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AR072753A1 - Derivados de oxazina como inhibidores de 11 beta - hidroxiesteroiode deshidrogenasa 1 - Google Patents

Derivados de oxazina como inhibidores de 11 beta - hidroxiesteroiode deshidrogenasa 1

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Publication number
AR072753A1
AR072753A1 ARP090102841A ARP090102841A AR072753A1 AR 072753 A1 AR072753 A1 AR 072753A1 AR P090102841 A ARP090102841 A AR P090102841A AR P090102841 A ARP090102841 A AR P090102841A AR 072753 A1 AR072753 A1 AR 072753A1
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AR
Argentina
Prior art keywords
alkyl
cycloalkyl
alkoxy
aminocarbonyl
dialkyl
Prior art date
Application number
ARP090102841A
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English (en)
Inventor
Bradford S Hamilton
Matthias Eckardt
Annette Schuler-Metz
Linghang Zhuang
Frank Himmelsbach
Original Assignee
Vitae Pharmaceuticals Inc
Boehringer Ingelheim Int
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Filing date
Publication date
Application filed by Vitae Pharmaceuticals Inc, Boehringer Ingelheim Int filed Critical Vitae Pharmaceuticals Inc
Publication of AR072753A1 publication Critical patent/AR072753A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D413/10—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 aromatic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/08—Antibacterial agents for leprosy
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
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  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pulmonology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Composiciones farmacéuticas de los mismos, que son utiles para el tratamiento terapéutico de enfermedades asociadas con la modulacion o inhibicion de 11beta-HSD1 en mamíferos. Se refiere además a composiciones farmacéuticas de los compuestos nuevos y a métodos para su uso en la reduccion o control de la produccion de cortisol en una célula o la inhibicion de la conversion de cortisona en cortisol en una célula. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1) en la que R1 está (a) ausente o (b) se selecciona de alquilo C1-6, cicloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-3-alcoxi C1-3, o alcoxi C1-3-alquilo C1-3 y está opcionalmente sustituido con hasta 4 grupos independientemente seleccionados de fluor, ciano, oxo, R4, R4O-, (R4)2N-, R4O2C-, R4S, R4S(=O)-, R4S(=O)2-, R4C(O)NR4-, (R4)2NC(=O)-, (R4)2NC(=O)O-, (R4)2NC(=O)NR4-, R4OC(=O)NR4-, (R4)2NC(=NCN)NR4-, (R4O)2P(O)O-, (R4O)2P(=O)NR4-, R4OS(=O)2NR4-, (R4)2NS(=O)2O-, (R4)2NS(=O)2NR4-, R4S(O)2NR4-, R4S(=O)2NHC(=O)-, R4S(=O)2NHC(=O)O-, R4S(=O)2NHC(=O)NR4-, R4OS(=O)2NHC(=O)-, R4OS(=O)2NHC(=O)O-, R4OS(=O)2NHC(=O)NR4-, (R4)2NS(=O)NHC(=O)-, (R4)2NS(=O)2NHC(=O)O-, (R4)2NS(=O)2NHC(=O)NR4-, R4C(=O)NHS(=O)2, R4C(=O)NHS(=O)2O-, R4C(=O)NHS(=O)2NR4-, R4OC(=O)NHS(=O)2-, R4OC(=O)NHS(=O)2O, ROC(=O)NHS(=O)2NR4-, (R4)2NC(=O)NHS(=O)2-, (R4)2NC(=O)NHS(=O)2O-, (R4)2NC(=O)NHS(=O)2NR4-, heterociclilo, heteroarilo, arilamino