AR071236A1 - Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1 - Google Patents

Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1

Info

Publication number
AR071236A1
AR071236A1 ARP090101584A ARP090101584A AR071236A1 AR 071236 A1 AR071236 A1 AR 071236A1 AR P090101584 A ARP090101584 A AR P090101584A AR P090101584 A ARP090101584 A AR P090101584A AR 071236 A1 AR071236 A1 AR 071236A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
nhs
2nhc
alkylamino
Prior art date
Application number
ARP090101584A
Other languages
English (en)
Original Assignee
Vitae Pharmaceuticals Inc
Boehringer Ingelheim Int
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
Priority claimed from PCT/US2008/009017 external-priority patent/WO2009017664A1/en
Application filed by Vitae Pharmaceuticals Inc, Boehringer Ingelheim Int filed Critical Vitae Pharmaceuticals Inc
Publication of AR071236A1 publication Critical patent/AR071236A1/es

Links

Classifications

    • 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
    • C07D413/02—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

xi C1-6, halocicloalcoxi C3-6, halocicloalquilalcoLa presente solicitud se refiere a sales farmacéutxi C4-7, alquiltio C1-6, cicloalquiltio C3-6, cicloalquilalquiltio C4-7, haloalquiltio C1-6, halocicicamente aceptables de los mismos y a composiciones farmacéuticas de los mismos, que son utiles paraloalquiltio C3-6, halocicloalquilalquiltio C4-7, alcanosulfinilo C1-6, cicloalcanosulfinilo C3-6, ci el tratamiento terapéutico de enfermedades asociacloalquilalcanosulfinilo C4-7, haloalcanosulfinilodas con la modulacion o inhibicion de 11beta-HSD1 en mamíferos, también se refiere a composiciones f C1-6, halocicloalcanosulfinilo C3-6, halocicloalqarmacéuticas de los compuestos y a métodos para suuilalcanosulfinilo C4-7, alcanosulfonilo C1-6, cic uso en la reduccion o control de la produccion deloalcanosulfonilo C3-6, cicloalquilalcanosulfonilo cortisol en una célula o la inhibicion de la conv C4-7, haloalcanosulfonilo C1-6, halocicloalcanosulfonilo C3-6, halocicloalquilalcanosulfonilo C4-7,ersion de cortisona en cortisol en una célula. Reivindicacion 1: Un compuesto de formula (1) en la q alquilamino C1-6, dialquilamino C1-6, alcoxi C1-6-alcoxi C1-6, haloalcoxi C1-6-alcoxi C1-6, alcoxicue: R1 está (a) ausente o (b) se selecciona entre arbonilo C1-6, H2NCO, H2NSO2, alquilaminocarboniloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-3-alcoxi C1-3 o alcoxi C1-3-alquilo C1-3 y e C1-6, dialquilaminocarbonilo C1-6, alcoxi C1-3-alstá opcionalmente sustituido hasta con cuatro grupquilaminocarbonilo C1-3, heterociclilcarbonilo, alquilaminosulfonilo C1-6, dialquilaminosulfonilo C1os seleccionados independientemente entre fluor, c-6, heterociclilsulfonilo, alquilcarbonilamino C1-iano, oxo, R4, R4O-, (R4)2N-, R4O2C-, R4S, R4S(=O)6, alquilcarbonilamino C1-6-alquilo C1-6, alquilsu-, R4S(=O)2-, R4C(=O)NR4-, (R4)2NC(=O)-, (R4)2NC(=O)O-, (R4)2NC(=O)NR4-, R4OC(=O)NR4-, (R4)2NC(=NCN)lfonilamino C1-6, alquilsulfonilamino C1-6-alquilo C1-6, alcoxicarbonil C1-6-alcoxi C1-6, alcoxi C1-NR4-, (R4O)2P(=O)O-, (R4O)2P(=O)NR4-, R4OS(=O)2NR4-, (R4)2NS(=O)2O-, (R4)2NS(=O)2NR4-, R4S(=O)2NR4-,6-alquilo C1-6, haloalcoxi C1-6-alquilo C1-6, hidroxialcoxi C1-6, heteroarilo, oxo, aminoalquilo C1- R4S(=O)2NHC(=O)-, R4S(=O)2NHC(=O)O-, R4S(=O)2NHC(=O)NR4-, R4OS(=O)2NHC(=O)-, R4OS(=O)2NHC(=O)O-, R46, alquilamino C1-6-alquilo C1-6, dialquilamino C1OS(=O)2NHC(=O)NR4-, (R4)2NS(=O)2NHC(=O)-, (R4)2NS(-6-alquilamino C1-6-alcoxi C2-6, alquilamino C1-6-alcoxi C2-6, dialquilamino C1-6-alcoxi C2-6, alqui=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-, R4lcarbonilo C1-6, cicloalquilcarbonilo C3-6, cicloaOC(=O)NHS(=O)2-, R4OC(=O)NHS(=O)2O-, R4OC(=O)NHS(=lquilaminocarbonilo C3-6, cicloalquil C3-6-alquil O)2NR4-, (R4)2NC(=O)NHS(=O)2-, (R4)2NC(=O)NHS(=O)2C1-6aminocarbonilo, dicicloalquilaminocarbonilo C3O-, (R4)2NC(=O)NHS(=O)2NR4, heterociclilo, heteroa-6, cicloalquilaminosulfonilo C3-6, cicloalquil C3-6-alquil C1-6aminosulfonilo, dicicloalquilaminosurilo, arilamino y heteroarilamino; A1 es (a) un enlace o (b) alquileno C1-3, CH2CH2O, donde el oxígelfonilo C3-6, cianoalquilo C1-6, aminocarbonilalquilo C1-6, alquilaminocarbonil C1-6-alquilo C1-6, dno está unido a Cy1 o CH2C(=O), donde el carbono dialquilaminocarbonil C1-6-alquilo C1-6, cicloalquiel carbonilo está unido a Cy1; Cy1 es arilo, heteroarilo, cicloalquilo monocíclico o heterociclilo mlaminocarbonil C3-6-alquilo C1-6, cicloalquil C3-6-alquil C1-6-aminocarbonilalquilo C1-6 y dicicloalonocíclico y está opcionalmente sustituido con 1 aquilaminocarbonil C3-6-alquilo C1-6; R3 se selecci 4 grupos seleccionados independientemente entre fona entre alquilo C1-6, alquenilo C2-6, alquinilo luor, cloro, bromo, yodo, ciano, nitro, amino, hidroxi, carboxi, alquilo C1-6, hidroxialquilo C1-6, C2-6, cicloalquil C3-5-alquilo C1-4, alcoxi C1-3-acicloalquilo C3-6, hidroxicicloalquilo C3-6, ciclolcoxi C1-3 o alcoxi C1-3-alquilo C1-3 y está opcionalmente sustituido hasta con cuatro grupos seleccalquilalquilo C4-7, alquenilo C2-6, haloalquenilo ionados independientemente entre fluor, ciano, oxoC2-6, hidroxialquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquinilo C2-4, haloalquilo C1-6, halo, R4, R4O-, (R4)2N-, R4O2C-, R4C(=O)O-, R4S, R4S(=cicloalquilo C3-6, halocicloalquilalquilo C4-7, alO)-, R4S(=O)2-, R4C(=O)NR4-, (R4)2NC(=O)-, (R4)2NCcoxi C1-6, cicloalcoxi C3-6, cicloalquilalcoxi C4-(=O)O-, (R4)2NC(=O)NR4-, R4OC(=O)NR4-, (R4)2NC(=NC7, haloalcoxi C1-6, halocicloalcoxi C3-6, halociclN)NR4-, (R4O)2P(=O)O-, (R4O)2P(=O)NR4-, R4OS(=O)2Noalquilalcoxi