JP2017538753A5 - - Google Patents
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- JP2017538753A5 JP2017538753A5 JP2017532941A JP2017532941A JP2017538753A5 JP 2017538753 A5 JP2017538753 A5 JP 2017538753A5 JP 2017532941 A JP2017532941 A JP 2017532941A JP 2017532941 A JP2017532941 A JP 2017532941A JP 2017538753 A5 JP2017538753 A5 JP 2017538753A5
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- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acid addition
- tautomer
- compound according
- acceptable acid
- 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.)
- Ceased
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- 150000001875 compounds Chemical class 0.000 claims description 27
- -1 5-methoxypyrazin-2-yl Chemical group 0.000 claims description 17
- 125000003545 alkoxy group Chemical group 0.000 claims description 16
- 150000003839 salts Chemical class 0.000 claims description 16
- 239000002253 acid Substances 0.000 claims description 15
- 206010012289 Dementia Diseases 0.000 claims description 12
- 125000000217 alkyl group Chemical group 0.000 claims description 12
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 239000001257 hydrogen Substances 0.000 claims description 10
- 125000005843 halogen group Chemical group 0.000 claims description 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 7
- 125000001153 fluoro group Chemical group F* 0.000 claims description 6
- 125000004076 pyridyl group Chemical group 0.000 claims description 6
- 208000024827 Alzheimer disease Diseases 0.000 claims description 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 230000002265 prevention Effects 0.000 claims description 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 4
- 125000001424 substituent group Chemical group 0.000 claims description 4
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims description 3
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims description 3
- 201000010374 Down Syndrome Diseases 0.000 claims description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 3
- 201000002832 Lewy body dementia Diseases 0.000 claims description 3
- 208000018737 Parkinson disease Diseases 0.000 claims description 3
- 206010039966 Senile dementia Diseases 0.000 claims description 3
- 206010064930 age-related macular degeneration Diseases 0.000 claims description 3
- 208000010877 cognitive disease Diseases 0.000 claims description 3
- 208000002780 macular degeneration Diseases 0.000 claims description 3
- 208000030159 metabolic disease Diseases 0.000 claims description 3
- 208000027061 mild cognitive impairment Diseases 0.000 claims description 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 3
- GZPHSAQLYPIAIN-UHFFFAOYSA-N 3-pyridinecarbonitrile Chemical compound N#CC1=CC=CN=C1 GZPHSAQLYPIAIN-UHFFFAOYSA-N 0.000 claims description 2
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims description 2
- 102000004190 Enzymes Human genes 0.000 claims description 2
- 108090000790 Enzymes Proteins 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000002541 furyl group Chemical group 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 2
- IXHBTMCLRNMKHZ-LBPRGKRZSA-N levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 2
- 125000002971 oxazolyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000005412 pyrazyl group Chemical group 0.000 claims description 2
- 125000005495 pyridazyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 2
- 125000000335 thiazolyl group Chemical group 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 125000001425 triazolyl group Chemical group 0.000 claims description 2
- 238000000034 method Methods 0.000 description 6
- 208000009829 Lewy Body Disease Diseases 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14198977.2 | 2014-12-18 | ||
| EP14198977 | 2014-12-18 | ||
| EP15164704.7 | 2015-04-22 | ||
| EP15164704 | 2015-04-22 | ||
| PCT/EP2015/079981 WO2016096979A1 (en) | 2014-12-18 | 2015-12-16 | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017538753A JP2017538753A (ja) | 2017-12-28 |
| JP2017538753A5 true JP2017538753A5 (enExample) | 2019-01-31 |
Family
ID=55070992
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017532941A Ceased JP2017538753A (ja) | 2014-12-18 | 2015-12-16 | 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 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US10106524B2 (enExample) |
| EP (1) | EP3233834B1 (enExample) |
| JP (1) | JP2017538753A (enExample) |
| KR (1) | KR20170095881A (enExample) |
| CN (1) | CN107108582B (enExample) |
| AU (1) | AU2015367594C1 (enExample) |
| CA (1) | CA2967164A1 (enExample) |
| EA (1) | EA031041B1 (enExample) |
| ES (1) | ES2768823T3 (enExample) |
| IL (1) | IL252863A0 (enExample) |
| MX (1) | MX2017008083A (enExample) |
| WO (1) | WO2016096979A1 (enExample) |
| ZA (1) | ZA201704116B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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) |
| 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) |
| 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) |
| 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 |
| AU2017353510A1 (en) | 2016-11-04 | 2019-05-02 | Janssen Pharmaceutica Nv | 4,4a,5,7-tetrahydro-3H-furo[3,4-b]pyridinyl compounds |
