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)
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101052122B1 (ko) | 2005-10-25 | 2011-07-26 | 시오노기세야쿠 가부시키가이샤 | 아미노디히드로티아진 유도체 |
| 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 |
| MX2009011498A (es) | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
| AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
| JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Ｂａｃｅ１阻害活性を有する２−アミノピリミジン−４−オンおよび２−アミノピリジン誘導体 |
| US8999980B2 (en) | 2009-12-11 | 2015-04-07 | Shionogi & Co., Ltd. | Oxazine derivatives |
| 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) |
| WO2012057247A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
| US8927721B2 (en) | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| EP2655376B1 (en) | 2010-12-22 | 2017-08-23 | Janssen Pharmaceutica NV | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| EP3447061B1 (en) | 2011-03-01 | 2021-11-24 | NuCana plc | Pharmaceutical formulation comprising a phosphoramidate derivative of 5-fluoro-2'-deoxyuridine for use in the treatment of cancer |
| WO2012117027A1 (en) | 2011-03-01 | 2012-09-07 | Janssen Pharmaceutica Nv | 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
| CN103415521B (zh) | 2011-03-09 | 2016-01-06 | 詹森药业有限公司 | 用作β分泌酶（BACE）抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物 |
| US8883779B2 (en) | 2011-04-26 | 2014-11-11 | Shinogi & Co., Ltd. | Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| MX368326B (es) * | 2013-06-12 | 2019-09-27 | Janssen Pharmaceutica Nv | Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace). |
| ES2721073T3 (es) * | 2013-06-12 | 2019-07-26 | Janssen Pharmaceutica Nv | Derivados de 4-amino-6-fenil-6,7-dihidro[1,2,3]triazolo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE) |
| 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) |
| US10106524B2 (en) | 2014-12-18 | 2018-10-23 | 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 |
| AU2023296166A1 (en) * | 2022-06-13 | 2024-11-28 | Shionogi & Co., Ltd. | Crystal of dihydropyridinone derivative or solvate thereof |
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 (cg-RX-API-DMAC7.html) | 1991-07-02 | 1994-06-11 | Hoffmann La Roche | |
| IL164703A0 (en) | 2002-04-19 | 2005-12-18 | Cellular Genomics Inc | ImidazoÄ1,2-AÜpyrazin-8-ylamines method of making and method of use thereof |
| MXPA05003120A (es) | 2002-09-23 | 2005-06-22 | Schering Corp | Imidazopirazinas como inhibidores de cinasa dependientes de ciclinas. |
| MXPA05006568A (es) | 2002-12-20 | 2005-09-22 | Pharmacia Corp | Compuestos de pirazol aciclico para la inhibicion de proteina cinasa-2 activada por proteina cinasa activada por mitogenos. |
| WO2004092177A1 (en) * | 2003-04-09 | 2004-10-28 | Biogen Idec Ma Inc. | Triazolopyrazines and methods of making and using the same |
| US7402592B2 (en) | 2003-10-15 | 2008-07-22 | Targacept, Inc. | Pharmaceutical compositions and methods for relieving pain and treating central nervous system disorders |
| WO2005108391A1 (en) | 2004-04-22 | 2005-11-17 | Eli Lilly And Company | Amides as bace inhibitors |
| AU2005264915A1 (en) | 2004-06-16 | 2006-01-26 | Wyeth | Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase |
| TW200624426A (en) | 2004-09-21 | 2006-07-16 | Lilly Co Eli | BACE inhibitors |
| RU2007126570A (ru) | 2005-01-14 | 2009-02-20 | Вайет (Us) | Аминоимидазолоны, применяемые для ингибирования бета-секретазы |
| US20070005404A1 (en) | 2005-06-09 | 2007-01-04 | Drive Diagnostics Ltd. | System and method for providing driving insurance |
| MX2007016183A (es) | 2005-06-14 | 2008-03-10 | Schering Corp | Preparacion y uso de compuestos como inhibidores de proteasas. |
| EP1896448A1 (en) | 2005-06-30 | 2008-03-12 | Wyeth | AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION |
| KR101052122B1 (ko) | 2005-10-25 | 2011-07-26 | 시오노기세야쿠 가부시키가이샤 | 아미노디히드로티아진 유도체 |
| 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. |
| US20080051420A1 (en) | 2006-06-14 | 2008-02-28 | Astrazeneca Ab | New Compounds 317 |
| 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 |
| MX2009011498A (es) | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
| TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| WO2009058300A1 (en) | 2007-10-30 | 2009-05-07 | 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) |
| CA2714414A1 (en) | 2008-02-13 | 2009-08-20 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, 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 |
| US20120238557A1 (en) | 2009-11-13 | 2012-09-20 | Shionogi & Co., Ltd. | Aminothiazine or aminooxazine derivative having amino linker |
| US8999980B2 (en) | 2009-12-11 | 2015-04-07 | Shionogi & Co., Ltd. | Oxazine derivatives |
| US20120258961A1 (en) | 2009-12-24 | 2012-10-11 | Shionogi & Co., Ltd. | 4-amino-1,3-thiazine or oxazine derivative |
| WO2011080176A1 (en) | 2009-12-31 | 2011-07-07 | Novartis Ag | Pyrazine derivatives and their use in the treatment of neurological disorders |
| 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) |
| WO2012057247A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
| EP2655376B1 (en) | 2010-12-22 | 2017-08-23 | Janssen Pharmaceutica NV | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| US9242943B2 (en) | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| WO2012117027A1 (en) | 2011-03-01 | 2012-09-07 | Janssen Pharmaceutica Nv | 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
| CN103415521B (zh) | 2011-03-09 | 2016-01-06 | 詹森药业有限公司 | 用作β分泌酶（BACE）抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物 |
| KR20140084146A (ko) | 2011-10-13 | 2014-07-04 | 노파르티스 아게 | 신규 옥사진 유도체 및 질환의 치료에서의 그의 용도 |
-
2012
- 2012-02-29 WO PCT/EP2012/053455 patent/WO2012117027A1/en not_active Ceased
- 2012-02-29 UA UAA201308783A patent/UA109800C2/ru unknown
- 2012-02-29 PT PT127072767T patent/PT2681219E/pt unknown
- 2012-02-29 EP EP12707276.7A patent/EP2681219B1/en active Active
- 2012-02-29 US US14/002,169 patent/US9346811B2/en not_active Expired - Fee Related
- 2012-02-29 EA EA201391251A patent/EA022649B1/ru not_active IP Right Cessation
- 2012-02-29 DK DK12707276.7T patent/DK2681219T3/en active
- 2012-02-29 HR HRP20160030TT patent/HRP20160030T1/hr unknown
- 2012-02-29 ES ES12707276.7T patent/ES2558779T3/es active Active
- 2012-02-29 MX MX2013010040A patent/MX338333B/es active IP Right Grant
- 2012-02-29 MY MYPI2013003200A patent/MY161407A/en unknown
- 2012-02-29 PL PL12707276T patent/PL2681219T3/pl unknown
- 2012-02-29 SI SI201230429T patent/SI2681219T1/sl unknown
- 2012-02-29 HU HUE12707276A patent/HUE026338T2/en unknown
- 2012-02-29 SG SG2013064746A patent/SG192963A1/en unknown
- 2012-02-29 JP JP2013555862A patent/JP5853033B2/ja not_active Expired - Fee Related
- 2012-02-29 CA CA2824360A patent/CA2824360C/en active Active
- 2012-02-29 BR BR112013022039A patent/BR112013022039A2/pt not_active Application Discontinuation
- 2012-02-29 PH PH1/2013/501807A patent/PH12013501807A1/en unknown
- 2012-02-29 AU AU2012222394A patent/AU2012222394B2/en not_active Ceased
- 2012-02-29 CN CN201280011146.5A patent/CN103415519B/zh not_active Expired - Fee Related
- 2012-02-29 KR KR1020137022392A patent/KR102012671B1/ko not_active Expired - Fee Related
-
2013
- 2013-08-28 IL IL228158A patent/IL228158A/en active IP Right Grant
- 2013-08-28 CL CL2013002486A patent/CL2013002486A1/es unknown
- 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 |