AR048934A1 - Morfolinas - Google Patents

Morfolinas

Info

Publication number
AR048934A1
AR048934A1 ARP050101666A ARP050101666A AR048934A1 AR 048934 A1 AR048934 A1 AR 048934A1 AR P050101666 A ARP050101666 A AR P050101666A AR P050101666 A ARP050101666 A AR P050101666A AR 048934 A1 AR048934 A1 AR 048934A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
phenyl
ochf2
ocf3
Prior art date
Application number
ARP050101666A
Other languages
English (en)
Original Assignee
Pfizer
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=32482498&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR048934(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer filed Critical Pfizer
Publication of AR048934A1 publication Critical patent/AR048934A1/es

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Classifications

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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
    • C07D413/06—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 carbon chain containing only aliphatic carbon atoms
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—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
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    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)

Abstract

Morfolinas utiles como agentes en el tratamiento de afecciones que incluyen trastornos urinarios, dolor, eyaculacion precoz, ADHD y fibromialgia. También se proporcionan composiciones farmacéuticas que comprenden uno o más compuestos de formula (1). Reivindicacion 1: Uso de un compuesto de formula (1) en la fabricacion de un medicamento para el tratamiento de un trastorno en mamíferos en el que está implicada la regulacion de la funcion del trasportador de monoaminas, en el que el trastorno se selecciona entre trastornos urinarios, dolor, eyaculacion precoz, ADHD y fibromialgia, y los derivados farmacéutica y/o veterinariamente aceptables de los mismos, en la que: R1 es H o alquilo C1-6; R2 es arilo, het, (CH2)zarilo o R4, donde cada uno de los grupos arilo, het y R4 está opcionalmente sustituido con al menos un sustituyente seleccionado independientemente entre alquilo C1-6, alcoxi C1-6, OH, halo, CF3, OCF3, OCHF2, O(CH2)yCF3, CN, CONH2, CON(H)-alquilo C1-6, CON(alquilo C1-6)2, hidroxi-alquilo C1-6, alcoxi C1-4-alquilo C1-6, alcoxi C1-4-alcoxi C1-4, SCF3, alquil C1-6-SO2-, alquil C1-4-S-alquilo C1-4, alquil C1-4-S-, alquil C1-4-NR10R11 y NR10R11; cada R3 se selecciona independientemente entre alquilo C1- 6, alcoxi C1-6, OH, halo, CF3, OCF3, OCHF2, O(CH2)yCF3, CN, CONH2, CON(H)-alquilo C1-6, CON(alquilo C1-6)2, hidroxi-alquilo C1-6, alcoxi C1-4-alquilo C1-6, alcoxi C1-4-alcoxi C1-4, SCF3, alquil C1-6-SO2-, alquil C1-4-S-alquilo C1-4, alquil C1-4-S-, alquil C1-4-NR10R11 y NR10R11; n es un numero entero entre 0 y 4, en la que cuando n es 2, los dos grupos R3 junto con el anillo fenilo al que están unidos pueden representar un anillo bicíclico benzocondensado que comprende un grupo fenilo condensado a un grupo carbocíclico de 5 o 6 miembros, o un grupo fenilo condensado a un grupo heterocíclico de 5 o 6 miembros que contiene al menos un heteroátomo N, O o S; R4 es un grupo fenilo condensado a un grupo carbocíclico de 5 o 6 miembros, o un grupo fenilo condensado a un grupo heterocíclico de 5 o 6 miembros que contiene al menos un heteroátomo N, O o S; R10 y R11 son iguales o diferentes y son independientemente H o alquilo C1-4; y es 1 o 2; z es un numero entero de 1 a 3; arilo es fenilo, naftilo, antracilo o fenantrilo; y het es un heterociclo aromático o no aromático de 4, 5 o 6 miembros que contiene al menos un heteroátomo N, O o S, opcionalmente condensado a un grupo carbocíclico de 5 o 6 miembros o a un segundo heterociclo de 4, 5 o 6 miembros que contiene al menos un heteroátomo N, O o S; con la condicion de que el compuesto no es 2-[(2-etoxifenoxi)(fenil)metil]morfolina. Reivindicacion 12: Un compuesto de formula (2) y los derivados farmacéutica y/o veterinariamente aceptables del mismo, en la que: R1, R2, R4, R10, R11, y, z, arilo y het son como se han definido en cualquiera de las reivindicaciones 1 a 10; R5 es alquilo C1-6, alcoxi C1-6, halo, CF3, OCF3, OCHF2, O(CH2)yCF3, CN, hidroxi-alquilo C1-6, alcoxi C1-4-alquilo C1-6, alcoxi C1-4-alcoxi C1-4, SCF3, alquil C1-6-SO2-, alquil C1-4-S-alquilo C1-4 o alquil C1-4-S-; cada uno de R6, R7 y R8 se selecciona independientemente entre H, alquilo C1-6, alcoxi C1-6, halo, CF3, OCF3, OCHF2, O(CH2)yCF3, CN, hidroxi-alquilo C1-6, alcoxi C1-4-alquilo C1-6, alcoxi C1-4-alcoxi C1-4, SCF3, alquil C1-6-SO2-, alquil C1-4-S-alquilo C1-4 o alquil C1-4-S-; cada dos de R6, R7 o R8 junto con el anillo fenilo al que están unidos pueden representar un anillo bicíclico benzocondensado que comprende un grupo fenilo condensado a un grupo carbocíclico de 5 o 6 miembros, o un grupo fenilo condensado a un grupo heterocíclico de 5 o 6 miembros que contiene al menos un heteroátomo N, O o S; con la condicion de que al menos uno de R6, R7 o R8 no es H. Reivindicacion 27: Un compuesto de formula (3), o una sal farmacéuticamente aceptable del mismo; en la que: los dos carbonos identificados con un ô*ö tienen la conformacion S; R1 es H o alquilo C1-6; R2 es fenilo o piridinilo que está opcionalmente sustituido con de uno a tres sustituyentes seleccionados independientemente entre alquilo C1-6, alcoxi C1-6, OH, halo, CF3, OCF3, OCHF2, o CN; n es un numero entero de 1 a 5; y R3 se selecciona independientemente entre alquilo C1-6, alcoxi C1-6, OH, halo, CF3, OCF3, OCHF2, o CN; con la condicion de que el compuesto no es 2-[(2-etoxifenoxi)(fenil)metil]morfolina.
ARP050101666A 2004-04-30 2005-04-28 Morfolinas AR048934A1 (es)

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