JP2014507455A5 - - Google Patents
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- Publication number
- JP2014507455A5 JP2014507455A5 JP2013557074A JP2013557074A JP2014507455A5 JP 2014507455 A5 JP2014507455 A5 JP 2014507455A5 JP 2013557074 A JP2013557074 A JP 2013557074A JP 2013557074 A JP2013557074 A JP 2013557074A JP 2014507455 A5 JP2014507455 A5 JP 2014507455A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- dementia
- alkyloxy
- cyano
- 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 13
- 206010012289 Dementia Diseases 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000005843 halogen group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- -1 chloro, fluoro, cyano, methyl Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 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
- 208000024827 Alzheimer disease Diseases 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
- 206010044688 Trisomy 21 Diseases 0.000 claims 2
- 230000032683 aging Effects 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 208000027061 mild cognitive impairment Diseases 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 1
- 208000006011 Stroke 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
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 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
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 230000002265 prevention Effects 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
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 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
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11157418.2 | 2011-03-09 | ||
| EP11157418 | 2011-03-09 | ||
| PCT/EP2012/053863 WO2012120023A1 (en) | 2011-03-09 | 2012-03-07 | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014507455A JP2014507455A (ja) | 2014-03-27 |
| JP2014507455A5 true JP2014507455A5 (enExample) | 2015-04-23 |
| JP5853035B2 JP5853035B2 (ja) | 2016-02-09 |
Family
ID=43833325
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013557074A Expired - Fee Related JP5853035B2 (ja) | 2011-03-09 | 2012-03-07 | 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 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US9845326B2 (enExample) |
| EP (1) | EP2683721B1 (enExample) |
| JP (1) | JP5853035B2 (enExample) |
| KR (1) | KR102012675B1 (enExample) |
| CN (1) | CN103415521B (enExample) |
| AU (1) | AU2012224632B2 (enExample) |
| BR (1) | BR112013022917A2 (enExample) |
| CA (1) | CA2825620C (enExample) |
| CL (1) | CL2013002511A1 (enExample) |
| CO (1) | CO6751283A2 (enExample) |
| EA (1) | EA023824B1 (enExample) |
| ES (1) | ES2534973T3 (enExample) |
| IL (1) | IL228239A (enExample) |
| MX (1) | MX340031B (enExample) |
| MY (1) | MY163346A (enExample) |
| PH (1) | PH12013501805A1 (enExample) |
| SG (1) | SG193342A1 (enExample) |
| UA (1) | UA109687C2 (enExample) |
| WO (1) | WO2012120023A1 (enExample) |
| ZA (1) | ZA201306719B (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006307314C1 (en) | 2005-10-25 | 2011-08-25 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| 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 |
| ES2476605T3 (es) | 2007-04-24 | 2014-07-15 | Shionogi & Co., Ltd. | Derivados de aminohidrotiazina sustituidos con grupos cíclicos |
| AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting 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 |
| UA110467C2 (uk) | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
| PH12012502377A1 (en) | 2010-06-09 | 2014-10-14 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| 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 |
| NZ610948A (en) | 2010-12-22 | 2014-06-27 | Janssen Pharmaceutica Nv | 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
| 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 |
| BR112013022917A2 (pt) | 2011-03-09 | 2016-12-06 | Janssen Pharmaceutica Nv | derivados 3,4-dihidro-pirrolo[1,2-a]pirazino-1-ilamina úteis como inibidores de beta-secretase (bace) |
| 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 |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| KR102243133B1 (ko) * | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-6,7-디하이드로[1,2,3]트리아졸로[1,5-a]피라진 유도체 |
| JP6325092B2 (ja) * | 2013-06-12 | 2018-05-16 | ヤンセン ファーマシューティカ エヌ．ベー． | βーセクレターゼ（ＢＡＣＥ）の阻害剤としての４−アミノ−６−フェニル−５，６−ジヒドロイミダゾ［１，５−Ａ］ピラジン誘導体 |
| KR102243135B1 (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-3(2h)-온 유도체 |
| RU2572076C2 (ru) * | 2014-03-26 | 2015-12-27 | Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт фармакологии имени В.В. Закусова" | 1-арилпирроло[1,2-a]пиразин-3-карбоксамиды с нейропсихотропной активностью |
| EP3233834B1 (en) | 2014-12-18 | 2019-11-13 | Janssen Pharmaceutica NV | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine derivatives useful as inhibitors of beta-secretase |
| WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | Metalloenzyme inhibitor compounds |
| CN117471007B (zh) * | 2023-10-31 | 2024-08-09 | 广东省中医院（广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院） | 一种血浆β-淀粉样蛋白检测方法 |
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| PH12012502377A1 (en) | 2010-06-09 | 2014-10-14 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
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| 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 |
| BR112013022917A2 (pt) * | 2011-03-09 | 2016-12-06 | Janssen Pharmaceutica Nv | derivados 3,4-dihidro-pirrolo[1,2-a]pirazino-1-ilamina úteis como inibidores de beta-secretase (bace) |
| 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 |
| IN2014DN03206A (enExample) | 2011-10-13 | 2015-05-22 | Novartis Ag | |
| UA111749C2 (uk) | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
| JP5989130B2 (ja) | 2011-12-06 | 2016-09-07 | ヤンセン ファーマシューティカ エヌ．ベー． | ５−（３−アミノフェニル）−５−アルキル−５，６−ジヒドロ−２ｈ−［１，４］オキサジン−３−アミン誘導体 |
| AU2013363151A1 (en) | 2012-12-20 | 2015-06-04 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors |
| JP6325092B2 (ja) | 2013-06-12 | 2018-05-16 | ヤンセン ファーマシューティカ エヌ．ベー． | βーセクレターゼ（ＢＡＣＥ）の阻害剤としての４−アミノ−６−フェニル−５，６−ジヒドロイミダゾ［１，５−Ａ］ピラジン誘導体 |
| KR102243133B1 (ko) | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-6,7-디하이드로[1,2,3]트리아졸로[1,5-a]피라진 유도체 |
| KR102243135B1 (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-3(2h)-온 유도체 |
| EP3233834B1 (en) | 2014-12-18 | 2019-11-13 | Janssen Pharmaceutica NV | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine derivatives useful as inhibitors of beta-secretase |
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2012
- 2012-03-07 BR BR112013022917A patent/BR112013022917A2/pt not_active Application Discontinuation
- 2012-03-07 JP JP2013557074A patent/JP5853035B2/ja not_active Expired - Fee Related
- 2012-03-07 MY MYPI2013003278A patent/MY163346A/en unknown
- 2012-03-07 CA CA2825620A patent/CA2825620C/en active Active
- 2012-03-07 EA EA201391296A patent/EA023824B1/ru not_active IP Right Cessation
- 2012-03-07 PH PH1/2013/501805A patent/PH12013501805A1/en unknown
- 2012-03-07 MX MX2013010280A patent/MX340031B/es active IP Right Grant
- 2012-03-07 WO PCT/EP2012/053863 patent/WO2012120023A1/en not_active Ceased
- 2012-03-07 EP EP12707319.5A patent/EP2683721B1/en not_active Not-in-force
- 2012-03-07 KR KR1020137022396A patent/KR102012675B1/ko not_active Expired - Fee Related
- 2012-03-07 SG SG2013067210A patent/SG193342A1/en unknown
- 2012-03-07 US US14/003,901 patent/US9845326B2/en active Active
- 2012-03-07 CN CN201280012485.5A patent/CN103415521B/zh not_active Expired - Fee Related
- 2012-03-07 ES ES12707319.5T patent/ES2534973T3/es active Active
- 2012-03-07 AU AU2012224632A patent/AU2012224632B2/en not_active Ceased
- 2012-07-03 UA UAA201308782A patent/UA109687C2/ru unknown
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2013
- 2013-08-29 CO CO13205187A patent/CO6751283A2/es active IP Right Grant
- 2013-08-30 CL CL2013002511A patent/CL2013002511A1/es unknown
- 2013-09-02 IL IL228239A patent/IL228239A/en active IP Right Grant
- 2013-09-06 ZA ZA2013/06719A patent/ZA201306719B/en unknown
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