EA023824B1 - ПРОИЗВОДНЫЕ 3,4-ДИГИДРОПИРРОЛО[1,2-a]ПИРАЗИН-1-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) - Google Patents
ПРОИЗВОДНЫЕ 3,4-ДИГИДРОПИРРОЛО[1,2-a]ПИРАЗИН-1-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) Download PDFInfo
- Publication number
- EA023824B1 EA023824B1 EA201391296A EA201391296A EA023824B1 EA 023824 B1 EA023824 B1 EA 023824B1 EA 201391296 A EA201391296 A EA 201391296A EA 201391296 A EA201391296 A EA 201391296A EA 023824 B1 EA023824 B1 EA 023824B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- group
- dementia
- alkyl
- compound according
- heteroaryl
- Prior art date
Links
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract description 5
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract description 5
- 239000003112 inhibitor Substances 0.000 title abstract 2
- MBVCQKKUMUXAMH-UHFFFAOYSA-N 3,4-dihydropyrrolo[1,2-a]pyrazin-1-amine Chemical class NC1=NCCN2C=CC=C12 MBVCQKKUMUXAMH-UHFFFAOYSA-N 0.000 title description 2
- 206010012289 Dementia Diseases 0.000 claims abstract description 19
- 150000001875 compounds Chemical class 0.000 claims abstract description 14
- 208000024827 Alzheimer disease Diseases 0.000 claims abstract description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 5
- 201000010374 Down Syndrome Diseases 0.000 claims abstract description 4
- 208000018737 Parkinson disease Diseases 0.000 claims abstract description 4
- 208000010877 cognitive disease Diseases 0.000 claims abstract description 4
- 208000027061 mild cognitive impairment Diseases 0.000 claims abstract description 4
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims abstract description 3
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims abstract description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 3
- 208000035475 disorder Diseases 0.000 claims abstract description 3
- 230000002265 prevention Effects 0.000 claims abstract description 3
- 230000008033 biological extinction Effects 0.000 claims description 3
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 6
- -1 chloro, fluoro, cyano, methyl Chemical group 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 239000013256 coordination polymer Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 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
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 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
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract description 6
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract description 4
- 239000000203 mixture Substances 0.000 abstract description 4
- 108090000790 Enzymes Proteins 0.000 abstract description 2
- 102000004190 Enzymes Human genes 0.000 abstract 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 abstract description 2
- 101710150192 Beta-secretase 1 Proteins 0.000 abstract 2
- 206010067889 Dementia with Lewy bodies Diseases 0.000 abstract 1
- 201000002832 Lewy body dementia Diseases 0.000 abstract 1
- 206010039966 Senile dementia Diseases 0.000 abstract 1
- 206010044688 Trisomy 21 Diseases 0.000 abstract 1
- 239000002439 beta secretase inhibitor Substances 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
Classifications
-
- 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
-
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- 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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 (2)
| Publication Number | Publication Date |
|---|---|
| EA201391296A1 EA201391296A1 (ru) | 2014-01-30 |
| EA023824B1 true EA023824B1 (ru) | 2016-07-29 |
Family
ID=43833325
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201391296A EA023824B1 (ru) | 2011-03-09 | 2012-03-07 | ПРОИЗВОДНЫЕ 3,4-ДИГИДРОПИРРОЛО[1,2-a]ПИРАЗИН-1-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) |
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 |
|---|---|---|---|---|