| CN112791078B (zh) | 2019-11-13 | 2022-12-06 | 润佳（苏州）医药科技有限公司 | 同位素富集的3-氨基-1-丙磺酸及其衍生物的用途 |
| CN113549007B (zh) * | 2021-07-23 | 2023-07-18 | 清华大学 | 一种哌啶乙酸酯类化合物的制备方法 |
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| WO1998057641A1 (en) | 1997-06-18 | 1998-12-23 | Merck & Co., Inc. | ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS |
| JP2005530739A (ja) | 2002-04-19 | 2005-10-13 | セルラー ジェノミクス，インコーポレーテッド | イミダゾ［１，２−ａ］ピラジン−８−イルアミン、生成方法、および使用方法 |
| MY134589A (en) | 2002-09-23 | 2007-12-31 | Schering Corp | Imidazopyrazines as cyclin dependent kinase inhibitors |
| CN1747949A (zh) | 2002-12-20 | 2006-03-15 | 法马西亚公司 | 无环吡唑化合物 |
| SI1678172T1 (sl) | 2003-10-15 | 2010-04-30 | Targacept Inc | AzabicikliŽŤne spojine za lajšanje boleŽŤine in zdravljenje motenj centralnega ĹľivŽŤnega sistema |
| US7618978B2 (en) | 2004-04-22 | 2009-11-17 | Eli Lilly And Company | Amides as BACE inhibitors |
| TW200602045A (en) | 2004-06-16 | 2006-01-16 | Wyeth Corp | Amino-5, 5-diphenylimidazolone derivatives for the inhibition of β-secretase |
| SV2006002232A (es) | 2004-09-21 | 2006-05-25 | Lilly Co Eli | Inhibidores bace ref. x-16940 |
| 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 |
| CN101394852A (zh) | 2005-06-14 | 2009-03-25 | 先灵公司 | 作为蛋白酶抑制剂的化合物的制备和用途 |
| CN101213183A (zh) | 2005-06-30 | 2008-07-02 | 惠氏公司 | 氨基-5-(6元)杂芳基咪唑酮化合物和在β-分泌酶调节中的用途 |
| AU2006307314C1 (en) | 2005-10-25 | 2011-08-25 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| 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 |
| US20080051420A1 (en) | 2006-06-14 | 2008-02-28 | Astrazeneca Ab | New Compounds 317 |
| ES2476605T3 (es) | 2007-04-24 | 2014-07-15 | Shionogi & Co., Ltd. | Derivados de aminohidrotiazina sustituidos con grupos cíclicos |
| TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| AU2008319310A1 (en) | 2007-10-30 | 2009-05-07 | Arena Pharmaceuticals, Inc. | Biphenyl derivatives as modulators of the histamine-H3 receptor useful for the treatment of disorders related thereto |
| ES2400173T3 (es) | 2008-01-28 | 2013-04-08 | Janssen Pharmaceutica Nv | Derivados de 6-sustituido-tio-2-amino-quinolina útiles como inhibidores de beta-secretasa (BACE) |
| JP5496915B2 (ja) | 2008-02-13 | 2014-05-21 | シージーアイ ファーマシューティカルズ，インコーポレーテッド | ６−アリール−イミダゾ［１，２−ａ］ピラジン誘導体、その製造方法、及びその使用方法 |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Ｂａｃｅ抑制劑 |
| PA8854101A1 (es) | 2008-12-18 | 2010-07-27 | Ortho Mcneil Janssen Pharm | Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa |
| WO2011002409A1 (en) | 2009-07-02 | 2011-01-06 | Astrazeneca Ab | 5h-pyrrolo[3,4-£>]pyrazin-7-amine derivatives inhibitors of beta-secretase |
| AR077277A1 (es) | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
| UY32799A (es) | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
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| UA110467C2 (uk) | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
| WO2011077726A1 (ja) * | 2009-12-24 | 2011-06-30 | 塩野義製薬株式会社 | ４－アミノ－１，３－チアジンまたはオキサジン誘導体 |
| US20120277244A1 (en) | 2009-12-31 | 2012-11-01 | Novartis Ag | Pyrazine derivatives and their use in the treatment of neurological disorders |
| US20130079349A1 (en) | 2010-06-09 | 2013-03-28 | Janssen Pharmaceutica Nv | 5-amino-3,6-dihydro-1h-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (bace) |
| 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) |
| KR20130089231A (ko) | 2010-06-28 | 2013-08-09 | 얀센 파마슈티카 엔.브이. | 알츠하이머병 및 다른 형태의 치매 치료용으로 유용한 3-아미노-5,6-디하이드로-1ｈ-피라진-2-온 유도체 |
| MX2013003246A (es) | 2010-09-22 | 2013-05-22 | Janssen Pharmaceutica Nv | Derivados de 4, 7-dihidro-pirazolo [1, 5-a] pirazin-6-ilamina utiles como inhibidores de beta-secretasa (bace). |
| 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) |
| MX2013008111A (es) | 2011-01-12 | 2013-10-30 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de transtornos neurologicos. |
| JP2014505689A (ja) | 2011-01-13 | 2014-03-06 | ノバルティス アーゲー | 代謝障害の処置用ｂａｃｅ−２阻害剤 |
| JP2012147763A (ja) | 2011-01-17 | 2012-08-09 | Toshitaka Kobayashi | 乾物穿孔具 |
| US9242943B2 (en) | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| 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 |
| KR101669349B1 (ko) * | 2012-01-26 | 2016-10-25 | 에프. 호프만-라 로슈 아게 | 플루오로메틸-5,6-다이하이드로-4h-[1,3]옥사진 |
| 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 |
-
2015
- 2015-12-16 EP EP15820456.0A patent/EP3233834B1/en active Active
- 2015-12-16 US US15/536,474 patent/US10106524B2/en not_active Expired - Fee Related
- 2015-12-16 JP JP2017532941A patent/JP2017538753A/ja not_active Ceased
- 2015-12-16 AU AU2015367594A patent/AU2015367594C1/en not_active Ceased
- 2015-12-16 CA CA2967164A patent/CA2967164A1/en not_active Abandoned
- 2015-12-16 MX MX2017008083A patent/MX2017008083A/es unknown
- 2015-12-16 WO PCT/EP2015/079981 patent/WO2016096979A1/en not_active Ceased
- 2015-12-16 ES ES15820456T patent/ES2768823T3/es active Active
- 2015-12-16 KR KR1020177016868A patent/KR20170095881A/ko not_active Withdrawn
- 2015-12-16 EA EA201791367A patent/EA031041B1/ru not_active IP Right Cessation
- 2015-12-16 CN CN201580069749.4A patent/CN107108582B/zh not_active Expired - Fee Related
-
2017
- 2017-06-13 IL IL252863A patent/IL252863A0/en unknown
- 2017-06-15 ZA ZA2017/04116A patent/ZA201704116B/en unknown