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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FR2783246B1 (fr) 1998-09-11 2000-11-17 Aventis Pharma Sa Derives d'azetidine, leur preparation et les medicaments les contenant
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
WO2001058869A2 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
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
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
FR2805818B1 (fr) 2000-03-03 2002-04-26 Aventis Pharma Sa Derives d'azetidine, leur preparation et les compositions pharmaceutiques les contenant
UA74367C2 (uk) 2000-03-23 2005-12-15 Сольве Фармас'Ютікалз Б.В. ПОХІДНІ 4,5-ДИГІДРО-1Н-ПІРАЗОЛУ, ЩО ВИЯВЛЯЮТЬ АНТАГОНІСТИЧНУ АКТИВНІСТЬ ЩОДО СВ<sub>1</sub>, СПОСІБ ЇХ ОДЕРЖАННЯ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ ТА СПОСІБ ЇЇ ВИГОТОВЛЕННЯ, СПОСІБ ЛІКУВАННЯ ЗАХВОРЮВАНЬ (ВАРІАНТИ)
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
CN100395234C (zh) * 2003-01-02 2008-06-18 霍夫曼-拉罗奇有限公司 新cb1受体反激动剂

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CN100360527C (zh) 2008-01-09
BR0317931A (pt) 2005-11-29
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TW200412344A (en) 2004-07-16
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JP4271660B2 (ja) 2009-06-03
EP1583762A1 (en) 2005-10-12
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AU2003293968A1 (en) 2004-07-29
ATE400571T1 (de) 2008-07-15
WO2004060888A1 (en) 2004-07-22
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KR20050092381A (ko) 2005-09-21
EP1583762B1 (en) 2008-07-09
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