AR067075A1 - Derivados de isoxasol - imidazol - Google Patents
Derivados de isoxasol - imidazolInfo
- Publication number
- AR067075A1 AR067075A1 ARP080102628A ARP080102628A AR067075A1 AR 067075 A1 AR067075 A1 AR 067075A1 AR P080102628 A ARP080102628 A AR P080102628A AR P080102628 A ARP080102628 A AR P080102628A AR 067075 A1 AR067075 A1 AR 067075A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- halo
- hydroxy
- membered
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000005843 halogen group Chemical group 0.000 abstract 5
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000004043 oxo group Chemical group O=* 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 239000002475 cognitive enhancer Substances 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229940079865 intestinal antiinfectives imidazole derivative Drugs 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Chemical group 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P25/28—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
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)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente se refiere a derivados de isoxazol-imidazol que poseen una afinidad y selectividad para el sitio de union del receptor de GASA A alfa5, con su elaboracion, composiciones farmacéuticas que las contienen y su uso como medicamentos. Los compuestos activos de la presente son utiles como potenciadores cognitivos o para el tratamiento de trastornos cognitivos como la enfermedad de Alzheimer. Reivindicacion 1: Compuesto de formula 1 en el que R1 y R2 son cada uno independientemente hidrogeno, halogeno, o haloalcoxi C1-7; R3 es fenilo o heteroarilo de 6 miembros, que está opcionalmente sustituido por uno o más halogeno, alquilo C1-7, opcionalmente sustituido con halo, hidroxi o ciano, alcoxi C1-7, -S(O)m-alquilo C1-7, en el que m es 0, 1 o 2, ciano, nitro, -C(O)Ra, en el que Ra es alquilo C1-7, alcoxi C1-7, hidroxi, -(CH2)n-cicloalquilo C3-7, -(CH2)n-(heterocicloalquilo de 3 a 7 miembros), opcionalmente sustituido por aiquilo C1-4, halo, hidroxi, u oxo, -O(CH2)n-cicloalquilo C3-7, -NC(O)alquilo C1-7, -NC(O)O-alquilo C1-7, -C(O)NRbRc, en el que Rb y Rc son independientemente hidrogeno, alquilo C1-7, -(CH2)p-heterocicloalquilo de 3 a 7 miembros), opcionalmente sustituido por alquilo C1-4, halo, hidroxi, u oxo, -(CH2)p-(heteroarilo de 5 o 6 miembros) o -(CH2)r-fenilo, cada uno opcionalmente sustituido por halo, alquilo C1-4, haloalquilo C1-7, alcoxi C1-7, ciano o nitro, -(CH2)q-cicloalquilo C3-7, haloalquilo C1-7, alquinilo C1-7, o Rb y Rc junto con el nitrogeno al que están unidos forman un heterocicloalquilo de 5 o 7 miembros, que contiene opcionalmente un heteroátomo adicional en el anillo seleccionados de entre nitrogeno, oxígeno o azufre, en el que el heterocicloalquilo de 5 o 7 miembros está opcionalmente sustituido por uno o más alquilo C1-4, halo, hidroxi, u oxo; n es 0, 1, 2, 3 o 4; p es 0, 1, 2, 3 o 4; q es 0, 1, 2, 3 o 4; r es 0, 1, 2, 3 o 4; o una sal farmacéuticamente aceptable de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07110846 | 2007-06-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR067075A1 true AR067075A1 (es) | 2009-09-30 |
Family
ID=39735035
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080102628A AR067075A1 (es) | 2007-06-22 | 2008-06-20 | Derivados de isoxasol - imidazol |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US7851469B2 (es) |
| EP (1) | EP2170873B1 (es) |
| JP (1) | JP5416103B2 (es) |
| KR (1) | KR101228194B1 (es) |
| CN (1) | CN101965344B (es) |
| AR (1) | AR067075A1 (es) |
| AT (1) | ATE519760T1 (es) |
| AU (1) | AU2008267894B2 (es) |
| BR (1) | BRPI0814718A2 (es) |
| CA (1) | CA2690975A1 (es) |
| CL (1) | CL2008001820A1 (es) |
| ES (1) | ES2369805T3 (es) |
| IL (1) | IL202667A0 (es) |
| MX (1) | MX2009014001A (es) |
| PE (1) | PE20090839A1 (es) |
| TW (1) | TW200911795A (es) |
| WO (1) | WO2009000662A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112013001237A2 (pt) | 2010-07-19 | 2016-05-17 | Syngenta Participations Ag | compostos de isoxazola, isoatiazola, furano e tiofeno como microbicidas |
| US20130210836A1 (en) | 2010-07-19 | 2013-08-15 | Syngenta Crop Protection Llc | Microbicides |
| US8466181B2 (en) * | 2010-12-10 | 2013-06-18 | Hoffmann-La Roche Inc. | 1,2,3-triazole-imidazole compounds |
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| WO2014001280A1 (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 |
| WO2014001279A1 (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 |
