C07D207/50

COMPOUNDS CONTAINING S-N-VALERYL-N-{[2'-(1H-TETRAZOLE-5-YL)-BIPHENYL-4-YL]-METHYL}-VALINE AND (2R,4S)-5-BIPHENYL-4-YL-4-(3-CARBOXY-PROPIONYLAMINO)-2-METHYL-PENTANOIC ACID ETHYL ESTER MOIETIES AND CATIONS

A compound comprising of the angiotensin receptor antagonist (ARB) valsartan, the neutral endopeptidase inhibitor (NEPi) (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methylpentanoic acid ethyl ester and one or more monovalent cations such as Na.sup.+ useful for the treatment of hypertension and/or heart failure.

NITRIC OXIDE DONORS

The present invention provides, in part a novel class of nonoate compounds which exhibit nitric oxide releasing activity and their pharmaceutically acceptable salts, esters and prodrugs. The compounds release nitric oxide upon activation by contact with plasma. The present invention also relates to the use of the disclosed compounds to deliver nitric oxide to treat disorders arising from nitric oxide dysregulation.

NITRIC OXIDE DONORS

The present invention provides, in part a novel class of nonoate compounds which exhibit nitric oxide releasing activity and their pharmaceutically acceptable salts, esters and prodrugs. The compounds release nitric oxide upon activation by contact with plasma. The present invention also relates to the use of the disclosed compounds to deliver nitric oxide to treat disorders arising from nitric oxide dysregulation.

ACTIVATION OF CARBONYL BETA-CARBONS FOR CHEMICAL TRANSFORMATIONS
20190337955 · 2019-11-07 ·

The present invention relates to a method for synthesizing a compound of Formula (I)

##STR00001## as defined herein, comprising: (i) activating a compound of Formula (II)

##STR00002## as defined herein, by reacting said compound of Formula (II) with a compound of Formula (III)

##STR00003## as defined herein, in the presence of a base, to obtain a compound of Formula (IV)

##STR00004## as defined herein; and (ii) reacting the compound of Formula (IV) with an electrophile to obtain the compound of Formula (I). The present invention further relates to the organocatalysts used in the described methods and their respective uses.

ACTIVATION OF CARBONYL BETA-CARBONS FOR CHEMICAL TRANSFORMATIONS
20190337955 · 2019-11-07 ·

The present invention relates to a method for synthesizing a compound of Formula (I)

##STR00001## as defined herein, comprising: (i) activating a compound of Formula (II)

##STR00002## as defined herein, by reacting said compound of Formula (II) with a compound of Formula (III)

##STR00003## as defined herein, in the presence of a base, to obtain a compound of Formula (IV)

##STR00004## as defined herein; and (ii) reacting the compound of Formula (IV) with an electrophile to obtain the compound of Formula (I). The present invention further relates to the organocatalysts used in the described methods and their respective uses.

Derivatives of pyrrole-2,5-diones having a fungicidal activity, their agronomical compositions and use thereof

Derivatives of pyrrole-2,5-diones having formula (I): (I) are described, together with agronomic compositions containing said derivatives having formula (I) and the use thereof for the control of phytopathogenic fungi in agricultural crops. ##STR00001##

Derivatives of pyrrole-2,5-diones having a fungicidal activity, their agronomical compositions and use thereof

Derivatives of pyrrole-2,5-diones having formula (I): (I) are described, together with agronomic compositions containing said derivatives having formula (I) and the use thereof for the control of phytopathogenic fungi in agricultural crops. ##STR00001##

SUBSTITUTED PYRROLIDINES AS FACTOR XIA INHIBITORS FOR THE TREATMENT THROMBOEMBOLIC DISEASES

The present invention provides compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof (wherein the substituents are as defined in the description). The compounds of the general formula (I) are inhibitors of factor XIa, and are useful in the prevention of and/or therapy for thromboembolic diseases.

##STR00001##

SUBSTITUTED PYRROLIDINES AS FACTOR XIA INHIBITORS FOR THE TREATMENT THROMBOEMBOLIC DISEASES

The present invention provides compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof (wherein the substituents are as defined in the description). The compounds of the general formula (I) are inhibitors of factor XIa, and are useful in the prevention of and/or therapy for thromboembolic diseases.

##STR00001##

CARBOCYCLIC PROLINAMIDE DERIVATIVES

This invention is directed to novel carbocyclic prolinamide derivatives of Formula (I), and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention. The compounds of the invention are inhibitors of HTRA1. Thus, the compounds of the invention are useful in the prevention and treatment of a wide range of diseases mediated (in whole or in part) by HTRA1. The compounds of the invention are also useful for inhibiting HTRA1 protease activity in an eye or locus of an arthritis or related condition.

##STR00001##