BR112013006353A2 - Derivados de 4,7-di-hifro-pirazolo[1,5-a]pirazin-6-ilamina úteis como inibidores de beta-secretase (bace) - Google Patents
Derivados de 4,7-di-hifro-pirazolo[1,5-a]pirazin-6-ilamina úteis como inibidores de beta-secretase (bace)Info
- Publication number
- BR112013006353A2 BR112013006353A2 BR112013006353A BR112013006353A BR112013006353A2 BR 112013006353 A2 BR112013006353 A2 BR 112013006353A2 BR 112013006353 A BR112013006353 A BR 112013006353A BR 112013006353 A BR112013006353 A BR 112013006353A BR 112013006353 A2 BR112013006353 A2 BR 112013006353A2
- Authority
- BR
- Brazil
- Prior art keywords
- beta
- secretase
- bace
- pyrazolo
- inhibitors
- Prior art date
Links
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract 4
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract 4
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 206010012289 Dementia Diseases 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 2
- 239000002439 beta secretase inhibitor Substances 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- 101150058765 BACE1 gene Proteins 0.000 abstract 1
- 101710150192 Beta-secretase 1 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
- 101150080892 asp2 gene Proteins 0.000 abstract 1
- -1 bace1 Proteins 0.000 abstract 1
- 238000003776 cleavage reaction Methods 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
- 238000000034 method Methods 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
- 230000007017 scission 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
derivados de 4,7-di-hifro-pirazolo[1,5-a]pirazin-6-ilamina úteis como inibidores de beta-secretase (bace). a presente invenção refere-se a novos derivados de 4,7-di-hidro-pirazolo[1,5-a]pirazim-6-ilamina como inibidores de beta-secretase, também conhecida como enzima de clivagem no sítio da amiloide, bace, bace1, asp2, ou memapsina2. a invenção também é direcionada a composições farmacêuticas compreendendo tais compostos, a processos para preparar tais compostos e composições, e ao uso de tais compostos e composições para a prevenção e tratamento de distúrbios nos quais beta-secretase está envolvida, tal como doença de alzheimer (da), déficit cognitivo leve, senilidade, demência, demências com corpos de lewy, síndrome de down, demência associada com derrame, demência associada com doença de parkinson ou demência associada com 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 |
|---|---|
| BR112013006353A2 true BR112013006353A2 (pt) | 2024-01-16 |
Family
ID=45873470
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112013006353A BR112013006353A2 (pt) | 2010-09-22 | 2011-09-20 | Derivados de 4,7-di-hifro-pirazolo[1,5-a]pirazin-6-ilamina úteis como inibidores de beta-secretase (bace) |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8609660B2 (pt) |
| EP (1) | EP2619207B1 (pt) |
| JP (1) | JP5797756B2 (pt) |
| KR (1) | KR101962216B1 (pt) |
| CN (1) | CN103097389B (pt) |
| AU (1) | AU2011306941B2 (pt) |
| BR (1) | BR112013006353A2 (pt) |
| CA (1) | CA2807904C (pt) |
| CL (1) | CL2013000782A1 (pt) |
| CO (1) | CO6660450A2 (pt) |
| EA (1) | EA021723B1 (pt) |
| ES (1) | ES2529641T3 (pt) |
| HK (1) | HK1182391A1 (pt) |
| IL (1) | IL225349A (pt) |
| IN (1) | IN2013MN00782A (pt) |
| MX (1) | MX2013003246A (pt) |
| MY (1) | MY160138A (pt) |
| NZ (1) | NZ606848A (pt) |
| SG (1) | SG188338A1 (pt) |
| WO (1) | WO2012038438A1 (pt) |
| ZA (1) | ZA201302128B (pt) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2628074C (en) | 2005-10-25 | 2014-01-14 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| CA2683887A1 (en) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group having inhibitory activity against production of amyloid beta protein |
| JP5490692B2 (ja) | 2008-06-13 | 2014-05-14 | 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 |
| EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
| EP2511268B2 (en) | 2009-12-11 | 2021-02-17 | Shionogi & Co., Ltd. | Oxazine derivative |
