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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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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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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)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA05007114A (es) 2003-01-02 2005-08-26 Hoffmann La Roche Nuevos agonistas inversos del receptor cb1.
US20070060596A1 (en) * 2003-10-24 2007-03-15 Giblin Gerard M P Heterocyclyl compounds
BRPI0513677B8 (pt) * 2004-07-30 2021-05-25 Exelixis Inc derivados de pirrol como agentes farmacêuticos
ES2435790T3 (es) 2004-12-03 2013-12-23 Intervet International B.V. Piperazinas sustituidas como antagonistas de CB1
WO2007003962A2 (en) 2005-06-30 2007-01-11 Prosidion Limited Gpcr agonists
MX2008009354A (es) * 2006-01-18 2008-09-30 Schering Corp Moduladores de receptores cannabinoides.
CL2008000017A1 (es) 2007-01-04 2008-08-01 Prosidion Ltd Compuestos derivados de heterociclos de nitrogeno y oxigeno, agonistas de gpcr; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la obesidad, diabetes, sindrome metabolico, hiperlipidemia, toleranci
AR064735A1 (es) 2007-01-04 2009-04-22 Prosidion Ltd Agonistas de gpcr y composicion farmaceutica en base al compuesto
RS52065B (en) 2007-01-04 2012-06-30 Prosidion Ltd PIPERIDINSKI GPCR AGONIST
JP2010514832A (ja) 2007-01-04 2010-05-06 プロシディオン・リミテッド ピペリジンgpcrアゴニスト
GB0700122D0 (en) 2007-01-04 2007-02-14 Prosidion Ltd GPCR agonists
WO2008130616A2 (en) * 2007-04-19 2008-10-30 Schering Corporation Diaryl morpholines as cb1 modulators
NZ582249A (en) * 2007-06-28 2012-06-29 Intervet Int Bv Substituted piperazines as cb1 antagonists
US20100286160A1 (en) * 2007-06-28 2010-11-11 Intervet Inc. Substituted piperazines as cb1 antagonists
GB0720389D0 (en) 2007-10-18 2008-11-12 Prosidion Ltd G-Protein Coupled Receptor Agonists
GB0720390D0 (en) 2007-10-18 2007-11-28 Prosidion Ltd G-Protein coupled receptor agonists
KR100954316B1 (ko) * 2007-12-05 2010-04-21 한국화학연구원 신규한 1-[1-(3,4-디알콕시벤질)-1h-피롤 화합물, 이의제조방법 및 이를 포함하는 천식 및 만성폐쇄성 폐질환을포함한 염증관련 질환, 관절염, 아토피 피부염, 암 및뇌질환의 치료 및 예방을 위한 약제학적 조성물
US8604067B2 (en) 2009-11-02 2013-12-10 Ahr Pharmaceuticals, Inc. ITE for cancer intervention and eradication
US10632106B2 (en) 2009-11-02 2020-04-28 Ariagen, Inc. Methods of cancer treatment with 2-(1′H-Indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester
EP2718290B1 (en) * 2011-06-07 2016-05-04 Clevexel Pharma Compositions and methods for modulating a kinase
EP2800745B1 (en) 2011-12-02 2020-02-12 Phenex Pharmaceuticals AG Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rory, nr1f3) activity and for the treatment of chronic inflammatory and autoimmune diseases
NZ728643A (en) * 2014-09-12 2020-04-24 Ariagen Inc Efficient and scalable synthesis of 2-(1’h-indole-3’-carbonyl)-thiazole-4-carboxylic acid methyl ester and its structural analogs
CN108239083B (zh) 2016-12-26 2021-08-17 阿里根公司 芳香烃受体调节剂
KR20200089718A (ko) 2017-11-20 2020-07-27 아리아젠, 인크. 인돌 화합물 및 이의 용도
EP3956327A1 (en) 2019-04-15 2022-02-23 Ariagen, Inc. Chiral indole compounds and their use
CN113069451B (zh) * 2021-04-02 2022-08-09 苏州大学 一种吡咯-2-磺酰胺化合物的制备方法及其在制备抗肿瘤药物中的应用

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3940418A (en) * 1972-04-07 1976-02-24 G. D. Searle & Co. Esters and amides of 4,5-dihydrobenz[g]indazole-3-carboxylic acids and related compounds
FR2713225B1 (fr) 1993-12-02 1996-03-01 Sanofi Sa N-pipéridino-3-pyrazolecarboxamide substitué.
FR2692575B1 (fr) * 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
US5342851A (en) * 1992-10-07 1994-08-30 Mcneil-Ppc, Inc. Substituted thiazole derivatives useful as platelet aggregation inhibitors
FR2714057B1 (fr) 1993-12-17 1996-03-08 Sanofi Elf Nouveaux dérivés du 3-pyrazolecarboxamide, procédé pour leur préparation et compositions pharmaceutiques les contenant.
US5596106A (en) * 1994-07-15 1997-01-21 Eli Lilly And Company Cannabinoid receptor antagonists
FR2741621B1 (fr) 1995-11-23 1998-02-13 Sanofi Sa Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant
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
CA2399791A1 (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
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
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
DZ3335A1 (fr) 2000-03-23 2001-09-27 Solvay Pharm Bv Derives de 4,5-dihydro-1h-pyrazole ayant une activite antagoniste de cb1
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
MXPA05007114A (es) * 2003-01-02 2005-08-26 Hoffmann La Roche Nuevos agonistas inversos del receptor cb1.

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CN1735611A (zh) 2006-02-15
CN100360527C (zh) 2008-01-09
EP1583762B1 (en) 2008-07-09
RU2005124359A (ru) 2006-05-27
PL378244A1 (pl) 2006-03-20
CL2003002769A1 (es) 2005-01-07
WO2004060888A1 (en) 2004-07-22
ATE400571T1 (de) 2008-07-15
US7135488B2 (en) 2006-11-14
JP2006513226A (ja) 2006-04-20
EP1583762A1 (en) 2005-10-12
US20040147572A1 (en) 2004-07-29
CA2511905A1 (en) 2004-07-22
DE60322114D1 (de) 2008-08-21
TW200412344A (en) 2004-07-16
JP4271660B2 (ja) 2009-06-03
KR100674769B1 (ko) 2007-02-28
KR20050092381A (ko) 2005-09-21
RU2330035C2 (ru) 2008-07-27
AR042690A1 (es) 2005-06-29
MXPA05007115A (es) 2005-11-16
AU2003293968A1 (en) 2004-07-29
BR0317931A (pt) 2005-11-29

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