JP5666578B2 - Bace阻害剤 - Google Patents
Bace阻害剤 Download PDFInfo
- Publication number
- JP5666578B2 JP5666578B2 JP2012519660A JP2012519660A JP5666578B2 JP 5666578 B2 JP5666578 B2 JP 5666578B2 JP 2012519660 A JP2012519660 A JP 2012519660A JP 2012519660 A JP2012519660 A JP 2012519660A JP 5666578 B2 JP5666578 B2 JP 5666578B2
- Authority
- JP
- Japan
- Prior art keywords
- mmol
- compound
- mixture
- thiazin
- give
- 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.)
- Expired - Fee Related
Links
- BWTLRGGAKJJXGW-UHFFFAOYSA-N C=CCC(CC(c1cccc(Br)c1)=O)O Chemical compound C=CCC(CC(c1cccc(Br)c1)=O)O BWTLRGGAKJJXGW-UHFFFAOYSA-N 0.000 description 1
- FZPDUQMVCUHXOC-UPCLLVRISA-N CC(C)(C)OC(NC(SC[C@@H]1COCC2)=N[C@]12c1cc(NC(c(nc2)ccc2Cl)=O)ccc1)=O Chemical compound CC(C)(C)OC(NC(SC[C@@H]1COCC2)=N[C@]12c1cc(NC(c(nc2)ccc2Cl)=O)ccc1)=O FZPDUQMVCUHXOC-UPCLLVRISA-N 0.000 description 1
- SYHIKASWLISSDU-SCLBCKFNSA-N CC(C)(C)OC(NC(SC[C@@H]1COCC2)=N[C@]12c1cccc(Br)c1)=O Chemical compound CC(C)(C)OC(NC(SC[C@@H]1COCC2)=N[C@]12c1cccc(Br)c1)=O SYHIKASWLISSDU-SCLBCKFNSA-N 0.000 description 1
- UDTVLUJDRFAZPE-UHFFFAOYSA-N CC(C)(C)[S+](C)OC1CC2(c3cc(Br)ccc3)N(Cc3ccccc3)OCC2C1 Chemical compound CC(C)(C)[S+](C)OC1CC2(c3cc(Br)ccc3)N(Cc3ccccc3)OCC2C1 UDTVLUJDRFAZPE-UHFFFAOYSA-N 0.000 description 1
- 0 CC1(*)C=C(*)C=C(CC23N=C(N)SC[C@@]2CC(C)(*)*C*C3)C=C1 Chemical compound CC1(*)C=C(*)C=C(CC23N=C(N)SC[C@@]2CC(C)(*)*C*C3)C=C1 0.000 description 1
- ZQDOSAAJSBWVGK-KSCKTEMCSA-N CO[C@H]1C[C@]2(c3cccc(-c4cc(OC)ccc4)c3)N=C(NC(c3ccccc3)=O)SC[C@@H]2C1 Chemical compound CO[C@H]1C[C@]2(c3cccc(-c4cc(OC)ccc4)c3)N=C(NC(c3ccccc3)=O)SC[C@@H]2C1 ZQDOSAAJSBWVGK-KSCKTEMCSA-N 0.000 description 1
- GFAVJTQPFPSTAZ-QHWMMSMNSA-N COc1cccc(-c2cc([C@@]3(C4)N=C(NC(c5ccccc5)=O)SC[C@@H]3C[C@H]4O)ccc2)c1 Chemical compound COc1cccc(-c2cc([C@@]3(C4)N=C(NC(c5ccccc5)=O)SC[C@@H]3C[C@H]4O)ccc2)c1 GFAVJTQPFPSTAZ-QHWMMSMNSA-N 0.000 description 1
- PPUZKAPOPPRMFE-UHFFFAOYSA-N Fc(c(Br)c1)cc(F)c1Br Chemical compound Fc(c(Br)c1)cc(F)c1Br PPUZKAPOPPRMFE-UHFFFAOYSA-N 0.000 description 1
- DSYFAJZNPXCGCV-TVQRCGJNSA-N NC(SC[C@@H]1CCC2)=N[C@]12c(cc1O)ccc1F Chemical compound NC(SC[C@@H]1CCC2)=N[C@]12c(cc1O)ccc1F DSYFAJZNPXCGCV-TVQRCGJNSA-N 0.000 description 1
- HTAGDFOCHJHXHE-UHFFFAOYSA-N OC1(CCOCC1)c1cc(Br)ccc1 Chemical compound OC1(CCOCC1)c1cc(Br)ccc1 HTAGDFOCHJHXHE-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
- C07D279/08—1,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22424109P | 2009-07-09 | 2009-07-09 | |
| US61/224,241 | 2009-07-09 | ||
| PCT/US2010/041034 WO2011005738A1 (en) | 2009-07-09 | 2010-07-06 | Bace inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012532874A JP2012532874A (ja) | 2012-12-20 |
| JP2012532874A5 JP2012532874A5 (enExample) | 2013-08-15 |
| JP5666578B2 true JP5666578B2 (ja) | 2015-02-12 |
Family
ID=42985394
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012519660A Expired - Fee Related JP5666578B2 (ja) | 2009-07-09 | 2010-07-06 | Bace阻害剤 |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US8278441B2 (enExample) |
| EP (1) | EP2451793B1 (enExample) |
| JP (1) | JP5666578B2 (enExample) |
| KR (1) | KR101362557B1 (enExample) |
| CN (1) | CN102471296B (enExample) |
| AR (1) | AR077277A1 (enExample) |
| AU (1) | AU2010270691B8 (enExample) |
| BR (1) | BR112012000525A2 (enExample) |
| CA (1) | CA2764429C (enExample) |
| CL (1) | CL2012000033A1 (enExample) |
| CO (1) | CO6480979A2 (enExample) |
| CR (1) | CR20120011A (enExample) |
| DO (1) | DOP2012000004A (enExample) |
| EA (1) | EA019892B1 (enExample) |
| EC (1) | ECSP12011581A (enExample) |
| HN (1) | HN2012000012A (enExample) |
| IL (1) | IL216742A0 (enExample) |
| MA (1) | MA33492B1 (enExample) |
| MX (1) | MX2012000510A (enExample) |
| NZ (1) | NZ596579A (enExample) |
| PE (1) | PE20120632A1 (enExample) |
