MY170715A - 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (bace) - Google Patents
5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (bace)Info
- Publication number
- MY170715A MY170715A MYPI2013002076A MYPI2013002076A MY170715A MY 170715 A MY170715 A MY 170715A MY PI2013002076 A MYPI2013002076 A MY PI2013002076A MY PI2013002076 A MYPI2013002076 A MY PI2013002076A MY 170715 A MY170715 A MY 170715A
- Authority
- MY
- Malaysia
- Prior art keywords
- beta
- secretase
- dementia
- bace
- pyrazin
- Prior art date
Links
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract 3
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- DZJJKLGKUNDJBW-UHFFFAOYSA-N 5,6-dihydroimidazo[1,2-a]pyrazin-8-amine Chemical class NC1=NCCN2C=CN=C12 DZJJKLGKUNDJBW-UHFFFAOYSA-N 0.000 title 1
- 101150058765 BACE1 gene Proteins 0.000 title 1
- 206010012289 Dementia Diseases 0.000 abstract 4
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 abstract 2
- 101710150192 Beta-secretase 1 Proteins 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- 206010059245 Angiopathy Diseases 0.000 abstract 1
- -1 BACEl Proteins 0.000 abstract 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 1
- 201000002832 Lewy body dementia Diseases 0.000 abstract 1
- 208000005314 Multi-Infarct Dementia Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 206010039966 Senile dementia Diseases 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 206010044688 Trisomy 21 Diseases 0.000 abstract 1
- 201000004810 Vascular dementia Diseases 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- IXHBTMCLRNMKHZ-LBPRGKRZSA-N levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 abstract 1
- 208000027061 mild cognitive impairment Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 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
- C07D487/02—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
- A61P25/28—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)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
The present invention relates to novel 5,6-dihydro-imidazo[l,2-a]pyrazin-8- ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACEl, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebrovascular amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid. (No suitable figure)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10196568 | 2010-12-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MY170715A true MY170715A (en) | 2019-08-27 |
Family
ID=43923528
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MYPI2013002076A MY170715A (en) | 2010-12-22 | 2011-12-21 | 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US9840507B2 (en) |
| EP (1) | EP2655376B1 (en) |
| JP (1) | JP5834091B2 (en) |
| KR (1) | KR101866987B1 (en) |
| CN (1) | CN103403007B (en) |
| AU (1) | AU2011347377B2 (en) |
| BR (1) | BR112013015430A2 (en) |
| CA (1) | CA2819175C (en) |
| CO (1) | CO6721049A2 (en) |
| EA (1) | EA022409B1 (en) |
| ES (1) | ES2648143T3 (en) |
| IL (1) | IL227054A (en) |
| MX (1) | MX347912B (en) |
| MY (1) | MY170715A (en) |
| NZ (1) | NZ610948A (en) |
| SG (1) | SG191097A1 (en) |
| UA (1) | UA109459C2 (en) |
| WO (1) | WO2012085038A1 (en) |
| ZA (1) | ZA201304646B (en) |
Families Citing this family (23)
| 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 (en) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | Aminodihydrothiazine derivatives substituted with cyclic groups |
| KR101324426B1 (en) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING β-SECRETASE-INHIBITING ACTIVITY |
| CN102186841A (en) | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 2-aminopyridin-4-one and 2-aminopyridine derivative both having bace1-inhibiting activity |
| MX2012006491A (en) | 2009-12-11 | 2012-07-03 | Shionogi & Co | OXAZINE DERIVATIVES |
| MX339640B (en) | 2010-06-09 | 2016-06-01 | Janssen Pharmaceutica Nv * | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace). |
| JP5816630B2 (en) | 2010-10-29 | 2015-11-18 | 塩野義製薬株式会社 | Naphthyridine derivatives |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | Fused 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) |
| CN103415519B (en) | 2011-03-01 | 2016-03-02 | 詹森药业有限公司 | As 6,7-dihydro-pyrazol [1, the 5-a] pyrazine-4-yl amine derivatives that beta-secretase (BACE) inhibitor is useful |
| 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 | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| KR102243134B1 (en) * | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase(bace) |
| MX368326B (en) * | 2013-06-12 | 2019-09-27 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace). |
| BR112015030597A2 (en) * | 2013-06-12 | 2017-07-25 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-6,7-dihydro [1,2,3] triazolo [1,5-a] pyrazine derivatives as beta-secretase (bace) inhibitors |
| CN104016925B (en) * | 2014-06-17 | 2016-03-30 | 遵义医学院 | The synthetic method of 4-alkylimidazole-2-carboxylic acid |
| ES2768823T3 (en) | 2014-12-18 | 2020-06-23 | Janssen Pharmaceutica Nv | 2,3,4,5-Tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrole-5-amine derivatives useful as beta-secretase inhibitors |
| LT3374359T (en) * | 2015-11-09 | 2020-03-25 | Astrazeneca Ab | Dihydroimidazopyrazinone derivatives useful in the treatment of cancer |
| WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | Metalloenzyme inhibitor compounds |
| AU2020321955A1 (en) | 2019-07-30 | 2022-03-17 | Eikonizo Therapapeutics, Inc. | HDAC6 inhibitors and uses thereof |
| TW202345813A (en) | 2022-04-08 | 2023-12-01 | 美商艾科尼佐療法股份有限公司 | Oxadiazole hdac6 inhibitors and uses thereof |
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| WO2011077726A1 (en) | 2009-12-24 | 2011-06-30 | 塩野義製薬株式会社 | 4-amino-1,3-thiazine or oxazine derivative |
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| BR112013006353A2 (en) | 2010-09-22 | 2024-01-16 | Janssen Pharmaceutica Nv | 4,7-DI-HYFRO-PYRAZOLO[1,5-A]PYRAZIN-6-YLAMINE DERIVATIVES USEFUL AS BETA-SECRETASE (BACE) INHIBITORS |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | Fused 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) |
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| CN103415519B (en) | 2011-03-01 | 2016-03-02 | 詹森药业有限公司 | As 6,7-dihydro-pyrazol [1, the 5-a] pyrazine-4-yl amine derivatives that beta-secretase (BACE) inhibitor is useful |
| 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 |
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| BR112015030597A2 (en) | 2013-06-12 | 2017-07-25 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-6,7-dihydro [1,2,3] triazolo [1,5-a] pyrazine derivatives as beta-secretase (bace) inhibitors |
| MX368326B (en) | 2013-06-12 | 2019-09-27 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace). |
| KR102243134B1 (en) | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase(bace) |
| ES2768823T3 (en) | 2014-12-18 | 2020-06-23 | Janssen Pharmaceutica Nv | 2,3,4,5-Tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrole-5-amine derivatives useful as beta-secretase inhibitors |
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2011
- 2011-12-21 EP EP11804561.6A patent/EP2655376B1/en active Active
- 2011-12-21 CA CA2819175A patent/CA2819175C/en active Active
- 2011-12-21 KR KR1020137019224A patent/KR101866987B1/en not_active Expired - Fee Related
- 2011-12-21 CN CN201180068086.6A patent/CN103403007B/en not_active Expired - Fee Related
- 2011-12-21 ES ES11804561.6T patent/ES2648143T3/en active Active
- 2011-12-21 NZ NZ610948A patent/NZ610948A/en not_active IP Right Cessation
- 2011-12-21 JP JP2013545343A patent/JP5834091B2/en not_active Expired - Fee Related
- 2011-12-21 MX MX2013007294A patent/MX347912B/en active IP Right Grant
- 2011-12-21 EA EA201390932A patent/EA022409B1/en not_active IP Right Cessation
- 2011-12-21 SG SG2013044730A patent/SG191097A1/en unknown
- 2011-12-21 AU AU2011347377A patent/AU2011347377B2/en not_active Ceased
- 2011-12-21 MY MYPI2013002076A patent/MY170715A/en unknown
- 2011-12-21 US US13/995,523 patent/US9840507B2/en not_active Expired - Fee Related
- 2011-12-21 WO PCT/EP2011/073522 patent/WO2012085038A1/en not_active Ceased
- 2011-12-21 UA UAA201306422A patent/UA109459C2/en unknown
- 2011-12-21 BR BR112013015430A patent/BR112013015430A2/en active Search and Examination
-
2013
- 2013-06-19 IL IL227054A patent/IL227054A/en active IP Right Grant
- 2013-06-21 ZA ZA2013/04646A patent/ZA201304646B/en unknown
- 2013-06-25 CO CO13150832A patent/CO6721049A2/en unknown
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| EP2655376B1 (en) | 2017-08-23 |
| MX2013007294A (en) | 2013-08-26 |
| ZA201304646B (en) | 2014-12-23 |
| US9840507B2 (en) | 2017-12-12 |
| KR20130132556A (en) | 2013-12-04 |
| ES2648143T3 (en) | 2017-12-28 |
| JP5834091B2 (en) | 2015-12-16 |
| MX347912B (en) | 2017-05-17 |
| WO2012085038A1 (en) | 2012-06-28 |
| CA2819175C (en) | 2019-01-08 |
| EA201390932A1 (en) | 2013-11-29 |
| AU2011347377B2 (en) | 2016-03-03 |
| NZ610948A (en) | 2014-06-27 |
| CN103403007B (en) | 2015-12-09 |
| AU2011347377A1 (en) | 2013-06-13 |
| EP2655376A1 (en) | 2013-10-30 |
| EA022409B1 (en) | 2015-12-30 |
| HK1189221A1 (en) | 2014-05-30 |
| SG191097A1 (en) | 2013-08-30 |
| JP2014500293A (en) | 2014-01-09 |
| KR101866987B1 (en) | 2018-07-19 |
| CA2819175A1 (en) | 2012-06-28 |
| IL227054A (en) | 2016-09-29 |
| UA109459C2 (en) | 2015-08-25 |
| BR112013015430A2 (en) | 2016-09-20 |
| US20130274266A1 (en) | 2013-10-17 |
| CN103403007A (en) | 2013-11-20 |
| CO6721049A2 (en) | 2013-07-31 |
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