Patent classifications
C07D213/85
COMPOUNDS, COMPOSITIONS, AND METHODS FOR TREATING OR AMELIORATING, OR PREVENTING VIRAL INFECTIONS
The present disclosure relates, in certain embodiments, to the finding that certain compounds that modulate the activity(ies) of Sigma receptors can be used to disrupt virus lifecycle, infection, and/or dissemination. The compounds contemplated in the disclosure are useful in the prevention, treatment, and/or amelioration of virus infection, either alone or in combination with at least one additional therapeutic agent, which can be an antiviral agent and/or an agent that treats, ameliorates, and/or prevents one or more virus infection symptoms and/or co-morbidities. In certain embodiments, the Sigma receptor is a Sigma-1 receptor (also known as Sigma1) or Sigma-2 receptor (also known as Sigma2 or TMEM97). In certain embodiments, Sigma1 inhibitors/antagonists that cause and/or trigger ER stress and/or autophagy are useful within the methods of the disclosure.
COMPOUNDS, COMPOSITIONS, AND METHODS FOR TREATING OR AMELIORATING, OR PREVENTING VIRAL INFECTIONS
The present disclosure relates, in certain embodiments, to the finding that certain compounds that modulate the activity(ies) of Sigma receptors can be used to disrupt virus lifecycle, infection, and/or dissemination. The compounds contemplated in the disclosure are useful in the prevention, treatment, and/or amelioration of virus infection, either alone or in combination with at least one additional therapeutic agent, which can be an antiviral agent and/or an agent that treats, ameliorates, and/or prevents one or more virus infection symptoms and/or co-morbidities. In certain embodiments, the Sigma receptor is a Sigma-1 receptor (also known as Sigma1) or Sigma-2 receptor (also known as Sigma2 or TMEM97). In certain embodiments, Sigma1 inhibitors/antagonists that cause and/or trigger ER stress and/or autophagy are useful within the methods of the disclosure.
IMPROVED SYNTHESIS OF KRAS G12C INHIBITOR COMPOUND
The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
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Acetyl-CoA carboxylase modulators
Provided herein are compounds that exhibit activity as acetyl-CoA carboxylase modulators (e.g., inhibitors) and are useful, for example, in methods for the control of fungal pathogens in plants.
Acetyl-CoA carboxylase modulators
Provided herein are compounds that exhibit activity as acetyl-CoA carboxylase modulators (e.g., inhibitors) and are useful, for example, in methods for the control of fungal pathogens in plants.
SARS-COV-2 INHIBITORS FOR TREATING CORONAVIRUS INFECTIONS
Provided herein are compounds, pharmaceutical compositions, and methods for treating a SARS-CoV-2 infection.
N-(4-HYDROXY-4-METHYL-CYCLOHEXYL)-4-PHENYL-BENZENESULFONAMIDE AND N-(4-HYDROXY-4-METHYL-CYCLOHEXYL)-4-(2-PYRIDYL)-BENZENESULFONAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain substituted N-(4-hydroxy-4-methyl-cyclohexyl)-4-phenyl-benzenesulfonamide and N-(4-hydroxy-4-methyl-cyclohexyl)-4-(2-pyridyl)benzenesulfonamide compounds (collectively referred to herein as HMC compounds) that are useful, for example, in the treatment of disorders (e.g., diseases) including, inflammation and/or joint destruction and/or bone loss; disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; inflammatory and autoimmune disorders, for example, rheumatoid arthritis; psoriasis; psoriatic arthritis; chronic obstructive pulmonary disease (COPD); asthma; atherosclerosis; inflammatory bowel disease; ankylosing spondylitis; multiple sclerosis; systemic lupus erythematosus; Sjogren's syndrome; a disorder associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, or Paget's disease; cancer, such as a haematological malignancy, such as multiple myeloma, leukemia, or lymphoma, or a solid tumour cancer, such as bladder cancer, breast cancer (female and/or male), colon cancer, renal cell carcinoma, kidney cancer, lung cancer, pancreatic cancer, gastric cancer, prostate cancer, brain cancer, skin cancer, thyroid cancer, basal cell ameloblastoma, or melanoma; a disorder associated with fibrosis, such as systemic sclerosis or scleroderma; or a rare vasculitide, such as Behçet's disease. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, for example, in therapy.
N-(4-HYDROXY-4-METHYL-CYCLOHEXYL)-4-PHENYL-BENZENESULFONAMIDE AND N-(4-HYDROXY-4-METHYL-CYCLOHEXYL)-4-(2-PYRIDYL)-BENZENESULFONAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain substituted N-(4-hydroxy-4-methyl-cyclohexyl)-4-phenyl-benzenesulfonamide and N-(4-hydroxy-4-methyl-cyclohexyl)-4-(2-pyridyl)benzenesulfonamide compounds (collectively referred to herein as HMC compounds) that are useful, for example, in the treatment of disorders (e.g., diseases) including, inflammation and/or joint destruction and/or bone loss; disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; inflammatory and autoimmune disorders, for example, rheumatoid arthritis; psoriasis; psoriatic arthritis; chronic obstructive pulmonary disease (COPD); asthma; atherosclerosis; inflammatory bowel disease; ankylosing spondylitis; multiple sclerosis; systemic lupus erythematosus; Sjogren's syndrome; a disorder associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, or Paget's disease; cancer, such as a haematological malignancy, such as multiple myeloma, leukemia, or lymphoma, or a solid tumour cancer, such as bladder cancer, breast cancer (female and/or male), colon cancer, renal cell carcinoma, kidney cancer, lung cancer, pancreatic cancer, gastric cancer, prostate cancer, brain cancer, skin cancer, thyroid cancer, basal cell ameloblastoma, or melanoma; a disorder associated with fibrosis, such as systemic sclerosis or scleroderma; or a rare vasculitide, such as Behçet's disease. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, for example, in therapy.
Charged ion channel blockers and methods for use
The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: ##STR00001##
The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.
Novel Fungicidal Pyridylamidines
The invention relates to compounds 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 and R.sup.10 are as defined in the claims. The invention further provides compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
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