AR083933A1 - Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak - Google Patents
Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jakInfo
- Publication number
- AR083933A1 AR083933A1 ARP110104324A ARP110104324A AR083933A1 AR 083933 A1 AR083933 A1 AR 083933A1 AR P110104324 A ARP110104324 A AR P110104324A AR P110104324 A ARP110104324 A AR P110104324A AR 083933 A1 AR083933 A1 AR 083933A1
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- alkyl
- cycloalkyl
- heterocycloalkyl
- heteroaryl
- aryl
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Abstract
Composiciones y métodos de uso que modulan la actividad de Janus quinasas (JAKs) y son de utilidad en el tratamiento de enfermedades relacionadas con la actividad de JAKs que incluyen, por ejemplo, trastornos inflamatorios, trastornos autoinmunes, cáncer y otras enfermedades.Reivindicación 1: Un compuesto de la fórmula (1), o una de sus sales farmacéuticamente aceptables; en donde: X es CH o N; Y es H, ciano, halo, alquilo C1-3 o haloalquilo C1-3; Z es CR4 o N; W es CH o N; cuando W es CH, entonces L es O, S, C(R6)2, C(=O), C(=O)N(R7), C(=O)O, C(=O)C(R6)2, S(=O), S(=O)2, S(O)N(R7), S(=O)2N(R7) o C(=NR7a)N(R7); o cuando W es N, entonces L es C(R6)2, C(=O), C(=O)O, C(=O)N(R7), C(=O)C(R6)2, S(=O), S(=O)2, S(=O)N(R7), S(=O)2N(R7) o C(=NR7a)N(R7); R1, R2, R3 y R4 son cada uno, de modo independiente, H, hidroxi, halo, alquilo C1-3 o haloalquilo C1-3; cada R5 es, de modo independiente, hidroxi, alcoxi C1-4, flúor, alquilo C1-4, hidroxi-alquilo C1-4, alcoxi C1-4-alquilo C1-4 o fluoroalquilo C1-4; cada R6 es, de modo independiente, H o alquilo C1-4; o dos grupos R6, junto con el átomo de carbono al que están unidos, forman un alquilo cicloalquilo de 3, 4, 5 ó 6 miembros; R7 es H o alquilo C1-4; R7a es H, OH, CN, alcoxi C1-4 o alquilo C1-4; o R y R7a, tomados junto con el resto C(=N)N al que están unidos, forman un anillo heterocicloalquilo de 4, 5, 6 ó 7 miembros o un anillo heteroarilo de 5 ó 6 miembros; A es H, alquilo C1-6, cicloalquilo C3-10, heterocicloalquilo C2-10, arilo C6-10 o heteroarilo C1-10; en donde dicho alquilo C1-6, cicloalquilo C3-10, heterocicloalquilo C2-10, arilo C6-10 y heteroarilo C1-10 están cada uno opcionalmente sustituidos con p sustituyentes R8 seleccionados de modo independiente; en donde p es 1, 2, 3, 4 ó 5; siempre que, cuando L es O, S, C(=O), C(=O)O, S(=O) o S(=O)2, entonces A no es H; cada R8 está seleccionado, de modo independiente, de halo, ciano, nitro, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10-alquilo C1-4, arilo C6-10, aril C6-10-alquilo C1-4, heteroarilo C1-10, heteroaril C1-10-alquilo C1-4, -ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NReRf, -C(=O)Rb, -C(=O)ORa, -C(=O)NReRf, -OC(=O)Rb, -OC(=O)NReRf, -NReRf, -NRcC(=O)Rd, -NRcC(=O)ORd, -NRcC(=O)NRd, -NRcS(=O)2Rd y -NRcS(=O)2NReRf; en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10-alquilo C1-4, arilo C6-10, aril C6-10-alquilo C1-4, heteroarilo C1-10 y heteroaril C1-10-alquilo C1-4 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos seleccionados de modo independiente; cada Ra, Rc, Rd, Re y Rf está seleccionado, de modo independiente, de H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10-alquilo C1-4, arilo C6-10, aril C6-10-alquilo C1-4, heteroarilo C1-10 y heteroaril C1-10-alquilo C1-4; en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10-alquilo C1-4, arilo C6-10, aril C6-10-alquilo C1-4, heteroarilo C1-10 y heteroaril C1-10-alquilo C1-4 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos seleccionados de modo independiente; cada Rb está seleccionado, de modo independiente, de alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10-alquilo C1-4, arilo C6-10, aril C6-10-alquilo C1-4, heteroarilo C1-10 y heteroaril C1-10-alquilo C1-4; en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10-alquilo C1-4, arilo C6-10, aril C6-10-alquilo C1-4, heteroarilo C1-10 y heteroaril C1-10-alquilo C1-4 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos Rg seleccionados de modo independiente; cada Rg está seleccionado, de modo independiente, de halo, ciano, nitro, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7, heteroaril C1-7-alquilo C1-3, -ORa1, -SRa1, -S(=O)Rb1, -S(=O)2Rb1, -NRc1S(=O)2Rd1 y -NRc1S(=O)2NRe1Rf1; en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7 y heteroaril C1-7-alquilo C1-3 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos seleccionados de modo independiente; cada Ra1, Rc1, Rd1, Re1 y Rf1 está seleccionado, de modo independiente, de H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7 y heteroaril C1-7-alquilo C1-3; en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7 y heteroaril C1-7-alquilo C1-3 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos Rh seleccionados de modo independiente; cada Rb1 está seleccionado, de modo independiente, de alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7 y heteroaril C1-7-alquilo C1-3; en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7 y heteroaril C1-7-alquilo C1-3 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos Rh seleccionados de modo independiente; cada Rh está seleccionado, de modo independiente, de ciano, halo, hidroxi, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquil C1-4-amino, dialquil C1-4-amino, hidroxi-alquilo C1-4, alcoxi C1-4-alquilo C1-4, ciano-alquilo C1-4, tio, alquil C1-6-tio, alquil C1-6-sulfinilo, alquil C1-6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6-carbonilo, alcoxi C1-6-carbonilo, alquil C1-6-carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di-(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di-(alquil C1-6)aminocarbonilamino; m es 0, 1 ó 2; y n es 0, 1, 2, 3 ó 4.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US41570510P | 2010-11-19 | 2010-11-19 |
Publications (1)
Publication Number | Publication Date |
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AR083933A1 true AR083933A1 (es) | 2013-04-10 |
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MX344478B (es) | 2016-12-16 |
AU2011329734A1 (en) | 2013-05-02 |
PE20140146A1 (es) | 2014-02-06 |
JP2014500260A (ja) | 2014-01-09 |
SG190839A1 (en) | 2013-07-31 |
US20120149681A1 (en) | 2012-06-14 |
CA2818542A1 (en) | 2012-05-24 |
CN103415515A (zh) | 2013-11-27 |
WO2012068450A1 (en) | 2012-05-24 |
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US8933085B2 (en) | 2015-01-13 |
NZ611151A (en) | 2015-06-26 |
US20190135813A1 (en) | 2019-05-09 |
JP5917545B2 (ja) | 2016-05-18 |
TW201249845A (en) | 2012-12-16 |
CN103415515B (zh) | 2015-08-26 |
US20150087632A1 (en) | 2015-03-26 |
ECSP13012703A (es) | 2013-08-30 |
CL2013001412A1 (es) | 2013-12-20 |
KR20140019300A (ko) | 2014-02-14 |
US10640506B2 (en) | 2020-05-05 |
EP2640723A1 (en) | 2013-09-25 |
IL226407A (en) | 2017-04-30 |
CR20130280A (es) | 2013-08-09 |
BR112013012502A2 (pt) | 2019-03-06 |
IL226407A0 (en) | 2013-07-31 |
EA201390736A1 (ru) | 2013-11-29 |
CO6761386A2 (es) | 2013-09-30 |
MX2013005603A (es) | 2013-06-13 |
EA026201B1 (ru) | 2017-03-31 |
UA113156C2 (xx) | 2016-12-26 |
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