AR074771A1 - Derivados de imidazol biciclicos sustituidos como moduladores de gamma secretasa - Google Patents
Derivados de imidazol biciclicos sustituidos como moduladores de gamma secretasaInfo
- Publication number
- AR074771A1 AR074771A1 ARP090104939A ARP090104939A AR074771A1 AR 074771 A1 AR074771 A1 AR 074771A1 AR P090104939 A ARP090104939 A AR P090104939A AR P090104939 A ARP090104939 A AR P090104939A AR 074771 A1 AR074771 A1 AR 074771A1
- Authority
- AR
- Argentina
- Prior art keywords
- halo
- alkyl
- alkyloxy
- substituents
- independently selected
- Prior art date
Links
Classifications
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- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61P25/14—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
- C07D455/02—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing not further condensed quinolizine ring systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La solicitud también se refiere a composiciones farmacéuticas que comprenden dichos nuevos compuestos como ingredientes activos, así como al uso de dichos compuestos como medicamentos. Reivindicación 1: Un compuesto de fórmula (1) o una forma estereoisomérica de dicho compuesto, en donde R0 es hidrógeno, halo o alquilo C1-4; R1 es hidrógeno, alquilo C1-4 o halo; X es CR7 o N; en donde R7 es hidrógeno o halo; A1 es CR2 o N; A2 es CR o N; A3 y A4, cada uno independientemente, son CH o N; con la condición de que no más de dos de A1, A2, A3 y A4 sean N; R2 es hidrógeno, halo o alquiloxi C1-4; R8 es hidrógeno o halo; R3 es hidrógeno; alquilo C1-6 opcionalmente sustituido con uno o varios sustituyentes, cada uno seleccionado independientemente del grupo que consiste en hidroxilo, halo, morfolinilo, piperidinilo, pirrolidinilo, tetrahidropiranilo, Ar, alquiloxi C1-6, cicloalquiloxi C3-7 y cicloalquilo C3-7; carboxilo; alquenilo C2-4; NR5R6-carbonilo; cicloalquilo C3-7; Ar; tetrahidropiranilo; alquilcarbonilo C1-6; alquiloxicarbonilo C1-6; o Ar-O-CH2-; en donde cada Ar es independientemente fenilo opcionalmente sustituido con uno o vados sustituyentes, cada uno seleccionado independientemente del grupo que consiste en halo, alquiloxi C1-4, ciano, NR5R6, morfolinilo, alquilo C1-4 y alquilo C1-4 sustituido con uno o varios sustituyentes, cada uno seleccionado independientemente del grupo que consiste en halo, alquiloxi C1-4 y NR5R6; bencimidazolilo opcionalmente sustituido con uno o varios sustituyentes, cada uno independientemente seleccionado de alquilo C1-4; o piridinilo opcionalmente sustituido con uno o varios sustituyentes, cada uno seleccionado independientemente del grupo que consiste en halo, alquiloxi C1-4, ciano, alquilo C1-4 y alquilo C1-4 sustituido con uno o varios sustituyentes, cada uno independientemente seleccionado de halo; cada R5 es independientemente hidrógeno, alquilo C1-4, alquilcarbonilo C1-6 o alquiloxi C1-4(CH2CH2O)n-CH2-carbonilo; n es un número entero seleccionado de 1, 2, 3, 4, 5 o 6; cada R6 es independientemente hidrógeno o alquilo C1-4; R4 es hidrógeno; ciano; halo; fenilo opcionalmente sustituido con uno o varios sustituyentes, cada uno seleccionado independientemente del grupo que consiste en halo y fenilo; fenilcarbonilo opcionalmente sustituido con uno o varios sustituyentes, cada uno independientemente seleccionado de halo; alquiloxi C1-4; aIquilo C1-6 opcionalmente sustituido con uno o varios sustituyentes, cada uno seleccionado independientemente del grupo que consiste en halo, NR5R6, alquiloxi C1-4, hidroxilo y formilamino; Y1 es CH o N; Y2 es CR9 o N; Y3 es CH o N; con la condición de que sólo uno de Y1, Y2 y Y3 represente N; R9 es hidrógeno; halo; alquiloxi C1-4; ciano; cicloalquilo C3-7; tetrahidropiranilo; alquenilo C2-4; fenilo opcionalmente sustituido con uno o varios sustituyentes, cada uno independientemente seleccionado de alquiloxi C1-4; o aIquilo C1-4 opcionalmente sustituido con uno o vados sustituyentes, cada uno seleccionado independientemente del grupo que consiste en halo y alquiloxi C1-4; o una sal de adición farmacéuticamente aceptable o un solvato de dicho compuesto.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08172202 | 2008-12-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074771A1 true AR074771A1 (es) | 2011-02-09 |
Family
ID=40451180
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104939A AR074771A1 (es) | 2008-12-18 | 2009-12-17 | Derivados de imidazol biciclicos sustituidos como moduladores de gamma secretasa |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8546440B2 (es) |
| EP (1) | EP2379552B1 (es) |
| JP (2) | JP2012512831A (es) |
| KR (1) | KR20110102455A (es) |
| CN (1) | CN102256974B (es) |
| AP (1) | AP2011005692A0 (es) |
| AR (1) | AR074771A1 (es) |
| AU (1) | AU2009327103B2 (es) |
| BR (1) | BRPI0922664A2 (es) |
| CA (1) | CA2742914A1 (es) |
| EA (1) | EA018625B1 (es) |
| ES (1) | ES2460642T3 (es) |
| IL (1) | IL213563A (es) |
| MX (1) | MX2011006543A (es) |
| NZ (1) | NZ594036A (es) |
| PA (1) | PA8854101A1 (es) |
| SG (1) | SG172213A1 (es) |
| TW (1) | TWI438203B (es) |
| UA (1) | UA104151C2 (es) |
| WO (1) | WO2010070008A1 (es) |
| ZA (1) | ZA201104504B (es) |
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| KR20110113197A (ko) | 2009-02-06 | 2011-10-14 | 오르토-맥닐-얀센 파마슈티칼스 인코포레이티드 | 감마 세크레타제 조절제로서의 신규 치환된 비사이클릭 헤테로사이클릭 화합물 |
| TWI461425B (zh) | 2009-02-19 | 2014-11-21 | Janssen Pharmaceuticals Inc | 作為伽瑪分泌酶調節劑之新穎經取代的苯并唑、苯并咪唑、唑并吡啶及咪唑并吡啶衍生物類 |
| EP2427453B1 (en) | 2009-05-07 | 2013-07-17 | Janssen Pharmaceuticals, Inc. | Substituted indazole and aza-indazole derivatives as gamma secretase modulators |
| TWI598347B (zh) | 2009-07-13 | 2017-09-11 | 基利科學股份有限公司 | 調節細胞凋亡信號之激酶的抑制劑 |
| CN102482227A (zh) | 2009-07-15 | 2012-05-30 | 杨森制药公司 | 作为γ分泌酶调节剂的取代的三唑和咪唑衍生物 |
| BR112012017442A2 (pt) | 2010-01-15 | 2016-04-19 | Janssen Pharmaceuticals Inc | derivados de triazol bicíclicos substituídos como moduladores de gamma secretase |
| ES2539257T3 (es) | 2010-07-28 | 2015-06-29 | Bayer Intellectual Property Gmbh | Imidazo[1,2-b]piridazinas sustituidas |
| AU2012230348A1 (en) | 2011-03-24 | 2013-08-29 | Cellzome Limited | Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators |
| CA2830027C (en) | 2011-03-31 | 2016-04-26 | Pfizer Inc. | Novel bicyclic pyridinones |
| US20140255392A1 (en) | 2011-04-06 | 2014-09-11 | Bayer Intellectual Property Gmbh | Substituted imidazopyridines and intermediates thereof |
| EP2694510B1 (en) | 2011-04-07 | 2015-10-14 | Bayer Intellectual Property GmbH | Imidazopyridazines as akt kinase inhibitors |
| CN103874702B (zh) | 2011-07-15 | 2015-12-09 | 杨森制药公司 | 作为γ分泌酶调节剂的经取代的吲哚衍生物 |