C4-7, alquiltio C1-6, cicloalquiltioR4-, (R4)2NS(=O)2O-, (R4)2NS(=O)2NR4-, R4S(=O)2NR4 C3-6, cicloalquilalquiltio C4-7, haloalquiltio C1-, R4S(=O)2NHC(=O)-, R4S(=O)2NHC(=O)O-, R4S(=O)2NH-6, halocicloalquiltio C3-6, halocicloalquilalquilC(=O)NR4-, R4OS(=O)2NHC(=O)-, R4OS(=O)2NHC(=O)O-, tio C4-7, alcanosulfinilo C1-6, cicloalcanosulfiniR4OS(=O)2NHC(=O)NR4-, (R4)2NS(=O)2NHC(=O)-, (R4)2Nlo C3-6, cicloalquilalcanosulfinilo C4-7, haloalcaS(=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-, nosulfinilo C1-6, halocicloalcanosulfinilo C3-6, halocicloalquilalcanosulfinilo C4-7, alcanosulfonilR4OC(=O)NHS(=O)2-, R4OC(=O)NHS(=O)2O-, R4OC(=O)NHS(=O)2NR4-, (R4)2NC(=O)NHS(=O)2-, (R4)2NC(=O)NHS(=Oo C1-6, cicloalcanosulfonilo C3-6, cicloalquilalca)2O-, (R4)2NC(=O)NHS(=O)2NR4, espirocicloalquilo; nosulfonilo C4-7, haloalcanosulfonilo C1-6, halocicloalcanosulfonilo (3-6, halocicloalquilalcanosulfheterociclilo (opcionalmente sustituido con alquilo, haloalquilo, halogeno o oxo), heteroarilo (opcionilo C4-7, alquilamino C1-6, dialquilamino C1-6, alcoxi C1-6-alcoxi C1-6, haloalcoxi C1-6-alcoxi C1onalmente sustituido con alquilo, haloalquilo, alc-6, alcoxicarbonilo C1-6, H2NCO, H2NSO2, alquilamioxi, alquiltio, alquilsulfonilo, halogeno, trifluonocarbonilo C1-6, dialquilaminocarbonilo C1-6, alcrometilo, dialquilamino, nitro, ciano, CO2H, CONH2, amido N-monoalquil sustituido, amido N,N-dialquioxi C1-3-alquilaminocarbonilo C1-3, heterociclilcal-sustituido u oxo), aril-amino (opcionalmente susrbonilo, alquilaminosulfonilo C1-6, dialquilaminostituido con alquilo, alcoxi, alquiltio, alquilsulfulfonilo C1-6, heterociclilsulfonilo, alquilcarbononilo, halogeno, trifluorometilo, dialquilamino, nilamino C1-6, alquil C1-6- carbonilaminoalquilo C1-6, alquilsulfonilamino C1-6, alquil C1-6-sulfonilitro, ciano, CO2H, CONH2, amido N-monoalquil-sustiaminoalquilo C1-6, alcoxicarbonil C1-6-alcoxi C1-6tuido y amido N,N-dialquil-sustituido) y heteroari, alcoxi C1-6-alquilo C1-6, haloalcoxi C1-6-alquillamino (opcionalmente sustituido con alquilo, haloo C1-6, hidroxialcoxi C1-6, heteroarilo, oxo, aminalquilo, alcoxi, alquiltio, alquilsulfonilo, halogeno, trifluorometilo, dialquilamino, nitro, ciano,oalquilo C1-6, alquilamino C1-6-alquilo C1-6, dial CO2H, CONH2, amido N-monoalquil-sustituido, amidoquilamino C1-6-alquilamino C1-6-alcoxi C2-6, alquilamino C1-6-alcoxi C2-6, dialquilamino C1-6-alcoxi N,N-dialquil-sustituido u oxo); y R4 se seleccion C2-6, alquilcarbonilo C1-6, cicloalquilcarbonilo a independientemente entre H, alquilo C1-6, haloalquilo C1-6, aminoalquilo C1-6, alquilamino C1-6-alC3-6, cicloalquilaminocarbonilo C3-6, cicloalquil quilo C1-6, dialquilamino C1-6-alquilo C1-6, hidroC3-6-alquil C1-6aminocarbonilo, dicicloalquilaminoxialquilo C1-6 y alcoxi C1-6-alquilo C1-6; o una scarbonilo C3-6, cicloalquilaminosulfonilo C3-6, cial farmacéuticamente aceptable, enantiomero o diascloalquil C3-6-alquil C1-6aminosulfonilo, dicicloalquilaminosulfonilo C3-6, cianoalquilo C1-6, aminotereomero del mismo, con la condicion de que el cocarbonilalquilo C1-6, alquilaminocarbonil C1-6-alqmpuesto no sea un compuesto representado por la fouilo C1-6, dialquilaminocarbonil C1-6-alquilo C1-6rmulas estructurales PR-258 o PR-291, o una sal farmacéuticamente aceptable, enantiomero o diastereo, cicloalquilaminocarbonil C3-6- alquilo C1-6, cicloalquil C3-6-alquil C1-6aminocarbonilalquilo C1-6mero del mismo. y dicicloalquilaminocarbonil C3-6-alquilo C1-6; el anillo de piridina en la formula (1) está opcionalmente sustituido con 1 a 4 grupos seleccionados independientemente entre 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, haloalquenilo C2-6, hidroxialquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquinilo C2-4, haloalquilo C1-6, halocicloalquilo C3-6, halocicloalquilalquilo C4-7, alcoxi C1-6, cicloalcoxi C3-6, cicloalquilalcoxi C4-7, haloalcoxi C1-6, halocicloalcoxi C3-6, halocicloalquilalcoxi C4-7, alquiltio C1-6, cicloalquiltio C3-6, cicloalquilalquiltio C4-7, haloalquiltio C1-6, halocicloalquiltio C3-6, halocicloalquilalquiltio C4-7, alcanosulfinilo C1-6, cicloalcanosulfinilo C3-6, cicloalquilalcanosulfinilo C4-7, haloalcanosulfinilo C1-6, halocicloalcanosulfinilo C3-6, halocicloalquilalcanosulfinilo C4-7, alcanosulfonilo C1-6, cicloalcanosulfonilo C3-6, cicloalquilalcanosulfonilo C4-7, haloalcanosulfonilo C1-6, halocicloalcanosulfonilo C3-6, halocicloalquilalcanosulfonilo C4-7, alquilamino C1-6, dialquilamino C1-6, alcoxi C1-6-alcoxi C1-6, haloalcoxi C1-6-alcoxi C1-6, alcoxicarbonilo C1-6, H2NCO, H2NSO2, alquilaminocarbonilo C1-6, dialquilaminocarbonilo C1-6, alcoxi C1-3-alquilaminocarbonilo C1-3, heterociclilcarbonilo, alquilaminosulfonilo C1-6, dialquilaminosulfonilo C1-6, heterociclilsulfonilo, alquilcarbonilamino C1-6, alquilcarbonilamino C1-6-alquilo C1-6, alquilsulfonilamino C1-6, alquilsulfonilamino C1-6-alquilo C1-6, alcoxicarbonil C1-6-alcoxi C1-6, alcoxi C1-6-alquilo C1-6, haloalcoxi C1-6-alquilo C1-6, hidroxialcoxi C1-6, heteroarilo, oxo, aminoalquilo C1-6, alquilamino C1-6-alquilo C1-6, dialquilamino C1-6-alquilamino C1-6-alcoxi C2-6, alquilamino C1-6-alcoxi C2-6, dialquilamino C1-6-alcoxi C2-6, alquilcarbonilo C1-6, cicloalquilcarbonilo C3-6, cicloalquilaminocar
ARP090101584A 2008-05-01 2009-04-30 Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1 AR071236A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US4965008P 2008-05-01 2008-05-01
US13714808P 2008-07-25 2008-07-25
PCT/US2008/009017 WO2009017664A1 (en) 2007-07-26 2008-07-25 CYCLIC INHIBITORS OF 11β-HYDROXYSTERIOD DEHYDROGENASE 1
US20677509P 2009-02-04 2009-02-04