| SG (1) | SG177594A1 (enExample) |
| TN (1) | TN2011000673A1 (enExample) |
| TW (1) | TWI405765B (enExample) |
| WO (1) | WO2011005738A1 (enExample) |
| ZA (1) | ZA201109385B (enExample) |
Families Citing this family (85)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| 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 |
| HRP20151030T1 (hr) | 2008-01-18 | 2015-11-06 | Eisai R&D Management Co., Ltd. | Kondenzirani derivat aminodihidrotiazina |
| MX2010013256A (es) | 2008-06-13 | 2010-12-21 | Shionogi & Co | Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa. |
| AU2009277485B2 (en) * | 2008-07-28 | 2013-05-02 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| WO2010038686A1 (ja) * | 2008-09-30 | 2010-04-08 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 新規な縮合アミノジヒドロチアジン誘導体 |
| EP2360155A4 (en) * | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| WO2011044184A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2511269A4 (en) * | 2009-12-11 | 2013-04-24 | Shionogi & Co | FUSED HETEROCYCLIC COMPOUND HAVING AN AMINO GROUP |
| 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 |
| GB201100181D0 (en) * | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| SG10201601516QA (en) * | 2011-01-21 | 2016-03-30 | Eisai R&D Man Co Ltd | Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| 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 |
| EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| 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 |
| US8604024B2 (en) | 2011-05-24 | 2013-12-10 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| US8598161B2 (en) | 2011-05-24 | 2013-12-03 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| US8927535B2 (en) * | 2011-07-06 | 2015-01-06 | Hoffman-La Roche Inc. | Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors |
| BR112014004181A2 (pt) | 2011-08-22 | 2017-06-13 | Merck Sharp & Dohme | composto, composição farmacêutica, e, método de tratamento, prevenção, e / ou retardo do início de uma doença ou patologia |
| WO2013030713A1 (en) | 2011-08-31 | 2013-03-07 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds |
| JO3143B1 (ar) | 2012-04-03 | 2017-09-20 | Lilly Co Eli | مركبات تتراهيدرو بيرولو ثيازين |
| HUE030534T2 (hu) | 2012-04-27 | 2017-05-29 | Eisai R&D Man Co Ltd | Eljárás 5-(difluormetil)pirazin-2-karbonsav elõállítására és elõállítási intermediere |
| WO2013164730A1 (en) | 2012-05-04 | 2013-11-07 | Pfizer Inc. | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2. |
| GB201212871D0 (en) | 2012-07-20 | 2012-09-05 | Eisai Ltd | Novel compounds |
| JP2015529239A (ja) | 2012-09-20 | 2015-10-05 | ファイザー・インク | アルキル置換ヘキサヒドロピラノ[3,4−d][1,3]チアジン−2−アミン化合物 |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| US9328124B2 (en) * | 2012-10-26 | 2016-05-03 | Eli Lilly And Company | BACE inhibitors |
| WO2014091352A1 (en) * | 2012-12-11 | 2014-06-19 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1 |
| WO2014098831A1 (en) | 2012-12-19 | 2014-06-26 | Bristol-Myers Squibb Company | 4,6-diarylaminothiazines as bace1 inhibitors and their use for the reduction of beta-amyloid production |
| CA2893333C (en) | 2012-12-19 | 2017-10-24 | Pfizer Inc. | Carbocyclic-and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| WO2014120658A1 (en) | 2013-01-29 | 2014-08-07 | Amgen Inc. | Fused multicyclic 3-amino-5,6-dihydro-2h-1,4-thiazine derivatives and their use as beta-secretase inhibitors |
| ES2769578T3 (es) | 2013-02-12 | 2020-06-26 | Buck Inst Res Aging | Hidantoínas que modulan el procesamiento de APP mediado por BACE |
| EP2956458B1 (en) | 2013-02-13 | 2017-08-09 | Pfizer Inc | Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| US9233981B1 (en) | 2013-02-15 | 2016-01-12 | Pfizer Inc. | Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| AU2014223334C1 (en) * | 2013-03-01 | 2018-10-18 | Amgen Inc. | Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| JP6374889B2 (ja) | 2013-03-08 | 2018-08-15 | アムジエン・インコーポレーテツド | β−セクレターゼ阻害剤としての過フッ素化シクロプロピル縮合1,3−オキサジン−2−アミン化合物、及び使用方法 |
