AR069525A1 - Derivados de isoxazolo- piridazina - Google Patents
Derivados de isoxazolo- piridazinaInfo
- Publication number
- AR069525A1 AR069525A1 ARP080105244A ARP080105244A AR069525A1 AR 069525 A1 AR069525 A1 AR 069525A1 AR P080105244 A ARP080105244 A AR P080105244A AR P080105244 A ARP080105244 A AR P080105244A AR 069525 A1 AR069525 A1 AR 069525A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- hydroxy
- halogen
- heterocyclyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente se refiere a compuestos de la formula (1) en la que X es O o NH; R1 es fenilo, piridinilo, o pirimidinilo, cada uno de ellos está opcionalmente sustituido por 1, 2 o 3 halogenos, R2 es alquilo C1-4, H o haloalquilo C1-4, R3, R4 y R5 con independencia entre si son: H, alquilo C1-7, opcionalmente sustituido por uno o más halogeno, ciano o hidroxi, alcoxi C1-7 opcionalmente sustituido por uno o más halogenos, CN, halogeno, NO2, -C(O)-Ra en el que Ra es hidroxi, alcoxi C1-7; alquilo C1-7, fenoxi o fenilo, NRbRc, en el que Rb y Rc con independencia entre si son: hidrogeno, alquilo C1-7, -C(O)-alquilo C1-7, opcionalmente sustituido por uno o más halogenos, -C(O)(CH2)m-O-alquilo C1-7, en el que m es el numero 0, 1, 2, 3, 4, 5 o 6, -C(O)C(O)O-alquilo C1-7, -C(O)CH2C(O)O-alquilo C1-7, -C(O)Ri, dicho Ri es fenilo o heteroarilo de 5 o 6 eslabones, cada uno de ellos está opcionalmente sustituido por uno o más E, -C(O)-cicloalquilo C3-7, opcionalmente sustituido por uno o más B, -C(O)-Rii, dicho Rii es heterociclilo de 3 a 7 eslabones, opcionalmente sustituido por uno o más A, heterociclilo de 3 a 7 eslabones, opcionalmente sustituido por uno o más A, heteroarilo de 5 o 6 eslabones, opcionalmente sustituido por uno o más E, -C(O)-NRdRe, en el que Rd y Re con independencia entre sí son: H, alquilo C1-7, opcionalmente sustituido por uno o más halogeno, hidroxi, o ciano, -(CH2)t-cicloalquilo C3-7, opcionalmente sustituido por uno o más B y t es el numero 0, 1, 2, 3 o 4, -(CH2)u-O-alquilo C1-7, en el que u es el numero 2, 3, 4, 5 o 6, -(CH2)x-heterociclilo, en el que x es el numero 0, 1, 2, 3 o 4, y dicho heterociclilo está opcionalmente sustituido por uno o más A; Rd y Re junto con el nitrogeno al que están unidos forman un resto heterociclilo opcionalmente sustituido por uno o más A, o R3 junto con el átomo de nitrogeno contiguo de la piridazina forma un anillo aromático fusionado de 5 eslabones con otros dos átomos de nitrogeno del anillo, el anillo fusionado está opcionalmente sustituido por Rf, dicho Rf es alquilo C1-7, -C(O)O-alquilo C1-7, -C(O)-alquilo C1-7, heteroarilo de 5 o 6 eslabones o fenilo, cada uno de ellos está opcionalmente sustituido por uno o más E, A es hidroxi, oxo, alquilo C1-7, alcoxi C1-7, haloalquilo C1-7, hidroxialquilo C1-7, halogeno o CN, B es halogeno, hidroxi, CN, alquilo C1-4 o haloalquilo C1-4, E es halogeno, CN, NO2, hidroxi, alquilo C1-7, alcoxi C1-7, haloalquilo C1-7, hidroxialquilo C1-7, ciano-alquilo C1-7, haloalcoxi C1-7, o cicloalquilo C3-7, o una sal farmacéuticamente aceptable de los mismos que tienen afinidad y selectividad para con l sitio de fijacion del receptor de GABA A alfa5 a su obtencion, medicamentos que contienen los compuestos y al uso de los mismos para preparar medicamentos. Los compuestos activos de la presente son utiles como mejoradores cognitivos o para el tratamiento de trastornos cognitivos, por ejemplo la enfermedad de Alzheimer.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07122293 | 2007-12-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR069525A1 true AR069525A1 (es) | 2010-01-27 |
