AR054125A1 - Derivados del fluoreno, composiciones farmaceuticas que los contienen y su utilizacion en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la actividad de la proteina hsp90 - Google Patents

Derivados del fluoreno, composiciones farmaceuticas que los contienen y su utilizacion en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la actividad de la proteina hsp90

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Publication number
AR054125A1
AR054125A1 ARP060101980A ARP060101980A AR054125A1 AR 054125 A1 AR054125 A1 AR 054125A1 AR P060101980 A ARP060101980 A AR P060101980A AR P060101980 A ARP060101980 A AR P060101980A AR 054125 A1 AR054125 A1 AR 054125A1
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Argentina
Prior art keywords
alkyl
optionally substituted
aryl
heteroaryl
heterocycloalkyl
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ARP060101980A
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English (en)
Inventor
Patrick Mailliet
Luc Bertin
Fabienne Thompson
Fabienne Pilorge
Didier Bernard
Herve Minoux
Chantal Carrez
Helene Goulaouic
Thierry Gouyon
Jean-Marie Ruxer
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Aventis Pharma Sa
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Publication of AR054125A1 publication Critical patent/AR054125A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Uso de los mismos en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la proteína HSP9U y composiciones farmacéuticas que los contienen. Reivindicacion 1: Los productos de la formula (1), en la que: A1, A2, A3 y A4, idénticos o diferentes, representan CRa o N o NRb; en el cual Rb representa alquilo, alcoxi u OH; R1 y R1' son tales que: o bien R1 y R1' idénticos o diferentes son tales que uno de R1 y R1' representa un átomo de hidrogeno o de halogeno o un radical seleccionado entre alquilo C1-3, alcoxi C1-3, alquil-OH, CF3, ciano, carboxi y carboxamido; y el tro de R1 y R1' se selecciona del grupo constituido por H; halogeno; CF3; hidroxi; mercapto; nitro; amino; NH-OH ; NH-CO-H ; NH-CO-OH, NH-CO- Oalquilo, NH-CO-NH2; carboxi; CN; CO-NH2; X-(CH2)m-alquilo; X-(CH2)m-cicloalquilo; X-(CH2)m-heterocicloalquilo; X-(CH2)m-arilo o X-(CH2)m-heteroarilo con X = enlace sencillo, CH2, CH=CH, CH2-O, CH2-NH, CH2-C(O), CH2-C(O)-O, CH2-C(O)-NH, CH2-NH-(CO), CH2-NH-S(O), CH2- NH-S(O)2, O, S, NH, O-C(O), C(O)-NH1 -NH-C(O), -NH-C(O)-C(O)-, -NH-C(O)-NH-, NH-CS, NH-S(O) o NH-S(O)2, -NH-CO-CH2-O-; -NH-CO-CH2-S-CH2-CO-NH-; -NH-CO-(CH2)2-SO2-; -NH-CO-CH2-N(CH3)-CO-; con m = 0, 1 o 2, estando todos los radicales alquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo opcionalmente sustituidos, conteniendo el radical cicloalquilo de 3 a 10 miembros, conteniendo el radical arilo de 6 a 10 miembros, y conteniendo los radicales heterocicloalquilo y heteroarilo, opcionalmente sustituidos, de 4 a 10 miembros de los cuales 1 a 4 son heteroátomos seleccionados entre O, S, N o NR3 en el cual R3 representa H o alquilo que está él mismo opcionalmente sustituido; o bien R1 y R'1 forman junto con los átomos de carbono a los cuales están unidos un radical =O; =S; =N-OH; =N-NH2; =N-NH-CO-NH2, =CH-OH; =Y1-(CH2)m-arilo o =Y1-(CH2)m-heteroarilo, en los cuales Y1 representa CH, CH-CO-, CH-CO-NH, N, N-O o N-NH, con m = 0, 1 o 2 y en los cuales arilo y heteroarilo son como se ha definido anteriormente y están opcionalmente sustituidos; o bien R1 R'1 forman junto con los átomos de carbono a los cuales están unidos un ciclo parcialmente saturado que consta de 4 a 6 miembros y que contiene eventualmente 1 a 3 heteroátomos seleccionados entre O, S, N o NR4 en el cual R4 representa H o alquilo que está él mismo opcionalmente sustituido; R2 y R'2, idénticos o diferentes, se seleccionan independientemente del grupo constituido por H, halogeno, CF3, nitro, ciano, alquilo, hidroxi, mercapto, amino, alquilamino, dialquilamino, alcoxi, alquiltio (metiltio), carboxi libre o esterificado por un radical alquilo, carboxamida, CO-NH(alquil) y CO N(alquil)2, estando opcionalmente sustituidos todos los radicales alquilo, alcoxi y alquiltio; p y p' idénticos o diferentes representan respectivamente los numeros enteros 1 a 4 y 1 a 3; Ra se selecciona del grupo constituido por H; halogeno; CF3; hidroxi; OCF3; SO2- NH2; SO2-NH(alk), SO2-N(alk)2; mercapto; nitro; amino; NH(alk); N(alk)2; NH-OH; NH-CO-H; NH-CO-NH2; carboxi libre o esterificado por un radical alquilo que está él mismo opcionalmente sustituido; CN; CO-NH2; Y-(CH2)n-alquilo; Y-(CH2)n-cicloalquilo, Y-(CH2)n-heterocicloalquilo, Y-(CH2)n- arilo o Y-(CH2)n-heteroarilo, en los cuales Y representa un enlace sencillo o bien =O, S, NH, O-C(O), C(O)-NH, -C(O)N(CH3)-; CO; NH-C(O), NH-S(O) o NH-S(O)2; con n = O, 1 , 2, o 3 radicales en los cuales los radicales alquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo están opcionalmente sustituidos, el radical cicloalquilo contiene de 3 a 10 miembros, el radical arilo contiene de 6 a 10 miembros, y los radicales heterocicloalquilo, y heteroarilo, opcionalmente sustituidos, contienen de 4 a 10 miembros de los cuales 1 a 4 son heteroátomos seleccionados entre O, S, N o NR3 en el cual R3 representa H o alquilo que está él mismo opcionalmente sustituido; estando todos los radicales alquilo, alcoxi, alquiltio, cicloalquilo, heterocicloalquilo, arilo y heteroarilo de los sustituyentes de los productos de la formula (1) opcionalmente sustituidos; estando dichos productos de la formula (1) en todas las formas de tautomeros e isomeros posibles; racémicos, enantiomeros y diastereoisomeros, así como las sales de adicion con los ácidos minerales y orgánicos o con las bases minerales y orgánicos de dichos productos de la formula (1).
ARP060101980A 2005-05-19 2006-05-17 Derivados del fluoreno, composiciones farmaceuticas que los contienen y su utilizacion en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la actividad de la proteina hsp90 AR054125A1 (es)

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FR0505037A FR2885904B1 (fr) 2005-05-19 2005-05-19 Nouveaux derives du fluorene, compositions les contenant et utilisation

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US (1) US7674795B2 (es)
EP (1) EP1888579B1 (es)
JP (1) JP4964874B2 (es)
KR (1) KR101288696B1 (es)
CN (1) CN101203518B (es)
AR (1) AR054125A1 (es)
AT (1) ATE518859T1 (es)
AU (1) AU2006248825B2 (es)
BR (1) BRPI0611424A2 (es)
CA (1) CA2608378C (es)
CR (1) CR9515A (es)
DO (1) DOP2006000112A (es)
EA (1) EA019027B1 (es)
FR (1) FR2885904B1 (es)
GT (1) GT200600206A (es)
HN (1) HN2006018410A (es)
IL (1) IL187163A (es)
JO (1) JO2753B1 (es)
MA (1) MA29493B1 (es)
MX (1) MX2007014443A (es)
MY (1) MY149037A (es)
NO (1) NO20076460L (es)
NZ (1) NZ563239A (es)
PA (1) PA8675701A1 (es)
PE (1) PE20061367A1 (es)
TN (1) TNSN07389A1 (es)
TW (1) TWI386406B (es)
UA (1) UA93203C2 (es)
UY (1) UY29549A1 (es)
WO (1) WO2006123061A2 (es)
ZA (1) ZA200709856B (es)

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AU2006248825A1 (en) 2006-11-23
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