AR044080A1 - 7-azaindoles y su uso como medicamentos - Google Patents

7-azaindoles y su uso como medicamentos

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Publication number
AR044080A1
AR044080A1 ARP040101395A ARP040101395A AR044080A1 AR 044080 A1 AR044080 A1 AR 044080A1 AR P040101395 A ARP040101395 A AR P040101395A AR P040101395 A ARP040101395 A AR P040101395A AR 044080 A1 AR044080 A1 AR 044080A1
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AR
Argentina
Prior art keywords
alkyl
aryl
mono
so3h
cooh
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ARP040101395A
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English (en)
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Elbion Ag
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Publication of AR044080A1 publication Critical patent/AR044080A1/es

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    • 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
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    • 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
    • C07D471/12—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 three hetero rings

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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
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Abstract

Procedimientos para su preparación, preparaciones farmacéuticas que contienen estos compuestos, así como al uso farmacéutico de estos compuestos que son inhibidores de la fosfodiesterasa 4, como componentes activos para el tratamiento de enfermedades que pueden modificarse al inhibir la actividad de la fosfodiesterasa 4, especialmente en células inmunocompetentes (por ejemplo, macrófagos y linfocitos), mediante los compuestos. Reivindicación 1: 7-azaindoles caracterizados porque tienen la fórmula general (1), en la cual: A puede equivaler a nitrógeno o un grupo N-óxido, B puede ser carbono, nitrógeno o un grupo N-óxido; R1 es i) alquilo-C1-10, de cadena recta o ramificada, eventualmente monosustituido o polisustituido con - OH, -SH, -NH2, -NH-alquilo-C1-6, -N(alquilo-C1-6)2, -NH-arilo-C6-14, -N(arilo-C6-14)2, -N(alquilo-C1-6)(arilo-C6-14)2, -NO2, -CN, -F, -Cl, -Br, -I, -O-alquilo (C1-6), -O-arilo (C6-14), -S-alquilo (C1-6), -S-arilo (C6-14), -SO3H, -SO2-alquilo (C1-6),- SO2-arilo (C6-14), -OSO2-alquilo (C1-6), -OSO2-arilo (C6-14), -COOH, -(CO)-alquilo (C1-5), -COO-alquilo (C1-5), -O(CO)-alquilo (C1-5), con carbociclos saturados mono-, bi- o tricíclicos o carbociclos mono- o poliinsaturados con anillos de 3-14 miembros y/o con heterociclos mono-, poliinsaturados con anillos de 5-15 miembros y 1-6 heteroátomos, que preferentemente son N, O y S, en donde los grupos arilo-C6-14, y a su vez los sustituyentes carbocíclicos y heterocíclicos eventualmente pueden estar sustituidos con alquilo-C1-6, -OH, -NH2, -NH-alquilo-C1-6, -N(alquilo C1-6)2, -NO2, -CN, -F, -Cl, -Br, -I, -O-alquilo (C1-6), -S-alquilo (C1-6), -SO3H, -SO2-alquilo (C1-6),-OSO2-alquilo (C1-6), -COOH, -(CO)alquilo (C1-5), -COO-alquilo (C1-5), y/o -O(CO)alquilo (C1-5), y en donde a su vez los grupos alquilo pueden estar mono- o polisustituidos en los sustituyentes carbocíclicos y heterocíclicos con -OH, -SH, -NH2, -F, -Cl, -Br, -I, -SO3H y/o -COOH, o ii) alquenilo C2-10, mono- o poliinsaturado, de cadena lineal o ramificada, eventualmente monosustituido o polisustituido con -OH, -SH, -NH2, -NH-alquilo (C1-6), -N(alquilo C1-6)2, -NH-arilo (C6-14), -N(arilo C6-14)2, -N(alquilo C1-6)(arilo C6-14)2, -NO2, -CN, -F, -Cl, -Br, -I, -O-alquilo (C1-6), -O-arilo (C6-14), -S-alquilo (C1-6), -S-arilo (C6-14), -SO3H, -SO2-alquilo (C1-6,)-SO2-arilo (C6-14), -OSO2-alquilo (C1-6), -OSO2-arilo (C6-14), -COOH, -(CO)-alquilo (C1-5), -COO-alquilo (C1-5), y/u -O(CO)alquilo (C1-5), con carbociclos saturados mono-, bi- o tricíclicos o carbociclos mono- o poliinsaturados con anillo de 3-14 miembros y/o con heterociclos mono- o poliinsaturados con anillos de 5-15 miembros y 1-6 heteroátomos, que preferentemente son N, O y S, en donde los grupos arilo-C6-14 y a su vez los sustituyentes carbocíclicos y heterocíclicos eventualmente pueden estar sustituidos con alquilo-C1-6, -OH, -NH2, -NH-alquilo (C1-6), -N(alquilo C1-6)2, -NO2, -CN, -F, -Cl, -Br, -I, -O-alquilo (C1-6), -S-alquilo (C1-6), -SO3H, -SO2-alquilo (C1-6),-OSO2-alquilo (C1-6), -COOH, -(CO)-alquilo-C1-5, -COO-alquilo (C1-5), y/u -O(CO)-alquilo (C1-5), y en donde a su vez los grupos alquilo pueden estar mono- o polisustituidos en los sustituyentes carbocíclicos y heterocíclicos con -OH, -SH, -NH2, -F, -Cl, -Br, -I, -SO3H y/o -COOH; R2 es hidrógeno o alquilo C1-3; R3 y R4 pueden ser iguales o diferentes y son hidrógeno, alquilo-C1-6, -OH, -SH, -NH2, NH-alquilo (C1-6), -N(-alquilo C1-6)2, -NO2, -CN, -SO3H, - SO3-alquilo (C1-6), -COOH, -COO-alquilo (C1-6), -O(CO)-alquilo (C1-6), -F, -Cl, -Br, -I, -O-alquilo (C1-6), -S-alquilo (C1-6), -fenilo o -piridilo, en donde a su vez los sustituyentes fenilo o piridilo pueden estar eventualmente mono- o polisustituidos con alquilo C1-3, -OH, -SH, -NH2, -NH-alquilo (C1-3), -N(alquilo C1-3)2, -NO2, -CN, -SO3H, -SO3-alquilo (C1-3), -COOH, -COO-alquilo (C1-3), -F, -Cl, -Br, -I, -O-alquilo (C1-3), -S-alquilo (C1-3) y/u -O(CO)-alquilo (C1-3), o sales de los compuestos de acuerdo con la fórmula (1).
ARP040101395A 2003-04-24 2004-04-23 7-azaindoles y su uso como medicamentos AR044080A1 (es)

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DE10318610A DE10318610A1 (de) 2003-04-24 2003-04-24 7-Azaindole und deren Verwendung als Therapeutika

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US (2) US7211583B2 (es)
EP (1) EP1613627A1 (es)
JP (1) JP2006524209A (es)
KR (1) KR20060021830A (es)
CN (1) CN100475814C (es)
AR (1) AR044080A1 (es)
AU (1) AU2004232483B2 (es)
BR (1) BRPI0409790A (es)
CA (1) CA2523063C (es)
DE (1) DE10318610A1 (es)
MX (1) MXPA05011439A (es)
NO (1) NO20055515L (es)
NZ (1) NZ543700A (es)
RU (1) RU2349592C2 (es)
TW (1) TWI365187B (es)
UA (1) UA82227C2 (es)
WO (1) WO2004094416A1 (es)
ZA (1) ZA200508321B (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10318610A1 (de) * 2003-04-24 2004-11-11 Elbion Ag 7-Azaindole und deren Verwendung als Therapeutika
CN101355876B (zh) 2005-11-09 2012-09-05 康宾纳特克斯公司 一种适用于眼部给药的组合物
WO2009147476A1 (en) * 2008-06-02 2009-12-10 Matrix Laboratories Ltd. Novel pde inhibitors, pharmaceutical compositions containing them and processes for their preparation
EP2344503B1 (en) * 2008-09-22 2014-04-16 Isis Innovation Ltd 5-azaindole bisphosphonates
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CA2523063A1 (en) 2004-11-04
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