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 (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2416603C9 (ru) | 2005-10-25 | 2012-06-20 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
| 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 |
| TWI488852B (zh) | 2009-12-11 | 2015-06-21 | Shionogi & Co | 衍生物 |
| KR101730937B1 (ko) | 2010-06-09 | 2017-04-27 | 얀센 파마슈티카 엔.브이. | 베타-세크레타아제(ｂａｃｅ) 저해제로 유용한 5,6-디하이드로-2ｈ-[1,4]옥사진-3-일-아민 유도체 |
| JP5766198B2 (ja) | 2010-10-29 | 2015-08-19 | 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 |
| 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 |
| SG191097A1 (en) | 2010-12-22 | 2013-08-30 | Janssen Pharmaceutica Nv | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| EP2683721B1 (en) | 2011-03-09 | 2015-01-28 | Janssen Pharmaceutica N.V. | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
| BR112013033488B8 (pt) | 2011-06-27 | 2022-11-22 | Eisai R&D Man Co Ltd | Métodos para facilitar o diagnóstico do comprometimento cognitivo devido a doença de alzheimer ou comprometimento cognitivo leve (mci)e kit |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| WO2014198854A1 (en) * | 2013-06-12 | 2014-12-18 | 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) |
| CA2912156C (en) | 2013-06-12 | 2021-07-20 | 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 (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 |
| MX2017008083A (es) | 2014-12-18 | 2017-10-31 | Janssen Pharmaceutica Nv | Compuestos 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2h-pirrol-5-amina inhibidores de beta-secretasa. |
| WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | 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 |
| AU2020321955A1 (en) | 2019-07-30 | 2022-03-17 | Eikonizo Therapapeutics, Inc. | HDAC6 inhibitors and uses thereof |
| IL316201A (en) | 2022-04-08 | 2024-12-01 | Eikonizo Therapeutics Inc | Oxadiazole HDAC6 inhibitors and their uses |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1747949A (zh) * | 2002-12-20 | 2006-03-15 | 法马西亚公司 | 无环吡唑化合物 |
| RU2008100164A (ru) * | 2005-06-14 | 2009-07-20 | Шеринг Корпорейшн (US) | Получение и применение соединений в качестве ингибиторов протеаз |
| 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 US US13/825,139 patent/US8609660B2/en not_active Expired - Fee Related
- 2011-09-20 WO PCT/EP2011/066343 patent/WO2012038438A1/en not_active Ceased
- 2011-09-20 KR KR1020137007365A patent/KR101962216B1/ko not_active Expired - Fee Related
- 2011-09-20 ES ES11757886.4T patent/ES2529641T3/es active Active
- 2011-09-20 IN IN782MUN2013 patent/IN2013MN00782A/en unknown
- 2011-09-20 CN CN201180045440.3A patent/CN103097389B/zh not_active Expired - Fee Related
- 2011-09-20 BR BR112013006353A patent/BR112013006353A2/pt not_active IP Right Cessation
- 2011-09-20 CA CA2807904A patent/CA2807904C/en not_active Expired - Fee Related
- 2011-09-20 MY MYPI2013000589A patent/MY160138A/en unknown
- 2011-09-20 SG SG2013015136A patent/SG188338A1/en unknown
- 2011-09-20 AU AU2011306941A patent/AU2011306941B2/en not_active Ceased
- 2011-09-20 MX MX2013003246A patent/MX2013003246A/es active IP Right Grant
- 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 PH PH1/2013/500345A patent/PH12013500345A1/en unknown
- 2011-09-20 EA EA201390419A patent/EA021723B1/ru not_active IP Right Cessation
- 2011-09-20 JP JP2013528719A patent/JP5797756B2/ja not_active Expired - Fee Related
-
2013
- 2013-03-20 CO CO13055809A patent/CO6660450A2/es unknown
- 2013-03-20 ZA ZA2013/02128A patent/ZA201302128B/en unknown
- 2013-03-20 IL IL225349A patent/IL225349A/en active IP Right Grant
- 2013-03-21 CL CL2013000782A patent/CL2013000782A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20130110161A (ko) | 2013-10-08 |
| EA201390419A1 (ru) | 2013-07-30 |
| ZA201302128B (en) | 2014-08-27 |
| EP2619207B1 (en) | 2014-11-12 |
| EA021723B1 (ru) | 2015-08-31 |
| WO2012038438A1 (en) | 2012-03-29 |
| CO6660450A2 (es) | 2013-04-30 |
| JP2013540740A (ja) | 2013-11-07 |
| PH12013500345A1 (en) | 2022-03-30 |
| JP5797756B2 (ja) | 2015-10-21 |
| NZ606848A (en) | 2015-01-30 |
| KR101962216B1 (ko) | 2019-03-26 |
| US8609660B2 (en) | 2013-12-17 |
| CA2807904A1 (en) | 2012-03-29 |
| HK1182391A1 (zh) | 2013-11-29 |
| CL2013000782A1 (es) | 2013-08-09 |
| CN103097389B (zh) | 2015-10-14 |
| ES2529641T3 (es) | 2015-02-24 |
| SG188338A1 (en) | 2013-04-30 |
| BR112013006353A2 (pt) | 2024-01-16 |
| IN2013MN00782A (es) | 2015-06-12 |
| US20130190318A1 (en) | 2013-07-25 |
| IL225349A (en) | 2016-07-31 |
| EP2619207A1 (en) | 2013-07-31 |
| IL225349A0 (en) | 2013-06-27 |
| MY160138A (en) | 2017-02-28 |
| CA2807904C (en) | 2018-09-11 |
| AU2011306941A1 (en) | 2013-02-28 |
| CN103097389A (zh) | 2013-05-08 |
| AU2011306941B2 (en) | 2014-06-12 |
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| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |