AR057987A1 - Compuestos agonistas de cb1 (receptor cannabinoide) - Google Patents
Compuestos agonistas de cb1 (receptor cannabinoide)Info
- Publication number
- AR057987A1 AR057987A1 ARP060105092A ARP060105092A AR057987A1 AR 057987 A1 AR057987 A1 AR 057987A1 AR P060105092 A ARP060105092 A AR P060105092A AR P060105092 A ARP060105092 A AR P060105092A AR 057987 A1 AR057987 A1 AR 057987A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- aryl
- heteroaryl
- haloalkoxy
- Prior art date
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Abstract
Los compuestos de la formula (1) son utiles en tratamientos del trastorno gastrointestinal funcional, dispepsia, intestino irritable, dolor. Reivindicacion 1: Un compuesto de la formula (1), donde por lo menos uno de A1 y A2 es N, y si ambos no son N, entonces el otro es CH; R1 se selecciona de hidrogeno, ciano, halogeno, hidroxi, NR6R7, alquenilo C2-6, alquinilo C2-6, alquilo C1-9, cicloalquilo C3-6 y haloalcoxi C1-6, donde dichos alquenilo C2-6, alquinilo C2-6, alquilo C1-9, cicloalquilo C3- 6 o haloalcoxi C1-6 están opcionalmente sustituidos con hidroxi, NR6aR7a, cicloalquilo C3-6, arilo y heteroarilo; R2 se selecciona de hidrogeno, ciano, halogeno, hidroxi, NR6R7, alquenilo C2-6, alquinilo C2-6, alquilo C1-6, cicloalquilo C3-6 y haloalcoxi C1-6, donde dichos alquenilo C2-6, alquinilo C2-6, alquilo C1-6, cicloalquilo C3-6 o haloalcoxi C1-6 están opcionalmente sustituidos con hidroxi, NR6aR7a, cicloalquilo C3-6, arilo y heteroarilo; R3 se selecciona del grupo de formulas (2), y donde R3 está opcionalmente sustituido con halogeno, ciano, nitro, NR6R7, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo o heteroarilo, donde dichos alquilo C1-6, cicloalquilo C3-6, arilo o heteroarilo están opcionalmente sustituidos con halogeno, ciano, nitro, NR6R7, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo, heteroarilo o un sistema de anillo saturado que consiste en 4 a 7 átomos seleccionados de C, N y O, y donde dichos alquilo C1-6, cicloalquilo C3-6, arilo, heteroarilo o sistema de anillo están opcionalmente sustituidos con alquilo C1-4, y donde dicho alquilo C1-4 está opcionalmente sustituido con NR6R7, arilo, hidroxi o alcoxi C1-4; R4 se selecciona de hidrogeno y alquilo C1- 6; R5 se selecciona de alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6 heteroarilo y arilo, donde dichos alquilo C1-6, cicloalquilo C3-6, heteroarilo o arilo están opcionalmente sustituidos con halogeno, ciano, nitro, NR6R7, alquilo C1- 6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo o heteroarilo; n se selecciona de 0, 1, 2, 3, 4 y 5; o R4 y R5 juntos forman un sistema de anillo saturado, insaturado o parcialmente saturado que consiste en 3 a 7 átomos seleccionados de C, O y N; o R4 y R5 juntos forman un sistema de anillo condensado saturado, insaturado o parcialmente saturado que consiste en 7 a 13 átomos seleccionados de C, O y N; donde dicho sistema de anillo está opcionalmente sustituido con halogeno, ciano, nitro, NR6R7, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo o heteroarilo, y donde dichos alquilo C1-6, cicloalquilo C3-6, arilo o heteroarilo están opcionalmente sustituidos con halogeno, ciano, nitro, NR6R7, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo o heteroarilo; R6, R6a, R7 y R7a se seleccionan de manera independiente de hidrogeno, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, alquenilo C2-6, alquinilo C2-6, arilo y heteroarilo; o R6 y R7 juntos pueden formar un sistema de anillo saturado que consiste en 4 a 7 átomos seleccionados de C, O y N, donde el sistema de anillo está opcionalmente sustituido con alquilo C1-6, alcoxi C1-6, halogeno o hidroxi; donde uno o más átomos de carbono de cada grupo alquilo o cicloalquilo definido para R1 pueden estar sustituidos con O, NH, C(O), SO o SO2, donde ningun N u O está en una posicion adyacente a cualquier otro O o N, y donde ningun SO o SO2 está en una posicion adyacente a cualquier otro SO o SO2; donde uno o más átomos de carbono de cada grupo alquilo o cicloalquilo definido para R2, R3, R4, R5, R6, R6a, R7 y R7a pueden estar sustituidos con O, NH, C(O) o SO2, donde ningun N u O está en una posicion adyacente a cualquier otro O o N; donde uno o más átomos de carbono de cada grupo alquilo o cicloalquilo definido para R1, R2, R3, R4, R5, R6, R6a, R7 y R7a pueden estar sustituidos con fluor; y con la condicion de que R1 no sea hidrogeno, halogeno, ciano, acetilamino, hidroxi, alcoxi C1-6, alquilo C1-6, haloalcoxi C1-6, alquenilo C2-6, haloalquilo C1-6, haloalquenilo C2-6 o NR6R7; al mismo tiempo que R2 es hidrogeno, halogeno, ciano, acetilamino, hidroxi, alcoxi C1-6, alquilo C1-6, haloalcoxi C1-6, alquenilo C2-6, haloalquilo C1-6, haloalquenilo C2-6 o NR6R7; a menos que R3 esté sustituido con un alquilo C1-4, donde dicho alquilo C1-4 está sustituido con un heteroarilo, cicloalquilo C3-6, arilo o un sistema de anillo saturado que consiste en 4 a 7 átomos seleccionados de C, O y N, donde dicho heteroarilo, cicloalquilo C3-6 o arilo está adicionalmente sustituido con alquilo C1-4 o halogeno, donde dicho alquilo C1-4 está opcionalmente sustituido con NR6R7, arilo, hidroxi o alcoxi C1-4, y donde dicho sistema de anillo está opcionalmente sustituido con alquilo C1-4, donde dicho alquilo C1-4 está opcionalmente sustituido con NR6R7, arilo, hidroxi o alcoxi C1-4; o a menos que R3 se seleccione entre el grupo de formulas (3), opcionalmente sustituidos con halogeno, ciano, nitro, NR6R7, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo o heteroarilo; o una de sus sales aceptables para uso farmacéutico, o diastereomeros, enantiomeros o sus mezclas.
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US (1) | US20090181968A1 (es) |
EP (1) | EP1957478A2 (es) |
JP (1) | JP2009517383A (es) |
CN (1) | CN101336238A (es) |
AR (1) | AR057987A1 (es) |
TW (1) | TW200804338A (es) |
UY (1) | UY29963A1 (es) |
WO (1) | WO2007061360A2 (es) |
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US8859596B2 (en) | 2008-09-16 | 2014-10-14 | Abbvie Inc. | Compounds as cannabinoid receptor ligands |
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CA3004297A1 (en) | 2015-11-06 | 2017-05-11 | Samumed, Llc | 2-(1h-indazol-3-yl)-3h-imidazo[4,5-c]pyridines and their anti-inflammatory uses thereof |
US10980806B2 (en) | 2016-03-24 | 2021-04-20 | University of Pittsburgh—of the Commonwealth System of Higher Education | Small molecule inhibitors of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer |
PL3464285T3 (pl) | 2016-06-01 | 2023-02-06 | Biosplice Therapeutics, Inc. | Sposób wytwarzania n-(5-(3-(7-(3-fluorofenylo)-3h-imidazo[4,5-c]pirydyn-2-ylo)-1h-indazol-5-ilo)pirydyn-3-ylo)-3-metylobutanoamidu |
JP2019535672A (ja) | 2016-10-21 | 2019-12-12 | サミュメッド リミテッド ライアビリティ カンパニー | インダゾール−3−カルボキサミドの使用方法およびwnt/β−カテニンシグナル伝達経路阻害剤としてのそれらの使用 |
MA46696A (fr) | 2016-11-07 | 2019-09-11 | Samumed Llc | Formulations injectables à dose unique prêtes à l'emploi |
CN107880024A (zh) * | 2017-12-11 | 2018-04-06 | 张玉玲 | 一种用于治疗炎症的***素受体激动剂及其合成方法 |
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SE0401345D0 (sv) * | 2004-05-25 | 2004-05-25 | Astrazeneca Ab | Therapeutic compounds: Pyridine as scaffold |
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- 2006-11-21 TW TW095143017A patent/TW200804338A/zh unknown
- 2006-11-21 AR ARP060105092A patent/AR057987A1/es unknown
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- 2006-11-22 US US12/094,334 patent/US20090181968A1/en not_active Abandoned
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- 2006-11-22 EP EP06813036A patent/EP1957478A2/en not_active Withdrawn
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TW200804338A (en) | 2008-01-16 |
CN101336238A (zh) | 2008-12-31 |
WO2007061360A3 (en) | 2007-07-26 |
EP1957478A2 (en) | 2008-08-20 |
WO2007061360A2 (en) | 2007-05-31 |
JP2009517383A (ja) | 2009-04-30 |
UY29963A1 (es) | 2007-06-29 |
US20090181968A1 (en) | 2009-07-16 |
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