AR045680A2 - Procedimiento para resolver enantiomeros, composicion farmaceutica, su uso y enantiomeros precursores - Google Patents

Procedimiento para resolver enantiomeros, composicion farmaceutica, su uso y enantiomeros precursores

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Publication number
AR045680A2
AR045680A2 ARP040101561A ARP040101561A AR045680A2 AR 045680 A2 AR045680 A2 AR 045680A2 AR P040101561 A ARP040101561 A AR P040101561A AR P040101561 A ARP040101561 A AR P040101561A AR 045680 A2 AR045680 A2 AR 045680A2
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Argentina
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alkyl
alkoxy
alkylamino
acylamino
trifluoromethyl
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ARP040101561A
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Pfizer Prod Inc
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Publication of AR045680A2 publication Critical patent/AR045680A2/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
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  • Immunology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un procedimiento para resolver enantiómeros de un compuesto que contiene la estructura de fórmula (1), sales de adición de ácidos farmacéuticamente aceptables del mismo, sales de adición de bases farmacéuticamente aceptables del mismo y la base libre del mismo; siendo y 0, 1 o 2; R4 se selecciona del grupo constituido por hidrógeno, alquilo C1-6, alquilsulfonilo C1-6, alquenilo C2-6, alquinilo C2-6 estando opcionalmente substituido los grupos alquilo, alquenilo y alquinilo con deuterio, hidroxi, amino, trifluorometilo, alcoxi C1-4, aciloxi C1-6, alquilamino C1-6, (alquil C1-6)2amino, ciano, nitro, alquenilo C2-6, alquinilo C2-6 o acilamino C1-6; o R4 es cicloalquilo C3-10 estando opcionalmente substituido el grupo cicloalquilo con deuterio, hidroxi, amino, trifluorometilo, aciloxi C1-6, acilamino C1-6, alquilamino C1-6, (alquil C1-6)2amino, ciano, cianoalquilo C1-6, trifluorometilalquilo C1-6, nitro, nitroalquilo C1-6 o acilamino C1-6; R5 es heterocicloalquilo C2-9 debiendo estar substituidos los grupos heterocicloalquilo con uno a cinco carboxilo, ciano, amino, deuterio, hidroxilo, alquilo C1-6, alcoxi C1-6, halo, acilo C1-6, alquilamino C1-6, aminoalquilo C1-6, alcoxi C1-6-CO-NH, alquilamino C1-6-CO-, alquenilo C2-6, alquinilo C2-6, alquilamino C1-6, aminoalquilo C1-6, hidroxialquilo C1-6, alcoxi C1-6 alquilo C1-6, aciloxi C1-6 alquilo C1-6, nitro, cianoalquilo C1-6, haloalquilo C1-6, nitroalquilo C1-6, trifluorometilo, trifluorometilalquilo C1-6, acilamino C1-6, acilamino C1-6 alquilo C1-6, alcoxi C1-6 acilamino C1-6, aminoacilo C1-6, aminoacil C1-6 alquilo C1-6, alquilamino C1-6 acilo C1-6, (alquil C1-6)2aminoacilo C1-6, R15R16N-CO-O-, R15R16N-CO-alquilo C1-6, alquil C1-6-S(O)m, R15R16NS(O)m, R15R16NS(O)malquilo C1-6, R15S(O)mR16N, R15S(O)mR16Nalquilo C1-6 siendo m 0, 1 o 2 y estando seleccionados independientemente cada R15 y R16 de hidrógeno o alquilo C1-6; o un grupo de fórmula (2) en la que a es 0, 1, 2, 3 o 4; b, c, e, f y g son cada uno independientemente 0 o 1; d es 0, 1, 2, o 3; X es S(O)n, siendo n 0, 1 o 2; oxígeno, carbonilo o -C(=N-ciano)-; Y es S(O)n siendo n 0, 1 o 2; o carbonilo; y Z es carbonilo, C(O)O-, C(O)NR- o S(O)n, siendo n 0, 1 o 2; R6 , R7 , R8 , R9 , R10 y R11 se seleccionan cada uno independientemente del grupo constituido por hidrógeno o alquilo C1-6 opcionalmente substituido con deuterio, hidroxilo, amino, trifluorometilo, aciloxi C1-6, acilamino C1-6, alquilamino C1-6, (alquil C1-6)2amino, ciano, cianoalquilo C1-6, trifluorometilalquilo C1-6, nitro, nitroalquilo C1-6 o acilamino C1-6; R12 es carboxilo, ciano, amino, oxo, deuterio, hidroxilo, trifluorometilo, alquilo C1-6, trifluorometilalquilo C1-6, alcoxi C1-6, halo, acilo C1-6, alquilamino C1-6, (alquil C1-6)2amino, aminoalquilo C1-6, alcoxi C1-6-CO-NH, alquilamino C1-6-CO-, alquenilo C2-6, alquinilo C2-6, alquilamino C1-6, hidroxialquilo C1-6, alcoxi C1-6 alquilo C1-6, aciloxi C1-6 alquilo C1-6, nitro, cianoalquilo C1-6, haloalquilo C1-6, nitroalquilo C1-6, trifluorometilo, trifluorometilalquilo C1-6, acilamino C1-6, acilamino C1-6 alquilo C1-6, alcoxi C1-6 acilamino C1-6, aminoacilo C1-6, aminoacil C1-6 alquilo C1-6, alquilamino C1-6acilo C1-6, (alquil C1-6)2aminoacilo C1-6, R15R16N-CO-O-, R15R16N-CO-alquilo C1-6, R15C(O)NH, R15OC(O)NH, R15NHC(O)NH, alquil C1-6-S(O)m, alquil C1-6-S(O)m-alquilo C1-6, R15R16NS(O)m, R15R16NS(O)malquilo C1-6, R15S(O)mR16N, R15S(O)nR16Nalquilo C1-6 siendo m 0, 1 o 2 y estando seleccionados R15 y R16 cada uno independientemente de hidrógeno o alquilo C1-6; caracterizado porque el citado procedimiento las etapas de: a) una mezcla racémica de enantiómeros de un compuesto, que contiene la estructura de la citada fórmula; en un disolvente, con un compuesto de resolución con una estereoespecificidad definida, formando una solución, siendo capaz el citado agente de resolución de unirse con al menos uno, pero no todos de los citados enantiómeros formando un precipitado, conteniendo al menos uno de los citados enantiómeros; b) dejar reposar la mezcla el tiempo suficiente para permitir una precipitación substancial de un enantiómero estereoespecífico de la mezcla racémica de la solución permaneciendo el otro de los citados enantiómeros en la citada solución; y c) dependiendo del enantiómero estereoespecífico del compuesto que se desee, recoger el precipitado y purificarlo o recoger la solución que contiene el otro de los citados enantiómeros y recristalizar el enantiómero contenido en la citada solución. Un procedimiento para preparar el compuesto de fórmula (3) o la sal farmacéuticamente aceptable del mismo; siendo R1 un grupo de fórmula (4), en la que