摘要:
This invention relates to novel quinuclidine derivatives represented by Formula (II) wherein represents an optional double bond; n is 1, 2 or 3; X represents a linker selected from -O-, -O-CH2-, -O-CH2-CH2-, -S-, -SO-, -SO2-, -CH2-, -S-CH2-CH2-,-CH2-, -C(=CH2)-, -NH-, -N(alkyl)-, -C(=O)-, -C(=S)-, oo, and ss; and Y represents O, S, SO2, or NR’ wherein R’ represents hydrogen or alkyl and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要:
This invention relates to novel quinuclidine derivatives represented by Formula (II) wherein represents an optional double bond; n is 1, 2 or 3; X represents a linker selected from -O-, -O-CH2-, -O-CH2-CH2-, -S-, -SO-, -SO2-, -CH2-, -S-CH2-CH2-,-CH2-, -C(=CH2)-, -NH-, -N(alkyl)-, -C(=O)-, -C(=S)-, oo, and ss; and Y represents O, S, SO2, or NR’ wherein R’ represents hydrogen or alkyl and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要:
This invention discloses a method of treatment of osteoarthritis pain by administration of a composition containing a nicotinic acetylcholine receptor ligand and a nicotinic acetylcholine receptor subtype 4 2 allosteric modulator. The present application also relates to compositions comprising such compounds for use in treating pain and related disorders mediated by controlling neurotransmitter release in a subject.
摘要:
The invention relates to heterocyclic derivatives, compositions comprising such compounds, and methods of preventing or treating conditions and disorders using such compounds and compositions. The heterocyclic derivatives, more particularly can be substituted oxadiazole compounds and derivatives thereof.
摘要:
Compounds of formula (I), pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals (nicotinic acetylcholine receptor ligands).
摘要:
The present invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are α-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are α-1 antagonist compositions and a method for antagonizing α-1 receptors and treating BPH.
摘要:
The present invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein W is a tricyclic heterocyclic ring system; which is an α-1 adrenergic antagonist and is useful in the treatment of BPH; also disclosed are α-1 antagonist compositions and a method for antagonizing α-1 receptors and treating BPH.
摘要:
The invention relates to amine-substituted aza-adamantane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. Radiolabelled compounds useful for evaluating the binding affinity to α7 nicotinic acetylcholine receptors also are described.
摘要:
Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.
摘要:
The present invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are α-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are α-1 antagonist compositions and a method for antagonizing α-1 receptors and treating BPH.