| ES2476027T3 (es) | 2005-10-25 | 2014-07-11 | Shionogi & Co., Ltd. | Derivados de aminodihidrotriazina |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| KR20100017255A (ko) | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 유도체 |
| MX2010013256A (es) | 2008-06-13 | 2010-12-21 | Shionogi & Co | Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa. |
| EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
| JPWO2011071135A1 (ja) | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | オキサジン誘導体 |
| EP2580200B1 (en) | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 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 |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| CN103403007B (zh) | 2010-12-22 | 2015-12-09 | 詹森药业有限公司 | 用作β-分泌酶(BACE)抑制剂的5,6-二氢-咪唑并[1,2-a]吡嗪-8-基胺衍生物 |
| BR112013022039A2 (pt) | 2011-03-01 | 2016-11-29 | Janssen Pharmaceutica Nv | derivados 6,7-di-hidro-pirazol[1,5-a]pirazin-4-ilamina úteis como inibidores de beta-secretase (bace) |
| KR102012675B1 (ko) * | 2011-03-09 | 2019-08-21 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(BACE)의 억제제로서 유용한 3,4-디하이드로-피롤로[1,2-a]피라진-1-일아민 유도체 |
| WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 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 |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| CA2911690C (en) * | 2013-06-12 | 2021-08-24 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
| AU2014280125B2 (en) | 2013-06-12 | 2018-03-15 | 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) |
| BR112015030498A2 (pt) | 2013-06-12 | 2017-07-25 | Janssen Pharmaceutica Nv | derivados 4-amino-6-fenil-5,6-di-hidroimidazo[1,5-a]pirazin-3(2h)-ona como inibidores de beta-secretase (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 |
| WO2016096979A1 (en) | 2014-12-18 | 2016-06-23 | Janssen Pharmaceutica Nv | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase |
| US10357493B2 (en) | 2017-03-10 | 2019-07-23 | Selenity Therapeutics (Bermuda), Ltd. | 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Family Cites Families (53)
| 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 | |
| WO1998057641A1 (en) | 1997-06-18 | 1998-12-23 | Merck & Co., Inc. | ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS |
| WO2003089434A2 (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 |
| AU2003272476B2 (en) | 2002-09-23 | 2007-07-05 | Schering Corporation | 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 |
| JP2007533641A (ja) | 2003-10-15 | 2007-11-22 | ターガセプト，インコーポレイテッド | 疼痛緩和および中枢神経系障害治療のためのアザビシクロ化合物 |
| JP2007533741A (ja) | 2004-04-22 | 2007-11-22 | イーライ リリー アンド カンパニー | Ｂａｃｅ阻害剤 |
| 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 |
| CN2781924Y (zh) | 2005-01-21 | 2006-05-24 | 厦门革新塑胶制品有限公司 | 折叠床中部支脚 |
| US20070005404A1 (en) | 2005-06-09 | 2007-01-04 | Drive Diagnostics Ltd. | System and method for providing driving insurance |
| CA2610828A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
| AU2006266167A1 (en) | 2005-06-30 | 2007-01-11 | Wyeth | Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation |
| ES2476027T3 (es) | 2005-10-25 | 2014-07-11 | Shionogi & Co., Ltd. | Derivados de aminodihidrotriazina |
| 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 |
| 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 |
| KR20100017255A (ko) | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 유도체 |
| EP2217592A1 (en) | 2007-10-30 | 2010-08-18 | Arena Pharmaceuticals, Inc. | Biphenyl derivatives as modulators of the histamine-h3 receptor useful for the treatment of disorders related thereto |
| RU2497821C2 (ru) | 2008-01-28 | 2013-11-10 | Янссен Фармацевтика Нв | ПРОИЗВОДНЫЕ 6-ЗАМЕЩЕННОГО-ТИО (ИЛИ -ОКСО-)-2-АМИНО-ХИНОЛИНА, ПРИМЕНЯЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ β-СЕКРЕТАЗЫ (BACE) |
| EP2252617A1 (en) | 2008-02-13 | 2010-11-24 | CGI Pharmaceuticals, Inc. | 6-aryl-imidaz0[l, 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 |
| 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 |