y heteroarilamino; A1 es (a) un enlace, o (b) alquileno C1-3, CH2CH2O, en el que el oxígeno está unido a Cy1, o CH2C(=O), en el que el carbono carbonílico esta unido a Cy1; Cy1 es arilo, heteroarilo, cicloalquilo monocíclico o heterociclilo monocíclico, y está opcionalmente sustituido con 1 a 4 grupos independientemente seleccionados de fluor, cloro, bromo, yodo, ciano, nitro, amino, hidroxi, carboxi, alquilo C1-6, hidroxialquilo C1-6, cicloalquilo C3-6, hidroxicicloalquilo C3-6, cicloalquilalquilo C4-7, alquenilo C2-6, halogenoalquenilo C2-6, hidroxialquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquinilo C2-4, halogenoalquilo C1-6, halogenocicloalquilo C3-6, halogenocicloalquilalquilo C4-7, alcoxi C1-6, cicloalcoxi C3-6, cicloalquilalcoxi C4-7, halogenoalcoxi C1-6, halogenocicloalcoxi C3-6, halogenocicloalquilalcoxi C4-7, alquiltio C1-6, cicloalquiltio C3-6, cicloalquilalquiltio C4-7, halogenoalquiltio C1-6, halogenocicloalquiltio C3-6, halogenocicloalquilalquiltio C4-7, alcanosulfinilo C1-6, cicloalcanosulfinilo C3-6, cicloalquilalcanosulfinilo C4-7, halogenoalcanosulfinilo C1-6, halogenocicloalcanosulfinilo C3-6, halogenocicloalquilalcanosulfinilo C4-7, alcanosulfonilo C1-6, cicloalcanosulfonilo C3-6, cicloalquilalcanosulfonilo C4-7, halogenoalcanosulfonilo C1-6, halogenocicloalcanosulfonilo C3-6, halogenocicloalquilalcanosulfonilo C4-7, alquilamino C1-6, dialquil C1-6 amino, alcoxi C1-6-alcoxi C1-6, halogenoalcoxi C1-6-alcoxi C1-6, alcoxi C1-6carbonilo, H2NCO, -H2NSO2, alquil C1-6-aminocarbonilo, dialquil C1-6-aminocarbonilo, alcoxi C1-3-alquil C1-3-aminocarbonilo, heterociclilcarbonilo, alquilaminosulfonilo C1-6, dialquil C1-6-aminosulfonilo, heterociclilsulfonilo, alquil C1-6-carbonilamino, alquil C1-6 carbonilamino-alquilo C1-6, alquilsulfonilamino C1-6, alquil C1-6-sulfonilamino-alquilo C1-6, alcoxi C1-6-carbonil-alcoxi C1-6, alcoxi C1-6-alquilo C1-6, halogenoalcoxi C1-6-alquilo C1-6, hidroxialcoxi C1-6, heteroarilo, oxo, aminoalquilo C1-6, alquil C1-6-aminoalquilo C1-6, dialquil C1-6-aminoalquil C1-6-aminoalcoxi C2-6, alquil C1-6-aminoalcoxi C2-6, dialquil C1-6-aminoalcoxi C2-6, alquil C1-6-carbonilo, cicloalquil C3-6-carbonilo, cicloalquil C3-6-aminocarbonilo, {cicloalquil C3-6}{alquil C1-6}aminocarbonilo, di-cicloalquil C3-6-aminocarbonilo, cicloalquil C3-6-aminosulfonilo, {cicloalquil C3-6}{alquilo C1-6}aminosulfonilo, di-cicloalquil C3-6-aminosulfonilo, ciano-alquilo C1-6, aminocarbonil-alquilo C1-6, alquil C1-6-aminocarbonil-alquilo C1-6, dialquil C1-6-aminocarbonil-alquilo C1-6, cicloalquil C3-6-aminocarbonil-alquilo C1-6, {cicloalquil C3-6}{alquil C1-6}aminocarbonilalquilo C1-6 y di-cicloalquil C1-6-aminocarbonil-alquilo C1-6; Cy2 es bencimidazolilo, benzotriazolilo, y piperidinilo y está opcionalmente sustituido con 1 a 4 grupos independientemente seleccionados de fluor, cloro, bromo, yodo, ciano, nitro, amino, hidroxi, carboxi, alquilo C1-6, hidroxialquilo C1-6, cicloalquilo C3-6, hidroxicicloalquilo C3-6, cicloalquilalquilo C4-7, alquenilo