AR087390A1 - Profarmacos de metilfenidato, procesos para su fabricacion y uso - Google Patents

Profarmacos de metilfenidato, procesos para su fabricacion y uso

Info

Publication number
AR087390A1
AR087390A1 ARP120102779A ARP120102779A AR087390A1 AR 087390 A1 AR087390 A1 AR 087390A1 AR P120102779 A ARP120102779 A AR P120102779A AR P120102779 A ARP120102779 A AR P120102779A AR 087390 A1 AR087390 A1 AR 087390A1
Authority
AR
Argentina
Prior art keywords
aryloxy
haloalkyl
arylsulfyl
alkylaryl
group
Prior art date
Application number
ARP120102779A
Other languages
English (en)
Inventor
Sven Guenther
Guochen Chi
Bindu Bera
Original Assignee
Kempharm Inc
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 Kempharm Inc filed Critical Kempharm Inc
Publication of AR087390A1 publication Critical patent/AR087390A1/es

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4458—Non condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
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    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
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    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
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    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/06—Antiarrhythmics
    • 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
    • C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/59—Hydrogenated pyridine rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Genetics & Genomics (AREA)
  • Psychiatry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Nutrition Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Physiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Toxicology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Child & Adolescent Psychology (AREA)

Abstract

Profármacos y composiciones para el tratamiento de diversas enfermedades y/o trastornos que comprenden metilfenidato o sus derivados, conjugados con al menos un alcohol, amina, oxoácido, tiol o sus derivados. En algunas formas de realización, los conjugados incluyen además al menos un conector. Esta tecnología también se refiere a la síntesis de metilfenidato o sus derivados, conjugados con al menos un alcohol, amina, oxoácido, tiol, o sus derivados o combinaciones. Acción sobre alteraciones del SNC.Reivindicación 1: Una composición de prodroga que comprende al menos un conjugado de metilfenidato con una estructura de la fórmula (1) o fórmula (2), donde X se selecciona entre el grupo que consiste en O, S, Se y NR1; donde Y se encuentra ausente o se selecciona entre el grupo que consiste en O, S, Se, NR2 y CR3R4; donde R1 y R2 se seleccionan en forma independiente entre el grupo que consiste en hidrógeno, alquenilo, alquenilaminocarbonilo, alcoxi, alcoxicarbonilo, alquilo, alquilamino, alquilaminocarbonilo, alquilamonio, alquilcarbonilo, alquilcarbonilamino, alquilcarboniloxi, alquilsulfinilo, alquilsulfonilo, alquiltio, alquinilo, alquinilaminocarbonilo, aminocarbonilo, arilo, arilo sustituido, arilalquenilo, arilalcoxi, arilalquilo, arilalquinilo, arilamino, arilaminocarbonilo, arilamonio, arilazo, arilcarbonilo, arilcarbonilamino, arilcarboniloxi, arilcicloalquilo, ariloxi, ariloxialquilo, arilsulfinilo, arilsulfinilalquilo, arilsulfonilo, arilsulfonilamino, ariltio, ariltioalquilo, cicloalquenilo, cicloalquenilalquilo, cicloalquilo, cicloalquilalquilo, cicloalquilamino, cicloalquiloxi, cicloalquinilo, cicloheteroalquilo, cicloheteroalquilalquilo, haloalcoxi, haloalquilo, heteroarilo, heteroarilalquenilo, heteroarilalquilo