Patent classifications
C07D317/66
Antagonists of the glucagon receptor
The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof and pharmaceutical compositions comprising the same.
SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof:
##STR00001##
wherein Q is selected from O, S and Se; J is S or Se; W.sup.1 and W.sup.2, when present, are independently selected from N and C; R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, C.sub.1-C.sub.12 alkyl, C.sub.2-C.sub.12 alkenyl, C.sub.2-C.sub.12 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, cycloalkenyl, amino, amido, alkylthio, acyl, arylalkyl and acylamido, all of which may be optionally substituted; and wherein at least one of W.sup.1 and W.sup.2 is present and is a nitrogen atom and when R.sup.1 or R.sup.2 are cyclic then the respective W.sup.1 or W.sup.2 may form part of the ring structure. The present invention also relates to pharmaceutical compositions including such compounds, to methods of treatment using such compounds, in particular in relation to NLRP3 inflammasome mediated disorders, and to associated diagnostic uses.
SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof:
##STR00001##
wherein Q is selected from O, S and Se; J is S or Se; W.sup.1 and W.sup.2, when present, are independently selected from N and C; R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, C.sub.1-C.sub.12 alkyl, C.sub.2-C.sub.12 alkenyl, C.sub.2-C.sub.12 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, cycloalkenyl, amino, amido, alkylthio, acyl, arylalkyl and acylamido, all of which may be optionally substituted; and wherein at least one of W.sup.1 and W.sup.2 is present and is a nitrogen atom and when R.sup.1 or R.sup.2 are cyclic then the respective W.sup.1 or W.sup.2 may form part of the ring structure. The present invention also relates to pharmaceutical compositions including such compounds, to methods of treatment using such compounds, in particular in relation to NLRP3 inflammasome mediated disorders, and to associated diagnostic uses.
COOL-SENSATION IMPARTER COMPOSITION CONTAINING 2,2,6-TRIMETHYLCYCLOHEXANECARBOXYLIC ACID DERIVATIVE
A cooling agent composition contains a 2,2,6-trimethylcyclohexanecarboxylic acid derivative represented by the following general formula (1). The symbol * represents an asymmetric carbon atom. X represents NH, N(ZAr.sup.2), O or S, Z represents a single bond or an alkylene group having 1 to 3 carbon atoms which may have a substituent, Ar.sup.2 represents an aryl group having 6 to 20 carbon atoms which may have a substituent or an aromatic heterocyclic group having 2 to 15 carbon atoms which may have a substituent. Y each independently represents a methylene group which may have a substituent, and n represents an integer of 0 to 3. Ar.sup.1 represents an aryl group having 6 to 20 carbon atoms which may have a substituent or an aromatic heterocyclic group having 2 to 15 carbon atoms which may have a substituent.
##STR00001##
GROUP 5 METAL COMPLEXES FOR CATALYTIC AMINE FUNCTIONALIZATION
This application pertains to group 5 metal complexes having the structure of Formula I:
##STR00001##
and their potential utility in catalyzing -alkylation of secondary amine-containing moieties.
COMPOUNDS AND METHODS FOR INDUCING CHONDROGENESIS
Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.
COMPOUNDS AND METHODS FOR INDUCING CHONDROGENESIS
Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.
Antagonists of T2R54 and compositions and uses thereof
The present disclosure generally provides compounds that antagonize certain T2R taste receptors, including related uses, methods, and compositions for the reduction of bitter taste and/or the enhancement of sweet taste. In certain aspects, the disclosure provides flavored articles or flavored compositions comprising such compounds, as well as uses of such compounds to reduce the bitter taste and/or enhance the sweet taste of such flavored articles or flavored compositions.
Antagonists of T2R54 and compositions and uses thereof
The present disclosure generally provides compounds that antagonize certain T2R taste receptors, including related uses, methods, and compositions for the reduction of bitter taste and/or the enhancement of sweet taste. In certain aspects, the disclosure provides flavored articles or flavored compositions comprising such compounds, as well as uses of such compounds to reduce the bitter taste and/or enhance the sweet taste of such flavored articles or flavored compositions.
ANTIFUNGAL COMPOUNDS AND USES THEREOF
Provided herein are compounds (e.g., compounds of Formulae (I), (II), and (III)) which are anti-fungal agents and can be used in the treatment of diseases, including infectious diseases. The invention provides methods of treating diseases in a subject (e.g., infectious diseases such as fungal infections), and methods of killing or inhibiting the growth of fungi in or on a subject or biological sample. The compounds may be used in subjects, in clinical settings, or in agricultural settings.
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