Publications (1)

Publication Number Publication Date
AR071236A1 true AR071236A1 (es) 2010-06-02

Family

ID=40760028

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090101584A AR071236A1 (es) 2008-05-01 2009-04-30 Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1

Country Status (8)

Country Link
US (1) US8569292B2 (es)
EP (1) EP2291371B1 (es)
JP (1) JP5696037B2 (es)
AR (1) AR071236A1 (es)
CA (1) CA2723039A1 (es)
CL (1) CL2009001058A1 (es)
TW (1) TW201004945A (es)
WO (1) WO2009134392A1 (es)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2125750B1 (en) 2007-02-26 2014-05-21 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5451611B2 (ja) 2007-07-26 2014-03-26 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１のサイクリックインヒビター
AR069207A1 (es) 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
JP5490014B2 (ja) 2007-12-11 2014-05-14 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の環状尿素阻害剤
TW200934490A (en) 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
WO2009094169A1 (en) 2008-01-24 2009-07-30 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2254872A2 (en) 2008-02-15 2010-12-01 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
EP2274287B1 (en) * 2008-03-18 2016-03-09 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
EP2291370B1 (en) 2008-05-01 2013-11-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5301563B2 (ja) 2008-05-01 2013-09-25 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
WO2009147189A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
ES2445199T3 (es) * 2008-06-05 2014-02-28 Glaxo Group Limited Derivados de benzpirazol como inhibidores de PI3-quinasas
EP2280959B1 (en) * 2008-06-05 2012-04-04 Glaxo Group Limited 4-amino-indazoles
JP5379160B2 (ja) 2008-07-25 2013-12-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
JP5777030B2 (ja) 2008-07-25 2015-09-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤
JP5390610B2 (ja) * 2008-07-25 2014-01-15 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の阻害剤の合成
EP2393807B1 (en) * 2009-02-04 2013-08-14 Boehringer Ingelheim International GmbH Cyclic inhibitors of 11 -hydroxysteroid dehydrogenase 1
JP5656880B2 (ja) 2009-03-09 2015-01-21 グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌｉｍｉｔｅｄ Ｐｉ３キナーゼの阻害剤としての４−オキサジアゾール−２−イル−インダゾール
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
PL2899191T3 (pl) 2009-04-30 2018-01-31 Glaxo Group Ltd Indazole podstawione oksazolem jako inhibitory kinazy PI3
WO2011011123A1 (en) 2009-06-11 2011-01-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
JP5749263B2 (ja) 2009-07-01 2015-07-15 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
US8552212B2 (en) 2009-11-05 2013-10-08 Boehringer Ingelheim International Gmbh Chiral phosphorus ligands
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2011149822A1 (en) 2010-05-26 2011-12-01 Boehringer Ingelheim International Gmbh 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives
JP5860042B2 (ja) * 2010-06-16 2016-02-16 ヴァイティー ファーマシューティカルズ，インコーポレイテッド 置換５、６及び７員複素環、そのような化合物を含有する医薬及びそれらの使用
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
JP5813106B2 (ja) 2010-06-25 2015-11-17 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
AU2011325286B2 (en) 2010-11-02 2015-04-16 Boehringer Ingelheim International Gmbh Pharmaceutical combinations for the treatment of metabolic disorders
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013126283A1 (en) 2012-02-20 2013-08-29 E. I. Du Pont De Nemours And Company Fungicidal pyrazoles
GB201702221D0 (en) 2017-02-10 2017-03-29 Univ Of Sussex Compounds
GB201803340D0 (en) 2018-03-01 2018-04-18 Univ Of Sussex Compounds

