AR087182A1 - DERIVADOS DE INDOL SUSTITUIDOS COMO MODULADORES DE g SECRETASA - Google Patents
DERIVADOS DE INDOL SUSTITUIDOS COMO MODULADORES DE g SECRETASAInfo
- Publication number
- AR087182A1 AR087182A1 ARP120102548A ARP120102548A AR087182A1 AR 087182 A1 AR087182 A1 AR 087182A1 AR P120102548 A ARP120102548 A AR P120102548A AR P120102548 A ARP120102548 A AR P120102548A AR 087182 A1 AR087182 A1 AR 087182A1
- Authority
- AR
- Argentina
- Prior art keywords
- hydrogen
- group
- substituents
- alkyloxy
- optionally substituted
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Los compuestos de acuerdo con la presente son moduladores de la g secretasa. Procesos para la preparación de dichos compuestos; a composiciones farmacéuticas que comprenden dichos compuestos como ingredientes activos, al igual que al uso de dichos compuestos como medicamentos.Reivindicación 1: Un compuesto de la fórmula (1), un tautómero o una forma estereoisómera de dicho compuesto, donde: R3 se selecciona del grupo que consiste en hidrógeno, alquiloxi C1-4, ciano y Het1; A1 es CR4a o N; donde R4a es hidrógeno, halo o alquiloxi C1-4 opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste en alquiloxi C1-4 y halo; A2 es CR4b o N; donde R4b es hidrógeno, halo, alquiloxi C1-4, ciano o Het2; A3 es CR4c o N; donde R4c es hidrógeno, halo o alquiloxi C1-4; siempre que el máximo de A1, A2 y A3 sea N; Het1 y Het2 representan, de manera independiente, un heteroarilo de 5 ó 6 miembros seleccionado del grupo que consiste en piridinilo, imidazolilo, oxazolilo, 1,2,4-triazolilo y pirazolilo; donde dicho heteroarilo de 5 ó 6 miembros puede estar sustituido con uno o más sustituyentes alquilo C1-4; Y es N o CRa; donde Ra es hidrógeno, halo o alquilo C1-4 opcionalmente sustituido con un hidroxilo; X es N o CH; R1 y R2 se toman juntos para formar un radical bivalente -R1-R2- que tiene la fórmula (CH2)m-Z-CH2- ó CH2-Z-(CH2)m-; m representa 2, 3 ó 4; Z representa un enlace directo, NR5 u O; donde R5 es hidrógeno, alquilcarbonilo C1-4, Ar1, (C=O)-Ar1 o alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes flúor; donde (CH2)m-Z-CH2- ó CH2-Z-(CH2)m- está sustituido en uno o más grupos CH2 con uno o dos sustituyentes seleccionados de manera independiente del grupo que consiste en Ar2, (C=O)-Ar2, O-Ar2, NR6-Ar2, alquil C1-4carbonilo, flúor, hidroxi y alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes flúor; cada Ar1 y Ar2 representa, de manera independiente, fenilo, pirazolilo o piridinilo; donde dicho fenilo, pirazolilo o piridinilo puede estar sustituido con uno o más sustituyentes seleccionados de manera independiente del grupo que consiste en halo, ciano, NR7R8, morfolinilo, cicloalquilo C3-7, alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes seleccionados de manera independiente del grupo que consiste en alquiloxi C1-4, flúor y cicloalquilo C3-7, y alquiloxi C1-4 opcionalmente sustituido con uno o más sustituyentes seleccionados de manera independiente del grupo que consiste en flúor y cicloalquilo C3-7; cada R6 es, de manera independiente, hidrógeno, o alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes seleccionados de manera independiente del grupo que consiste en flúor y cicloalquilo C3-7; cada R7 es, de manera independiente, hidrógeno, alquilo C1-4 o alquilcarbonilo C1-4; cada R8 es, de manera independiente, hidrógeno o alquilo C1-4; o una de sus sales de adición farmacéuticamente aceptables o uno de sus solvatos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11174120 | 2011-07-15 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR087182A1 true AR087182A1 (es) | 2014-02-26 |
Family
ID=46506432
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP120102548A AR087182A1 (es) | 2011-07-15 | 2012-07-13 | DERIVADOS DE INDOL SUSTITUIDOS COMO MODULADORES DE g SECRETASA |
