C07C257/18

Blood brain barrier-penetrating oximes for cholistenerases reactivation

The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.

LINKED DIARYL COMPOUNDS WITH ANTICANCER PROPERTIES AND METHODS OF USING THE SAME

Provided are compositions comprising linked diaryl compounds that possess anticancer properties. Methods of use are also disclosed herein. The method comprises administering an effective amount of a compound described herein to an individual in need thereof.

LINKED DIARYL COMPOUNDS WITH ANTICANCER PROPERTIES AND METHODS OF USING THE SAME

Provided are compositions comprising linked diaryl compounds that possess anticancer properties. Methods of use are also disclosed herein. The method comprises administering an effective amount of a compound described herein to an individual in need thereof.

MODULATORS OF THE RELAXIN RECEPTOR 1

Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R.sup.1, and R.sup.2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.

##STR00001##

Benzamides and related inhibitors of factor XA

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

Benzamides and related inhibitors of factor XA

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

Metal complex with a bridged cyclopentadienyl amidine ligand

The present invention relates to a new metal complex of the formula (1) ##STR00001## wherein: M is a group 4-6 metal R.sup.1 means is a substituent comprising a heteroatom of group 15, through which R.sup.1 is bonded to the imine carbon atom; R.sup.2-R.sup.5 are the same or different and each represents a hydrogen atom, an optionally substituted C1-10 alkyl group, an optionally substituted C1-10 alkoxy group, an optionally substituted C6-20 aryl group, an optionally substituted C6-20 aryloxy group, an optionally substituted C7-20 aralkyl group, an optionally substituted C7-20 aralkyloxy group, a silyl group substituted with optionally substituted C1-20 hydrocarbon group(s), a C1-20 hydrocarbon-substituted amino group or the adjacent R.sup.2-R.sup.5 may be linked to each other to form a ring; R.sup.6-R.sup.9 are the same or different and each represents a hydrogen atom, a halogen atom, an optionally substituted C1-10 alkyl group, an optionally substituted C1-10 alkoxy group, an optionally substituted C6-20 aryl group, an optionally substituted C6-20 aryloxy group, an optionally substituted C7-20 aralkyl group, an optionally substituted C7-20 aralkyloxy group, a silyl group substituted with optionally substituted C1-20 hydrocarbon group(s), a C1-20 hydrocarbon-substituted amino group or the adjacent R.sup.6-R.sup.9 may be linked to each other to form a ring; L is an optional neutral Lewis basic ligand, and j is an integer denoting the number of neutral ligands L; and X Is an anionic ligand, and r is an integer denoting the number of anionic ligands X.

Metal complex with a bridged cyclopentadienyl amidine ligand

The present invention relates to a new metal complex of the formula (1) ##STR00001## wherein: M is a group 4-6 metal R.sup.1 means is a substituent comprising a heteroatom of group 15, through which R.sup.1 is bonded to the imine carbon atom; R.sup.2-R.sup.5 are the same or different and each represents a hydrogen atom, an optionally substituted C1-10 alkyl group, an optionally substituted C1-10 alkoxy group, an optionally substituted C6-20 aryl group, an optionally substituted C6-20 aryloxy group, an optionally substituted C7-20 aralkyl group, an optionally substituted C7-20 aralkyloxy group, a silyl group substituted with optionally substituted C1-20 hydrocarbon group(s), a C1-20 hydrocarbon-substituted amino group or the adjacent R.sup.2-R.sup.5 may be linked to each other to form a ring; R.sup.6-R.sup.9 are the same or different and each represents a hydrogen atom, a halogen atom, an optionally substituted C1-10 alkyl group, an optionally substituted C1-10 alkoxy group, an optionally substituted C6-20 aryl group, an optionally substituted C6-20 aryloxy group, an optionally substituted C7-20 aralkyl group, an optionally substituted C7-20 aralkyloxy group, a silyl group substituted with optionally substituted C1-20 hydrocarbon group(s), a C1-20 hydrocarbon-substituted amino group or the adjacent R.sup.6-R.sup.9 may be linked to each other to form a ring; L is an optional neutral Lewis basic ligand, and j is an integer denoting the number of neutral ligands L; and X Is an anionic ligand, and r is an integer denoting the number of anionic ligands X.

Benzamide Compounds and Related Methods of Use

Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.

Class A GPCR-binding compound modifier
12275687 · 2025-04-15 · ·

To provide a novel class-A GPCR antagonist, a production method therefor, or a novel compound that interacts with a Na.sup.+-water cluster binding site of a class-A GPCR. Used is a compound or a salt thereof comprising a structure comprising a class-A GPCR-binding compound linked to a functional group that can bind to a Na.sup.+-water cluster binding site of the class-A GPCR. Also used is a method for producing a class-A GPCR antagonist, comprising the step of linking one compound with another compound that can bind to a Na.sup.+-water cluster binding site of the class-A GPCR.