| JPWO2011071135A1 (ja) | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | オキサジン誘導体 |
| 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 |
| 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 |
| BR112012015916A2 (pt) | 2009-12-31 | 2017-04-25 | Novartis Ag | derivados de pirazina e seu uso no tratamento de distúrbios neurológicos |
| MX2012014382A (es) | 2010-06-09 | 2013-01-29 | Janssen Pharmaceutica Nv | Derivados de 5-amino-3, 6-dihidro-1h-pirazin-2-ona utiles como inhibidores de beta-secretasa (bace). |
| EP2580200B1 (en) | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| BR112012033291A2 (pt) | 2010-06-28 | 2016-11-22 | Janssen Pharmaceutica Nv | derivados de 3-amino-5,6-di-hidro-1h-piranzin-2-ona úteis para o tratamento de doença de alzheimer e outras formas de demência |
| PH12013500345A1 (en) | 2010-09-22 | 2022-03-30 | Janssen Pharmaceutica Nv | 4,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-6-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| CN103403007B (zh) | 2010-12-22 | 2015-12-09 | 詹森药业有限公司 | 用作β-分泌酶(BACE)抑制剂的5,6-二氢-咪唑并[1,2-a]吡嗪-8-基胺衍生物 |
| CA2824097A1 (en) | 2011-01-12 | 2012-07-19 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| 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 |
| BR112013022039A2 (pt) | 2011-03-01 | 2016-11-29 | Janssen Pharmaceutica Nv | derivados 6,7-di-hidro-pirazol[1,5-a]pirazin-4-ilamina úteis como inibidores de beta-secretase (bace) |
| KR102012675B1 (ko) | 2011-03-09 | 2019-08-21 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(BACE)의 억제제로서 유용한 3,4-디하이드로-피롤로[1,2-a]피라진-1-일아민 유도체 |
| WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 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 |
| WO2013054291A1 (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 |
| EP2788335B1 (en) | 2011-12-06 | 2016-04-13 | Janssen Pharmaceutica, N.V. | 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives for the treatment of disorders in which beta-secretase is involved |
| CN104870000A (zh) | 2012-12-20 | 2015-08-26 | 默沙东公司 | 作为bace抑制剂的c5,c6氧杂环稠合的亚胺基噻嗪二氧化物化合物,组合物及其用途 |
| AU2014280125B2 (en) | 2013-06-12 | 2018-03-15 | 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) |
| CA2911690C (en) | 2013-06-12 | 2021-08-24 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
| BR112015030498A2 (pt) | 2013-06-12 | 2017-07-25 | Janssen Pharmaceutica Nv | derivados 4-amino-6-fenil-5,6-di-hidroimidazo[1,5-a]pirazin-3(2h)-ona como inibidores de beta-secretase (bace) |
| WO2016096979A1 (en) | 2014-12-18 | 2016-06-23 | Janssen Pharmaceutica Nv | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase |
-
2012
- 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 JP JP2013557074A patent/JP5853035B2/ja not_active Expired - Fee Related
- 2012-03-07 AU AU2012224632A patent/AU2012224632B2/en not_active Ceased
- 2012-03-07 PH PH1/2013/501805A patent/PH12013501805A1/en unknown
- 2012-03-07 ES ES12707319.5T patent/ES2534973T3/es active Active
- 2012-03-07 WO PCT/EP2012/053863 patent/WO2012120023A1/en not_active Ceased
- 2012-03-07 EA EA201391296A patent/EA023824B1/ru not_active IP Right Cessation
- 2012-03-07 EP EP12707319.5A patent/EP2683721B1/en not_active Not-in-force
- 2012-03-07 MX MX2013010280A patent/MX340031B/es active IP Right Grant
- 2012-03-07 US US14/003,901 patent/US9845326B2/en active Active
- 2012-03-07 CA CA2825620A patent/CA2825620C/en active Active
- 2012-03-07 BR BR112013022917A patent/BR112013022917A2/pt not_active Application Discontinuation
- 2012-03-07 CN CN201280012485.5A patent/CN103415521B/zh not_active Expired - Fee Related
- 2012-03-07 MY MYPI2013003278A patent/MY163346A/en unknown
- 2012-07-03 UA UAA201308782A patent/UA109687C2/ru unknown
-
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
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| MX2013010280A (es) | 2013-10-01 |
| CO6751283A2 (es) | 2013-09-16 |
| IL228239A0 (en) | 2013-11-25 |
| JP5853035B2 (ja) | 2016-02-09 |
