AR059229A1 - Derivados de piperidinilo como moduladores de la actividad del receptor de quimiocina - Google Patents
Derivados de piperidinilo como moduladores de la actividad del receptor de quimiocinaInfo
- Publication number
- AR059229A1 AR059229A1 ARP070100372A ARP070100372A AR059229A1 AR 059229 A1 AR059229 A1 AR 059229A1 AR P070100372 A ARP070100372 A AR P070100372A AR P070100372 A ARP070100372 A AR P070100372A AR 059229 A1 AR059229 A1 AR 059229A1
- Authority
- AR
- Argentina
- Prior art keywords
- cr8r8
- alkyl
- heterocyclyl
- nr14r14
- rcf3
- Prior art date
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- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D211/40—Oxygen atoms
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- C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
- C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
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- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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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- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
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- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/70—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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Abstract
Moduladores de piperidinilo substituidos de MIP-1alfa o CCR-1 o estereoisomeros o sales farmacéuticamente aceptables de los mismos y composicion farmacéutica. Estos compuestos son utiles para tratar y prevenir enfermedades inflamatorias tales como asma y enfermedades alérgicas, así como patologías autoinmunes tales como artritis reumatoide y rechazo al transplante usando los modulares aquí descritos. Reivindicacion 1: Un compuesto de la formula (1) o estereoisomeros o profárrmacos o formas de sales farmacéuticamente aceptables de los mismos, caracterizado porque: la línea punteada representa un enlace doble opcional; T es como se muestra en los restos de formulas (2), R1 es alquilo, cicloalquilo, arilo, heterociclilo o heteroarilo, todos los cuales pueden ser opcionalmente substituidos con 0-5 R1a; R1a cada que se presenta, se selecciona independientemente de alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, halo, -NH2, -CN, -NO2, -C(=O)OH, -C(=O)O(CR8R8)rR10, -O(CF2)rCF3, -O(CR8R8)rR10, -OH, -SH, -S(CR8R8)rR10, -S(O)3H, -P(O)3H2, -C(=O)NR9R9, NR9R9, -S(O)NR9R9, -NR9S(O)2(CF2)rCF3, -C(=O)NR9S(O)2R6, -S(O)2NR9C(=O)OR6, -S(O)2NR9C(=O)NR9R9, -C(=O)NR9S(O)2(CF2)rCF3, -C(=O)(CR8R8)rR10, -NR9C(=O)H, -NR9C(=O)(CR8R8)rR10, -OC(=O)(CR8R8)rR10, -C(=NR14)NR9R9, -NHC(=NR14)NR14R14, -S(=O)(CR8R8)rR10, -S(O)2(CR8R8)rR10, -NR9C(=O)OR8, -NR9S(O)2R8, -S(O)2NR9C(O)R6, ariloxi o arilalquilo, en donde el arilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, ariloxi y arilalquilo pueden ser opcionalmente substituidos con 0-3 R1b; R1b cada que se presenta, se selecciona independientemente alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, halo, -NH2, -CN, -NO2, -C(=O)OH, -C(=O)O(CR8R8)rR10, -O(CF2)rCF3, - O(CR8R8)rR10, -OH, -SH, -S(CR8R8)rR10, -S(O)3H, -P(O)3H2, -C(=O)NR9R9, NR9R9, -S(O)NR9R9, -NR9S(O)2(CF2)rCF3, -C(=O)NR9S(O)2R6, -S(O)2NR9C(=O)OR6, -S(O)2NR9C(=O)NR9R9, -C(=O)NR9S(O)2(CF2)rCF3, -C(=O)(CR8R8)rR10, -NR9C(=O)H, -NR9C(=O)(CR8R8)rR10, - OC(=O)(CR8R8)rR10, -C(=NR14)NR9R9, -NHC(=NR14)NR14R14, -S(=O)(CR8R8)rR10, -S(O)2(CR8R8)rR10, -NR9C(=O)OR8, -NR9S(O)2R8, ariloxi o arilalquilo; R2 es alquilo, cicloalquilo, cicloalquilalquilo, o alquenilo, en donde el alquilo puede ser opcionalmente substituido con -OH; R3, cada que se presenta, es alquilo; o cualquiera de los dos R3's enlazados al mismo átomo de carbono pueden formar un anillo de 3 hasta 6 miembros; W es hidrogeno, F, -OH, -CN, -NH2; R5 es halo, -CN o -Oalquilo; o W y un R5 se toman junto con los átomos de carbono a los cuales cada uno se enlaza para formar un anillo que contiene oxígeno de 3 hasta 6 miembros en donde el anillo puede ser opcionalmente substituido con uno o más R5's; R6, cada que se presenta, es independientemente alquilo, cicloalquilo, cicloalquilalquilo, arilo, arilalquilo, heteroarilo o heteroarilalquilo; R8, cada que se presenta, es independientemente H o alquilo; R9, cada que se presenta, es independientemente hidrogeno, alquilo, cicloalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo o heterociclilalquilo, en donde el arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo o heterociclilalquilo pueden ser opcionalmente substituidos con 0-5 R9a, y el heteroarilo, heteroarilalquilo heterociclilo o heterociclilalquilo contiene 1-4 heteroátomos seleccionados de N, O, y S; R9a, cada que se presenta, se selecciona independientemente de alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, halo, -NH2, -CN, -NO2, -C(=O)OH, -C(=O)O(CR8R8)rR14, -O(CF2)rCF3, -O(CR8R8)rR14, -OH, -SH, -S(CR8R8)rR14, -S(O)3H, -P(O)3H2, -C(=O)NR14R14, - NR14R14, -S(O)NR14R14, -NR14S(O)2(CF2)rCF3, -C(=O)NR14S(O)2R6, -S(O)2NR14C(=O)OR6, -S(O)2NR14C(=O)NR14R14, -C(=O)NR14S(O)2(CF2)rCF3, -C(=O)(CR8R8)rR14, -NR14C(=O)H, -NR14C(=O)(CR8R8)rR14, -OC(=O)(CR8R8)rR14, -C(=NR14)NR14R14, -NHC(=NR14)R14R14, - S(=O)(CR8R8)rR14, -S(O)2(CR8R8)rR14, -NR14C(=O)OR8, -NR14S(O)2R8, ariloxi o arilalquilo; R10, cada que se presenta, se selecciona independientemente de alquilo, arilo, arilalquilo, heterociclilo o heterociclilalquilo, en donde el alquilo, arilo, arilalquilo, heterociclilo o heterociclilalquilo pueden ser opcionalmente substituidos con 0-3 R10a, y el heterociclilo o heterociclilalquilo contiene 1-4 heteroátomos seleccionados de N, O, y S; R10a, cada que se presenta, se selecciona independientemente de alquilo, haloalquilo, arilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, halo, -NH2, -CN, -NO2, -C(=O)OH, -C(=O)O(CR8R8)rR14, -O(CF2)rCF3, - O(CR8R8)rR14, -OH, -SH, -S(CR8R8)rR14, -S(O)3H, -P(O)3H2, -C(=O)NR14R14, -NR14R14, -S(O)NR14R14, -NR14S(O)2(CF2)rCF3, -C(=O)NR14S(O)2R6, -S(O)2NR14C(=O)OR6, -S(O)2NR14C(=O)NR14R14, -C(=O)NR14S(O)2(CF2)rCF3, -C(=O)(CR8R8)rR14, -NR14C(=O)H, - NR14C(=O)(CR8R8)rR14, -OC(=O)(CR8R8)rR14, -C(=NR14)NR14R14, -NHC(=NR14)R14R14, -S(=O)(CR8R8)rR14, -S(O)2(CR8R8)rR14, -NR14C(=O)OR8, -NR14S(O)2R8, ariloxi o arilalquilo; R14, cada que se presenta, se selecciona independientemente de H, alquilo, cicloalquilo o fenilo; m, cada que se presenta, es 0-2; n es 1-3; y r es 0-5.
