AR085099A1 - Derivados de (1,2,4)triazolo[4,3-a]quinoxalina como inhibidores de fosfodiesterasas - Google Patents
Derivados de (1,2,4)triazolo[4,3-a]quinoxalina como inhibidores de fosfodiesterasasInfo
- Publication number
- AR085099A1 AR085099A1 ARP120100303A ARP120100303A AR085099A1 AR 085099 A1 AR085099 A1 AR 085099A1 AR P120100303 A ARP120100303 A AR P120100303A AR P120100303 A ARP120100303 A AR P120100303A AR 085099 A1 AR085099 A1 AR 085099A1
- Authority
- AR
- Argentina
- Prior art keywords
- triazolo
- quinoxaline
- halo
- methyl
- optionally substituted
- Prior art date
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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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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Abstract
La presente se refiere a derivados de (1,2,4)triazolo[4,3-a]quinoxalina que son inhibidores de fosfodiesterasa 2 y/o 10, útiles en el tratamiento de enfermedades del sistema nervioso central.Reivindicación 1: Un compuesto de fórmula (1) o una de sus sales aceptables desde el punto de vista farmacéutico; en donde: R1 representa -fenilo, 2-piridilo, 3-piridilo o 4-piridilo, en cada caso sustituido con un sustituyente diferente de H en una posición orto de la ligadura a la estructura de la cadena principal y en forma opcional sustituido con sustituyentes adicionales diferentes de H; R2 representa hidrógeno, alquilo C1-4, en forma opcional sustituido con hasta 2 halo, por ej., átomos de flúor; R3, R4, R5 y R6 representan, en forma independiente unos de otros hidrógeno, halógeno, alquilo C1-4, en forma opcional sustituido con hasta 5, con preferencia hasta 3 halo, por ej., átomos de flúor, y/o -O(halo)alquilo C1-2, cicloalquilo C3-8, en forma opcional sustituido con halo, -haloalquilo C1-2 y/o O(halo)alquilo C1-2, CN, OH, -O-alquilo C1-4, en forma opcional sustituido con hasta 5, con preferencia hasta 3 halo, por ej., átomos de flúor, y/o -O(halo)alquilo C1-2, cicloalquilo C3-8 en forma opcional sustituido con halo, -haloalquilo C1-2 y/o -O(halo)alquilo C1-2, -O(CH2)n-R10, en donde n puede ser 1 ó 2; R10 representa: un grupo cíclico que puede ser no sustituido o sustituido con preferencia hasta 4 veces por halógeno, alquilo C1-4, en forma opcional sustituido con hasta 5, con preferencia hasta 3 átomos de halógeno, u O-alquilo C1-4, en forma opcional sustituido con hasta 5, con preferencia hasta 3 átomos de halógeno, pero no los siguientes compuestos: 1-(2-hidroxifenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina, 1-(2-clorofenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina, 1-(2-nitrofenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina, 1-(2-metoxifenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina, 1-(5-amino-2-clorofenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina, 1-(5-amino-2-metoxifenil)-4-metil(1,2,4)triazolo[4,3-a]quinoxalina, 1-(5-amino-2-metilfenil)-4-metil-(1,2,4)triazolo[4, 3-a]quinoxalina, o 1-(2-hidroxi-3-metoxifenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US201161437848P | 2011-01-31 | 2011-01-31 |
Publications (1)
Publication Number | Publication Date |
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AR085099A1 true AR085099A1 (es) | 2013-09-11 |
Family
ID=45833359
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP120100303A AR085099A1 (es) | 2011-01-31 | 2012-01-31 | Derivados de (1,2,4)triazolo[4,3-a]quinoxalina como inhibidores de fosfodiesterasas |
Country Status (24)