Family
ID=40328910
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080105244A AR069525A1 (es) | 2007-12-04 | 2008-12-02 | Derivados de isoxazolo- piridazina |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7943619B2 (es) |
| EP (1) | EP2231651B1 (es) |
| JP (1) | JP5301558B2 (es) |
| KR (1) | KR101175855B1 (es) |
| CN (1) | CN101868458B (es) |
| AR (1) | AR069525A1 (es) |
| AU (1) | AU2008333327B2 (es) |
| BR (1) | BRPI0820113A2 (es) |
| CA (1) | CA2707821C (es) |
| CL (1) | CL2008003593A1 (es) |
| IL (1) | IL205753A0 (es) |
| MX (1) | MX2010006182A (es) |
| PE (1) | PE20091446A1 (es) |
| TW (1) | TW200924775A (es) |
| WO (1) | WO2009071477A1 (es) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
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| PL2767536T3 (pl) | 2007-12-04 | 2016-01-29 | Hoffmann La Roche | Pochodne izoksazolo-pirydyny |
| JP2012506386A (ja) * | 2008-10-21 | 2012-03-15 | メタボレックス， インコーポレイテッド | アリールｇｐｒ１２０受容体アゴニストおよびその使用 |
| US8227461B2 (en) * | 2009-04-30 | 2012-07-24 | Hoffmann-La Roche Inc. | Isoxazoles |
| CA2759598C (en) * | 2009-05-05 | 2017-09-12 | F. Hoffmann-La Roche Ag | Isoxazole-thiazole derivatives as gaba a receptor inverse agonists for use in the treatment of cognitive disorders |
| BRPI1013844A2 (pt) * | 2009-05-05 | 2016-04-12 | Hoffmann La Roche | derivados de piridina-isoxazol |
| CA2760746C (en) * | 2009-05-05 | 2017-07-11 | F. Hoffmann-La Roche Ag | Isoxazole-pyrazole derivatives |
| CA2760597C (en) * | 2009-05-05 | 2017-08-22 | F. Hoffmann-La Roche Ag | Isoxazole-pyridazine derivatives |
| AR081331A1 (es) | 2010-04-23 | 2012-08-08 | Cytokinetics Inc | Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos |
| AR081626A1 (es) * | 2010-04-23 | 2012-10-10 | Cytokinetics Inc | Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos |
| EP2560488B1 (en) | 2010-04-23 | 2015-10-28 | Cytokinetics, Inc. | Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use |
| EP2638035B1 (en) * | 2010-11-09 | 2014-12-17 | F.Hoffmann-La Roche Ag | Triazole derivatives as ligands for Gaba receptors |
| MX346185B (es) * | 2010-11-15 | 2017-03-10 | Agenebio Inc | Derivados de piridazina, composiciones y metodos para tratar deterioro cognitivo. |
| WO2013045519A1 (en) | 2011-09-27 | 2013-04-04 | Genfit | Derivatives of 6-substituted triazolopyridazines as rev-erb agonists |
| US8604062B2 (en) | 2011-10-20 | 2013-12-10 | Hoffman-La Roche Inc. | Process for the preparation of isoxazolyl-methoxy nicotinic acids |
| US9273011B2 (en) * | 2011-10-28 | 2016-03-01 | Inhibitaxin Limited | Substituted pyridazines for the treatment of pain |
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| WO2014001279A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| WO2014001281A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| WO2014001280A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| WO2014001278A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| JP6223443B2 (ja) | 2012-06-26 | 2017-11-01 | サニオナ・エイピイエス | フェニルトリアゾール誘導体及びｇａｂａａ受容体複合体を調節するための該フェニルトリアゾール誘導体の使用 |