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US7723360B2 (en) | 2004-08-06 | 2010-05-25 | Boehringer Ingelheim International Gmbh | Alkyl-and piperidine-substituted benzimidazole derivatives |
US7576106B2 (en) * | 2005-10-11 | 2009-08-18 | Chemocentryx, Inc. | Piperidine derivatives and methods of use |
US7615556B2 (en) * | 2006-01-27 | 2009-11-10 | Bristol-Myers Squibb Company | Piperazinyl derivatives as modulators of chemokine receptor activity |
US7601844B2 (en) * | 2006-01-27 | 2009-10-13 | Bristol-Myers Squibb Company | Piperidinyl derivatives as modulators of chemokine receptor activity |
CN101808991A (zh) * | 2007-07-24 | 2010-08-18 | 百时美施贵宝公司 | 作为趋化因子受体活性调节剂的哌啶基衍生物 |
-
2007
- 2007-01-23 US US11/625,874 patent/US7601844B2/en active Active
- 2007-01-25 CA CA2651987A patent/CA2651987C/en not_active Expired - Fee Related
- 2007-01-25 EP EP11188797.2A patent/EP2471773B1/en active Active
- 2007-01-25 MX MX2008009512A patent/MX2008009512A/es active IP Right Grant
- 2007-01-25 EP EP11188840.0A patent/EP2471774B1/en not_active Not-in-force
- 2007-01-25 AU AU2007212236A patent/AU2007212236B2/en not_active Ceased
- 2007-01-25 KR KR1020087020904A patent/KR101348491B1/ko not_active IP Right Cessation
- 2007-01-25 NZ NZ570036A patent/NZ570036A/en not_active IP Right Cessation
- 2007-01-25 EA EA200801757A patent/EA019192B1/ru not_active IP Right Cessation
- 2007-01-25 JP JP2008552563A patent/JP5124481B2/ja not_active Expired - Fee Related
- 2007-01-25 WO PCT/US2007/061012 patent/WO2007092681A2/en active Application Filing
- 2007-01-25 PE PE2007000089A patent/PE20071236A1/es not_active Application Discontinuation
- 2007-01-25 EP EP07763650A patent/EP2049486A2/en not_active Withdrawn
- 2007-01-25 BR BRPI0707307-0A patent/BRPI0707307A2/pt not_active IP Right Cessation
- 2007-01-26 TW TW096103072A patent/TWI424993B/zh not_active IP Right Cessation
- 2007-01-29 AR ARP070100372A patent/AR059229A1/es not_active Application Discontinuation
-
2008
- 2008-07-22 IL IL192976A patent/IL192976A/en not_active IP Right Cessation
- 2008-07-31 NO NO20083359A patent/NO20083359L/no not_active Application Discontinuation
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2009
- 2009-07-20 US US12/505,724 patent/US7985861B2/en active Active
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2011
- 2011-06-08 US US13/155,460 patent/US20110245226A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
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JP2009526764A (ja) | 2009-07-23 |
JP5124481B2 (ja) | 2013-01-23 |
CA2651987A1 (en) | 2007-08-16 |
US20110245226A1 (en) | 2011-10-06 |
US7601844B2 (en) | 2009-10-13 |
EP2471773A1 (en) | 2012-07-04 |
WO2007092681A3 (en) | 2009-03-12 |
AU2007212236B2 (en) | 2012-05-24 |
KR101348491B1 (ko) | 2014-01-06 |
US7985861B2 (en) | 2011-07-26 |
EP2471773B1 (en) | 2016-03-23 |
TW200738660A (en) | 2007-10-16 |
PE20071236A1 (es) | 2007-12-14 |
KR20080095890A (ko) | 2008-10-29 |
NZ570036A (en) | 2011-06-30 |
WO2007092681A2 (en) | 2007-08-16 |
MX2008009512A (es) | 2009-02-26 |
EP2471774B1 (en) | 2016-08-24 |
EP2471774A1 (en) | 2012-07-04 |
AU2007212236A1 (en) | 2007-08-16 |
BRPI0707307A2 (pt) | 2011-05-03 |
US20090298833A1 (en) | 2009-12-03 |
IL192976A (en) | 2015-05-31 |
TWI424993B (zh) | 2014-02-01 |
EP2049486A2 (en) | 2009-04-22 |
EA019192B1 (ru) | 2014-01-30 |
NO20083359L (no) | 2008-10-15 |
EA200801757A1 (ru) | 2009-08-28 |
US20070208056A1 (en) | 2007-09-06 |
CA2651987C (en) | 2014-09-23 |
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