STAT3 including, for example, cancer and other diseases.

Animal and human anti-malarial agents

Provided herein are Purine Compounds of Formula (I) ##STR00001##
or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, compositions comprising an effective amount of a Purine Compound, and methods for treating or preventing malaria comprising the administration of an effective amount of a Purine Compound.