| KR20150033678A (ko) | 2012-06-26 | 2015-04-01 | 사니오나 에이피에스 | 페닐 트리아졸 유도체 및 이의 gabaa 수용체 복합체 조절용 용도 |
| US20210084900A1 (en) | 2017-05-04 | 2021-03-25 | Basf Se | Substituted 5-(haloalkyl)-5-hydroxy-isoxazoles for Combating Phytopathogenic Fungi |
| BR102019014802A2 (pt) | 2018-07-20 | 2020-02-04 | Boehringer Ingelheim Int | difluorometil-fenil triazóis |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| GB9808663D0 (en) | 1998-04-23 | 1998-06-24 | Merck Sharp & Dohme | Therapeutic agents |
| US6660753B2 (en) | 1999-08-19 | 2003-12-09 | Nps Pharmaceuticals, Inc. | Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
| IT1314191B1 (it) | 1999-10-18 | 2002-12-06 | Recordati Chem Pharm | Derivati isossazolcarbossamidici |
| 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 |
| EA005934B1 (ru) | 2001-07-05 | 2005-08-25 | Х. Лундбекк А/С | Замещённые анилиновые пиперидины в качестве селективных антагонистов мсн |
| 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 |
| WO2004022555A1 (en) | 2002-09-06 | 2004-03-18 | Vertex Pharmaceuticals Incorporated | Isoxazoles and their use in the treatment of ischemic diseases |
| ES2887054T3 (es) * | 2003-04-11 | 2021-12-21 | Ptc Therapeutics Inc | Compuesto de ácido 1,2,4-oxadiazol benzoico y su uso para la supresión sin sentido y el tratamiento de enfermedades |
| GB0318447D0 (en) | 2003-08-05 | 2003-09-10 | Merck Sharp & Dohme | Therapeutic agents |
| EP1756086B1 (en) | 2004-06-01 | 2008-06-04 | F.Hoffmann-La Roche Ag | Pyridin-4-yl-ethynyl-imidazoles and pyrazoles as mglu5 receptor antagonists |
| EP1773807A2 (en) | 2004-06-14 | 2007-04-18 | Takeda San Diego, Inc. | Kinase inhibitors |
| US7351724B2 (en) | 2004-10-15 | 2008-04-01 | The Scripps Research Institute | Oxadiazole ketone inhibitors of fatty acid amide hydrolase |
| US20070060589A1 (en) | 2004-12-21 | 2007-03-15 | Purandare Ashok V | Inhibitors of protein arginine methyl transferases |
| EP1832584B1 (en) * | 2004-12-28 | 2011-12-21 | ASKA Pharmaceutical Co., Ltd. | Pyrimidinylisoxazole derivative |
| ATE537171T1 (de) * | 2005-12-27 | 2011-12-15 | Hoffmann La Roche | Aryl-isoxazol-4-yl-imidazoä1,5-aüpyridin-deriva e |
| CN101351461B (zh) * | 2005-12-27 | 2011-09-07 | 弗·哈夫曼-拉罗切有限公司 | 芳基-异*唑-4-基-咪唑衍生物 |
| RU2426732C2 (ru) * | 2006-01-17 | 2011-08-20 | Ф. Хоффманн-Ля Рош Аг | АРИЛ-ИЗОКСАЗОЛ-4-ИЛ-ИМИДАЗО[1,2-a]ПИРИДИН, ПРИГОДНЫЙ ДЛЯ ЛЕЧЕНИЯ БОЛЕЗНИ АЛЬЦГЕЙМЕРА ЧЕРЕЗ ПОСРЕДСТВО GABA-РЕЦЕПТОРОВ |
-
2008
- 2008-06-12 JP JP2010512649A patent/JP5416103B2/ja not_active Expired - Fee Related
- 2008-06-12 MX MX2009014001A patent/MX2009014001A/es active IP Right Grant
- 2008-06-12 KR KR1020107001422A patent/KR101228194B1/ko not_active Expired - Fee Related
- 2008-06-12 EP EP08760925A patent/EP2170873B1/en not_active Not-in-force
- 2008-06-12 CN CN2008800239424A patent/CN101965344B/zh not_active Expired - Fee Related
- 2008-06-12 AT AT08760925T patent/ATE519760T1/de active
- 2008-06-12 BR BRPI0814718-3A2A patent/BRPI0814718A2/pt not_active IP Right Cessation
- 2008-06-12 ES ES08760925T patent/ES2369805T3/es active Active
- 2008-06-12 AU AU2008267894A patent/AU2008267894B2/en not_active Ceased
- 2008-06-12 WO PCT/EP2008/057384 patent/WO2009000662A1/en not_active Ceased
- 2008-06-12 CA CA2690975A patent/CA2690975A1/en not_active Abandoned
- 2008-06-16 US US12/139,535 patent/US7851469B2/en not_active Expired - Fee Related
- 2008-06-19 CL CL2008001820A patent/CL2008001820A1/es unknown
- 2008-06-19 TW TW097122892A patent/TW200911795A/zh unknown
- 2008-06-20 AR ARP080102628A patent/AR067075A1/es unknown
- 2008-06-20 PE PE2008001060A patent/PE20090839A1/es not_active Application Discontinuation
-
2009
- 2009-12-10 IL IL202667A patent/IL202667A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CL2008001820A1 (es) | 2009-05-29 |
| WO2009000662A1 (en) | 2008-12-31 |
| BRPI0814718A2 (pt) | 2015-02-24 |
| AU2008267894A1 (en) | 2008-12-31 |
| IL202667A0 (en) | 2010-06-30 |
| CN101965344B (zh) | 2013-03-06 |
| PE20090839A1 (es) | 2009-07-02 |
| CN101965344A (zh) | 2011-02-02 |
| ATE519760T1 (de) | 2011-08-15 |
| KR101228194B1 (ko) | 2013-01-30 |
| TW200911795A (en) | 2009-03-16 |
| JP5416103B2 (ja) | 2014-02-12 |
| MX2009014001A (es) | 2010-01-28 |
| CA2690975A1 (en) | 2008-12-31 |
| ES2369805T3 (es) | 2011-12-07 |
| JP2010530862A (ja) | 2010-09-16 |
| EP2170873A1 (en) | 2010-04-07 |
| EP2170873B1 (en) | 2011-08-10 |
| US20090005370A1 (en) | 2009-01-01 |
| US7851469B2 (en) | 2010-12-14 |
| KR20100023042A (ko) | 2010-03-03 |
| AU2008267894B2 (en) | 2012-08-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |