Patent classifications
A61K31/53
METHODS OF SYNTHESIZING THYROID HORMONE ANALOGS AND POLYMORPHS THEREOF
The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.
PHARMACEUTICAL COMPOSITION FOR TREATING FATTY LIVER DISEASE
Provided is a pharmaceutical composition for treating and/or preventing fatty liver disease, particularly nonalcoholic fatty liver disease, the pharmaceutical composition having an excellent ACC2-selective inhibitory action and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration.
A pharmaceutical composition for treating and/or preventing fatty liver disease, the pharmaceutical composition comprising a compound represented by Formula (I):
##STR00001## wherein R.sup.1 is haloalkyl or non-aromatic carbocyclyl, R.sup.2 is a hydrogen atom or halogen, R.sup.3 is halogen, ring A is a group represented by the formula:
##STR00002## -L.sup.1- is —O—(CH.sub.2)—, —(CH.sub.2).sub.2—, or the like, R.sup.4 is alkyl or haloalkyl, and R.sup.5 is alkylcarbonyl or carbamoyl, or a pharmaceutically acceptable salt thereof.
PHARMACEUTICAL COMPOSITION FOR TREATING FATTY LIVER DISEASE
Provided is a pharmaceutical composition for treating and/or preventing fatty liver disease, particularly nonalcoholic fatty liver disease, the pharmaceutical composition having an excellent ACC2-selective inhibitory action and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration.
A pharmaceutical composition for treating and/or preventing fatty liver disease, the pharmaceutical composition comprising a compound represented by Formula (I):
##STR00001## wherein R.sup.1 is haloalkyl or non-aromatic carbocyclyl, R.sup.2 is a hydrogen atom or halogen, R.sup.3 is halogen, ring A is a group represented by the formula:
##STR00002## -L.sup.1- is —O—(CH.sub.2)—, —(CH.sub.2).sub.2—, or the like, R.sup.4 is alkyl or haloalkyl, and R.sup.5 is alkylcarbonyl or carbamoyl, or a pharmaceutically acceptable salt thereof.
ALLOSTERIC EGFR INHIBITORS AND METHODS OF USE THEREOF
The disclosure relates to compounds that act as allosteric inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.
ALLOSTERIC EGFR INHIBITORS AND METHODS OF USE THEREOF
The disclosure relates to compounds that act as allosteric inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.
Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection
The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections. ##STR00001## X is selected from the group consisting of O and H; R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl, and R.sup.2 is selected from (C.sub.1 to C.sub.10) alkyl, (C.sub.1 to C.sub.10) alkenyl, (C.sub.1 to C.sub.10) alkynyl, (C.sub.3 to C.sub.10) cycloalkyl, and (C.sub.5 to C.sub.10) cycloalkenyl, and NR.sup.3aR.sup.3b is defined in the specification. These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.
Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection
The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections. ##STR00001## X is selected from the group consisting of O and H; R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl, and R.sup.2 is selected from (C.sub.1 to C.sub.10) alkyl, (C.sub.1 to C.sub.10) alkenyl, (C.sub.1 to C.sub.10) alkynyl, (C.sub.3 to C.sub.10) cycloalkyl, and (C.sub.5 to C.sub.10) cycloalkenyl, and NR.sup.3aR.sup.3b is defined in the specification. These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.
Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection
The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections. ##STR00001## X is selected from the group consisting of O and H; R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl, and R.sup.2 is selected from (C.sub.1 to C.sub.10) alkyl, (C.sub.1 to C.sub.10) alkenyl, (C.sub.1 to C.sub.10) alkynyl, (C.sub.3 to C.sub.10) cycloalkyl, and (C.sub.5 to C.sub.10) cycloalkenyl, and NR.sup.3aR.sup.3b is defined in the specification. These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.
TRIAZINE DERIVATIVES HAVING VIRUS REPLICATION INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same. Furthermore, the present invention provides a crystalline form useful as an active pharmaceutical ingredient, and a pharmaceutical composition comprising the same.
A compound represented by Formula:
##STR00001##
, or a pharmaceutically acceptable salt thereof.
PYRROLO[2,1-F][1,2,4]TRIAZINE DERIVATIVE AND USE THEREOF
The present disclosure provides a compound, which is a compound of Formula (I) or a stereoisomer, a tautomer, a N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound of Formula (I):
##STR00001##