PE20091466A1 - Derivados de 4,5-dihidro-oxazol-2-il-amina - Google Patents
Derivados de 4,5-dihidro-oxazol-2-il-aminaInfo
- Publication number
- PE20091466A1 PE20091466A1 PE2009000228A PE2009000228A PE20091466A1 PE 20091466 A1 PE20091466 A1 PE 20091466A1 PE 2009000228 A PE2009000228 A PE 2009000228A PE 2009000228 A PE2009000228 A PE 2009000228A PE 20091466 A1 PE20091466 A1 PE 20091466A1
- Authority
- PE
- Peru
- Prior art keywords
- dihydro
- oxazole
- ilamine
- biphenyl
- phenyl
- Prior art date
Links
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 4-METHOXY-3-METHYL-PHENYL Chemical class 0.000 abstract 2
- 101710150192 Beta-secretase 1 Proteins 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 1
- AKQZEFRALAUBFS-UHFFFAOYSA-N ilamine Natural products COC(C)C(O)(C(=O)OCC1=CCN2CCCC12)C(C)(C)O AKQZEFRALAUBFS-UHFFFAOYSA-N 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- GPKUICFDWYEPTK-UHFFFAOYSA-N methoxycyclohexatriene Chemical class COC1=CC=C=C[CH]1 GPKUICFDWYEPTK-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D263/28—Nitrogen atoms not forming part of a nitro radical
-
- 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
- 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
- C07D413/10—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 carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Psychiatry (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (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
SE REFIERE A COMPUESTOS DERIVADOS DE 4,5-DIHIDRO-OXAZOL-2-IL-AMINA DE FORMULA (I) DONDE R1 Y R1' SON CADA UNO H, HALOGENO, ALCOXI INFERIOR, ENTRE OTROS; R2 ES H, HALOGENO, CN, ALCOXI INFERIOR, ENTRE OTROS; R3 ES H, CN, ALQUILO INFERIOR, ENTRE OTROS; R4 ES H O ALQUILO INFERIOR; X ES UN ENLACE, -NH-C(O)-, -NH- O -O-CH2; Ar ES ARILO O HETEROARILO; m ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: (RS)-4-(3'-CLORO-BIFENIL-3-IL)-4-(4-METOXI-FENIL)-4,5-DIHIDRO-OXAZOL-2-ILAMINA, (RS)-4-(6-FLUOR-3'-METOXI-BIFENIL-3-IL)-4-(4-METOXI-3-METIL-FENIL)-4,5-DIHIDRO-OXAZOL-2-ILAMINA, (RS)-4-(4-DIFLUORMETOXI-3-METIL-FENIL)-4-(2'-FLUOR-5'-METOXI-BIFENIL-3-IL)-4,5-DIHIDRO-OXAZOL-2-ILAMINA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ASP2 (B-SECRETASA, BACE 1 O MEMAPSINA-2) SIENDO UTILES PARA EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08151546 | 2008-02-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20091466A1 true PE20091466A1 (es) | 2009-09-24 |
Family
ID=40545768
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2009000228A PE20091466A1 (es) | 2008-02-18 | 2009-02-16 | Derivados de 4,5-dihidro-oxazol-2-il-amina |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US7989449B2 (es) |
| EP (1) | EP2245019B1 (es) |
| JP (1) | JP5258904B2 (es) |
| KR (1) | KR101259240B1 (es) |
| CN (1) | CN101952260B (es) |
| AR (1) | AR070395A1 (es) |
| AU (1) | AU2009216825A1 (es) |
| BR (1) | BRPI0907563A2 (es) |
| CA (1) | CA2712228C (es) |
| CL (1) | CL2009000349A1 (es) |
| ES (1) | ES2398017T3 (es) |
| IL (1) | IL206765A0 (es) |
| MX (1) | MX2010008347A (es) |
| PE (1) | PE20091466A1 (es) |
| TW (1) | TW200938537A (es) |
