AR061643A1 - Derivados de ureas de piperidina o pirrolidina, metodos para su preparacion, una composicion farmaceutica que los comprende y el empleo de estos en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por la enzima 11beta-hsd1. - Google Patents

Derivados de ureas de piperidina o pirrolidina, metodos para su preparacion, una composicion farmaceutica que los comprende y el empleo de estos en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por la enzima 11beta-hsd1.

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Publication number
AR061643A1
AR061643A1 ARP070102822A ARP070102822A AR061643A1 AR 061643 A1 AR061643 A1 AR 061643A1 AR P070102822 A ARP070102822 A AR P070102822A AR P070102822 A ARP070102822 A AR P070102822A AR 061643 A1 AR061643 A1 AR 061643A1
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AR
Argentina
Prior art keywords
alkyl
group
atom
coor5
alkoxy
Prior art date
Application number
ARP070102822A
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English (en)
Inventor
Patrick Mougenot
Claudie Namane
Eric Nicolai
Francois Pacquet
Christophe Philippo
Olivier Venier
Olivier Crespin
Cecile Pascal
Michel Aletru
Alain Braun
Stefan Gussregen
Original Assignee
Sanofi Aventis
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Publication date
Priority claimed from FR0605786A external-priority patent/FR2902790A1/fr
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR061643A1 publication Critical patent/AR061643A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61P25/28—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
    • 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
    • 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
    • A61P3/08—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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/06—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
    • 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
    • C07D417/14—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

