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AR082458A1 - Combinacion que comprende un farmaco antipsicotico y un agonista de taar1 - Google Patents

Combinacion que comprende un farmaco antipsicotico y un agonista de taar1

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Publication number
AR082458A1
AR082458A1 ARP110102780A AR082458A1 AR 082458 A1 AR082458 A1 AR 082458A1 AR P110102780 A ARP110102780 A AR P110102780A AR 082458 A1 AR082458 A1 AR 082458A1
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AR
Argentina
Prior art keywords
phenyl
lower alkyl
halogen
hydrogen
dihydro
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English (en)
Inventor
Marius Hoener
Susanne Raab
Celine Risterucci
Sabine Sewing
Original Assignee
Hoffmann La Roche
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44512842&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR082458(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR082458A1 publication Critical patent/AR082458A1/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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links

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Abstract

Combinación farmacéutica destinada al tratamiento de la esquizofrenia y de episodios maniacos agudos asociados a trastornos bipolares, que comprende un compuesto que es activo sobre un receptor 1 asociado a aminas traza (agonista TAAR1) y un fármaco antipsicótico. Composiciones farmacéuticas que comprenden una combinación de un fármaco antipsicótico atípico y un agonista de TAAR1 tal como se describe en reivindicación 2, 3 y 4.Reivindicación 1: Combinación que comprende un fármaco antipsicótico atípico y un agonista de TAAR1. Reivindicación 2: Combinación según la reivindicación 1, que comprende olanzapina y un agonista de TAAR1 de fórmula (1) en la que: R1 es hidrógeno, deuterio, tritio, alquilo inferior, hidroxi, alcoxi inferior, alquilo inferior sustituido con halógeno, alcoxi inferior sustituido con halógeno, halógeno, fenilo opcionalmente sustituido con halógeno, o es feniloxi, bencilo, benciloxi, -COO-alquilo inferior, -O-(CH2)o-O-alquilo inferior, NH-cicloalquilo, cicloalquilo o tetrahidropirán-4-iloxi, en los que los sustituyentes para n > 1 pueden ser iguales o diferentes; X es un enlace, -CHR-, -CHRCHR’-, -OCH2-, -NRCHR’, -OCHRCHR’, -CH2OCHR-, -CH2CH2CH2-, -SCH2-, -S(O)2CH2-, -CH2SCH2-, -CH2N(R)CH2-, -cicloalquil-CH2- o SiRR’-CH2-; R/R’ puede ser, independientemente uno de otro, hidrógeno, alquilo inferior o alquilo inferior sustituido con halógeno; R2 es hidrógeno, fenilo o alquilo inferior; Y es fenilo, naftilo, tiofenilo, piridinilo, cicloalquilo, 1,2,3,4-tetrahidronaftalén-2-ilo, 2,3-dihidrobenzo[1,4]dioxin-6-ilo o benzo[1,3jdioxol-5-ilo; n es 0, 1, 2 ó 3; o es 2 ó 3; o una sal de adición de ácido farmacéuticamente aceptable de los mismos, o un agonista de TAAR1 de fórmula (2) en la que R es hidrógeno o alquilo inferior; R1 es -(CH2)n-(O)o-heterocicloalquilo, opcionalmente sustituido con alquilo inferior, hidroxi, halógeno, o con -(CH2)p-arilo; n es 0, 1 ó 2; o es 0 ó1; p es 0, 1 ó 2; R2 es cicloalquilo, heterocicloalquilo, o es arilo o heteroarilo, en el que los anillos aromáticos se sustituyen opcionalmente con uno o dos sustituyentes, seleccionados de entre alquilo inferior, halógeno, heteroarilo, CF3, OCF3, OCH2CF3, alcoxi inferior, CH2-alcoxi inferior, alquinilo inferior o ciano; X es un enlace, -NR’-, -CH2NH-, -CHR’’-, -(CH2)q-O- o -(CH2)2-; R’ es hidrógeno o alquilo inferior; R’’ es hidrógeno, alquilo inferior, alcoxi inferior; q es 0, 1 ó 2; o una sal de adición de ácido farmacéuticamente aceptable de los mismos. Reivindicación 3: Combinación según la reivindicación 2, que comprende olanzapina y un agonista de TAAR1 de fórmula (3) en la que R1 es hidrógeno, alquilo inferior, hidroxi, alcoxi inferior, alquilo inferior sustituido con halógeno, alcoxi inferior sustituido con halógeno o halógeno, en el que los sustituyentes para n = 2 pueden ser iguales o diferentes; X es un enlace, -NRCHR’, -CHRCHR’ o -OCHRCHR’; R/R’ puede ser, independientemente uno de otro, hidrógeno, alquilo inferior; n es 1 ó 2; o un agonista de TAAR1 de fórmula (2) en la que R es hidrógeno; R1 es pirrolidinilo; R2 es arilo o heteroarilo, en el que los anillos aromáticos se sustituyen opcionalmente con halógeno; X es un enlace o -NR’-; R’ es hidrógeno o alquilo inferior; o una sal de adición de ácido farmacéuticamente aceptable de los mismos. Reivindicación 4: Combinación según las reivindicaciones 1 a 3, que comprende olanzapina y un agonista de TAAR1, siendo los agonistas de TAAR1: S1 = (S)-4-((S)-2-fenil-butil)-4,5-dihidro-oxazol-2-ilamina, S2 = (S)-4-(3-fluoro-2-metil-fenil)-4,5-dihidro-oxazol-2-ilamina, S3 = (S)-4-(4-cloro-2-trifluorometil-fenil)-4,5-dihidro-oxazol-2-ilamina, S4 = (S)-4-[(etil-fenil-amino)-metil]-4,5-dihidro-oxazol-2-ilamina, S5 = 3-[(S)-1-((S)-2-amino-4,5-dihidro-oxazol-4-ilmetil)-propoxi]-fenol, S6 = (4-pirrolidin-3-il-fenil)-amida de ácido 5-cloro-piridin-2-carboxílico, S7 = 4-cloro-N-(4-pirrolidin-3-il-fenil)-benzamida, S8 = 1-(5-cloro-piridin-2-il)-3-(4-pirrolidin-3-il-fenil)urea, S9 = (S)-4-[(S)-1-(4-fluoro-fenil)-etoximetil]-4,5-dihidro-oxazol-2-ilamina, S10 = {4-[2-((S)-2-amino-4,5-dihidro-oxazol-4-il)-etil]-fenil}-amida de ácido 5-cloro-pirimidin-2-carboxílico, S11 = N-{4-[2-((S)-2-amino-4,5-dihidro-oxazol-4-il)-etil]-fenil}-4-cloro-benzamida, S12 = (R)-2-cloro-6-metil-N-(4-(morfolin-2-il)fenil)isonicotinamida, S13 = (S)-N-(4-(morfolin-2-il)fenil)-6-(2,2,2-trifluoroetoxi)nicotinamida, S14 = (S)-N-(4-(morfolin-2-il)fenil)-2-(trifluorometil)isonicotinamida, S15 = (S)-1-(4-fluorobencil)-3-(4-(morfolin-2-il)fenil)urea, S16 = (S)-1-(3-cianofenil)-3-(4-(morfolin-2-il)fenil)urea, y S17 = (S)-6-cloro-N-(4-(morfolin-2-il)fenil)nicotinamida. Reivindicación 5: Compuesto S2 = (S)-4-(3-fluoro-2-metil-fenil)-4,5-dihidro-oxazol-2-ilamina, comprendido por las fórmulas (1) ó (3) según las reivindicaciones 2 y 3. Reivindicación 6: Combinación según las reivindicaciones 1 a 4, que comprende olanzapina y un agonista de TAAR1 para el tratamiento de la esquizofrenia y de los episodios de manía asociados al trastorno bipolar, con una incidencia reducida de síndrome metabólico. Reivindicación 7: Combinación según la reivindicación 6, que comprende olanzapina y un agonista de TAAR1 para el tratamiento de la esquizofrenia y de los episodios de manía asociados al trastorno bipolar, con eficacia antidiabética. Reivindicación 9: Combinación según la reivindicación 8, que comprende olanzapina y un agonista de TAAR1 para el tratamiento de la esquizofrenia y de los episodios de manía asociados al trastorno bipolar, con eficacia antidiabética, que resulta en la reducción de la masa grasa y el peso corporal. Reivindicación 16: Método para el tratamiento de la esquizofrenia y los episodios maníacos asociados al trastorno bipolar según la reivindicación 15, en el que la incidencia reducida de síndrome metabólico resulta de la eficacia antidiabética con reducción de las excursiones de la glucosa sanguínea, la masa grasa y el peso corporal, que comprende administrar en un ser humano que necesita del mismo una cantidad efectiva de una combinación que comprende un fármaco antipsicótico atípico y un agonista de TAAR1.
ARP110102780 2010-08-02 2011-08-02 Combinacion que comprende un farmaco antipsicotico y un agonista de taar1 AR082458A1 (es)

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JP (2) JP5749802B2 (es)
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MX2013000745A (es) 2013-03-05
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JP2013536181A (ja) 2013-09-19
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