Patent classifications
C07C381/10
2-AMINO-N-(AMINO-OXO-ARYL-LAMBDA6-SULFANYLIDENE)ACETAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(amino-oxo-aryl-λ.sup.6-sulfanylidene)acetamide compounds (referred to herein as ANASIA compounds) that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-tRNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.
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Compounds
The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R.sup.1 is a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and R.sup.2 is a cyclic group substituted at the a-position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3. ##STR00001##
Compounds
The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R.sup.1 is a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and R.sup.2 is a cyclic group substituted at the a-position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3. ##STR00001##
USP30 INHIBITORS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of USP30, and the treatment of USP30-mediated disorders.
NOVEL CHEMOKINE CXCR1 AND CXCR2 RECEPTOR ANTAGONIST COMPOUNDS, AND USE THEREOF IN THE TREATMENT OF CHEMOKINE-MEDIATED PATHOLOGIES
Novel chemokine CXCR1 and CXCR2 receptor antagonist compounds of general formula (I) are described. Also described, are pharmaceutical compositions including the compounds, and use of the compounds and the compositions for the treatment of chemokine-mediated pathologies, more specifically in the field of dermatology.
NOVEL CHEMOKINE CXCR1 AND CXCR2 RECEPTOR ANTAGONIST COMPOUNDS, AND USE THEREOF IN THE TREATMENT OF CHEMOKINE-MEDIATED PATHOLOGIES
Novel chemokine CXCR1 and CXCR2 receptor antagonist compounds of general formula (I) are described. Also described, are pharmaceutical compositions including the compounds, and use of the compounds and the compositions for the treatment of chemokine-mediated pathologies, more specifically in the field of dermatology.
MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO
- Ronald J. Heemstra ,
- RONALD ROSS, JR. ,
- Kyle A. DeKorver ,
- Kaitlyn Gray ,
- Daniel I. Knueppel ,
- PETER VEDNOR ,
- Timothy P. Martin ,
- Joseph D. Eckelbarger ,
- John F. Daeuble, SR. ,
- Ricky Hunter ,
- David A. Demeter ,
- Tony K. Trullinger ,
- Erich W. Baum ,
- Zoltan L. Benko ,
- Nakyen Choy ,
- Gary D. Crouse ,
- Fangzheng Li ,
- Jeffrey Nissen ,
- Monica B. Olson ,
- MICHELLE RIENER ,
- Thomas C. Sparks ,
- Frank J. Wessels ,
- Maurice C. Yap
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
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MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO
- Ronald J. Heemstra ,
- RONALD ROSS, JR. ,
- Kyle A. DeKorver ,
- Kaitlyn Gray ,
- Daniel I. Knueppel ,
- PETER VEDNOR ,
- Timothy P. Martin ,
- Joseph D. Eckelbarger ,
- John F. Daeuble, SR. ,
- Ricky Hunter ,
- David A. Demeter ,
- Tony K. Trullinger ,
- Erich W. Baum ,
- Zoltan L. Benko ,
- Nakyen Choy ,
- Gary D. Crouse ,
- Fangzheng Li ,
- Jeffrey Nissen ,
- Monica B. Olson ,
- MICHELLE RIENER ,
- Thomas C. Sparks ,
- Frank J. Wessels ,
- Maurice C. Yap
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
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NOVEL HDAC INHIBITORS AND THERAPEUTIC USE THEREOF
Described herein are novel compounds, compositions and methods for treatment of diseases including cancer using such compounds, compositions, and methods. The compounds include those of Formula (I):
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NOVEL HDAC INHIBITORS AND THERAPEUTIC USE THEREOF
Described herein are novel compounds, compositions and methods for treatment of diseases including cancer using such compounds, compositions, and methods. The compounds include those of Formula (I):
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