TW201408672A - □烷化合物 - Google Patents
□烷化合物 Download PDFInfo
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- TW201408672A TW201408672A TW102119181A TW102119181A TW201408672A TW 201408672 A TW201408672 A TW 201408672A TW 102119181 A TW102119181 A TW 102119181A TW 102119181 A TW102119181 A TW 102119181A TW 201408672 A TW201408672 A TW 201408672A
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- Prior art keywords
- mixture
- group
- compound
- mmol
- oxazole
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- 125000003016 chromanyl group Chemical class O1C(CCC2=CC=CC=C12)* 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 282
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- 208000010877 cognitive disease Diseases 0.000 claims abstract description 30
- 208000027061 mild cognitive impairment Diseases 0.000 claims abstract description 30
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- 238000002360 preparation method Methods 0.000 claims description 101
- 125000000217 alkyl group Chemical group 0.000 claims description 67
- 229910052736 halogen Inorganic materials 0.000 claims description 66
- 150000002367 halogens Chemical group 0.000 claims description 65
- 125000000623 heterocyclic group Chemical group 0.000 claims description 60
- 150000003839 salts Chemical class 0.000 claims description 58
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims description 53
- 125000001424 substituent group Chemical group 0.000 claims description 45
- 241000237858 Gastropoda Species 0.000 claims description 28
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 28
- 238000000034 method Methods 0.000 claims description 22
- 125000002950 monocyclic group Chemical group 0.000 claims description 22
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- 238000011282 treatment Methods 0.000 claims description 22
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 18
- 239000001301 oxygen Substances 0.000 claims description 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 15
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- GQHTUMJGOHRCHB-UHFFFAOYSA-N 2,3,4,6,7,8,9,10-octahydropyrimido[1,2-a]azepine Chemical compound C1CCCCN2CCCN=C21 GQHTUMJGOHRCHB-UHFFFAOYSA-N 0.000 description 14
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Classifications
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- 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
-
- 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
- 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
-
- 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)
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- 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)
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| SG (1) | SG11201407796YA (enExample) |
| TW (1) | TW201408672A (enExample) |
| WO (1) | WO2013181202A2 (enExample) |
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| WO2013181202A2 (en) | 2012-05-30 | 2013-12-05 | Astellas Pharma Inc. | Chromane compounds |
| UY36347A (es) * | 2014-10-07 | 2016-04-01 | Astrazeneca Ab | Compuestos y su uso como inhibidores de bace |
| 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 |
| 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 |
| 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 |
| 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 |
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|---|---|---|---|---|
| EP1196609A2 (en) | 1999-06-28 | 2002-04-17 | Oklahoma Medical Research Foundation | Catalytically active recombinant memapsin and methods of use thereof |
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-
2013
- 2013-05-29 WO PCT/US2013/043016 patent/WO2013181202A2/en not_active Ceased
- 2013-05-29 BR BR112014029597A patent/BR112014029597A2/pt not_active IP Right Cessation
- 2013-05-29 EP EP13797843.3A patent/EP2854797A4/en not_active Withdrawn
- 2013-05-29 SG SG11201407796YA patent/SG11201407796YA/en unknown
- 2013-05-29 CN CN201380028374.8A patent/CN104394862A/zh active Pending
- 2013-05-29 AR ARP130101885 patent/AR091203A1/es unknown
- 2013-05-29 MX MX2014014066A patent/MX2014014066A/es unknown
- 2013-05-29 CA CA2873678A patent/CA2873678A1/en not_active Abandoned
- 2013-05-29 JP JP2015515133A patent/JP2015518048A/ja active Pending
- 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 HK HK15109582.8A patent/HK1208817A1/xx unknown
- 2013-05-29 KR KR20147036874A patent/KR20150023536A/ko not_active Withdrawn
- 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
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|---|---|
| AR091203A1 (es) | 2015-01-21 |
| US20140179695A1 (en) | 2014-06-26 |
| CA2873678A1 (en) | 2013-12-05 |
| HK1208817A1 (en) | 2016-03-18 |
| EP2854797A2 (en) | 2015-04-08 |
| WO2013181202A2 (en) | 2013-12-05 |
| KR20150023536A (ko) | 2015-03-05 |
| JP2015518048A (ja) | 2015-06-25 |
| MX2014014066A (es) | 2015-03-19 |
| WO2013181202A3 (en) | 2014-01-30 |
| EA026380B1 (ru) | 2017-04-28 |
| SG11201407796YA (en) | 2014-12-30 |
| CN104394862A (zh) | 2015-03-04 |
| AU2013267555A1 (en) | 2014-12-04 |
| EA201492271A1 (ru) | 2015-10-30 |
| US20150225386A1 (en) | 2015-08-13 |
| US8975415B2 (en) | 2015-03-10 |
| US9242973B2 (en) | 2016-01-26 |
| EP2854797A4 (en) | 2016-01-13 |
| BR112014029597A2 (pt) | 2017-11-07 |
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