AR035517A1 - Derivados de piperazina, proceso para prepararlos, composiciones farmaceuticas que los comprenden, y uso de dichos compuestos en la elaboracion de medicamentos - Google Patents

Derivados de piperazina, proceso para prepararlos, composiciones farmaceuticas que los comprenden, y uso de dichos compuestos en la elaboracion de medicamentos

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Publication number
AR035517A1
AR035517A1 ARP010105788A ARP010105788A AR035517A1 AR 035517 A1 AR035517 A1 AR 035517A1 AR P010105788 A ARP010105788 A AR P010105788A AR P010105788 A ARP010105788 A AR P010105788A AR 035517 A1 AR035517 A1 AR 035517A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
cycloalkyl
alkoxy
independently selected
Prior art date
Application number
ARP010105788A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
Vernalis Res Ltd
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 Hoffmann La Roche, Vernalis Res Ltd filed Critical Hoffmann La Roche
Publication of AR035517A1 publication Critical patent/AR035517A1/es

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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/325—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Abstract

Derivados de piperazina que tienen la fórmula (1), así como también sus ésteres, solvatos y sales farmacéuticamente utilizables, en donde: R1 y R2 son independientemente seleccionados de hidrógeno, alquilo, cicloalquilo, arilo y aralquilo, o R1 y R2 junto con el átomo de carbono al cual están unidos forman un anillo carbocíclico de 3- a 8-miembros que está opcionalmente sustituido con alquilo; R3 y R4 son independientemente seleccionados de hidrógeno, alquilo, cicloalquilo, arilo y aralquilo; A1 es oxígeno o azufre, en donde en caso de que A1 sea oxígeno y A2 sea fenilo sin sustituir uno de R1, R2, R3 y R4 no es hidrógeno; A2 es aeilo, heteroarilo o cicloalquilo cada uno opcionalmente sustituido con uno o más sustituyentes independientemente seleccionados de halógeno, alquilo, cicloalquilo, arilo, aralquilo, alcoxilo, aralcoxilo, ariloxilo, hidroxilo, ciano, nitro, amino, alcoxicarbonilo, cicloalcoxicarbonilo, ariloxicarbonilo, aralcoxicarbonilo, heteroariloxicarbonilo, carbamoílo, cicloalcoxilo, alquilsulfoniloxilo, arilsulfoniloxilo, carbamoiloxilo, heteroarilalcoxilo, alqueniloxilo, tetrahidrofuranilalcoxilo, alquiniloxilo y cicloalquilalcoxilo, en donde alquilo, cicloalquilo, arilo, aralquilo, alcoxilo, aralcoxilo, ariloxilo, alcoxicarbonilo, cicloalcoxicarbonilo, ariloxicarbonilo, aralcoxicarbonilo, heteroariloxicarbonilo, cicloalcoxilo, alquilsulfoniloxilo, arilsulfoniloxilo, heteroarilalcoxilo, alqueniloxilo, tetrahidrofuranilalcoxilo, alquiniloxilo y cicloalquilalcoxilo están opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados de alquilo, alcoxilo, halógeno, nitro, oxo, trifluorometilo, alcoxilo sustituido con 1 a 3 halógeno, tiofenilo, arilo, amino, alquilcarbonilo y ariloxilo, o dos sustituyentes de arilo, heteroarilo o cicloalquilo forman junto con los átomos de carbono a los que están unidos un anillo carbocíclico de 5- a 7-miembros que está opcionalmente sustituido con uo o más sustituyentes independientemente seleccionados de alquilo, alcoxilo y halógeno; n es 1 ó 2; m es 0 ó 1; en donde se excluyen el éster (4-nitrofenil)metílico del ácido 2-metil-1-piperazinacarboxílico y el éster [(4-trifluormetil)fenil]metílico del ácido 1-piperazinacarboxílico. Se pueden usar en forma de preparaciones farmacéuticas para el tratamiento o prevención de trastornos del sistema nervioso central, enfermedades cardiovasculares, enfermedades gastrointestinales, diabetes, obesidad y apnea del sueno. También se dan a conocer un proceso para prepararlos, composiciones farmacéuticas que los comprenden y el uso de dichos compuestos en la elaboración de medicamentos.
ARP010105788A 2000-12-15 2001-12-12 Derivados de piperazina, proceso para prepararlos, composiciones farmaceuticas que los comprenden, y uso de dichos compuestos en la elaboracion de medicamentos AR035517A1 (es)

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