| US10329301B2 (en) | 2013-12-20 | 2019-06-25 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| US10815242B2 (en) | 2015-06-19 | 2020-10-27 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| CN107344939A (zh) * | 2016-05-06 | 2017-11-14 | 如东赛默罗生物科技有限公司 | 咪唑[2,1-a]酞嗪类衍生物、其制备方法、药物组合物和用途 |
| JP7084405B2 (ja) * | 2016-12-08 | 2022-06-14 | エフ．ホフマン－ラ ロシュ アーゲー | Ｇａｂａ ａ ａｌｐｈａ５ ｐａｍとしての新規イソキサゾリルエーテル誘導体 |
| US11505555B2 (en) | 2016-12-19 | 2022-11-22 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| WO2019238633A1 (en) | 2018-06-13 | 2019-12-19 | F. Hoffmann-La Roche Ag | New isoxazolyl ether derivatives as gaba a alpha5 pam |
| WO2019246300A1 (en) | 2018-06-19 | 2019-12-26 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| BR102019014802A2 (pt) * | 2018-07-20 | 2020-02-04 | Boehringer Ingelheim Int | difluorometil-fenil triazóis |
| HU231223B1 (hu) | 2018-09-28 | 2022-01-28 | Richter Gedeon Nyrt. | GABAA A5 receptor modulátor hatású biciklusos vegyületek |
| CN112979655A (zh) * | 2019-12-16 | 2021-06-18 | 上海赛默罗生物科技有限公司 | ***并哒嗪类衍生物、其制备方法、药物组合物和用途 |
| US20240043418A1 (en) | 2020-03-26 | 2024-02-08 | Richter Gedeon Nyrt. | 1,3-dihydro-2h-pyrrolo[3,4-c]pyridine derivatives as gabaa a5 receptor modulators |
| TW202202495A (zh) | 2020-03-26 | 2022-01-16 | 匈牙利商羅特格登公司 | 作為ｇａｍｍａ－胺基丁酸Ａ受體次單元ａｌｐｈａ ５受體調節劑之㖠啶及吡啶并〔３，４－ｃ〕嗒𠯤衍生物 |
| WO2022234271A1 (en) | 2021-05-05 | 2022-11-10 | University College Cardiff Consultants Limited | Heteroaryl compounds useful in the treatment of cognitive disorders |
| HUP2100338A1 (hu) | 2021-09-29 | 2023-04-28 | Richter Gedeon Nyrt | GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok |
| CN116854680A (zh) * | 2022-03-28 | 2023-10-10 | 上海赛默罗生物科技有限公司 | 异噁唑-杂环类衍生物、药物组合物和用途 |
| WO2024088928A1 (en) * | 2022-10-25 | 2024-05-02 | F. Hoffmann-La Roche Ag | Process for manufacturing alogabat |
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| DE3525205A1 (de) * | 1984-09-11 | 1986-03-20 | Hoechst Ag, 6230 Frankfurt | Pflanzenschuetzende mittel auf basis von 1,2,4-triazolderivaten sowie neue derivate des 1,2,4-triazols |
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| WO2001034603A2 (en) | 1999-11-12 | 2001-05-17 | Neurogen Corporation | Bicyclic and tricyclic heteroaromatic compounds |
| PA8535601A1 (es) | 2000-12-21 | 2002-11-28 | Pfizer | Derivados benzimidazol y piridilimidazol como ligandos para gabaa |
| GB0108475D0 (en) | 2001-04-04 | 2001-05-23 | Merck Sharp & Dohme | New compounds |
| WO2003004027A1 (en) | 2001-07-05 | 2003-01-16 | Synaptic Pharmaceutical Corporation | Substituted anilinic piperidines as mch selective antagonists |
| EP1285914B1 (en) | 2001-08-13 | 2007-12-19 | PheneX Pharmaceuticals AG | Nr1h4 nuclear receptor binding compounds |
| EP1448561B1 (en) | 2001-11-20 | 2008-02-20 | Eli Lilly And Company | Beta 3 adrenergic agonists |
| GB0128160D0 (en) * | 2001-11-23 | 2002-01-16 | Merck Sharp & Dohme | Novel compounds |
| US7319109B2 (en) | 2002-11-22 | 2008-01-15 | Smith Kline Beecham Corporation | Farnesoid X receptor agonists |
| GB0318447D0 (en) | 2003-08-05 | 2003-09-10 | Merck Sharp & Dohme | Therapeutic agents |
| RU2408589C2 (ru) * | 2004-05-14 | 2011-01-10 | Айрм Ллк | Соединения и композиции в качестве модуляторов ppar-рецепторов, активируемых пролифератором пероксисом |
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| EP1812427A4 (en) | 2004-10-15 | 2009-10-14 | Scripps Research Inst | FATTY ACID AMIDE HYDROLASE OXADIAZOLE KETONE INHIBITORS |
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| EP1899299B1 (en) * | 2005-06-27 | 2010-10-20 | Bristol-Myers Squibb Company | C-linked cyclic antagonists of p2y1 receptor useful in the treatment of thrombotic conditions |
| DE502006008095D1 (de) | 2005-07-20 | 2010-11-25 | Prospective Concepts Ag | Pneumatisch verstellbare seitenwangen für fahrzeugsitze |
| CA2623043A1 (en) | 2005-09-19 | 2007-04-12 | F. Hoffman-La Roche Ag | Isoxazolo derivatives as gaba a alpha5 inverse agonists |
| WO2007052843A1 (ja) | 2005-11-04 | 2007-05-10 | Takeda Pharmaceutical Company Limited | 複素環アミド化合物およびその用途 |
| JP5081161B2 (ja) | 2005-12-19 | 2012-11-21 | スミスクライン ビーチャム コーポレーション | ファルネソイドｘ受容体アゴニスト |
| JP2007230909A (ja) | 2006-03-01 | 2007-09-13 | Univ Of Tokyo | 置換イソキサゾール誘導体 |
| EP1894928A1 (en) | 2006-08-29 | 2008-03-05 | PheneX Pharmaceuticals AG | Heterocyclic fxr binding compounds |
| EP1894924A1 (en) | 2006-08-29 | 2008-03-05 | Phenex Pharmaceuticals AG | Heterocyclic FXR binding compounds |
| WO2008130951A1 (en) * | 2007-04-17 | 2008-10-30 | Bristol-Myers Squibb Company | Fused heterocyclic 11-beta-hydroxysteroid dehydrogenase type i inhibitors |
-
2008
- 2008-11-25 US US12/277,331 patent/US7943619B2/en active Active
- 2008-11-26 CA CA2707821A patent/CA2707821C/en not_active Expired - Fee Related
- 2008-11-26 BR BRPI0820113 patent/BRPI0820113A2/pt not_active Application Discontinuation
- 2008-11-26 MX MX2010006182A patent/MX2010006182A/es active IP Right Grant
- 2008-11-26 KR KR1020107011907A patent/KR101175855B1/ko not_active IP Right Cessation
- 2008-11-26 AU AU2008333327A patent/AU2008333327B2/en not_active Expired - Fee Related
- 2008-11-26 WO PCT/EP2008/066226 patent/WO2009071477A1/en active Application Filing
- 2008-11-26 JP JP2010536410A patent/JP5301558B2/ja not_active Expired - Fee Related
- 2008-11-26 EP EP08855943.0A patent/EP2231651B1/en active Active
- 2008-11-26 CN CN2008801172173A patent/CN101868458B/zh active Active
- 2008-12-01 TW TW097146621A patent/TW200924775A/zh unknown
- 2008-12-02 AR ARP080105244A patent/AR069525A1/es unknown
- 2008-12-02 CL CL2008003593A patent/CL2008003593A1/es unknown
- 2008-12-02 PE PE2008002009A patent/PE20091446A1/es not_active Application Discontinuation
-
2010
- 2010-05-13 IL IL205753A patent/IL205753A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2008333327B2 (en) | 2012-12-06 |
| MX2010006182A (es) | 2010-07-01 |
| AU2008333327A1 (en) | 2009-06-11 |
| BRPI0820113A2 (pt) | 2015-05-05 |
| CA2707821C (en) | 2016-06-07 |
| PE20091446A1 (es) | 2009-09-24 |
| KR20100074320A (ko) | 2010-07-01 |
| JP2011505402A (ja) | 2011-02-24 |
| KR101175855B1 (ko) | 2012-08-24 |
| CN101868458A (zh) | 2010-10-20 |
| US7943619B2 (en) | 2011-05-17 |
| US20090143385A1 (en) | 2009-06-04 |
| EP2231651B1 (en) | 2018-11-21 |
| JP5301558B2 (ja) | 2013-09-25 |
| CL2008003593A1 (es) | 2010-01-04 |
| EP2231651A1 (en) | 2010-09-29 |
| IL205753A0 (en) | 2010-11-30 |
| TW200924775A (en) | 2009-06-16 |
| CA2707821A1 (en) | 2009-06-11 |
| WO2009071477A1 (en) | 2009-06-11 |
| CN101868458B (zh) | 2012-11-28 |
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