IL228158A - History of 7,6-Dihydro-pyrazolo [5,1- a] Pirazine-4-Illamine used as an inhibitor of thescretase - Google Patents
History of 7,6-Dihydro-pyrazolo [5,1- a] Pirazine-4-Illamine used as an inhibitor of thescretaseInfo
- Publication number
- IL228158A IL228158A IL228158A IL22815813A IL228158A IL 228158 A IL228158 A IL 228158A IL 228158 A IL228158 A IL 228158A IL 22815813 A IL22815813 A IL 22815813A IL 228158 A IL228158 A IL 228158A
- Authority
- IL
- Israel
- Prior art keywords
- mixture
- mmol
- vacuo
- compound
- acid
- Prior art date
Links
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
- C07D487/02—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 two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11156463 | 2011-03-01 | ||
| PCT/EP2012/053455 WO2012117027A1 (en) | 2011-03-01 | 2012-02-29 | 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL228158A0 IL228158A0 (en) | 2013-11-25 |
| IL228158A true IL228158A (en) | 2016-07-31 |
Family
ID=45808845
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL228158A IL228158A (en) | 2011-03-01 | 2013-08-28 | History of 7,6-Dihydro-pyrazolo [5,1- a] Pirazine-4-Illamine used as an inhibitor of thescretase |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US9346811B2 (enExample) |
| EP (1) | EP2681219B1 (enExample) |
| JP (1) | JP5853033B2 (enExample) |
| KR (1) | KR102012671B1 (enExample) |
| CN (1) | CN103415519B (enExample) |
| AU (1) | AU2012222394B2 (enExample) |
| BR (1) | BR112013022039A2 (enExample) |
| CA (1) | CA2824360C (enExample) |
| CL (1) | CL2013002486A1 (enExample) |
| CO (1) | CO6751282A2 (enExample) |
| CY (1) | CY1117663T1 (enExample) |
| DK (1) | DK2681219T3 (enExample) |
| EA (1) | EA022649B1 (enExample) |
| ES (1) | ES2558779T3 (enExample) |
| HR (1) | HRP20160030T1 (enExample) |
| HU (1) | HUE026338T2 (enExample) |
| IL (1) | IL228158A (enExample) |
| MX (1) | MX338333B (enExample) |
| MY (1) | MY161407A (enExample) |
| PH (1) | PH12013501807A1 (enExample) |
| PL (1) | PL2681219T3 (enExample) |
| PT (1) | PT2681219E (enExample) |
| SG (1) | SG192963A1 (enExample) |
| SI (1) | SI2681219T1 (enExample) |
| UA (1) | UA109800C2 (enExample) |
| WO (1) | WO2012117027A1 (enExample) |
| ZA (1) | ZA201306545B (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2476027T3 (es) | 2005-10-25 | 2014-07-11 | Shionogi & Co., Ltd. | Derivados de aminodihidrotriazina |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| KR20100017255A (ko) | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 유도체 |
| MX2010013256A (es) | 2008-06-13 | 2010-12-21 | Shionogi & Co | Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa. |
| EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
| JPWO2011071135A1 (ja) | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | オキサジン誘導体 |
| EP2580200B1 (en) | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| CN103403007B (zh) | 2010-12-22 | 2015-12-09 | 詹森药业有限公司 | 用作β-分泌酶(BACE)抑制剂的5,6-二氢-咪唑并[1,2-a]吡嗪-8-基胺衍生物 |
| BR112013022039A2 (pt) | 2011-03-01 | 2016-11-29 | Janssen Pharmaceutica Nv | derivados 6,7-di-hidro-pirazol[1,5-a]pirazin-4-ilamina úteis como inibidores de beta-secretase (bace) |
| SI3447061T1 (sl) | 2011-03-01 | 2022-02-28 | NuCana plc | Farmacevtska formulacija, ki obsega fosforamidni derivat 5-fluoro-2'-deoksiuridina za uporabo pri zdravljenju raka |
| KR102012675B1 (ko) | 2011-03-09 | 2019-08-21 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(BACE)의 억제제로서 유용한 3,4-디하이드로-피롤로[1,2-a]피라진-1-일아민 유도체 |
| WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するbace1阻害剤 |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| CA2911690C (en) * | 2013-06-12 | 2021-08-24 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
