Patent classifications
C07D211/44
Modulators of potassium ion and TRPV1 channels and uses thereof
Novel compounds usable in modulating an activity or function of a voltage-dependent potassium channel and/or of TRPV1 are provided. The compounds are represented by Formula I as described and defined in the specification.
Nitroso compounds as nitroxyl donors and methods of use thereof
The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
Nitroso compounds as nitroxyl donors and methods of use thereof
The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
COMPOUNDS USEFUL FOR INHIBITING RAF DIMERS
The disclosure provides compounds of Formula I (Formula I) (c) And the pharmaceutically acceptable salts thereof. The A, B, C, and D rings and the variables R.sup.A, R.sup.B, R.sup.C, R.sup.D, L.sub.0, L.sub.1, L.sub.2, and L.sub.2, are defined herein. Compounds and salts of Formula I are useful as inhibitors of RAF kinase dimerization, including dimerization of wild type and mutant BRAF kinases. The disclosure includes pharmaceutical compositions comprising a compound or salt of Formula I. The disclosure also includes methods of treating a cancer susceptible to treatment with an inhibitor of BRAF dimers or BRAF dimerization, comprising administering a therapeutically effective amount of a compound or salt of Formula I to a patient in need of such treatment. These cancers susceptible to treatment with an inhibitor of BRAF dimers or BRAF dimerization include melanoma, thyroid cancer, hairy cell leukemia, ovarian cancer, lung cancer, and colorectal cancer.
##STR00001##
Fluorinated benzilic acid ester compound and salt thereof
A benzilic acid ester compound represented by the following formula (I) or a salt thereof, ##STR00001## wherein R represents optionally substituted fluorinated lower alkyl, is disclosed.
Fluorinated benzilic acid ester compound and salt thereof
A benzilic acid ester compound represented by the following formula (I) or a salt thereof, ##STR00001## wherein R represents optionally substituted fluorinated lower alkyl, is disclosed.
Hepatitis B capsid assembly modulators
Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.
REMODILINS FOR AIRWAY REMODELING AND ORGAN FIBROSIS
Disclosed herein is a class of molecules termed remodilins that are effective in treating asthma, pulmonary fibrosis, and associated disorders. The molecules ameliorate asthma and pulmonary fibrosis symptoms by various mechanisms, including inhibiting airway smooth muscle contractile protein accumulation, reducing airway constrictor hyperresponsiveness, inhibiting bronchial fibroblast transformation into myofibroblasts, and/or treating or preventing airway or pulmonary fibrosis.
MODIFIED AMINE LIPIDS
The disclosure provides ionizable amine lipids and salts thereof (e.g., pharmaceutically acceptable salts thereof) useful for the delivery of biologically active agents, for example delivering biologically active agents to cells to prepare engineered cells. The ionizable amine lipids disclosed herein are useful as ionizable lipids in the formulation of lipid nanoparticle-based compositions.
METHOD FOR PRODUCING KAKEROMYCIN AND DERIVATIVES THEREOF
Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1):
##STR00001##
wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2):
##STR00002##
wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.