Country Status (16)
Country | Link |
---|---|
US (1) | US9115143B2 (es) |
EP (1) | EP2731948B1 (es) |
JP (1) | JP6068464B2 (es) |
KR (1) | KR101913135B1 (es) |
CN (1) | CN103874702B (es) |
AR (1) | AR087182A1 (es) |
AU (1) | AU2012285931B2 (es) |
BR (1) | BR112014000713A2 (es) |
CA (1) | CA2841102C (es) |
EA (1) | EA023045B1 (es) |
ES (1) | ES2555167T3 (es) |
IL (1) | IL230422B (es) |
IN (1) | IN2014MN00258A (es) |
MX (1) | MX2014000626A (es) |
TW (1) | TWI567079B (es) |
WO (1) | WO2013010904A1 (es) |
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CN103502225B (zh) | 2011-03-24 | 2015-11-25 | 杨森制药公司 | 作为γ分泌酶调节剂的经取代的三唑基哌嗪以及三唑基哌啶衍生物 |
AU2012285931B2 (en) | 2011-07-15 | 2017-01-12 | Cellzome Limited | Novel substituted indole derivatives as gamma secretase modulators |
WO2013171712A1 (en) | 2012-05-16 | 2013-11-21 | Janssen Pharmaceuticals, Inc. | Substituted 3, 4 - dihydro - 2h - pyrido [1, 2 -a] pyrazine - 1, 6 - dione derivatives useful for the treatment of (inter alia) alzheimer's disease |
EP2738172A1 (en) * | 2012-11-28 | 2014-06-04 | Almirall, S.A. | New bicyclic compounds as crac channel modulators |
KR102209418B1 (ko) | 2012-12-20 | 2021-01-29 | 얀센 파마슈티카 엔.브이. | 감마 세크레타제 조절 인자로서의 신규 삼환 3,4-디하이드로-2H-피리도[1,2-α]피라진-1,6-디온 유도체 |
US10246454B2 (en) | 2013-01-17 | 2019-04-02 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators |
US10562897B2 (en) | 2014-01-16 | 2020-02-18 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators |
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-
2012
- 2012-07-12 AU AU2012285931A patent/AU2012285931B2/en not_active Ceased
- 2012-07-12 WO PCT/EP2012/063667 patent/WO2013010904A1/en active Application Filing
- 2012-07-12 KR KR1020147003465A patent/KR101913135B1/ko active IP Right Grant
- 2012-07-12 US US14/233,078 patent/US9115143B2/en not_active Expired - Fee Related
- 2012-07-12 CA CA2841102A patent/CA2841102C/en not_active Expired - Fee Related
- 2012-07-12 EP EP12733754.1A patent/EP2731948B1/en active Active
- 2012-07-12 IN IN258MUN2014 patent/IN2014MN00258A/en unknown
- 2012-07-12 JP JP2014519557A patent/JP6068464B2/ja not_active Expired - Fee Related
- 2012-07-12 ES ES12733754.1T patent/ES2555167T3/es active Active
- 2012-07-12 TW TW101125035A patent/TWI567079B/zh not_active IP Right Cessation
- 2012-07-12 BR BR112014000713A patent/BR112014000713A2/pt active Search and Examination
- 2012-07-12 CN CN201280034912.XA patent/CN103874702B/zh not_active Expired - Fee Related
- 2012-07-12 EA EA201490287A patent/EA023045B1/ru not_active IP Right Cessation
- 2012-07-12 MX MX2014000626A patent/MX2014000626A/es unknown
- 2012-07-13 AR ARP120102548A patent/AR087182A1/es not_active Application Discontinuation
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Also Published As
Publication number | Publication date |
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KR101913135B1 (ko) | 2018-10-30 |
EP2731948B1 (en) | 2015-09-09 |
CA2841102C (en) | 2019-08-13 |
WO2013010904A1 (en) | 2013-01-24 |
CA2841102A1 (en) | 2013-01-24 |
KR20140063595A (ko) | 2014-05-27 |
TWI567079B (zh) | 2017-01-21 |
US9115143B2 (en) | 2015-08-25 |
EA201490287A1 (ru) | 2014-05-30 |
BR112014000713A2 (pt) | 2017-01-10 |
IL230422B (en) | 2018-03-29 |
EP2731948A1 (en) | 2014-05-21 |
ES2555167T3 (es) | 2015-12-29 |
EA023045B1 (ru) | 2016-04-29 |
TW201315736A (zh) | 2013-04-16 |
AU2012285931B2 (en) | 2017-01-12 |
MX2014000626A (es) | 2014-04-30 |
CN103874702B (zh) | 2015-12-09 |
IN2014MN00258A (es) | 2015-09-25 |
NZ619683A (en) | 2015-01-30 |
US20140148450A1 (en) | 2014-05-29 |
JP2014518286A (ja) | 2014-07-28 |
JP6068464B2 (ja) | 2017-01-25 |
CN103874702A (zh) | 2014-06-18 |
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