| AU2014280125B2 (en) * | 2013-06-12 | 2018-03-15 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (BACE) |
| BR112015030498A2 (pt) | 2013-06-12 | 2017-07-25 | Janssen Pharmaceutica Nv | derivados 4-amino-6-fenil-5,6-di-hidroimidazo[1,5-a]pirazin-3(2h)-ona como inibidores de beta-secretase (bace) |
| WO2016096979A1 (en) | 2014-12-18 | 2016-06-23 | Janssen Pharmaceutica Nv | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase |
| US10357493B2 (en) | 2017-03-10 | 2019-07-23 | Selenity Therapeutics (Bermuda), Ltd. | Metalloenzyme inhibitor compounds |
| TWI782056B (zh) | 2017-07-14 | 2022-11-01 | 日商鹽野義製藥股份有限公司 | 具有mgat2抑制活性的縮合環衍生物 |
| EP3909583A4 (en) | 2019-01-11 | 2022-08-17 | Shionogi & Co., Ltd | DIHYDROPYRAZOLOPYRAZINONE DERIVATIVES WITH MGAT2 INHIBITORY ACTIVITY |
| KR20250022711A (ko) * | 2022-06-13 | 2025-02-17 | 시오노기 앤드 컴파니, 리미티드 | 다이하이드로피리딘온 유도체 또는 그 용매화물의 결정 |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4188389A (en) | 1978-11-03 | 1980-02-12 | Ayerst Mckenna & Harrison, Inc. | 1,2,3,4-Tetrahydropyrrolo(1,2-A)pyrazines |
| TW224974B (enExample) | 1991-07-02 | 1994-06-11 | Hoffmann La Roche | |
| WO2003089434A2 (en) | 2002-04-19 | 2003-10-30 | Cellular Genomics, Inc. | IMIDAZO[1,2-a]PYRAZIN-8-YLAMINES METHOD OF MAKING AND METHOD OF USE THEREOF |
| AU2003272476B2 (en) | 2002-09-23 | 2007-07-05 | Schering Corporation | Imidazopyrazines as cyclin dependent kinase inhibitors |
| BR0317430A (pt) | 2002-12-20 | 2005-10-25 | Pharmacia Corp | Compostos inibidores de quinase-2 de proteìna ativada por quinase de proteìna ativada por mitógeno |
| WO2004092177A1 (en) * | 2003-04-09 | 2004-10-28 | Biogen Idec Ma Inc. | Triazolopyrazines and methods of making and using the same |
| JP2007533641A (ja) | 2003-10-15 | 2007-11-22 | ターガセプト,インコーポレイテッド | 疼痛緩和および中枢神経系障害治療のためのアザビシクロ化合物 |
| JP2007533741A (ja) | 2004-04-22 | 2007-11-22 | イーライ リリー アンド カンパニー | Bace阻害剤 |
| TW200602045A (en) | 2004-06-16 | 2006-01-16 | Wyeth Corp | Amino-5, 5-diphenylimidazolone derivatives for the inhibition of β-secretase |
| SV2006002232A (es) | 2004-09-21 | 2006-05-25 | Lilly Co Eli | Inhibidores bace ref. x-16940 |
| CA2593515A1 (en) | 2005-01-14 | 2006-07-20 | Wyeth | Amino-imidazolones for the inhibition of beta-secretase |
| US20070005404A1 (en) | 2005-06-09 | 2007-01-04 | Drive Diagnostics Ltd. | System and method for providing driving insurance |
| CA2610828A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
| AU2006266167A1 (en) | 2005-06-30 | 2007-01-11 | Wyeth | Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation |
| ES2476027T3 (es) | 2005-10-25 | 2014-07-11 | Shionogi & Co., Ltd. | Derivados de aminodihidrotriazina |
| TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| US20090099217A1 (en) | 2006-04-05 | 2009-04-16 | Astex Therapeutics Ltd. | 2-Aminopyrimidin-4-Ones And Their Use For Treating Or Preventing Alpha Beta-Related Pathologies |
| GB2443654A (en) | 2006-05-30 | 2008-05-14 | Matthew Emmerson Allen | System for detecting and testing drivers who show abnormal driving behaviour. |
| TW200815443A (en) * | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds I |
| CN101501040A (zh) * | 2006-06-14 | 2009-08-05 | 阿斯利康(瑞典)有限公司 | 氨基-咪唑啉以及它们作为治疗认知缺损、阿尔茨海默病、神经变性和痴呆的药物的用途 |
| US20080051420A1 (en) * | 2006-06-14 | 2008-02-28 | Astrazeneca Ab | New Compounds 317 |
| KR20100017255A (ko) | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 유도체 |
| TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| EP2217592A1 (en) | 2007-10-30 | 2010-08-18 | Arena Pharmaceuticals, Inc. | Biphenyl derivatives as modulators of the histamine-h3 receptor useful for the treatment of disorders related thereto |
| RU2497821C2 (ru) | 2008-01-28 | 2013-11-10 | Янссен Фармацевтика Нв | ПРОИЗВОДНЫЕ 6-ЗАМЕЩЕННОГО-ТИО (ИЛИ -ОКСО-)-2-АМИНО-ХИНОЛИНА, ПРИМЕНЯЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ β-СЕКРЕТАЗЫ (BACE) |
