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AR046056A1 - Derivados de tiofeno-2-carboxamida y su uso como antagonistas de los receptores canabinoides cb1 - Google Patents

Derivados de tiofeno-2-carboxamida y su uso como antagonistas de los receptores canabinoides cb1

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Publication number
AR046056A1
AR046056A1 ARP040103632A ARP040103632A AR046056A1 AR 046056 A1 AR046056 A1 AR 046056A1 AR P040103632 A ARP040103632 A AR P040103632A AR P040103632 A ARP040103632 A AR P040103632A AR 046056 A1 AR046056 A1 AR 046056A1
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AR
Argentina
Prior art keywords
group
alkyl
substituted
phenyl
unsubstituted
Prior art date
Application number
ARP040103632A
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English (en)
Inventor
Francis Barth
Jean Philippe Ducoux
Murielle Rinaldi-Carmona
Christian Congy
Original Assignee
Sanofi Aventis
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Filing date
Publication date
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR046056A1 publication Critical patent/AR046056A1/es

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    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Abstract

La presente se refiere a derivados de tiofeno-2-carboxamida y su uso como antagonistas de los receptores canabinoides CB1.Procedimiento de preparación y aplicación en terapéutica. Reivindicación 1: Compuesto que responde a la fórmula (1) en la cual R1 representa H o un alquilo C1-4; R2 representa un grupo alquilo C4-10, un radical carbocíclico no aromático C3-12, no sustituido una o varias veces por un grupo alquilo C1-4, alcoxi C1-4 o hidroxilo; un 1,2,3,4-tetrahidronaftilo-1- o -2; un radical heterocíclico monooxigenado o monoazufrado, saturado, de 5 a 7 átomos, no sustituidos o sustituidos una o varias veces por un grupo alquilo C1-4; un radical heterocíclico mononitrogenado, saturado, de 5 a 7 átomos, donde el átomo de N está sustituido por un grupo alquilo C1-4, fenilo, bencilo, alcoxicarbonilo C1-4 o alcanoilo C1-4; un grupo alquileno C1-3 que lleva un radical carbocíclico no aromático C3-10 no sustituido o sustituido una o varias veces por un grupo alquilo C1-4; un grupo fenilalquileno en el cual el alquileno es C1-3, no sustituido o sustituido en el alquileno por uno o varios grupos metilo, y/o sustituido en el fenilo por uno o varios sustituyentes idénticos o diferentes elegidos entre un átomo de halógeno o un grupo alquilo C1-4, trifluorometilo, alcoxi C1-4, trifluorometoxi; un metileno sustituido por un radical benzotienilo, benzofurilo, tienilo, o furilo, y dichos radicales están no sustituidos o sustituidos por uno o varios grupos alquilo C1-4; un grupo NR9R10; o R1 y R2 junto con el átomo de N al cual están unidos constituyen, o bien un radical piperazin-1-ilo o 1,4-diazepan-1-ilo sustituido en 4- por un grupo fenilo o bencilo, o bien un radical piperidin-1-ilo o pirrolidin-1-ilo mono- o gem- disustituido por un grupo fenilo, bencilo, alquilo C1-4, hidroxilo, alcoxi C1-4, ciano, alcanoilo C1-3, alcoxicarbonilamino C1-4, alcanoilamino C1-3; los grupos fenilo o bencilo están no sustituidos o sustituidos una o varias veces por un átomo de halógeno y/o un grupo alquilo C1-4 y/o alcoxi C1-4, y/o trifluorometilo; R3, R4, R5, R6, R7, R8 representan, cada uno independientemente entre si, un átomo de H o de halógeno, un grupo alquilo C1-6, alcoxi C1-6, trifluorometilo o un grupo S(O)nAlk; R9 representa un átomo de H o un grupo metilo; R10 representa un grupo alquilo 1-6, fenilo o cicloalquilo C3-10, y los grupos fenilo y cicloalquilo están no sustituidos o sustituidos por uno o varios átomos de halógeno y/o grupos alquilo C1-4; o R9 y R10 junto con el átomo de N al cual están unidos, constituyen un radical heterocíclico, saturado o insaturado, de 5 a 11 átomos, puenteado o no, que comprende o no un C espiránico y que contiene, o no, un segundo heteroátomo elegido entre O o N, y dicho radical está no sustituido o sustituido por un grupo hidroxilo o fenilo o una o varias veces por un grupo alquilo C1-4 y/o alcoxi C1-4; R11 representa un átomo de H, un grupo alquilo C1-4 o cicloalquilo C3-7; n representa 0, 1 o 2; Alk representa un grupo alquilo C1-4; en estado de base o de sales de adición con un ácido, así como en estado de hidrato o de solvato.
ARP040103632A 2003-10-10 2004-10-07 Derivados de tiofeno-2-carboxamida y su uso como antagonistas de los receptores canabinoides cb1 AR046056A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR0311861A FR2860792B1 (fr) 2003-10-10 2003-10-10 Derives de thiophene-2-carboxamide, leur preparation et leur application en therapeutique

Publications (1)

Publication Number Publication Date
AR046056A1 true AR046056A1 (es) 2005-11-23

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ARP040103632A AR046056A1 (es) 2003-10-10 2004-10-07 Derivados de tiofeno-2-carboxamida y su uso como antagonistas de los receptores canabinoides cb1

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Country Link
US (1) US7462631B2 (es)
EP (1) EP1678159A2 (es)
JP (1) JP2007508279A (es)
AR (1) AR046056A1 (es)
FR (1) FR2860792B1 (es)
TW (1) TW200526647A (es)
WO (1) WO2005035488A2 (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2880023B1 (fr) * 2004-12-23 2007-02-23 Sanofi Aventis Sa Derives de n-[(4,5-diphenyl-3-alkyl-2-thienyl) methyl] amine leur preparation et leur application en therapeutique
FR2880890B1 (fr) * 2005-01-19 2007-03-30 Sanofi Aventis Sa Derives de n-[(4,5-diphenyl-2-thienyl)methyl]sulfonamide, leur preparation et leur application en therapeutique
FR2881744B1 (fr) * 2005-02-09 2007-04-27 Sanofi Aventis Sa Derives de n-[(4,5-diphenyl-2-thienyl)methyl]amine, leur preparation et leur application en therapeutique
DE102008015032A1 (de) 2008-03-17 2009-09-24 Aicuris Gmbh & Co. Kg Substituierte Pyrazolamide und ihre Verwendung
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TW200526647A (en) 2005-08-16
FR2860792B1 (fr) 2006-02-24
WO2005035488A2 (fr) 2005-04-21
US20060264470A1 (en) 2006-11-23
US7462631B2 (en) 2008-12-09
EP1678159A2 (fr) 2006-07-12

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