CO4970750A1 - BICICLIC BENZAMIDES OF 3-OR 4-SUBSTITUTED DERIVATIVES 4- (AMINOMETIL) -PIPERIDINES - Google Patents

BICICLIC BENZAMIDES OF 3-OR 4-SUBSTITUTED DERIVATIVES 4- (AMINOMETIL) -PIPERIDINES

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Publication number
CO4970750A1
CO4970750A1 CO98048802A CO98048802A CO4970750A1 CO 4970750 A1 CO4970750 A1 CO 4970750A1 CO 98048802 A CO98048802 A CO 98048802A CO 98048802 A CO98048802 A CO 98048802A CO 4970750 A1 CO4970750 A1 CO 4970750A1
Authority
CO
Colombia
Prior art keywords
alkyl
substituted
hydrogen
6alkyl
halo
Prior art date
Application number
CO98048802A
Other languages
Spanish (es)
Inventor
Jean-Paul Rene Marie Andre Bosman
De Cleyn Michel Anna Jozef
Michel Surkyn
Original Assignee
Janssen Pharmaceutica Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Priority to CO98048802A priority Critical patent/CO4970750A1/en
Publication of CO4970750A1 publication Critical patent/CO4970750A1/en

Links

Abstract

Un compuesto de fórmula (I)a una forma estereoquímicamente isomérica de la misma y una forma N-óxido de la misma o a una sal de adición de base o ácido farmacéuticamente aceptable de la misma donde R1 y R2 tomados conjuntamente forman un radical divalente de fórmula -O-CH2 -O - (a-1), -O-CH2 -CH2 - (a-2), -O-CH2 -CH2 -O- (a-3), -O-CH2 -CH2 -CH2 - (a-4) -O-CH2 -CH2 -CH2 -O- (a-5)-O-CH2 -CH2 -CH2 -CH2 - (a-6)donde en dichos radicales divalentes uno o dos átomos de hidrógeno pueden estar substituidos con alquilo C1-6 .R3 es hidrógeno o halo; R4 es hidrógeno o alquilo C1-6 ; R5 es hidrógeno o alquilo C1-6 ; L es cicloalquilo C3-6 , cicloalcanona C5-6 o alquenilo C2-6 , o L es un radical de fórmula-Alk-R6 (b-1), -Alk-X-R7 (b-2), -Alk-Y-C(=O)-R9 (b-3)o -Alk-Y-C(=O)-NR11 R12 (b-4), donde cada Alk es alcanodiilo C1-2 ; y R6 es hidrógeno, hidroxi, ciano, alquisulfonilamino C1-6 , cicloalquilo C3-6 , cicloalcanona C5-6 o Het1 ; R7 es hidrógeno, alquiloC1-6 , hidroxialquilo C1-6 , cicloalquilo C3-6 , o Het2 ; X es O, S, SO2 o NR8 ; siendo dicho R8 hidrógeno o alquilo C1-6 ; R9 es hidrógeno, alquilo C1-6 , cicloalquilo C3-6 , alquiloxi C1-6 , o hidroxi; Y es NR10 o un enlace directo, siendo dicho R10 - 2 -hidrógeno o alquilo C1-6 , R11 y R12 son cada uno independientemente hidrógeno, alquilo C1-6 , cicloalquilo C3-6 o R11 y R12 combinados con el átomo de nitrógeno portador de R11 y R12 pueden formar un anillo pirrolidinilo o piperidinilo y ambos pueden estar opcionalmente substituidos con alquilo C1-6 , amino o mono o di (alquilo C1-6 )amino, o dichos R11 y R12 combinados con el nitrógeno portador de R11 y R12 pueden formar un radical piperazinilo o 4-morfolinilo estando ambos opcionalmente substituidos con alquilo C1-6 ; yHet1 y Het2 son cada uno independientemente seleccionados de furano; furano substituido con alquilo C1-6 o halo; tetrahidrofurano; un tetrahidrofurano substituido con alquilo C1-6 ; un dioxolano; un dioxolano substituido con alquilo C1-6 ; un dioxano; un dioxano substituido con alquilo C1-6 ; tetrahidropirano; un tetrahidropirano substituido con alquilo C1-6 , pirrolidinilo; pirrolidinilo substituido con uno o dos substituyentes cada uno independientemente seleccionado de halo, hidroxi, ciano o alquilo C1-6 ; piridinilo; piridinilo substituido con uno o dos substituyentes cada uno independientemente seleccionado de halo, hidroxi, ciano, alquilo C1-6 ; pirimidinilo; pirimidinilo substituido con uno o dos substituyentes cada uno de ellos independientemente seleccionados de halo, hidroxi, ciano, alquilo C1-6 , alquiloxi C1-6 , amino y mono y di(alquilo C1-6 )amino; piridacinilo; piridacinilo substituido con uno o dos substituyentes cada uno independientemente seleccionado de hidroxi, alquiloxi C1-6 , alquilo C1-6 , halo, piracinilo; piracinilo substituido con uno o dos substituyentes cada uno de ellos seleccionados de halo, hidroxi, ciano, alquilo C1-6 , alquiloxi C1-6 , amino, monoAND#8209; y di (alquilo C1-6 )amino y alquiloxicarbonilo C1-6 ; Het1 puede ser también un radical de fórmula