Family Cites Families (177)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3378587A (en) 1963-03-14 1968-04-16 Du Pont 3, 3'-diaminomethyl-1, 1'-biadamantane
NL127995C (es) 1963-12-20 Geigy Ag J R
US3341538A (en) 1965-06-18 1967-09-12 Geigy Chem Corp Certain 2, 6-methano-3-benzazocines
DE2108954A1 (en) 1971-02-25 1972-09-07 Boehringer Sohn Ingelheim 2-(furylmethyl)-6,7-benzomorphans - useful as cns active agents
DE1801556A1 (de) 1968-10-05 1970-05-21 Huels Chemische Werke Ag Verfahren zur Herstellung von substituierten Hexahydropyrimidinonen-(2)
GB1304175A (es) 1969-03-31 1973-01-24
DE2105743C3 (de) 1971-02-08 1979-11-29 Boehringer Sohn Ingelheim 2-(Furylmethyl)- a -5,9-dialkyl -6,7benzomorphane, Verfahren zu ihrer Herstellung und deren Verwendung
US3681349A (en) 1970-03-05 1972-08-01 Morton Norwich Products Inc 1-(substituted benzyl) tetrahydro-2-(1h) pyrimidones
US4043927A (en) 1972-03-07 1977-08-23 Sun Ventures, Inc. Friction or tractive drive containing ethers of adamantanes
DE2229695A1 (de) 1972-06-19 1974-01-31 Boehringer Sohn Ingelheim 2-(heteroaryl-methyl)-5,9 beta-dialkyl6,7-benzomorphane, deren saeureadditionssalze sowie verfahren zu deren herstellung
DE2338369A1 (de) 1973-07-26 1975-02-13 Schering Ag Mikrobiologische hydroxylierung von 2,6-methano-3-benzazocinen
SU511005A3 (ru) 1973-10-27 1976-04-15 К.Х.Берингер Зон., (Фирма) Способ получени (метоксиметилфурилметил)6,7-бензоморфанов или морфинанов
US4009171A (en) 1974-02-21 1977-02-22 Sterling Drug Inc. N-acylated-11-oxygenated-2,6-methano-3-benzazocine intermediates
DE2411382C3 (de) 1974-03-09 1979-09-06 C.H. Boehringer Sohn, 6507 Ingelheim 2-Tetrahydrofurfuryl-6,7-benzomorphane, Verfahren zur Herstellung und deren Verwendung
US4136145A (en) 1974-07-05 1979-01-23 Schering Aktiengesellschaft Medicament carriers in the form of film having active substance incorporated therein
US4136162A (en) 1974-07-05 1979-01-23 Schering Aktiengesellschaft Medicament carriers in the form of film having active substance incorporated therein
DE2437610A1 (de) 1974-08-05 1976-02-26 Boehringer Sohn Ingelheim Neue 5,9-beta-disubstituierte 2-tetrahydrofurfuryl-6,7-benzomorphane, deren saeureadditionssalze, ihre verwendung als arzneimittel und verfahren zu deren herstellung
US4108857A (en) 1975-08-18 1978-08-22 Sterling Drug Inc. Imidazolylmethyl methanobenzazocines
DE2828039A1 (de) 1978-06-26 1980-01-10 Boehringer Sohn Ingelheim 2-(2-alkoxyethyl)-2'-hydroxy-6,7-benzomorphane deren saeureadditionssalze diese enthaltende arzneimittel und verfahren zu deren herstellung
US5393735A (en) 1990-08-09 1995-02-28 Rohm And Haas Company Herbicidal glutarimides
CA2023492A1 (en) 1989-08-31 1991-03-01 Barry Clifford Lange Herbicidal glutarimides
US5098916A (en) 1990-03-29 1992-03-24 G. D. Searle & Co. Propanobicyclic amine derivatives for cns disorders
EP0454444A1 (en) 1990-04-24 1991-10-30 Nissan Chemical Industries Ltd. Glutarimide derivatives and herbicides
US5215992A (en) 1990-04-30 1993-06-01 G. D. Searle & Co. Ethanobicyclic amine derivatives for CNS disorders
US5089506A (en) 1990-04-30 1992-02-18 G. D. Searle & Co. Ethanobicyclic amine derivatives for cns disorders
CA2049244A1 (en) 1990-08-16 1992-02-17 Steven H. Christiansen Process for absorption of sulfur compounds from fluids using heterocyclic compounds having at least one ring nitrogen atom
DE69109871T2 (de) 1990-10-10 1995-09-14 Schering Corp., Kenilworth, N.J. Pyridin- und pyridin-n-oxid-derivate von diarylmethyl- piperidinen oder piperazinen, deren zusammensetzungen und anwendung.
US5610294A (en) 1991-10-11 1997-03-11 The Du Pont Merck Pharmaceutical Company Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
KR0146931B1 (ko) 1992-04-30 1998-08-17 고바야시 유끼오 옥사졸리딘 유도체 및 그의 약학적으로 허용가능한 염
GB9225377D0 (en) 1992-12-04 1993-01-27 Ici Plc Herbicides
HU224548B1 (hu) 1993-04-07 2005-10-28 Taiho Pharmaceutical Co. Ltd. Tiazolidinszármazékok és ezeket tartalmazó gyógyszerkészítmények, valamint eljárás előállításukra
TW280812B (es) 1993-07-02 1996-07-11 Bayer Ag
EP0640594A1 (en) 1993-08-23 1995-03-01 Fujirebio Inc. Hydantoin derivative as metalloprotease inhibitor
DE19500118A1 (de) 1994-05-18 1995-11-23 Bayer Ag Substituierte Diazacyclohexandi(thi)one
US5780466A (en) 1995-01-30 1998-07-14 Sanofi Substituted heterocyclic compounds method of preparing them and pharmaceutical compositions in which they are present
FR2729954B1 (fr) 1995-01-30 1997-08-01 Sanofi Sa Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant
GB9510459D0 (en) 1995-05-24 1995-07-19 Zeneca Ltd Bicyclic amines
US5776959A (en) 1995-06-05 1998-07-07 Washington University Anticonvulsant and anxiolytic lactam and thiolactam derivatives
GB9517622D0 (en) 1995-08-29 1995-11-01 Univ Edinburgh Regulation of intracellular glucocorticoid concentrations
JP3192662B2 (ja) 1996-07-31 2001-07-30 日研化学株式会社 ６―フェニルテトラヒドロ―１，３―オキサジン―２―オン誘導体及びそれを含む医薬組成物
US5866702A (en) 1996-08-02 1999-02-02 Cv Therapeutics, Incorporation Purine inhibitors of cyclin dependent kinase 2
