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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
Abstract
REFERIDA A UN DERIVADO DE PIRAZINA DE FORMULA (I), DONDE R1 ES H, CIANO, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R2 ES ARILO, HETEROARILO, ENTRE OTROS; R3 ES H, CIANO, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R4 ES H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R5 ES H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R6 ES H, ALQUILO C1-C8, HALOALQUILO C1-C8, ENTRE OTROS; R7 ES H, ALQUILO C1-C8, HALOALQUILOC1-C8, ENTRE OTROS; E1 ES C(R8)(R9) O C(R8)(R9)-C(R10)(R11); E2 ES C(R12)(R13) O C(R12)(R13)-C(R14)(R15); R8 Y R9 SON H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R10 Y R11 SON H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R12 Y R13 SON H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R14 Y R15 SON H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: [3-(6-AMINO-2,4-DIMETIL-3-OXO-2,3,4,5-TETRAHIDRO-PIRAZIN-2-IL)-4-FLUORO-FENIL]-AMIDA DEL ACIDO 5-BROMO-PIRIDIN-2-CARBOXILICO, [3-(6-AMINO-2,4-DIMETIL-2,3,4,5-TETRAHIDRO-PIRAZIN-2-IL)-4-FLUORO-FENIL]-AMIDA DEL ACIDO 5-BROMO-PIRIDIN-2-CARBOXILICO,[3-(6-AMINO-2,4-DIMETIL-3-OXO-2,3,4,5-TETRAHIDRO-PIRAZIN-2-IL)-4-FENIL]-AMIDA DEL ACIDO 5-BROMO-PIRIDIN-2-CARBOXILICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE BACE Y SON UTILES EN EL TRATAMIENTO DE TRASTORNOS NEUROLOGICOS TALES COMO LA ENFERMEDAD DE ALZHEIMER
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 (es) |
| EP (1) | EP2519515B1 (es) |
| JP (1) | JP5600754B2 (es) |
| KR (1) | KR101419157B1 (es) |
| CN (1) | CN102712621B (es) |
| AU (1) | AU2010338365B2 (es) |
| BR (1) | BR112012015916A2 (es) |
| CA (1) | CA2785341A1 (es) |
| CL (1) | CL2012001762A1 (es) |
| CR (1) | CR20120332A (es) |
| CU (1) | CU20120099A7 (es) |
| EA (1) | EA201200952A1 (es) |
| EC (1) | ECSP12012065A (es) |
| ES (1) | ES2445536T3 (es) |
| GT (1) | GT201200219A (es) |
| HN (1) | HN2012001413A (es) |
| IL (1) | IL220268A0 (es) |
| MX (1) | MX2012007754A (es) |
| NZ (1) | NZ600136A (es) |
| PE (1) | PE20121640A1 (es) |
| PH (1) | PH12012501007A1 (es) |
| PL (1) | PL2519515T3 (es) |
| PT (1) | PT2519515E (es) |
| SG (1) | SG181431A1 (es) |
| TN (1) | TN2012000249A1 (es) |
| WO (1) | WO2011080176A1 (es) |
| ZA (1) | ZA201203614B (es) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101346357B (zh) | 2005-10-25 | 2014-04-02 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
| EP2689780A1 (en) | 2007-04-24 | 2014-01-29 | Shionogi & Co., Ltd. | Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group |
| JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| 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 |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| KR20120104570A (ko) | 2009-12-11 | 2012-09-21 | 시오노기세야쿠 가부시키가이샤 | 옥사진 유도체 |
| 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 |
| ES2459593T3 (es) * | 2010-06-09 | 2014-05-09 | Janssen Pharmaceutica, N.V. | Derivados de 5-amino-3,6-dihidro-1H-pirazin-2-ona útiles como inhibidores de beta-secretasa (BACE) |
| EA201291413A1 (ru) * | 2010-06-28 | 2013-05-30 | Янссен Фармацевтика Нв | Производные 3-амино-5,6-дигидро-1h-пиразин-2-она, применимые для лечения болезни альцгеймера и других форм деменции |
| CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| BR112013015430A2 (pt) | 2010-12-22 | 2016-09-20 | Janssen Pharmaceutica Nv | derivados de 5,6-diidro-imidazo[1,2-a]pirazin-8-ilamina úteis como inibidores de beta-secretase (bace) |
| US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
| DK2663561T3 (en) | 2011-01-13 | 2016-06-06 | Novartis Ag | New heterocyclic derivatives and their use in treating neurological disorders |
| CN103596569A (zh) * | 2011-01-13 | 2014-02-19 | 诺瓦提斯公司 | 用于治疗代谢障碍的bace-2抑制剂 |
