PE20121640A1 - Derivados de pirazina como inhibidores de bace - Google Patents
Derivados de pirazina como inhibidores de baceInfo
- Publication number
- PE20121640A1 PE20121640A1 PE2012000897A PE2012000897A PE20121640A1 PE 20121640 A1 PE20121640 A1 PE 20121640A1 PE 2012000897 A PE2012000897 A PE 2012000897A PE 2012000897 A PE2012000897 A PE 2012000897A PE 20121640 A1 PE20121640 A1 PE 20121640A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- halogen
- pyridin
- tetrahydro
- bromo
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 8
- 150000002367 halogens Chemical class 0.000 abstract 8
- 239000002253 acid Substances 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- MNNQIBXLAHVDDL-UHFFFAOYSA-N 5-bromopyridine-2-carboxylic acid Chemical compound OC(=O)C1=CC=C(Br)C=N1 MNNQIBXLAHVDDL-UHFFFAOYSA-N 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29172409P | 2009-12-31 | 2009-12-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20121640A1 true PE20121640A1 (es) | 2012-12-17 |
Family
ID=43598456
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2012000897A PE20121640A1 (es) | 2009-12-31 | 2010-12-22 | Derivados de pirazina como inhibidores de bace |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US20120277244A1 (enExample) |
| EP (1) | EP2519515B1 (enExample) |
| JP (1) | JP5600754B2 (enExample) |
| KR (1) | KR101419157B1 (enExample) |
| CN (1) | CN102712621B (enExample) |
| AU (1) | AU2010338365B2 (enExample) |
| BR (1) | BR112012015916A2 (enExample) |
| CA (1) | CA2785341A1 (enExample) |
| CL (1) | CL2012001762A1 (enExample) |
| CR (1) | CR20120332A (enExample) |
| CU (1) | CU20120099A7 (enExample) |
| EA (1) | EA201200952A1 (enExample) |
| EC (1) | ECSP12012065A (enExample) |
| ES (1) | ES2445536T3 (enExample) |
| GT (1) | GT201200219A (enExample) |
| HN (1) | HN2012001413A (enExample) |
| IL (1) | IL220268A0 (enExample) |
| MX (1) | MX2012007754A (enExample) |
| NZ (1) | NZ600136A (enExample) |
| PE (1) | PE20121640A1 (enExample) |
| PH (1) | PH12012501007A1 (enExample) |
| PL (1) | PL2519515T3 (enExample) |
| PT (1) | PT2519515E (enExample) |
| SG (1) | SG181431A1 (enExample) |
| TN (1) | TN2012000249A1 (enExample) |
| WO (1) | WO2011080176A1 (enExample) |
| ZA (1) | ZA201203614B (enExample) |
Families Citing this family (31)
| 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 |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| 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) |
| EA201291366A1 (ru) * | 2010-06-09 | 2013-04-30 | Янссен Фармацевтика Нв | Производные 5-амино-3,6-дигидро-1h-пиразин-2-она в качестве ингибиторов бета-секретазы (bace) |
| SG186408A1 (en) * | 2010-06-28 | 2013-01-30 | Janssen Pharmaceutica Nv | 3-amino-5, 6-dihydro-1h-pyrazin-2-one derivatives useful for the treatment of alzheimer's disease and other forms of dementia |
| 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) |
| US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
| KR101569260B1 (ko) | 2011-01-13 | 2015-11-13 | 노파르티스 아게 | 신규 헤테로시클릭 유도체 및 신경계 장애의 치료에서의 그의 용도 |
| EA201391033A1 (ru) * | 2011-01-13 | 2014-01-30 | Новартис Аг | Ингибиторы bace-2 для лечения метаболических расстройств |
| US9346811B2 (en) | 2011-03-01 | 2016-05-24 | Janssen Pharmaceutica Nv | 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (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 |
| EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2012138734A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| BR112013026341A2 (pt) | 2011-04-13 | 2019-09-24 | Merck Sharp & Dohe Corp. | composto, composição farmacêutica, e, método para tratar, prevenir e/ou atrasar o início de uma doença ou patologia |
| 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 |
| RU2014111055A (ru) | 2011-08-22 | 2015-09-27 | Мерк Шарп И Доум Корп. | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
| US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| 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 |
| CN104870000A (zh) | 2012-12-20 | 2015-08-26 | 默沙东公司 | 作为bace抑制剂的c5,c6氧杂环稠合的亚胺基噻嗪二氧化物化合物,组合物及其用途 |
| 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 |
| 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) |
| 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 |
| CN107011134B (zh) * | 2017-04-28 | 2021-02-05 | 浙江中欣氟材股份有限公司 | 一种2-氟-5-溴苯乙酮的合成方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL6911868A (enExample) | 1968-08-31 | 1970-03-03 | ||
| AUPQ319899A0 (en) * | 1999-10-01 | 1999-10-28 | Fujisawa Pharmaceutical Co., Ltd. | Amide compounds |
| WO2002060492A1 (en) * | 2001-01-30 | 2002-08-08 | Cytopia Pty Ltd | Methods of inhibiting kinases |
| WO2004078163A2 (en) | 2003-02-28 | 2004-09-16 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| US7728025B2 (en) | 2003-12-29 | 2010-06-01 | Banyu Pharmaceutical Co., Ltd. | 2-heteroaryl-substituted benzimidazole derivative |
| US20050215884A1 (en) * | 2004-02-27 | 2005-09-29 | Greicius Michael D | Evaluation of Alzheimer's disease using an independent component analysis of an individual's resting-state functional MRI |
| ES2537898T3 (es) * | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| PT2404919E (pt) * | 2005-11-08 | 2013-10-22 | Vertex Pharma | Composto heterocíclico útil como um modulador de transportadores de cassete de ligação a atp |
| EP2094682A2 (en) * | 2006-12-22 | 2009-09-02 | Novartis AG | Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections |
| BRPI0906962B8 (pt) | 2008-01-18 | 2021-05-25 | Eisai R&D Man Co Ltd | composto de aminodiidrotiazina fundido |
| 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 |
| UY32799A (es) * | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
| EA201291366A1 (ru) * | 2010-06-09 | 2013-04-30 | Янссен Фармацевтика Нв | Производные 5-амино-3,6-дигидро-1h-пиразин-2-она в качестве ингибиторов бета-секретазы (bace) |
| SG186408A1 (en) * | 2010-06-28 | 2013-01-30 | Janssen Pharmaceutica Nv | 3-amino-5, 6-dihydro-1h-pyrazin-2-one derivatives useful for the treatment of alzheimer's disease and other forms of dementia |
-
2010
- 2010-12-22 US US13/518,907 patent/US20120277244A1/en not_active Abandoned
- 2010-12-22 EP EP20100796064 patent/EP2519515B1/en active Active
- 2010-12-22 PE PE2012000897A patent/PE20121640A1/es not_active Application Discontinuation
- 2010-12-22 JP JP2012546418A patent/JP5600754B2/ja not_active Expired - Fee Related
- 2010-12-22 PH PH1/2012/501007A patent/PH12012501007A1/en unknown
- 2010-12-22 ES ES10796064T patent/ES2445536T3/es active Active
- 2010-12-22 KR KR1020127019872A patent/KR101419157B1/ko not_active Expired - Fee Related
- 2010-12-22 BR BR112012015916A patent/BR112012015916A2/pt not_active IP Right Cessation
- 2010-12-22 NZ NZ60013610A patent/NZ600136A/xx not_active IP Right Cessation
- 2010-12-22 SG SG2012036935A patent/SG181431A1/en unknown
- 2010-12-22 PT PT10796064T patent/PT2519515E/pt unknown
- 2010-12-22 CA CA 2785341 patent/CA2785341A1/en not_active Abandoned
- 2010-12-22 MX MX2012007754A patent/MX2012007754A/es active IP Right Grant
- 2010-12-22 EA EA201200952A patent/EA201200952A1/ru unknown
- 2010-12-22 CN CN201080060047.7A patent/CN102712621B/zh not_active Expired - Fee Related
- 2010-12-22 WO PCT/EP2010/070502 patent/WO2011080176A1/en not_active Ceased
- 2010-12-22 AU AU2010338365A patent/AU2010338365B2/en not_active Ceased
- 2010-12-22 PL PL10796064T patent/PL2519515T3/pl unknown
-
2012
- 2012-05-17 ZA ZA2012/03614A patent/ZA201203614B/en unknown
- 2012-05-22 TN TNP2012000249A patent/TN2012000249A1/en unknown
- 2012-06-07 IL IL220268A patent/IL220268A0/en unknown
- 2012-06-19 CR CR20120332A patent/CR20120332A/es unknown
- 2012-06-25 CU CU20120099A patent/CU20120099A7/es unknown
- 2012-06-27 CL CL2012001762A patent/CL2012001762A1/es unknown
- 2012-06-28 HN HN2012001413A patent/HN2012001413A/es unknown
- 2012-06-28 GT GT201200219A patent/GT201200219A/es unknown
- 2012-07-25 EC ECSP12012065 patent/ECSP12012065A/es unknown
-
2015
- 2015-07-21 US US14/805,446 patent/US20150322038A1/en not_active Abandoned
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |