Abstract: Provided herein are novel lipase inhibitors and methods for using the same to treat inflammation, multisystem organ failure, necrotic pancreatic acinar cell death, acute pancreatitis, sepsis (e.g., culture negative sepsis), burns, and acne. For example, provided herein are two novel lipase inhibitors useful in the methods described herein: or a pharmaceutically acceptable salt thereof.

Abstract: The present disclosure provides compounds of Formula IA and Formula IB and their pharmaceutical compositions as selective agonists of REV-ERB-?: where R1, R2, R3, R4, R5, RX1, RX2, nA, nB, X, Y, and Z are described herein. The compounds are useful in various methods and uses, such as in the treatment of diseases including hyperglycemia, dyslipidemia, atherosclerosis, and autoimmune and inflammatory disorders or diseases, and as cancer therapeutics, such as for the treatment of glioblastoma, hepatocellular carcinoma, and colorectal cancer, and for immune-oncology purposes.

Abstract: Provided herein are novel lipase inhibitors and methods for using the same to treat inflammation, multisystem organ failure, necrotic pancreatic acinar cell death, acute pancreatitis, sepsis (e.g., culture negative sepsis), burns, and acne. For example, provided herein are two novel lipase inhibitors useful in the methods described herein: or a pharmaceutically acceptable salt thereof.

Abstract: Provided herein are novel lipase inhibitors and methods for using the same to treat inflammation, multisystem organ failure, necrotic pancreatic acinar cell death, acute pancreatitis, sepsis (e.g., culture negative sepsis), burns, and acne. For example, provided herein are two novel lipase inhibitors useful in the methods described herein: or a pharmaceutically acceptable salt thereof.

Abstract: This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.

Abstract: Provided herein are novel lipase inhibitors and methods for using the same to treat inflammation, multisystem organ failure, necrotic pancreatic acinar cell death, acute pancreatitis, sepsis (e.g., culture negative sepsis), burns, and acne. For example, provided herein are two novel lipase inhibitors useful in the methods described herein: or a pharmaceutically acceptable salt thereof.

Abstract: Provided herein are novel lipase inhibitors and methods for using the same to treat inflammation, multisystem organ failure, necrotic pancreatic acinar cell death, acute pancreatitis, sepsis (e.g., culture negative sepsis), burns, and acne. For example, provided herein are two novel lipase inhibitors useful in the methods described herein: or a pharmaceutically acceptable salt thereof.

Abstract: Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: wherein X is absent, CH2, or C(O); R1 is H, OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino; R2 is H or C1-6 alkyl; R3 is H, C1-6 alkyl, —C(O)(C1-3 alkyl), or —C(O)O(C1-3 alkyl); R4 is C3-10 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R5 groups; and R5 is OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino.

Abstract: Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: wherein X is absent, CH2, or C(O); R1 is H, OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino; R2 is H or C1-6 alkyl; R3 is H, C1-6 alkyl, —C(O)(C1-3 alkyl), or —C(O)O(C1-3 alkyl); R4 is C3-10 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R5 groups; and R5 is OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino.

Abstract: Provided herein are novel lipase inhibitors and methods for using the same to treat inflammation, multisystem organ failure, necrotic pancreatic acinar cell death, acute pancreatitis, sepsis (e.g., culture negative sepsis), burns, and acne. For example, provided herein are two novel lipase inhibitors useful in the methods described herein: or a pharmaceutically acceptable salt thereof.

Abstract: Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: wherein X is absent, CH2, or C(O); R1 is H, OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino; R2 is H or C1-6 alkyl; R3 is H, C1-6 alkyl, —C(O)(C1-3 alkyl), or —C(O)O(C1-3 alkyl); R4 is C3-10 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R5 groups; and R5 is OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino.

Abstract: Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: wherein X is absent, CH2, or C(O); R1 is H, OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino; R2 is H or C1-6 alkyl; R3 is H, C1-6 alkyl, —C(O)(C1-3 alkyl), or —C(O)O(C1-3 alkyl); R4 is C3-10 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R5 groups; and R5 is OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino.

Abstract: Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: wherein X is absent, CH2, or C(O); R1 is H, OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino; R2 is H or C1-6 alkyl; R3 is H, C1-6 alkyl, —C(O)(C1-3 alkyl), or —C(O)O(C1-3 alkyl); R4 is C3-10 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R5 groups; and R5 is OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino.

Abstract: Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: wherein X is absent, CH2, or C(O); R1 is H, OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino; R2 is H or C1-6 alkyl; R3 is H, C1-6 alkyl, —C(O)(C1-3 alkyl), or —C(O)O(C1-3 alkyl); R4 is C3-10 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R5 groups; and R5 is OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino.

Abstract: The present disclosure relates generally to thienopyrimidine and thienopyridine compounds and methods of use thereof. In particular embodiments, the present disclosure provides compositions comprising thienopyrimidine and thienopyridine compounds of Formula 3: and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins.

Abstract: Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease.

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.