C07D207/46

Guanidine compounds and use thereof

The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer, by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.

Plant growth inhibiting agent, and plant growth inhibiting method using same

An object of the present invention is to provide a novel plant growth inhibiting agent and a plant growth inhibiting method using the same. The plant growth inhibiting agent of the present invention comprises, as an active ingredient, a compound represented by the following formula (I′) and/or a salt thereof. In the formula (I′), R.sup.1a represents a substituted or unsubstituted C.sub.1 to C.sub.20 alkyl group, a substituted or unsubstituted C.sub.6 to C.sub.14 aryl group, a substituted or unsubstituted C.sub.3 to C.sub.13 heteroaryl group, or the like; R.sup.2 represents a substituted or unsubstituted C.sub.1 to C.sub.20 alkylene group, a substituted or unsubstituted C.sub.6 to C.sub.14 arylene group, or the like; R.sup.3a represents OH, a substituted or unsubstituted C.sub.1 to C.sub.6 alkoxy group, or the like; X represents an oxygen atom; Y represents a substituent; q represents any integer of 0 to 3; n represents 0 or 1; and m represents 0 or 1. ##STR00001##

Plant growth inhibiting agent, and plant growth inhibiting method using same

An object of the present invention is to provide a novel plant growth inhibiting agent and a plant growth inhibiting method using the same. The plant growth inhibiting agent of the present invention comprises, as an active ingredient, a compound represented by the following formula (I′) and/or a salt thereof. In the formula (I′), R.sup.1a represents a substituted or unsubstituted C.sub.1 to C.sub.20 alkyl group, a substituted or unsubstituted C.sub.6 to C.sub.14 aryl group, a substituted or unsubstituted C.sub.3 to C.sub.13 heteroaryl group, or the like; R.sup.2 represents a substituted or unsubstituted C.sub.1 to C.sub.20 alkylene group, a substituted or unsubstituted C.sub.6 to C.sub.14 arylene group, or the like; R.sup.3a represents OH, a substituted or unsubstituted C.sub.1 to C.sub.6 alkoxy group, or the like; X represents an oxygen atom; Y represents a substituent; q represents any integer of 0 to 3; n represents 0 or 1; and m represents 0 or 1. ##STR00001##

Substituted alkylphenols as HCN1 antagonists

Provided herein are compounds (e.g., compounds of Formula (I) and Formula (II), that modulate HCN channels, intermembrane proteins that serve as nonselective voltage-gated cation channels in the plasma membranes of heart and brain cells. Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating HCN-related disorders (e.g., pain) with the compounds in a subject, by administering the compounds and/or compositions described herein.

BRANCHED TYPE HETERO MONODISPERSED POLYETHYLENE GLYCOL, PRODUCTION METHOD THEREOF, AND CONJUGATE THEREOF

An intermediate for production of a branched type hetero monodispersed polyethylene glycol which is represented by formula (2), the intermediate being represented by formula (3) or (40):

##STR00001##

where X.sup.1, L.sup.1, L.sup.3, Y.sup.1, Y.sup.2, and n are as defined herein.

Tunable fluorescence using cleavable linkers

The invention relates to cleavable chemistry in general, and in particular, to tunable fluorescence using cleavable linkers present in fluorochrome-quencher conjugates.

Tunable fluorescence using cleavable linkers

The invention relates to cleavable chemistry in general, and in particular, to tunable fluorescence using cleavable linkers present in fluorochrome-quencher conjugates.

Prosthetic compounds for labeling internalizing biomolecules
09839704 · 2017-12-12 · ·

Prosthetic compounds are disclosed that are effective for radiolabeling biomolecules with 18F. Representative biomolecules include antibodies (e.g., monoclonal antibodies (mAbs) and nanobodies (sdAbs)), antibody fragments, and peptides that may have an affinity for particular types of cells, such as cancer cells. The prosthetic compounds effectively address the art-recognized difficulties associated with the retention of radioactivity within the targeted cells, due to internalization of the biomolecule, followed by proteolytic degradation. Representative prosthetic compounds include (i) a succinimidyloxycarbonyl moiety, (ii) a radioactive moiety bearing 18F, and (iii) a charged moiety, i.e., a moiety that is charged under the physiological conditions of the internal cell environment.

Prosthetic compounds for labeling internalizing biomolecules
09839704 · 2017-12-12 · ·

Prosthetic compounds are disclosed that are effective for radiolabeling biomolecules with 18F. Representative biomolecules include antibodies (e.g., monoclonal antibodies (mAbs) and nanobodies (sdAbs)), antibody fragments, and peptides that may have an affinity for particular types of cells, such as cancer cells. The prosthetic compounds effectively address the art-recognized difficulties associated with the retention of radioactivity within the targeted cells, due to internalization of the biomolecule, followed by proteolytic degradation. Representative prosthetic compounds include (i) a succinimidyloxycarbonyl moiety, (ii) a radioactive moiety bearing 18F, and (iii) a charged moiety, i.e., a moiety that is charged under the physiological conditions of the internal cell environment.

Dendritic core compounds

The invention relates to compounds that are useful for the preparation of dendrimer compounds, the use of these compounds for preparing dendrimers and processes for preparing the compounds.