Patent classifications
C07D295/20
MODULATORS OF VASOPRESSIN RECEPTORS WITH THERAPEUTIC POTENTIAL
Compounds comprising piperazines, piperidines, spiro-furanopiperidines, and analogs thereof are provided that are modulators, such as positive allosteric modulators, of one or more subclasses of vasopressin receptors. The compounds can be selective modulators of one or more subclasses of vasopressin receptors. Compounds of the invention can be used in the treatment of a condition wherein modulating a vasopressin receptor is medically indicated for treatment of the condition.
MODULATORS OF VASOPRESSIN RECEPTORS WITH THERAPEUTIC POTENTIAL
Compounds comprising piperazines, piperidines, spiro-furanopiperidines, and analogs thereof are provided that are modulators, such as positive allosteric modulators, of one or more subclasses of vasopressin receptors. The compounds can be selective modulators of one or more subclasses of vasopressin receptors. Compounds of the invention can be used in the treatment of a condition wherein modulating a vasopressin receptor is medically indicated for treatment of the condition.
Carbocyclic sulfone RORγ modulators
Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders. ##STR00001##
Carbocyclic sulfone RORγ modulators
Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders. ##STR00001##
SULFONAMIDE DERIVATIVES AND THEIR USE AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS
The present invention relates to compounds of formulae I and II. The compounds are useful for treating hypertension, atherosclerosis, pulmonary diseases, diabetes, pain, fibrosis, addictive disorders, inflammation, and immunological disorders or a condition treatable or preventable by inhibition of soluble epoxide hydrolase. Preferred compounds are N-((adamantan-1-yl)carbamoyl)-benzenesulfonamide derivatives. Exemplary compounds are e.g. N(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)-4-methylbenzenesulfonamide (example 14, compound 4a) 4-(tert-butyl)-N(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)benzenesulfonamide (example 15, compound 4b) N(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)-4-(trifluoromethyl)benzenesulfonamide (example 16, compound 4j). The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof.
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Guanidine compound
[Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.
Guanidine compound
[Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.