| TWI593692B (zh) | 2013-03-12 | 2017-08-01 | 美國禮來大藥廠 | 四氫吡咯并噻嗪化合物 |
| 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) |
| 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) |
| JO3318B1 (ar) * | 2013-06-18 | 2019-03-13 | Lilly Co Eli | مثبطات bace |
| US9096615B2 (en) | 2013-07-30 | 2015-08-04 | Amgen Inc. | Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof |
| CA2944971C (en) | 2014-04-10 | 2019-05-07 | Pfizer Inc. | 2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8h)-yl-1,3-thiazol-4-yl amides |
| US9550762B2 (en) | 2014-08-08 | 2017-01-24 | Amgen, Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| JO3458B1 (ar) | 2014-11-10 | 2020-07-05 | H Lundbeck As | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
| CR20170187A (es) | 2014-11-10 | 2018-02-01 | H Lundbeck As | 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer |
| MA40941A (fr) | 2014-11-10 | 2017-09-19 | H Lundbeck As | 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 |
| 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 |
| AR103680A1 (es) | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
| US9938266B2 (en) | 2015-03-19 | 2018-04-10 | Eli Lilly And Company | Selective BACE1 inhibitors |
| AR104241A1 (es) | 2015-04-29 | 2017-07-05 | Lilly Co Eli | Derivados de tetrahidrofuro tiazina como inhibidores de bace1 selectivos |
| WO2017024180A1 (en) | 2015-08-06 | 2017-02-09 | Amgen Inc. | Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| TW201717948A (zh) | 2015-08-10 | 2017-06-01 | H 朗德貝克公司 | 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療 |
| EP3334738A1 (en) * | 2015-08-12 | 2018-06-20 | H. Lundbeck A/S | 2-amino-7a-phenyl-3,4,4a,5,7,7a-hexahydrofuro[3,4-b]pyridines as bace1 inhibitors |
| US10011596B2 (en) | 2015-08-12 | 2018-07-03 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors |
| EP3353182A1 (en) | 2015-09-24 | 2018-08-01 | Pfizer Inc | Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors |
| WO2017051294A1 (en) | 2015-09-24 | 2017-03-30 | Pfizer Inc. | N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2h-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl] amides useful as bace inhibitors |
| EP3353183A1 (en) | 2015-09-24 | 2018-08-01 | Pfizer Inc | N-[2-(2-amino-6,6-disubstituted-4, 4a, 5, 6-tetrahydropyrano [3,4-d][1,3]thiazin-8a (8h)-yl) -1, 3-thiazol-4-yl]amides |
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| EP3555106B1 (en) | 2016-12-15 | 2022-03-09 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| CA3047286A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555085B1 (en) | 2016-12-15 | 2020-12-02 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
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| CN101061113A (zh) * | 2004-11-23 | 2007-10-24 | 默克公司 | 作为β-内分泌抑制剂用于治疗阿耳茨海默氏病的2,3,4,6-四取代吡啶衍生物 |
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| WO2007058581A1 (en) * | 2005-11-15 | 2007-05-24 | Astrazeneca Ab | Novel 2-aminopyrimidine derivatives and their use |
| 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 |
| ITTO20070665A1 (it) * | 2007-09-24 | 2009-03-25 | Rottapharm Spa | Derivati amidinici, tioureici e guanidinici di 2-amminobenzotiazoli e amminobenzotiazine, nuovi agenti farmacologici per il trattamento delle patologie neurodegenerative. |
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| MX2010013256A (es) | 2008-06-13 | 2010-12-21 | Shionogi & Co | Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa. |
| WO2010038686A1 (ja) * | 2008-09-30 | 2010-04-08 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 新規な縮合アミノジヒドロチアジン誘導体 |
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