JP2014506907A5 - - Google Patents
Download PDFInfo
- 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
Links
- 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 | 2011-03-01 | ||
| EP11156463.9 | 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 (enExample) | 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)
| Country | Link |
|---|---|
| US (1) | US9346811B2 (enExample) |
| EP (1) | EP2681219B1 (enExample) |
| JP (1) | JP5853033B2 (enExample) |
| KR (1) | KR102012671B1 (enExample) |
| CN (1) | CN103415519B (enExample) |
| AU (1) | AU2012222394B2 (enExample) |
| BR (1) | BR112013022039A2 (enExample) |
| CA (1) | CA2824360C (enExample) |
| CL (1) | CL2013002486A1 (enExample) |
| CO (1) | CO6751282A2 (enExample) |
| CY (1) | CY1117663T1 (enExample) |
| DK (1) | DK2681219T3 (enExample) |
| EA (1) | EA022649B1 (enExample) |
| ES (1) | ES2558779T3 (enExample) |
| HR (1) | HRP20160030T1 (enExample) |
| HU (1) | HUE026338T2 (enExample) |
| IL (1) | IL228158A (enExample) |
| MX (1) | MX338333B (enExample) |
| MY (1) | MY161407A (enExample) |
| PH (1) | PH12013501807A1 (enExample) |
| PL (1) | PL2681219T3 (enExample) |
| PT (1) | PT2681219E (enExample) |
| SG (1) | SG192963A1 (enExample) |
| SI (1) | SI2681219T1 (enExample) |
| UA (1) | UA109800C2 (enExample) |
| WO (1) | WO2012117027A1 (enExample) |
| ZA (1) | ZA201306545B (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2597087B1 (en) | 2005-10-25 | 2016-03-30 | Shionogi&Co., Ltd. | Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors |
| AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
| 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 |
| NZ589590A (en) | 2008-06-13 | 2012-05-25 | Shionogi & Co | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
| US8703785B2 (en) | 2008-10-22 | 2014-04-22 | Shionogi & Co., Ltd. | 2-aminopyrimidin-4-one and 2-aminopyridine derivatives both having BACE1-inhibiting activity |
| BR112012013854A2 (pt) | 2009-12-11 | 2019-09-24 | Shionogi & Co | derivados de oxazina. |
| JP5711813B2 (ja) | 2010-06-09 | 2015-05-07 | 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５，６−ジヒドロ−２Ｈ−［１，４］オキサジン−３−イル−アミン誘導体 |
| 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 |
| 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 |
| US9840507B2 (en) | 2010-12-22 | 2017-12-12 | Janssen Pharmaceutica, Nv | 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (BACE) |
| HRP20160030T1 (hr) | 2011-03-01 | 2016-02-12 | Janssen Pharmaceutica N.V. | Derivati 6,7-dihidro-pirazolo[1,5-a]pirazin-4-ilamina koji su korisni kao inhibitori beta-sekretaze (bace) |
| CA2828326C (en) | 2011-03-01 | 2019-05-07 | Nucana Biomed Limited | Phosphoramidate derivatives of 5 - fluoro - 2' - deoxyuridine for use in the treatment of cancer |
| US9845326B2 (en) | 2011-03-09 | 2017-12-19 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydropyrrolo[1,2-A]pyrazines as beta-secretase (BACE) inhibitors |
| JPWO2012147763A1 (ja) | 2011-04-26 | 2014-07-28 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤 |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| 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) |
| BR112015030597A2 (pt) * | 2013-06-12 | 2017-07-25 | Janssen Pharmaceutica Nv | derivados 4-amino-6-fenil-6,7-di-hidro[1,2,3]triazolo[1,5-a]pirazina como inibidores de beta-secretase (bace) |
| MX369629B (es) * | 2013-06-12 | 2019-11-14 | Janssen Pharmaceutica Nv | Derivados de 4-a mino-6-fenil-5,6-dihidroimidazo[1,5 a]pirazina como inhibidores de beta-secretasa (bace). |
| 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 |
