HUP0303281A2 - Benzodiazepinszármazékok, mint GABA A receptor modulátorok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents
Benzodiazepinszármazékok, mint GABA A receptor modulátorok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0303281A2 HUP0303281A2 HU0303281A HUP0303281A HUP0303281A2 HU P0303281 A2 HUP0303281 A2 HU P0303281A2 HU 0303281 A HU0303281 A HU 0303281A HU P0303281 A HUP0303281 A HU P0303281A HU P0303281 A2 HUP0303281 A2 HU P0303281A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- lower alkyl
- compounds
- gaba
- atom
- Prior art date
Links
- 238000002360 preparation method Methods 0.000 title abstract 2
- 102000004300 GABA-A Receptors Human genes 0.000 title 1
- 108090000839 GABA-A 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
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000001766 1,2,4-oxadiazol-3-yl group Chemical group [H]C1=NC(*)=NO1 0.000 abstract 1
- 125000004505 1,2,4-oxadiazol-5-yl group Chemical group O1N=CN=C1* 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 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
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 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
- 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
-
- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- 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)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
A találmány (I) általános képletű vegyületekre vonatkozik, amelyképletben R1 jelentése hidrogénatom, halogénatom, kis szénatomszámúalkil-, kis szénatomszámú alkoxi-, hidroxi-, ciano-, trifluor-metil-,trifluor-metoxi- vagy kis szénatomszámú alkil-tio-csoport; R2jelentése -C(O)O-kis szénatomszámú alkil-, izoxazol-, 1,2,4-oxadiazol-3-il- vagy 1,2,4-oxadiazol-5-il-csoport, amely gyűrűk kisszénatomszámú alkil-, trifluor-metil- vagy cikloalkilcsoporttalhelyettesítve lehetnek; R3 jelentése hidrogénatom, kis szénatomszámúalkil-, -(CH2)n-cikloalkil-, -(CH2)n-halogén-, -(CH2)n-piridin-4-il-vagy -(CH2)n-fenilcsoport, mimellett a fenilgyűrű adott esetben egyvagy két alábbi helyettesítőt hordozhat: kis szénatomszámúalkoxicsoport, halogénatom, metilszulfonil-, fenil-, trifluor-metoxi-,nitro-, trifluor-metil-, -NR2- vagy adott esetben kis szénatomszámúalkil- vagy kis szénatomszámú alkoxicsoporttal helyettesített -(CH2)p-indolil-, vagy pirrolidinil-5-oxo-, -C(O)-NR2-, -(CH2)n-OH-, -(CH2)n-NR2- vagy -(CH2)n-benzo[1,3]dioxolcsoport; R jelentése hidrogénatomvagy kis szénatomszámú alkilcsoport; és n értéke 0, 1, 2 vagy 3] és evegyületek gyógyászatilag alkalmas savaddíciós sói. A találmányszerinti vegyületek a GABA a5 receptorhoz jó affinitást mutatnak ésezért a fenti receptorral kapcsolatos betegségek kezelésérealkalmazhatók. A találmány továbbá kiterjed a vegyületek előállításieljárásására és ezeket tartalmazó gyógyszerkészítményekre is. Ó
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 (2)
| Publication Number | Publication Date |
|---|---|
| HUP0303281A2 true HUP0303281A2 (hu) | 2004-01-28 |
| HUP0303281A3 HUP0303281A3 (en) | 2005-05-30 |
Family
ID=8170315
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0303281A HUP0303281A3 (en) | 2000-11-16 | 2001-11-08 | Benzodiazepine derivatives as gaba a receptor modulators, process for their preparation and pharmaceutical compositions containing them |
Country Status (40)
| Country | Link |
|---|---|
| US (1) | US6743789B2 (hu) |
| EP (1) | EP1337535B1 (hu) |
| JP (1) | JP4088151B2 (hu) |
| KR (1) | KR100504300B1 (hu) |
| CN (1) | CN1191255C (hu) |
| AR (1) | AR031345A1 (hu) |
| AT (1) | ATE268776T1 (hu) |
| AU (2) | AU2002217007B2 (hu) |
| BG (1) | BG107817A (hu) |
| BR (1) | BR0115393A (hu) |
| CA (1) | CA2427576C (hu) |
| CZ (1) | CZ295256B6 (hu) |
| DE (1) | DE60103776T2 (hu) |
| DK (1) | DK1337535T3 (hu) |
| EC (1) | ECSP034607A (hu) |
| ES (1) | ES2220831T3 (hu) |
| GC (1) | GC0000375A (hu) |
| GT (1) | GT200100230A (hu) |
| HR (1) | HRP20030360A2 (hu) |
| HU (1) | HUP0303281A3 (hu) |
| IL (1) | IL155813A0 (hu) |
| JO (1) | JO2359B1 (hu) |
| MA (1) | MA26962A1 (hu) |
| MX (1) | MXPA03004251A (hu) |
| MY (1) | MY141675A (hu) |
| NO (1) | NO324706B1 (hu) |
| NZ (1) | NZ525413A (hu) |
| PA (1) | PA8532401A1 (hu) |
| PE (1) | PE20020583A1 (hu) |
| PL (1) | PL362925A1 (hu) |
| PT (1) | PT1337535E (hu) |
| RU (1) | RU2278865C2 (hu) |
| SI (1) | SI1337535T1 (hu) |
| SK (1) | SK7232003A3 (hu) |
| TR (1) | TR200402073T4 (hu) |
| TW (1) | TWI239333B (hu) |
| UY (1) | UY27026A1 (hu) |
| WO (1) | WO2002040487A2 (hu) |
| YU (1) | YU35603A (hu) |
| ZA (1) | ZA200303435B (hu) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6686352B2 (en) * | 2001-05-18 | 2004-02-03 | Hoffmann-La Roche Inc. | Substituted imidazo [1,5-a] pyrimido [5,4-d] [1] benzazepine derivatives |
| WO2004113321A1 (ja) * | 2003-06-19 | 2004-12-29 | Daiichi Pharmaceutical Co., Ltd. | 選択的なアミノ置換基導入法 |
| DK1691811T3 (da) | 2003-12-11 | 2014-10-20 | Sunovion Pharmaceuticals Inc | Kombination af et sedativ og en neurotransmittermodulator og fremgangsmåder til forbedring af søvnkvaliteten og behandling af depression |
| EP1784390A2 (en) | 2004-08-13 | 2007-05-16 | 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 |
| MX2007004639A (es) * | 2004-10-20 | 2007-06-08 | Hoffmann La Roche | Derivados de imidazo-benzodiazepina. |
| RU2007114763A (ru) | 2004-10-20 | 2008-11-27 | Ф.Хоффманн-Ля Рош Аг (Ch) | Галогенозамещенные производные бензодиазепинов |
| RU2393161C2 (ru) * | 2004-12-14 | 2010-06-27 | Ф. Хоффманн-Ля Рош Аг | Тетрациклические имидазо-бензодиазепины в качестве модуляторов гамк-рецепторов |
| US8510055B2 (en) | 2005-08-03 | 2013-08-13 | The Johns Hopkins University | Methods for characterizing and treating cognitive impairment in aging and disease |
| EP2682481A3 (en) * | 2005-08-03 | 2014-09-17 | The Johns-Hopkins University | Methods for characterizing and treating cognitive impairment in aging and disease |
| ES2348356T3 (es) * | 2005-10-11 | 2010-12-03 | F. Hoffmann-La Roche Ag | Derivados de imidazo-benzodiazepina. |
| JP2009513672A (ja) | 2005-10-31 | 2009-04-02 | ブレインセルス，インコーポレイティド | 神経発生のｇａｂａ受容体媒介調節 |
| 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 |
| BRPI0922303B1 (pt) * | 2008-11-28 | 2019-11-12 | Hoffmann La Roche | arilciclo-hexiléteres de di-hidrotetra-azabenzoazulenos, seu processo de preparação, composição farmacêutica que os compreende e uso |
| CU20090172A6 (es) | 2009-10-09 | 2011-10-05 | Facultad De Quimica Universidad De La Habana | Sistemas tricíclicos y tetracíclicos con actividad sobre el sistema nervioso central y vascular |
| BR112013012062B1 (pt) | 2010-11-15 | 2020-06-02 | Agenebio, Inc | Composto derivado da piridazina ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica e uso do composto |
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| EP2897963A4 (en) * | 2012-09-21 | 2016-03-30 | Uwm Res Foundation Inc | Novel GABAA AGONISTS AND METHOD FOR USE TO COMBAT AIRWAY HYPER REAGIBILITY AND IGNITIONS IN ASTHMA |
| CA2934553C (en) | 2013-12-20 | 2023-10-31 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| MA42624A (fr) * | 2015-06-19 | 2021-04-28 | Agenebio Inc | Dérivés de benzodiazépine, compositions et méthodes de traitement de la déficience cognitive |
| 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 |
| US20180170941A1 (en) * | 2016-12-19 | 2018-06-21 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| US11505555B2 (en) | 2016-12-19 | 2022-11-22 | 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 |
| US11414425B2 (en) | 2018-06-19 | 2022-08-16 | 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 |
| IL319072A (en) | 2022-08-19 | 2025-04-01 | Agenebio Inc | History of Benzazepine, Compositions and Methods for Treating Cognitive Impairment |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK174086D0 (da) | 1986-04-16 | 1986-04-16 | Ferrosan As | Nye benzodiazepinderivater samt fremgangsmaade til fremstilling af samme |
| TW201311B (hu) * | 1991-06-17 | 1993-03-01 | Hoffmann La Roche |
-
2001
- 2001-11-07 TW TW090127658A patent/TWI239333B/zh not_active IP Right Cessation
- 2001-11-08 JP JP2002543495A patent/JP4088151B2/ja not_active Expired - Fee Related
- 2001-11-08 YU YU35603A patent/YU35603A/sh unknown
- 2001-11-08 SI SI200130125T patent/SI1337535T1/xx unknown
- 2001-11-08 KR KR10-2003-7006609A patent/KR100504300B1/ko not_active Expired - Fee Related
- 2001-11-08 CZ CZ20031597A patent/CZ295256B6/cs not_active IP Right Cessation
- 2001-11-08 WO PCT/EP2001/012887 patent/WO2002040487A2/en not_active Ceased
- 2001-11-08 IL IL15581301A patent/IL155813A0/xx unknown
- 2001-11-08 RU RU2003116895/04A patent/RU2278865C2/ru not_active IP Right Cessation
- 2001-11-08 EP EP01996541A patent/EP1337535B1/en not_active Expired - Lifetime
- 2001-11-08 ES ES01996541T patent/ES2220831T3/es not_active Expired - Lifetime
- 2001-11-08 AT AT01996541T patent/ATE268776T1/de not_active IP Right Cessation
- 2001-11-08 DK DK01996541T patent/DK1337535T3/da active
- 2001-11-08 DE DE60103776T patent/DE60103776T2/de not_active Expired - Lifetime
- 2001-11-08 AU AU2002217007A patent/AU2002217007B2/en not_active Ceased
- 2001-11-08 US US10/007,883 patent/US6743789B2/en not_active Expired - Fee Related
- 2001-11-08 PT PT01996541T patent/PT1337535E/pt unknown
- 2001-11-08 PL PL01362925A patent/PL362925A1/xx not_active Application Discontinuation
- 2001-11-08 CA CA002427576A patent/CA2427576C/en not_active Expired - Fee Related
- 2001-11-08 AU AU1700702A patent/AU1700702A/xx active Pending
- 2001-11-08 BR BR0115393-5A patent/BR0115393A/pt not_active IP Right Cessation
- 2001-11-08 HR HR20030360A patent/HRP20030360A2/hr not_active Application Discontinuation
- 2001-11-08 NZ NZ525413A patent/NZ525413A/en unknown
- 2001-11-08 SK SK723-2003A patent/SK7232003A3/sk unknown
- 2001-11-08 TR TR2004/02073T patent/TR200402073T4/xx unknown
- 2001-11-08 CN CNB018189415A patent/CN1191255C/zh not_active Expired - Fee Related
- 2001-11-08 MX MXPA03004251A patent/MXPA03004251A/es active IP Right Grant
- 2001-11-08 HU HU0303281A patent/HUP0303281A3/hu unknown
- 2001-11-12 JO JO2001183A patent/JO2359B1/en active
- 2001-11-13 GC GCP20011724 patent/GC0000375A/en active
- 2001-11-14 PE PE2001001135A patent/PE20020583A1/es not_active Application Discontinuation
- 2001-11-15 MY MYPI20015253A patent/MY141675A/en unknown
- 2001-11-15 PA PA20018532401A patent/PA8532401A1/es unknown
- 2001-11-15 GT GT200100230A patent/GT200100230A/es unknown
- 2001-11-15 AR ARP010105323A patent/AR031345A1/es not_active Application Discontinuation
- 2001-11-15 UY UY27026A patent/UY27026A1/es not_active Application Discontinuation
-
2003
- 2003-05-05 ZA ZA200303435A patent/ZA200303435B/en unknown
- 2003-05-15 EC EC2003004607A patent/ECSP034607A/es unknown
- 2003-05-15 NO NO20032208A patent/NO324706B1/no unknown
- 2003-05-16 BG BG107817A patent/BG107817A/bg unknown
- 2003-05-16 MA MA27163A patent/MA26962A1/fr unknown
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