C2-6, halogenoalquenilo C2-6, hidroxialquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquinilo C2-4, halogenoalquilo C1-6, halogenocicloalquilo C3-6, halogenocicloalquilalquilo C4-7, alcoxi C1-6, cicloalcoxi C3-6, cicloalquilalcoxi C4-7, halogenoalcoxi C1-6, halogenocicloalcoxi C3-6, halogenocicloalquilalcoxi C4-7, alquiltio C1-6, cicloalquiltio C3-6, cicloalquil C4-7alquiltio, halogenoalquiltio C1-6, halogenocicloalquiltio C3-6, halogenocicloalquilalquiltio C4-7, alcanosulfinilo C1-6, cicloalcanosulfinilo C3-6, cicloalquilalcanosulfinilo C4-7, halogenoalcanosulfinilo C1-6, halogenocicloalcanosulfinilo C3-6, halogenocicloalquil C4-7-alcanosulfinilo, alcanosulfonilo C1-6, cicloalcanosulfonilo C3-6, cicloalquilalcanosulfonilo C4-7, halogenoalcanosulfonilo C1-6, halogenocicloalcanosulfonilo C3-6, halogenocicloalquilalcanosulfonilo C4-7, alquilamino C1-6, dialquil C1-6-amino, alcoxi C1-6-alcoxi C1-6, halogenoalcoxi C1-6-alcoxi C1-6, alcoxi C1-6-carbonilo, H2NCO, H2NSO2, alquil C1-6-aminocarbonilo, dialquil C1-6-aminocarbonilo, alcoxi C1-3-alquil C1-3-aminocarbonilo, heterociclilcarbonilo, alquilaminosulfonilo C1-6, dialquil C1-6-aminosulfonilo, heterociclilsulfonilo, alquil C1-6-carbonilamino, alquil C1-6-carbonilamino-alquilo C1-6, alquilsulfonilamino C1-6, alquilsulfonilamino C1-6-alquilo C1-6, alcoxi C1-6-carbonil-alcoxi C1-6, alcoxi C1-6-alquilo C1-6, halogenoalcoxi C1-6-alquilo C1-6, hidroxialcoxi C1-6, heteroarilo, oxo, aminoalquilo C1-6, alquil C1-6-aminoalquilo C1-6, dialquil C1-6-aminoalquil C1-6-aminoalcoxi C2-6, alquil C1-6-aminoalcoxi C2-6, dialquil C1-6-aminoalcoxi C2-6, alquil C1-6-carbonilo, hidroxialquil C1-6-carbonilo, cicloalquil C3-6-carbonilo, cicloalquil C3-6-aminocarbonilo, {cicloalquil C3-6}{alquil C1-6}aminocarbonilo, di-cicloalquil C3-6-aminocarbonilo, cicloalquil C3-6-aminosulfonilo, {cicloalquil C3-6}{alquilo C1-6}aminosulfonilo, di-cicloalquil C3-6-aminosulfonilo, ciano-alquilo C1-6, aminocarbonil-alquilo C1-6, alquil C1-6-aminocarbonil-alquilo C1-6, dialquil C1-6-aminocarbonil-alquilo C1-6, cicloalquil C3-6-aminocarbonil-alquilo C1-6, {cicloalquil C3-6}{alquil C1-6}aminocarbonilalquilo C1-6 y di-cicloalquil C1-6-aminocarbonil-alquilo C1-6; en el que el piperidinilo representado por Cy1 está unido a Cy1 por un átomo de carbono del anillo; o cuando R3 es metoximetilo, Cy2 es (a) halogeno o -O-SO3-R en el que R es (i) alquilo C1-4 opcionalmente sustituido con uno o más halogenos o (ii) fenilo, opcionalmente sustituido con halogeno, alquilo C1-4 u NO2; o (b) cicloalquilo, arilo, heterociclilo o heteroarilo, opcionalmente sustituido con 1 a 4 grupos independientemente seleccionados de fluor, cloro, bromo, yodo, ciano, nitro, amino, hidroxi, carboxi, alquilo C1-6, hidroxialquilo C1-6, cicloalquilo C3-6, hidroxicicloalquilo C3-6, cicloalquilalquilo C4-7, alquenilo C2-6, halogenoalquenilo C2-6, hidroxialquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquinilo C2-4, halogenoalquilo C1-6, halogenocicloalquilo C3-6, halogenocicloalquilalquilo C4-7, alcoxi