AR078313A1 - Derivados de piridinil-imidazolona inhibidores de quinasas pi3k,composiciones farmaceuticas que los comprenden, metodo para prepararlos y uso de los mismos en el tratamiento de enfermedades autoinmunes e inflamatorias, entre otras - Google Patents

Derivados de piridinil-imidazolona inhibidores de quinasas pi3k,composiciones farmaceuticas que los comprenden, metodo para prepararlos y uso de los mismos en el tratamiento de enfermedades autoinmunes e inflamatorias, entre otras

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Publication number
AR078313A1
AR078313A1 ARP100103476A ARP100103476A AR078313A1 AR 078313 A1 AR078313 A1 AR 078313A1 AR P100103476 A ARP100103476 A AR P100103476A AR P100103476 A ARP100103476 A AR P100103476A AR 078313 A1 AR078313 A1 AR 078313A1
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AR
Argentina
Prior art keywords
hal
atoms
het1
het
replaced
Prior art date
Application number
ARP100103476A
Other languages
English (en)
Inventor
Joerg Bomke
Ulrich Emde
Hans-Peter Buchstaller
Markus Klein
Christina Esdar
Original Assignee
Merck Patent Gmbh
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
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR078313A1 publication Critical patent/AR078313A1/es

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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
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    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Veterinary Medicine (AREA)
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  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los compuestos de la formula (1), en donde X1 es CR1 o N; X2 es CR1 o N; en donde X1 o X2 es N y el otro es CR1; Y es Het o Ar; L es [C(Ra)2]m; R1 es H, A, Hal, OH, OA, NH2, NHA o NA2; R2 es H, A, Hal, OH, OA, NH2, NHA o NA2; R3 es H, A, Hal, OH, OA, NH2, NRA' o NA2; R4 es H, A', OH o OA'; R5 es H o A'; R6 es H, A'', CN, Hal, Het, Het1 o Ar; R7 es H, A'', CN, Hal, Het, Het1 o Ar; R8 es H, A'', Het1, CN, Hal, NHHet1, NA'Het1, Ar o Het; R9 es H, A'', CN, Hal, Het, Het1 o Ar; R10 es H, A'', CN, Hal, Het, Het1 o Ar; A es alquilo con 1-10 átomos de C no ramificado o ramificado, en donde 1-7 átomos de H pueden estar reemplazados por F y/o Cl, o alquilo cíclico con 3-7 átomos de C; A' es alquilo no ramificado o ramificado con 1-6 átomos de C, en donde 1-5 átomos de H pueden estar reemplazados por F y/o Cl; A'' es alquilo con 1-10 átomos de C no ramificado o ramificado, en donde 1-7 átomos de H pueden estar reemplazados por OH, CN, NH2, CONH2, COOH, COOA, NHCOA, -CsH, F, Cl y/o Br, y/o en donde uno o dos grupos no adyacentes CH y/o CH2 pueden estar reemplazados por O, NH, NA', S, SO, SO2 y/o grupos CH=CH; A''' es alquilo con 1-10 átomos de C no ramificado o ramificado, en donde 1-7 átomos de H pueden estar reemplazados por F y/o Cl, y/o en donde uno o dos grupos no adyacentes CH y/o CH2 pueden estar reemplazados por O, NH y/o NA'; Ra es H o A'; Het es un heterociclo insaturado o aromático mono- o bicíclico con 1 a 4 átomos de N, O y/o S, que no está sustituido o que puede estar mono-, di- o trisustituido con A, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2, NHCOA, (CH2)nCONH2, (CH2)nCONHA, (CH2)nCONA2, CN, =O, Hal, (CH2)nOH, (CH2)nOA, COOH, COOA, O(CH2)nOH, O(CH2)nOA, O(CH2)nNH2, NH(CH2)nNH2, SO2A y/o SO2NH2; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con CN, (CH2)nCONH2, (CH2)nCONHA, (CH2)nCONA2, (CH2)nOH, (CH2)nOA, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2, NHCOOA, NHCOA, Hal, COOH, COOA, A, NHSO2A, SO2NH2, SO2NHA, SO2NA2 y/o SO2A; Het1 es un heterociclo saturado monocíclico con 1 a 4 átomos de N, O y/o S, que no está sustituido o que puede estar mono-, disustituido con A, NH2, piridilmetilo y/u =O; Hal es F, Cl, Br o I; m es 0 o 1; n es 0, 1, 2, 3 o 4; así como sus sales, tautomeros y estereoisomeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de PI3K y se pueden usar, por ejemplo, para el tratamiento de enfermedades autoinmunes, inflamaciones, enfermedades cardiovasculares, enfermedades neurodegenerativas y tumores.
ARP100103476A 2009-09-28 2010-09-24 Derivados de piridinil-imidazolona inhibidores de quinasas pi3k,composiciones farmaceuticas que los comprenden, metodo para prepararlos y uso de los mismos en el tratamiento de enfermedades autoinmunes e inflamatorias, entre otras AR078313A1 (es)

Applications Claiming Priority (1)

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DE102009043260A DE102009043260A1 (de) 2009-09-28 2009-09-28 Pyridinyl-imidazolonderivate

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AR078313A1 true AR078313A1 (es) 2011-10-26

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US (1) US8802866B2 (es)
EP (1) EP2483268B1 (es)
JP (1) JP5763647B2 (es)
CN (1) CN102574842B (es)
AR (1) AR078313A1 (es)
AU (1) AU2010297616B2 (es)
CA (1) CA2775475C (es)
DE (1) DE102009043260A1 (es)
ES (1) ES2593431T3 (es)
IL (1) IL218617A (es)
WO (1) WO2011035855A1 (es)

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AU2010297616A1 (en) 2012-05-17
US20120220587A1 (en) 2012-08-30
EP2483268B1 (de) 2016-06-29
DE102009043260A1 (de) 2011-04-28
ES2593431T3 (es) 2016-12-09
US8802866B2 (en) 2014-08-12
CA2775475A1 (en) 2011-03-31
JP5763647B2 (ja) 2015-08-12
IL218617A (en) 2016-07-31
AU2010297616B2 (en) 2016-01-28
CN102574842A (zh) 2012-07-11
WO2011035855A1 (de) 2011-03-31
IL218617A0 (en) 2012-05-31
JP2013505900A (ja) 2013-02-21
CA2775475C (en) 2017-09-19
EP2483268A1 (de) 2012-08-08
CN102574842B (zh) 2015-01-21

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