NO20082747L - Arylisoksazol-4-yl-imidazolderivater - Google Patents
Arylisoksazol-4-yl-imidazolderivaterInfo
- Publication number
- NO20082747L NO20082747L NO20082747A NO20082747A NO20082747L NO 20082747 L NO20082747 L NO 20082747L NO 20082747 A NO20082747 A NO 20082747A NO 20082747 A NO20082747 A NO 20082747A NO 20082747 L NO20082747 L NO 20082747L
- Authority
- NO
- Norway
- Prior art keywords
- lower alkyl
- halogen
- aryl
- substituted
- optionally substituted
- Prior art date
Links
- QLMNERAESCRARF-UHFFFAOYSA-N 4-(1h-imidazol-2-yl)-1,2-oxazole Chemical class C1=CNC(C2=CON=C2)=N1 QLMNERAESCRARF-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 15
- 229910052736 halogen Inorganic materials 0.000 abstract 9
- 150000002367 halogens Chemical class 0.000 abstract 9
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 239000002475 cognitive enhancer Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 229960003692 gamma aminobutyric acid Drugs 0.000 abstract 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 229940079865 intestinal antiinfectives imidazole derivative Drugs 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group 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
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Foreliggende oppfinnelse angår aryl-isoksazol-4-yl-imidazolderivater med formel (I): hvor R1 til R3 hver, uavhengig, er hydrogen eller halogen; R4 er hydrogen, lavere alkyl, cykloalkyl, -(CH2)n-O-lavere alkyl eller lavere alkyl substituert med hydroksy; R5 er -(CH2)m-aryl eller -(CH2)m-heteroaryl som eventuelt er substituert med én eller flere substituenter valgt fra gruppen bestående av: halogen, cyano, nitro, lavere alkyl, lavere alkoksy, lavere alkylsulfanyl, lavere alkyl substituert med halogen, -C(O)-lavere alkyl, -C(O)-O-lavere alkyl, -NH-C(O)-O-lavere alkyl eller -C(O)-NH-R', hvor R' er lavere alkynyl eller lavere alkyl substituert med halogen, eller er -(CH2)n-cykloalkyl, -(CH2)n-heterocyklyl, -(CH2)n-heteroaryl eller -(CH2)n-aryl, eventuelt substituert med halogen; R6 er hydrogen, -C(O)H, -(CH2)n-O-lavere alkyl, -C(O)O-lavere alkyl, lavere alkyl substituert med hydroksy eller halogen, eller er cykloalkyl, aryl, eller er -(CH2)n-O-CH2-aryl, eventuelt substituert med halogen eller lavere alkyl, eller er -(CH2)n-O-CH2-heteroaryl, eventuelt substituert med halogen, lavere alkyl eller lavere alkyl substituert med halogen, eller er -(CH2)n-NH-(CH2)o-heterocyklyl; n er 0, 1, 2 eller 3; m er 0 eller 1; o er 1, 2 eller 3; så vel som farmasøytisk akseptable syreaddisjonssalter derav. Det er funnet at denne klasse av forbindelser viser høy affinitet til, og selektivitet overfor, GABA A ?5-reseptor-bindingsseter, og kan være anvendelig som kognitiv forbedrer eller for behandling av kognitive lidelser som Alzheimers sykdom.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05113011 | 2005-12-27 | ||
| PCT/EP2006/069722 WO2007074078A2 (en) | 2005-12-27 | 2006-12-14 | Aryl-isoxazol-4-yl-imidazole derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NO20082747L true NO20082747L (no) | 2008-09-22 |
Family
ID=38218337
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20082747A NO20082747L (no) | 2005-12-27 | 2008-06-13 | Arylisoksazol-4-yl-imidazolderivater |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US7414061B2 (no) |
| EP (1) | EP1968973B1 (no) |
| JP (1) | JP2009521516A (no) |
| KR (1) | KR101121372B1 (no) |
| CN (1) | CN101351461B (no) |
| AR (1) | AR058760A1 (no) |
| AT (1) | ATE527255T1 (no) |
| AU (1) | AU2006331437B2 (no) |
| BR (1) | BRPI0620773A2 (no) |
| CA (1) | CA2633367A1 (no) |
| DK (1) | DK1968973T3 (no) |
| ES (1) | ES2371935T3 (no) |
| IL (1) | IL192235A0 (no) |
| NO (1) | NO20082747L (no) |
| PL (1) | PL1968973T3 (no) |
| PT (1) | PT1968973E (no) |
| RU (1) | RU2425045C2 (no) |
| TW (1) | TWI324998B (no) |
| WO (1) | WO2007074078A2 (no) |
| ZA (1) | ZA200805353B (no) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2090570B1 (en) | 2006-09-05 | 2011-11-09 | Kyowa Hakko Kirin Co., Ltd. | Imidazole derivative |
| ES2369805T3 (es) * | 2007-06-22 | 2011-12-07 | F. Hoffmann-La Roche Ag | Derivados de isoxazol-imidazol. |
| KR20120102117A (ko) | 2007-12-04 | 2012-09-17 | 에프. 호프만-라 로슈 아게 | 아이속사졸로-피리딘 유도체 |
| TW201033201A (en) * | 2009-02-19 | 2010-09-16 | Hoffmann La Roche | Isoxazole-isoxazole and isoxazole-isothiazole derivatives |
| 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 |
| WO2014001278A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| WO2014001279A1 (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 |
| JP6224097B2 (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 |
| WO2014001280A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| CN104703981B (zh) * | 2012-10-01 | 2017-03-29 | 霍夫曼-拉罗奇有限公司 | 作为cns活性药剂的苯并咪唑类化合物 |
| BR102019014802A2 (pt) | 2018-07-20 | 2020-02-04 | Boehringer Ingelheim Int | difluorometil-fenil triazóis |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4112451A1 (de) * | 1991-04-12 | 1992-10-15 | Schering Ag | Isoxazolylimidazolderivate, verfahren zu deren herstellung und deren verwendung in arzneimitteln |
| DE69902754T2 (de) * | 1998-02-09 | 2003-08-07 | 3-Dimensional Pharmaceuticals, Inc. | Heteroaryl-amidinen,-methylamidinen und -guanidinen als protease inhibitoren, insbesondere als urokinase inhibitoren |
| IT1314191B1 (it) | 1999-10-18 | 2002-12-06 | Recordati Chem Pharm | Derivati isossazolcarbossamidici |
| 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 |
| GB0128160D0 (en) * | 2001-11-23 | 2002-01-16 | Merck Sharp & Dohme | Novel compounds |
| JP2006502168A (ja) * | 2002-09-06 | 2006-01-19 | バーテックス ファーマシューティカルズ インコーポレイテッド | イソオキサゾールおよびその使用 |
| US20080153869A1 (en) | 2004-06-14 | 2008-06-26 | Bressi Jerome C | Kinase Inhibitors |
| JP5015172B2 (ja) * | 2005-12-23 | 2012-08-29 | エフ．ホフマン−ラ ロシュ アーゲー | アリール−イソオキサゾロ−４−イル−オキサジアゾール誘導体 |
| CA2633536A1 (en) * | 2005-12-27 | 2007-07-05 | F. Hoffmann-La Roche Ag | Aryl-isoxazol-4-yl-imidazo[1, 5-a]pyridine derivatives |
-
2006
- 2006-12-14 PT PT06841367T patent/PT1968973E/pt unknown
- 2006-12-14 ES ES06841367T patent/ES2371935T3/es active Active
- 2006-12-14 DK DK06841367.3T patent/DK1968973T3/da active
- 2006-12-14 AT AT06841367T patent/ATE527255T1/de active
- 2006-12-14 BR BRPI0620773-1A patent/BRPI0620773A2/pt not_active IP Right Cessation
- 2006-12-14 EP EP06841367A patent/EP1968973B1/en not_active Not-in-force
- 2006-12-14 WO PCT/EP2006/069722 patent/WO2007074078A2/en not_active Ceased
- 2006-12-14 CA CA002633367A patent/CA2633367A1/en not_active Abandoned
- 2006-12-14 CN CN2006800496053A patent/CN101351461B/zh not_active Expired - Fee Related
- 2006-12-14 KR KR1020087018343A patent/KR101121372B1/ko not_active Expired - Fee Related
- 2006-12-14 RU RU2008125039/04A patent/RU2425045C2/ru not_active IP Right Cessation
- 2006-12-14 JP JP2008547937A patent/JP2009521516A/ja active Pending
- 2006-12-14 PL PL06841367T patent/PL1968973T3/pl unknown
- 2006-12-14 AU AU2006331437A patent/AU2006331437B2/en not_active Ceased
- 2006-12-18 US US11/640,622 patent/US7414061B2/en not_active Expired - Fee Related
- 2006-12-25 TW TW095148810A patent/TWI324998B/zh active
- 2006-12-27 AR ARP060105809A patent/AR058760A1/es unknown
-
2008
- 2008-06-13 NO NO20082747A patent/NO20082747L/no not_active Application Discontinuation
- 2008-06-16 IL IL192235A patent/IL192235A0/en unknown
- 2008-06-19 ZA ZA200805353A patent/ZA200805353B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR101121372B1 (ko) | 2012-04-12 |
| RU2008125039A (ru) | 2010-02-10 |
| ES2371935T3 (es) | 2012-01-11 |
| RU2425045C2 (ru) | 2011-07-27 |
| AU2006331437A1 (en) | 2007-07-05 |
| JP2009521516A (ja) | 2009-06-04 |
| IL192235A0 (en) | 2009-02-11 |
| TWI324998B (en) | 2010-05-21 |
| EP1968973A2 (en) | 2008-09-17 |
| CA2633367A1 (en) | 2007-07-05 |
| US7414061B2 (en) | 2008-08-19 |
| ZA200805353B (en) | 2009-10-28 |
| PT1968973E (pt) | 2011-12-09 |
| WO2007074078A3 (en) | 2008-01-17 |
| EP1968973B1 (en) | 2011-10-05 |
| ATE527255T1 (de) | 2011-10-15 |
| CN101351461A (zh) | 2009-01-21 |
| DK1968973T3 (da) | 2011-10-31 |
| AR058760A1 (es) | 2008-02-20 |
| BRPI0620773A2 (pt) | 2011-11-22 |
| AU2006331437B2 (en) | 2012-07-05 |
| CN101351461B (zh) | 2011-09-07 |
| PL1968973T3 (pl) | 2012-03-30 |
| US20070161654A1 (en) | 2007-07-12 |
| WO2007074078A2 (en) | 2007-07-05 |
| TW200736251A (en) | 2007-10-01 |
| KR20080080229A (ko) | 2008-09-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC2A | Withdrawal, rejection or dismissal of laid open patent application |