ES2309383T3 - Pirrolil tiazoles y su empleo como agonistas inversos de receptores cb1. - Google Patents

Pirrolil tiazoles y su empleo como agonistas inversos de receptores cb1. Download PDF

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ES2309383T3
ES2309383T3 ES03789381T ES03789381T ES2309383T3 ES 2309383 T3 ES2309383 T3 ES 2309383T3 ES 03789381 T ES03789381 T ES 03789381T ES 03789381 T ES03789381 T ES 03789381T ES 2309383 T3 ES2309383 T3 ES 2309383T3
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lower alkyl
lower alkoxy
fluorinated
amino
hydroxy
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Wolfgang Guba
Wolfgang Haap
Hans Peter Marty
Robert Narquizian
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F Hoffmann La Roche AG
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    • C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond

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Abstract

Compuestos de la fórmula (I) (Ver fórmula) en la que R 1 es hidrógeno o alquilo inferior; R 2 es hidrógeno, alquilo inferior, alquenilo inferior, alcoxi inferior-alquilo inferior, (alcoxi inferior)carbonilamino, -(CH2)m-R 2a o -NHC(O)-R 2a ; o R 1 y R 2 junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico saturado de 5 ó 6 eslabones que contiene eventualmente uno o dos heteroátomos adicionales elegidos con independencia entre sí entre nitrógeno, oxígeno y azufre, dicho anillo heterocíclico está eventualmente mono-, di- o trisustituido, con independencia entre sí, por hidroxi, alquilo inferior, alcoxi inferior, amino, (alquilo inferior)amino, alquilo inferior fluorado o alcoxi inferior fluorado; R 2a es cicloalquilo, eventualmente mono-, di-, tri- o tetrasustituido, con independencia entre sí, por hidroxi, alquilo inferior, alcoxi inferior, alquilo inferior fluorado o alcoxi inferior fluorado; cicloalquenilo, eventualmente mono-, di- o trisustituido, con independencia entre sí, por hidroxi, alquilo inferior, alcoxi inferior, alquilo inferior fluorado o alcoxi inferior fluorado; un anillo heterocíclico saturado monovalente de 5 ó 6 eslabones que contiene de uno a tres heteroátomos elegidos con independencia entre sí entre nitrógeno, oxígeno y azufre, dicho anillo heterocíclico está eventualmente mono-, di- o trisustituido, con independencia entre sí, por hidroxi, alquilo inferior, alcoxi inferior, amino, (alquilo inferior)amino, alquilo inferior fluorado o alcoxi inferior fluorado; un anillo heteroaromático monovalente de 5 ó 6 eslabones que contiene de uno a tres heteroátomos elegidos con independencia entre sí entre nitrógeno, oxígeno y azufre, dicho anillo heteroaromático está eventualmente mono-, di- o trisustituido, con independencia entre sí, por hidroxi, alquilo inferior, alcoxi inferior, halógeno, amino, (alquilo inferior)amino; o fenilo, que puede estar eventualmente mono-, di- o trisustituido, con independencia entre sí, por hidroxi, alquilo inferior, alcoxi inferior, halógeno, (alquilo inferior)amino, alquilo inferior halogenado, alcoxi inferior halogenado o nitro; R 3 es alquilo inferior, alquenilo inferior, alcoxi inferior-alquilo inferior, di-fenil-alquilo inferior o -(CH2)n-R 3a ; R 3a es cicloalquilo, que puede estar eventualmente fusionado con un anillo fenilo; o cicloalquilo que puede estar eventualmente mono-, di- o trisustituido, con independencia entre sí, por hidroxi, alquilo inferior, alcoxi inferior, alquilo inferior fluorado o alcoxi inferior fluorado; cicloalquenilo, que puede estar eventualmente mono-, di- o trisustituido, con independencia entre sí, por hidroxi, alquilo inferior, alcoxi inferior, alquilo inferior fluorado o alcoxi inferior fluorado; un anillo heterocíclico saturado monovalente de 5 ó 6 eslabones que contiene de uno a tres heteroátomos elegidos con independencia entre sí entre nitrógeno, oxígeno y azufre, dicho anillo heterocíclico está eventualmente mono-, di- o trisustituido, con independencia entre sí, por hidroxi, alquilo inferior, alcoxi inferior, amino, (alquilo inferior)amino, alquilo inferior fluorado o alcoxi inferior fluorado; un anillo heteroaromático monovalente de 5 ó 6 eslabones que contiene de uno a tres heteroátomos elegidos con independencia entre sí entre nitrógeno, oxígeno y azufre, dicho anillo heteroaromático está eventualmente mono-, di- o trisustituido, con independencia entre sí, por hidroxi, alquilo inferior, alcoxi inferior, halógeno, amino o (alquilo inferior)amino; o fenilo, que puede estar eventualmente mono-, di- o trisustituido, con independencia entre sí, por hidroxi, alquilo inferior, alcoxi inferior, halógeno, (alquilo inferior)amino, alquilo inferior halogenado, alcoxi inferior halogenado o nitro; R 4 es...
ES03789381T 2003-01-02 2003-12-22 Pirrolil tiazoles y su empleo como agonistas inversos de receptores cb1. Expired - Lifetime ES2309383T3 (es)

