JP2014506907A5 - - Google Patents
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- Publication number
- JP2014506907A5 JP2014506907A5 JP2013555862A JP2013555862A JP2014506907A5 JP 2014506907 A5 JP2014506907 A5 JP 2014506907A5 JP 2013555862 A JP2013555862 A JP 2013555862A JP 2013555862 A JP2013555862 A JP 2013555862A JP 2014506907 A5 JP2014506907 A5 JP 2014506907A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- alkyloxy
- hydrogen
- dementia
- 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.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 14
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 206010012289 Dementia Diseases 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 2
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 208000009829 Lewy Body Disease Diseases 0.000 claims 2
- 201000002832 Lewy body dementia Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 230000032683 aging Effects 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 208000027061 mild cognitive impairment Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000005412 pyrazyl group Chemical group 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- -1 chloro, fluoro, cyano, methyl Chemical group 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000005495 pyridazyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11156463.9 | 2011-03-01 | ||
| EP11156463 | 2011-03-01 | ||
| PCT/EP2012/053455 WO2012117027A1 (en) | 2011-03-01 | 2012-02-29 | 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014506907A JP2014506907A (ja) | 2014-03-20 |
| JP2014506907A5 true JP2014506907A5 (cg-RX-API-DMAC7.html) | 2015-04-16 |
| JP5853033B2 JP5853033B2 (ja) | 2016-02-09 |
Family
ID=45808845
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013555862A Expired - Fee Related JP5853033B2 (ja) | 2011-03-01 | 2012-02-29 | 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 |
Country Status (27)
Families Citing this family (23)
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| KR101052122B1 (ko) | 2005-10-25 | 2011-07-26 | 시오노기세야쿠 가부시키가이샤 | 아미노디히드로티아진 유도체 |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| MX2009011498A (es) | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
| AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
| JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 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 |
| US8999980B2 (en) | 2009-12-11 | 2015-04-07 | Shionogi & Co., Ltd. | Oxazine derivatives |
| EP2580200B1 (en) | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| WO2012057247A1 (ja) | 2010-10-29 | 2012-05-03 | 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 |
| US8927721B2 (en) | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| EP2655376B1 (en) | 2010-12-22 | 2017-08-23 | Janssen Pharmaceutica NV | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| EP3447061B1 (en) | 2011-03-01 | 2021-11-24 | NuCana plc | Pharmaceutical formulation comprising a phosphoramidate derivative of 5-fluoro-2'-deoxyuridine for use in the treatment of cancer |
| WO2012117027A1 (en) | 2011-03-01 | 2012-09-07 | Janssen Pharmaceutica Nv | 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
| CN103415521B (zh) | 2011-03-09 | 2016-01-06 | 詹森药业有限公司 | 用作β分泌酶（BACE）抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物 |
| US8883779B2 (en) | 2011-04-26 | 2014-11-11 | Shinogi & Co., Ltd. | Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| MX368326B (es) * | 2013-06-12 | 2019-09-27 | Janssen Pharmaceutica Nv | Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace). |
| 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) |
| CA2911690C (en) * | 2013-06-12 | 2021-08-24 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
| US10106524B2 (en) | 2014-12-18 | 2018-10-23 | Janssen Pharmaceutica Nv | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrol-5-amine compound inhibitors of beta-secretase |
| US10357493B2 (en) | 2017-03-10 | 2019-07-23 | Selenity Therapeutics (Bermuda), Ltd. | Metalloenzyme inhibitor compounds |
| TWI782056B (zh) * | 2017-07-14 | 2022-11-01 | 日商鹽野義製藥股份有限公司 | 具有ｍｇａｔ２抑制活性的縮合環衍生物 |
| EP3909583A4 (en) | 2019-01-11 | 2022-08-17 | Shionogi & Co., Ltd | DIHYDROPYRAZOLOPYRAZINONE DERIVATIVES WITH MGAT2 INHIBITORY ACTIVITY |
| AU2023296166A1 (en) * | 2022-06-13 | 2024-11-28 | Shionogi & Co., Ltd. | Crystal of dihydropyridinone derivative or solvate thereof |
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| TW224974B (cg-RX-API-DMAC7.html) | 1991-07-02 | 1994-06-11 | Hoffmann La Roche | |
| IL164703A0 (en) | 2002-04-19 | 2005-12-18 | Cellular Genomics Inc | ImidazoÄ1,2-AÜpyrazin-8-ylamines method of making and method of use thereof |
| MXPA05003120A (es) | 2002-09-23 | 2005-06-22 | Schering Corp | Imidazopirazinas como inhibidores de cinasa dependientes de ciclinas. |
| MXPA05006568A (es) | 2002-12-20 | 2005-09-22 | Pharmacia Corp | Compuestos de pirazol aciclico para la inhibicion de proteina cinasa-2 activada por proteina cinasa activada por mitogenos. |
| WO2004092177A1 (en) * | 2003-04-09 | 2004-10-28 | Biogen Idec Ma Inc. | Triazolopyrazines and methods of making and using the same |