Country | Link |
---|---|
US (1) | US9540379B2 (es) |
EP (1) | EP2670754B1 (es) |
JP (1) | JP6027547B2 (es) |
KR (1) | KR20140019342A (es) |
CN (1) | CN103459395A (es) |
AR (1) | AR085099A1 (es) |
AU (1) | AU2012213471B2 (es) |
BR (1) | BR112013019354A2 (es) |
CA (1) | CA2824929A1 (es) |
CL (1) | CL2013002003A1 (es) |
CO (1) | CO6811848A2 (es) |
EA (1) | EA023792B1 (es) |
EC (1) | ECSP13012824A (es) |
GE (1) | GEP20156333B (es) |
IL (1) | IL226826A (es) |
MA (1) | MA34844B1 (es) |
MX (1) | MX2013008667A (es) |
PE (1) | PE20141023A1 (es) |
SG (1) | SG192210A1 (es) |
TN (1) | TN2013000325A1 (es) |
TW (1) | TWI535718B (es) |
UA (1) | UA111963C2 (es) |
UY (1) | UY33888A (es) |
WO (1) | WO2012104293A1 (es) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
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EA027418B1 (ru) * | 2011-06-27 | 2017-07-31 | Янссен Фармацевтика Нв | ПРОИЗВОДНЫЕ 1-АРИЛ-4-МЕТИЛ[1,2,4]ТРИАЗОЛО[4,3-a]ХИНОКСАЛИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ, СПОСОБЫ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ ИХ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ |
WO2013034755A1 (en) * | 2011-09-09 | 2013-03-14 | H. Lundbeck A/S | Triazolopyrazine derivatives and their use for treating neurological and psychiatric disorders |
WO2013034758A1 (en) * | 2011-09-09 | 2013-03-14 | H. Lundbeck A/S | Substituted triazolopyrazines and uses thereof |
US9056863B2 (en) * | 2011-09-09 | 2015-06-16 | H. Lundbeck A/S | Substituted 2,3,5,9,9B-pentaazacyclopenta[a]naphthalenes and uses thereof |
RU2657540C2 (ru) | 2012-06-26 | 2018-06-14 | Янссен Фармацевтика Нв | Комбинации, содержащие ингибиторы pde 2, такие как 1-арил-4-метил-[1,2,4]триазоло[4,3-а]хиноксалиновые соединения, и ингибиторы pde 10, для применения в лечении неврологических или метаболических расстройств |
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WO2014139983A1 (en) | 2013-03-13 | 2014-09-18 | H. Lundbeck A/S | [1,2,4]triazolo[4,3-a]quinoxalines as dual pde2/pde10 inhibitors |
WO2015106032A1 (en) | 2014-01-08 | 2015-07-16 | Intra-Cellular Therapies, Inc. | Products and pharmaceutical compositions |
PL3597649T3 (pl) | 2014-04-23 | 2022-04-04 | Dart Neuroscience Llc | Kompozycje zawierające podstawione związki [1,2,4]triazolo[1,5-a]pirymidyn-7-ylowe jako inhibitory pde2 |
EP3215508A1 (en) | 2014-11-05 | 2017-09-13 | Dart NeuroScience (Cayman) Ltd. | Substituted 5-methyl-[1, 2, 4]triazolo [1,5-a) pyrimidin-2-amine compounds as pde2 inhibitors |
MX2017007377A (es) | 2014-12-06 | 2017-11-06 | Intra-Cellular Therapies Inc | Compuestos organicos. |
WO2016090380A1 (en) | 2014-12-06 | 2016-06-09 | Intra-Cellular Therapies, Inc. | Organic compounds |
EP3156405A1 (en) | 2015-10-13 | 2017-04-19 | Boehringer Ingelheim International GmbH | Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxamide |
EP3440071A1 (en) | 2016-03-21 | 2019-02-13 | Perlara PBC | Fused heterocyclic organic compounds and uses thereof |
CN106212487B (zh) * | 2016-07-28 | 2018-11-13 | 浙江工业大学 | 一种含甲氧基苯并吡嗪结构的1,2,4-三唑衍生物作为杀菌剂的应用 |
CA3083176A1 (en) | 2017-11-23 | 2019-05-31 | Oslo University Hospital Hf | Treatment of tachycardia |
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WO2009086303A2 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
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WO2010104933A1 (en) | 2009-03-11 | 2010-09-16 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
TW201111383A (en) * | 2009-05-29 | 2011-04-01 | Wyeth Llc | Substituted imidazo[1,5-a]quinoxalines as inhibitors of phosphodiesterase 10 |