| EP2252617A1 (en) | 2008-02-13 | 2010-11-24 | CGI Pharmaceuticals, Inc. | 6-aryl-imidaz0[l, 2-a]pyrazine derivatives, method of making, and method of use thereof |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| WO2011002409A1 (en) * | 2009-07-02 | 2011-01-06 | Astrazeneca Ab | 5h-pyrrolo[3,4-£>]pyrazin-7-amine derivatives inhibitors of beta-secretase |
| UY32799A (es) | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
| US8188079B2 (en) | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
| EP2500344A4 (en) | 2009-11-13 | 2013-05-01 | Shionogi & Co | AMINOTHIAZIN OR AMINOOXAZINE DERIVATIVES WITH AN AMINO TERMINATION |
| JPWO2011071135A1 (ja) | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | オキサジン誘導体 |
| WO2011077726A1 (ja) | 2009-12-24 | 2011-06-30 | 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 |
| BR112012015916A2 (pt) | 2009-12-31 | 2017-04-25 | Novartis Ag | derivados de pirazina e seu uso no tratamento de distúrbios neurológicos |
| EP2580200B1 (en) | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| CN103403007B (zh) | 2010-12-22 | 2015-12-09 | 詹森药业有限公司 | 用作β-分泌酶(BACE)抑制剂的5,6-二氢-咪唑并[1,2-a]吡嗪-8-基胺衍生物 |
| US9242943B2 (en) | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| BR112013022039A2 (pt) | 2011-03-01 | 2016-11-29 | Janssen Pharmaceutica Nv | derivados 6,7-di-hidro-pirazol[1,5-a]pirazin-4-ilamina úteis como inibidores de beta-secretase (bace) |
| KR102012675B1 (ko) | 2011-03-09 | 2019-08-21 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(BACE)의 억제제로서 유용한 3,4-디하이드로-피롤로[1,2-a]피라진-1-일아민 유도체 |
| WO2013054291A1 (en) | 2011-10-13 | 2013-04-18 | Novartis Ag | Novel oxazine derivatives and their use in the treatment of disease |
-
2012
- 2012-02-29 BR BR112013022039A patent/BR112013022039A2/pt not_active Application Discontinuation
- 2012-02-29 CN CN201280011146.5A patent/CN103415519B/zh not_active Expired - Fee Related
- 2012-02-29 MY MYPI2013003200A patent/MY161407A/en unknown
- 2012-02-29 SG SG2013064746A patent/SG192963A1/en unknown
- 2012-02-29 PT PT127072767T patent/PT2681219E/pt unknown
- 2012-02-29 SI SI201230429T patent/SI2681219T1/sl unknown
- 2012-02-29 DK DK12707276.7T patent/DK2681219T3/en active
- 2012-02-29 US US14/002,169 patent/US9346811B2/en not_active Expired - Fee Related
- 2012-02-29 CA CA2824360A patent/CA2824360C/en active Active
- 2012-02-29 PH PH1/2013/501807A patent/PH12013501807A1/en unknown
- 2012-02-29 HR HRP20160030TT patent/HRP20160030T1/hr unknown
- 2012-02-29 ES ES12707276.7T patent/ES2558779T3/es active Active
- 2012-02-29 EA EA201391251A patent/EA022649B1/ru not_active IP Right Cessation
- 2012-02-29 HU HUE12707276A patent/HUE026338T2/en unknown
- 2012-02-29 JP JP2013555862A patent/JP5853033B2/ja not_active Expired - Fee Related
- 2012-02-29 EP EP12707276.7A patent/EP2681219B1/en active Active
- 2012-02-29 WO PCT/EP2012/053455 patent/WO2012117027A1/en not_active Ceased
- 2012-02-29 PL PL12707276T patent/PL2681219T3/pl unknown
- 2012-02-29 AU AU2012222394A patent/AU2012222394B2/en not_active Ceased
- 2012-02-29 UA UAA201308783A patent/UA109800C2/ru unknown
- 2012-02-29 KR KR1020137022392A patent/KR102012671B1/ko not_active Expired - Fee Related
- 2012-02-29 MX MX2013010040A patent/MX338333B/es active IP Right Grant
-
2013
- 2013-08-28 CL CL2013002486A patent/CL2013002486A1/es unknown
- 2013-08-28 IL IL228158A patent/IL228158A/en active IP Right Grant
- 2013-08-29 CO CO13205178A patent/CO6751282A2/es unknown
- 2013-08-30 ZA ZA2013/06545A patent/ZA201306545B/en unknown
-
2016
- 2016-01-28 CY CY20161100087T patent/CY1117663T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed | ||
| KB | Patent renewed |