Patent classifications
C07D277/06
Imaging composition and uses thereof
The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.
Substituted pyrrolidines as G-protein coupled receptor 43 agonists
The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases. ##STR00001##
Substituted pyrrolidines as G-protein coupled receptor 43 agonists
The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases. ##STR00001##
EP300/CREBBP INHIBITOR
The present invention provides a compound having excellent histone acetyl transferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof:
##STR00001## wherein ring Q.sup.1, ring Q.sup.2, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 respectively have the same meanings as defined in the specification.
Inhibition of glutaminase C
The present invention relates to a method of reducing the production of glutamate from glutamine by glutaminase C in a cell or tissue. The method involves inhibiting glutaminase C activity in the cell or tissue under conditions effective to reduce production of glutamate from glutamine. Compounds for carrying out this method are also disclosed.
Inhibition of glutaminase C
The present invention relates to a method of reducing the production of glutamate from glutamine by glutaminase C in a cell or tissue. The method involves inhibiting glutaminase C activity in the cell or tissue under conditions effective to reduce production of glutamate from glutamine. Compounds for carrying out this method are also disclosed.
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
The invention provides compounds having the general Formula (I);
##STR00001##
and pharmaceutically acceptable salts thereof; wherein the variables R.sup.A, R.sup.AA, subscript n, subscript q, ring A, X.sup.2, L, subscript m, X.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, D and E have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
The invention provides compounds having the general Formula (I);
##STR00001##
and pharmaceutically acceptable salts thereof; wherein the variables R.sup.A, R.sup.AA, subscript n, subscript q, ring A, X.sup.2, L, subscript m, X.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, D and E have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
N-HETEROCYCLIC COMPOUNDS USED AS NITRIFICATION INHIBITOR
The use of an N-heterocyclic compound of the general formula (a) or (b) with the following definitions: X.sup.1 being S or X.sup.2 being S or O and at least one of X.sup.1 and X.sup.2 being S R.sup.2 H or C.sub.1-4-alkyl, R.sup.3 H or C.sub.1-4-alkyl R.sup.6 and R.sup.7 are hydrogen or together form a covalent carbon-carbon bond in general formula (a) R.sup.1 being H, C.sub.1-12-alkyl or CH.sub.2NR.sup.4R.sub.5 with R.sup.4 hydrogen or C.sub.1-4-alkyl, R.sup.5 C.sub.1-12-hydrocarbon residue which can contain one to three halogen atoms and/or one to four heteroatoms, selected from the group consisting of nitro-gen, oxygen and sulfur, it also being possible for R.sup.4 and R.sup.5, together with the nitrogen atom joining them, to form a 5- or 6-membered saturated or unsaturated heterocyclic radical, which optionally may also contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, in general formula (b) R.sup.1 being H or C.sub.1-17-hydrocarbon, preferably H, or CH.sub.2R.sup.5 with R.sup.5 being H or C.sub.1-16-hydrocarbon residue, which hydrocarbon can contain one to three halogen atoms and/or one to six heteroatoms, selected from the group consisting of nitrogen, oxygen and sulfur, and preferably in general formula (a) and (b) X.sup.1 and X.sup.2 being S, as nitrification inhibitor.
##STR00001##
N-HETEROCYCLIC COMPOUNDS USED AS NITRIFICATION INHIBITOR
The use of an N-heterocyclic compound of the general formula (a) or (b) with the following definitions: X.sup.1 being S or X.sup.2 being S or O and at least one of X.sup.1 and X.sup.2 being S R.sup.2 H or C.sub.1-4-alkyl, R.sup.3 H or C.sub.1-4-alkyl R.sup.6 and R.sup.7 are hydrogen or together form a covalent carbon-carbon bond in general formula (a) R.sup.1 being H, C.sub.1-12-alkyl or CH.sub.2NR.sup.4R.sub.5 with R.sup.4 hydrogen or C.sub.1-4-alkyl, R.sup.5 C.sub.1-12-hydrocarbon residue which can contain one to three halogen atoms and/or one to four heteroatoms, selected from the group consisting of nitro-gen, oxygen and sulfur, it also being possible for R.sup.4 and R.sup.5, together with the nitrogen atom joining them, to form a 5- or 6-membered saturated or unsaturated heterocyclic radical, which optionally may also contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, in general formula (b) R.sup.1 being H or C.sub.1-17-hydrocarbon, preferably H, or CH.sub.2R.sup.5 with R.sup.5 being H or C.sub.1-16-hydrocarbon residue, which hydrocarbon can contain one to three halogen atoms and/or one to six heteroatoms, selected from the group consisting of nitrogen, oxygen and sulfur, and preferably in general formula (a) and (b) X.sup.1 and X.sup.2 being S, as nitrification inhibitor.
##STR00001##