AR046544A1 - ORAL ACID ADMINISTRATION [2- (8,9 - DIOXO - 2,6 - DIAZABICICLO [5.2.0] NON -1 (7) - EN - 2 - IL) RENT] PHOSPHONIC YDERIVADOS - Google Patents

ORAL ACID ADMINISTRATION [2- (8,9 - DIOXO - 2,6 - DIAZABICICLO [5.2.0] NON -1 (7) - EN - 2 - IL) RENT] PHOSPHONIC YDERIVADOS

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Publication number
AR046544A1
AR046544A1 ARP040103716A AR046544A1 AR 046544 A1 AR046544 A1 AR 046544A1 AR P040103716 A ARP040103716 A AR P040103716A AR 046544 A1 AR046544 A1 AR 046544A1
Authority
AR
Argentina
Prior art keywords
group
aryl
disorders
cycloalkyl
hydrogen
Prior art date
Application number
Other languages
Spanish (es)
Inventor
Eric J Benjamin
William F Cloud
Michael R Brandt
Gerald F Tremblay
Mohammed Islam
Original Assignee
Wyeth Corp
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37598185&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR046544(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of AR046544A1 publication Critical patent/AR046544A1/en

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Abstract

Formas farmacéuticas sólidas de dosificación de ácido [2-(8,9-dioxo-2,6-diazabiciclo[5.2.0]non-1(7)-en-2-il)alquil]fosfónico y derivados del mismo. Métodos de uso para el tratamiento, inter alia, de trastornos vasculares cerebrales, trastornos de ansiedad; trastornos anímicos; esquizofrenia; trastornos esquizofreniformes; trastornos esquizoafectivo; deficiencia cognitiva; trastornos neurodegenerativos crónicos; enfermedades inflamatorias; fibromialgia; complicaciones de herpes zoster; prevención de tolerancia a analgesia con opioides; síntomas de retirada de fármacos adictivos; y dolor. Composiciones farmacéuticas. Proceso. Reivindicación 1: Una forma farmacéutica de dosificación sólida, que comprende: al menos un compuesto de fórmula (1) o una sal farmacéuticamente aceptable del mismo, en la que: R1 es hidrógeno, un grupo alquilo C1-6, un grupo acilo C2-7, un grupo alcanosulfonilo C1-6 o un grupo aroilo C6-14; A es alquilenilo C1-4 o alquenilenilo C2-4; R2 y R3 se seleccionan independientemente entre hidrógeno, o un compuesto del grupo de fórmulas (2), con la condición de que al menos uno de R2 y R3 sea distinto de hidrógeno; R4 y R5 se seleccionan independientemente entre hidrógeno, un grupo alquilo C1-4, un grupo arilo C5-7, un grupo aralquilo C6-15 con C5-7 en el anillo arilo, un grupo alquenilo C2-7 o un grupo alquinilo C2-7 o R4 y R5 pueden formar juntos un anillo espero C3-8 carbocíclico; R6 es un grupo alquilo C1-12 lineal o ramificado, un grupo alquenilo o alquinilo C2-7 lineal o ramificado, un grupo arilo C5-13, un grupo aralquilo C6-21 con C5-13 en el resto arilo; un grupo heteroarilo de 5 a 13 miembros, un grupo heteroalquilo de 6 a 21 miembros con 5 a 13 miembros en el resto heteroarilo, un grupo cicloalquilo C4-8, un grupo cicloalquilalquilo C5-16 con C4-8 en el anillo cicloalquilo; R7 y R8 se seleccionan independientemente entre hidrógeno, un grupo alquilo C1-12 lineal o ramificado, un grupo alquenilo o alquinilo C2-7 lineal o ramificado, un grupo arilo C5-13, un grupo aralquilo C6-21 con C5-13 en el resto arilo, un grupo heteroarilo de 5 a 13 miembros, un grupo heteroarilo de 6 a 21 miembros con 5 a 13 miembros en el resto heteroarilo o R7 y R8 pueden formar juntos un grupo cicloalquilo o heterocicloalquilo que tiene en el anillo C4-8 y opcionalmente de uno a dos átomos seleccionados entre nitrógeno, oxígeno o azufre; donde cualquier grupo R1 a R8 con un resto arilo, heteroarilo, cicloalquilo o heterocicloalquilo puede sustituirse opcionalmente en el resto arilo, heteroarilo, cicloalquilo o heterocicloalquilo con 1 a aproximadamente 5 sustituyentes seleccionados independientemente entre un grupo halo, ciano, nitro, o hidroxilo, un grupo alquilo C1-6, o un grupo alcoxi C1-6; y al menos un potenciador de la absorción farmacéuticamente aceptable. Reivindicación 19: Una forma de dosificación de acuerdo con cualquiera de las reivindicaciones 1 a 18, en la que dicho potenciador de absorción farmacéuticamente aceptable es un tensioactivo, sal biliar, ácido graso, sal de ácido graso, agente quelante, acil carnitina, acil colina o una mezcla de los mismos. Reivindicación 21: Una forma de dosificación de acuerdo con la reivindicación 20, en la que dicho tensioactivo iónico es lauril sulafo sódico, dioctil sulfosuccinato sódico o una mezcla de los mismos. Reivindicación 105: Una composición farmacéutica sólida de liberación inmediata en forma de dosificación unitaria simple o de forma unitaria múltiple, que comprende: ácido [2-(8,9-dioxo-2,6-diazabiciclo[5.2.0]non-1(7)-en-2-il)alquil]fosfónico o una sal farmacéuticamente aceptable del mismo; en la que dicha composición muestra una Cmax en plasma, después de la administración a un sujeto en necesidad del mismo, del compuesto de fórmula (1) de aproximadamente 80 ng/ml a aproximadamente 4200 ng/ml.Solid dosage forms of [2- (8,9-dioxo-2,6-diazabicyclo [5.2.0] non-1 (7) -en-2-yl) alkyl] phosphonic acid and derivatives thereof. Methods of use for the treatment, inter alia, of cerebral vascular disorders, anxiety disorders; mood disorders; schizophrenia; schizophreniform disorders; schizoaffective disorders; cognitive deficiency; chronic neurodegenerative disorders; inflammatory diseases; fibromyalgia; complications of herpes zoster; prevention of tolerance to opioid analgesia; withdrawal symptoms of addictive drugs; and pain Pharmaceutical compositions Process. Claim 1: A solid dosage pharmaceutical form, comprising: at least one compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen, a C1-6 alkyl group, a C2- acyl group 7, a C1-6 alkanesulfonyl group or a C6-14 aroyl group; A is C1-4 alkylenyl or C2-4 alkenylenyl; R2 and R3 are independently selected from hydrogen, or a compound from the group of formulas (2), with the proviso that at least one of R2 and R3 is other than hydrogen; R4 and R5 are independently selected from hydrogen, a C1-4 alkyl group, a C5-7 aryl group, a C6-15 aralkyl group with C5-7 in the aryl ring, a C2-7 alkenyl group or a C2- alkynyl group 7 or R4 and R5 can together form a ring I expect C3-8 carbocyclic; R6 is a linear or branched C1-12 alkyl group, a linear or branched C2-7 alkenyl or alkynyl group, a C5-13 aryl group, a C6-21 aralkyl group with C5-13 in the aryl moiety; a 5 to 13 membered heteroaryl group, a 6 to 21 membered heteroalkyl group with 5 to 13 members in the heteroaryl moiety, a C4-8 cycloalkyl group, a C5-16 cycloalkylalkyl group with C4-8 in the cycloalkyl ring; R7 and R8 are independently selected from hydrogen, a linear or branched C1-12 alkyl group, a linear or branched C2-7 alkenyl or alkynyl group, a C5-13 aryl group, a C6-21 aralkyl group with C5-13 in the aryl moiety, a 5-13 membered heteroaryl group, a 6 to 21 membered heteroaryl group with 5 to 13 members on the heteroaryl moiety or R7 and R8 can together form a cycloalkyl or heterocycloalkyl group having the C4-8 ring and optionally one to two atoms selected from nitrogen, oxygen or sulfur; wherein any group R1 to R8 with an aryl, heteroaryl, cycloalkyl or heterocycloalkyl moiety may optionally be substituted on the aryl, heteroaryl, cycloalkyl or heterocycloalkyl moiety with 1 to about 5 substituents independently selected from a halo, cyano, nitro, or hydroxyl group, a C1-6 alkyl group, or a C1-6 alkoxy group; and at least one pharmaceutically acceptable absorption enhancer. Claim 19: A dosage form according to any one of claims 1 to 18, wherein said pharmaceutically acceptable absorption enhancer is a surfactant, bile salt, fatty acid, fatty acid salt, chelating agent, acyl carnitine, acyl choline or a mixture thereof. Claim 21: A dosage form according to claim 20, wherein said ionic surfactant is sodium lauryl sulafo, dioctyl sodium sulfosuccinate or a mixture thereof. Claim 105: A solid pharmaceutical composition of immediate release in single unit dosage form or multiple unit form, comprising: acid [2- (8,9-dioxo-2,6-diazabicyclo [5.2.0] non-1 ( 7) -en-2-yl) alkyl] phosphonic or a pharmaceutically acceptable salt thereof; wherein said composition shows a plasma Cmax, after administration to a subject in need thereof, of the compound of formula (1) from about 80 ng / ml to about 4200 ng / ml.