| AU2012325909B2 (en) | 2011-10-20 | 2016-06-09 | Glaxosmithkline Llc | Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators |
| KR20140077965A (ko) | 2011-10-20 | 2014-06-24 | 글락소스미스클라인 엘엘씨 | 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체 |
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| UA110688C2 (uk) | 2012-09-21 | 2016-01-25 | Пфайзер Інк. | Біциклічні піридинони |
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| 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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2009
- 2009-12-15 PA PA20098854101A patent/PA8854101A1/es unknown
- 2009-12-16 WO PCT/EP2009/067321 patent/WO2010070008A1/en active Application Filing
- 2009-12-16 MX MX2011006543A patent/MX2011006543A/es active IP Right Grant
- 2009-12-16 SG SG2011044310A patent/SG172213A1/en unknown
- 2009-12-16 US US13/133,027 patent/US8546440B2/en active Active
- 2009-12-16 CA CA2742914A patent/CA2742914A1/en not_active Abandoned
- 2009-12-16 BR BRPI0922664A patent/BRPI0922664A2/pt not_active IP Right Cessation
- 2009-12-16 ES ES09797025.5T patent/ES2460642T3/es active Active
- 2009-12-16 AU AU2009327103A patent/AU2009327103B2/en not_active Ceased
- 2009-12-16 KR KR1020117016065A patent/KR20110102455A/ko not_active Application Discontinuation
- 2009-12-16 JP JP2011541412A patent/JP2012512831A/ja active Pending
- 2009-12-16 UA UAA201105485A patent/UA104151C2/ru unknown
- 2009-12-16 EA EA201170829A patent/EA018625B1/ru not_active IP Right Cessation
- 2009-12-16 CN CN200980151827.XA patent/CN102256974B/zh active Active
- 2009-12-16 EP EP09797025.5A patent/EP2379552B1/en active Active
- 2009-12-16 AP AP2011005692A patent/AP2011005692A0/xx unknown
- 2009-12-16 NZ NZ594036A patent/NZ594036A/xx not_active IP Right Cessation
- 2009-12-17 TW TW098143263A patent/TWI438203B/zh not_active IP Right Cessation
- 2009-12-17 AR ARP090104939A patent/AR074771A1/es not_active Application Discontinuation
-
2011
- 2011-06-15 IL IL213563A patent/IL213563A/en not_active IP Right Cessation
- 2011-06-17 ZA ZA2011/04504A patent/ZA201104504B/en unknown
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2015
- 2015-06-25 JP JP2015127609A patent/JP2015164969A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| AU2009327103B2 (en) | 2014-12-04 |
| ES2460642T3 (es) | 2014-05-14 |
| NZ594036A (en) | 2012-10-26 |
| IL213563A0 (en) | 2011-07-31 |
| TW201035093A (en) | 2010-10-01 |
| EP2379552A1 (en) | 2011-10-26 |
| EP2379552B1 (en) | 2014-02-26 |
| JP2012512831A (ja) | 2012-06-07 |
| AP2011005692A0 (en) | 2011-06-30 |
| UA104151C2 (ru) | 2014-01-10 |
| CN102256974B (zh) | 2014-07-30 |
| EA201170829A1 (ru) | 2011-12-30 |
| US8546440B2 (en) | 2013-10-01 |
| PA8854101A1 (es) | 2010-07-27 |
| MX2011006543A (es) | 2011-07-20 |
| AU2009327103A1 (en) | 2011-07-21 |
| TWI438203B (zh) | 2014-05-21 |
| KR20110102455A (ko) | 2011-09-16 |
| SG172213A1 (en) | 2011-07-28 |
| CA2742914A1 (en) | 2010-06-24 |
| BRPI0922664A2 (pt) | 2016-01-05 |
| IL213563A (en) | 2015-06-30 |
| EA018625B1 (ru) | 2013-09-30 |
| US20110237580A1 (en) | 2011-09-29 |
| WO2010070008A1 (en) | 2010-06-24 |
| ZA201104504B (en) | 2014-01-29 |
| CN102256974A (zh) | 2011-11-23 |
| JP2015164969A (ja) | 2015-09-17 |
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