y es 0, 1 o 2; R4 se selecciona del grupo constituido por hidrógeno, alquilo C1-6, alquilsulfonilo C1-6, alquenilo C2-6, alquinilo C2-6 estando opcionalmente substituido los grupos alquilo, alquenilo y alquinilo con deuterio, hidroxilo, amino, trifluorometilo, alcoxi C1-4, aciloxi C1-6, alquilamino C1-6, (alquil C1-6)2amino, ciano, nitro, alquenilo C2-6, alquinilo C2-6 o acilamino C2-6; o R4 es cicloalquilo C3-10 estando opcionalmente substituido el grupo cicloalquilo con deuterio, hidroxilo, amino, trifluorometilo, aciloxi C1-6, acilamino C1-6, alquilamino C1-6, (alquil C1-6)2amino, ciano, cianoalquilo C1-6, trifluorometilalquilo C1-6, nitro, nitroalquilo C1-6 o acilamino C1-6; R5 es heterocicloalquilo C1-9 debiendo estar substituido los grupos heterocicloalquilo con uno a cinco carboxilo, ciano, amino, deuterio, hidroxilo, alquilo C1-6, alcoxi C1-6, halo, acilo C1-6, alquilamino C1-6, aminoalquilo C1-6, alcoxi C1-6-CO-NH, alquilamino C1-6-CO-, alquenilo C2-6, alquinilo C2-6, hidroxialquilo C1-6, alcoxi C1-6 alquilo C1-6, aciloxi C1-6 alquilo C1-6, nitro, cianoalquilo C1-6, haloalquilo C1-6, nitroalquilo C1-6, trifluorometilo, trifluorometilalquilo C1-6, acilamino C1-6, acilamino C1-6 alquilo C1-6, alcoxi C1-6 acilamino C1-6, aminoacilo C1-6, aminoacil C1-6 alquilo C1-6, alquilamino C1-6 acilo C1-6, (alquil C1-6)2aminoacilo C1-6, R15R16 N-CO-O-, R15R16N-CO-alquilo C1-6, alquil C1-6-S(O)m, R15R16NS(O)m, R15R16NS(O)malquilo C1-6, R15S(O)mR16N, R15S(O)mR16Nalquilo C1-6 siendo m 0, 1 o 2 y estando seleccionados independientemente cada R15 y R16 de hidrógeno o alquilo C1-6; o un grupo de fórmula (2) en la que a es 0, 1, 2, 3 o 4; b, c, e, f y g son cada uno independientemente 0 o 1; d es 0, 1, 2, o 3; X es S(O)n siendo n 0, 1 o 2; oxígeno, carbonilo o -C(=N-ciano)-; Y es S(O)n siendo n 0, 1 o 2; o carbonilo; y Z es carbonilo, C(O)O-, C(O)NR- o S(O)n siendo n 0, 1 o 2; R6, R7, R8, R9, R10 y R11 se seleccionan cada uno independientemente del grupo constituido por hidrógeno o alquilo C1-6 opcionalmente substituido con deuterio, hidroxilo, amino, trifluorometilo, aciloxi C1-6, acilamino C1-6, alquilamino C1-6, (alquil C1-6)2amino, ciano, cianoalquilo C1-6, trifluorometilalquilo C1-6, nitro, nitroalquilo C1-6 o acilamino C1-6; R12 es carboxilo, ciano, amino, oxo, deuterio, hidroxilo, trifluorometilo, alquilo C1-6, trifluorometilalquilo C1-6, alcoxi C1-6, halo, acilo C1-6, alquilamino C1-6, (alquil C1-6)2amino, aminoalquilo C1-6, alcoxi C1-6-CO-NH, alquilamino C1-6-CO-, alquenilo C2-6, alquinilo C2-6, alquilamino C1-6, hidroxialquilo C1-6, alcoxi C1-6 alquilo C1-6, aciloxi C1-6 alquilo C1-6, nitro, cianoalquilo C1-6, haloalquilo C1-6, nitroalquilo C1-6, trifluorometilo, trifluorometilalquilo C1-6, acilamino C1-6, acilamino C1-6 alquilo C1-6, alcoxi C1-6 acilamino C1-6, aminoacilo C1-6, aminoacil C1-6 alquilo C1-6, alquilamino C1-6 acilo