C1-6, cicloalcoxi C3-6, cicloalquilalcoxi C4-7, halogenoalcoxi C1-6, halogenocicloalcoxi C3-6, halogenocicloalquilalcoxi C4-7, alquiltio C1-6, cicloalquiltio C3-6, cicloalquilalquiltio C4-7, halogenoalquiltio C1-6, halogenocicloalquiltio C3-6, halogenocicloalquilalquiltio C4-7, alcanosulfinilo C1-6, cicloalcanosulfinilo C3-6, cicloalquilalcanosulfinilo C4-7, halogenoalcanosulfinilo C1-6, halogenocicloalcanosulfinilo C3-6, halogenocicloalquilalcanosulfinilo C4-7, alcanosulfonilo C1-6, cicloalcanosulfonilo C3-6, cicloalquilalcanosulfonilo C4-7, halogenoalcanosulfonilo C1-6, halogenocicloalcanosulfonilo C3-6, halogenocicloalquilalcanosulfonilo C4-7, alquilamino C1-6, dialquil C1-6-amino, alcoxi C1-6-alcoxi C1-6, halogenoalcoxi C1-6-alcoxi C1-6, alcoxi C1-6-carbonilo, H2NCO, H2NSO2, alquil C1-6-aminocarbonilo, dialquil C1-6-aminocarbonilo, alcoxi C1-3-alquil C1-3-aminocarbonilo, heterociclilcarbonilo, alquilaminosulfonilo C1-6, dialquil C1-6-aminosulfonilo, heterociclilsulfonilo, alquil C1-6-carbonilamino, alquil C1-6 carbonilamino-alquilo C1-6, alquilsulfonilamino C1-6, alquil C1-6 sulfonilamino-alquilo C1-6, alcoxi C1-6-carbonil-alcoxi C1-6, alcoxi C1-6-alquilo C1-6, halogenoalcoxi C1-6-alquilo C1-6, hidroxialcoxi C1-6, heteroarilo, oxo, aminoalquilo C1-6, alquil C1-6-aminoalquilo C1-6, dialquil C1-6-aminoalquil C1-6-aminoalcoxi C2-6, alquil C1-6-aminoalcoxi C2-6, dialquil C1-6-aminoalcoxi C2-6, alquil C1-6-carbonilo, cicloalquil C3-6-carbonilo, cicloalquil C3-6-aminocarbonilo, {cicloalquil C3-6}{alquil C1-6}aminocarbonilo, di-cicloalquil C3-6-aminocarbonilo, cicloalquil C3-6-aminosulfonilo, {cicloalquil C3-6}{alquilo C1-6}aminosulfonilo, di-cicloalquil C3-6-aminosulfonilo, ciano-alquilo C1-6, aminocarbonil-alquilo C1-6, alquil C1-6-aminocarbonil-alquilo C1-6, dialquil C1-6-aminocarbonil-alquilo C1-6, cicloalquil C3-6-aminocarbonil-alquilo C1-6, {cicloalquil C3-6}{alquil C1-6}aminocarbonilalquilo C1-6 y di-cicloalquil C1-6-aminocarbonil-alquilo C1-6; Y es alquilo C1-6, halogenoalquilo C1-6 u oxo; n es 0, 1 o 2; E es (a) un enlace o (b) alquileno C1-3 o alqueniloxi C1-2, en el que el O está unido a R2, cada uno de los cuales está opcionalmente sustituido con 1 a 4 grupos independientemente seleccionados de metilo, etilo trifluorometilo u oxo; R2 es alquilo C1-6, arilo, heteroarilo, cicloalquilo, o heterociclilo y está opcionalmente sustituido con hasta 4 grupos independientemente seleccionados de fluor, cloro, bromo, yodo, ciano, nitro, amino, hidroxi, carboxi, alquilo C1-6, hidroxialquilo C1-6, cicloalq
ARP090102841A 2008-07-25 2009-07-24 Derivados de oxazina como inhibidores de 11 beta - hidroxiesteroiode deshidrogenasa 1 AR072753A1 (es)

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US13593308P 2008-07-25 2008-07-25
US20676709P 2009-02-04 2009-02-04

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US (1) US8846668B2 (es)
EP (1) EP2324017B1 (es)
JP (1) JP5777030B2 (es)
AR (1) AR072753A1 (es)
CA (1) CA2729998A1 (es)
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