| WO2012120023A1 (en) | 2012-09-13 |
| SG193342A1 (en) | 2013-10-30 |
| UA109687C2 (xx) | 2015-09-25 |
| ES2534973T3 (es) | 2015-04-30 |
| US20130345228A1 (en) | 2013-12-26 |
| AU2012224632A1 (en) | 2013-08-01 |
| ZA201306719B (en) | 2015-04-29 |
| MX340031B (es) | 2016-06-21 |
| BR112013022917A2 (pt) | 2016-12-06 |
| JP2014507455A (ja) | 2014-03-27 |
| PH12013501805A1 (en) | 2013-11-18 |
| CA2825620A1 (en) | 2012-09-13 |
| CA2825620C (en) | 2019-04-23 |
| KR102012675B1 (ko) | 2019-08-21 |
| US9845326B2 (en) | 2017-12-19 |
| EP2683721A1 (en) | 2014-01-15 |
| MY163346A (en) | 2017-09-15 |
| HK1189223A1 (zh) | 2014-05-30 |
| CL2013002511A1 (es) | 2014-01-24 |
| KR20140019332A (ko) | 2014-02-14 |
| EP2683721B1 (en) | 2015-01-28 |
| NZ615720A (en) | 2014-08-29 |
| EA201391296A1 (ru) | 2014-01-30 |
| IL228239A (en) | 2016-06-30 |
| CN103415521A (zh) | 2013-11-27 |
| CN103415521B (zh) | 2016-01-06 |
| AU2012224632B2 (en) | 2016-06-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EA023824B1 (ru) | ПРОИЗВОДНЫЕ 3,4-ДИГИДРОПИРРОЛО[1,2-a]ПИРАЗИН-1-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) | |
| PH12019501355A1 (en) | Small molecule inhibitors of the jak family of kinases | |
| EP4249076A3 (en) | (s)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-2-methoxy-n-(pyridin-2-yl)benzamide as btk-inhibitor | |
| NZ630721A (en) | Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use | |
| EA201891463A1 (ru) | ПРОИЗВОДНЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИН-4-ИЛА В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ (JAK) | |
| PH12019501254A1 (en) | Small molecule inhibitors of the jak family of kinases | |
| EA201391251A1 (ru) | ПРОИЗВОДНЫЕ 6,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-4-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) | |
| PH12013502445A1 (en) | Pyridin-2 (1h) -one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases | |
| EA201290244A1 (ru) | ПРОИЗВОДНЫЕ ИМИДАЗО[1,2-b]ПИРИДАЗИНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE10 | |
| EA201290878A1 (ru) | ПРОИЗВОДНЫЕ ИМИДАЗО[1,2-a]ПИРАЗИНА И ИХ ПРИМЕНЕНИЕ ДЛЯ ПРОФИЛАКТИКИ ИЛИ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ, ПСИХИАТРИЧЕСКИХ И МЕТАБОЛИЧЕСКИХ РАССТРОЙСТВ И ЗАБОЛЕВАНИЙ | |
| NZ612041A (en) | Compounds and their use as bace inhibitors | |
| NZ608718A (en) | Imidazo[1,2-b]pyridazine and imidazo[4,5-b]pyridine derivatives as jak inhibitors | |
| EA200601350A1 (ru) | Азотсодержащие гетероциклические производные и их фармацевтические применения | |
| MX2010007714A (es) | Piridinas fusionadas activas como inhibidores de c-met. | |
| JP2018507877A5 (enExample) | ||
| SG10201804791UA (en) | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof | |
| EA201001696A1 (ru) | СОЕДИНЕНИЯ ХИНУКЛИДИНА В КАЧЕСТВЕ ЛИГАНДОВ НИКОТИНОВОГО АЦЕТИЛХОЛИНОВОГО РЕЦЕПТОРА α7 | |
| MX2010006748A (es) | Pirazolo[1,5-a]pirimidinas utiles como inhibidores de jak2. | |
| PE20090493A1 (es) | DERIVADOS DE LA 6-CICLOAMINO-3-(PIRIDAZIN-4-IL)IMIDAZO[1,2-b]-PIRIDAZINA, SU PREPARACION Y SU APLICACION EN TERAPEUTICA | |
| EA201390971A1 (ru) | ИМИДАЗО[5,1-f][1,2,4]ТРИАЗИНЫ ДЛЯ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ РАССТРОЙСТВ | |
| NZ613235A (en) | Substituted n-(1h-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide compounds as type iii receptor tyrosine kinase inhibitors | |
| SG195085A1 (en) | Pyrazolo[3,4-d]pyrimidine compounds and their use as pde2 inhibitors and/or cyp3a4 inhibitors | |
| EA201171306A1 (ru) | ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ ИМИДАЗО[1,2-α]ПИРИДИНА, ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ И СПОСОБЫ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ β-СЕКРЕТАЗЫ | |
| PH12019500497A1 (en) | Heteroaryl carboxamide compounds as inhibitors of ripk2 | |
| EA201491116A1 (ru) | Производные 6-дифторметил-5,6-дигидро-2h-[1,4]оксазин-3-амина |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM |