AR077598A1 - Compuestos heterociclicos fusionados como modulares de canales ionicos - Google Patents
Compuestos heterociclicos fusionados como modulares de canales ionicosInfo
- Publication number
- AR077598A1 AR077598A1 ARP100102716A ARP100102716A AR077598A1 AR 077598 A1 AR077598 A1 AR 077598A1 AR P100102716 A ARP100102716 A AR P100102716A AR P100102716 A ARP100102716 A AR P100102716A AR 077598 A1 AR077598 A1 AR 077598A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- heteroaryl
- cycloalkyl
- aryl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—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
- 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
Abstract
Compuestos que son inhibidores del canal de sodio y a su uso en el tratamiento de diversos estados patologicos, incluyendo enfermedades cardiovasculares y diabetes. Uso de los compuestos y a composiciones farmacéuticas que los contienen. Reivindicacion 1: Un compuesto de la formula (1) en donde R1 es arilo o heteroarilo, en donde dicho arilo o heteroarilo están opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados, de modo independiente, del grupo que consiste en hidroxilo, halo, -NO2, CN, -SF5, -Si(CH3)3-O-CF3, -O-R20, -S-R20, -C(O)-R20, C(O)OH, -N(R20)(R22), -C(O)-N(R20)(R22), -N(R20)-C(O)-R22, -N(R20)-S(=O)2-R26, -S(=O)2- R20, -S(=O)2-N(R20)(R22), alcoxi C1-3, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo, heteroarilo y heterociclilo; en donde dicho alcoxi, alquilo, alquenilo, alquinilo, heteroarilo, cicloalquilo o heterociclilo están opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, -NO2, -O-CF3, -O-CF2, fenilo, heterociclilo, heteroarilo, cicloalquilo, -N(R20)(R22), -C(O)-R20, -C(O)-O-R20, -C(O)-N(R20)(R22), -CN y -O-R20, W1 es N o CR2 en donde R2 está seleccionado, de modo independiente, del grupo que consiste en hidrogeno, alquilo opcionalmente sustituido, amino, alcoxi opcionalmente sustituido, -CF3, -O-CF3, -CN y -N(R20)C(O)-R22; W2 es N o CR3 en donde R3 está seleccionado, de modo independiente, del grupo que consiste en hidrogeno, alquilo opcionalmente sustituido, -CF3, -halo y -O-R24; W3 es N o CR4, en donde R4 está seleccionado, de modo independiente, del grupo que consiste en hidrogeno, hidroxilo, halo, alquilo C1-4, alcoxi C1-3, -R25-N(R20)(R22), -R25-O-R20, -R25-C(O)-O-R20, -R25-C(O)-N(R20)(R22), -R25-C(O)-O-N(R20)(R22), -R25-N(R20)-C(O)-R22 y -R25-O-C(O)-N(R20)(R22), en donde dicho alquilo está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, Q está seleccionado de un enlace covalente o alquinileno C2-4; X1 es N o CRa, en donde Ra es hidrogeno, alquilo C1-15, alcoxi C1-4, -C(O)-O-R26, -C(O)-N(R26)(R28), -N(R20)-S(=O)2-R20, cicloalquilo, arilo, heteroarilo, heterociclilo, en donde dicho alquilo está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, -NO2, -O-CF3, -O-CHF2, cicloalquilo, -CN y alcoxi C1-4; y dicho alcoxi, cicloalquilo, arilo, heterociclilo o heteroarilo están opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, -NO2, -O-CF3, -O-CHF2, fenilo, heterociclilo, heteroarilo, cicloalquilo, -N(R20)(R22), -C(O)-R20, -C(O)-O-R20, -C(O)-N(R20)(R22), -CN y -O-R20;o Ra es -Y-Z-R25-R23-R20, en donde, Y es un enlace covalente o está seleccionado de alquileno C1-3 opcionalmente sustituido con uno o dos grupos alquilo C1-3 o fluor; Z es alquinileno C2-4, -O-, -S-, -NRö, -NR5'-C(O)-, -NRö-C(O)-NR5'- o -C(O)-NR3-, en donde cada Rö y R5' es, de modo independiente, hidrogeno o alquilo inferior C1-6; y en donde también dicho alquilo está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, -NO2, -O-CF3, -O-CF2, fenilo, heterociclilo, heteroarilo, cicloalquilo, -N(R20)(R22), -C(O)-R20, -C(O)-O-R20, -C(O)-N(R20)(R22), -CN y -O-R20, X2 es N o CRb; Rb está seleccionado del grupo que consiste en hidrogeno, alquilo sustituido, -CF3, -O-CF3, -O-R20, -S-R20, -N(R20)(R22), -N(R20)-C(O)-R22, -CF2-R20, -CF2-C(O)-O-R20 , -CF2-C(O)-N(R20)-S(=O)2-R26, -CF2-tetrazolilo, -C(O)-N(R20)-S(=O)2-R26, -N(R20)-C(O)-N(R20)(R22), -C(O)-R20, -C(O)-O-R20, -C(O)-N(R20)( R22) y -N(R20)-S(=O)2-R26, -R25-heteroarilo opcionalmente sustituido, -R25-arilo opcionalmente sustituido; R20 y R22 están seleccionados en cada instancia, de modo independiente, del grupo que consiste en hidrogeno, alquilo C1-15, alquenilo C2-15, alquinilo C2-15, cicloalquilo, heterociclilo, arilo y heteroarilo, en donde el alquilo, alquenilo, alquinilo, heterociclilo, arilo y heteroarilo están opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, alquilo, mono- o dialquilamino, alquilo o arilo o heteroarilamida, -NO2, -SO2R26, -CN, alcoxi C1-3, -CF3, -OCF3, arilo, cicloalquilo y heteroarilo; o cuando R20 y R22 están unidos a un átomo de nitrogeno comun R20 y R22 se pueden reunir para formar un anillo heterocíclico que entonces está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, alquilo, mono- o dialquilamino, alquilo o arilo o heteroarilamida, -NO2, -SO2R26, -CN, alcoxi C1-3, -CF3 y -OCF3, arilo, cicloalquilo; R23 es un enlace covalente o está seleccionado del grupo que consiste en cicloalquileno, heterociclileno, arileno y heteroarileno, en donde el cicloalquileno, heterociclileno, arileno y heteroarileno están opcionalmente sustituidos con uno a tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, alquilo, mono- o dialquilamino, alquilo o arilo o heteroarilamida, -NO2, -SO2R26, -CN, alcoxi C1-3, -CF3, -OCF3, arilo, cicloalquilo y heteroarilo; R24 está seleccionado en cada instancia, de modo independiente, de alquilo o arilo cualquiera de los cuales puede estar opcionalmente sustituido con 1, 2 o 3 grupos seleccionados, de modo independiente, de hidroxilo, -OCF3, halo, alcoxi C1-3, -O-R20 o alquil opcionalmente sustituido con halo, -NO2, -CF3, -O-CF3, -N(R20)(R22), -C(O)-R20, -C(O)-O-R20, -C(O)-N(R20)(R22), -CN o -O-R20; R25 es en cada instancia, de modo independiente, un enlace covalente o está seleccionado de alquileno C1-3 opcionalmente sustituido con uno o dos grupos alquilo C1-3; y R26 y R28 están seleccionados cada uno, de modo independiente, de hidrogeno, alquilo o cicloalquilo, en donde el alquilo, fenilo y cicloalquilo pueden estar sustituidos también con 1 a 3 sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, alcoxi C1-4, -CF3 y -OCF3; o una de sus sales, ésteres, profármacos o solvatos farmacéuticamente aceptables, siempre que a) cuando X1 es CRa, Ra es -Y-Z-R25-R23-R20, Y no es un enlace covalente y Z es -O-, -S-, -SO2-, -C(O)-NR3-, -NR5'-C(O)- o NRö-, entonces R25 no pueda ser un enlace; b) cuando X1 es CRa, Ra es -Y-Z-R25-R23-R20,Y es enlace covalente y Z es -O-, -S-, -SO2- o NRö-, entonces R25 sea un enlace covalente y R23 no sea cicloalquileno; c) cuando Z es -NR5'-C(O)-, entonces Y no sea un enlace covalente; d) R23 y R25 no puedan ser enlaces covalentes; e) cuando X1 es CRa, Q es un enlace, R1 es heteroarilo y W1, W2 y W3 son todos CH, entonces el heteroarilo R1 pueda luego no estar sustituido con fenilo; f) cuando W1, W2 y W3 no son N, R2 es alquilo sustituido, X1 es CRa y X2 es N, entonces Ra no sea alquilo, cicloalquilo o heterociclilo; y g) cuando Q es un enlace covalente, R1 es fenilo, W1, W2 y W3 son CH, X1 es CRa y X2 es N, entonces Ra no sea alquilo C1-3 no sustituido; h) cuando Q es un enlace covalente, W1 y W2 son CH, W3 es NH, X1 es CRa y X2 es N, entonces R1 no sea heterarilo sustituido con arilo.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22886409P | 2009-07-27 | 2009-07-27 | |
US36003710P | 2010-06-30 | 2010-06-30 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR077598A1 true AR077598A1 (es) | 2011-09-07 |
Family
ID=42751632
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100102716A AR077598A1 (es) | 2009-07-27 | 2010-07-27 | Compuestos heterociclicos fusionados como modulares de canales ionicos |
Country Status (22)
Country | Link |
---|---|
US (2) | US8952034B2 (es) |
EP (1) | EP2464645B1 (es) |
CN (1) | CN102725290B (es) |
AR (1) | AR077598A1 (es) |
AU (1) | AU2010276537B2 (es) |
CA (1) | CA2774715C (es) |
CY (1) | CY1119584T1 (es) |
DK (1) | DK2464645T3 (es) |
EA (1) | EA025824B1 (es) |
ES (1) | ES2642586T3 (es) |
HR (1) | HRP20171454T8 (es) |
HU (1) | HUE034911T2 (es) |
LT (1) | LT2464645T (es) |
ME (1) | ME02847B (es) |
NZ (1) | NZ598942A (es) |
PL (1) | PL2464645T3 (es) |
PT (1) | PT2464645T (es) |
RS (1) | RS56410B1 (es) |
SI (1) | SI2464645T1 (es) |
TW (2) | TWI490217B (es) |
UY (1) | UY32805A (es) |
WO (1) | WO2011014462A1 (es) |
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NO3175985T3 (es) | 2011-07-01 | 2018-04-28 | ||
WO2013112932A1 (en) | 2012-01-27 | 2013-08-01 | Gilead Sciences, Inc. | Combination therapies using late sodium ion channel blockers and potassium ion channel blockers |
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2010
- 2010-07-26 AU AU2010276537A patent/AU2010276537B2/en active Active
- 2010-07-26 CA CA2774715A patent/CA2774715C/en active Active
- 2010-07-26 PT PT107377244T patent/PT2464645T/pt unknown
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- 2010-07-26 EA EA201290121A patent/EA025824B1/ru unknown
- 2010-07-26 ME MEP-2017-235A patent/ME02847B/me unknown
- 2010-07-26 SI SI201031540T patent/SI2464645T1/sl unknown
- 2010-07-26 DK DK10737724.4T patent/DK2464645T3/en active
- 2010-07-26 US US12/843,702 patent/US8952034B2/en active Active
- 2010-07-26 EP EP10737724.4A patent/EP2464645B1/en active Active
- 2010-07-26 PL PL10737724T patent/PL2464645T3/pl unknown
- 2010-07-26 RS RS20170990A patent/RS56410B1/sr unknown
- 2010-07-26 LT LTEP10737724.4T patent/LT2464645T/lt unknown
- 2010-07-26 HU HUE10737724A patent/HUE034911T2/hu unknown
- 2010-07-26 WO PCT/US2010/043264 patent/WO2011014462A1/en active Application Filing
- 2010-07-26 CN CN201080043104.0A patent/CN102725290B/zh active Active
- 2010-07-26 ES ES10737724.4T patent/ES2642586T3/es active Active
- 2010-07-27 AR ARP100102716A patent/AR077598A1/es not_active Application Discontinuation
- 2010-07-27 TW TW099124710A patent/TWI490217B/zh active
- 2010-07-27 UY UY0001032805A patent/UY32805A/es not_active Application Discontinuation
- 2010-07-27 TW TW104112388A patent/TWI542587B/zh active
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2014
- 2014-05-09 US US14/274,422 patent/US9371329B2/en active Active
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2017
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Also Published As
Publication number | Publication date |
---|---|
US8952034B2 (en) | 2015-02-10 |
CA2774715A1 (en) | 2011-02-03 |
CN102725290B (zh) | 2016-03-09 |
AU2010276537B2 (en) | 2015-04-16 |
US20110021521A1 (en) | 2011-01-27 |
TWI542587B (zh) | 2016-07-21 |
NZ598942A (en) | 2014-02-28 |
RS56410B1 (sr) | 2018-01-31 |
CY1119584T1 (el) | 2018-03-07 |
AU2010276537A1 (en) | 2012-05-24 |
HRP20171454T1 (hr) | 2017-12-01 |
HUE034911T2 (hu) | 2018-03-28 |
UY32805A (es) | 2011-02-28 |
EP2464645A1 (en) | 2012-06-20 |
CA2774715C (en) | 2018-04-03 |
TW201116528A (en) | 2011-05-16 |
PT2464645T (pt) | 2017-10-11 |
EA201290121A1 (ru) | 2012-10-30 |
CN102725290A (zh) | 2012-10-10 |
US20140303158A1 (en) | 2014-10-09 |
PL2464645T3 (pl) | 2017-12-29 |
LT2464645T (lt) | 2017-10-25 |
ES2642586T3 (es) | 2017-11-16 |
TWI490217B (zh) | 2015-07-01 |
TW201542545A (zh) | 2015-11-16 |
HRP20171454T8 (hr) | 2018-01-12 |
EP2464645B1 (en) | 2017-07-05 |
EA025824B1 (ru) | 2017-02-28 |
SI2464645T1 (sl) | 2017-10-30 |
WO2011014462A1 (en) | 2011-02-03 |
DK2464645T3 (en) | 2017-10-23 |
US9371329B2 (en) | 2016-06-21 |
ME02847B (me) | 2018-01-20 |
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