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EP03000002 2003-01-02

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ES2309383T3 true ES2309383T3 (es) 2008-12-16

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US (1) US7135488B2 (es)
EP (1) EP1583762B1 (es)
JP (1) JP4271660B2 (es)
KR (1) KR100674769B1 (es)
CN (1) CN100360527C (es)
AR (1) AR042690A1 (es)
AT (1) ATE400571T1 (es)
AU (1) AU2003293968A1 (es)
BR (1) BR0317931A (es)
CA (1) CA2511905A1 (es)
CL (1) CL2003002769A1 (es)
DE (1) DE60322114D1 (es)
ES (1) ES2309383T3 (es)
MX (1) MXPA05007115A (es)
PL (1) PL378244A1 (es)
RU (1) RU2330035C2 (es)
TW (1) TW200412344A (es)
WO (1) WO2004060888A1 (es)

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CN113480530A (zh) 2016-12-26 2021-10-08 阿里根公司 芳香烃受体调节剂
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FR2789079B3 (fr) 1999-02-01 2001-03-02 Sanofi Synthelabo Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant
FR2800375B1 (fr) 1999-11-03 2004-07-23 Sanofi Synthelabo Derives tricycliques d'acide pyrazolecarboxylique, leur preparation, les compositions pharmaceutiques en contenant
JP2004502642A (ja) * 2000-02-11 2004-01-29 ブリストル−マイヤーズ スクイブ カンパニー カンナビノイドレセプターモジュレーター、それらの製造方法、および呼吸系および非呼吸系疾患の処置のためのカンナビノイドレセプターモジュレーターの使用
FR2805810B1 (fr) 2000-03-03 2002-04-26 Aventis Pharma Sa Compositions pharmaceutiques contenant des derives de 3- amino-azetidine, les nouveaux derives et leur preparation
FR2805818B1 (fr) 2000-03-03 2002-04-26 Aventis Pharma Sa Derives d'azetidine, leur preparation et les compositions pharmaceutiques les contenant
FR2805817B1 (fr) 2000-03-03 2002-04-26 Aventis Pharma Sa Compositions pharmaceutiques contenant des derives d'azetidine, les nouveaux derives d'azetidine et leur preparation
PL208098B1 (pl) 2000-03-23 2011-03-31 Solvay Pharm Bv Pochodne 4,5-dihydro-1H-pirazolu, kompozycja farmaceutyczna, sposób wytwarzania związków oraz ich zastosowanie
FR2814678B1 (fr) 2000-10-04 2002-12-20 Aventis Pharma Sa Association d'un antagoniste du recepteur cb1 et de sibutramine, les compositions pharmaceutiques les contenant et leur utilisation pour la traitement de l'obesite
TW200413328A (en) * 2003-01-02 2004-08-01 Hoffmann La Roche Novel CB 1 receptor inverse agonists

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CA2511905A1 (en) 2004-07-22
WO2004060888A1 (en) 2004-07-22
TW200412344A (en) 2004-07-16
US20040147572A1 (en) 2004-07-29
KR100674769B1 (ko) 2007-02-28
ATE400571T1 (de) 2008-07-15
AR042690A1 (es) 2005-06-29
RU2005124359A (ru) 2006-05-27
KR20050092381A (ko) 2005-09-21
MXPA05007115A (es) 2005-11-16
BR0317931A (pt) 2005-11-29
EP1583762A1 (en) 2005-10-12
AU2003293968A1 (en) 2004-07-29
CN1735611A (zh) 2006-02-15
US7135488B2 (en) 2006-11-14
CL2003002769A1 (es) 2005-01-07
EP1583762B1 (en) 2008-07-09
PL378244A1 (pl) 2006-03-20
DE60322114D1 (de) 2008-08-21
JP4271660B2 (ja) 2009-06-03
CN100360527C (zh) 2008-01-09
JP2006513226A (ja) 2006-04-20

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