heteroarilamino, heteroarilcarbonilo, heteroarilcarbonilamino, heteroariloxo, heteroariloxi, heteroarilsulfinilo, heteroarilsulfonilo, heteroariltio, hidroxi, policicloalquenilo, policicloalquenilalquilo, policicloalquilo, policicloalquilalquilo, y polietilenglicol; donde R3 y R4 se seleccionan en forma independiente entre el grupo que consiste en hidrógeno, alquenilo, alquenilaminocarbonilo, alcoxi, alcoxicarbonilo, alquilo, alquilamino, alquilaminocarbonilo, alquilamonio, alquilcarbonilo, alquilcarbonilamino, alquilcarboniloxi, alquilsulfinilo, alquilsulfonilo, alquiltio, alquinilo, alquinilaminocarbonilo, amina, amino, aminocarbonilo, amonio, arilo, arilo sustituido, arilalquenilo, arilalcoxi, arilalquilo, arilalquinilo, arilamino, arilaminocarbonilo, arilamonio, arilazo, arilcarbonilo, arilcarbonilamino, arilcarboniloxi, arilcicloalquilo, ariloxi, ariloxialquilo, arilsulfinilo, arilsulfinilalquilo, arilsulfonilo, arilsulfonilamino, ariltio, ariltioalquilo, ciano, cicloalquenilo, cicloalquenilalquilo, carboxilo, cicloalquilo, cicloalquilalquilo, cicloalquilamino, cicloalquiloxi, cicloalquinilo, cicloheteroalquilo, cicloheteroalquilalquilo, halo, haloalcoxi, haloalquilo, heteroarilo, heteroarilalquenilo, heteroarilalquilo, heteroarilamino, heteroarilcarbonilo, heteroarilcarbonilamino, heteroariloxo, heteroariloxi, heteroarilsulfinilo, heteroarilsulfonilo, heteroariltio, hidroxi, nitro, oxo, policicloalquenilo, policicloalquenilalquilo, policicloalquilo, policicloalquilalquilo, polietilenglicol y tiol; donde L se encuentra ausente o es -[-A-Z-]n-; donde A se selecciona en forma independiente para cada subunidad repetida entre el grupo que consiste en CR5R6, arilo, arilo sustituido, arileno, carbociclo, cicloalquenilo, cicloalquilo, cicloalquinilo, heterociclo y heteroarilo; donde R5 y R6 se seleccionan en forma independiente entre sí y en forma independiente para cada subunidad repetida entre el grupo que consiste en hidrógeno, alquenilo, alquenilaminocarbonilo, alcoxi, alcoxicarbonilo, alquilo, alquilamino, alquilaminocarbonilo, alquilamonio, alquilcarbonilo, alquilcarbonilamino, alquilcarboniloxi, alquilsulfinilo, alquilsulfonilo, alquiltio, alquinilo, alquinilaminocarbonilo, amina, amino, aminocarbonilo, amonio, arilo, arilo sustituido, arilalquenilo, arilalcoxi, arilalquilo, arilalquinilo, arilamino, arilaminocarbonilo, arilamonio, arilazo, arilcarbonilo, arilcarbonilamino, arilcarboniloxi, arilcicloalquilo, ariloxi, ariloxialquilo, arilsulfinilo, arilsulfinilalquilo, arilsulfonilo, arilsulfonilamino, ariltio, ariltioalquilo, ciano, cicloalquenilo, cicloalquenilalquilo, carboxilo, cicloalquilo, cicloalquilalquilo, cicloalquilamino, cicloalquiloxi, cicloalquinilo, cicloheteroalquilo, cicloheteroalquilalquilo, halo, haloalcoxi, haloalquilo, heteroarilo, heteroarilalquenilo, heteroarilalquilo, heteroarilamino heteroarilcarbonilo, heteroarilcarbonilamino, heteroariloxo, heteroariloxi, heteroarilsulfinilo, heteroarilsulfonilo, heteroariltio, hidroxi, nitro, oxo, policicloalquenilo, policicloalquenilalquilo, policicloalquilo, policicloalquilalquilo, polietilenglicol y tiol; donde Z está ausente o se selecciona en forma independiente para cada subunidad repetida entre el grupo que consiste en O, S, Se y NH; donde n es 0 - 50; donde G se selecciona en forma independiente para cada subunidad repetida entre el grupo que consiste en alcohol, amina, aminoácido, amonio, oxoácido, péptido, poli(etilenglicol) (PEG), tiol, derivados de los mismos y combinaciones de los mismos; donde E es un oxoácido; y donde m es 0 - 5.
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