JP4088151B2 - Ｇａｂａａ受容体モデュレーターとしてのベンゾジアゼピン誘導体 - Google Patents
Ｇａｂａａ受容体モデュレーターとしてのベンゾジアゼピン誘導体 Download PDFInfo
- Publication number
- JP4088151B2 JP4088151B2 JP2002543495A JP2002543495A JP4088151B2 JP 4088151 B2 JP4088151 B2 JP 4088151B2 JP 2002543495 A JP2002543495 A JP 2002543495A JP 2002543495 A JP2002543495 A JP 2002543495A JP 4088151 B2 JP4088151 B2 JP 4088151B2
- Authority
- JP
- Japan
- Prior art keywords
- benzodiazepine
- triazolo
- imidazo
- ethyl
- oxadiazol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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- 102000027484 GABAA receptors Human genes 0.000 title 1
- 108091008681 GABAA receptors Proteins 0.000 title 1
- 229940053197 benzodiazepine derivative antiepileptics Drugs 0.000 title 1
- 125000003310 benzodiazepinyl group Chemical class N1N=C(C=CC2=C1C=CC=C2)* 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 93
- 150000003839 salts Chemical class 0.000 claims abstract description 20
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 112
- -1 3-Cyclopropyl-1,2,4-oxadiazol-5-yl Chemical group 0.000 claims description 90
- NZTCFMPWFGWRBN-UHFFFAOYSA-N 3H-[1,2,4]triazolo[4,3-d][1,4]benzodiazepine-10-carboxylic acid Chemical compound N1=NCN2C=CN=C3C(=C21)C=C(C=C3)C(=O)O NZTCFMPWFGWRBN-UHFFFAOYSA-N 0.000 claims description 79
- 238000000034 method Methods 0.000 claims description 73
- 125000000217 alkyl group Chemical group 0.000 claims description 24
- 229910052739 hydrogen Inorganic materials 0.000 claims description 17
- 239000001257 hydrogen Substances 0.000 claims description 17
- 229910052736 halogen Inorganic materials 0.000 claims description 14
- 239000002253 acid Substances 0.000 claims description 12
- 150000002367 halogens Chemical class 0.000 claims description 11
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 11
- SFPHNARDXIEZPB-UHFFFAOYSA-N C1=NNN2C=CN=C3C(=C21)C=C(C=C3)C(=O)O Chemical compound C1=NNN2C=CN=C3C(=C21)C=C(C=C3)C(=O)O SFPHNARDXIEZPB-UHFFFAOYSA-N 0.000 claims description 10
- 125000003545 alkoxy group Chemical group 0.000 claims description 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 238000002360 preparation method Methods 0.000 claims description 9
- 125000001424 substituent group Chemical group 0.000 claims description 9
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- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 abstract description 16
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-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
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- 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
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- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00124332 | 2000-11-16 | ||
| PCT/EP2001/012887 WO2002040487A2 (en) | 2000-11-16 | 2001-11-08 | Benzodiazepine derivatives as gaba a receptor modulators |
Publications (3)
| Publication Number | Publication Date |
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| JP2004517070A JP2004517070A (ja) | 2004-06-10 |
| JP2004517070A5 JP2004517070A5 (enExample) | 2005-05-26 |
| JP4088151B2 true JP4088151B2 (ja) | 2008-05-21 |
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| US6686352B2 (en) * | 2001-05-18 | 2004-02-03 | Hoffmann-La Roche Inc. | Substituted imidazo [1,5-a] pyrimido [5,4-d] [1] benzazepine derivatives |
| EP1634879A4 (en) * | 2003-06-19 | 2007-09-05 | Daiichi Seiyaku Co | METHOD FOR THE SELECTIVE INTRODUCTION OF AN AMINO SUBSTITUENT |
| JP5646126B2 (ja) | 2003-12-11 | 2014-12-24 | サノビオン ファーマシューティカルズ インクＳｕｎｏｖｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃ． | 鎮静剤と神経伝達物質調節剤の併用、および睡眠の質の向上方法および鬱の治療方法 |
| WO2006020959A2 (en) | 2004-08-13 | 2006-02-23 | Amgen Inc. | Substituted benzofused heterocycles |
| CA2581918A1 (en) * | 2004-10-12 | 2006-04-20 | Henner Knust | Imidazo(1,5-a)triazolo(1,5-d) benzodiazepine deratives for the treatment of cognitive disorders |
| RU2007114763A (ru) * | 2004-10-20 | 2008-11-27 | Ф.Хоффманн-Ля Рош Аг (Ch) | Галогенозамещенные производные бензодиазепинов |
| ES2399439T3 (es) * | 2004-10-20 | 2013-04-01 | F. Hoffmann-La Roche Ag | Derivados de imidazo-benzodiazepina |
| BRPI0515800A (pt) * | 2004-12-14 | 2008-08-05 | Hoffmann La Roche | imidazo-benzodiazepinas tetracìclicas como moduladores de receptores de gaba |
| US8510055B2 (en) | 2005-08-03 | 2013-08-13 | The Johns Hopkins University | Methods for characterizing and treating cognitive impairment in aging and disease |
| EP1924712B1 (en) * | 2005-08-03 | 2018-10-03 | The Johns Hopkins University | Methods for characterizing and treating cognitive impairment in aging and disease |
| EP1937688B1 (en) | 2005-10-11 | 2010-08-11 | F. Hoffmann-La Roche AG | Imidazo benzodiazepine derivatives |
| CA2625210A1 (en) | 2005-10-31 | 2007-05-10 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| US9156836B2 (en) * | 2008-05-16 | 2015-10-13 | Synta Pharmaceuticals Corp. | Tricyclic triazole compounds that modulate HSP90 activity |
| KR101385433B1 (ko) * | 2008-11-18 | 2014-04-14 | 에프. 호프만-라 로슈 아게 | 다이하이드로테트라아자벤조아줄렌의 알킬사이클로헥실에터 |
| DK2370441T3 (da) * | 2008-11-28 | 2013-10-21 | Hoffmann La Roche | Arylcyclohexylethere af dihydrotetraazabenzoazulener til anvendelse som vasopressin v1a-receptorantagonister |
| CU20090172A7 (es) | 2009-10-09 | 2011-10-05 | Ct De Investigación Y Desarrollo De Medicamentos | Sistemas tricíclicos y tetracíclicos con actividad sobre el sistema nervioso central y vascular |
| DK3034079T3 (en) | 2010-11-15 | 2018-02-05 | Agenebio Inc | PYRIDAZINE DERIVATIVES, COMPOSITIONS AND PROCEDURES FOR TREATING COGNITIVE WEAKNESS |
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| WO2014047413A1 (en) * | 2012-09-21 | 2014-03-27 | Uwm Research Foundation, Inc. | Novel gabaa agonists and methods of using to control airway hyperresponsiveness and inflammation in asthma |
| CA3123897C (en) * | 2013-12-20 | 2024-02-06 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| CN108026107B (zh) | 2015-06-19 | 2021-07-30 | 艾吉因生物股份有限公司 | 用于治疗认知损害的苯并二氮杂环庚三烯衍生物、组合物和方法 |
| US10059718B2 (en) * | 2016-01-04 | 2018-08-28 | Tabomedex Biosciences, LLC | Fused quadracyclic compounds, compositions and uses thereof |
| US10973479B2 (en) | 2016-05-16 | 2021-04-13 | Canon Medical Systems Corporation | X-ray diagnosis apparatus, X-ray diagnosis apparatus controlling method, and X-ray diagnosis system |
| BR112019012821A2 (pt) | 2016-12-19 | 2019-11-26 | Agenebio Inc | derivados de benzodiazepina, composições e métodos para o tratamento do comprometimento cognitivo |
| US20180170941A1 (en) * | 2016-12-19 | 2018-06-21 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| KR102512548B1 (ko) | 2017-12-22 | 2023-03-22 | 삼성디스플레이 주식회사 | 유기 전계 발광 소자 및 유기 전계 발광 소자용 함질소 화합물 |
| WO2019246300A1 (en) | 2018-06-19 | 2019-12-26 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| KR102151969B1 (ko) * | 2019-12-11 | 2020-09-04 | 주식회사 지투비 | 투과도 가변창의 제조방법 및 그에 의해 제조된 투과도 가변창 |
| CN112979658B (zh) * | 2021-02-22 | 2022-05-31 | 南湖实验室 | 一种氟马西尼的制备方法 |
| US20240132513A1 (en) | 2022-08-19 | 2024-04-25 | Agenebio, Inc. | Benzazepine derivatives, compositions, and methods for treating cognitive impairment |
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| DK174086D0 (da) | 1986-04-16 | 1986-04-16 | Ferrosan As | Nye benzodiazepinderivater samt fremgangsmaade til fremstilling af samme |
| TW201311B (enExample) * | 1991-06-17 | 1993-03-01 | Hoffmann La Roche |
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