CN102015667B - 作为用于治疗阿尔茨海默氏病的bace抑制剂的氨基二氢噻嗪衍生物 - Google Patents
作为用于治疗阿尔茨海默氏病的bace抑制剂的氨基二氢噻嗪衍生物 Download PDFInfo
- Publication number
- CN102015667B CN102015667B CN2009801153849A CN200980115384A CN102015667B CN 102015667 B CN102015667 B CN 102015667B CN 2009801153849 A CN2009801153849 A CN 2009801153849A CN 200980115384 A CN200980115384 A CN 200980115384A CN 102015667 B CN102015667 B CN 102015667B
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- methyl
- compound
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- 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.)
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- BZBAYMUKLAYQEO-UHFFFAOYSA-N Bc1ccccc1 Chemical compound Bc1ccccc1 BZBAYMUKLAYQEO-UHFFFAOYSA-N 0.000 description 1
- ZQEBQCWDENSRSH-IBGZPJMESA-N CC(C)(C)OC(NC1=N[C@@H](CCc2cc(-c3cncnc3)c(C)cc2C)CCS1)=O Chemical compound CC(C)(C)OC(NC1=N[C@@H](CCc2cc(-c3cncnc3)c(C)cc2C)CCS1)=O ZQEBQCWDENSRSH-IBGZPJMESA-N 0.000 description 1
- XXRCBGDCSKWIOV-ZZUHDNHVSA-N CC(C1)SC(N)=N[C@]1(C)c(c(F)c1)cc(Br)c1F Chemical compound CC(C1)SC(N)=N[C@]1(C)c(c(F)c1)cc(Br)c1F XXRCBGDCSKWIOV-ZZUHDNHVSA-N 0.000 description 1
- VKHUQKSYHCDUFG-UHFFFAOYSA-N CCOC(C(CC(c1cc(Br)ccc1)=C)O)=O Chemical compound CCOC(C(CC(c1cc(Br)ccc1)=C)O)=O VKHUQKSYHCDUFG-UHFFFAOYSA-N 0.000 description 1
- XQGRIBYZZQKGPC-UHFFFAOYSA-N CNC(NC(c1ccccc1)=O)=S Chemical compound CNC(NC(c1ccccc1)=O)=S XQGRIBYZZQKGPC-UHFFFAOYSA-N 0.000 description 1
- FTPQPNKWJHOSAD-XLLULAGJSA-N C[C@@H]1N=C(NC(c2ccccc2)=O)SC(C)(CI)C1 Chemical compound C[C@@H]1N=C(NC(c2ccccc2)=O)SC(C)(CI)C1 FTPQPNKWJHOSAD-XLLULAGJSA-N 0.000 description 1
- MJQMRGWYPNIERM-HNNXBMFYSA-N C[C@]1(c(c(F)c2)cc(-c3cncnc3)c2F)N=C(N)SCC1 Chemical compound C[C@]1(c(c(F)c2)cc(-c3cncnc3)c2F)N=C(N)SCC1 MJQMRGWYPNIERM-HNNXBMFYSA-N 0.000 description 1
- AOEATMPDADSVRS-NSHDSACASA-N C[C@]1(c(cc2)cc(Br)c2F)N=C(N)SCC1 Chemical compound C[C@]1(c(cc2)cc(Br)c2F)N=C(N)SCC1 AOEATMPDADSVRS-NSHDSACASA-N 0.000 description 1
- LXDTUEPFNUISSH-INIZCTEOSA-N C[C@]1(c2cc(-c3cccnc3F)ccc2)N=C(N)SCC1 Chemical compound C[C@]1(c2cc(-c3cccnc3F)ccc2)N=C(N)SCC1 LXDTUEPFNUISSH-INIZCTEOSA-N 0.000 description 1
Classifications
-
- 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
- C07D279/06—1,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings
-
- 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
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- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4988108P | 2008-05-02 | 2008-05-02 | |
| US61/049881 | 2008-05-02 | ||
| US61/049,881 | 2008-05-02 | ||
| PCT/US2009/040589 WO2009134617A1 (en) | 2008-05-02 | 2009-04-15 | Aminodihydrothiazine derivatives as bace inhibitors for the treatment of alzheimer's disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102015667A CN102015667A (zh) | 2011-04-13 |
| CN102015667B true CN102015667B (zh) | 2013-06-12 |
Family
ID=40839645
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2009801153849A Expired - Fee Related CN102015667B (zh) | 2008-05-02 | 2009-04-15 | 作为用于治疗阿尔茨海默氏病的bace抑制剂的氨基二氢噻嗪衍生物 |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US7648983B2 (https=) |
| EP (1) | EP2297120B1 (https=) |
| JP (3) | JP5658139B2 (https=) |
| KR (1) | KR101253835B1 (https=) |
| CN (1) | CN102015667B (https=) |
| AR (1) | AR071187A1 (https=) |
| AU (1) | AU2009241515B2 (https=) |
| CA (1) | CA2723207C (https=) |
| CL (1) | CL2009000860A1 (https=) |
| CO (1) | CO6311079A2 (https=) |
| CR (1) | CR11776A (https=) |
| DK (1) | DK2297120T3 (https=) |
| DO (1) | DOP2010000328A (https=) |
| EA (1) | EA016955B1 (https=) |
| EC (1) | ECSP10010582A (https=) |
| ES (1) | ES2549087T3 (https=) |
| HR (1) | HRP20150941T1 (https=) |
| HU (1) | HUE025520T2 (https=) |
| IL (1) | IL208350A (https=) |
| MA (1) | MA32351B1 (https=) |
| MX (1) | MX2010011972A (https=) |
| NZ (1) | NZ588300A (https=) |
| PE (1) | PE20091816A1 (https=) |
| PL (1) | PL2297120T3 (https=) |
| PT (1) | PT2297120E (https=) |
| RS (1) | RS54260B1 (https=) |
| SI (1) | SI2297120T1 (https=) |
| SV (1) | SV2010003718A (https=) |
| TW (1) | TWI431004B (https=) |
| UA (1) | UA102251C2 (https=) |
| WO (1) | WO2009134617A1 (https=) |
| ZA (1) | ZA201006868B (https=) |
Families Citing this family (86)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| PE20070135A1 (es) | 2005-06-14 | 2007-03-09 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil proteasas |
| WO2006138265A2 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
| CA2628074C (en) | 2005-10-25 | 2014-01-14 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| PE20080155A1 (es) | 2006-06-12 | 2008-03-10 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil-proteasa |
| US8653067B2 (en) | 2007-04-24 | 2014-02-18 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating Alzheimer's disease |
| JP5383484B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | 環式基で置換されたアミノジヒドロチアジン誘導体 |
| PL2233474T3 (pl) | 2008-01-18 | 2015-12-31 | Eisai R&D Man Co Ltd | Skondensowana pochodna aminodihydrotiazyny |
| CA2723222C (en) | 2008-04-22 | 2013-04-02 | Schering Corporation | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as bace-1 inhibitors, compositions, and their use |
| TWI431004B (zh) * | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| CN102105475B (zh) * | 2008-07-28 | 2014-04-09 | 卫材R&D管理有限公司 | 螺氨基二氢噻嗪衍生物 |
| WO2010021680A2 (en) | 2008-08-19 | 2010-02-25 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| MY148558A (en) | 2008-09-11 | 2013-04-30 | Amgen Inc | Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use |
| JP5666304B2 (ja) * | 2008-09-30 | 2015-02-12 | 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 |
| CN102186841A (zh) | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物 |
| MX2011009571A (es) | 2009-03-13 | 2011-10-19 | Boehringer Ingelheim Int | Inhibidores de beta-secretasa. |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| WO2011044187A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Iminothiadiazine dioxide compounds as bace 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 |
| AU2013234424B9 (en) * | 2009-10-08 | 2014-07-03 | Merck Sharp & Dohme Llc | Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| JPWO2011070781A1 (ja) | 2009-12-09 | 2013-04-22 | 塩野義製薬株式会社 | 置換アミノチアジン誘導体 |
| WO2011071057A1 (ja) * | 2009-12-09 | 2011-06-16 | 塩野義製薬株式会社 | 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物 |
| MX2012006491A (es) | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
| 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 |
| JP5828848B2 (ja) | 2010-02-24 | 2015-12-09 | ヴァイティー ファーマシューティカルズ,インコーポレイテッド | ベータセクレターゼインヒビター |
| US8497264B2 (en) | 2010-03-15 | 2013-07-30 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| EP2547685A1 (en) | 2010-03-15 | 2013-01-23 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta - secretase modulators |
| MX339640B (es) | 2010-06-09 | 2016-06-01 | Janssen Pharmaceutica Nv * | Derivados de 5, 6-dihidro-2h-[1, 4] oxazin-3-il-amina utiles como inhibidores de la beta-secretasa (bace). |
| 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). |
| US8921363B2 (en) | 2010-08-05 | 2014-12-30 | Amgen Inc. | Derivatives of 1 H-isoindol-3-amine, 1 H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as beta-secretase inhibitors |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| 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 |
| US8957083B2 (en) | 2010-11-23 | 2015-02-17 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
| EP2655376B1 (en) | 2010-12-22 | 2017-08-23 | Janssen Pharmaceutica NV | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| ES2624288T3 (es) | 2011-01-21 | 2017-07-13 | Eisai R&D Management Co., Ltd. | Métodos y compuestos útiles en la síntesis de derivados de aminodihidrotiazina condensados |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| US9346827B2 (en) | 2011-02-07 | 2016-05-24 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use |
| EP2675810A1 (en) | 2011-02-15 | 2013-12-25 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use |
| CN103415519B (zh) | 2011-03-01 | 2016-03-02 | 詹森药业有限公司 | 作为β-分泌酶(BACE)抑制剂有用的6,7-二氢-吡唑[1,5-a]吡嗪-4-基胺衍生物 |
| AU2012224632B2 (en) | 2011-03-09 | 2016-06-16 | Janssen Pharmaceutica Nv | 3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives useful as inhibitors of beta-secretase (BACE) |
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| 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 |
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