US6794390B2 (en) 1996-08-02 2004-09-21 Cv Therapeutics, Inc. Purine inhibitors of cyclin dependent kinase 2 & ikappabalpha
GB9623944D0 (en) 1996-11-15 1997-01-08 Zeneca Ltd Bicyclic amine derivatives
US6159990A (en) 1997-06-18 2000-12-12 Synaptic Pharmaceutical Corporation Oxazolidinones as α1A receptor antagonists
US5936124A (en) 1998-06-22 1999-08-10 Sepacor Inc. Fluoxetine process from benzoylpropionic acid
DE19918725A1 (de) 1999-04-24 2000-10-26 Bayer Ag Substituierte N-Cyano-sulfonsäureanilide
DE19929348A1 (de) 1999-06-26 2000-12-28 Bayer Ag Verfahren zur Herstellung von 2-Heterocyclylmethyl-benzoesäurederivaten
US7256005B2 (en) 1999-08-10 2007-08-14 The Chancellor, Masters And Scholars Of The University Of Oxford Methods for identifying iminosugar derivatives that inhibit HCV p7 ion channel activity
US6436928B1 (en) 1999-12-17 2002-08-20 Schering Corporation Selective neurokinin antagonists
CA2393672A1 (en) 1999-12-17 2001-06-21 Schering Corporation Selective neurokinin antagonists
GB0003397D0 (en) 2000-02-14 2000-04-05 Merck Sharp & Dohme Therapeutic agents
DE10034623A1 (de) 2000-07-17 2002-01-31 Bayer Ag Heterocyclisch substituierte Pyridine als Cytokin-Inhibitoren
DE10034800A1 (de) 2000-07-18 2002-01-31 Bayer Ag Substituierte Benzostickstoffheterocyclen
DE10034803A1 (de) 2000-07-18 2002-01-31 Bayer Ag Substituierte Sulfonsäureanilide
DE10035908A1 (de) 2000-07-21 2002-03-07 Asta Medica Ag Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel
DE10035927A1 (de) 2000-07-21 2002-03-07 Asta Medica Ag Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel
DE10035928A1 (de) 2000-07-21 2002-03-07 Asta Medica Ag Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel
DE60114227T2 (de) 2000-08-16 2006-04-20 Neurogen Corp., Branford 2,4-substituierte pyridinderivate
US7294637B2 (en) 2000-09-11 2007-11-13 Sepracor, Inc. Method of treating addiction or dependence using a ligand for a monamine receptor or transporter
AU9087301A (en) 2000-09-11 2002-03-26 Sepracor Inc Ligands for monoamine receptors and transporters, and methods of use thereof
JP2002179572A (ja) 2000-10-06 2002-06-26 Nikken Chem Co Ltd アレルギー性眼疾患治療剤
US6841671B2 (en) 2000-10-26 2005-01-11 Pfizer Inc. Spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
US20030143668A1 (en) 2001-06-18 2003-07-31 National Institute Of Advanced Industrial Guanosine triphosphate-binding protein coupled receptors
JP3873115B2 (ja) 2001-09-25 2007-01-24 独立行政法人産業技術総合研究所 環状ウレタン製造方法
PE20030477A1 (es) 2001-10-15 2003-06-06 Schering Corp ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a
KR20050044581A (ko) 2001-11-22 2005-05-12 오노 야꾸힝 고교 가부시키가이샤 피페리딘-2-온 유도체 화합물 및 그 화합물을 유효성분으로서 함유하는 약제
JP2003300884A (ja) 2002-04-08 2003-10-21 Nikken Chem Co Ltd ＴＮＦ−α産生阻害剤
AU2003219410A1 (en) 2002-04-26 2003-11-10 Pfizer Products Inc. Triaryl-oxy-aryl-spiro-pyrimidine-2, 4, 6-trione metalloproteinase inhibitors
WO2003091258A1 (en) 2002-04-26 2003-11-06 Pfizer Products Inc. N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
DE60335359D1 (de) 2002-04-30 2011-01-27 Kudos Pharm Ltd Phthalazinonderivate
EP1506174B1 (en) 2002-05-17 2015-09-30 Taiwanj Pharmaceuticals Co., Ltd. Use of naltrexone for treating kidney and liver damage
DE60312998T2 (de) 2002-07-03 2007-12-13 Schering Corp. 1-amido-4-phenyl-4-benzyloxymethyl-piperidin derivative und verwandte verbindungen als neurokinin-1 (nk-1) antagonsisten zur behandlung von erbrechen, depressionen, angstzustände und husten
AU2003249812A1 (en) 2002-07-18 2004-02-09 Queen's University At Kingston Dihydrouracil compounds as anti-ictogenic or anti-epileptogenic agents
GB0218630D0 (en) 2002-08-10 2002-09-18 Tanabe Seiyaku Co Novel compounds
TWI347946B (en) 2002-10-11 2011-09-01 Otsuka Pharma Co Ltd 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound
AU2003302027A1 (en) * 2002-11-21 2004-06-15 Vicore Pharma Ab New tricyclic angiotensin ii agonists
GB0228410D0 (en) 2002-12-05 2003-01-08 Glaxo Group Ltd Novel Compounds
EP1581520A4 (en) 2002-12-13 2006-08-23 Smithkline Beecham Corp COMPOUNDS, COMPOSITIONS AND METHODS
AU2004226452B2 (en) 2003-03-26 2008-07-24 Merck Sharp & Dohme Corp. Bicyclic piperidine derivatives as melanocortin-4 receptor agonists
ATE467616T1 (de) 2003-04-11 2010-05-15 High Point Pharmaceuticals Llc Verbindungen mit aktivität an der 11beta- hydroxasteroiddehydrogenase
US7700583B2 (en) 2003-04-11 2010-04-20 High Point Pharmaceuticals, Llc 11β-hydroxysteroid dehydrogenase type 1 active compounds
DE10358004A1 (de) 2003-12-11 2005-07-14 Abbott Gmbh & Co. Kg Ketolactam-Verbindungen und ihre Verwendung
US7186844B2 (en) 2004-01-13 2007-03-06 Mitsubishi Gas Chemical Co., Inc. Method for producing cyclic carbamate ester
JP4324669B2 (ja) 2004-01-21 2009-09-02 独立行政法人産業技術総合研究所 環状ウレタンの製造方法
JP2005239670A (ja) 2004-02-27 2005-09-08 Ono Pharmaceut Co Ltd 含窒素複素環化合物およびその医薬用途
WO2005086700A2 (en) 2004-03-09 2005-09-22 Merck & Co., Inc. Hiv integrase inhibitors
WO2005090282A1 (en) 2004-03-12 2005-09-29 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
