Patent classifications
C07D237/24
Pyridazinone and pyridone compounds
The invention relates to pyridazinone and pyridone compounds having formula (I) or (I′), and pharmaceutically acceptable salts, hydrates, and solvates thereof ##STR00001##
wherein R.sub.1/R.sub.4 and X and X.sub.3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.
Pyridazinone and pyridone compounds
The invention relates to pyridazinone and pyridone compounds having formula (I) or (I′), and pharmaceutically acceptable salts, hydrates, and solvates thereof ##STR00001##
wherein R.sub.1/R.sub.4 and X and X.sub.3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.
Novel method for the production of 18F-labeled active esters and their application exemplified by the preparation of a PSMA-specific PET-tracer
Novel efficient, time-saving and reliable radiofluorination procedures for the production of .sup.18F-labelled active esters via nucleophilic substitution of the corresponding onium precursors with .sup.18F.sup.− are described. The active ester including [.sup.18F]F-Py-TFP and [.sup.18F]TFB produced by one of these methods was used to prepare PSMA-specific PET tracers such as [.sup.18F]DCFPyL. The key advantages of these inventive methods are efficiency, short time of preparation and excellent amenability to automation. A pharmaceutical composition containing at least one PSMA-specific PET tracers prepared by the inventive method is useful for positron emission tomography (PET) imaging, especially imaging prostate tumor.
Novel method for the production of 18F-labeled active esters and their application exemplified by the preparation of a PSMA-specific PET-tracer
Novel efficient, time-saving and reliable radiofluorination procedures for the production of .sup.18F-labelled active esters via nucleophilic substitution of the corresponding onium precursors with .sup.18F.sup.− are described. The active ester including [.sup.18F]F-Py-TFP and [.sup.18F]TFB produced by one of these methods was used to prepare PSMA-specific PET tracers such as [.sup.18F]DCFPyL. The key advantages of these inventive methods are efficiency, short time of preparation and excellent amenability to automation. A pharmaceutical composition containing at least one PSMA-specific PET tracers prepared by the inventive method is useful for positron emission tomography (PET) imaging, especially imaging prostate tumor.
Herbicidally active 2-(substituted-phenyl)-cyclopentane-1,3-dione compounds and derivatives thereof
The present invention relates to a compound of formula (I): wherein the substituents are as defined herein, and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are thought to be suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof. ##STR00001##
Herbicidally active 2-(substituted-phenyl)-cyclopentane-1,3-dione compounds and derivatives thereof
The present invention relates to a compound of formula (I): wherein the substituents are as defined herein, and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are thought to be suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof. ##STR00001##
NOVEL NON-CODING HETEROCYCLIC AMINO ACIDS (NCHAA) AND THEIR USE AS HERBICIDES
The invention relates to a novel substituted amino acids, agricultural compositions comprising the novel substituted amino acids, and their use for controlling undesired plant growth alone or in combination with crop protection agents such as pesticides or plant growth regulators.
HERBICIDAL COMPOUNDS
Use of the compounds of the formula (I) wherein the substituents are as defined herein as herbicides. Compounds of formula (I) are also claimed.
##STR00001##
HERBICIDAL COMPOUNDS
Use of the compounds of the formula (I) wherein the substituents are as defined herein as herbicides. Compounds of formula (I) are also claimed.
##STR00001##
CRYSTAL FORM OF 6-(CYCLOPROPANECARBOXAMIDO)-4-((2-METHOXY-3-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)AMINO)-N-(METHYL-D3) PYRIDAZINE-3-CARBOXAMIDE
Disclosed is crystalline Form A of 6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl) amino)-N-(methyl-d.sub.3)pyridazine-3-carboxamide. Form A is a neat crystalline form. Characterization data for Form A are disclosed.