AU2012224632B2 - 3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives useful as inhibitors of beta-secretase (BACE) - Google Patents
3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives useful as inhibitors of beta-secretase (BACE) Download PDFInfo
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- AU2012224632B2 AU2012224632B2 AU2012224632A AU2012224632A AU2012224632B2 AU 2012224632 B2 AU2012224632 B2 AU 2012224632B2 AU 2012224632 A AU2012224632 A AU 2012224632A AU 2012224632 A AU2012224632 A AU 2012224632A AU 2012224632 B2 AU2012224632 B2 AU 2012224632B2
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- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract description 22
- 239000003112 inhibitor Substances 0.000 title abstract description 8
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
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- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 16
- 125000001424 substituent group Chemical group 0.000 claims description 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 14
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- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
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- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 30
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
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- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
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| 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) |
| 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 |
| 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) |
| 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) |
| 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). |
| 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 |
| US10357493B2 (en) | 2017-03-10 | 2019-07-23 | Selenity Therapeutics (Bermuda), Ltd. | Metalloenzyme inhibitor compounds |
| EP4003319A4 (en) | 2019-07-30 | 2023-11-08 | Eikonizo Therapeutics, Inc. | HDAC6 INHIBITORS AND THEIR USES |
| 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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| WO2006076284A2 (en) * | 2005-01-14 | 2006-07-20 | Wyeth | AMINO-IMIDAZOLONES FOR THE INHIBITION OF ß-SECRETASE |
| WO2009022961A1 (en) * | 2007-05-15 | 2009-02-19 | Astrazeneca Ab | Pyrrolopyridine derivatives and their use as bace inhibitors |
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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 (enExample) | 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 |
| 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 |
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- 2012-03-07 JP JP2013557074A patent/JP5853035B2/ja not_active Expired - Fee Related
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| JP2014507455A (ja) | 2014-03-27 |
| CA2825620C (en) | 2019-04-23 |
| KR102012675B1 (ko) | 2019-08-21 |
| EP2683721B1 (en) | 2015-01-28 |
| US9845326B2 (en) | 2017-12-19 |
| MX2013010280A (es) | 2013-10-01 |
| CN103415521B (zh) | 2016-01-06 |
| AU2012224632A1 (en) | 2013-08-01 |
| IL228239A (en) | 2016-06-30 |
| UA109687C2 (xx) | 2015-09-25 |
| CA2825620A1 (en) | 2012-09-13 |
| BR112013022917A2 (pt) | 2016-12-06 |
| EA201391296A1 (ru) | 2014-01-30 |
| US20130345228A1 (en) | 2013-12-26 |
| WO2012120023A1 (en) | 2012-09-13 |
| CN103415521A (zh) | 2013-11-27 |
| KR20140019332A (ko) | 2014-02-14 |
| ZA201306719B (en) | 2015-04-29 |
| JP5853035B2 (ja) | 2016-02-09 |
| MX340031B (es) | 2016-06-21 |
| HK1189223A1 (zh) | 2014-05-30 |
| CL2013002511A1 (es) | 2014-01-24 |
| MY163346A (en) | 2017-09-15 |
| NZ615720A (en) | 2014-08-29 |
| EP2683721A1 (en) | 2014-01-15 |
| ES2534973T3 (es) | 2015-04-30 |
| IL228239A0 (en) | 2013-11-25 |
| SG193342A1 (en) | 2013-10-30 |
| CO6751283A2 (es) | 2013-09-16 |
| EA023824B1 (ru) | 2016-07-29 |
| PH12013501805A1 (en) | 2013-11-18 |
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