Abstract:
PROBLEM TO BE SOLVED: To provide a neuron nicotinic cholinergic compound selectively useful for the control of synapse transmission and provide a pharmaceutical composition containing the compound. SOLUTION: The invention relates to a new 3-pyridyloxymethyl heterocyclic ether of formula (I) and a pharmaceutical composition containing the compound in combination with a pharmacologically allowable carrier. In the formula, * is a chiral center; n is an integer selected from 1, 2 and 3; X is oxygen or sulfur; R 1 is hydrogen, allyl or a 1-6C alkyl; R 2 is hydrogen or CH2OH, CH2F, CH2CN or the like, when n=2; and A is methylene or ethylene which may be substituted with an alkyl group. COPYRIGHT: (C)2008,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a new 3-pyridyl enantiomer. SOLUTION: The present invention relates to a method of controlling pain in mammals, including humans, comprising administering selected compounds of formula I or a pharmaceutically acceptable salt thereof to a mammal or patient in need of treatment thereof. The invention further relates to selected (R) and (S) compounds of formula I which are useful as analgesics as well as neuronal cell death preventors and anti-inflammatory agents. COPYRIGHT: (C)2009,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide furopyridine, thienopyridine, pyrrolopyridine, and related pyrimidine, pyridazine and triazine compounds controlling chemical synaptic transmission; to provide medicinal compositions of the compounds effective for therapy; and to provide these compositions for selectively controlling the synaptic transmission. SOLUTION: The novel heterocyclic ether compound is represented by formula (I) (wherein, A, m, R, X, Y 1 , Y 2 and Y 3 are specifically defined). The medicinal composition thereof is effective for the therapy. The compositions are used for selectively controlling the synaptic transmission in mammals. COPYRIGHT: (C)2008,JPO&INPIT
Abstract:
The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R 1 , R 2 , R 3 , R 4 , and L 2 , are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
Abstract:
The present invention relates to compounds of formula (I), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2 , R3 , R4 , and L1 are defined in the specfication, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. The present invention also relates to compounds of formula (II), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1a, R2a and (Rx)n are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
Abstract:
Novel 3-pyridyloxymethyl heterocyclic ether compounds having formula (I), wherein * is a chiral center and n, X, R1, R2, A andB are specifically defined, which are useful in controlling chemical synaptic transmission; therapeutically-effective pharmaceutical compositions therof; and use of said compositions to selectively control synaptic transmission in mammals.
Abstract:
La presente invención se refiere a compuestos de la fórmula (I), o sales farmacéuticas, profármacos, sales de profármaco, o combinaciones de los mismos, fórmula (I), en donde R1, R2, R3, R4, y L1 se definen en la especificación, composiciones que comprenden dichos compuestos, y métodos para el tratamiento de condiciones y trastornos utilizando dichos compuestos y composiciones. La presente invención también se refiere a compuestos de la fórmula (II), o sales farmacéuticas, profármacos, sales de profármacos, o combinaciones de los mismos, fórmula (II), en donde R1a, R2a, Rx, y n son como se define en la especificación, composiciones que comprenden dichos compuestos, y métodos para el tratamiento de condiciones y trastornos utilizando dichos compuestos y composiciones.
Abstract:
Compounds of formula (I) Z-Ar 1 -Ar 2 wherein Z is a diazabicyclic amine, Ar 1 is a 5- or 6-membered aromatic ring, and Ar 2 is selected from the group consisting of an unsubstituted or substituted 5-or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazoyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ±7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.
Abstract:
Un compuesto de fórmula (Ver fórmula) o una sal farmacéuticamente aceptable del mismo, en la que: Z es CH2CH2; L1 se selecciona entre el grupo compuesto por un enlace covalente y (CH2)n; n es 1-5; R1 se selecciona entre el grupo compuesto por (Ver fórmulas) R2 se selecciona entre el grupo compuesto por hidrógeno, alcoxicarbonilo, alquilo, aminoalquilo, aminocarbonilalquilo, benciloxicarbonilo, cianoalquilo, dihidro-3-piridinilcarbonilo, hidroxi, hidroxialquilo, fenoxicarbonilo, y -NH2; R4 se selecciona entre el grupo compuesto por hidrógeno, alquilo, y halógeno; R5 se selecciona entre el grupo compuesto por hidrógeno, alcoxi, alquilo, halógeno, nitro, y -NH2; R6 se selecciona entre el grupo compuesto por hidrógeno, alquenilo, alcoxi, alcoxialcoxi, alcoxialquilo, alcoxicarbonilo, alcoxicarbonilalquilo, alquilo, alquilcarbonilo, alquilcarboniloxi, alquiltio, alquinilo, aminoalquilo, amino-carbonilo, aminocarbonilalquilo, aminosulfonilo, carboxi, carboxialquilo, ciano, cianoalquilo, formilo, formilalquilo, haloalcoxi, haloalquilo, halógeno, hidroxi, hidroxialquilo, mercapto, mercaptoalquilo, nitro, 5-tetrazolilo, -NR7SO2R8, NR10R11, en las que R10 y R11 son hidrógeno, alquilo, alquilcarbonilo y formilo. -C(NR7)NR7R8, -CH2C(NR7)NR7R8, -C(NOR7)R8, -C(NCN)R7, -C(NNR7R8)R8, -S(O)2OR7, y -S(O)2R7; y R7 y R8 se seleccionan independientemente entre el grupo compuesto por hidrógeno y alquilo.