SI2681219T1 - Derivati 6,7-dihidro-pirazolo(1,5-a)pirazin-4-ilamina uporabni kot inhibitorji beta-sekretaze (BACE) - Google Patents
Derivati 6,7-dihidro-pirazolo(1,5-a)pirazin-4-ilamina uporabni kot inhibitorji beta-sekretaze (BACE)Info
- Publication number
- SI2681219T1 SI2681219T1 SI201230429T SI201230429T SI2681219T1 SI 2681219 T1 SI2681219 T1 SI 2681219T1 SI 201230429 T SI201230429 T SI 201230429T SI 201230429 T SI201230429 T SI 201230429T SI 2681219 T1 SI2681219 T1 SI 2681219T1
- Authority
- SI
- Slovenia
- Prior art keywords
- bace
- secretase
- pyrazin
- pyrazolo
- dihydro
- Prior art date
Links
- IWEFEVCBSHDDLF-UHFFFAOYSA-N 6,7-dihydropyrazolo[1,5-a]pyrazin-4-amine Chemical class NC1=NCCN2N=CC=C12 IWEFEVCBSHDDLF-UHFFFAOYSA-N 0.000 title 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title 1
- 101150058765 BACE1 gene Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 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
- C07D487/02—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)
- Psychology (AREA)
- Hospice & Palliative Care (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 (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11156463 | 2011-03-01 | ||
| EP12707276.7A EP2681219B1 (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) |
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| SI2681219T1 true SI2681219T1 (sl) | 2016-02-29 |
Family
ID=45808845
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI201230429T SI2681219T1 (sl) | 2011-03-01 | 2012-02-29 | Derivati 6,7-dihidro-pirazolo(1,5-a)pirazin-4-ilamina uporabni kot inhibitorji beta-sekretaze (BACE) |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US9346811B2 (https=) |
| EP (1) | EP2681219B1 (https=) |
| JP (1) | JP5853033B2 (https=) |
| KR (1) | KR102012671B1 (https=) |
| CN (1) | CN103415519B (https=) |
| AU (1) | AU2012222394B2 (https=) |
| BR (1) | BR112013022039A2 (https=) |
| CA (1) | CA2824360C (https=) |
| CL (1) | CL2013002486A1 (https=) |
| CO (1) | CO6751282A2 (https=) |
| CY (1) | CY1117663T1 (https=) |
| DK (1) | DK2681219T3 (https=) |
| EA (1) | EA022649B1 (https=) |
| ES (1) | ES2558779T3 (https=) |
| HR (1) | HRP20160030T1 (https=) |
| HU (1) | HUE026338T2 (https=) |
| IL (1) | IL228158A (https=) |
| MX (1) | MX338333B (https=) |
| MY (1) | MY161407A (https=) |
| PH (1) | PH12013501807A1 (https=) |
| PL (1) | PL2681219T3 (https=) |
| PT (1) | PT2681219E (https=) |
| SG (1) | SG192963A1 (https=) |
| SI (1) | SI2681219T1 (https=) |
| UA (1) | UA109800C2 (https=) |
| WO (1) | WO2012117027A1 (https=) |
| ZA (1) | ZA201306545B (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2628074C (en) | 2005-10-25 | 2014-01-14 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| US8653067B2 (en) | 2007-04-24 | 2014-02-18 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating Alzheimer's disease |
| JP5383484B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | 環式基で置換されたアミノジヒドロチアジン誘導体 |
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| CN102186841A (zh) | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物 |
| MX2012006491A (es) | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
| MX339640B (es) | 2010-06-09 | 2016-06-01 | Janssen Pharmaceutica Nv * | Derivados de 5, 6-dihidro-2h-[1, 4] oxazin-3-il-amina utiles como inhibidores de la beta-secretasa (bace). |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| JP5816630B2 (ja) | 2010-10-29 | 2015-11-18 | 塩野義製薬株式会社 | ナフチリジン誘導体 |
| 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) |
| CN103415519B (zh) | 2011-03-01 | 2016-03-02 | 詹森药业有限公司 | 作为β-分泌酶(BACE)抑制剂有用的6,7-二氢-吡唑[1,5-a]吡嗪-4-基胺衍生物 |
| DK3031812T3 (en) | 2011-03-01 | 2018-09-17 | NuCana plc | CHEMICAL COMPOUNDS |
| AU2012224632B2 (en) | 2011-03-09 | 2016-06-16 | Janssen Pharmaceutica Nv | 3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives useful as inhibitors of beta-secretase (BACE) |
| 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 |
| KR102243134B1 (ko) * | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진 유도체 |
| 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). |
| BR112015030597A2 (pt) * | 2013-06-12 | 2017-07-25 | Janssen Pharmaceutica Nv | derivados 4-amino-6-fenil-6,7-di-hidro[1,2,3]triazolo[1,5-a]pirazina como inibidores de beta-secretase (bace) |
| ES2768823T3 (es) | 2014-12-18 | 2020-06-23 | Janssen Pharmaceutica Nv | Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa |
| WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | 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 |
| MX2021008050A (es) | 2019-01-11 | 2021-08-05 | Shionogi & Co | Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2). |
| AU2020321955A1 (en) | 2019-07-30 | 2022-03-17 | Eikonizo Therapapeutics, Inc. | HDAC6 inhibitors and uses thereof |
| TW202345813A (zh) | 2022-04-08 | 2023-12-01 | 美商艾科尼佐療法股份有限公司 | 㗁二唑hdac6抑制劑及其用途 |
| KR20250022711A (ko) * | 2022-06-13 | 2025-02-17 | 시오노기 앤드 컴파니, 리미티드 | 다이하이드로피리딘온 유도체 또는 그 용매화물의 결정 |
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| TW224974B (https=) | 1991-07-02 | 1994-06-11 | Hoffmann La Roche | |
| KR20050008691A (ko) | 2002-04-19 | 2005-01-21 | 셀룰러 지노믹스 아이엔씨 | 이미다조[1,2-a]피라진-8-일 아민, 그의 제조방법 및사용방법 |
| NZ538685A (en) | 2002-09-23 | 2008-02-29 | Schering Corp | Imidazopyrazines as cyclin dependent kinase inhibitors |
| ZA200504898B (en) | 2002-12-20 | 2006-11-29 | Pharmacia Corp | Acyclic pyrazole compounds |
| WO2004092177A1 (en) * | 2003-04-09 | 2004-10-28 | Biogen Idec Ma Inc. | Triazolopyrazines and methods of making and using the same |
| WO2005037832A2 (en) | 2003-10-15 | 2005-04-28 | Targacept, Inc. | Azabicycyclic compounds for relieving pain and treating central nervous system disorders |
| US7618978B2 (en) | 2004-04-22 | 2009-11-17 | Eli Lilly And Company | Amides as BACE inhibitors |
| BRPI0512213A (pt) | 2004-06-16 | 2008-02-19 | Wyeth Corp | método para tratamento, prevenção ou melhora de uma doença ou distúrbio; composição farmacêutica; processo para a preparação de um composto; e uso de um composto |
| 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 |
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| WO2006138265A2 (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 |
| CA2628074C (en) | 2005-10-25 | 2014-01-14 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| CN101460480A (zh) | 2006-04-05 | 2009-06-17 | 阿斯利康(瑞典)有限公司 | 2-氨基嘧啶-4-酮类化合物及其用于治疗或预防Aβ相关病理的用途 |
| GB2443654A (en) | 2006-05-30 | 2008-05-14 | Matthew Emmerson Allen | System for detecting and testing drivers who show abnormal driving behaviour. |
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| 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 |
| JP5383484B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | 環式基で置換されたアミノジヒドロチアジン誘導体 |
| TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| JP2011502122A (ja) | 2007-10-30 | 2011-01-20 | アリーナ ファーマシューティカルズ, インコーポレイテッド | ヒスタミンh3関連障害の治療のために有用なヒスタミンh3−レセプターの調節因子としてのビフェニル誘導体 |
| WO2009097278A1 (en) | 2008-01-28 | 2009-08-06 | Janssen Pharmaceutica N.V. | 6-SUBSTITUTED-THIO-2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE) |
| WO2009102468A1 (en) | 2008-02-13 | 2009-08-20 | 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 |
| US20120238557A1 (en) | 2009-11-13 | 2012-09-20 | Shionogi & Co., Ltd. | Aminothiazine or aminooxazine derivative having amino linker |
| MX2012006491A (es) | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
| 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 |
| NZ600136A (en) | 2009-12-31 | 2013-09-27 | Novartis Ag | Pyrazine derivatives and their use in the treatment of neurological disorders |
| MX339640B (es) * | 2010-06-09 | 2016-06-01 | Janssen Pharmaceutica Nv * | Derivados de 5, 6-dihidro-2h-[1, 4] oxazin-3-il-amina utiles como inhibidores de la beta-secretasa (bace). |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE 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) |
| US9242943B2 (en) | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| CN103415519B (zh) | 2011-03-01 | 2016-03-02 | 詹森药业有限公司 | 作为β-分泌酶(BACE)抑制剂有用的6,7-二氢-吡唑[1,5-a]吡嗪-4-基胺衍生物 |
| AU2012224632B2 (en) | 2011-03-09 | 2016-06-16 | Janssen Pharmaceutica Nv | 3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives useful as inhibitors of beta-secretase (BACE) |
| US9284284B2 (en) | 2011-10-13 | 2016-03-15 | Novartis Ag | Oxazine derivatives and their use in the treatment of disease |
-
2012
- 2012-02-29 CN CN201280011146.5A patent/CN103415519B/zh not_active Expired - Fee Related
- 2012-02-29 UA UAA201308783A patent/UA109800C2/ru unknown
- 2012-02-29 DK DK12707276.7T patent/DK2681219T3/en active
- 2012-02-29 PL PL12707276T patent/PL2681219T3/pl 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 MX MX2013010040A patent/MX338333B/es active IP Right Grant
- 2012-02-29 PH PH1/2013/501807A patent/PH12013501807A1/en unknown
- 2012-02-29 WO PCT/EP2012/053455 patent/WO2012117027A1/en not_active Ceased
- 2012-02-29 CA CA2824360A patent/CA2824360C/en active Active
- 2012-02-29 SI SI201230429T patent/SI2681219T1/sl unknown
- 2012-02-29 JP JP2013555862A patent/JP5853033B2/ja not_active Expired - Fee Related
- 2012-02-29 ES ES12707276.7T patent/ES2558779T3/es active Active
- 2012-02-29 HR HRP20160030TT patent/HRP20160030T1/hr unknown
- 2012-02-29 HU HUE12707276A patent/HUE026338T2/en unknown
- 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 BR BR112013022039A patent/BR112013022039A2/pt not_active Application Discontinuation
- 2012-02-29 EA EA201391251A patent/EA022649B1/ru not_active IP Right Cessation
- 2012-02-29 KR KR1020137022392A patent/KR102012671B1/ko not_active Expired - Fee Related
- 2012-02-29 AU AU2012222394A patent/AU2012222394B2/en not_active Ceased
-
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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