AR091203A1 - Compuestos de cromano - Google Patents
Compuestos de cromanoInfo
- Publication number
- AR091203A1 AR091203A1 ARP130101885A AR091203A1 AR 091203 A1 AR091203 A1 AR 091203A1 AR P130101885 A ARP130101885 A AR P130101885A AR 091203 A1 AR091203 A1 AR 091203A1
- Authority
- AR
- Argentina
- Prior art keywords
- halogen
- substituted
- lower alkyl
- heterocyclic group
- unsubstituted
- Prior art date
Links
- VZWXIQHBIQLMPN-UHFFFAOYSA-N chromane Chemical class C1=CC=C2CCCOC2=C1 VZWXIQHBIQLMPN-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 208000010877 cognitive disease Diseases 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 208000027061 mild cognitive impairment Diseases 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000010412 Glaucoma Diseases 0.000 abstract 1
- 238000009825 accumulation Methods 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 230000007062 hydrolysis Effects 0.000 abstract 1
- 238000006460 hydrolysis reaction Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes 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
- C07D413/14—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
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/20—Spiro-condensed systems
-
- 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
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Psychiatry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Peptides Or Proteins (AREA)
Abstract
Una composición farmacéutica para prevenir o tratar enfermedades o condiciones asociadas y/o mediadas por la actividad de la b-secretasa, la hidrólisis de un sitio b-secretasa de una proteína precursora b-amiloide y/o la acumulación de proteínas b-amiloides. Se incluye una composición farmacéutica para prevenir o tratar enfermedades que incluyen, no taxativamente, glaucoma, deterioro cognitivo leve (DCL) o mal de Alzheimer, especialmente ésta última. Reivindicación 1: Un compuesto caracterizado porque es de la fórmula (1) o una sal del mismo, donde A¹ es O; A² es -C(RA²¹RA²²)-; y RA²¹ y RA²² son H; B es un grupo heterocíclico monocíclico saturado que contiene oxígeno o cicloalquilo, donde dicho cicloalquilo no está sustituido o está sustituido con halógeno; X es alquilo inferior; Y es alquilo inferior; R¹ y R⁴ son H; R³ es H o halógeno; y R² es -N(H)-C(O)-(grupo heterocíclico), donde dicho grupo heterocíclico no está sustituido o está sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halógeno, alquilo inferior que no está sustituido o está sustituido con halógeno, -CN, y -O-(alquilo inferior).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261653321P | 2012-05-30 | 2012-05-30 | |
| US201361782038P | 2013-03-14 | 2013-03-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR091203A1 true AR091203A1 (es) | 2015-01-21 |
Family
ID=49674034
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130101885 AR091203A1 (es) | 2012-05-30 | 2013-05-29 | Compuestos de cromano |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US8975415B2 (es) |
| EP (1) | EP2854797A4 (es) |
| JP (1) | JP2015518048A (es) |
| KR (1) | KR20150023536A (es) |
| CN (1) | CN104394862A (es) |
| AR (1) | AR091203A1 (es) |
| AU (1) | AU2013267555A1 (es) |
| BR (1) | BR112014029597A2 (es) |
| CA (1) | CA2873678A1 (es) |
| EA (1) | EA026380B1 (es) |
| HK (1) | HK1208817A1 (es) |
| MX (1) | MX2014014066A (es) |
| SG (1) | SG11201407796YA (es) |
| TW (1) | TW201408672A (es) |
| WO (1) | WO2013181202A2 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR091203A1 (es) | 2012-05-30 | 2015-01-21 | Astellas Pharma Inc | Compuestos de cromano |
| TW201629025A (zh) * | 2014-10-07 | 2016-08-16 | 阿斯特捷利康公司 | 化合物及其作為ｂａｃｅ抑制劑之用途 |
| CN110724135B (zh) * | 2019-11-18 | 2023-04-28 | 上海医药工业研究院有限公司 | 一种艾拉普林中间体及其制备方法 |
| CN110713483B (zh) * | 2019-11-18 | 2023-04-07 | 上海医药工业研究院 | 艾拉普林中间体及艾拉普林的制备方法 |
| CN110818694B (zh) * | 2019-11-18 | 2023-04-21 | 上海医药工业研究院有限公司 | 艾拉普林中间体及其应用 |
| CN110790753B (zh) * | 2019-11-18 | 2023-04-07 | 上海医药工业研究院 | 艾拉普林对甲苯磺酸盐、其制备方法和应用 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4484410B2 (ja) | 1999-06-28 | 2010-06-16 | オクラホマ メディカル リサーチ ファウンデーション | メマプシン２のインヒビターおよびその使用 |
| US20040121947A1 (en) | 2000-12-28 | 2004-06-24 | Oklahoma Medical Research Foundation | Compounds which inhibit beta-secretase activity and methods of use thereof |
| JP4547152B2 (ja) | 2001-10-23 | 2010-09-22 | オクラホマ メディカル リサーチ ファウンデーション | β−セクレターゼ阻害剤および使用方法 |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| MY149978A (en) | 2003-12-15 | 2013-11-15 | Merck Sharp & Dohme | Heterocyclic aspartyl protease inhibitors |
| WO2007100536A1 (en) | 2006-02-24 | 2007-09-07 | Wyeth | DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE |
| WO2010013794A1 (en) | 2008-07-28 | 2010-02-04 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| WO2010013302A1 (ja) * | 2008-07-28 | 2010-02-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | スピロアミノジヒドロチアジン誘導体 |
| JP5444240B2 (ja) * | 2008-07-28 | 2014-03-19 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | スピロアミノジヒドロチアジン誘導体 |
| US8450308B2 (en) * | 2008-08-19 | 2013-05-28 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| MY148558A (en) * | 2008-09-11 | 2013-04-30 | Amgen Inc | Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use |
| DK2406240T3 (en) * | 2009-03-13 | 2016-02-01 | Vitae Pharmaceuticals Inc | INHIBITORS OF BETA-secretase |
| US8461160B2 (en) | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
| WO2011072064A1 (en) * | 2009-12-08 | 2011-06-16 | Array Biopharma Inc. | S piro [chroman - 4, 4 ' - imidazol] ones as beta - secretase inhibitors |
| EP2539322B1 (en) * | 2010-02-24 | 2014-01-01 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| WO2011115938A1 (en) * | 2010-03-15 | 2011-09-22 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta - secretase modulators |
| JP5584352B2 (ja) * | 2010-03-15 | 2014-09-03 | アムジエン・インコーポレーテツド | β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途 |
| WO2011123674A1 (en) * | 2010-03-31 | 2011-10-06 | Array Biopharma Inc. | Compounds for treating neurodegenerative diseases |
| WO2011130741A1 (en) | 2010-04-16 | 2011-10-20 | Array Biopharma Inc. | Compounds for treating neurodegenerative diseases |
| AR083169A1 (es) | 2010-09-24 | 2013-02-06 | Array Biopharma Inc | Compuestos para tratar enfermedades neurodegenerativas |
| WO2012054510A1 (en) | 2010-10-19 | 2012-04-26 | Comentis, Inc. | Oxadiazole compounds which inhibit beta-secretase activity and methods of use thereof |
| US20120157448A1 (en) | 2010-11-22 | 2012-06-21 | Adam Cook | Compounds for treating neurodegenerative diseases |
| WO2012071279A1 (en) | 2010-11-23 | 2012-05-31 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
| US8415483B2 (en) | 2010-12-22 | 2013-04-09 | Astrazeneca Ab | Compounds and their use as BACE 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 |
| WO2012112462A1 (en) | 2011-02-15 | 2012-08-23 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use |
| US9079919B2 (en) | 2011-05-27 | 2015-07-14 | Hoffmann-La Roche Inc. | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors |
| WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| ES2566373T3 (es) | 2011-10-10 | 2016-04-12 | Astrazeneca Ab | Inhibidores monofluoro beta-secretasa |
| AR091203A1 (es) | 2012-05-30 | 2015-01-21 | Astellas Pharma Inc | Compuestos de cromano |
| EP2669286A1 (en) | 2012-05-31 | 2013-12-04 | Ares Trading S.A. | Spiro tetrahydro-benzothiophen derivatives useful for the treatment of neurodegenerative diseases |
-
2013
- 2013-05-29 AR ARP130101885 patent/AR091203A1/es unknown
- 2013-05-29 JP JP2015515133A patent/JP2015518048A/ja active Pending
- 2013-05-29 HK HK15109582.8A patent/HK1208817A1/xx unknown
- 2013-05-29 KR KR20147036874A patent/KR20150023536A/ko not_active Withdrawn
- 2013-05-29 WO PCT/US2013/043016 patent/WO2013181202A2/en not_active Ceased
- 2013-05-29 EP EP13797843.3A patent/EP2854797A4/en not_active Withdrawn
- 2013-05-29 EA EA201492271A patent/EA026380B1/ru not_active IP Right Cessation
- 2013-05-29 AU AU2013267555A patent/AU2013267555A1/en not_active Abandoned
- 2013-05-29 MX MX2014014066A patent/MX2014014066A/es unknown
- 2013-05-29 SG SG11201407796YA patent/SG11201407796YA/en unknown
- 2013-05-29 BR BR112014029597A patent/BR112014029597A2/pt not_active IP Right Cessation
- 2013-05-29 CA CA2873678A patent/CA2873678A1/en not_active Abandoned
- 2013-05-29 CN CN201380028374.8A patent/CN104394862A/zh active Pending
- 2013-05-30 TW TW102119181A patent/TW201408672A/zh unknown
-
2014
- 2014-02-27 US US14/192,667 patent/US8975415B2/en not_active Expired - Fee Related
-
2015
- 2015-01-22 US US14/603,110 patent/US9242973B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US20150225386A1 (en) | 2015-08-13 |
| EA201492271A1 (ru) | 2015-10-30 |
| EP2854797A2 (en) | 2015-04-08 |
| BR112014029597A2 (pt) | 2017-11-07 |
| TW201408672A (zh) | 2014-03-01 |
| US9242973B2 (en) | 2016-01-26 |
| AU2013267555A1 (en) | 2014-12-04 |
| JP2015518048A (ja) | 2015-06-25 |
| SG11201407796YA (en) | 2014-12-30 |
| WO2013181202A3 (en) | 2014-01-30 |
| CN104394862A (zh) | 2015-03-04 |
| CA2873678A1 (en) | 2013-12-05 |
| WO2013181202A2 (en) | 2013-12-05 |
| HK1208817A1 (en) | 2016-03-18 |
| EA026380B1 (ru) | 2017-04-28 |
| US20140179695A1 (en) | 2014-06-26 |
| US8975415B2 (en) | 2015-03-10 |
| KR20150023536A (ko) | 2015-03-05 |
| MX2014014066A (es) | 2015-03-19 |
| EP2854797A4 (en) | 2016-01-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |