Abstract:
PROBLEM TO BE SOLVED: To provide novel azaadamantane derivatives.SOLUTION: The invention relates to compounds that are azaadamantane derivatives of formula (I), particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof. In the formula, Ldenotes -O- or -NR-; A denotes -Ar, -Ar-L-Aror -Ar-L-Ar; Ardenotes aryl or heteroaryl; Ardenotes aryl or monocyclic heteroaryl; Ardenotes aryl or heteroaryl; Ardenotes bicyclic heteroaryl; Ardenotes aryl or heteroaryl; Ldenotes a binding, -O -, -NR-, -CH- or -C(O)NR-; L3 denotes a binding, -O-, -NR-or -CH-; and Rdenotes hydrogen or alkyl.
Abstract translation:待解决的问题:提供新的氮杂金刚烷衍生物。 解决方案:本发明涉及式(I)的氮杂金刚烷衍生物,特别是醚或胺取代的氮杂金刚烷衍生物及其盐和前药的化合物。 在该式中,L 1 SB>表示-O-或-NR a SB> - ; A表示-Ar 1 SB>,-Ar 2 SB> -L 2 SB> 3 SB>或-Ar 4 SB> -L 3 SB> -Ar 5 SB>; Ar 1 SB>表示芳基或杂芳基; Ar 2表示芳基或单环杂芳基; Ar 3 SB>表示芳基或杂芳基; Ar 4 SB>表示双环杂芳基; Ar 5 SB>表示芳基或杂芳基; L 2 SB>表示结合,-O - , - NR a SB> - ,-CH 2 SB> - 或-C(O)NR a SB> - ; L3表示结合,-O-,-NR a SB> - 或-CH 2 SB> 并且R a SB>表示氢或烷基。 版权所有(C)2013,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a series of N-substituted diazabicyclic compound, a method for selectively controlling releasing of a synaptic transmission substance in mammals by using the compound, and a pharmaceutical composition including the compound.SOLUTION: The present invention provides a compound expressed by formula (I), a pharmaceutical composition of the compound, and use of the composition to control synaptic transmission in mammals (in a nicotinic acetylcholine receptor ligand). In formula (I), A is selected from a group consisting of CH2, CH2CH2, and the like; B is selected from a group consisting of CH2 and CH2CH2, however, when A is CH2CH2CH2, B is CH2; Y is selected from a group consisting of CH2 and CH2CH2; Z is selected from a group consisting of CH2 and CH2CH2, however, when Y is CH2CH2, Z is a covalent bond, and when Z is CH2CH2, Y is a covalent bond; and Rl is pyridine or the like.
Abstract:
The invention relates to compounds that are azaadamantane derivatives of formula (I), particularly ether- or amine -substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.
Abstract:
The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
Abstract:
Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y and Y form various tricyclic cores, X and X are C, CH, or N, as defined herein, and R 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 alpha7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.
Abstract:
The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
Abstract:
The invention relates to a composition comprising a neuronal nicotinic receptor ligand and an a4ß2 positive allosteric modulator, a method of using the same, and a related article of manufacture.
Abstract:
The present invention provides an amine compound of formula (I) or a pharmaceutically acceptable salt thereof which is an antagonist for alpha-2 adrenoreceptors and which inhibits serotonin (5-hydroxytryptamine, 5-HT) uptake.