| US7402592B2 (en) | 2003-10-15 | 2008-07-22 | Targacept, Inc. | Pharmaceutical compositions and methods for relieving pain and treating central nervous system disorders |
| WO2005108391A1 (en) | 2004-04-22 | 2005-11-17 | Eli Lilly And Company | Amides as bace inhibitors |
| AU2005264915A1 (en) | 2004-06-16 | 2006-01-26 | Wyeth | Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase |
| TW200624426A (en) | 2004-09-21 | 2006-07-16 | Lilly Co Eli | BACE inhibitors |
| RU2007126570A (ru) | 2005-01-14 | 2009-02-20 | Вайет (Us) | Аминоимидазолоны, применяемые для ингибирования бета-секретазы |
| US20070005404A1 (en) | 2005-06-09 | 2007-01-04 | Drive Diagnostics Ltd. | System and method for providing driving insurance |
| MX2007016183A (es) | 2005-06-14 | 2008-03-10 | Schering Corp | Preparacion y uso de compuestos como inhibidores de proteasas. |
| EP1896448A1 (en) | 2005-06-30 | 2008-03-12 | Wyeth | AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION |
| KR101052122B1 (ko) | 2005-10-25 | 2011-07-26 | 시오노기세야쿠 가부시키가이샤 | 아미노디히드로티아진 유도체 |
| TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| US20090099217A1 (en) | 2006-04-05 | 2009-04-16 | Astex Therapeutics Ltd. | 2-Aminopyrimidin-4-Ones And Their Use For Treating Or Preventing Alpha Beta-Related Pathologies |
| GB2443654A (en) | 2006-05-30 | 2008-05-14 | Matthew Emmerson Allen | System for detecting and testing drivers who show abnormal driving behaviour. |
| US20080051420A1 (en) | 2006-06-14 | 2008-02-28 | Astrazeneca Ab | New Compounds 317 |
| TW200815443A (en) * | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds I |
| CN101501040A (zh) * | 2006-06-14 | 2009-08-05 | 阿斯利康(瑞典)有限公司 | 氨基-咪唑啉以及它们作为治疗认知缺损、阿尔茨海默病、神经变性和痴呆的药物的用途 |
| MX2009011498A (es) | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
| TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
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| RU2497821C2 (ru) | 2008-01-28 | 2013-11-10 | Янссен Фармацевтика Нв | ПРОИЗВОДНЫЕ 6-ЗАМЕЩЕННОГО-ТИО (ИЛИ -ОКСО-)-2-АМИНО-ХИНОЛИНА, ПРИМЕНЯЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ β-СЕКРЕТАЗЫ (BACE) |
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| US8999980B2 (en) | 2009-12-11 | 2015-04-07 | Shionogi & Co., Ltd. | Oxazine derivatives |
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| WO2011080176A1 (en) | 2009-12-31 | 2011-07-07 | Novartis Ag | Pyrazine derivatives and their use in the treatment of neurological disorders |
| EP2580200B1 (en) | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| WO2012057247A1 (ja) | 2010-10-29 | 2012-05-03 | 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 |
| EP2655376B1 (en) | 2010-12-22 | 2017-08-23 | Janssen Pharmaceutica NV | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| US9242943B2 (en) | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| WO2012117027A1 (en) | 2011-03-01 | 2012-09-07 | Janssen Pharmaceutica Nv | 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
| CN103415521B (zh) | 2011-03-09 | 2016-01-06 | 詹森药业有限公司 | 用作β分泌酶（BACE）抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物 |
| KR20140084146A (ko) | 2011-10-13 | 2014-07-04 | 노파르티스 아게 | 신규 옥사진 유도체 및 질환의 치료에서의 그의 용도 |
-
2012
- 2012-02-29 WO PCT/EP2012/053455 patent/WO2012117027A1/en not_active Ceased
- 2012-02-29 UA UAA201308783A patent/UA109800C2/ru unknown
- 2012-02-29 PT PT127072767T patent/PT2681219E/pt unknown
- 2012-02-29 EP EP12707276.7A patent/EP2681219B1/en active Active
- 2012-02-29 US US14/002,169 patent/US9346811B2/en not_active Expired - Fee Related
- 2012-02-29 EA EA201391251A patent/EA022649B1/ru not_active IP Right Cessation
- 2012-02-29 DK DK12707276.7T patent/DK2681219T3/en active
- 2012-02-29 HR HRP20160030TT patent/HRP20160030T1/hr unknown
- 2012-02-29 ES ES12707276.7T patent/ES2558779T3/es active Active
- 2012-02-29 MX MX2013010040A patent/MX338333B/es active IP Right Grant
- 2012-02-29 MY MYPI2013003200A patent/MY161407A/en unknown
- 2012-02-29 PL PL12707276T patent/PL2681219T3/pl unknown
- 2012-02-29 SI SI201230429T patent/SI2681219T1/sl unknown
- 2012-02-29 HU HUE12707276A patent/HUE026338T2/en unknown
- 2012-02-29 SG SG2013064746A patent/SG192963A1/en unknown
- 2012-02-29 JP JP2013555862A patent/JP5853033B2/ja not_active Expired - Fee Related
- 2012-02-29 CA CA2824360A patent/CA2824360C/en active Active
- 2012-02-29 BR BR112013022039A patent/BR112013022039A2/pt not_active Application Discontinuation
- 2012-02-29 PH PH1/2013/501807A patent/PH12013501807A1/en unknown
- 2012-02-29 AU AU2012222394A patent/AU2012222394B2/en not_active Ceased
- 2012-02-29 CN CN201280011146.5A patent/CN103415519B/zh not_active Expired - Fee Related
- 2012-02-29 KR KR1020137022392A patent/KR102012671B1/ko not_active Expired - Fee Related
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2013
- 2013-08-28 IL IL228158A patent/IL228158A/en active IP Right Grant
- 2013-08-28 CL CL2013002486A patent/CL2013002486A1/es unknown
- 2013-08-29 CO CO13205178A patent/CO6751282A2/es unknown
- 2013-08-30 ZA ZA2013/06545A patent/ZA201306545B/en unknown
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2016
- 2016-01-28 CY CY20161100087T patent/CY1117663T1/el unknown