C07D307/87

Quaternary ammonium salt prodrugs

The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X.sup.. In one embodiment, the present invention provides a prodrug compound of Formula I: ##STR00001##
where R.sub.1-R.sub.5 are defined in the written description of the invention. The prodrug compounds of the invention can be used to treat any condition for which the tertiary amine-containing parent drug or tertiary imine-containing parent drug is useful as a treatment.

Quaternary ammonium salt prodrugs

The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X.sup.. In one embodiment, the present invention provides a prodrug compound of Formula I: ##STR00001##
where R.sub.1-R.sub.5 are defined in the written description of the invention. The prodrug compounds of the invention can be used to treat any condition for which the tertiary amine-containing parent drug or tertiary imine-containing parent drug is useful as a treatment.

Hydantoin derivatives as Kv3 inhibitors
09669030 · 2017-06-06 · ·

The present invention relates to the prophylaxis of acute noise-induced hearing loss by administering a compound of formula (I): wherein: W is group (Wa), group (Wb) or group (Wc): ##STR00001##

Hydantoin derivatives as Kv3 inhibitors
09669030 · 2017-06-06 · ·

The present invention relates to the prophylaxis of acute noise-induced hearing loss by administering a compound of formula (I): wherein: W is group (Wa), group (Wb) or group (Wc): ##STR00001##

LIGANDS FOR ANTIBODY AND Fc-FUSION PROTEIN PURIFICATION BY AFFINITY CHROMATOGRAPHY

The present invention relates to the use for affinity purification of an antibody or a fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material.

LIGANDS FOR ANTIBODY AND Fc-FUSION PROTEIN PURIFICATION BY AFFINITY CHROMATOGRAPHY

The present invention relates to the use for affinity purification of an antibody or a fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material.

NOVEL ESTROGEN RECEPTOR LIGANDS

Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R.sup.1 to R.sup.9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.

##STR00001##

Method For Improving The Oxygen-Releasing Ability Of Hemoglobin To Organs Or Peripheral Tissues In Human Bodies And A Medication Thereof
20170129866 · 2017-05-11 ·

A method for improving the oxygen-releasing ability of hemoglobin, hemoglobin variants, recombinant hemoglobin or hemoglobin-based blood substitutes to organs or peripheral tissues in human bodies is disclosed by administering a compound of phthalides to a subject in need thereof. The compound of phthalides is characterized by a phthalide functional group which is represented as Formula I, and forms at least one hydrogen bond with Arg141 of hemoglobin, hemoglobin variants, recombinant hemoglobin or hemoglobin-based blood substitutes, stabilizing the 1/2 interface of hemoglobin, further stabilizing the oxygenated hemoglobin, hemoglobin variants, recombinant hemoglobin or hemoglobin-based blood substitutes in the low oxygen affinity T state and facilitating the oxygen release to the organs or the peripheral tissues. A medication for improving the oxygen-releasing ability of hemoglobin, hemoglobin variants, recombinant hemoglobin, or hemoglobin-based blood substitutes to organs or peripheral tissues in human bodies is also disclosed.

Method For Improving The Oxygen-Releasing Ability Of Hemoglobin To Organs Or Peripheral Tissues In Human Bodies And A Medication Thereof
20170129866 · 2017-05-11 ·

A method for improving the oxygen-releasing ability of hemoglobin, hemoglobin variants, recombinant hemoglobin or hemoglobin-based blood substitutes to organs or peripheral tissues in human bodies is disclosed by administering a compound of phthalides to a subject in need thereof. The compound of phthalides is characterized by a phthalide functional group which is represented as Formula I, and forms at least one hydrogen bond with Arg141 of hemoglobin, hemoglobin variants, recombinant hemoglobin or hemoglobin-based blood substitutes, stabilizing the 1/2 interface of hemoglobin, further stabilizing the oxygenated hemoglobin, hemoglobin variants, recombinant hemoglobin or hemoglobin-based blood substitutes in the low oxygen affinity T state and facilitating the oxygen release to the organs or the peripheral tissues. A medication for improving the oxygen-releasing ability of hemoglobin, hemoglobin variants, recombinant hemoglobin, or hemoglobin-based blood substitutes to organs or peripheral tissues in human bodies is also disclosed.

Organoleptic compounds

The present invention relates to novel compounds and their use as fragrance materials.