EP2266985A1 (en) | 2009-06-26 | 2010-12-29 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | Tricyclic Pyrimidine Derivatives as Wnt antagonists |
WO2012096929A2 (en) | 2011-01-11 | 2012-07-19 | Sunovion Pharmaceuticals Inc. | Heteroaryl compounds and methods of use thereof |
EA027418B1 (ru) | 2011-06-27 | 2017-07-31 | Янссен Фармацевтика Нв | ПРОИЗВОДНЫЕ 1-АРИЛ-4-МЕТИЛ[1,2,4]ТРИАЗОЛО[4,3-a]ХИНОКСАЛИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ, СПОСОБЫ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ ИХ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ |
US9056863B2 (en) | 2011-09-09 | 2015-06-16 | H. Lundbeck A/S | Substituted 2,3,5,9,9B-pentaazacyclopenta[a]naphthalenes and uses thereof |
WO2013034758A1 (en) | 2011-09-09 | 2013-03-14 | H. Lundbeck A/S | Substituted triazolopyrazines and uses thereof |
RU2657540C2 (ru) | 2012-06-26 | 2018-06-14 | Янссен Фармацевтика Нв | Комбинации, содержащие ингибиторы pde 2, такие как 1-арил-4-метил-[1,2,4]триазоло[4,3-а]хиноксалиновые соединения, и ингибиторы pde 10, для применения в лечении неврологических или метаболических расстройств |
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-
2012
- 2012-01-30 US US13/361,002 patent/US9540379B2/en active Active
- 2012-01-31 MX MX2013008667A patent/MX2013008667A/es active IP Right Grant
- 2012-01-31 EA EA201300871A patent/EA023792B1/ru not_active IP Right Cessation
- 2012-01-31 CA CA2824929A patent/CA2824929A1/en not_active Abandoned
- 2012-01-31 UA UAA201310356A patent/UA111963C2/uk unknown
- 2012-01-31 WO PCT/EP2012/051546 patent/WO2012104293A1/en active Application Filing
- 2012-01-31 EP EP12708774.0A patent/EP2670754B1/en active Active
- 2012-01-31 GE GEAP201213211A patent/GEP20156333B/en unknown
- 2012-01-31 CN CN2012800157168A patent/CN103459395A/zh active Pending
- 2012-01-31 JP JP2013550908A patent/JP6027547B2/ja active Active
- 2012-01-31 KR KR1020137023101A patent/KR20140019342A/ko not_active Application Discontinuation
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- 2012-01-31 TW TW101103150A patent/TWI535718B/zh not_active IP Right Cessation
- 2012-01-31 MA MA36142A patent/MA34844B1/fr unknown
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- 2012-01-31 AU AU2012213471A patent/AU2012213471B2/en not_active Ceased
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Also Published As
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CN103459395A (zh) | 2013-12-18 |
EA023792B1 (ru) | 2016-07-29 |
US20120302564A1 (en) | 2012-11-29 |
TN2013000325A1 (en) | 2015-01-20 |
ECSP13012824A (es) | 2013-10-31 |
GEP20156333B (en) | 2015-07-27 |
CA2824929A1 (en) | 2012-08-09 |
EP2670754B1 (en) | 2017-05-24 |
WO2012104293A1 (en) | 2012-08-09 |
NZ611630A (en) | 2015-03-27 |
KR20140019342A (ko) | 2014-02-14 |
IL226826A (en) | 2016-10-31 |
UY33888A (es) | 2012-08-31 |
SG192210A1 (en) | 2013-09-30 |
PE20141023A1 (es) | 2014-09-04 |
AU2012213471B2 (en) | 2016-07-14 |
BR112013019354A2 (pt) | 2019-09-24 |
CO6811848A2 (es) | 2013-12-16 |
CL2013002003A1 (es) | 2013-12-06 |
TW201245198A (en) | 2012-11-16 |
US9540379B2 (en) | 2017-01-10 |
EA201300871A1 (ru) | 2014-01-30 |
EP2670754A1 (en) | 2013-12-11 |
MX2013008667A (es) | 2013-10-01 |
AU2012213471A1 (en) | 2013-07-04 |
JP6027547B2 (ja) | 2016-11-16 |
TWI535718B (zh) | 2016-06-01 |
MA34844B1 (fr) | 2014-01-02 |
JP2014503576A (ja) | 2014-02-13 |
UA111963C2 (uk) | 2016-07-11 |
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