A61K31/46

8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Compositions and methods for treating synucleinopathies

The present invention describes the use of a 5HT3-antagonist, in combination with a 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine, to reduce adverse effects and to facilitate the neuroprotective treatment of a patient suffering from a synucleinopathic disorder to enable a therapeutically effective 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine daily dose without the dose-limiting adverse effects caused by pramipexole when administered alone.

Compositions and methods for treating synucleinopathies

The present invention describes the use of a 5HT3-antagonist, in combination with a 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine, to reduce adverse effects and to facilitate the neuroprotective treatment of a patient suffering from a synucleinopathic disorder to enable a therapeutically effective 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine daily dose without the dose-limiting adverse effects caused by pramipexole when administered alone.

LAG TIME REDUCTION/ICE SPRAY
20220409533 · 2022-12-29 ·

The present invention relates to a kit, comprising at least one cold spray and at least one dosage form for transdermally administering at least one pharmaceutically active ingredient, to said kit for use in the treatment of a patient, to the use of a cold spray in order to shorten the resorption delay time in the application of a dosage form for transdermally administering at least one pharmaceutically active ingredient, and to a method for treating a patient.

LAG TIME REDUCTION/ICE SPRAY
20220409533 · 2022-12-29 ·

The present invention relates to a kit, comprising at least one cold spray and at least one dosage form for transdermally administering at least one pharmaceutically active ingredient, to said kit for use in the treatment of a patient, to the use of a cold spray in order to shorten the resorption delay time in the application of a dosage form for transdermally administering at least one pharmaceutically active ingredient, and to a method for treating a patient.

Xanomeline derivatives and methods for treating neurological disorders

Provided herein are compounds comprising compounds of formula I ##STR00001##
and/or salts thereof;
wherein at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, and R.sup.13 is fluorine, and the remainder are independently chosen from hydrogen and fluorine; and R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.20, R.sup.21, R.sup.22, and R.sup.23 are independently chosen from hydrogen and deuterium; with the proviso that when R.sup.1, R.sup.2, and R.sup.3 are fluorine, then at least one of R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, and R.sup.13 is fluorine or at least one of R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.20, R.sup.21, R.sup.22, and R.sup.23 is deuterium. Also provided are medicaments comprising these compounds and methods for treating central nervous system disorders with the compounds and medicaments described herein.

Xanomeline derivatives and methods for treating neurological disorders

Provided herein are compounds comprising compounds of formula I ##STR00001##
and/or salts thereof;
wherein at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, and R.sup.13 is fluorine, and the remainder are independently chosen from hydrogen and fluorine; and R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.20, R.sup.21, R.sup.22, and R.sup.23 are independently chosen from hydrogen and deuterium; with the proviso that when R.sup.1, R.sup.2, and R.sup.3 are fluorine, then at least one of R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, and R.sup.13 is fluorine or at least one of R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.20, R.sup.21, R.sup.22, and R.sup.23 is deuterium. Also provided are medicaments comprising these compounds and methods for treating central nervous system disorders with the compounds and medicaments described herein.

METHODS FOR PALMAR OR PLANTAR ADMINISTRATION OF PHARMACEUTICAL COMPOSITIONS
20220401412 · 2022-12-22 ·

Disclosed herein are methods for palmar or plantar administration of anticholinergic compounds to a subject in need thereof. Also disclosed herein are methods of treating palmar or plantar hyperhidrosis in a subject in need thereof by administering anticholinergic compounds to the palmar or plantar skin of the subject.

METHODS FOR PALMAR OR PLANTAR ADMINISTRATION OF PHARMACEUTICAL COMPOSITIONS
20220401412 · 2022-12-22 ·

Disclosed herein are methods for palmar or plantar administration of anticholinergic compounds to a subject in need thereof. Also disclosed herein are methods of treating palmar or plantar hyperhidrosis in a subject in need thereof by administering anticholinergic compounds to the palmar or plantar skin of the subject.

Oral dissolving films containing microencapsulated vaccines and methods of making same

An oral dissolving film containing nano- or micro-encapsulated bioactive material and methods of forming the film. The film may be prepared by dispensing a mixture of a film-forming agent, a crosslinking agent, a solution of nano- or micro-encapsulated bioactive material, and a photoinitiator into a plurality of wells in a tray using a 3D printer. The dispensed material is exposed to radiation in order to crosslink the material and form a film.