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
- Authority
- 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 | 2014-12-18 | ||
| EP14198977.2 | 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 (https=) | 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 (https=) |
| EP (1) | EP3233834B1 (https=) |
| JP (1) | JP2017538753A (https=) |
| KR (1) | KR20170095881A (https=) |
| CN (1) | CN107108582B (https=) |
| AU (1) | AU2015367594C1 (https=) |
| CA (1) | CA2967164A1 (https=) |
| EA (1) | EA031041B1 (https=) |
| ES (1) | ES2768823T3 (https=) |
| IL (1) | IL252863A0 (https=) |
| MX (1) | MX2017008083A (https=) |
| WO (1) | WO2016096979A1 (https=) |
| ZA (1) | ZA201704116B (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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) |
| 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) |
| 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) |
| 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. |
| CA3039586A1 (en) | 2016-11-04 | 2018-05-11 | Janssen Pharmaceutica Nv | 4,4a,5,7-tetrahydro-3h-furo[3,4-b]pyridinyl compounds |
| CN116059192B (zh) | 2019-11-13 | 2024-10-29 | 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 |
Family Cites Families (56)
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| US4188389A (en) | 1978-11-03 | 1980-02-12 | Ayerst Mckenna & Harrison, Inc. | 1,2,3,4-Tetrahydropyrrolo(1,2-A)pyrazines |
| TW224974B (https=) | 1991-07-02 | 1994-06-11 | Hoffmann La Roche | |
| WO1998057641A1 (en) | 1997-06-18 | 1998-12-23 | Merck & Co., Inc. | ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS |
| CA2482991A1 (en) | 2002-04-19 | 2003-10-30 | Cellular Genomics, Inc. | Imidazo[1,2-a]pyrazin-8-ylamines method of making and method of use thereof |
| TW200413378A (en) | 2002-09-23 | 2004-08-01 | Schering Corp | Novel 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 |
| AU2004282201A1 (en) | 2003-10-15 | 2005-04-28 | Targacept, Inc. | Azabicycyclic compounds for relieving pain and treating central nervous system disorders |
| WO2005108358A2 (en) | 2004-04-22 | 2005-11-17 | Eli Lilly And Company | Pyrrolidine derivatives useful as bace inhibitors |
| BRPI0512213A (pt) | 2004-06-16 | 2008-02-19 | Wyeth Corp | método para tratamento, prevenção ou melhora de uma doença ou distúrbio; composição farmacêutica; processo para a preparação de um composto; e uso de um composto |
| TW200624426A (en) | 2004-09-21 | 2006-07-16 | Lilly Co Eli | BACE inhibitors |
| CA2593515A1 (en) | 2005-01-14 | 2006-07-20 | Wyeth | Amino-imidazolones for the inhibition of beta-secretase |
| US20070005404A1 (en) | 2005-06-09 | 2007-01-04 | Drive Diagnostics Ltd. | System and method for providing driving insurance |
| RU2008100164A (ru) | 2005-06-14 | 2009-07-20 | Шеринг Корпорейшн (US) | Получение и применение соединений в качестве ингибиторов протеаз |
| WO2007005404A1 (en) | 2005-06-30 | 2007-01-11 | Wyeth | AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION |
| RU2416603C9 (ru) | 2005-10-25 | 2012-06-20 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина |
| 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 |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| CA2702320A1 (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 |
| US8076358B2 (en) | 2008-01-28 | 2011-12-13 | Janssen Pharmaceutica Nv | 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of β-secretase (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 |
| US8188079B2 (en) | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
| EP2500344A4 (en) | 2009-11-13 | 2013-05-01 | Shionogi & Co | AMINOTHIAZIN OR AMINOOXAZINE DERIVATIVES WITH AN AMINO TERMINATION |
| UA103272C2 (uk) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2 |
| TWI488852B (zh) | 2009-12-11 | 2015-06-21 | Shionogi & Co | 衍生物 |
| US20120258961A1 (en) * | 2009-12-24 | 2012-10-11 | Shionogi & Co., Ltd. | 4-amino-1,3-thiazine or oxazine derivative |
| WO2011080176A1 (en) | 2009-12-31 | 2011-07-07 | Novartis Ag | Pyrazine derivatives and their use in the treatment of neurological disorders |
| 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 |
| 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 |
| US8609660B2 (en) | 2010-09-22 | 2013-12-17 | Janssen Pharmaceutica Nv | 4,7-dihydro-pyrazolo[1,5-a]pyrazin-6-ylamine derivatives useful as inhibitors of beta-secretase (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 |
| 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) |
| CN103429589A (zh) | 2011-01-12 | 2013-12-04 | 诺瓦提斯公司 | 噁嗪衍生物及其在治疗神经障碍中的用途 |
| MX2013008192A (es) | 2011-01-13 | 2013-12-16 | Novartis Ag | Inhibidores de bace-2 para tratamiento de transtornos metabolicos. |
| 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 |
| 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) |
| TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
| CA2851445A1 (en) | 2011-10-13 | 2013-04-18 | Novartis Ag | Novel oxazine derivatives and their use in the treatment of disease |
| UA111749C2 (uk) | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
| ES2582473T3 (es) * | 2011-12-06 | 2016-09-13 | Janssen Pharmaceutica, N.V. | Derivados de 5-(3-aminofenil)-5-alquil-5,6-dihidro-2H-[1,4]oxazin-3-amina para el tratamiento de trastornos en que está implicada la beta-secretasa |
| UA113538C2 (xx) * | 2012-01-26 | 2017-02-10 | Фторметил-5,6-дигідро-4h-$1,3]оксазини | |
| 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. |
-
2015
- 2015-12-16 MX MX2017008083A patent/MX2017008083A/es unknown
- 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 ES ES15820456T patent/ES2768823T3/es active Active
- 2015-12-16 EA EA201791367A patent/EA031041B1/ru not_active IP Right Cessation
- 2015-12-16 WO PCT/EP2015/079981 patent/WO2016096979A1/en not_active Ceased
- 2015-12-16 CA CA2967164A patent/CA2967164A1/en not_active Abandoned
- 2015-12-16 US US15/536,474 patent/US10106524B2/en not_active Expired - Fee Related
- 2015-12-16 EP EP15820456.0A patent/EP3233834B1/en active Active
- 2015-12-16 CN CN201580069749.4A patent/CN107108582B/zh not_active Expired - Fee Related
- 2015-12-16 KR KR1020177016868A patent/KR20170095881A/ko not_active Withdrawn
-
2017
- 2017-06-13 IL IL252863A patent/IL252863A0/en unknown
- 2017-06-15 ZA ZA2017/04116A patent/ZA201704116B/en unknown
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