| 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 |
| JP7608166B2 (ja) | 2019-01-11 | 2025-01-06 | 塩野義製薬株式会社 | Ｍｇａｔ２阻害活性を有するジヒドロピラゾロピラジノン誘導体 |
| EP4003319A4 (en) | 2019-07-30 | 2023-11-08 | Eikonizo Therapeutics, Inc. | HDAC6 INHIBITORS AND THEIR USES |
| EP4538275A1 (en) * | 2022-06-13 | 2025-04-16 | Shionogi & Co., Ltd | Crystal of dihydropyridinone derivative or solvate thereof |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4188389A (en) | 1978-11-03 | 1980-02-12 | Ayerst Mckenna & Harrison, Inc. | 1,2,3,4-Tetrahydropyrrolo(1,2-A)pyrazines |
| TW224974B (enExample) | 1991-07-02 | 1994-06-11 | Hoffmann La Roche | |
| US6919340B2 (en) | 2002-04-19 | 2005-07-19 | Cellular Genomics, Inc. | Imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof |
| MY134589A (en) | 2002-09-23 | 2007-12-31 | Schering Corp | Imidazopyrazines as cyclin dependent kinase inhibitors |
| BR0317430A (pt) | 2002-12-20 | 2005-10-25 | Pharmacia Corp | Compostos inibidores de quinase-2 de proteìna ativada por quinase de proteìna ativada por mitógeno |
| US7674791B2 (en) * | 2003-04-09 | 2010-03-09 | Biogen Idec Ma Inc. | Triazolopyrazines and methods of making and using the same |
| WO2005037832A2 (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 |
| NZ552031A (en) | 2004-06-16 | 2009-06-26 | Wyeth Corp | Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase |
| TW200624426A (en) | 2004-09-21 | 2006-07-16 | Lilly Co Eli | BACE inhibitors |
| EP1836208A2 (en) | 2005-01-14 | 2007-09-26 | Wyeth Incoporated | AMINO-IMIDAZOLONES FOR THE INHIBITION OF ß-SECRETASE |
| US20070005404A1 (en) | 2005-06-09 | 2007-01-04 | Drive Diagnostics Ltd. | System and method for providing driving insurance |
| EP1896032B1 (en) | 2005-06-14 | 2012-10-31 | Merck Sharp & Dohme Corp. | The preparation and use of compounds as protease inhibitors |
| CA2613435A1 (en) | 2005-06-30 | 2007-01-11 | Wyeth | Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for .beta.-secretase modulation |
| EP2597087B1 (en) | 2005-10-25 | 2016-03-30 | Shionogi&Co., Ltd. | Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors |
| TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| CN101460480A (zh) | 2006-04-05 | 2009-06-17 | 阿斯利康(瑞典)有限公司 | 2-氨基嘧啶-4-酮类化合物及其用于治疗或预防Aβ相关病理的用途 |
| 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 |
| 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 |
| TW200815443A (en) * | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds I |
| AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
| TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| WO2009058300A1 (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 |
| BRPI0906625A2 (pt) | 2008-01-28 | 2015-07-14 | Janssen Pharmaceutica Nv | Derivados de tio-2-amino-quinolina-6-substituída úteis como inibidores da beta-secretase (bace) |
| NZ587039A (en) | 2008-02-13 | 2013-01-25 | Gilead Connecticut Inc | 6-aryl-imidazo[1, 2-a]pyrazine derivatives, method of making, and method of use thereof |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Ｂａｃｅ抑制劑 |
| WO2011002409A1 (en) * | 2009-07-02 | 2011-01-06 | Astrazeneca Ab | 5h-pyrrolo[3,4-£>]pyrazin-7-amine derivatives inhibitors of beta-secretase |
| AR077328A1 (es) * | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
| 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 |
| BR112012013854A2 (pt) | 2009-12-11 | 2019-09-24 | Shionogi & Co | derivados de oxazina. |
| US20120258961A1 (en) | 2009-12-24 | 2012-10-11 | Shionogi & Co., Ltd. | 4-amino-1,3-thiazine or oxazine derivative |
| ES2445536T3 (es) | 2009-12-31 | 2014-03-03 | Novartis Ag | Derivados de la pirazina y su uso en el tratamiento de trastornos neurológicos |
| JP5711813B2 (ja) * | 2010-06-09 | 2015-05-07 | 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５，６−ジヒドロ−２Ｈ−［１，４］オキサジン−３−イル−アミン誘導体 |
| 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 |
| US9840507B2 (en) | 2010-12-22 | 2017-12-12 | 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 |
| HRP20160030T1 (hr) | 2011-03-01 | 2016-02-12 | Janssen Pharmaceutica N.V. | Derivati 6,7-dihidro-pirazolo[1,5-a]pirazin-4-ilamina koji su korisni kao inhibitori beta-sekretaze (bace) |
| US9845326B2 (en) | 2011-03-09 | 2017-12-19 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydropyrrolo[1,2-A]pyrazines as beta-secretase (BACE) inhibitors |
| KR20140084146A (ko) | 2011-10-13 | 2014-07-04 | 노파르티스 아게 | 신규 옥사진 유도체 및 질환의 치료에서의 그의 용도 |
-
2012
- 2012-02-29 HR HRP20160030TT patent/HRP20160030T1/hr unknown
- 2012-02-29 WO PCT/EP2012/053455 patent/WO2012117027A1/en not_active Ceased
- 2012-02-29 MX MX2013010040A patent/MX338333B/es active IP Right Grant
- 2012-02-29 PL PL12707276T patent/PL2681219T3/pl unknown
- 2012-02-29 CA CA2824360A patent/CA2824360C/en active Active
- 2012-02-29 SG SG2013064746A patent/SG192963A1/en unknown
- 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 PT PT127072767T patent/PT2681219E/pt unknown
- 2012-02-29 JP JP2013555862A patent/JP5853033B2/ja not_active Expired - Fee Related
- 2012-02-29 EP EP12707276.7A patent/EP2681219B1/en active Active
- 2012-02-29 KR KR1020137022392A patent/KR102012671B1/ko not_active Expired - Fee Related
- 2012-02-29 CN CN201280011146.5A patent/CN103415519B/zh not_active Expired - Fee Related
- 2012-02-29 DK DK12707276.7T patent/DK2681219T3/en active
- 2012-02-29 AU AU2012222394A patent/AU2012222394B2/en not_active Ceased
- 2012-02-29 ES ES12707276.7T patent/ES2558779T3/es active Active
- 2012-02-29 MY MYPI2013003200A patent/MY161407A/en unknown
- 2012-02-29 SI SI201230429T patent/SI2681219T1/sl unknown
- 2012-02-29 BR BR112013022039A patent/BR112013022039A2/pt not_active Application Discontinuation
- 2012-02-29 HU HUE12707276A patent/HUE026338T2/en unknown
- 2012-02-29 UA UAA201308783A patent/UA109800C2/ru unknown
- 2012-02-29 PH PH1/2013/501807A patent/PH12013501807A1/en unknown
-
2013
- 2013-08-28 CL CL2013002486A patent/CL2013002486A1/es unknown
- 2013-08-28 IL IL228158A patent/IL228158A/en active IP Right Grant
- 2013-08-29 CO CO13205178A patent/CO6751282A2/es unknown
- 2013-08-30 ZA ZA2013/06545A patent/ZA201306545B/en unknown
-
2016
- 2016-01-28 CY CY20161100087T patent/CY1117663T1/el unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2014506907A5 (enExample) | ||
| JP2014507455A5 (enExample) | ||
| JP2015537020A5 (enExample) | ||
| JP2013510120A5 (enExample) | ||
| HRP20160030T1 (hr) | Derivati 6,7-dihidro-pirazolo[1,5-a]pirazin-4-ilamina koji su korisni kao inhibitori beta-sekretaze (bace) | |
| JP2013056919A5 (enExample) | ||
| JP2018513215A5 (enExample) | ||
| JP2016506935A5 (enExample) | ||
| JP2013542261A5 (enExample) | ||
| JP2013545785A5 (enExample) | ||
| JP2016516043A5 (enExample) | ||
| JP2012092103A5 (enExample) | ||
| JP2014511892A5 (enExample) | ||
| JP2015520140A5 (enExample) | ||
| JP2014508811A5 (enExample) | ||
| JP2013032389A5 (enExample) | ||
| JP2018537413A5 (ja) | 化合物、医薬的に許容される塩又はその立体異性体及び医薬組成物 | |
| JP2014051526A5 (enExample) | ||
| JP2017533968A5 (enExample) | ||
| UA115881C2 (uk) | Алкоксипіразоли як активатори розчинної гуанілатциклази | |
| JP2015500223A5 (enExample) | ||
| JP2015504081A5 (enExample) | ||
| JP2015500257A5 (enExample) | ||
| JP2014534981A5 (enExample) | ||
| JP2014508804A5 (enExample) |