| WO (1) | WO2009103626A1 (es) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7700603B2 (en) * | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) * | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP1896032B1 (en) | 2005-06-14 | 2012-10-31 | Merck Sharp & Dohme Corp. | The preparation and use of compounds as protease inhibitors |
| EP1896478B1 (en) * | 2005-06-14 | 2014-05-21 | Merck Sharp & Dohme Corp. | Aspartyl protease inhibitors |
| ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| AU2007258435A1 (en) | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| EP2689780A1 (en) | 2007-04-24 | 2014-01-29 | Shionogi & Co., Ltd. | Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group |
| AU2009239536C1 (en) * | 2008-04-22 | 2012-12-13 | Merck Sharp & Dohme Corp. | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| EP2305672B1 (en) | 2008-06-13 | 2019-03-27 | Shionogi & Co., Ltd. | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY |
| US8450308B2 (en) * | 2008-08-19 | 2013-05-28 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| BRPI0918449A2 (pt) * | 2008-09-11 | 2019-09-24 | Amgen Inc | compostos de anel espiro-tricíclico como moduladores de beta-secretas e métodos de uso |
| EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
| ES2571057T3 (es) * | 2009-03-13 | 2016-05-23 | Vitae Pharmaceuticals Inc | Inhibidores de beta-secretasa |
| US20110065695A1 (en) * | 2009-09-11 | 2011-03-17 | Jeremy Beauchamp | Use of aminodihydrothiazines for the treatment or prevention of diabetes |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| US8354441B2 (en) | 2009-11-11 | 2013-01-15 | Hoffmann-La Roche Inc. | Oxazoline derivatives |
| JPWO2011070781A1 (ja) | 2009-12-09 | 2013-04-22 | 塩野義製薬株式会社 | 置換アミノチアジン誘導体 |
| UA103272C2 (uk) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2 |
| CN102834384A (zh) | 2009-12-11 | 2012-12-19 | 盐野义制药株式会社 | *嗪衍生物 |
| JPWO2011077726A1 (ja) | 2009-12-24 | 2013-05-02 | 塩野義製薬株式会社 | 4−アミノ−1,3−チアジンまたはオキサジン誘導体 |
| JP5828848B2 (ja) | 2010-02-24 | 2015-12-09 | ヴァイティー ファーマシューティカルズ,インコーポレイテッド | ベータセクレターゼインヒビター |
| CA2791281A1 (en) | 2010-03-15 | 2011-09-22 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators |
| WO2011115928A1 (en) | 2010-03-15 | 2011-09-22 | Amgen Inc. | Amino -dihydrooxazine and amino - dihydrothiazine spiro compounds as beta - secretase modulators and their medical use |
| US8815881B2 (en) * | 2010-08-09 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds |
| JP5816630B2 (ja) | 2010-10-29 | 2015-11-18 | 塩野義製薬株式会社 | ナフチリジン誘導体 |
| WO2012057247A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
| AU2012206561B2 (en) * | 2011-01-13 | 2015-12-17 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of neurological disorders |
| US8399459B2 (en) * | 2011-02-02 | 2013-03-19 | Hoffmann-La Roche Inc. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| US9346827B2 (en) | 2011-02-07 | 2016-05-24 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use |
| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| DE102011055815A1 (de) | 2011-11-29 | 2013-05-29 | Aicuris Gmbh & Co. Kg | Carboxamid-substituierte Heteroaryl-Pyrazole und ihre Verwendung |
| TWI557112B (zh) | 2012-03-05 | 2016-11-11 | 百靈佳殷格翰國際股份有限公司 | β-分泌酶抑制劑 |