JP2005272321A (ja) 2004-03-23 2005-10-06 Ono Pharmaceut Co Ltd 含窒素複素環化合物およびその医薬用途
GB0411404D0 (en) 2004-05-21 2004-06-23 Glaxo Group Ltd Novel compounds
GB0414438D0 (en) 2004-06-28 2004-07-28 Syngenta Participations Ag Chemical compounds
DOP2005000123A (es) 2004-07-02 2011-07-15 Merck Sharp & Dohme Inhibidores de cetp
EP1621536A1 (en) 2004-07-27 2006-02-01 Aventis Pharma S.A. Amino cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
EP1621535A1 (en) 2004-07-27 2006-02-01 Aventis Pharma S.A. Substituted cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
EP1621539A1 (en) 2004-07-27 2006-02-01 Aventis Pharma S.A. Heterocycle -substituted cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
JP2008510823A (ja) 2004-08-23 2008-04-10 メルク エンド カムパニー インコーポレーテッド Ａｋｔ活性阻害剤
UA87328C2 (en) 2004-08-30 2009-07-10 Янссен Фармацевтика Н.В. N-2 adamantanyl-2-phenoxy-acetamide derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
EP1791821B1 (en) 2004-09-10 2013-06-05 Janssen Pharmaceutica NV Novel imidazolidin-2-one derivatives as selective androgen receptor modulators (sarms)
EP1807072B1 (en) * 2004-10-29 2009-01-07 Eli Lilly And Company Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
NZ554906A (en) 2004-11-10 2011-01-28 Incyte Corp Lactam compounds and their use as pharmaceuticals
US20060167044A1 (en) 2004-12-20 2006-07-27 Arnaiz Damian O Piperidine derivatives and their use as anti-inflammatory agents
JP2008525357A (ja) 2004-12-23 2008-07-17 キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ 抗ムスカリン活性を有するアゾール誘導体
EP1848719B1 (en) 2004-12-28 2012-02-01 Exelixis, Inc. [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases
WO2006078992A2 (en) 2005-01-19 2006-07-27 Neurogen Corporation Heteroaryl substituted piperazinyl-pyridine analogues
KR20070107060A (ko) 2005-02-16 2007-11-06 쉐링 코포레이션 Ｃｘｃｒ3 길항제 활성을 갖는 피라지닐 치환된피페라진-피페리딘
WO2006088836A2 (en) 2005-02-16 2006-08-24 Schering Corporation Piperazine-piperidines with cxcr3 antagonist activity
KR20070107075A (ko) 2005-02-16 2007-11-06 쉐링 코포레이션 Ｃｘｃｒ３ 길항제 활성을 갖는 신규의 헤테로사이클릭치환된 피리딘 또는 페닐 화합물
US7776862B2 (en) 2005-02-16 2010-08-17 Schering Corporation Pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity
RU2007134259A (ru) 2005-02-16 2009-03-27 Шеринг Корпорейшн (US) Гетероциклические замещенные пиперазины, обладающие антагонистическим действием к cxcr3
EP1853583B1 (en) 2005-02-16 2011-09-07 Schering Corporation Amine-linked pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity
CN101111485B (zh) 2005-02-24 2010-10-27 日本农药株式会社 新颖的卤代烷基磺酰苯胺衍生物、除草剂及其使用方法
WO2006104280A1 (ja) * 2005-03-31 2006-10-05 Takeda Pharmaceutical Company Limited 糖尿病の予防・治療剤
ES2384450T3 (es) 2005-04-12 2012-07-05 Vicore Pharma Ab Nuevos agonistas de la angiotensina ii triclique.
WO2007008529A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc Celullar cholesterol absorption modifiers
BRPI0614801A2 (pt) 2005-08-16 2009-05-19 Genzyme Corp compostos de ligação a receptor de quimiocina
JP2009511582A (ja) 2005-10-11 2009-03-19 シェーリング コーポレイション Ｃｘｃｒ３拮抗薬活性を有する置換複素環式化合物
JP2009513590A (ja) 2005-10-27 2009-04-02 ユセベ ファルマ ソシエテ アノニム ラクタム又はラクタム誘導体部分を含む化合物、これらの製造方法、及びこれらの使用
JP2007140188A (ja) 2005-11-18 2007-06-07 Fujifilm Corp ポジ型感光性組成物及びそれを用いたパターン形成方法
AU2006316867A1 (en) 2005-11-22 2007-05-31 Amgen Inc. Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
WO2007067504A2 (en) 2005-12-05 2007-06-14 Incyte Corporation Lactam compounds and methods of using the same
EP1801098A1 (en) 2005-12-16 2007-06-27 Merck Sante 2-Adamantylurea derivatives as selective 11B-HSD1 inhibitors
WO2007076055A2 (en) 2005-12-22 2007-07-05 Entremed, Inc. Compositions and methods comprising proteinase activated receptor antagonists
DE102005062990A1 (de) 2005-12-28 2007-07-05 Grünenthal GmbH Substituierte Thiazole und ihre Verwendung zur Herstellung von Arzneimitteln
US7910592B2 (en) 2005-12-30 2011-03-22 Merck Sharp & Dohme Corp. CETP inhibitors
WO2007079186A2 (en) 2005-12-30 2007-07-12 Merck & Co., Inc. 1, 3-oxazolidin-2-one derivatives useful as cetp inhibitors
JP5199121B2 (ja) 2005-12-30 2013-05-15 メルク・シャープ・エンド・ドーム・コーポレイション Ｃｅｔｐ阻害剤
US8865707B2 (en) 2005-12-30 2014-10-21 Merck Sharp & Dohme Corp. Cholesteryl ester transfer protein inhibitors
WO2007084314A2 (en) 2006-01-12 2007-07-26 Incyte Corporation MODULATORS OF 11-ß HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
US20070208001A1 (en) 2006-03-03 2007-09-06 Jincong Zhuo Modulators of 11- beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
WO2007109456A2 (en) 2006-03-16 2007-09-27 Pharmacopeia, Inc. Substituted biphenyl isoxazole sulfonamides as dual angiotensin endothelin receptor antagonists
JP2007254409A (ja) 2006-03-24 2007-10-04 Taisho Pharmaceut Co Ltd イミダゾリジノン誘導体
US7435833B2 (en) 2006-04-07 2008-10-14 Abbott Laboratories Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
MX2008013305A (es) 2006-04-20 2008-10-27 Du Pont Agentes heterociclicos de cinco miembros para el control de plagas de invertebrados.
