MX2013003246A - Derivados de 4, 7-dihidro-pirazolo [1, 5-a] pirazin-6-ilamina utiles como inhibidores de beta-secretasa (bace). - Google Patents
Derivados de 4, 7-dihidro-pirazolo [1, 5-a] pirazin-6-ilamina utiles como inhibidores de beta-secretasa (bace).Info
- Publication number
- MX2013003246A MX2013003246A MX2013003246A MX2013003246A MX2013003246A MX 2013003246 A MX2013003246 A MX 2013003246A MX 2013003246 A MX2013003246 A MX 2013003246A MX 2013003246 A MX2013003246 A MX 2013003246A MX 2013003246 A MX2013003246 A MX 2013003246A
- Authority
- MX
- Mexico
- Prior art keywords
- beta
- dementia
- bace
- secretase
- 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
- JGRFABHJUCHTPN-UHFFFAOYSA-N 4,7-dihydropyrazolo[1,5-a]pyrazin-6-amine Chemical class C1C(N)=NCC2=CC=NN21 JGRFABHJUCHTPN-UHFFFAOYSA-N 0.000 title 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 4
- 206010012289 Dementia Diseases 0.000 abstract 4
- 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
- 101000894895 Homo sapiens 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
- 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
- 201000002832 Lewy body dementia Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 206010039966 Senile dementia Diseases 0.000 abstract 1
- 206010044688 Trisomy 21 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
- A61P25/28—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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invención se refiere a derivados novedosos de 4, 7-dihidro-pirazolo[1 ,5-a]pirazin-6-il-amina como inhibidores de beta-secretasa, también conocida como la enzima de corte de amiloide en el sitio beta, BACE, BACE1, Asp2 o memapsin2; la invención también está dirigida a composiciones farmacéuticas que comprenden estos compuestos, a procedimientos para preparar estos compuestos y composiciones, y al uso de estos compuestos y composiciones para la prevención y tratamiento de trastornos en los que está implicada la beta-secretasa, tales como la enfermedad de Alzheimer (AD), deterioro cognitivo leve, senilidad, demencia, demencia con cuerpos de Lewy, síndrome de Down, demencia asociada con derrame cerebral, demencia asociada con enfermedad de Parkinson o demencia asociada con beta-amiloide.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10178315 | 2010-09-22 | ||
| EP11157858 | 2011-03-11 | ||
| PCT/EP2011/066343 WO2012038438A1 (en) | 2010-09-22 | 2011-09-20 | 4,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-6-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2013003246A true MX2013003246A (es) | 2013-05-22 |
Family
ID=45873470
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2013003246A MX2013003246A (es) | 2010-09-22 | 2011-09-20 | Derivados de 4, 7-dihidro-pirazolo [1, 5-a] pirazin-6-ilamina utiles como inhibidores de beta-secretasa (bace). |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8609660B2 (es) |
| EP (1) | EP2619207B1 (es) |
| JP (1) | JP5797756B2 (es) |
| KR (1) | KR101962216B1 (es) |
| CN (1) | CN103097389B (es) |
| AU (1) | AU2011306941B2 (es) |
| BR (1) | BR112013006353A2 (es) |
| CA (1) | CA2807904C (es) |
| CL (1) | CL2013000782A1 (es) |
| CO (1) | CO6660450A2 (es) |
| EA (1) | EA021723B1 (es) |
| ES (1) | ES2529641T3 (es) |
| IL (1) | IL225349A (es) |
| IN (1) | IN2013MN00782A (es) |
| MX (1) | MX2013003246A (es) |
| MY (1) | MY160138A (es) |
| NZ (1) | NZ606848A (es) |
| PH (1) | PH12013500345A1 (es) |
| SG (1) | SG188338A1 (es) |
| WO (1) | WO2012038438A1 (es) |
| ZA (1) | ZA201302128B (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
| US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
| WO2010047372A1 (ja) | 2008-10-22 | 2010-04-29 | 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 |
| RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| AR081587A1 (es) | 2010-06-09 | 2012-10-03 | Janssen Pharmaceutica Nv | DERIVADOS DE 5,6-DIHIDRO-2H-[1,4]OXAZIN-3-IL-AMINA UTILES COMO INHIBIDORES DE LA b-SECRETASA (BACE) |
| CA2816285A1 (en) | 2010-10-29 | 2012-05-03 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| ES2648143T3 (es) | 2010-12-22 | 2017-12-28 | Janssen Pharmaceutica Nv | Derivados de 5,6-dihidro-imidazo[1,2-a]pirazin-8-ilamina útiles como inhibidores de la beta-secretasa (BACE) |
| JP5853035B2 (ja) | 2011-03-09 | 2016-02-09 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ | β−セクレターゼ（ＢＡＣＥ）の阻害剤として有用な３，４−ジヒドロ−ピロロ［１，２−ａ］ピラジン−１−イルアミン誘導体 |
| 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 |
| CA2840196C (en) | 2011-06-27 | 2022-09-20 | Eisai R&D Management Co., Ltd. | Microrna biomarkers indicative of alzheimer's disease |
| JP2016501827A (ja) | 2012-10-24 | 2016-01-21 | 塩野義製薬株式会社 | Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
| EP3008067B1 (en) | 2013-06-12 | 2017-03-29 | Janssen Pharmaceutica N.V. | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (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) |
| 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 |
| JP2017538753A (ja) | 2014-12-18 | 2017-12-28 | ヤンセン ファーマシューティカ エヌ．ベー． | ２，３，４，５−テトラヒドロピリジン−６−アミンおよび３，４−ジヒドロ−２Ｈ−ピロール−５−アミンの化合物のβセクレターゼ阻害剤 |
| US10357493B2 (en) | 2017-03-10 | 2019-07-23 | Selenity Therapeutics (Bermuda), Ltd. | Metalloenzyme inhibitor compounds |
| WO2019025250A1 (en) | 2017-08-04 | 2019-02-07 | Basf Se | SUBSTITUTED TRIFLUOROMETHYLOXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI |
| CN108440320A (zh) * | 2018-05-09 | 2018-08-24 | 上海凌凯医药科技有限公司 | 一种高手性选择性合成α-双取代α-氨基酸的方法 |
| CN114727974A (zh) | 2019-07-30 | 2022-07-08 | 艾科尼佐治疗股份有限公司 | Hdac6抑制剂及其用途 |
| WO2022169985A1 (en) | 2021-02-03 | 2022-08-11 | Eikonizo Therapeutics, Inc. | Hdac6 inhibitors and uses thereof |
| AU2023250964A1 (en) | 2022-04-08 | 2024-11-07 | Eikonizo Therapeutics, Inc. | Oxadiazole hdac6 inhibitors and uses thereof |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US8722708B2 (en) * | 2005-06-14 | 2014-05-13 | Merck Sharp & Dohme Inc. | Substituted isoindolines as aspartyl protease inhibitors |
| TW200804290A (en) * | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| WO2011002409A1 (en) * | 2009-07-02 | 2011-01-06 | Astrazeneca Ab | 5h-pyrrolo[3,4-£>]pyrazin-7-amine derivatives inhibitors of beta-secretase |
-
2011
- 2011-09-20 EP EP11757886.4A patent/EP2619207B1/en active Active
- 2011-09-20 NZ NZ606848A patent/NZ606848A/en not_active IP Right Cessation
- 2011-09-20 CN CN201180045440.3A patent/CN103097389B/zh not_active Expired - Fee Related
- 2011-09-20 SG SG2013015136A patent/SG188338A1/en unknown
- 2011-09-20 AU AU2011306941A patent/AU2011306941B2/en not_active Ceased
- 2011-09-20 EA EA201390419A patent/EA021723B1/ru not_active IP Right Cessation
- 2011-09-20 ES ES11757886.4T patent/ES2529641T3/es active Active
- 2011-09-20 WO PCT/EP2011/066343 patent/WO2012038438A1/en not_active Ceased
- 2011-09-20 US US13/825,139 patent/US8609660B2/en not_active Expired - Fee Related
- 2011-09-20 JP JP2013528719A patent/JP5797756B2/ja not_active Expired - Fee Related
- 2011-09-20 MY MYPI2013000589A patent/MY160138A/en unknown
- 2011-09-20 CA CA2807904A patent/CA2807904C/en not_active Expired - Fee Related
- 2011-09-20 BR BR112013006353A patent/BR112013006353A2/pt not_active IP Right Cessation
- 2011-09-20 IN IN782MUN2013 patent/IN2013MN00782A/en unknown
- 2011-09-20 PH PH1/2013/500345A patent/PH12013500345A1/en unknown
- 2011-09-20 MX MX2013003246A patent/MX2013003246A/es active IP Right Grant
- 2011-09-20 KR KR1020137007365A patent/KR101962216B1/ko not_active Expired - Fee Related
-
2013
- 2013-03-20 IL IL225349A patent/IL225349A/en active IP Right Grant
- 2013-03-20 ZA ZA2013/02128A patent/ZA201302128B/en unknown
- 2013-03-20 CO CO13055809A patent/CO6660450A2/es unknown
- 2013-03-21 CL CL2013000782A patent/CL2013000782A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL225349A0 (en) | 2013-06-27 |
| IL225349A (en) | 2016-07-31 |
| MY160138A (en) | 2017-02-28 |
| ZA201302128B (en) | 2014-08-27 |
| CA2807904C (en) | 2018-09-11 |
| JP2013540740A (ja) | 2013-11-07 |
| HK1182391A1 (zh) | 2013-11-29 |
| EA201390419A1 (ru) | 2013-07-30 |
| EP2619207A1 (en) | 2013-07-31 |
| ES2529641T3 (es) | 2015-02-24 |
| CL2013000782A1 (es) | 2013-08-09 |
| US20130190318A1 (en) | 2013-07-25 |
| EA021723B1 (ru) | 2015-08-31 |
| JP5797756B2 (ja) | 2015-10-21 |
| IN2013MN00782A (es) | 2015-06-12 |
| US8609660B2 (en) | 2013-12-17 |
| SG188338A1 (en) | 2013-04-30 |
| PH12013500345A1 (en) | 2022-03-30 |
| BR112013006353A2 (pt) | 2024-01-16 |
| CO6660450A2 (es) | 2013-04-30 |
| AU2011306941A1 (en) | 2013-02-28 |
| NZ606848A (en) | 2015-01-30 |
| KR101962216B1 (ko) | 2019-03-26 |
| CA2807904A1 (en) | 2012-03-29 |
| CN103097389B (zh) | 2015-10-14 |
| CN103097389A (zh) | 2013-05-08 |
| EP2619207B1 (en) | 2014-11-12 |
| AU2011306941B2 (en) | 2014-06-12 |
| KR20130110161A (ko) | 2013-10-08 |
| WO2012038438A1 (en) | 2012-03-29 |
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Legal Events
| Date | Code | Title | Description |
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| FG | Grant or registration |