Het1 y Het2 pueden ser también cada uno independientemente seleccionados de los radicales de fórmula R13 y R14 son cada uno independientemente hidrógeno o alquilo C1-4 .A compound of formula (I) to a stereochemically isomeric form thereof and an N-oxide form thereof or to a pharmaceutically acceptable acid or base addition salt thereof where R1 and R2 taken together form a divalent radical of formula -O-CH2 -O - (a-1), -O-CH2 -CH2 - (a-2), -O-CH2 -CH2 -O- (a-3), -O-CH2 -CH2 -CH2 - (a-4) -O-CH2 -CH2 -CH2 -O- (a-5) -O-CH2 -CH2 -CH2 -CH2 - (a-6) where in said divalent radicals one or two hydrogen atoms can be substituted with C1-6 alkyl. R3 is hydrogen or halo; R4 is hydrogen or C1-6 alkyl; R5 is hydrogen or C1-6 alkyl; L is C3-6 cycloalkyl, C5-6 cycloalkanone or C2-6 alkenyl, or L is a radical of formula-Alk-R6 (b-1), -Alk-X-R7 (b-2), -Alk-YC (= O) -R9 (b-3) or -Alk-YC (= O) -NR11 R12 (b-4), where each Alk is C1-2 alkanediyl; and R6 is hydrogen, hydroxy, cyano, C1-6 alkylsulfonylamino, C3-6 cycloalkyl, C5-6 cycloalkanone or Het1; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or Het2; X is O, S, SO2, or NR8; said R8 being hydrogen or C1-6 alkyl; R9 is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkyloxy, or hydroxy; Y is NR10 or a direct bond, said R10-2-hydrogen or C1-6 alkyl being, R11 and R12 are each independently hydrogen, C1-6 alkyl, C3-6 cycloalkyl or R11 and R12 combined with the carrier nitrogen atom R11 and R12 can form a pyrrolidinyl or piperidinyl ring and both can be optionally substituted with C1-6 alkyl, amino or mono or di (C1-6 alkyl) amino, or said R11 and R12 combined with the nitrogen bearing R11 and R12 they can form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C1-6alkyl; yHet1 and Het2 are each independently selected from furan; furan substituted with C1-6alkyl or halo; tetrahydrofuran; a C1-6alkyl-substituted tetrahydrofuran; a dioxolane; a dioxolane substituted with C1-6alkyl; a dioxane; a dioxane substituted with C1-6alkyl; tetrahydropyran; a tetrahydropyran substituted with C1-6alkyl, pyrrolidinyl; pyrrolidinyl substituted with one or two substituents each independently selected from halo, hydroxy, cyano or C1-6 alkyl; pyridinyl; pyridinyl substituted with one or two substituents each independently selected from halo, hydroxy, cyano, C1-6 alkyl; pyrimidinyl; pyrimidinyl substituted with one or two substituents each independently selected from halo, hydroxy, cyano, C 1-6 alkyl, C 1-6 alkyloxy, amino and mono and di (C 1-6 alkyl) amino; pyridacinyl; pyridacinyl substituted with one or two substituents each independently selected from hydroxy, C1-6 alkyloxy, C1-6 alkyl, halo, pyrazinyl; Pyrazinyl substituted with one or two substituents each selected from halo, hydroxy, cyano, C1-6alkyl, C1-6alkyloxy, amino, monoAND # 8209; and di (C1-6alkyl) amino and C1-6alkyloxycarbonyl; Het1 can also be a radical of formula Het1 and Het2 can also each be independently selected from radicals of formula R13 and R14 are each independently hydrogen or C1-4alkyl.

CO98048802A 1998-08-26 1998-08-26 BICICLIC BENZAMIDES OF 3-OR 4-SUBSTITUTED DERIVATIVES 4- (AMINOMETIL) -PIPERIDINES CO4970750A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CO98048802A CO4970750A1 (en) 1998-08-26 1998-08-26 BICICLIC BENZAMIDES OF 3-OR 4-SUBSTITUTED DERIVATIVES 4- (AMINOMETIL) -PIPERIDINES

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CO98048802A CO4970750A1 (en) 1998-08-26 1998-08-26 BICICLIC BENZAMIDES OF 3-OR 4-SUBSTITUTED DERIVATIVES 4- (AMINOMETIL) -PIPERIDINES

Publications (1)

Publication Number Publication Date
CO4970750A1 true CO4970750A1 (en) 2000-11-07

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Family Applications (1)

Application Number Title Priority Date Filing Date
CO98048802A CO4970750A1 (en) 1998-08-26 1998-08-26 BICICLIC BENZAMIDES OF 3-OR 4-SUBSTITUTED DERIVATIVES 4- (AMINOMETIL) -PIPERIDINES

Country Status (1)

Country Link
CO (1) CO4970750A1 (en)

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