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

Abstract

Métodos para su preparacion, una composicion farmacéutica que los comprende y el empleo de éstos en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por la enzima 11b-HSD1. Reivindicacion 1: Compuestos que responden a la formula (1): en la que: X representa un átomo de carbono, de oxigeno, de azufre o de nitrogeno o el grupo O=S=O; R1a,b,c,d y R2a,b,c,d idénticos o diferentes, representan cada uno un átomo de hidrogeno o de halogeno, alquilo C1-5, alcoxi C1-5, halogenoalquilo C1-5, hidroxi, hidroxi-alquilo C1-5, ciano, -COOR5, -NR6R7, -COOR5-alquilo C1-5, NR6R7-alquilo C1-5, -CONR6R7, CONR6R7-alquilo C1-5, -SO2NR6R7, -COR5, arilo o heteroarilo, arilo-alquilo C1-5, heteroarilo-alquilo C1-5, heterocicloalquil-alquilo C1-5, todos los grupos arilo, heteroarilo que pueden estar opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados entre grupos ciano, COOR5, CONR6R7, SO2R5, alcoxi C1-5, OCH2CONR6R7, un átomo de halogeno, halogenoalquilo C1-5 y solo un grupo arilo-alquilo C1-5 puede opcionalmente estar sustituido con un grupo heteroarilo; o (R2a) o (R2b) pueden asimismo formar con el átomo de carbono al que están unidos un grupo C=O, C=CF2; o (R2a) y/o (R2b) pueden asimismo formar con el o los átomos a los que están unidos un grupo cicloalquilo C3-6, pudiendo ser estos ciclos espiro cuando son transportados por el mismo átomo de carbono y ser opcionalmente sustituidos con uno a tres átomos de halogenos; o (R1d) y (R2a) pueden formar igualmente con los átomos a los que están unidos un grupo cicloalquilo C3-7; los grupos R3a,b representan cada uno, un átomo de hidrogeno, fluor o un grupo alquilo C1-5, alcoxi C1-5, alcoxi-alquilo C1-5, hidroxi, hidroxi- alquilo C1-5, halogenoalquilo C1-5, ciano, -COOR5, -NR6R7, -COOR5-alquilo C1-5, NR6R7-alquilo C1-5, -CONR6R7, CONR6R7-alquilo C1-5; R4 representa: un grupo alquilo C1-5; un grupo cicloalquilo C3-6; un grupo heterocicloalquilo; un grupo arilo mono- o bi-cíclico que tiene de 5 a 10 átomos de carbono; un grupo heteroarilo mono- o bicíclico que tiene de 2 a 9 átomos de carbono; cuando R4 es un grupo arilo o heteroarilo o heterocicloalquilo, puede ser opcionalmente sustituido con 1 a 4 sustituyentes seleccionados entre los átomos de halogeno, los grupos alquilo C1-5, alcoxi C1-5, halogenoalquilo C1-5, hidroxi, hidroxi-alquilo C1-5, alcoxi C1-5-alquilo C1-5, ciano, fenilo opcionalmente sustituido, bencilo opcionalmente sustituido, -COOR5, - NR6R7, -COOR5-alquilo C1-5, -NR6R7-alquilo C1-5, -CONR6R7, SO2NR6R7; o R3a,b y R4 son, transportados por átomos de carbono diferentes o transportados por un mismo átomo de carbono y, cuando son transportados por el mismo átomo de carbono, pueden formar juntos un ciclo en posicion espiro, en particular un ciclo de formula (2), (3), (4) o (5) en las que: el enlace de puntos es un enlace simple o un enlace doble; s es un numero entero igual a 0, 1, 2 o 3; t es un numero entero igual a 0, 1, 2 o 3, no pudiendo ser s y t iguales a la vez a 0; R8 representa un átomo de hidrogeno o de halogeno, alquilo C1-5, alcoxi C1-5, trifluorometilo, hidroxi, hidroximetilo, ciano, -COOR5, -NR6R7; R9 representa un átomo de hidrogeno o alquilo C1-5, hidroxi; Y representa un enlace o un átomo de carbono o de nitrogeno; n es un numero entero igual a 0 o 1; o, p, q y r, idénticos o diferentes, son numeros enteros iguales a 0, 1 o 2; i y j son numeros enteros iguales a 0, 1, 2, 3 o 4; R5 representa un átomo de hidrogeno, alquilo C1-5, cicloalquilo C3-6, halogenoalquilo C1-5; R6 y R7, idénticos o diferentes, representan cada uno un átomo hidrogeno, alquilo C1-5, cicloalquilo C3-6, alquilcarbonilo C1-5, hidroximetilalquilo C1-5, alcoximetilo C1- 5, alquilo C1-5, arilo, heterocicloalquilo opcionalmente sustituido, -SO2R5 o pueden formar junto con el átomo de nitrogeno al que están unidos un heterocicloalquilo opcionalmente sustituido, entendiéndose que cuando X = CH2, n = 0, R1a,b,c,d = H, R2a,b,c,d = H, R3a,b = H entonces el grupo R4 debe ser diferente de fenilo opcionalmente sustituido con un átomo de halogeno o un grupo alquilo C1-5, trifluorometilo, alcoxi C1-5; en estado de base o de sal de adicion de ácido, así como en estado de hidrato o de solvato.
ARP070102822A 2006-06-27 2007-06-26 Derivados de ureas de piperidina o pirrolidina, metodos para su preparacion, una composicion farmaceutica que los comprende y el empleo de estos en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por la enzima 11beta-hsd1. AR061643A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0605786A FR2902790A1 (fr) 2006-06-27 2006-06-27 Derives d'urees de piperidine ou pyrrolidine,leur preparation et leur application en therapeutique
FR0611239 2006-12-22

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AR061643A1 true AR061643A1 (es) 2008-09-10

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US (1) US7947834B2 (es)
EP (1) EP2044057A2 (es)
JP (1) JP2009541463A (es)
KR (1) KR20090021192A (es)
AR (1) AR061643A1 (es)
AU (1) AU2007264791A1 (es)
BR (1) BRPI0713042A2 (es)
CA (1) CA2652852A1 (es)
CL (1) CL2007001886A1 (es)
IL (1) IL195820A0 (es)
MX (1) MX2008016563A (es)
PE (1) PE20080212A1 (es)
RU (1) RU2009102527A (es)
TW (1) TW200811158A (es)
UY (1) UY30448A1 (es)
WO (1) WO2008000950A2 (es)

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KR20090021192A (ko) 2009-02-27
BRPI0713042A2 (pt) 2013-01-08
PE20080212A1 (es) 2008-04-25
IL195820A0 (en) 2009-09-01
US7947834B2 (en) 2011-05-24
EP2044057A2 (fr) 2009-04-08
RU2009102527A (ru) 2010-08-10
JP2009541463A (ja) 2009-11-26
TW200811158A (en) 2008-03-01
CA2652852A1 (fr) 2008-01-03
WO2008000950A2 (fr) 2008-01-03
WO2008000950A3 (fr) 2008-02-14
US20090176775A1 (en) 2009-07-09
MX2008016563A (es) 2009-03-02
AU2007264791A1 (en) 2008-01-03
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