| DE102012016908A1 (de) | 2012-08-17 | 2014-02-20 | Aicuris Gmbh & Co. Kg | Tris-(Hetero)Aryl-Pyrazole und ihre Verwendung |
| TW201422592A (zh) | 2012-08-27 | 2014-06-16 | Boehringer Ingelheim Int | β-分泌酶抑制劑 |
| JP2015532282A (ja) | 2012-09-28 | 2015-11-09 | ヴァイティー ファーマシューティカルズ,インコーポレイテッド | β−セクレターゼの阻害剤 |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US9540397B2 (en) * | 2014-10-10 | 2017-01-10 | Hoffmann-La Roche Inc. | BACE1 inhibitors |
| JP6674960B2 (ja) | 2015-03-20 | 2020-04-01 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Bace1阻害剤 |
| US20190201410A1 (en) * | 2016-06-02 | 2019-07-04 | Purdue Pharma L.P. | Trace amine associated receptor 1 agonists and partial agonists for pain treatment |
| CN113729026A (zh) * | 2021-10-09 | 2021-12-03 | 合肥巨卓农业技术开发有限公司 | 一种包含啶磺草胺和异丙隆的复合除草剂 |
| TW202342013A (zh) * | 2022-02-10 | 2023-11-01 | 英屬開曼群島商百濟神州有限公司 | 雜環化合物、其組成物及用其進行治療之方法 |
| WO2024112544A1 (en) * | 2022-11-22 | 2024-05-30 | Albemarle Corporation | Liquid weighting agents for oil-based fluids |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK302185A (da) * | 1984-07-05 | 1986-01-06 | Rolland Sa A | 2-amino-oxazoliner samt fremgangsmaade til deres fremstilling |
| MXPA06014793A (es) * | 2004-06-16 | 2007-02-16 | Wyeth Corp | Derivados de amino-5, 5-difenilimidazolona para la inhibicion de ??-secretasa. |
| TW200734311A (en) * | 2005-11-21 | 2007-09-16 | Astrazeneca Ab | New compounds |
| WO2007058601A1 (en) * | 2005-11-21 | 2007-05-24 | Astrazeneca Ab | Novel 2-amino-imidazole-4-one compounds and their use in the manufacture of a medicament to be used in the treatment of cognitive impairment, alzheimer’s disease, neurodegeneration and dementia |
| CN101600700B (zh) * | 2007-02-02 | 2013-08-21 | 弗·哈夫曼-拉罗切有限公司 | 作为taar1配体用于cns病症的新的2-氨基噁唑啉 |
-
2009
- 2009-02-09 WO PCT/EP2009/051452 patent/WO2009103626A1/en not_active Ceased
- 2009-02-09 MX MX2010008347A patent/MX2010008347A/es active IP Right Grant
- 2009-02-09 AU AU2009216825A patent/AU2009216825A1/en not_active Abandoned
- 2009-02-09 CA CA2712228A patent/CA2712228C/en not_active Expired - Fee Related
- 2009-02-09 BR BRPI0907563-1A patent/BRPI0907563A2/pt not_active IP Right Cessation
- 2009-02-09 CN CN2009801052316A patent/CN101952260B/zh not_active Expired - Fee Related
- 2009-02-09 JP JP2010547144A patent/JP5258904B2/ja not_active Expired - Fee Related
- 2009-02-09 ES ES09711573T patent/ES2398017T3/es active Active
- 2009-02-09 KR KR1020107018239A patent/KR101259240B1/ko not_active Expired - Fee Related
- 2009-02-09 EP EP09711573A patent/EP2245019B1/en not_active Not-in-force
- 2009-02-12 US US12/369,782 patent/US7989449B2/en not_active Expired - Fee Related
- 2009-02-16 TW TW098104870A patent/TW200938537A/zh unknown
- 2009-02-16 CL CL2009000349A patent/CL2009000349A1/es unknown
- 2009-02-16 AR ARP090100540A patent/AR070395A1/es unknown
- 2009-02-16 PE PE2009000228A patent/PE20091466A1/es not_active Application Discontinuation
-
2010
- 2010-07-01 IL IL206765A patent/IL206765A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2712228C (en) | 2013-04-16 |
| MX2010008347A (es) | 2010-11-12 |
| IL206765A0 (en) | 2010-12-30 |
| CN101952260B (zh) | 2013-02-13 |
| AU2009216825A1 (en) | 2009-08-27 |
| EP2245019A1 (en) | 2010-11-03 |
| KR101259240B1 (ko) | 2013-04-29 |
| EP2245019B1 (en) | 2012-11-14 |
| US20090209529A1 (en) | 2009-08-20 |
| US7989449B2 (en) | 2011-08-02 |
| CA2712228A1 (en) | 2009-08-27 |
| JP5258904B2 (ja) | 2013-08-07 |
| TW200938537A (en) | 2009-09-16 |
| AR070395A1 (es) | 2010-03-31 |
| BRPI0907563A2 (pt) | 2015-08-04 |
| JP2011512378A (ja) | 2011-04-21 |
| KR20100130595A (ko) | 2010-12-13 |
| ES2398017T3 (es) | 2013-03-13 |
| CL2009000349A1 (es) | 2010-02-19 |
| CN101952260A (zh) | 2011-01-19 |
| WO2009103626A1 (en) | 2009-08-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20091466A1 (es) | Derivados de 4,5-dihidro-oxazol-2-il-amina | |
| PE20090617A1 (es) | Compuestos amino-5-[-4-(difluorometoxi)fenil]-5-fenilimidazolona para la inhibicion de -secretasa | |
| PE20061106A1 (es) | Derivados de 2-(4-oxo-4h-quinazolin-3-il)acetamida | |
| PE20100138A1 (es) | Derivados de morfolino pirimidina usados en enfermedades relacionadas en mtor quinasa y/o pi3k | |
| PE20121500A1 (es) | 2-amino-5,5-difluor-5,6-dihidro-4h-oxazinas como inhibidores de bace 1 y/o bace 2 | |
| PE20050691A1 (es) | Proceso para preparar carboxamidas 2-aminotiazol-5-aromaticas como inhibidores de la cinasa | |
| PE20121282A1 (es) | Antagonistas de espiro-oxindol de mdm2 | |
| PE20090709A1 (es) | Compuestos heterociclico de 5 miembros | |
| PE20070528A1 (es) | Compuestos heterociclicos como ligandos del receptor vaniloide del subtipo 1 | |
| PE20130242A1 (es) | Derivados de isoxazolo-piridina | |
| PE20121640A1 (es) | Derivados de pirazina como inhibidores de bace | |
| PE20090160A1 (es) | COMPUESTOS AMINO-5-[4-(DIFLUOROMETOXI)FENIL SUSTITUIDO]-5-FENILIMIDAZOLONA COMO INHIBIDORES DE ß-SECRETASA | |
| PE20141827A1 (es) | Inhibidores de proteinas quinasas | |
| PE20140171A1 (es) | Pirazoles fungicidas y sus mezclas | |
| NO20063599L (no) | Ytterligere heterosykliske forbindelser og deres anvendelse som metabotrofiske glutamatreseptorantagonister | |
| PE20120403A1 (es) | Aril-piridinas como inhibidoras de sintasa de aldosterona | |
| PE20091656A1 (es) | Compuestos heterociclicos como inhibidores de la cinasa raf | |
| PE20110875A1 (es) | Derivados de isoindol como inhibidores de bace | |
| NO20063469L (no) | Polyeheterosykliske forbindelser og deres anvendelse som metabotrofe glutamat reseptorantagonister | |
| PE20090290A1 (es) | Derivados de pirrolopiridina como inhibidores de bace | |
| PE20081845A1 (es) | Nuevos derivados de aminopirimidina como inhibidores de plk1 | |
| NO20063468L (no) | Triazolforbindelser og deres anvendelse som metabotrofe glutamatreseptorantagonister | |
| PE20120640A1 (es) | Nuevos derivados de (6-oxo-1,6-dihidro-pirimidin-2-il)-amida, su preparacion y su utilizacion farmaceutica como inhibidores de fosforilacion de akt (pkb) | |
| ATE435223T1 (de) | Pyrimidin-, chinazolin-, pteridin- und triazinderivate | |
| PE20090876A1 (es) | Nuevos derivados de 6-aril/heteroalquiloxi benzotiazol y bencimidazol, su procedimiento de preparacion, su aplicacion como medicamentos, composiciones farmaceuticas y nueva utilizacion principalmente como inhibidores de cmet |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |