KR101419157B1 - 피라진 유도체 및 신경계 장애의 치료에서의 그의 용도 - Google Patents
피라진 유도체 및 신경계 장애의 치료에서의 그의 용도 Download PDFInfo
- Publication number
- KR101419157B1 KR101419157B1 KR1020127019872A KR20127019872A KR101419157B1 KR 101419157 B1 KR101419157 B1 KR 101419157B1 KR 1020127019872 A KR1020127019872 A KR 1020127019872A KR 20127019872 A KR20127019872 A KR 20127019872A KR 101419157 B1 KR101419157 B1 KR 101419157B1
- Authority
- KR
- South Korea
- Prior art keywords
- alkyl
- alkoxy
- halogen
- amino
- phenyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 0 *[C@](*N(*)*1)(c2c(*)c(NC(*)=O)c(*)c(*)c2*)N=C1N Chemical compound *[C@](*N(*)*1)(c2c(*)c(NC(*)=O)c(*)c(*)c2*)N=C1N 0.000 description 2
- KDEOLGIEXQPNFC-UHFFFAOYSA-N CCC(C(N)=NC1(C)c2cccc(NC(c(cc3)ncc3Br)=O)c2)N(C)C1=O Chemical compound CCC(C(N)=NC1(C)c2cccc(NC(c(cc3)ncc3Br)=O)c2)N(C)C1=O KDEOLGIEXQPNFC-UHFFFAOYSA-N 0.000 description 1
- PBVWMRZIDFSIRJ-UHFFFAOYSA-N Cc1cc(Br)cnc1C(Nc(cc1)cc(C(CN(C2)C(C3CC3)=O)(C(F)F)N=C2N)c1F)=O Chemical compound Cc1cc(Br)cnc1C(Nc(cc1)cc(C(CN(C2)C(C3CC3)=O)(C(F)F)N=C2N)c1F)=O PBVWMRZIDFSIRJ-UHFFFAOYSA-N 0.000 description 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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29172409P | 2009-12-31 | 2009-12-31 | |
| US61/291,724 | 2009-12-31 | ||
| PCT/EP2010/070502 WO2011080176A1 (en) | 2009-12-31 | 2010-12-22 | Pyrazine derivatives and their use in the treatment of neurological disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20120102795A KR20120102795A (ko) | 2012-09-18 |
| KR101419157B1 true KR101419157B1 (ko) | 2014-07-11 |
Family
ID=43598456
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020127019872A Expired - Fee Related KR101419157B1 (ko) | 2009-12-31 | 2010-12-22 | 피라진 유도체 및 신경계 장애의 치료에서의 그의 용도 |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US20120277244A1 (https=) |
| EP (1) | EP2519515B1 (https=) |
| JP (1) | JP5600754B2 (https=) |
| KR (1) | KR101419157B1 (https=) |
| CN (1) | CN102712621B (https=) |
| AU (1) | AU2010338365B2 (https=) |
| BR (1) | BR112012015916A2 (https=) |
| CA (1) | CA2785341A1 (https=) |
| CL (1) | CL2012001762A1 (https=) |
| CR (1) | CR20120332A (https=) |
| CU (1) | CU20120099A7 (https=) |
| EA (1) | EA201200952A1 (https=) |
| EC (1) | ECSP12012065A (https=) |
| ES (1) | ES2445536T3 (https=) |
| GT (1) | GT201200219A (https=) |
| HN (1) | HN2012001413A (https=) |
| IL (1) | IL220268A0 (https=) |
| MX (1) | MX2012007754A (https=) |
| NZ (1) | NZ600136A (https=) |
| PE (1) | PE20121640A1 (https=) |
| PH (1) | PH12012501007A1 (https=) |
| PL (1) | PL2519515T3 (https=) |
| PT (1) | PT2519515E (https=) |
| SG (1) | SG181431A1 (https=) |
| TN (1) | TN2012000249A1 (https=) |
| WO (1) | WO2011080176A1 (https=) |
| ZA (1) | ZA201203614B (https=) |
Families Citing this family (31)
| 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 |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| TWI488852B (zh) | 2009-12-11 | 2015-06-21 | Shionogi & Co | 衍生物 |
| 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) |
| 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 |
| CN102985412A (zh) * | 2010-06-28 | 2013-03-20 | 詹森药业有限公司 | 可用于治疗阿尔茨海默病及其它形式的痴呆的3-氨基-5,6-二氢-1h-吡嗪-2-酮衍生物 |
| 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) |
| US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
| PT2663561E (pt) | 2011-01-13 | 2016-06-07 | Novartis Ag | Derivados heterocíclicos novos e sua utilização no tratamento de distúrbios neurológicos |
| MX2013008192A (es) * | 2011-01-13 | 2013-12-16 | Novartis Ag | Inhibidores de bace-2 para tratamiento de transtornos metabolicos. |
| JP5853033B2 (ja) | 2011-03-01 | 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６，７−ジヒドロ−ピラゾロ［１，５−ａ］ピラジン−４−イルアミン誘導体 |
| 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) |
| EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | 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 |
| JP2014514302A (ja) | 2011-04-13 | 2014-06-19 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｂａｃｅ阻害薬としての５−置換されたイミノチアジン類およびそれのモノおよびジオキシド、組成物およびそれらの使用 |
| TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
| 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 |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| EP2934539B1 (en) | 2012-12-20 | 2019-03-27 | Merck Sharp & Dohme Corp. | C5, c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors |
| 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 |
| 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) |
| 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. |
| 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001025229A1 (en) * | 1999-10-01 | 2001-04-12 | Fujisawa Pharmaceutical Co., Ltd. | Amide compounds |
| WO2008079933A2 (en) * | 2006-12-22 | 2008-07-03 | Novartis Ag | Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections |
| EP1942105A1 (en) * | 2005-10-25 | 2008-07-09 | Shionogi Co., Ltd. | Aminodihydrothiazine derivative |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL6911868A (https=) | 1968-08-31 | 1970-03-03 | ||
| US20040102455A1 (en) * | 2001-01-30 | 2004-05-27 | Burns Christopher John | Method 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 |
| CA2553160C (en) | 2003-12-29 | 2010-09-28 | 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 |
| CN102775396B (zh) * | 2005-11-08 | 2014-10-08 | 沃泰克斯药物股份有限公司 | Atp-结合弹夹转运蛋白的杂环调控剂 |
| RU2476431C2 (ru) | 2008-01-18 | 2013-02-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Конденсированное производное аминодигидротиазина |
| 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 |
| 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) |
| CN102985412A (zh) * | 2010-06-28 | 2013-03-20 | 詹森药业有限公司 | 可用于治疗阿尔茨海默病及其它形式的痴呆的3-氨基-5,6-二氢-1h-吡嗪-2-酮衍生物 |
-
2010
- 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 PH PH1/2012/501007A patent/PH12012501007A1/en unknown
- 2010-12-22 SG SG2012036935A patent/SG181431A1/en unknown
- 2010-12-22 EA EA201200952A patent/EA201200952A1/ru unknown
- 2010-12-22 JP JP2012546418A patent/JP5600754B2/ja not_active Expired - Fee Related
- 2010-12-22 KR KR1020127019872A patent/KR101419157B1/ko not_active Expired - Fee Related
- 2010-12-22 PE PE2012000897A patent/PE20121640A1/es not_active Application Discontinuation
- 2010-12-22 CA CA 2785341 patent/CA2785341A1/en not_active Abandoned
- 2010-12-22 AU AU2010338365A patent/AU2010338365B2/en not_active Ceased
- 2010-12-22 BR BR112012015916A patent/BR112012015916A2/pt not_active IP Right Cessation
- 2010-12-22 EP EP20100796064 patent/EP2519515B1/en active Active
- 2010-12-22 CN CN201080060047.7A patent/CN102712621B/zh not_active Expired - Fee Related
- 2010-12-22 MX MX2012007754A patent/MX2012007754A/es active IP Right Grant
- 2010-12-22 PL PL10796064T patent/PL2519515T3/pl unknown
- 2010-12-22 PT PT10796064T patent/PT2519515E/pt unknown
- 2010-12-22 US US13/518,907 patent/US20120277244A1/en not_active Abandoned
- 2010-12-22 ES ES10796064T patent/ES2445536T3/es active Active
-
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 GT GT201200219A patent/GT201200219A/es unknown
- 2012-06-28 HN HN2012001413A patent/HN2012001413A/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
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001025229A1 (en) * | 1999-10-01 | 2001-04-12 | Fujisawa Pharmaceutical Co., Ltd. | Amide compounds |
| EP1942105A1 (en) * | 2005-10-25 | 2008-07-09 | Shionogi Co., Ltd. | Aminodihydrothiazine derivative |
| WO2008079933A2 (en) * | 2006-12-22 | 2008-07-03 | Novartis Ag | Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections |
Also Published As
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| KR101419157B1 (ko) | 피라진 유도체 및 신경계 장애의 치료에서의 그의 용도 | |
| KR101422965B1 (ko) | 옥사진 유도체, 및 신경계 장애의 치료를 위한 ｂａｃｅ 억제제로서의 그의 용도 | |
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| US8524897B2 (en) | Crystalline oxazine derivative | |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A201 | Request for examination | ||
| E13-X000 | Pre-grant limitation requested |
St.27 status event code: A-2-3-E10-E13-lim-X000 |
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| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
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| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
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| PA0105 | International application |
St.27 status event code: A-0-1-A10-A15-nap-PA0105 |
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