| WO2011154431A1 (en) | 2010-06-09 | 2011-12-15 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| EP2634186A4 (en) | 2010-10-29 | 2014-03-26 | Shionogi & Co | naphthyridine |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| CN103403007B (zh) | 2010-12-22 | 2015-12-09 | 詹森药业有限公司 | 用作β-分泌酶(BACE)抑制剂的5,6-二氢-咪唑并[1,2-a]吡嗪-8-基胺衍生物 |
| WO2012120023A1 (en) | 2011-03-09 | 2012-09-13 | Janssen Pharmaceutica Nv | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| EP2703399A4 (en) | 2011-04-26 | 2014-10-15 | Shionogi & Co | OXAZINE DERIVATIVE AND BACE-1 HEMMER THEREOF |
| JP6154809B2 (ja) | 2011-06-27 | 2017-06-28 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | アルツハイマー病を示すマイクロｒｎａバイオマーカー |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| 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) |
| CN105452251B (zh) | 2013-06-12 | 2017-12-26 | 詹森药业有限公司 | 作为β‑分泌酶(BACE)抑制剂的4‑氨基‑6‑苯基‑5,6‑二氢咪唑并[1,5‑A]吡嗪‑3(2H)‑酮衍生物 |
| EP3008066B1 (en) | 2013-06-12 | 2018-08-15 | Janssen Pharmaceutica N.V. | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
| EA031041B1 (ru) | 2014-12-18 | 2018-11-30 | Янссен Фармацевтика Нв | Соединения 2,3,4,5-тетрагидропиридин-6-амин и 3,4-дигидро-2h-пиррол-5-амин - ингибиторы бета-секретазы |
| 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 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040209897A1 (en) * | 2002-12-20 | 2004-10-21 | Pharmacia Corporation | Mitogen activated protein kinase-activated protein kinase-2 inhibiting compounds |
| EP2345411B1 (en) * | 2005-06-14 | 2013-10-02 | Merck Sharp & Dohme Corp. | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
| 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 KR KR1020137007365A patent/KR101962216B1/ko active IP Right Grant
- 2011-09-20 BR BR112013006353A patent/BR112013006353A2/pt not_active IP Right Cessation
- 2011-09-20 ES ES11757886.4T patent/ES2529641T3/es active Active
- 2011-09-20 EP EP11757886.4A patent/EP2619207B1/en active Active
- 2011-09-20 CN CN201180045440.3A patent/CN103097389B/zh 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 EA EA201390419A patent/EA021723B1/ru not_active IP Right Cessation
- 2011-09-20 IN IN782MUN2013 patent/IN2013MN00782A/en unknown
- 2011-09-20 CA CA2807904A patent/CA2807904C/en not_active Expired - Fee Related
- 2011-09-20 SG SG2013015136A patent/SG188338A1/en unknown
- 2011-09-20 WO PCT/EP2011/066343 patent/WO2012038438A1/en active Application Filing
- 2011-09-20 NZ NZ606848A patent/NZ606848A/en not_active IP Right Cessation
- 2011-09-20 MX MX2013003246A patent/MX2013003246A/es active IP Right Grant
- 2011-09-20 AU AU2011306941A patent/AU2011306941B2/en not_active Ceased
-
2013
- 2013-03-20 ZA ZA2013/02128A patent/ZA201302128B/en unknown
- 2013-03-20 IL IL225349A patent/IL225349A/en active IP Right Grant
- 2013-03-20 CO CO13055809A patent/CO6660450A2/es unknown
- 2013-03-21 CL CL2013000782A patent/CL2013000782A1/es unknown
- 2013-08-21 HK HK13109786.4A patent/HK1182391A1/zh not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| NZ606848A (en) | 2015-01-30 |
| CN103097389A (zh) | 2013-05-08 |
| KR101962216B1 (ko) | 2019-03-26 |
| EA201390419A1 (ru) | 2013-07-30 |
| US20130190318A1 (en) | 2013-07-25 |
| JP5797756B2 (ja) | 2015-10-21 |
| IL225349A (en) | 2016-07-31 |
| KR20130110161A (ko) | 2013-10-08 |
| US8609660B2 (en) | 2013-12-17 |
| CA2807904A1 (en) | 2012-03-29 |
| AU2011306941A1 (en) | 2013-02-28 |
| CL2013000782A1 (es) | 2013-08-09 |
| ZA201302128B (en) | 2014-08-27 |
| SG188338A1 (en) | 2013-04-30 |
| MY160138A (en) | 2017-02-28 |
| AU2011306941B2 (en) | 2014-06-12 |
| IN2013MN00782A (pt) | 2015-06-12 |
| MX2013003246A (es) | 2013-05-22 |
| JP2013540740A (ja) | 2013-11-07 |
| EA021723B1 (ru) | 2015-08-31 |
| WO2012038438A1 (en) | 2012-03-29 |
| CN103097389B (zh) | 2015-10-14 |
| EP2619207A1 (en) | 2013-07-31 |
| EP2619207B1 (en) | 2014-11-12 |
| CA2807904C (en) | 2018-09-11 |
| CO6660450A2 (es) | 2013-04-30 |
| ES2529641T3 (es) | 2015-02-24 |
| HK1182391A1 (zh) | 2013-11-29 |
| IL225349A0 (en) | 2013-06-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE AS 10A, 11A E 12A ANUIDADES. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2768 DE 23/01/2024. |