| CN103415519B (zh) | 2011-03-01 | 2016-03-02 | 詹森药业有限公司 | 作为β-分泌酶(BACE)抑制剂有用的6，7-二氢-吡唑[1，5-a]吡嗪-4-基胺衍生物 |
| PH12013501805A1 (en) | 2011-03-09 | 2013-11-18 | Janssen Pharmaceutica Nv | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| RU2013150349A (ru) | 2011-04-13 | 2015-05-20 | Мерк Шарп И Доум Корп. | 5-замещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов васе, содержащие их композиции и их применение |
| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| US9181236B2 (en) | 2011-08-22 | 2015-11-10 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
| US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| AU2013363151A1 (en) | 2012-12-20 | 2015-06-04 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors |
| US9751886B2 (en) | 2013-06-12 | 2017-09-05 | 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) |
| CN105283457B (zh) | 2013-06-12 | 2018-09-18 | 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]吡嗪衍生物 |
| WO2014198851A1 (en) | 2013-06-12 | 2014-12-18 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
| ES2768823T3 (es) | 2014-12-18 | 2020-06-23 | Janssen Pharmaceutica Nv | Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa |
| 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 (es) | 1968-08-31 | 1970-03-03 | ||
| AUPQ319899A0 (en) * | 1999-10-01 | 1999-10-28 | Fujisawa Pharmaceutical Co., Ltd. | Amide compounds |
| JP2004528295A (ja) * | 2001-01-30 | 2004-09-16 | サイトピア ピーティワイ リミテッド | キナーゼ阻害方法 |
| CA2514733A1 (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 |
| JP4707560B2 (ja) | 2003-12-29 | 2011-06-22 | Ｍｓｄ株式会社 | 新規２−ヘテロアリール置換ベンズイミダゾール誘導体 |
| 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 |
| CN101346357B (zh) * | 2005-10-25 | 2014-04-02 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
| ES2778846T3 (es) * | 2005-11-08 | 2020-08-12 | Vertex Pharma | Moduladores heterocíclicos de transportadores de casete de unión a ATP |
| AU2007336933A1 (en) * | 2006-12-22 | 2008-07-03 | 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 |
| 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 |
| UY32799A (es) * | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
| ES2459593T3 (es) * | 2010-06-09 | 2014-05-09 | Janssen Pharmaceutica, N.V. | Derivados de 5-amino-3,6-dihidro-1H-pirazin-2-ona útiles como inhibidores de beta-secretasa (BACE) |
| EA201291413A1 (ru) * | 2010-06-28 | 2013-05-30 | Янссен Фармацевтика Нв | Производные 3-амино-5,6-дигидро-1h-пиразин-2-она, применимые для лечения болезни альцгеймера и других форм деменции |
-
2010
- 2010-12-22 US US13/518,907 patent/US20120277244A1/en not_active Abandoned
- 2010-12-22 SG SG2012036935A patent/SG181431A1/en unknown
- 2010-12-22 PL PL10796064T patent/PL2519515T3/pl unknown
- 2010-12-22 EP EP20100796064 patent/EP2519515B1/en active Active
- 2010-12-22 PH PH1/2012/501007A patent/PH12012501007A1/en unknown
- 2010-12-22 KR KR1020127019872A patent/KR101419157B1/ko not_active Expired - Fee Related
- 2010-12-22 MX MX2012007754A patent/MX2012007754A/es active IP Right Grant
- 2010-12-22 CA CA 2785341 patent/CA2785341A1/en not_active Abandoned
- 2010-12-22 CN CN201080060047.7A patent/CN102712621B/zh not_active Expired - Fee Related
- 2010-12-22 EA EA201200952A patent/EA201200952A1/ru unknown
- 2010-12-22 PT PT10796064T patent/PT2519515E/pt unknown
- 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 ES ES10796064T patent/ES2445536T3/es active Active
- 2010-12-22 AU AU2010338365A patent/AU2010338365B2/en not_active Ceased
- 2010-12-22 WO PCT/EP2010/070502 patent/WO2011080176A1/en not_active Ceased
- 2010-12-22 NZ NZ60013610A patent/NZ600136A/xx not_active IP Right Cessation
- 2010-12-22 BR BR112012015916A patent/BR112012015916A2/pt not_active IP Right Cessation
-
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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