ARP040103716 2003-10-15 2004-10-13 ORAL ACID ADMINISTRATION [2- (8,9 - DIOXO - 2,6 - DIAZABICICLO [5.2.0] NON -1 (7) - EN - 2 - IL) RENT] PHOSPHONIC YDERIVADOS AR046544A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US51156003P 2003-10-15 2003-10-15

Publications (1)

Publication Number Publication Date
AR046544A1 true AR046544A1 (en) 2005-12-14

Family

ID=37598185

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040103716 AR046544A1 (en) 2003-10-15 2004-10-13 ORAL ACID ADMINISTRATION [2- (8,9 - DIOXO - 2,6 - DIAZABICICLO [5.2.0] NON -1 (7) - EN - 2 - IL) RENT] PHOSPHONIC YDERIVADOS

Country Status (3)

Country Link
CN (1) CN1893954A (en)
AR (1) AR046544A1 (en)
ZA (1) ZA200603035B (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2498756T4 (en) * 2009-11-09 2023-03-20 Wyeth Llc TABLET FORMULATIONS OF NERATINIM MALEATE
EP4003309A1 (en) * 2019-07-31 2022-06-01 F. Hoffmann-La Roche AG New pharmaceutical formulation

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Publication number Publication date
CN1893954A (en) 2007-01-10
ZA200603035B (en) 2009-09-30

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