ATE473210T1 (de) * 2006-04-24 2010-07-15 Lilly Co Eli Substituierte pyrrolidinone als hemmer von 11- beta-hydroxysteroiddehydrogenase 1
US7968585B2 (en) 2006-04-25 2011-06-28 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
US8178005B2 (en) 2006-06-20 2012-05-15 Chemtura Corporation Liquid phosphite compositions having different alkyl groups
PE20080344A1 (es) 2006-06-27 2008-06-09 Sanofi Aventis Compuestos 8-azabiciclo[3.2.1]oct-8-il-1,2,3,4-tetrahidroquinolina sustituidos como inhibidores 11b-hsd1
WO2008012623A1 (en) 2006-07-25 2008-01-31 Pfizer Products Inc. Benzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
WO2008012622A2 (en) 2006-07-25 2008-01-31 Pfizer Products Inc. Azabenzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
WO2008021337A1 (en) * 2006-08-15 2008-02-21 Wyeth Oxazinan-2-one derivatives useful as pr modulators
US7649007B2 (en) 2006-08-15 2010-01-19 Wyeth Llc Oxazolidine derivatives as PR modulators
WO2008021338A2 (en) 2006-08-15 2008-02-21 Wyeth Tricyclic oxazolidone derivatives useful as pr modulators
CA2663280A1 (en) 2006-09-14 2008-03-20 Neuromed Pharmaceuticals Ltd. Diaryl piperidine compounds as calcium channel blockers
CA2662574A1 (en) 2006-09-22 2008-03-27 Novartis Ag Heterocyclic organic compounds
DE102007005799B4 (de) 2006-10-18 2018-01-25 Heinz-Jürgen Mühlen Verfahren zur Erzeugung eines wasserstoffreichen Produktgases
EP2104665A2 (en) * 2006-10-19 2009-09-30 F. Hoffmann-Roche AG Imidazolone and imidazolidinone derivatives as 11b-hsd1 inhibitors for diabetes
EP1935420A1 (en) 2006-12-21 2008-06-25 Merck Sante 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors
EP2125750B1 (en) * 2007-02-26 2014-05-21 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2008118332A2 (en) 2007-03-23 2008-10-02 Schering Corporation Hydrazido-peptides as inhibitors of hcv ns3-protease
KR20090127298A (ko) 2007-03-29 2009-12-10 에프. 호프만-라 로슈 아게 헤테로사이클릭 항바이러스 화합물
JP5451611B2 (ja) * 2007-07-26 2014-03-26 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１のサイクリックインヒビター
JP2009110842A (ja) 2007-10-31 2009-05-21 Sumitomo Chemical Co Ltd ボタンスイッチ被覆用積層樹脂体
AR069207A1 (es) 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
JP5769970B2 (ja) 2007-11-16 2015-08-26 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ベンゾモルファン及び関連骨格のアリール−及びヘテロアリールカルボニル誘導体、かかる化合物を含有する医薬及びこれらの使用
KR101460359B1 (ko) 2007-12-13 2014-11-10 삼성전자주식회사 이동통신 시스템에서의 핸드오버 방법 및 장치
TW200934490A (en) 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
WO2009094169A1 (en) 2008-01-24 2009-07-30 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5734666B2 (ja) 2008-02-11 2015-06-17 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の１，３−オキサアゼパン−２−オン及び１，３−ジアゼパン−２−オン阻害剤
CA2711757C (en) 2008-02-12 2016-07-26 Boehringer Ingelheim International Gmbh Urea derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use
EP2254872A2 (en) 2008-02-15 2010-12-01 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
JP5108557B2 (ja) 2008-02-27 2012-12-26 東京エレクトロン株式会社 ロードロック装置および基板冷却方法
EP2274287B1 (en) 2008-03-18 2016-03-09 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
TW200944526A (en) 2008-04-22 2009-11-01 Vitae Pharmaceuticals Inc Carbamate and urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
EP2291370B1 (en) 2008-05-01 2013-11-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2291373B1 (en) 2008-05-01 2013-09-11 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5301563B2 (ja) 2008-05-01 2013-09-25 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
TW200950780A (en) 2008-05-13 2009-12-16 Boehringer Ingelheim Int Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use
US20110224242A1 (en) 2008-07-23 2011-09-15 Bioalliance Pharma Styrlyquinolines, their process of preparation and their therapeutic uses
JP5777030B2 (ja) 2008-07-25 2015-09-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤
JP5390610B2 (ja) 2008-07-25 2014-01-15 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の阻害剤の合成
JP5379160B2 (ja) 2008-07-25 2013-12-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
US8309597B2 (en) 2008-07-25 2012-11-13 Boehringer Ingelheim International Gmbh 1,1′-diadamantyl carboxylic acids, medicaments containing such compounds and their use
EP2318403B1 (en) 2008-08-25 2015-12-23 Boehringer Ingelheim International GmbH Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use
TW201022266A (en) 2008-10-23 2010-06-16 Boehringer Ingelheim Int Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use
EP2393813B1 (en) 2009-02-04 2013-07-31 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11 ß-hydroxysteroid dehydrogenase 1 useful for the treatment of diseases related to elevated level of cortisol
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
JP5670440B2 (ja) 2009-06-02 2015-02-18 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
AR078887A1 (es) 2009-11-06 2011-12-07 Boehringer Ingelheim Int Derivados arilo y heteroarilcarbonilo de hexahidroindenopiridina y octahidrobenzoquinolina y composiciones farmaceuticas que los contienen.