C1-6, (alquil C1-6)2aminoacilo C1-6, R15R16N-CO-O-, R15R16N-CO-alquilo C1-6, R15C(O)NH, R15OC(O)NH, R15NHC(O)NH, alquil C1-6-S(O)m, alquil C1-6-S(O)m-alquilo C1-6, R15R16NS(O)m, R15R16NS(O)malquilo C1-6, R15S(O)mR16N, R15S(O)nR16Nalquilo C1-6 siendo m 0, 1 o 2 y estando seleccionados R15 y R16 cada uno independientemente de hidrógeno o alquilo C1-6; R2 y R3 se seleccionan cada uno independientemente del grupo constituido por hidrógeno, deuterio, amino, halo, hidroxilo, nitro, carboxilo, alquenilo C2-6, alquinilo C2-6, trifluorometilo, trifluorometoxi, alquilo C1-6, alcoxi C1-6, cicloalquilo C3-10 estando opcionalmente substituidos los grupos alquilo, alcoxi o cicloalquilo con uno a tres grupos seleccionados de halo, hidroxilo, carboxilo, amino alquiltio C1-6, alquilamino C1-6, (alquil C1-6)2amino, heteroarilo C5-9, heterocicloalquilo C2-9, cicloalquilo C3-9 o arilo C6-10; o R2 y R3 son cada uno independientemente cicloalquilo C3-10, cicloalcoxi C3-10, alquilamino C1-6, (alquil C1-6)2amino, arilamino C6-10, alquiltio C1-6, ariltio C6-10, alquilsulfinilo C1-6, arilsulfinilo C6-10, alquilsulfonilo C1-6, arilsulfonilo C6-10, acilo C1-6, alcoxi C1-6-CO-NH-, alquilamino C1-6-CO-, heteroarilo C5-9, heterocicloalquilo C2-9 o arilo C6-10 estando opcionalmente substituidos los grupos heteroarilo, heterocicloalquilo y arilo con uno a tres halo, alquilo C1-6, alquil C1-6-CO-NH-, alcoxi C1-6-CO-NH-, alquil C1-6-CO-NH-alquilo C1-6, alcoxi C1-6-CO-NH-alquilo C1-6, alcoxi C1-6-CO-NH-alcoxi C1-6, carboxilo, carboxialquilo C1-6, carboxialcoxi C1-6, benciloxicarbonilalcoxi C1-6, alcoxicarbonil C1-6 alcoxi C1-6, arilo C6-10, amino, aminoalquilo C1-6, alcoxicarbonilamino C1-6, aril C6-10 alcoxicarbonilamino C1-6, alquilamino C1-6, (alquil C1-6)2amino, alquilamino C1-6 alquilo C1-6, (alquil C1-6)2aminoalquilo, hidroxilo, alcoxi C1-6, carboxilo, carboxialquilo C1-6, alcoxicarbonilo C1-6, alcoxicarbonil C1-6 alquilo C1-6, alcoxi C1-6-CO-NH-, alquil C1-6-CO-NH-, ciano, heterocicloalquilo C5-9, amino-CO-NH-, alquilamino C1-6-CO-NH-, (alquil C1-6)2amino-CO-NH-, arilamino C6-10-CO-NH-, heteroarilamino C5-9-CO-NH-, alquilamino C1-6-CO-NH-alquilo C1-6, (alquil C1-6)2amino-CO-NH-alquilo C1-6, arilamino C6-10-CO-NH-alquilo C1-6, heteroarilamino C5-9-CO-NH-alquilo C1-6, alquilsulfonilo C1-6, alquilsulfonilamino C1-6, alquilsulfonilamino C1-6 alquilo C1-6, arilsulfonilo C6-10, arilsulfonilamino C6-10, arilsulfonilamino C6-10 alquilo C1-6, alquilsulfonilamino C1-6, a
ARP040101561A 2001-05-31 2004-05-07 Procedimiento para resolver enantiomeros, composicion farmaceutica, su uso y enantiomeros precursores AR045680A2 (es)

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ARP040101561A AR045680A2 (es) 2001-05-31 2004-05-07 Procedimiento para resolver enantiomeros, composicion farmaceutica, su uso y enantiomeros precursores

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