AR066557A1 - Derivados de 1h-indazol-5-il-[1, 3, 4]oxadiazol-2-ilo, un metodo para su preparacion, y el uso de los mismos en medicamentos para el tratamiento de enfermedades mediadas por la modulacion de la sgk. - Google Patents

Derivados de 1h-indazol-5-il-[1, 3, 4]oxadiazol-2-ilo, un metodo para su preparacion, y el uso de los mismos en medicamentos para el tratamiento de enfermedades mediadas por la modulacion de la sgk.

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Publication number
AR066557A1
AR066557A1 ARP080102031A ARP080102031A AR066557A1 AR 066557 A1 AR066557 A1 AR 066557A1 AR P080102031 A ARP080102031 A AR P080102031A AR P080102031 A ARP080102031 A AR P080102031A AR 066557 A1 AR066557 A1 AR 066557A1
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Argentina
Prior art keywords
het
mono
atoms
naso2a
so2n
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ARP080102031A
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Markus Klein
Norbert Beier
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Merck Patent Gmbh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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 chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
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  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Derivados heterocíclicos de indazol de la formula 1 en donde L es R1, R2 o -(X) mR3, Q es O, NH o N-NH2, R es H o A, X es CR7R8, CR7R8CR9R10, CR7R8C(OR9) R10, NR7, O, NR6CR7R8, CR7R8NR9, OCR7R8, OCR7R8CR9R10, CR7R8O, CR7R8CR9R10O, NR6CR7R8CR9R10,CR7R8SO2, NR7CONR8,NR7CONR8CR9R10, COCR7R8, CONR7, CONR7CR8R9, CONHNH, NR7CR8R9CONR10, NR7CO o NR7COCR8R9, Y es H, A, Ar o Het, R1 es CR9=CR9R10 o CR12=CR13R14, R2 es CECR12 o CEC-Het,R3, R4, R5 son en cada caso, de modo independiente entre sí, H,A, Hal, OH, CA, -[C(R7)2]nAr, -[C(R7)2]nHet, OAr, OHet, SH, SA, SAr, SHet, NH2, NHA, NAA', NHAr, N(Ar)2, NHHet, N(Het)2, NAAr, NAHet, SOA, SOAr, SOHet, SO2A, SO2Ar, SO2Het, NO2, CN, COOH,. COOA, CONH2, CONHA, CONA2, NHCOA, NACOA, NHCONH2, NHCONHA,NRCONA2, NHSO2A, NASO2A, CHO, COA, COAr, COHet, SO3H, SO2NH2, SO2NHAr, SO2N(Ar)2, SO2NHHet o SO2N(Het)2; R6, R7, R8, R9 y R10 son en cada caso, de modo independiente entre sí, H o A, R11 es alquilo con 1-6 átomos de C, en donde 1-5 átomos de H puedeestar reemplazados por F, R12, R13y R14 son en cada caso, de modo independiente entre sí, H o Ar, A, A' son en cada caso, de modo independiente entre sí, alquilo no sustituido o mono-, di- o trisustituido con R3, =S, =NR7 y/u =0 (oxígeno delcarbonilo) con 1-10 átomos de C, en donde uno, dos o tres grupos CH2 pueden estar reemplazados O, S, SO, SO2, NH, NR11 y/o por grupos -CH=CH y/o también 1-7 átomos de H pueden estar reemplazados por F y/o Cl, o alquilo cíclico con 3-7 átomos de C,Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di-, tri- o tetrasustituido con A, Hal, OH, OA, Ar', OAr', Het, OHet, SH, SA, SAr', SHet, NH2, NHA, NAA', NHAr', N(Ar')2, NHHet, N(Het)2, NAAr', NAHet, SOA, SOAr', SOHet, SO2A, SO2Ar', SO2Het,NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NACOA, NHCONH2, NHCONHA, NHCONA2, NHSO2A, NASO2A, CHO, COA, COAr', COHet, SO3H, SO2NH2, SO2NHAr', SO2N(Ar')2, SO2NHHet y/o SO2N(Het)2, Het es un heterociclo mono- o bicíclico saturado, insaturado oaromático con 1 a 4 átomos de N, O y/o S, que puede estar mono-, di- o trisustituido con A, Hal, OH, OA, Ar, OAr, Het', OHet', SH, SA, SAr', SHet', NH2, NHA, NAA', NHAr', N(Ar')2, NHHet', N(Het')2, NAAr', NAHet', SOA, SOAr', SOHet', SO2A, SO2Ar',SO2Het', NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NACOA, NHCONH2, NHCONHA, NHCONA2, NHSO2A, NASO2A, CHO, COA, COAr', COHet', SO3H, SO2NH2, SO2NHAr', SO2N(Ar')2, SO2NHHet' o SO2N(Het')2, =S, =NR7 y/u =0 (oxígeno del carbonilo), Ar' es fenilono sustituido o mono-, di-, tri- o tetrasustituido con A, Hal, OH, OA, Ofenilo, SH, SA, NH2, NHA, NAA', NHfenilo, SOA, SOfenilo, SO2A, SO2fenilo, NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NACOA, NHCONH2, NHCONHA, NHCONA2, NHSO2A, NASO2A, CHO,COA, COfenilo, SO3H, SO2NH2, SO2NHfenilo y/o SO2N(fenilo)2, Het' es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O Y/o S, que puede estar mono-, di- o trisustituido con A,.Hal, OH, OA, NH2, NHA, NAA', SOA,SOAr', SO2A, SO2Ar', NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NACOA, NHCONH2, NHCONHA, NHCONA2, NHSO2A, NASO2A, CHO, COA, COAr', SO3H, SO2NH2, SO2NHAr', SO2N(Ar')2, =S,. =NR7 y/u =0 (oxígeno del carbonilo), Hal es F, Cl, Br o I, m es 0, 1,2, o 3, n es 0, 1, o 2, así como sus derivados, sales, solvatos y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la SGK y pueden atizarse en medicamentos para el tratamiento deenfermedades causadas por SGK y dolencias tales como diabetes, obesidad, síndrome metabolico (dislipidemia), hipertonía sistémica y pulmonar, enfermedades cardiocircuiatorias y enfermedades renales, en general en cualquier tipo de fibrosis yprocesos inflamatorios.
ARP080102031A 2007-05-14 2008-05-14 Derivados de 1h-indazol-5-il-[1, 3, 4]oxadiazol-2-ilo, un metodo para su preparacion, y el uso de los mismos en medicamentos para el tratamiento de enfermedades mediadas por la modulacion de la sgk. AR066557A1 (es)

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DE102007022565A DE102007022565A1 (de) 2007-05-14 2007-05-14 Heterocyclische Indazolderivate

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EP (1) EP2155728B1 (es)
JP (1) JP5543335B2 (es)
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AU (1) AU2008250706B2 (es)
CA (1) CA2687162C (es)
DE (1) DE102007022565A1 (es)
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IL (1) IL202034A (es)
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EP2155728B1 (de) 2015-07-29
DE102007022565A1 (de) 2008-11-20
JP5543335B2 (ja) 2014-07-09
WO2008138448A2 (de) 2008-11-20
US20110190355A1 (en) 2011-08-04
CA2687162A1 (en) 2008-11-20
CA2687162C (en) 2015-06-23
EP2155728A2 (de) 2010-02-24
JP2010526840A (ja) 2010-08-05
IL202034A0 (en) 2010-06-16
ES2548444T3 (es) 2015-10-16
IL202034A (en) 2015-07-30
AU2008250706A1 (en) 2008-11-20
US8334309B2 (en) 2012-12-18
WO2008138448A3 (de) 2009-03-05

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