Also Published As

Publication number Publication date
US20110263584A1 (en) 2011-10-27
EP2291371B1 (en) 2015-06-10
EP2291371A1 (en) 2011-03-09
CA2723039A1 (en) 2009-11-05
JP2011520792A (ja) 2011-07-21
CL2009001058A1 (es) 2010-09-10
JP5696037B2 (ja) 2015-04-08
US8569292B2 (en) 2013-10-29
WO2009134392A1 (en) 2009-11-05
TW201004945A (en) 2010-02-01

Similar Documents

Publication Publication Date Title
AR071236A1 (es) Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1
AR073348A1 (es) Inhibidores ciclicos de 11 beta-hidroxiesteroide deshidrogenasa 1
AR071609A1 (es) Inhibidores ciclicos de 11(beta) -hidroxiesteroide deshidrogenasa 1
AR069207A1 (es) Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
AR070517A1 (es) Piperidinas inhibidoras de 11 beta-hidroxiesteroide deshidrogenasa 1
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
AR067673A1 (es) Derivados de 1,3 oxazinan - 2 - ona como inhibidores ciclicos de la 11 beta -hidroxiesteroide deshidrogenasa 1. composiciones farmaceuticas.
PE20150230A1 (es) Nuevos diazaespirocicloalcanos y azaespirocicloalcanos
JP2011524336A5 (es)
AR049646A1 (es) Derivados de sulfamato y sulfamida utiles para el tratamiento de la epilepsia y trastornos relacionados
BRPI0511504A (pt) composto ou um sal farmaceuticamente aceitável do mesmo, e, agente preventivo ou terapêutico para uma doença resultante de beta-amilóides
WO2008062905A3 (en) Heteromonocyclic compound and use thereof
AR056886A1 (es) Compuestos de pirrolopiridina sustituida inhibidores de quinasas, composiciones farmaceuticas que los contienen y usos en el tratamiento del cancer
BRPI0608732A2 (pt) composto ou um sal, hidrato, solvato, complexo ou pró-droga farmaceuticamente aceitável do mesmo, sal de um composto, processo para a preparação de um composto, uso de um composto, composição farmacêutica, e, produto
BRPI0607600A2 (pt) derivados de 4-oxoquinazolin-3-il-benzamida para o tratamento de doenças relacionadas com citocina
BRPI0519287A2 (pt) derivados de amida
AR078408A1 (es) Derivados de indol como moduladores de los crac
MA30821B1 (fr) Derives de pyrazoline utiles comme antagonistes des recepteurs de mineralocorticoïdes
PE20091818A1 (es) DERIVADOS POLISUSTITUIDOS DE 2-ARIL-6-FENIL-IMIDAZO[1,2-a] PIRIDINAS, SU PREPARACION Y SU APLICACION EN TERAPEUTICA
AR065811A1 (es) Derivados de 2-amino-4h-imidazol-4-ona,composiciones farmaceuticas que los contienen y usos para el tratamiento de la enfermedad de alzheimer y otros trastornos neurodegenerativos.
AR054083A1 (es) Compuestos imidazol y su utilizacion paar preparar medicamentos
DE602006010738D1 (de) Pyrroloä2,3-cüpyridinderivate
ATE467632T1 (de) Pyrroloä2,3-büpyridinderivate als modulatoren des h3-rezeptors
AR040278A1 (es) Ligandos del receptor de glucocorticoides para el tratamiento de trastornos metabolicos
CL2011003302A1 (es) Compuestos derivados de amida del acido alquil-sulfonico; composicion farmaceutica; uso de los compuestos como moduladores de la disfuncion de glutamato para prevenir o tratar trastornos neurologicos y psiquiatricos como esquizofrenia, enfermedad de alzheimer, trastornos de deficit de atencion/hiperactividad, perdida de audicion, entre otros.

Legal Events

Date Code Title Description
FB Suspension of granting procedure